Pharmacology Flashcards

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Copyright © 2010 by Saunders, an imprint of Elsevier Inc.


Common Drug Endings

Drug Endings Drug Classification Drug Example

-zosin Alpha-adrenergic blocker used for HTN and BPH Prazosin-olol, -lol Beta-adrenergic blocker (BB) Metoprolol-zepam, -zolam Benzodiazepine (BZD) Diazepam,

alprazolam-pril Angiotensin-converting enzyme (ACE) inhibitor Lisinopril-artan Angiotensin-receptor blocker (ARB) Candesartan-dipine Calcium channel blocker (CCB) Amlodipine-statin Lipid-lowering drug Atorvastatin-ase, -plase Thrombolytic used to dissolve clots Alteplase-parin Anticoagulant Enoxaparin-sone Corticosteroid Prednisone-dronate Bisphosphonate for osteoporosis Alendronate-terol Bronchodilator used for asthma and COPD Albuterol

Continued

Common Drug Endings-cont’d

Drug Endings Drug Classification Drug Example

-tidine Histamine2 blocker-acid reducer Cimetidine-prazole Protein pump inhibitor-acid reducer Omeprazole-cillin Penicillin antibiotic Amoxicillincef-, ceph- Cephalosporin antibiotic Cefazolin-cycline Tetracycline antibiotic Tetracycline-floxacin Fluoroquinolone antibiotic Levofloxacin-thromycin Macrolide antibiotic Azithromycin-micin, mycin Aminoglycoside antibiotic Gentamicin-azole Antifungal Itraconazole-triptan Serotonin-receptor agonists used for migraines Sumatriptan-denafil, -dalafil PED5 inhibitors for erectile dysfunction Sildenafil-curium, Neuromuscular blockers used for muscle Pancuronium

-curonium relaxation during surgery

HTN, Hypertension; BPH, benign prostatic hypertrophy; COPD, chronic obstructive pulmonarydisease; PED5, Phosphodiesterase type 5.

DRUGS THAT SHOULD BE AVOIDED DURINGPREGNANCY BECAUSE OF

PROVEN OR STRONGLY SUSPECTEDTERATOGENICITY

The risks for most drugs used in pregnancy have not been determined.

(The benefits of treatment must balance the risks.)Category A: Remote risk of fetal harmCategory B: Slightly more risk than ACategory C: Greater risk than BCategory D: Proven risk of fetal harmCategory X: Proven risk of fetal harm

DRUGS THAT SHOULD BE AVOIDED DURINGPREGNANCY BECAUSE OF

PROVEN OR STRONGLY SUSPECTEDTERATOGENICITY

Anticancer/Immunosuppressants drugs (methotrexate)Antiseizure drugs (carbamazepine, valproic acid, phenytoin, and others)

Androgens (danazol, finasteride, dutasteride)ACE inhibitors (lisinopril and others)

Angiotensin-receptor blockers (losartan and others)Antithyroid drugs (propylthiouracil, methimazole)

Fluoroquinolone antibiotics (ciprofloxacin, levofloxacin)HMG-CoA reductase inhibitors [ie, statins] (atorvastatin and others)

Isotretinoin (Accutane) used for acneLithium used for bipolar disorder

Nonsteroidal anti-inflammatory drugs (ibuprofen and others)Megadoses of vitamin A

Tetracycline antibiotics (minocycline, doxycycline)Warfarin (Coumadin)

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Functions of Peripheral Adrenergic Receptor Subtypes

ReceptorSubtype Location Response to Receptor Activation

Alpha1 Eye Mydriasis: “Wide eyed with fear”Arterioles and veins (skin, viscera, Constriction: (BP increases), blood ismucous membranes) shunted away from the skin and viscera into

skeletal muscle; “cold with fear”Sex organs, male EjaculationBladder neck and prostatic capsule Contraction

Alpha2 Presynaptic nerve terminals Inhibition of transmitter release (NE):Decreased sympathetic nervous system (SNS) outflow to the blood vessels and heart reduces BP and pain

Beta1 Heart Increase in rate and force of contraction andin AV conduction velocity

Kidney Release of renin to raise BPBeta2 Arterioles (heart, lung, and skeletal Dilation increases blood flow to organs

muscle)Bronchi Dilation improves oxygenationUterus Relaxation prevents laborLiver Glycogenolysis increases blood glucoseSkeletal muscle Enhanced contraction, glycogenolysis

Dopamine Kidney Dilation of kidney vasculature

NE, Norepinephrine; AV, atrioventricular.

Functions of Peripheral Cholinergic Receptor Subtypes

ReceptorSubtype Location Response to Receptor Activation

Nicotinicn All autonomic nervous system Stimulation of parasympathetic and ganglia and the adrenal medulla sympathetic postganglionic nerves and

release of epinephrine from the adrenal medulla

Nicotinicm Neuromuscular junction Contraction of skeletal muscleMuscarinic All parasympathetic target organs:

Eye Miosis (pupils constrict)Heart Decreased rateLung Constriction of bronchi

Promotion of secretionsBladder Voiding of the urinary bladderGastrointestinal (GI) tract Salivation

Increases gastric secretions, intestinal tone,and motilityDefecation

Sweat glands Generalized sweatingSex organs ErectionBlood vessels Vasodilation (BP decreases)

MUSCARINIC AGONISTSPrototype: Bethanechol (Urecholine)

Other Muscarinic AgonistsCevimeline (Evoxac) for xerostomia (dry mouth) and inflammation of the cornea and conjunctiva

Pilocarpine for topical therapy of glaucomaMuscarine is found in poisonous mushrooms

MUSCARINIC AGONISTSPrototype: Bethanechol (Urecholine)

Mechanism of ActionActivates muscarinic receptors

Causes contraction of the detrusor muscle of the bladder and relaxation of the trigone and sphincter; the result is bladder emptying

UsesPostoperative and postpartum urinary retention

Adverse EffectsHypotension due to vasodilation and bradycardia

GI effects (excessive salivation, increased gastric acid, cramps, and diarrhea)Bladder rupture in patients with urinary obstructionExacerbation of asthma due to bronchoconstriction

Dysrhythmias in hyperthyroid patients due to reflex tachycardia

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MUSCARINIC POISONINGMUSCARINIC POISONINGManifestation of Muscarinic Poisoning

Stimulation of muscarinic receptors causes profuse salivation,lacrimation (tearing), visual disturbances,

bronchospasm, diarrhea, bradycardia,hypotension, and cardiovascular collapse

Sources of Muscarinic PoisoningIngestion of Inocybe and Clitocybe mushrooms

Overdose with direct-acting muscarinic agonists (bethanechol, pilocarpine)Overdose with cholinesterase inhibitors (neostigmine [Prostigmin])

TreatmentAdministration of atropine (a muscarinic blocking agent)

Supportive care

MUSCARINIC ANTAGONISTS(ANTICHOLINERGIC DRUGS)

Prototype: Atropine

Other Muscarinic AntagonistsDrugs for an overactive bladder (eg, oxybutynin [Ditropan])

Scopolamine for motion sicknessIpratropium bromide (Atrovent) for COPD, rhinitis, and asthma

Antisecretory anticholinergics (glycopyrrolate [Robinul])Dicyclomine (Bentyl) for irritable bowel syndrome

Centrally acting anticholinergics for Parkinson’s disease:(trihexyphenidyl [Artane] and benztropine [Cogentin])

MUSCARINIC ANTAGONISTS(ANTICHOLINERGIC DRUGS)

Prototype: AtropineMechanism of ActionBlocks muscarinic receptors

Prevents receptor activation by endogenous acetylcholineIncreases heart rate (tachycardia)

Decreases salivary, bronchial, sweat, and acid-secreting cell secretionsRelaxes bronchial smooth muscles (bronchodilation)

Decreases bladder tone and GI motility (urinary retention)Dilates pupils (mydriasis)

Cycloplegia (relaxation of the ciliary muscle)Mild central nervous system (CNS) excitation, hallucinations, and delirium

UsesPreanesthesia to prevent bradycardia

Dilation of pupil for ocular examination or surgeryTreatment of bradycardia

Intestinal hypertonicity and hypermotility for dysenteryAntidote for muscarinic agonist poisoning

Adverse EffectsBlurry vision, photophobia, increased intraocular pressure

Urinary retention, dry mouth, constipationAnhidrosis and tachycardia (BUDCAT)

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ANTICHOLINERGIC SIDE EFFECTSBUDCAT

ANTICHOLINERGIC SIDE EFFECTSB- blurry vision, photophobia, and increased intraocular pressureU- urinary retentionD- dry mouth (xerostomia), decreased secretionsC- constipationA- anhidrosis (absence of sweat)T- tachycardia

Other Drugs with Anticholinergic Side EffectsFirst-generation antihistamines (diphenhydramine [Benadryl])

Antiemetics (prochlorperazine [Compazine], promethazine [Phenergan])First- and second-generation antipsychotic agents Tricyclic antidepressants (imipramine [Tofranil])

ANTICHOLINERGIC DRUGS FOR OVERACTIVEBLADDER (OAB)

Prototype: Oxybutynin (Ditropan, Ditropan XL, Oxytrol)

Other Anticholinergic Drugs for OABDarifenacin (Enablex)Solifenacin (Vesicare)

Tolterodine (Detrol, Detrol LA)Trospium (Sanctura, Sanctura XR)

ANTICHOLINERGIC DRUGS FOR OVERACTIVEBLADDER (OAB)

Prototype: Oxybutynin (Ditropan, Ditropan XL, Oxytrol)

Mechanism of ActionBlocks muscarinic (M3) receptors in the bladderInhibits bladder contractions and the urge to void

UsesOveractive bladder (urge incontinence)

Adverse EffectsBlurry vision, photophobia, increased intraocular pressure

Urinary retention, dry mouth, constipationAnhidrosis and tachycardia (BUDCAT)

CNS effects

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CHOLINESTERASE INHIBITORSPrototype: Neostigmine (Prostigmin)

Other Reversible Cholinesterase InhibitorsAmbenonium (Mytelase)

Pyridostigmine (Mestinon)Edrophonium (Tensilon)

Physostigmine (Antilirium) for anticholinergic poisoningEchothiophate for treatment of glaucoma

Cholinesterase Inhibitors Used to Treat Alzheimer’s Disease

Donepezil (Aricept)Galantamine (Razadyne)Rivastigmine (Exelon)

Tacrine (Cognex)

CHOLINESTERASE INHIBITORSPrototype: Neostigmine (Prostigmin)

Mechanism of ActionPrevents degradation of acetylcholine (ACh)ACh accumulates at neuromuscular junction

Enhances effect of ACh to stimulate skeletal muscle contractionMuscarinic receptor activation

UsesMyasthenia gravis

Reversal of neuromuscular blockade in postoperative patientsGlaucoma, Alzheimer’s disease, and poisoning by muscarinic antagonists

Adverse EffectsExcessive glandular secretions, increased GI motilityUrinary urgency, bradycardia, sweating, and miosis

Toxic doses reduce force of muscle contractionCholinergic crisis—treat with atropine

NEUROMUSCULAR BLOCKERSPrototype: Succinylcholine (Anectine, Quelicin)

(Depolarizing neuromuscular blocker)

Nondepolarizing Neuromuscular BlockersAtracurium (Tracrium)

Cisatracurium (Nimbex)Pancuronium

Rocuronium (Zemuron)Vecuronium (Norcuron)

NEUROMUSCULAR BLOCKERSPrototype: Succinylcholine (Anectine, Quelicin)

(Depolarizing neuromuscular blocker)

Mechanism of ActionCauses paralysis of muscle by preventing repolarization (fasciculations)

UsesMuscle relaxation during endotracheal intubation

Short operative proceduresFacilitation of mechanical ventilationAdjunct to electroconvulsive therapy

Diagnosis of myasthenia gravis

Adverse EffectsProlonged paralysis in genetically determined individuals

Hypotension Malignant hyperthermia—treat with dantrolene

Hyperkalemia with cardiac arrestMuscle pain

Antibiotics can intensify effect

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ADRENERGIC AGONISTSPrototype: Epinephrine

Other Adrenergic Agonists(Catecholamines and noncatecholamines)

Norepinephrine (Levophed)Isoproterenol (Isuprel)

DopamineDobutamine

PhenylephrineTerbutalineEphedrine

ADRENERGIC AGONISTSPrototype: Epinephrine

Mechanism of ActionActivates all four adrenergic receptors (alpha1, alpha2, beta1, and beta2)

Pupil dilation, arterial and venous vasoconstrictionIncreases heart rate and force of contraction

Bronchial dilation, glycogenolysis, enhanced muscle contraction

UsesCardiac arrest, heart failure, anaphylactic shock

AV heart block and asthmaDelays absorption of local anesthetic and controls superficial bleeding

Dilates pupil (mydriasis) for eye procedures

Adverse EffectsHypertensive crisis, dysrhythmias, angina pectoris

Necrosis after extravasationHyperglycemia in diabetic patients

ADRENERGIC AGONISTS Prototype: Phenylephrine

(Noncatecholamine)

Other Sympathomimetics Used for Nasal CongestionOxymetazoline (Afrin)

Pseudoephedrine (Sudafed)

ADRENERGIC AGONISTS Prototype: Phenylephrine

(Noncatecholamine)

Mechanism of ActionActivates alpha1 receptors

Constricts blood vessels of the skin, viscera, and mucous membranes

UsesTreatment of nasal congestionDelay of anesthetic absorption

Dilation of the pupil for ocular exam

Adverse EffectsHypertension

Necrosis

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ALPHA-ADRENERGIC ANTAGONISTS Prototype: Prazosin (Minipress)

Other Alpha BlockersTerazosin (Hytrin)

Doxazosin (Cardura)Tamsulosin (Flomax) for BPH onlyAlfuzosin (Uroxatral) for BPH only

Phentolamine for tissue necrosis

ALPHA-ADRENERGIC ANTAGONISTS Prototype: Prazosin (Minipress)

Mechanism of ActionBlocks alpha1 receptors

Dilates arteries and veinsRelaxes smooth muscle in the bladder neck and prostatic capsule

UsesEssential hypertension

Reversal of toxicity from alpha1 agonistsBenign prostatic hyperplasia

PheochromocytomaRaynaud’s disease

Adverse EffectsOrthostatic hypotension, reflex tachycardia

Nasal congestionInhibition of ejaculation

Use with sildenafil (Viagra) can lead to hypotensionSodium retention and increased blood volume

BETA-ADRENERGIC ANTAGONISTSFirst-Generation Nonselective Beta Blockers

Prototype: Propranolol (Inderal, InnoPran)

Other First-Generation Nonselective Beta BlockersNadolol (Corgard)

Sotalol (Betapace) for dysrhythmiasCarvedilol (Coreg) blocks beta1, beta2, and alpha1 receptors

Labetalol (Trandate) blocks beta1, beta2, and alpha1 receptors

BETA-ADRENERGIC ANTAGONISTSFirst-Generation Nonselective Beta Blockers

Prototype: Propranolol (Inderal, InnoPran)Mechanism of Action

Blocks beta1 and beta2 receptorsReduces heart rate, decreases force of ventricular contraction

Decreases conduction through AV node, decreases cardiac outputSuppresses secretion of renin

Bronchoconstriction through beta2 blockade in the lungReduces glycogenolysis through beta2 blockade in muscle and liver

UsesHypertension, angina pectoris, cardiac dysrhythmias

Myocardial infarction, hyperthyroidismMigraine headache prophylaxis, “stage fright”

Adverse EffectsBradycardia, AV heart block, heart failure

Rebound cardiac excitation (tachycardia) after abrupt withdrawal Bronchoconstriction in asthmatics

Inhibition of glycogenolysis, CNS effects mask tachycardia associated with hypoglycemia indicated in diabetics

Avoid in patients with asthma, diabetes, depression, or severe allergies

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BETA-ADRENERGIC ANTAGONISTSSecond-Generation Cardioselective Beta Blockers

Prototype: Metoprolol (Lopressor, Toprol XL)

Other Cardioselective Beta BlockersAcebutolol (Sectral)Atenolol (Tenormin)Betaxolol (Kerlone)Bisoprolol (Zebeta)

Esmolol (Brevibloc) for dysrhythmias

BETA-ADRENERGIC ANTAGONISTSSecond-Generation Cardioselective Beta Blockers

Prototype: Metoprolol (Lopressor, Toprol XL)Mechanism of Action

Blocks cardiac beta1 receptorsReduces heart rate, decreases force of ventricular contraction

Decreases conduction through AV node, decreases cardiac outputSuppresses renin

Minimal blockade of beta2 receptors (less bronchoconstriction)Not likely to inhibit glycogenolysis

Preferred for patients with asthma or diabetes

UsesHypertension, angina pectoris, heart failure

Myocardial infarction

Adverse EffectsBradycardia, reduction of cardiac output, AV heart block

Rebound cardiac excitation (tachycardia) after abrupt withdrawalMasks tachycardia associated with hypoglycemia in diabetics

BETA-ADRENERGIC ANTAGONISTSThird-Generation Vasodilating

Alpha and Beta Blockers

Prototype: Labetalol (Normodyne, Trandate)

Other Alpha and Beta BlockersCarvedilol (Coreg) for heart failure

(blocks beta1, beta2, and alpha1 receptors)Nebivolol (Bystolic) blocks beta receptors

(promotes release of nitric acid, a vasodilator)

BETA-ADRENERGIC ANTAGONISTSThird-Generation Vasodilating

Alpha and Beta Blockers

Prototype: Labetalol (Normodyne, Trandate)Mechanism of Action

Blocks alpha1 receptors on veins, causing vasodilationBlocks beta1 receptors in the heart and beta2 receptors in the lung

UsesHypertension, hypertensive crisis

Adverse EffectsDizziness, orthostatic hypotension, ventricular dysrhythmias

Nasal congestion, sexual dysfunction,bronchospasm

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CENTRALLY ACTING ALPHA2 AGONISTSPrototype: Clonidine (Catapres)

Other Alpha2 AgonistsGuanabenz (Wytensin)

Guanfacine (Tenex)Methyldopa*

*Adverse effects of methyldopa are hemolytic anemia and hepatotoxicity A positive Coombs’ test can occur with methyldopa

CENTRALLY ACTING ALPHA2 AGONISTSPrototype: Clonidine (Catapres)

Mechanism of ActionActivates alpha2 receptors in the CNS

Reduces sympathetic outflow to the heart and blood vessels Reduces stimulation of adrenergic receptors in the periphery

Net effect of cardiac suppression and vasodilation is decreased blood pressure

UsesHypertension

Epidural infusion to relieve severe cancer pain

Adverse EffectsDrowsiness and sedationXerostomia (dry mouth)

HypotensionBradycardia, decrease in cardiac output

Rebound hypertension in response to abrupt withdrawalFetal harm

DOPAMINERGICS FOR PARKINSON’S DISEASEPrototype: Levodopa/Carbidopa (Sinemet)

Other Drugs That Increase DopaminePramipexole (Mirapex)

Ropinirole (Requip)Entacapone (Comtan)Selegiline (Eldepryl)

Amantadine (Symmetrel)

DOPAMINERGICS FOR PARKINSON’S DISEASEPrototype: Levodopa/Carbidopa (Sinemet)

Mechanism of ActionLevodopa increases synthesis of dopamine in the striatum

Carbidopa enhances effect of levodopa

UsesReduces symptoms of Parkinson’s disease

Adverse EffectsEffects take several months to develop

Loss of effect occurs over timeNausea, vomiting, dyskinesias

Postural hypotension, psychosisDark sweat and urine, may activate melanoma

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CHOLINESTRASE INHIBITORS FOR ALZHEIMER’S DISEASE

Prototype: Donepezil (Aricept)

Other Cholinesterase InhibitorsTacrine (Cognex) rarely used due to hepatotoxicity

Rivastigmine (Exelon)Galantamine (Razadyne)

Other Drugs for Alzheimer’s DiseaseMemantine (Namenda)

N-methyl-D-aspartate (NMDA)–receptor antagonists for moderate to severe disease

CHOLINESTRASE INHIBITORS FOR ALZHEIMER’S DISEASE

Prototype: Donepezil (Aricept)Mechanism of Action

Prevents the breakdown of acetylcholine (ACh)Increases ACh at cholinergic synapses

May slow progression of Alzheimer’s diseaseMinimal improvement of memory and cognitive function

UsesAlzheimer’s disease

Adverse EffectsCholinergic effects

Nausea, vomiting, dyspepsia, diarrheaBradycardia

Bronchoconstriction

ANTIEPILEPTIC DRUGS (AEDs)Prototype: Phenytoin (Dilantin)

Other AEDsCarbamazepine (Tegretol)

Valproic acid (Depakene, Depakote, Depacon)Ethosuximide (Zarontin)

PhenobarbitalFosphenytoin (Cerebyx), a prodrug form of phenytoin

ANTIEPILEPTIC DRUGS (AEDs)Prototype: Phenytoin (Dilantin)

Mechanism of ActionInhibits entry of sodium into neurons

Suppresses action potential of neurons

UsesEpilepsy

Cardiac dysrhythmias

Adverse EffectsNystagmus, sedation, ataxia, diplopia, cognitive impairment

Gingival hyperplasia, rash, hirsutism, liver damageFetal harm, bleeding tendencies in newbornsNarrow therapeutic range (10 to 20 mcg/mL)Inject slowly (do not exceed 50 mg/minute)

Dysrhythmias and hypotension if injected too fastUse normal saline to prevent precipitation

Induces the metabolism of other drugs such as:oral contraceptives, warfarin, and glucocorticoids (drug effect is decreased)

Withdraw over 6 to 8 weeks to prevent seizures

All AEDs may increase suicidal thoughts and behaviors

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ANTIEPILEPTIC DRUGS (AEDs)Prototype: Valproic Acid (Depakote)

Newer Antiepileptic DrugsOxcarbazepine (Trileptal)Lamotrigine (Lamictal)Gabapentin (Neurontin)

Pregabalin (Lyrica)Levetiracetam (Keppra)Topiramate (Topamax)

Tiagabine (Gabitril)Zonisamide (Zonegran)

Felbamate (Felbatol)Vigabatrin (Sabril)

ANTIEPILEPTIC DRUGS (AEDs)Prototype: Valproic Acid (Depakote)

Mechanism of ActionBlocks sodium channels to suppress neurons

Suppresses calcium influxIncreases inhibitory influence of gamma-aminobutyric acid (GABA)

UsesEpilepsy, bipolar disorder, migraine headaches

Adverse EffectsNausea, vomiting, indigestion

Hepatotoxicity, pancreatitis, fetal harmWeight gain, rash, hair loss, tremor

Blood dyscrasias

MUSCLE RELAXANTSPrototype: Metaxalone (Skelaxin)

Other Centrally Acting Muscle RelaxantsBaclofen (Lioresal)Diazepam (Valium)

DantroleneCarisoprodol (Soma)

Cyclobenzaprine (Flexeril, Fexmid)Cyclobenzaprine ER (Amrix)

Chlorzoxazone (Paraflex, Parafon Forte, Remular-S)Methocarbamol (Robaxin)

Orphenadrine (Norflex)Tizanidine (Zanaflex)

MUSCLE RELAXANTSPrototype: Metaxalone (Skelaxin)

Mechanism of ActionUnclear; sedative properties may cause relaxation

UsesRelief of spasm resulting from muscle injury

Adverse EffectsCNS depressionHepatotoxicity

Physical dependence

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LOCAL ANESTHETICSPrototype: Lidocaine

Other Local AnestheticsProcaine (Novocain)

Bupivacaine (Marcaine)

LOCAL ANESTHETICSPrototype: Lidocaine

Mechanism of ActionStops axonal conduction by blocking sodium channels in axonal membrane

Stops nerve conduction

UsesSurgical anesthesia

Adverse EffectsCentral nervous system excitation followed by depression

Convulsions, respiratory depressionBradycardia, heart block, reduced contractile force

Cardiac arrest, hypotension, allergic reactions

GENERAL ANESTHETICSInhaled Anesthetics

Halothane (Fluothane)Isoflurane (Forane)Enflurane (Ethrane)

Desflurane (Suprane)Sevoflurane (Ultane)

Nitrous oxide

Intravenous AnestheticsThiopental sodium (Pentothal)Methohexital sodium (Brevital)

Diazepam (Valium)Midazolam (Versed)Propofol (Diprivan)

Etomidate (Amidate)Ketamine (Ketalar)

Droperidol plus fentanyl (Innovar)

GENERAL ANESTHESTICS

Mechanism of ActionEnhance transmission at inhibitory synapses (GABA)Depress transmission at excitatory synapses (NMDA)

UsesSurgery

Adverse EffectsRespiratory and cardiac depression

Sensitization of the heart to catecholamines, leading to dysrhythmiasMalignant hyperthermia—treat with dantrolene

Aspiration of gastric contentsToxicity to operating room personnel

Hepatotoxicity

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OPIOID ANALGESICSPrototype: Morphine

Other Strong Opioid AgonistsFentanyl (Sublimaze, Duragesic, Fentora, Actiq, Ionsys)

Alfentanil (Alfenta) sufentanil (Sufenta)Remifentanil (Ultiva)Meperidine (Demerol)

Methadone (Diskets, Dolophine, Methadose)Heroin

Hydromorphone (Dilaudid)Oxymorphone (Opana)

Levorphanol (Levo-Dromoran)

Moderate to Strong Opioid AgonistsCodeine

Oxycodone (OxyContin, Percodan, Percocet)Hydrocodone (Vicodin, Lortab)

Propoxyphene (Darvon)

OPIOID ANALGESICSPrototype: Morphine

Mechanism of ActionActivates mu receptors

Produces analgesia, euphoria, sedation

UsesRelief of pain

Adverse EffectsRespiratory depression, constipation

Orthostatic hypotension, urinary retention, cough suppressionBiliary colic, emesis, elevation of intracranial pressureEuphoria, dysphoria, sedation, miosis, neurotoxicity

Tolerance and physical dependenceProlonged use affects hormone and immune functions

Reversed with naloxone (Narcan)

AGONIST-ANTAGONIST OPIOIDSPrototype: Pentazocine (Talwin)

Other Partial AgonistsNalbuphine (Nubain)Butorphanol (Stadol)

Buprenorphine (Buprenex, Subutex, Suboxone)

AGONIST-ANTAGONIST OPIOIDSPrototype: Pentazocine (Talwin)

Mechanism of ActionActs as an agonist at kappa receptors and antagonist at mu receptors

Produces analgesia and sedationMild respiratory depression, increased cardiac work

UsesRelief of mild to moderate pain

Adverse EffectsPhysical dependence

Unpleasant reactions (anxiety, strange thoughts, nightmares, hallucinations)If administered to a patient physically dependent on a pure opioid agonist,

withdrawal syndrome can occur

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OPIOID ANTAGONISTSPrototype: Naloxone (Narcan)

Other Opioid AntagonistsMethylnaltrexone (Relistor)

Nalmefene (Revex)Naltrexone (ReVia, Vivitrol)

OPIOID ANTAGONISTSPrototype: Naloxone (Narcan)

Mechanism of ActionReverses the effects of opioids

UsesReversal of opioid overdose

Reversal of postoperative opioid effectReversal of neonatal respiratory depression

Adverse EffectsMinimal

NONOPIOID CENTRALLY ACTING ANALGESICSPrototype: Tramadol (Ultram, Ultram ER)

Other Nonopioid AnalgesicsClonidine (Duraclon)

Ziconotide (Prialt) Dexmedetomidine (Precedex)

NONOPIOID CENTRALLY ACTING ANALGESICSPrototype: Tramadol (Ultram, Ultram ER)

Mechanism of ActionAnalog of codeine, weakly activates mu opioid receptors

Blocks uptake of norepinephrine and serotonin Activates monoaminergic spinal inhibition of pain

UsesRelieves moderate to severe pain

Adverse EffectsMild sedation, dizziness, headache, dry mouth, constipation

Increases the risk of seizureMinimal respiratory depression

CNS depression if used with ETOHHTN if used with monoamine oxidase (MAO) inhibitors

Serotonin syndrome if used with antidepressants or triptansLow potential for abuse; not a scheduled drug

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ERGOT ALKALOIDSPrototype: Ergotamine (Ergomar)

Other Ergot AlkaloidsDihydroergotamine (D.H.E. 45, Migranal)Ergotamine 1 caffeine (Cafergot, Ercaf)

ERGOT ALKALOIDSPrototype: Ergotamine (Ergomar)

Mechanism of ActionAlters transmission at serotonergic, dopaminergic,

and alpha-adrenergic junctionsActivates serotonin receptors

Suppresses inflammation by blocking calcitonin gene–related peptide(CGRP)

Promotes constriction

Uses Migraine and cluster headaches

Adverse EffectsNausea and vomiting

Weakness in the legs, myalgias, tingling in the fingers and toesAngina-like pain

Tachycardia or bradycardiaOverdose can cause ergotism (ischemia due to constriction of vessels)

Fetal harm

SEROTONIN1B/1D–RECEPTOR AGONISTS (TRIPTANS)Prototype: Sumatriptan (Imitrex)

Other TriptansNaratriptan (Amerge)Rizatriptan (Maxalt)Zolmitriptan (Zomig)Almotriptan (Axert)Frovatriptan (Frova)Eletriptan (Replax)

Sumatriptan 1 naproxen (Treximet)

SEROTONIN1B/1D–RECEPTOR AGONISTS (TRIPTANS)Prototype: Sumatriptan (Imitrex)

Mechanism of ActionBinds to 5-HT1B/1D (serotonin) receptors to cause vasoconstriction

Reduces release of inflammatory peptides (CGRT)Diminishes perivascular inflammation

Relieves migraine pain and associated symptoms

UsesMigraine headache

Adverse EffectsChest symptoms (heavy arms and chest pressure)

Coronary vasospasmTeratogenesis

Vertigo, malaise, fatigue, tingling sensation

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FIRST-GENERATION (CONVENTIONAL)ANTIPSYCHOTICS

Prototype: Chlorpromazine (Thorazine)

Other First-Generation Conventional NeurolepticsLow Potency

Chlorpromazine (Thorazine)Thioridazine (Mellaril)

Medium PotencyLoxapine (Loxitane)Molindone (Modan)

Pherphenazine

High PotencyHaloperidol (Haldol), Haldol Decanoate (depot preparation)

Fluphenazine (Prolixin Decanoate [depot preparation])Trifluoperazine, Thiothixene (Navane)

Pimozide (Orap)

FIRST-GENERATION (CONVENTIONAL)ANTIPSYCHOTICS

Prototype: Chlorpromazine (Thorazine)Mechanism of Action

Relieves positive symptoms of schizophreniaBlocks receptors for dopamine (D2), acetylcholine (ACh),

histamine, and norepinephrine (NE)

UsesSchizophrenia, bipolar disorder, Tourette’s syndrome

Prevention of emesis, and dementia

Adverse EffectsExtrapyramidal symptoms (EPS)

(acute dystonia, parkinsonism, akathisia, tardive dyskinesia)Neuroleptic malignant syndrome

(lead pipe rigidity, high fever, autonomic instability)Anticholinergic effects (BUDCAT), orthostatic hypotension

Sedation, neuroendocrine effects, seizuresSexual dysfunction, increased risk of sunburn

Agranulocytosis, dysrhythmias (prolongs QT interval)Counteracts the effect of levodopa used in Parkinson’s disease

Rate of mortality doubles when used in elderly patients with dementiaIncreases prolactin levels

SECOND-GENERATION (ATYPICAL) ANTIPSYCHOTICSPrototype: Clozapine (Clozaril)

Other Second-Generation (Atypical) AntipsychoticsRisperidone (Risperdal)

Risperdal Consta (depot preparation)Paliperidone (Invega)Olanzapine (Zyprexa)Quetiapine (Seroquel)Ziprasidone (Geodon)Aripiprazole (Abilify)

SECOND-GENERATION (ATYPICAL) ANTIPSYCHOTICSPrototype: Clozapine (Clozaril)

Mechanism of ActionRelieves positive, negative, and cognitive signs and symptoms of

schizophreniaBlocks receptors for serotonin (5-HT), D2, ACh, histamine, and NE

UsesSchizophrenia

Levodopa-induced psychosisBipolar disorder

Adverse EffectsAgranulocytosis

Metabolic effects (weight gain, diabetes, dyslipidemia)Seizures, myocarditis, orthostatic hypotension

Rate of mortality doubles when used in elderly patients with dementiaSedation, weight gain, anticholinergic effects (BUDCAT)

Lower risk of extrapyramidal effectsCosts 10 times more than conventional agents

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TRICYCLIC ANTIDEPRESSANTS (TCAs)Prototype: Imipramine (Tofranil)

Other TCAsAmitriptyline

Clomipramine (Anafranil)Desipramine (Norpramin)

Doxepin (Sinequan)Maprotiline

Nortriptyline (Aventyl, Pamelor)Protriptyline (Vivactil)

Trimipramine (Surmontil)

TRICYCLIC ANTIDEPRESSANTS (TCAs)Prototype: Imipramine (Tofranil)

Mechanism of ActionInhibits reuptake of norepinephrine (NE) and serotonin

(more serotonin and NE are available at the synapse)

UsesDepression, bipolar disorder, neuropathic pain

Chronic insomniaAttention deficit/hyperactivity disorder

Panic disorder, obsessive-compulsive disorder (OCD)

Adverse EffectsOrthostatic hypotension, anticholinergic effects (BUDCAT)

Diaphoresis (sweating), sedationCardiotoxicity, seizures, hypomania

Increased risk of suicide, especially in younger individualsMany drug interactions

Selective serotonin reuptake inhibitors (SSRIs) preferred for treatment ofdepression

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)Prototype: Fluoxetine (Prozac, Sarafem)

Other SSRIsParoxetine (Paxil, Paxil CR, Pexeva)

Fluvoxamine (Luvox)Sertraline (Zoloft)

Citalopram (Celexa)Escitalopram (Lexapro)

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)Prototype: Fluoxetine (Prozac, Sarafem)

Mechanism of ActionInhibits serotonin reuptake (more serotonin is available at the synapse)

UsesMajor depression, bipolar disorder

Obsessive-compulsive disorderPanic disorder, bulimia nervosaPremenstrual dysphoric disorder

Adverse EffectsSexual dysfunction, nausea, headache, insomnia

Weight gain, serotonin syndromeWithdrawal syndrome

Neonatal abstinence syndrome and persistent pulmonary hypertensionTeratogenesis

Increased risk of suicideExtrapyramidal side effects

Bruxism (clenching and grinding of the teeth)Decrease in platelet aggregation, leading to bleeding

Hyponatremia

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SEROTONIN/NOREPINEPHRINE REUPTAKEINHIBITORS (SNRIs)

Prototype: Venlafaxine (Effexor)

Other SNRIsDuloxetine (Cymbalta)

(indicated for physical pain and diabetic neuropathy; can cause liver toxicity)Desvenlafaxine (Pristiq)

SEROTONIN/NOREPINEPHRINE REUPTAKEINHIBITORS (SNRIs)

Prototype: Venlafaxine (Effexor)Mechanism of Action

Blocks norepinephrine (NE) and 5-HT uptake; weak blockade of dopamine uptake

(more transmitter available at synapse)

UsesMajor depression, generalized anxiety disorder

Social anxiety disorder (social phobia)

Adverse EffectsNausea, headache, anorexia, nervousness, sweating, somnolence, and insomnia

Weight loss, diastolic hypertensionSexual dysfunction, hyponatremia

Increased risk of suicideIntense withdrawal syndrome with abrupt discontinuation

(anxiety, agitation, tremors, headache, vertigo, nausea, tachycardia, tinnitus)Neonatal withdrawal syndrome

Serotonin syndromeFetal harm

MONOAMINE OXIDASE INHIBITORS (MAOIs)Prototype: Isocarboxazid (Marplan)

Other MAOIsPhenelzine (Nardil)

Tranylcypromine (Parnate)Transdermal selegiline (Emsam)

MONOAMINE OXIDASE INHIBITORS (MAOIs)Prototype: Isocarboxazid (Marplan)

Mechanism of ActionIncreases NE and serotonin by blocking the enzyme that inactivates them

UsesAtypical depression, bulimia nervosa, OCD, and panic attacks

Adverse EffectsCNS stimulation (anxiety, insomnia, agitation, hypomania, and mania)

Orthostatic hypotension due to vasodilationHypertensive crisis from high levels of dietary tyramine

Many drug interactionsSSRIs preferred for treatment of depression

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ATYPICAL ANTIDEPRESSANTSPrototype: Bupropion (Wellbutrin, Zyban)

Other Atypical AntidepressantsNefazodone (can cause liver failure)

Mirtazapine (Remeron)AmoxapineReboxetine

Trazodone (Desyrel) has sedative effects

ATYPICAL ANTIDEPRESSANTSPrototype: Bupropion (Wellbutrin, Zyban)

Mechanism of ActionUnclear; may be related to blockade of dopamine uptake

UsesMajor depressive disorder

Prevention of seasonal affective disorder (SAD)Smoking cessation

Relief of neuropathic pain (unlabeled use)Attention deficit/hyperactivity disorder (unlabeled use)

Adverse EffectsRisk of seizure

May increase the risk of suicideAgitation, headache, dry mouth, constipation, weight loss,

GI upset, dizziness, tremor, insomnia, blurred vision, and tachycardia

MOOD-STABILIZING DRUGSPrototype: Lithium (Lithobid, Lithonate, Lithotabs)

Other Mood-Stabilizing DrugsAntiepileptic Drugs

Valproic acidCarbamazepine

Lamotrigine (Lamictal)

Atypical AntipsychoticsOlanzapine (Zyprexa)Aripiprazole (Abilify)Ziprasidone (Geodon)

MOOD-STABILIZING DRUGSPrototype: Lithium (Lithobid, Lithonate, Lithotabs)

Mechanism of ActionMechanism unclear; may alter ions and neurotransmitters

May protect against neuronal atrophy and/or promote neuronal growth

UsesStabilizes mood in patients with bipolar disorder

Reduces euphoria, hyperactivity, and other symptomsPreferred for patients with classic (euphoric) mania

Adverse EffectsAccumulates to toxic levels in the presence of a low sodium level

Lithium levels must be kept below 1.5 mEq/LBlood levels are drawn 12 hours after evening dose

Signs of toxicity include fine hand tremor, GI upset, thirst, polyuria, andmuscle weakness

Chronic use can lead to renal toxicity and hypothyroidismFDA Pregnancy Risk Category D

Reversible leukocytosis, dermatologic reactionsDrug interactions occur with diuretics, NSAIDs, and anticholinergics

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MOOD-STABILIZING ANTIEPILEPTIC DRUGSPrototype: Valproic Acid (Depakote)

Other AEDs used for BPDCarbamazepine (Equetro, Tegretol)—monitor CBC

Lamotrigine (Lamictal)

MOOD-STABILIZING ANTIEPILEPTIC DRUGSPrototype: Valproic Acid (Depakote)

Mechanism of ActionSuppresses mania and stabilizes mood

UsesMood stabilizer for patients with bipolar disorder

Adverse EffectsGI disturbances, weight gain

Thrombocytopenia, pancreatitis, liver failureTarget trough level is 50 to 120 mg/mL

Fetal harm

BENZODIAZEPINES (BZDs)Prototype: Alprazolam (Xanax)

Chlordiazepoxide (Librium)Clonazepam (Klonopin)Clorazepate (Tranxene)

Diazepam (Valium)Estazolam (ProSom)

Flurazepam (Dalmane)Lorazepam (Ativan)Midazolam (Versed)Oxazepam (Serax)Quazepam (Doral)

Temazepam (Restoril)Triazolam (Halcion)

BENZODIAZEPINES (BZDs)Prototype: Alprazolam (Xanax)

Mechanism of ActionDepresses central nervous system function

Reduces anxiety, promotes sleepPotentiates the actions of GABA (an inhibitory neurotransmitter)

UsesAnxiety, insomnia, seizure disorder, induction of anesthesiaMuscle spasm, panic disorder, and withdrawal from alcohol

Adverse EffectsCNS depression, anterograde amnesia

Sleep driving and other complex sleep-related behaviorsParadoxic effects

Weak respiratory depression if given orallyIV administration can cause severe respiratory depression

Abuse and addiction, teratogenicDo not mix with other CNS depressants or alcohol

Reversal agent is flumazenil (Romazicon)

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BENZODIAZEPINE-LIKE DRUGSPrototype: Zolpidem (Ambien)

Other BZD-like drugsZaleplon (Sonata)

Eszopiclone (Lunesta)

Melatonin AgonistRamelteon (Rozerem)

BENZODIAZEPINE-LIKE DRUGSPrototype: Zolpidem (Ambien)

Mechanism of ActionPotentiate the actions of GABA (an inhibitory neurotransmitter)

UsesShort-term management of insomnia

Adverse EffectsDaytime drowsiness, dizziness

Sleep driving and other complex sleep-related behaviorsDo not use with alcohol or other CNS depressants

BARBITURATESCNS Depressants

ThiopentalSecobarbital

Phenobarbital

Miscellaneous Sedative-HypnoticsChloral hydrate (Aquachloral Supprettes, Somnote)

Meprobamate (Miltown)Paraldehyde (Paral)

Trazodone (Desyrel) antidepressantDiphenhydramine (Sominex)

Doxylamine (Unisom)

BARBITURATESCNS Depressants

Mechanism of ActionPotentiate the actions of GABA (an inhibitory neurotransmitter)

UsesInsomnia

Suppression of seizures, induction of general anesthesiaTreatment of manic states

Adverse EffectsRespiratory depression, decreased blood pressure and heart rate

Induction of hepatic drug-metabolizing enzymes (increases the metabolismof other drugs rendering them less effective)

May lead to tolerance and dependenceFrequently used as vehicles for suicide

Teratogenic

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CNS STIMULANTS Prototype: Methylphenidate

(Ritalin, Metadate, Concerta, Daytrana)

Other CNS StimulantsDexmethylphenidate (Focalin)

DexedrineAdderall

Modafinil (Provigil)Atomoxetine (Strattera)—nonstimulant

CNS STIMULANTSPrototype: Methylphenidate

(Ritalin, Metadate, Concerta, Daytrana)Mechanism of Action

Promotes norepinephrine (NE) and dopamine (DA) releaseInhibits NE and DA reuptake

UsesAttention deficit/hyperactivity disorder (ADHD)

Narcolepsy

Adverse EffectsInsomnia, reduced appetite, weight loss

Palpitations, hypertension, angina, dysrhythmias, psychosisAbrupt discontinuation can lead to withdrawal reactions

Potential for abuse (Schedule II)Sudden death

DISULFIRAM (ANTABUSE)Aversion Therapy for Alcoholism

DISULFIRAM (ANTABUSE)Aversion Therapy for Alcoholism

Mechanism of ActionDisrupts alcohol metabolism by blocking enzyme

Acetaldehyde accumulates and produces unpleasant effects

UsesAlcohol abuse

Adverse EffectsNausea, vomiting, flushing, palpitations, headacheSweating, blurry vision, hypotension, chest pain Shock occurs with ingestion of 7 mL of alcohol

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HIGH-CEILING (LOOP) DIURETICSPrototype: Furosemide (Lasix)

Other High-Ceiling DiureticsEthacrynic acid (Edecrin)

Bumetanide (Bumex)Torsemide (Demadex)

HIGH-CEILING (LOOP) DIURETICSPrototype: Furosemide (Lasix)

Mechanism of ActionBlocks reabsorption of sodium and chloride in the descending limb of

Henle’s loop to promote urinationProduces profound diuresis

UsesRapid mobilization of fluid

Pulmonary edema resulting from heart failure or renal or liver diseaseEspecially useful in patients with renal insufficiency

Adverse EffectsHyponatremia, hypochloremia, dehydration, hypotension, hypokalemia

Ototoxicity, hyperglycemia, hyperuricemia, fetal harmRaises LDL and lowers HDL (minimally)

May cause dysrhythmias when used with digoxin (reduces potassium)

THIAZIDE DIURETICSPrototype: Hydrochlorothiazide (HCTZ)

Other Thiazides and Related DiureticsChlorothiazide (Diuril)

Methyclothiazide (Enduron)Chlorthalidone (Hygroton, Thalitone)

Metolazone (Zaroxolyn)

THIAZIDE DIURETICSPrototype: Hydrochlorothiazide (HCTZ)

Mechanism of ActionBlocks reabsorption of sodium and chloride in the early segment of the distal

convoluting tubule to promote urination

UsesTreatment of hypertension

Mobilization of edema with mild heart failure, hepatic or renal diseaseIneffective when GFR is low (,15 to 20 mL/min)

Adverse EffectsHyponatremia, hypochloremia, dehydration

Hypokalemia, magnesium deficiency, and hypotensionHyperglycemia, hyperuricemia, increase in LDL and triglycerides

May cause dysrhythmias when used with digoxin (reduces potassium)Fetal harm

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POTASSIUM-SPARING DIURETICSPrototype: Spironolactone (Aldactone)

Other Potassium-Sparing DiureticsTriamterene (Dyrenium)

Amiloride (Midamor)

Other Aldosterone Blockers Eplerenone (Inspra)

Not considered a diureticUsed for heart failure

POTASSIUM-SPARING DIURETICSPrototype: Spironolactone (Aldactone)

Mechanism of ActionBlocks the actions of aldosterone in the distal nephron

Produces minimal diuresisCauses retention of potassium and increased excretion of sodium

UsesHypertension and edema

Used in combination with other diuretics to counterbalance potassium lossHeart failure

(Blocks the negative effects of aldosterone on the heart and blood vessels)Primary hyperaldosteronism, premenstrual syndrome

Polycystic ovary syndrome, and acne

Adverse EffectsHyperkalemia, dysrhythmias

Endocrine effects (Gynecomastia, menstrual irregularities, impotence, and hirsutism)

OSMOTIC DIURETICSPrototype: Mannitol (Osmitrol)

OSMOTIC DIURETICSPrototype: Mannitol (Osmitrol)

Mechanism of ActionCreates an osmotic force in the lumen of the nephron

Promotes diuresis by inhibiting passive reabsorption of water

UsesProphylaxis of renal failure

Reduction of intracranial pressureReduction of intraocular pressure

Adverse EffectsEdema

CHF and pulmonary edema

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ANGIOTENSIN-CONVERTING ENZYME (ACE)INHIBITORS

Prototype: Ramipril (Altace)

Other ACE InhibitorsBenazepril (Lotensin)Captopril (Capoten)Enalapril (Vasotec)

Fosinopril (Monopril)Lisinopril (Prinivil and Zestril)

Moexipril (Univasc)Perindopril (Aceon)Quinapril (Accupril)Trandolapril (Mavik)

ANGIOTENSIN-CONVERTING ENZYME (ACE)INHIBITORS

Prototype: Ramipril (Altace)Mechanism of Action

Inhibits ACE, reducing levels of angiotensin IIDilates arterioles and veins to reduce blood volume and BP

Prevents pathologic changes in cardiac structure

UsesHypertension, heart failure, MI

Diabetic and nondiabetic nephropathyPrevention of MI, stroke, and death

Adverse EffectsHypotension, cough, hyperkalemia

Renal failure in patients with renal artery stenosisFetal injuryAngioedema

Neutropenia, dysgeusia, and rash with captopril

ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs)Prototype: Losartan (Diovan)

Other ARBsCandesartan (Atacand)Eprosartan (Teveten)Irbesartan (Avalide)Losartan (Hyzaar)

Olmesartan (Benicar)Telmisartan (Micardis)

ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs)Prototype: Losartan (Diovan)

Mechanism of ActionBlocks the action of angiotensin II

Dilates arterioles and veins to reduce blood volume and BPPrevents pathologic changes in cardiac structure

Does not cause cough or significant hyperkalemia

UsesHypertension, heart failure, MI, and diabetic nephropathy

Prevention of MI, stroke, and death

Adverse EffectsRenal failure in patients with renal artery stenosis

HypotensionAngioedemaFetal harm

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DIRECT RENIN INHIBITORS (DRIs)Prototype: Aliskiren (Tekturna)

DIRECT RENIN INHIBITORS (DRIs)Prototype: Aliskiren (Tekturna)

Mechanism of ActionBinds with renin and inhibits the formation of angiotensin I

UsesHypertension

Adverse EffectsAngioedema and cough

GI effects (diarrhea)Hyperkalemia

Fetal injury and death

ALDOSTERONE ANTAGONISTSPrototype: Eplerenone (Inspra)

Other Aldosterone AntagonistsSpironolactone

ALDOSTERONE ANTAGONISTSPrototype: Eplerenone (Inspra)

Mechanism of ActionBlocks aldosterone, increases excretion of sodium and water

Retention of potassiumReduces blood volume and blood pressure

Prevents cardiovascular remodeling

UsesHypertension, heart failure

Adverse EffectsHyperkalemia

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CALCIUM CHANNEL BLOCKERSNondihydropyridines

Prototypes: Verapamil (Calan) and Diltiazem(Cardizem)

CALCIUM CHANNEL BLOCKERSNondihydropyridines

Prototypes: Verapamil (Calan) and Diltiazem(Cardizem)

Mechanism of ActionBlock calcium channels in the heart and blood vesselsDilate peripheral arterioles to reduce blood pressure

Increase coronary perfusionBlock SA and AV nodes to reduce heart rate and contractility

Reduce force of myocardial contraction

UsesAngina, essential hypertension, cardiac dysrhythmias

Adverse EffectsConstipation, dizziness, facial flushing, peripheral edema, hypotension

Bradycardia, AV block, decreased cardiac contractilityChronic eczematous rash and gingival hyperplasia

Verapamil increases digoxin level by 60%

CALCIUM CHANNEL BLOCKERSDihydropyridine

Prototype: Amlodipine (Norvasc)

Other Dihydropyridine Calcium Channel BlockersNifedipine (Adalat, Procardia)

Nicardipine (Cardene)Isradipine (DynaCirc)Felodipine (Plendil)

Nimodipine (Nimotop)Nisoldipine (Sular)

CALCIUM CHANNEL BLOCKERSDihydropyridine

Prototype: Amlodipine (Norvasc)Mechanism of Action

Blocks calcium channels in the blood vesselsLittle effect on heart rate or contractility

Vasodilation in peripheral arterioles lowers blood pressureCalcium channel blockade in coronary arteries increases perfusion

UsesHypertension

Angina

Adverse EffectsHypotension, edema, flushing, dizziness, headache

Peripheral edema, gingival hyperplasia, chronic eczematous rashDoes not slow heart rate, as do verapamil and diltiazem

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VASODILATORSPrototype: Hydralazine (Apresoline)

Other VasodilatorsBiDil (hydralazine and isosorbide dinitrate)

MinoxidilDiazoxide (Hyperstat IV)

Sodium nitroprusside (Nitropress)Angiotensin-converting enzymes (ACE) inhibitors

Angiotensin II receptor blockers (ARBs)Direct renin inhibitors (DRIs)

Calcium channel blockers (CCBs)Alpha-adrenergic blocking agents

Ganglionic blocking agentsAdrenergic neuron blocking agents

Centrally acting alpha2 agonistsNesiritide (Natrecor)

Drugs used for pulmonary artery hypertension

VASODILATORSPrototype: Hydralazine (Apresoline)

Mechanism of ActionSelective dilation of arterioles (mechanism unknown)

Decrease in peripheral resistance and arterial blood pressureIncrease in heart rate and myocardial contractility by reflex

UsesEssential hypertension, hypertensive crisis, heart failure

Adverse EffectsReflex tachycardia

Increased blood volumeSystemic lupus erythematosus–like syndromeHeadache, dizziness, weakness, and fatigue

CARDIAC (DIGITALIS) GLYCOSIDESPrototype: Digoxin (Lanoxin)

Positive Inotropic Agent for Heart Failure

Other Drugs Used to Treat Heart FailureDiuretics

ACE inhibitorsAngiotensin receptor blockers

Beta blockersAldosterone blockers

CARDIAC (DIGITALIS) GLYCOSIDESPrototype: Digoxin (Lanoxin)

Positive Inotropic Agent for Heart FailureMechanism of Action

Increases the force of ventricular contraction to increase cardiac outputInhibits Na1, K1-ATPase to increase Ca11 inside myocytes

Competes with K1 for binding to Na1, K1-ATPase↓ K → ↑ Na1, K1-ATPase inhibition → digoxin toxicityChanges electrical activity of heart and slows heart rate

Increased cardiac output → decreased sympathetic tone, increased urine production,and decreased release of renin

UsesHeart failure and dysrhythmias

Adverse EffectsAnorexia, nausea and vomiting, fatigue

Visual disturbances (blurry vision, yellow tinge, halos)Dysrhythmias

Digoxin toxicity (therapeutic level, 0.5 to 0.8 ng/mL)Hold if HR , 60 bpm or K1 is low

Inject slowly over 5 minutesGive Digibind for digoxin overdose

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CLASS I: SODIUM CHANNEL BLOCKERSPrototype: Procainamide (Procanbid)

Class IA Sodium Channel Blocker

Other Class IA Sodium Channel BlockersQuinidine

Disopyramide (Norpace)

CLASS I: SODIUM CHANNEL BLOCKERSPrototype: Procainamide (Procanbid)

Class IA Sodium Channel BlockerMechanism of Action

Blocks cardiac sodium channelsSlows conduction in the atria, ventricles, and His-Purkinje system

Delays depolarization

UsesAtrial and ventricular dysrhythmias

Adverse EffectsSystemic lupus erythematosus–like syndrome

Blood dyscrasiasQRS widening and prolongation

CLASS I: SODIUM CHANNEL BLOCKERSClass IB Sodium Channel Blocker

Prototype: Lidocaine (Xylocaine)

Other Sodium Channel–Blocking AntidysrhythmicsClass IB

Mexiletine (Mexitil)Phenytoin (Dilantin)

Class ICFlecainide (Tambocor)Propafenone (Rythmol)

Other Class IMoricizine (Ethmozine)

CLASS I: SODIUM CHANNEL BLOCKERSClass IB Sodium Channel Blocker

Prototype: Lidocaine (Xylocaine) Mechanism of Action

Blocks cardiac sodium channelsSlows conduction in the atria, ventricles, and His-Purkinje system

Reduces automaticity in the ventricles and His-Purkinje systemAccelerates repolarization

UsesShort-term therapy for ventricular dysrhythmias

Adverse EffectsNo significant impact on the ECG

Drowsiness, confusion, and paresthesiasToxic doses may produce convulsions and respiratory arrest

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CLASS II: BETA BLOCKERSPrototype: Propranolol (Inderal)

Other Class II AgentsAcebutolol (Sectral)Esmolol (Brevibloc)

CLASS II: BETA BLOCKERSPrototype: Propranolol (Inderal)

Mechanism of ActionNonselective beta-adrenergic antagonist

Attenuates sympathetic stimulation of the heartBlocks both beta1 and beta2 receptorsReduces automaticity of the SA node

Reduces velocity of conduction through the AV node (prolongs PR interval)Reduces myocardial contractility

UsesSinus tachycardia, severe recurrent ventricular tachycardia

Exercise-induced tachydysrhythmiasParoxysmal atrial tachycardia provoked by emotion or exercise

Angina of effort

Adverse EffectsProlongs PR interval on the ECG

Bradycardia, heart failure, AV block, and sinus arrestHypotension, bronchospasm in patients with asthma

CLASS III: POTASSIUM CHANNEL BLOCKERSPrototype: Amiodarone (Cordarone, Pacerone)

Other Class III Agents Bretylium

Sotalol (Betapace) class II and class IIIDofetilide (Tikosyn)Ibutilide (Corvert)

CLASS III: POTASSIUM CHANNEL BLOCKERSPrototype: Amiodarone (Cordarone, Pacerone)

Mechanism of ActionDelays repolarization

Reduces automaticity in the SA node, reduces contractilityReduces conduction velocity in the AV node, ventricles, and His-Purkinje system

Dilates coronary and peripheral blood vessels

UsesRecurrent ventricular fibrillationUnstable ventricular tachycardia

Adverse EffectsPulmonary toxicities (pneumonitis and fibrosis)

Widening of the QRS complex, prolongation of the PR and QT intervalsSinus bradycardia, AV block, precipitation of heart failure, hypotension

Toxicities in pregnancyCorneal microdeposits, optic neuropathy

Blue-gray discoloration of the skinGI reactions (anorexia, nausea, vomiting)

CNS reactions (ataxia, dizziness, tremor, mood alterations, hallucinations)Hepatitis, thyroid dysfunction

Grapefruit juice increases levels to toxicity

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CLASS IV: CALCIUM CHANNEL BLOCKERSPrototypes: Verapamil (Calan, Isoptin, Verelan)

Diltiazem (Cardizem, others)

Other Antidysrhythmic DrugsAdenosine (Adenocard)

Digoxin (Lanoxin)

CLASS IV: CALCIUM CHANNEL BLOCKERSPrototypes: Verapamil (Calan, Isoptin, Verelan)

Diltiazem (Cardizem, others)Mechanism of Action

Block calcium channels in the heartSlow SA node automaticity, delay AV node conduction

Reduce myocardial contractility

UsesAtrial fibrillation or atrial flutter

Supraventricular tachycardia

Adverse EffectsBradycardia, AV block, and heart failure

Hypotension, peripheral edema, and constipationCan elevate digoxin levels

Grapefruit juice increases levels to toxicity

HMG-CoA REDUCTASE INHIBITORS (STATINS)Prototype: Atorvastatin (Lipitor)

Other “Statins”Fluvastatin (Lescol)

Lovastatin (Mevacor, Altoprev)Pravastatin (Pravachol)Rosuvastatin (Crestor)Simvastatin (Zocor)

Cholestin (dietary supplement made from red yeast)

HMG-CoA REDUCTASE INHIBITORS (STATINS)Prototype: Atorvastatin (Lipitor)

Mechanism of ActionInhibits the enzyme (HMG-CoA) that synthesizes cholesterol

Increases the number of LDL receptors on liver cells to remove more LDLDecreases production of VLDLs and raises HDL levels

Stabilizes plaque, slows progression of coronary calcificationImproves endothelial function

Enhances the ability of blood vessels to dilateReduces the risk of thrombosis

Inhibits platelet deposition and aggregationMay increase bone formation

UsesHypercholesterolemia

Primary and secondary prevention of CV eventsPost MI therapy

Prevention of CV events in people with diabetesAdverse Effects

Headache, rash, GI complaintsMyopathy, increases CK levels, rhabdomyolysis, dark urine, renal failure

Hepatotoxicity, increases ALT and ASTRare peripheral neuropathy

FDA Pregnancy risk Category XDrug Interactions

Macrolide antibiotics, azole antifungalsHIV protease inhibitors, amiodarone, cyclosporine, and grapefruit juice raise some

statins to toxic levels

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NICOTINIC ACIDPrototype: Nicotinic Acid (Niacor, Niaspan)

Drug CombinationsLovastatin/niacin (Advicor)Simvastatin/niacin (Simcor)

NICOTINIC ACIDPrototype: Nicotinic Acid (Niacor, Niaspan)

Mechanism of ActionReduces LDL and triglycerides

Increases HDL

UsesLowers triglycerides in patients at risk for pancreatitis

Dyslipidemia Reduces the risk of major coronary events

Reduces total mortality

Adverse EffectsFlushing and itching (take 325 mg ASA 30 minutes before dose)

Gastric upset, nausea, vomiting, diarrheaHepatotoxicity

May raise blood sugar in patients with diabetesMay increase incidence of gout

BILE-ACID SEQUESTRANTSPrototype: Colesevelam (WelChol)

Other AgentsCholestyramine (Questran)

Colestipol (Colestid)

BILE-ACID SEQUESTRANTSPrototype: Colesevelam (WelChol)

Mechanism of ActionBinds (sequesters) bile acids in the GI tract

Prevents the absorption and promotes their excretionForms insoluble complex with bile acids

Increases LDL receptorsSafest of all lipid-lowering drugs


Often used in combination with statinApproved to control hyperglycemia in patients with type 2 diabetes

Adverse EffectsConstipation, bloating, indigestion

Interferes with absorption of other drugsMay impede absorption of fat-soluble vitamins

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EZETIMIBE (ZETIA)Cholesterol-Lowering Drug

Drug CombinationsSimvastatin/ezetimibe (Vytorin)

EZETIMIBE (ZETIA)Cholesterol-Lowering Drug

Mechanism of ActionInhibits cholesterol absorption in the small intestineReduces LDL, triglycerides, and apolipoprotein B

Small increase in HDL


Used in combination with statins

Adverse EffectsReports of myopathy, rhabdomyolysis, pancreatitis, and thrombocytopenia

May increase risk of liver damage when used with statins

FIBRIC ACID DERIVATIVES (FIBRATES)Prototype: Gemfibrozil (Lopid)

Other Fibric Acid DerivativesFenofibrate (TriCor, Antara, Lofibra, Triglide)

Fenofibric acid (TriLipix)—approved for use with statins

FIBRIC ACID DERIVATIVES (FIBRATES)Prototype: Gemfibrozil (Lopid)

Mechanism of ActionReduces triglycerides by lowering VLDL

Raises HDL levels

UsesHypertriglyceridemia

Adverse EffectsRash, nausea, abdominal pain, diarrhea

Gallstone formationMyopathy, liver injury

Increases warfarin levels, leading to hemorrhageDo not combine gemfibrozil with statins

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ORGANIC NITRATES (ANTIANGINAL AGENTS)Prototype: Nitroglycerin

Similar AgentsIsosorbide mononitrate

Isosorbide dinitrateAmyl nitrite

Other Antianginal AgentsBeta blockers

Calcium blockersRanolazine (Ranexa)

ORGANIC NITRATES (ANTIAGINAL AGENTS)Prototype: Nitroglycerin

Mechanism of ActionDilates veins, decreases venous return to the heart

Reduces ventricular filling and wall tension (preload)Reduces cardiac oxygen demand

UsesAngina, myocardial infarction

Adverse EffectsHeadache, orthostatic hypotension

Reflex tachycardiaTolerance to drug effect

Vasospasm if withdrawn abruptlyUse with sildenafil (Viagra), other drugs for erectile dysfunction may

lead to severe hypotension

ANTICOAGULANTSPrototype: Heparin

Low-Molecular-Weight Heparins (LMWH)Enoxaparin (Lovenox)Dalteparin (Fragmin)Tinzaparin (Innohep)

LMWH can be given on a fixed dose; does not require aPTT monitoring

Selective Factor Xa InhibitorsFondaparinux (Arixtra)

Rivaroxaban (Xarelto)

Direct Thrombin InhibitorsBivalirudin (Angiomax)

Lepirudin (Refludan)Argatroban

Desirudin (Ipravask)

ANTICOAGULANTSPrototype: HeparinMechanism of Action

Suppresses the formation of fibrin in veinsInactivates clotting factors thrombin and Xa

Anticoagulant effect develops quickly

UsesUsed for pulmonary embolism, evolving stroke, DVT

Open heart surgery, renal dialysisPrevention of postoperative thrombosisDisseminated intravascular coagulation

Acute myocardial infarction

MonitorActivated partial thromboplastin time (aPTT)

Normal aPTT: 40 seconds; therapeutic level: 60 to 80 seconds

Adverse EffectsBleeding—antidote is protamine sulfate

Heparin-induced thrombocytopenia (HIT)Decreased platelet count (,100,000/mm3) leads to thrombosis

Hypersensitivity reaction (fever, chills, urticaria)May be used during pregnancy

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ANTICOAGULANTPrototype: Warfarin (Coumadin, Jantoven)

Oral Anticoagulant

ANTICOAGULANTPrototype: Warfarin (Coumadin, Jantoven)

Mechanism of ActionSuppresses coagulation by reducing production of clotting factors

Antagonizes vitamin KInhibits vitamin K–dependent clotting factors

Blocks synthesis of factors VII, IX, X, and prothrombinEffect takes a few days

UsesLong-term prophylaxis of venous thrombosis and pulmonary embolism

Prevention of thromboembolism in patients with mechanical heart valvesPrevention of thrombosis in patients with atrial fibrillationPrevention of transient ischemic attacks and recurrent MI

MonitorProthrombin time (PT)—reported as INR

Goal INR for atrial fibrillation: 2-3Goal INR for mechanical valves: 3-4.5

Adverse EffectsHemorrhage—antidote is vitamin K (phytonadione)

Skin disorders, GI disturbances, red-orange color of urineIncreased risk of fractures with long-term use

Many drug-drug interactionsKeep intake of vitamin K foods constant

Fetal harm

ANTIPLATELET DRUGSPrototype: Aspirin

ANTIPLATELET DRUGSPrototype: AspirinMechanism of Action

Irreversible inhibition of COX-1 and COX-2Suppresses platelet aggregation

Decreases prostaglandin synthesisReduces the risk of arterial thrombosisReduces inflammation, pain, and fever

UsesIschemic stroke, transient ischemic attacks (TIAs)

Chronic stable angina, unstable anginaCoronary stenting, acute MI, previous MI

Primary prevention of MI

Adverse EffectsGastric distress (heartburn and nausea)

GI bleeding, gastric ulceration and perforationNot used in children because of the risk of Reye’s syndrome

Fetal harm (prolongs labor, premature closure of the patent ductus)Salicylism (tinnitus, sweating, headache, dizziness)

Hypersensitivity in patients with allergiesRenal impairment

Bleeding

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ANTIPLATELET DRUGSADENOSINE DIPHOSPHATE RECEPTOR (ADP)

ANTAGONISTSPrototype: Clopidogrel (Plavix)

Other, Similar AgentTiclopidine (Ticlid)—major adverse effects

ANTIPLATELET DRUGSADENOSINE DIPHOSPHATE RECEPTOR (ADP)

ANTAGONISTSPrototype: Clopidogrel (Plavix)

Mechanism of ActionBlocks ADP receptors so that platelets are unable to aggregate

UsesPrevents blockage of coronary artery stints

Reduces thrombotic events—MI, ischemic stroke, vascular death

Adverse EffectsDyspepsia, diarrhea, rash

Intracranial hemorrhage, GI bleedingRare thrombotic thrombocytopenia (TTP)

ANTIPLATELET DRUGSGLYCOPROTEIN llb/llla–RECEPTOR ANTAGONISTS

Prototype: Abciximab (RePro)

Other, Similar AgentsEptifibatide (Integrilin)Tirofiban (Aggrastat)

Dipyridamole (Persantine)Cilostazol (Pletal)

ANTIPLATELET DRUGSGLYCOPROTEIN llb/llla–RECEPTOR ANTAGONISTS

Prototype: Abciximab (RePro)Mechanism of Action

Causes reversible blockade of platelet GP IIb/IIIa receptorsInterferes with the final step in platelet aggregation

UsesPrevents ischemic events in patients with acute coronary syndrome

Used during percutaneous angioplasty

Adverse EffectsHemorrhage

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THROMBOLYTIC DRUGSPrototype: Alteplase (tPA)

Other, Similar AgentsStreptokinase (Streptase)Tenecteplase (TNKase)

Reteplase (Retavase)Urokinase (Abbokinase)

THROMBOLYTIC DRUGSPrototype: Alteplase (tPA)

Mechanism of ActionConverts plasminogen to plasmin

Plasmin is an enzyme that digests the fibrin matrix of clotsDissolves existing thrombi

Does not prevent thrombi from forming

UsesAcute myocardial infarction, pulmonary embolism, and ischemic stroke

Adverse EffectsBleeding

Intracranial hemorrhage

FERROUS SULFATEOral Iron Preparation

Other Oral Iron PreparationsFerrous fumarateFerrous gluconate

Carbonyl iron

FERROUS SULFATEOral Iron Preparation

Mechanism of ActionEssential to the function of hemoglobin and myoglobin

(oxygen-storing molecule of muscle)

UsesIron deficiency anemia (microcytic hypochromic anemia)

Adverse EffectsNausea, heartburn (pyrosis), bloating, constipation, diarrhea

May turn stool dark green or blackLiquid iron preparation stains teeth

Toxic to children (lethal dose is 2 to 10 grams)

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CYANOCOBALAMIN (VITAMIN B12)CYANOCOBALAMIN (VITAMIN B12)Mechanism of Action

Essential for synthesis of DNACatalyzes conversion of folic acid to its active form

UsesB12 deficiency, pernicious anemia

Macrocytic normochromic anemia (megaloblastic anemia)

Adverse EffectsHypokalemia

Never given IVFolic acid can mask the hematologic effects of B12 deficiency

FOLIC ACID (FOLATE)FOLIC ACID (FOLATE)Mechanism of Action

Essential for synthesis of DNA

UsesTreatment of folic acid deficiency (megaloblastic anemia)

Used prophylactically to prevent neural tube defects (NTDs)

Adverse EffectsDoes not correct neurologic consequences

Can correct anemia but may mask B12 deficiencyAlways give folic acid with B12

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ERYTHROPOIETIC GROWTH FACTORSPrototype: Epoetin Alfa

(Erythropoietin, Epogen, Procrit)

Other Erythropoietic Growth FactorsDarbepoetin Alpha (Aranesp)—long acting

Methoxy polyethylene glycol (Mircera)

ERYTHROPOIETIC GROWTH FACTORSPrototype: Epoetin Alfa

(Erythropoietin, Epogen, Procrit)Mechanism of Action

Stimulates production of red blood cells in the bone marrow

UsesAnemia of chronic renal failure

Anemia due to AIDS treatment with AZT (zidovudine)Anemia caused by chemotherapyAnemia in patients facing surgery

Adverse EffectsHypertension

Increase in cardiovascular events (heart failure, thrombosis, stroke and MI)Hemoglobin level should not exceed 12 g/dL

Rise in hemoglobin should not exceed 1 g/dL in 2 weeksRed cell aplasia (anemia due to autoimmune response)

LEUKOPOIETIC GROWTH FACTORSPrototype: Filgrastim (Neupogen)

Other Leukopoietic Growth FactorsPegfilgrastim (Neulasta)Sargramostim (Leukine)

LEUKOPOIETIC GROWTH FACTORSPrototype: Filgrastim (Neupogen)

Mechanism of ActionActs on bone marrow to increase production of neutrophils

UsesPatients undergoing myelosuppressive chemotherapy

Patients undergoing bone marrow transplantationHarvesting of peripheral blood progenitor cells

Severe chronic neutropeniaReduces risk of infection

Adverse EffectsBone pain, leukocytosis

Elevates uric acid levels, LDH, and alkaline phosphataseSplenomegaly

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THROMBOPOIETIC GROWTH FACTORSPrototype: Oprelvekin (Neumega)

THROMBOPOIETIC GROWTH FACTORSPrototype: Oprelvekin (Neumega)

Mechanism of ActionStimulates production of platelets (thrombocytes)

UsesPatients undergoing myelosuppressive chemotherapy

Increases platelets to minimize thrombocytopenia

Adverse EffectsRetention of sodium and water by kidneys

Peripheral edemaTachycardia, atrial fibrillation, atrial flutter

Severe allergic reactionsConjunctival injection

ORAL AGENTS FOR TYPE 2 DIABETESBIGUANIDES

Prototype: Metformin (Glucophage, Fortamet, Glumetza, Riomet)

ORAL AGENTS FOR TYPE 2 DIABETESBIGUANIDES

Prototype: Metformin (Glucophage, Fortamet, Glumetza, Riomet)

Mechanism of ActionInhibits glucose production in the liver (gluconeogenesis)

Inhibits glucose absorption in the intestinesSensitizes insulin receptors on fat and skeletal muscleEnhances glucose uptake and metabolism by muscle

Lowers basal and postprandial blood sugar

UsesType 2 diabetes

Prevention of type 2 diabetesTreatment of polycystic ovary syndrome (PCOS)

Adverse EffectsDecreased appetite, nausea, diarrhea, and weight loss

Rare cases of lactic acidosisAvoid in patients with renal disease (Cr .1.4 mg/dL)

Avoid in patients with ethyl alcohol (ETOH) abuse, infection, liver disease, or CHFDiscontinue 48 hours prior to test with contrast medium to avoid lactic acidosis

Can reduce vitamin B12 and folic acid absorption

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ORAL AGENTS FOR TYPE 2 DIABETESSULFONYLUREAS

Prototype: Glipizide (Glucotrol, Glucotrol ER)

Other SulfonylureasGlyburide (DiaBeta, Micronase)

Glimepiride (Amaryl)

ORAL AGENTS FOR TYPE 2 DIABETESSULFONYLUREAS

Prototype: Glipizide (Glucotrol, Glucotrol ER)Mechanism of Action

Stimulates insulin release from the pancreas

UsesType 2 diabetes

Adverse EffectsHypoglycemia

Possible increased risk of sudden cardiac deathFetal harm

Disulfiram-like reaction when taken with ETOH

ORAL AGENTS FOR TYPE 2 DIABETESMEGLITINIDES

Prototype: Repaglinide (Prandin)

Other MeglitinideNateglinide (Starlix)

ORAL AGENTS FOR TYPE 2 DIABETESMEGLITINIDES

Prototype: Repaglinide (Prandin)Mechanism of Action

Stimulates pancreatic insulin release

UsesType 2 diabetes


Administer 30 minutes before a meal

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ORAL AGENTS FOR TYPE 2 DIABETESTHIAZOLIDINEDIONES (GLITAZONES, TZDs)

Prototype: Rosiglitazone (Avandia)

Other TZDsPioglitazone (Actos)

ORAL AGENTS FOR TYPE 2 DIABETESTHIAZOLIDINEDIONES (GLITAZONES, TZDs)

Prototype: Rosiglitazone (Avandia)Mechanism of Action

Increases insulin sensitivity

UsesType 2 diabetes

Adverse EffectsMild headache and upper respiratory infections

Raises LDL levelsFluid retention—caution in patients with CHF

Hepatotoxicity—monitor ALTMay increase cardiovascular events

ORAL AGENTS FOR TYPE 2 DIABETESALPHA-GLUCOSIDASE INHIBITORS

Prototype: Acarbose (Precose)

Other Alpha-Glucosidase InhibitorMiglitol (Glyset)

ORAL AGENTS FOR TYPE 2 DIABETESALPHA-GLUCOSIDASE INHIBITORS

Prototype: Acarbose (Precose)Mechanism of Action

Delays absorption of carbohydratesLowers postprandial blood glucose levels

UsesType 2 diabetes

Adverse EffectsFlatulence, cramps, abdominal distention, and diarrhea

Hypoglycemia, liver dysfunction

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ORAL AGENTS FOR TYPE 2 DIABETESGLIPTINS

Prototype: Sitagliptin (Januvia)

ORAL AGENTS FOR TYPE 2 DIABETESGLIPTINS

Prototype: Sitagliptin (Januvia)Mechanism of Action

Increases the incretin system Inhibits the enzyme DPP-4, which breaks down incretin hormonesSuppresses glucagon release from the alpha cells of the pancreas

Stimulates insulin release from the beta cells of the pancreasTurns off glucose production in the liver

UsesType 2 diabetes

Adverse EffectsNasal inflammation, upper respiratory tract infection

Minimal hypoglycemia

NEW INJECTABLE DRUGS FOR DIABETESINCRETIN MIMETIC

Prototype: Exenatide (Byetta)

NEW INJECTABLE DRUGS FOR DIABETESINCRETIN MIMETIC

Prototype: Exenatide (Byetta)Mechanism of Action

Action similar to natural incretins released in the GI tractSlows gastric emptying

Stimulates glucose-dependent release of insulinInhibits postprandial release of glucagon

Suppresses appetiteDecreases postprandial blood glucose

UsesType 2 diabetes


Nausea, vomiting, and diarrheaRare incidences of pancreatitis

Weight loss

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NEW INJECTABLE DRUGS FOR DIABETESAMYLIN MIMETIC

Prototype: Pramlintide (Symlin)

NEW INJECTABLE DRUGS FOR DIABETESAMYLIN MIMETIC

Prototype: Pramlintide (Symlin)Mechanism of Action

Mimics the effects of amylin (hormone made in the pancreas)Reduces postprandial levels of glucose

Delays gastric emptyingSuppresses glucagon secretionIncreases the sense of satiety

Enhances the effects of mealtime insulin

UsesType 1 and type 2 diabetes

Adverse EffectsHypoglycemia when combined with other agents

NauseaInjection site reactions

INJECTABLE DRUGS FOR DIABETESGLUCAGON

INJECTABLE DRUGS FOR DIABETESGLUCAGON

Mechanism of ActionHormone that increases plasma levels of glucose

Opposite effect of insulin

UsesTreats hypoglycemia from insulin overdose

Used only if intravenous glucose is not available

Adverse EffectsNausea and vomiting

Place patient on side after administration

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THYROID HORMONESPrototype: Levothyroxine (Synthroid, Levoxyl)

Synthetic Preparation of T4

Other Thyroid Hormone PreparationsLiothyronine (Cytomel, Triostat) T3

Liotrix (Thyrolar) T3, T4 combinationArmour Thyroid—desiccated animal thyroid glands

THYROID HORMONESPrototype: Levothyroxine (Synthroid, Levoxyl)

Synthetic Preparation of T4Mechanism of Action

Converted to T3 in the bodyThyroid hormone replacement

UsesHypothyroidism

Adverse EffectsThyrotoxicosis if dosage is excessive

Tachycardia, angina, nervousness, insomniaHyperthermia, sweating, and tremor

Increases warfarin levelsTakes about 1 month to reach plateau

Take on an empty stomachDo not mix with calcium or iron

ANTITHYROID DRUGSPrototype: Propylthiouracil (PTU)

Other Antithyroid DrugsMethimazole (Tapazole)Radioactive iodine (131I)

Nonradioactive iodine—(Lugol’s solution)Sodium iodide (IV)

Potassium iodide (Thyro-Block)Propranolol (Inderal) suppresses tachycardia

ANTITHYROID DRUGSPrototype: Propylthiouracil (PTU)

Mechanism of ActionInhibits thyroid hormone synthesis

Inhibits conversion of T4 to T3 in the periphery

UsesHyperthyroidism, Graves’ disease

Thyrotoxic crisis

Adverse EffectsAgranulocytosis, hypothyroidism

Fetal harm, rash, nausea, arthralgia, headacheDizziness, paresthesias, and liver injury

May take 6 to 12 months to develop

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ERECTILE DYSFUNCTION DRUGSPDE-5 Inhibitors

Prototype: Sildenafil (Viagra)

Other Erectile Dysfunction DrugsTadalafil (Cialis)

Vardenafil (Levitra)Papaverine plus phentolamine injection

Alprostadil (prostaglandin E1)

ERECTILE DYSFUNCTION DRUGSPDE-5 Inhibitors

Prototype: Sildenafil (Viagra)Mechanism of Action

Enhances the normal erectile response to sexual stimuli by inhibiting PDE-5

UsesErectile dysfunction

Adverse EffectsHypotension, priapism

Nonarteritic ischemic optic neuropathy (NAION)Sudden hearing loss, dizziness, vertigo, tinnitusHeadache, flushing, dyspepsia, nasal congestion

Visual changes (blue color tinge, light sensitivity, blurring)Use with nitrates and alpha blockers leads to hypotension

DRUGS FOR BENIGN PROSTATIC HYPERTROPHY (BPH)5-alpha-Reductase Inhibitors

Prototype: Finasteride (Proscar)

Other 5-alpha Reductase InhibitorDutasteride (Avodart)

Alpha1-Adrenergic AntagonistsTerazosin (Hytrin)

Doxazosin (Cardura)Tamsulosin (Flomax)—used for BPH onlyAlfuzosin (Uroxatral)—used for BPH only

Other Drugs for BPHSaw palmetto

Tolterodine (Detrol)PDE-5 inhibitors

Botox

DRUGS FOR BENIGN PROSTATIC HYPERTROPHY (BPH)5-alpha-Reductase Inhibitors

Prototype: Finasteride (Proscar)Mechanism of Action

Reduces levels of dihydrotestosterone (DHT)Promotes regression of prostate epithelial tissueReduces mechanical obstruction of the urethra

Adverse EffectsReduces ejaculate volume and libidoGynecomastia (breast enlargement)

Reduces prostate-specific antigen (PSA)May mask an elevated PSA

Benefits develop slowly over 6 to 12 months

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LIVE VIRUS VACCINESVaricella (Varivax)

Oral Polio Vaccine (OPV) not used in the United States

Measles, Mumps, and Rubella Virus Vaccine (MMR)

Live Influenza Attenuated Vaccine (LIAV)

Yellow fewer vaccine

Zoster vaccine (Zostavax)

Rotavirus vaccine (Rotarix, Rota Teq)

LIVE VIRUS VACCINESLive virus vaccines are contraindicated in pregnancyGive with caution in immunocompromised patients

IMMUNOSUPPRESSANTSPrototype: Cyclosporine

(Sandimmune, Gengraf, Neoral)

Other ImmunosuppressantsTacrolimus (Prograf)

Sirolimus (Rapamune)GlucocorticoidsCytotoxic drugs

Antibodies

IMMUNOSUPPRESSANTSPrototype: Cyclosporine

(Sandimmune, Gengraf, Neoral)Mechanism of Action

Suppresses production of inflammatory cellsReduces B cells and cytotoxic T cells

UsesPrevents rejection of organ transplants

Adverse EffectsNephrotoxicity, infection, hepatotoxicity, lymphomas

Hypertension, tremor, hirsutism, leukopenia Gingival hyperplasia, gynecomastia

Anaphylaxis, fetal harm

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FIRST-GENERATION H1 ANTAGONISTSAntihistamines

Prototype: Diphenhydramine (Benadryl)

Other First-Generation AntihistaminesBrompheniramine

Chlorpheniramine (Chlor-Trimeton)DexchlorpheniramineClemastine (Tavist)

Promethazine (Phenergan)Hydroxyzine (Vistaril)

FIRST-GENERATION H1 ANTAGONISTSAntihistamines

Prototype: Diphenhydramine (Benadryl)Mechanism of Action

Blocks H1 receptorsBlocks some muscarinic receptors

Reduces actions of histamineReduces flushing, itching, and secretion of mucus

UsesSeasonal allergic rhinitis, urticaria, severe allergy, motion sickness, insomnia

Cold symptoms, sleep aid, mild transfusion reactions, allergic reactions

Adverse EffectsSedation, confusion, fatigue

Paradoxical excitation can occurGastrointestinal disturbances

Anticholinergic effects (BUDCAT)

SECOND-GENERATION (NONSEDATING) H1ANTAGONISTS

Prototype: Loratadine (Claritin)

Antihistamine

Other Second-Generation Nonsedating H1Antagonists

Desloratadine (Clarinex)Fexofenadine (Allegra)

Cetirizine (Zyrtec)Levocetirizine (Xyzal)

Azelastine (Astelin) nasal spray

SECOND-GENERATION (NONSEDATING) H1ANTAGONISTS

Prototype: Loratadine (Claritin)

AntihistamineMechanism of Action

Blocks H1 receptorsReduces actions of histamine

Reduces flushing, itching, secretion of mucusDoes not cross brain-blood barrier to cause sedation

UsesAllergic rhinitis, urticaria, and mild transfusion reactions

Adverse EffectsReduce dose if hepatic or renal impairment occurs

Cetirizine (Zyrtec) may cause mild sedation in some patients

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CYCLOOXYGENASE INHIBITORSNonsteroidal Anti-inflammatory Drug (NSAID)

Prototype: Aspirin

CYCLOOXYGENASE INHIBITORSNonsteroidal Anti-inflammatory Drug (NSAID)

Prototype: AspirinMechanism of Action

Irreversible inhibition of cyclooxygenase (COX-1 and COX-2)Suppresses platelet aggregation

Decreases prostaglandin synthesisReduces inflammation, pain, and fever

UsesSuppression of inflammation

AnalgesiaReduction of fever in adults

DysmenorrheaSuppression of platelet aggregation to protect against MI and stroke

Prevention of colorectal cancer Possible protection against Alzheimer’s disease

Adverse EffectsGastric distress (heartburn and nausea)

GI bleeding, gastric ulceration and perforationNot used in children because of the risk of Reye’s syndrome

Fetal harm (prolongs labor, premature closure of the patent ductus)Salicylism (tinnitus, sweating, headache, dizziness)

Hypersensitivity in patients with allergiesRenal impairment

Bleeding

CYCLOOXYGENASE INHIBITORSFirst Generation—Nonaspirin NSAIDsPrototype: Ibuprofen (Advil, Motrin)

Other NSAIDsFenoprofen (Nalfon)

Flurbiprofen (Ansaid)Ketoprofen

Naproxen (Aleve, Anaprox, Naprelan, Naprosyn)Oxaprozin (Daypro)

Diclofenac (Voltaren, Cataflam)—risk of liver failureVoltaren Gel and Flector Patch

Diclofenac Plus Misoprostol (Arthrotec)Diflunisal (Dolobid)

EtodolacIndomethacin (Indocin)

Ketorolac (Toradol), available IM or IVMefenamic acid (Ponstel)

MeclofenamateMeloxicam (Mobic)

NabumetonePiroxicam (Feldene)Sulindac (Clinoril)Tolmetin (Tolectin)

CYCLOOXYGENASE INHIBITORSFirst Generation—Nonaspirin NSAIDs

Prototype: Ibuprofen (Advil, Motrin)Mechanism of Action

Reversible inhibition of COX-1 and COX-2Inhibits prostaglandin synthesis

Has anti-inflammatory, analgesic, and antipyretic actions

UsesFever, pain, arthritis, dysmenorrhea

Closure of the ductus arteriosus in preterm infants

Adverse EffectsBleeding, gastric ulceration, renal impairment

Cross-hypersensitivity with aspirinMay precipitate Reye’s syndrome

Fetal harmRisk of MI and stroke

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CYCLOOXYGENASE INHIBITORSecond-Generation NSAID (COX-2 Inhibitor)

Prototype: Celecoxib (Celebrex)

CYCLOOXYGENASE INHIBITORSecond-Generation NSAID (COX-2 Inhibitor)

Prototype: Celecoxib (Celebrex)Mechanism of Action

Selective inhibition of COX-2Decreases prostaglandin synthesis at the site of injury

Reduces pain and inflammation Spares COX-1 inhibition

Minimal gastric, renal, and platelet effect

UsesOsteoarthritis, rheumatoid arthritis, dysmenorrhea

Acute pain

Adverse EffectsDyspepsia, mild renal impairment

Not used in patients with sulfonamide allergyPremature closure of ductus arteriosus

No inhibition of platelets Increased risk of MI and stroke

ACETAMINOPHEN (TYLENOL)Analgesic and Antipyretic

ACETAMINOPHEN (TYLENOL)Analgesic and Antipyretic

Mechanism of ActionReduces prostaglandin synthesis in the CNS

Has no anti-inflammatory properties

UsesPain and fever

Preferred in childrenNo GI injury, no effect on platelets or kidneys

Adverse EffectsToxic metabolite builds up in ETOH abusers

Hepatic necrosis can occurMaximum dose is 4 grams/day

Acetylcysteine (Mucomyst) given for overdoseInhibits metabolism of warfarin (risk of bleeding)

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GLUCOCORTICOIDSShort Acting

CortisoneHydrocortisone

Intermediate ActingPrednisone

PrednisoloneMethylprednisone

Triamcinolone

Long ActingBetamethasoneDexamethasone

GLUCOCORTICOIDSMechanism of Action

Suppress immune responses and inflammationInhibit prostaglandins, leukotrienes, and histamine

Suppress phagocytes and lymphocytes

UsesRheumatoid arthritis, SLE, inflammatory bowel disease

Bursitis, osteoarthritis, anaphylaxis, asthmaSkin disorders, neoplasms, suppression of allograft rejection

Prevention of respiratory distress syndrome (RDS) in preterm infantsReplacement therapy for patients with Addison’s disease

Adverse EffectsAdrenal insufficiency resulting from suppression of HPA axis

Osteoporosis, infection, glucose intolerance (increases blood sugar)Myopathy, sodium and water retention, potassium loss

Growth retardation, mood changesCataracts, glaucoma

Peptic ulcer disease, iatrogenic Cushing’s syndromeFetal harm

DISEASE-MODIFYING ANTIRHEUMATIC DRUGS(DMARDs I)

Prototype: Methotrexate (Rheumatrex, Trexall) Other DMARDs ISulfasalazine (Azulfidine)

Leflunomide (Arava)Hydroxychloroquine (Plaquenil)

DMARDs IIEtanercept (Enbrel)

Infliximab (Remicade)Adalimumab (Humira)Rituximab (Rituxan)Abatacept (Orencia)

DMARDs IIIPenicillamine (Cuprimine)

Azathioprine (Imuran)Cyclosporine

Anakinra (Kineret)Protein A column (Prosorba)

DISEASE-MODIFYING ANTIRHEUMATIC DRUGS(DMARDs I)

Prototype: Methotrexate (Rheumatrex, Trexall)Mechanism of Action

Blocks conversion of folic acid to its active formReduces joint destruction, retards disease progression

Takes 3 to 5 months to see effect

UsesRheumatoid arthritis, non-Hodgkin’s lymphoma

Lymphocytic leukemia, psoriasis, and Crohn’s disease

Adverse EffectsBone marrow suppression, hepatic fibrosisGI ulceration, pneumonitis, and fetal harm

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DRUGS FOR HYPERURICEMIAPrototype: Allopurinol (Zyloprim)

Other Drugs for HyperuricemiaProbenecid

Sulfinpyrazone (Anturane)

Drugs for Acute Gouty ArthritisNSAIDs

GlucocorticoidsColchicine (GI toxicities)

DRUGS FOR HYPERURICEMIAPrototype: Allopurinol (Zyloprim)

Mechanism of ActionInhibits uric acid formation

UsesChronic tophaceous gout

Hyperuricemia secondary to chemotherapyNot useful for acute gouty attacks

Adverse EffectsHypersensitivity syndrome

Nausea, vomiting, abdominal discomfortDrowsiness, headache, metallic taste

Cataracts with prolonged use (.3 years)

BISPHOSPHONATESPrototype: Alendronate (Fosamax)

Other BisphosphonatesRisedronate (Actonel)Ibandronate (Boniva)Tiludronate (Skelid)

Etidronate (Didronel)Zoledronate (Reclast, Zometa)

Other Drugs Used to Treat OsteoporosisSelective Estrogen Receptor Modulators (SERMs)

Raloxifene (Evista)

Parathyroid HormoneTeriparatide (Forteo)

BISPHOSPHONATESPrototype: Alendronate (Fosamax)

Mechanism of ActionSuppresses resorption of bone

Reduces both the number and activity of osteoclasts

UsesPostmenopausal osteoporosis

Osteoporosis in menGlucocorticoid-induced osteoporosis

Paget’s disease of the bone

Adverse EffectsEsophagitis

Musculoskeletal pain, ocular problemsOsteonecrosis of the jaw

Atrial fibrillation

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ANTI-INFLAMMATORY DRUGS FOR ASTHMAINHALED CORTICOSTEROIDS (ICSs)

Prototype: Fluticasone Propionate (Flovent)

Other Inhaled CorticosteroidsBeclomethasone dipropionate (QVAR)

Budesonide (Pulmicort Turbohaler, Pulmicort Respules)Flunisolide (AeroBid)

Mometasone furoate (Asmanex Twisthaler)Triamcinolone acetonide (Azmacort)

Combination ICSs and Long-Acting Beta2 AgonistsFluticasone and salmeterol (Advair)

Budesonide and formoterol (Symbicort)

ANTI-INFLAMMATORY DRUGS FOR ASTHMAINHALED CORTICOSTEROIDS (ICSs)

Prototype: Fluticasone Propionate (Flovent)Mechanism of Action

Suppresses the inflammation of asthmaDecreases leukotrienes, histamine, and prostaglandins

Decreases eosinophils and leukocytesReduces edema of the airway and mucus production

Reduces bronchial hyperactivityIncreases number of beta2 receptors

Increases responsiveness to beta2 agonists

UsesControl of asthma

Administered on a fixed scheduleTakes 2-8 days to see an effect, maximum benefit in 4-6 weeks

Adverse EffectsOropharyngeal candidiasis—rinse mouth after use

Minimal adrenal suppression and bone lossSlows growth but does not reduce adult height

Slight increased risk of cataracts, glaucoma, and osteoporosis

ANTI-INFLAMMATORY DRUGS FOR ASTHMALEUKOTRIENE MODIFIERS

Prototype: Montelukast (Singulair)

Other Leukotriene ModifiersZileuton (Zyflo)—associated with rare liver injury

Zafirlukast (Accolate)—associated with rare liver injury

ANTI-INFLAMMATORY DRUGS FOR ASTHMALEUKOTRIENE MODIFIERS

Prototype: Montelukast (Singulair)Mechanism of Action

Blocks leukotriene receptorsReduces inflammation, bronchoconstriction, and edema

Decreases secretion of mucusReduces eosinophils and other inflammatory cells

Reduces dosage of inhaled corticosteroids

UsesControl of asthma (not used as first-line therapy)

Prevention of exercise-induced bronchospasmAllergic rhinitis

Not used for rescue

Adverse EffectsGI upset

Delayed effectPossible rare neuropsychiatric effects (mood changes, suicidal thoughts)

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ANTI-INFLAMMATORY DRUGS FOR ASTHMAPrototype: Cromolyn (Intal)

ANTI-INFLAMMATORY DRUGS FOR ASTHMAPrototype: Cromolyn (Intal)

Mechanism of ActionSuppresses inflammation, prevents release of histamine

Stabilizes mast cell membraneNot a bronchodilator

UsesControl of asthma

Must be given on a fixed schedule (not used for rescue)Prevents exercise-induced bronchospasm

Allergic rhinitis (intranasal cromolyn)

Adverse EffectsSafest of all antiasthma medications

Rarely, can cause cough or bronchospasm

BRONCHODILATORSBETA2-ADRENERGIC AGONISTS (Inhaled Short-Acting Agents)

Prototype: Albuterol (Proventil, Ventolin, Accuneb)

Other Beta2-Adrenergic AgonistLevalbuterol (Xopenex, Xopenex HFA)

Oral Beta2-Adrenergic AgonistsAlbuterol (generic) tablets or syrup

Albuterol (VoSpire ER)Terbutaline (Brethine)

(Inhaled beta2 agents are preferred)

BRONCHODILATORSBETA2-ADRENERGIC AGONISTS(Inhaled Short-Acting Agents)

Prototype: Albuterol (Proventil, Ventolin, Accuneb)Mechanism of Action

Activation of beta2-adrenergic receptors in the lungPromotes bronchodilation

Rapid onset of action for rescue breathingSuppresses histamine release in the lung

Increases ciliary motility

UsesRapid relief of asthma symptoms

Adverse EffectsTachycardia, angina, and tremor

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BRONCHODILATORSBETA2-ADRENERGIC AGONISTS (Inhaled Long-Acting Agents)

Prototype: Salmeterol (Serevent)

Other Long-Acting Inhaled Beta2-Adrenergic AgonistsFormoterol (Foradil)

Arformoterol (Brovana)

BRONCHODILATORSBETA2-ADRENERGIC AGONISTS (Inhaled Long-Acting Agents)

Prototype: Salmeterol (Serevent)Mechanism of Action

Activates beta2-adrenergic receptors in the lungPromotes bronchodilation

Suppresses histamine release in the lungIncreases ciliary motility

UsesAsthma

Should not be used aloneShould be used in conjunction with an ICS

Adverse EffectsEffect is delayed by 20 to 30 minutesNot to be used for rescue breathing

Tachycardia, angina, tremor, and leg cramps

BRONCHODILATORSMETHYLXANTHINES

Prototype: Theophylline

Other MethylxanthinesAminophylline

BRONCHODILATORSMETHYLXANTHINES

Prototype: TheophyllineMechanism of Action

Produces bronchodilation by relaxing bronchi

UsesAsthma

(Beta2 agonists and inhaled corticosteroids preferred)

Adverse EffectsNarrow therapeutic range (5-15 mcg/mL)

Dysrhythmias, ventricular fibrillationConvulsions, cardiorespiratory collapse, and death

Many drug-drug reactions

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INTRANASAL GLUCOCORTICOIDS (ICSs)Prototype: Fluticasone (Flonase)

Other Intranasal GlucocorticoidsBeclomethasone (Beconase AQ)Budesonide (Rhinocort Aqua)

Flunisolide (Nasarel)Mometasone (Nasonex)

Triamcinolone (Nasacort AQ)

Other Drugs Used for Allergic RhinitisOral and nasal antihistamines

Intranasal cromolyn sodium (NasalCrom)Topical sympathomimetics (Oxymetazoline-Afrin)

Oral sympathomimetics (phenylephrine, pseudoephedrine)Ipratropium bromide (Atrovent) nasal spray

Montelukast (Singulair)

INTRANASAL GLUCOCORTICOIDS (ICSs)Prototype: Fluticasone (Flonase)

Mechanism of ActionAnti-inflammatory actions suppress symptoms of allergic rhinitis

Prevent or suppress congestion, rhinorrhea, sneezing, nasal itching

UsesSeasonal and perennial rhinitis

Adverse EffectsDrying of the nasal mucosa, burning or itching

Sore throat, epistaxis (nose bleed), and headache

ANTITUSSIVESPrototype: Dextromethorphan

Nonopioid Antitussive

Other Nonopioid AntitussivesDiphenhydramine (Benadryl)

Benzonatate (Tessalon)

Opioid AntitussivesCodeine

Hydrocodone

ANTITUSSIVESPrototype: Dextromethorphan

Nonopioid AntitussiveMechanism of Action

Acts in the CNS to suppress coughElevates the cough threshold

UsesAcute cough

Adverse EffectsMild inebriation and mind-body dissociation when abused

Can increase analgesic response to morphine

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HISTAMINE2-RECEPTOR ANTAGONISTPrototype: Cimetidine (Tagamet)

Other Histamine2-Receptor AntagonistsRanitidine (Zantac)Famotidine (Pepcid)

Nizatidine (Axid)

HISTAMINE2-RECEPTOR ANTAGONISTPrototype: Cimetidine (Tagamet)

Mechanism of ActionBlocks H2 receptors on parietal cells of the stomach

Reduces volume of gastric juice and hydrogen ion content

UsesGastric and duodenal ulcers

Gastroesophageal reflux disease (GERD)Treatment of Zollinger-Ellison syndrome

Aspiration pneumonitisHeartburn, acid indigestion, and sour stomach

Adverse EffectsSignificant side effects are uncommon

Antiandrogenic effectsConfusion, hallucinations, CNS depression or excitation

Pneumonia

PROTON PUMP INHIBITORS (PPIs)Prototype: Omeprazole (Prilosec)

Other PPIsLansoprazole (Prevacid)Rabeprazole (Aciphex)Pantoprazole (Protonix)Esomeprazole (Nexium)

Other Antiulcer DrugsSucralfate (Carafate)

Misoprostol (Cytotec)Antacids

Combination Drugs for Helicobacter pylori–associated ulcersHelidacPylera

Prevpac

PROTON PUMP INHIBITORS (PPIs)Prototype: Omeprazole (Prilosec)

Mechanism of ActionInhibits the enzyme that generates acid production

UsesDuodenal and gastric ulcers, erosive esophagitis

GERD, dyspepsiaZollinger-Ellison syndrome

Adverse EffectsHeadache, diarrhea, nausea, and vomiting

Gastric cancer, and hip fractures

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ANTIEMETIC DRUGSSerotonin-Receptor Antagonists

Prototype: Ondansetron (Zofran)

Other Serotonin-Receptor AntagonistsGranisetron (Kytril)

Dolasetron (Anzemet)Palonosetron (Aloxi)

Other Agents Used for NauseaGlucocorticoids

Aprepitant (Emend)Benzodiazepines

ANTIEMETIC DRUGSSerotonin-Receptor Antagonists

Prototype: Ondansetron (Zofran)Mechanism of Action

Suppresses emesis by blocking 5-HT3 receptors in the chemoreceptor trigger zone (CTZ)

UsesReduces nausea and vomiting caused by

chemotherapy, radiation therapy, and anesthesia (postoperatively)

Adverse EffectsHeadache, diarrhea, and dizziness

ANTIEMETIC DRUGSDopamine Antagonists

Prototype: Prochlorperazine (Compazine)

Other Dopamine AntagonistsPhenothiazines

Chlorpromazine (Thorazine)Perphenazine (Trilafon)

Promethazine (Phenergan)

ButyrophenonesHaloperidol (Haldol)Droperidol (Inapsine)

Metoclopramide (Reglan)

CannabinoidsDronabinol (Marinol)Nabilone (Cesamet)

ANTIEMETIC DRUGSDopamine Antagonists

Prototype: Prochlorperazine (Compazine)Mechanism of Action

Suppresses emesis by blocking dopamine2 receptors in the CTZ

UsesNausea and vomiting

Used after surgery, cancer chemotherapy, or other conditions

Adverse Effects Extrapyramidal reactions, anticholinergic effects

Hypotension and sedation

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PROKINETIC AGENTSPrototype: Metoclopramide (Reglan)

PROKINETIC AGENTSPrototype: Metoclopramide (Reglan)

Mechanism of ActionSuppresses emesis by blocking receptors for dopamine and serotonin in the

chemoreceptor trigger (CTZ)Increases upper GI motility by enhancing the actions of acetylcholine

UsesSuppresses postoperative nausea and vomiting

Suppresses emesis associated with chemotherapy, radiation therapy, toxinsand opioids

Relieves diabetic gastroparesisSuppresses gastroesophageal reflux disease (GERD)

Adverse EffectsSedation and diarrhea

Extrapyramidal reactions, especially in children

HYDROXYZINE (VISTARIL, ATARAX)Antiemetic Drug

Anticholinergic-Antihistamine

HYDROXYZINE (VISTARIL, ATARAX)Antiemetic Drug

Anticholinergic-AntihistamineMechanism of Action

Blocks histaminergic and cholinergic receptors

UsesNausea

Adverse EffectsSedation, blurry vision, urinary retention, dry mouth

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PENICILLINS (PCNs)Narrow-Spectrum Penicillin (Penicillinase Sensitive)

Beta-Lactam Antibiotic

Prototype: Benzylpenicillin (Penicillin G)

Parenteral PCN G (three salts)(1) Potassium PCN G (IM or IV)

(2) Procaine PCN G (never used IV)(3) Benzathine PCN G (never used IV)

Prescribed in units (1 unit = 0.6 mg)

Oral PCNPenicillin V (Veetids)

PENICILLINS (PCNs)Narrow-Spectrum Penicillin (Penicillinase Sensitive)

Beta-Lactam Antibiotic

Prototype: Benzylpenicillin (Penicillin G)Mechanism of Action

Disruption of the bacterial cell wall

UsesParenteral antibiotic treats gram-positive and gram-negative

Streptococcus and Neisseria organisms, anaerobes, and othersDrug of choice for syphilis

Adverse EffectsAllergic reaction, pain at site of injection

NeurotoxicitiesDo not mix PCN with aminoglycosides in IV solutions

ANTISTAPHYLOCCAL PENICILLINSPenicillinase-Resistant Penicillins

(PCNs that cannot be inactivated by bacterial beta-lactamases)

Prototype: Nafcillin (Unipen)

Other Antistaphyloccal PenicillinsOxacillin

Dicloxacillin Methicillin (no longer available)

ANTISTAPHYLOCCAL PENICILLINSPenicillinase-Resistant Penicillins

(PCNs that cannot be inactivated by bacterial beta-lactamases)

Prototype: Nafcillin (Unipen)Mechanism of Action


UsesTreats infections caused by penicillinase-producing strains of Staphylococcus

(ie, S. aureus, S. epidermidis)

Adverse EffectsAllergic reaction, GI effects

Thrombophlebitis, hypokalemia

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AMINOPENICILLINSBroad-Spectrum Antibiotics

Prototype: Amoxicillin

Other AminopenicillinsAmpicillin

(Amoxicillin is preferred for oral therapy)

AMINOPENICILLINSBroad-Spectrum Antibiotics

Prototype: AmoxicillinMechanism of Action


UsesSame antimicrobial spectrum as PCN

plus increased activity against gram-negative bacilli Treats infections caused by Haemophilus influenzae, Escherichia coli,

and Salmonella and Shigella organismsIneffective against Staphylococcus aureus

Adverse EffectsDiarrhea

ANTIPSEUDOMONIAL PENICILLINSExtended-Spectrum Penicillins

Prototypes: Ticarcillin, Piperacillin

Antipseudomonal Penicillins with Beta-Lactamase Inhibitors

Ticarcillin with clavulanic acid (Timentin)Piperacillin with tazobactam (Zosyn)

ANTIPSEUDOMONIAL PENICILLINSExtended-Spectrum Penicillins

Prototypes: Ticarcillin, Piperacillin Mechanism of Action


UsesAntimicrobial spectra same as for aminopenicillinsplus Pseudomonas aeruginosa, Bacteroides fragilis,

and Enterobacter, Proteus, and Klebsiella spp.Used with aminoglycosides (not in the same IV)

Can be destroyed by bacterial penicillinases

Adverse EffectsSodium overload

Interference with platelet function, leading to increased bleeding time

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FIRST-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Cephalexin (Keflex)

Other First-Generation CephalosporinsCefadroxil (Duricef)

Cefazolin (IV)

FIRST-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Cephalexin (Keflex)Mechanism of Action

Weakens the bacterial cell wall

UsesGram-positive infections

Surgical prophylaxis

Adverse EffectsAllergic reaction

Pain at injection siteThrombophlebitis

Rare antibiotic-associated pseudomembranous colitis (AAPMC)

SECOND-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Cefprozil (Cefzil)

Other Second-Generation CephalosporinsCefaclor (Ceclor)

Cefotetan (Cefotan)Cefoxitin (Mefoxin)Cefuroxime (Ceftin)

Zinacef

SECOND-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Cefprozil (Cefzil)Mechanism of Action


UsesEnhanced activity against gram-negative bacteria

Upper respiratory tract infectionsAcute otitis media (AOM) and sinusitis

Adverse EffectsAllergic reaction

Bleeding tendencies (cefotetan)Thrombophlebitis

Rare antibiotic-associated pseudomembranous colitis (AAPMC)

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THIRD-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Ceftriaxone (Rocephin)

Other Third-Generation AntibioticsOral

Cefdinir (Omnicef)Cefditoren (Spectracef)

Cefixime (Suprax)Cefpodoxime (Vantin)

Ceftibuten (Cedax)

IM, IVCefoperazone (Cefobid) Cefotaxime (Claforan)

Ceftazidime (Fortaz) [for Pseudomonas aeruginosa]Ceftizoxime (Cefizox)

Fourth-Generation CephalosporinCefepime (Maxipime)

THIRD-GENERATION CEPHALOSPORINSBeta-Lactam Antibiotics

Prototype: Ceftriaxone (Rocephin)Mechanism of Action


UsesActive against gram-negative organisms

Able to penetrate cerebrospinal fluid (CSF)Treats meningitis caused by gram-negative and gram-positive bacteria

Effective for Neisseria gonorrhoeae infection

Adverse EffectsAllergic reactionThrombophlebitis

Rare antibiotic-associated pseudomembranous colitis (AAPMC)Fatal precipitate forms with calcium(Do not mix with Ringer’s lactate)

CARBAPENEMSBroad-Spectrum Beta-Lactam Antibiotics

Prototype: Imipenem (Primaxin)

Other CarbapenemsMeropenem (Merrem IV)

Ertapenem (Invanz)Doripenem (Doribax)

CARBAPENEMSBroad-Spectrum Beta-Lactam Antibiotics

Prototype: Imipenem (Primaxin)Mechanism of Action


UsesActive against gram-positive cocci,

gram-negative cocci, gram-negative bacilli, and anaerobic bacteria

Adverse EffectsGI effects

Hypersensitivity reactionsSuprainfectionsSeizures (rare)

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VANCOMYCIN (VANCOCIN)Antibiotic

VANCOMYCIN (VANCOCIN)Antibiotic

Mechanism of ActionInhibits bacterial cell wall synthesis

UsesActive against gram-positive bacteria

Effective for serious infections, such as methicillin-resistant Staphylococcus aureus(MRSA)

Second choice to treat antibiotic-associated pseudomembranous colitis Oral form used in patients who do not respond to metronidazole to delay resistance

Used for patients allergic to penicillin

Adverse EffectsOtotoxicity

Rapid infusion can lead to red man syndrome (ie, flushing,tachycardia, and hypotension)

ThrombophlebitisImmune-mediated thrombocytopenia

NOTE: Infuse over 60 minutes or longer

TETRACYCLINESBroad-Spectrum Antibiotics

Prototype: Doxycycline (Vibramycin)

Other TetracyclinesTetracycline (Sumycin)Minocycline (Minocin)

Demeclocycline (Declomycin)

TETRACYCLINESBroad-Spectrum Antibiotics

Prototype: Doxycycline (Vibramycin)Mechanism of Action

Suppresses bacterial growth by inhibiting protein synthesisBinds to 30S ribosomal subunit to prevent the addition of amino acids

BacteriostaticUses

Rocky Mountain spotted fever, typhus fever, Q feverInfections caused by Chlamydia trachomatis

Brucellosis, choleraPneumonia caused by Mycoplasma pneumoniae

Lyme disease, anthraxGastric infections with Helicobacter pylori (peptic ulcer disease [PUD])

Periodontal disease and acneCommunity-acquired methicillin-resistant S. aureus (CA-MRSA)

Adverse EffectsGI irritation, suprainfection (AAPMC)

Overgrowth with fungi (Candida albicans)Discoloration of teeth (avoid in children ,8 years old)

Do not give to pregnant womenHepatotoxicity, exacerbation of renal impairment

Photosensitivity, vestibular toxicityChelating agents interfere with absorption

Do not administer with:milk products, calcium, iron, magnesium, and laxatives

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MACROLIDESBroad-Spectrum Antibiotic

Prototype: Erythromycin

Other MacrolidesClarithromycin (Biaxin)

Azithromycin (Zithromax)Dirithromycin (Dynabac)

Troleandomycin (Tao)

MACROLIDESBroad-Spectrum Antibiotic

Prototype: ErythromycinMechanism of Action

Inhibits bacterial cell wall synthesisBinds to the 50S ribosomal subunit to block addition of amino acids

UsesActive against most gram-positive and some gram-negative organisms

Treats atypicals such as:Pneumonia caused by Legionella pneumophila and Mycoplasma pneumoniae

Bordetella pertussis, Corynebacterium diphtheriaCan be used as an alternative to PCN in allergic individuals

Treats chlamydial infections (urethritis, cervicitis)

Adverse EffectsGI effects, liver injury

Inhibitor of cytochrome P450Increases levels of theophylline, carbamazepine, and some statins

QT prolongation and sudden cardiac death

CLINDAMYCIN (CLEOCIN)Antibiotic

CLINDAMYCIN (CLEOCIN)Antibiotic

Mechanism of ActionInhibits bacterial protein synthesis

UsesUsed as an alternative to penicillin for serious gram-positive anaerobic

infectionsBacteroides fragilis, Fusobacterium sp., Clostridium perfringens

Adverse EffectsAntibiotic-associated pseudomembranous colitis (AAPMC)

Diarrhea

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LINEZOLID (ZYVOX)Oxazolidinones Antibiotic

LINEZOLID (ZYVOX)Oxazolidinones Antibiotic

Mechanism of ActionBacteriostatic inhibitor of protein synthesis

Binds to the 23S portion of the 50S ribosomal subunit

UsesActive against aerobic and gram-positive bacteria

Enterococcus faecium (vancomycin sensitive and vancomycin resistant)Staphylococcus aureus (methicillin-sensitive and methicillin-resistant strains)

Staphylococcus epidermidis (methicillin-resistant strains)Streptococcus pneumoniae (PCN sensitive and PCN resistant)


Myelosuppression (reversible)Neuropathy

HTN (blocks MAO)

AMINOGLYCOSIDESNarrow-Spectrum Antibiotics

Prototype: Gentamicin

Other AminoglycosidesTobramycin

Amikacin (Amikin)

AMINOGLYCOSIDESNarrow-Spectrum Antibiotics

Prototype: GentamicinMechanism of Action

Disrupts bacterial protein synthesisBinds to the 30S ribosomal subunit

UsesEffective against aerobic gram-negative bacilli

Serratia marcescens, Proteus mirabilis, Pseudomonas aeruginosa

Adverse EffectsNephrotoxicity (renal dosing required to avoid toxic drug levels)

Ototoxicity (requires peak and trough level monitoring)Intensifies neuromuscular blockade, leading to respiratory arrest

Incompatible with PCN

Ch85


ofProteinSynthesis

Ch86

Am

inoglycosides:BactericidalInhibitorsofProtein

Synthesis

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SULFONAMIDES AND TRIMETHROPRIMPrototype: Trimethoprim/Sulfamethoxazole

(Bactrim, Septra)

SULFONAMIDES AND TRIMETHROPRIMPrototype: Trimethoprim/Sulfamethoxazole

(Bactrim, Septra)Mechanism of Action

Combination antibiotic that inhibits bacterial synthesis of folic acid

UsesUrinary tract infections

Pneumocystis pneumonia (PCP) caused by Pneumocystis jiroveci


Hypersensitivity reactions (Stevens-Johnson syndrome)Not for use in patients with sulfa allergies

Hematologic effects: Agranulocytosis,leukopenia, thrombocytopenia, aplastic anemia

Hemolytic anemia in patients with G6PD deficiencyKernicterus (do not use in infants ,2 months or pregnant women near term)

Crystalluria, leading to renal damage (increase fluids)CNS effects, hyperkalemia, photosensitivity

Increases the effects of sulfonylurea, leading to hypoglycemia

FLUOROQUINOLONESPrototype: Ciprofloxacin (Cipro)

Other FluoroquinolonesRespiratory fluoroquinolones:

Moxifloxacin (Avelox)* and Levofloxacin (Levaquin)Gemifloxacin (Factive)*

*Prolongs QT interval

FLUOROQUINOLONESPrototype: Ciprofloxacin (Cipro)

Mechanism of ActionInhibits bacterial DNA and cell division

UsesInfections of the urinary, respiratory, and GI tracts, bones,

joints, skin, and soft tissuesAnthrax

Adverse EffectsAchilles tendon rupture and tendinitis (black box warning)

GI upsetCNS effects (dizziness, headache, and restlessness)

Do not take with milk products or ironElevates levels of warfarin

Not recommended for children under age 18 Avoid in pregnancy

Ch87

Sulfonamides

andTrim

ethoprimCh

90M

iscellaneousA

ntibacterialDrugs

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METRONIDAZOLE (FLAGYL)Antibacterial Drug

METRONIDAZOLE (FLAGYL)Antibacterial DrugMechanism of Action

Causes cell death by damaging bacterial DNA

UsesProtozoal infections

Infections caused by obligate anaerobic bacteria (Bacteroides fragilis)Infections of the CNS, abdominal organs, bones, joints, skin, and soft tissue

Infections of the genitourinary tract (Trichomonas vaginalis)Drug of choice for antibiotic-associated colitis caused by

Clostridium difficileEradicates Helicobacter pylori

Used as prophylaxis in colorectal or abdominal surgery

Adverse EffectsNausea, headache, dry mouth, metallic taste

Vertigo, numbness in the extremitiesDark discoloration of urine

Disulfiram-like effect (vomiting) when used with alcoholIncreases warfarin levels

ANTIFUNGAL AGENTSPrototype: Itraconazole (Sporanox)

Other Azole AntifungalsFluconazole (Diflucan)Voriconazole (Vfend)

Ketoconazole (Nizoral)Posaconazole (Noxafil)Miconazole (Monistat)

Clotrimazole

Other Antifungal DrugsAmphotericin B (causes nephrotoxicity)

Caspofungin (Cancidas)Micafungin (Mycamine)Anidulafungin (Eraxis)Flucytosine (Ancibon)Nystatin (Mycostatin)Terbinafine (Lamisil)Butenafine (Lotrimin)

Ciclopirox (Loprox, Penlac Nail Lacquer)

ANTIFUNGAL AGENTSPrototype: Itraconazole (Sporanox)

Mechanism of ActionCauses bacterial cell wall to leak

UsesSystemic and superficial mycoses (fungi)

Adverse EffectsGI effects, headache, abdominal pain, and edema

Cardiac suppressionLiver injury

Inhibits hepatic drug-metabolizing enzymesDrug reactions with digoxin, warfarin, sulfonylureas, statins,

proton pump inhibitors (PPIs)

Ch90

Miscellaneous

AntibacterialD

rugsCh

91A

ntifungalAgents

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ANTIFUNGAL AGENTGriseofulvin

ANTIFUNGAL AGENTGriseofulvin

Mechanism of ActionInhibits fungal mitosis

UsesSuperficial mycoses (fungi)

Dermatophytic infections of the skin, hair, and nailsNot active against Candida species or systemic mycoses

May take 3 to 8 weeks to have an effect

Adverse EffectsMay diminish effects of warfarin

ANTIVIRAL DRUGSPrototype: Acyclovir (Zovirax)

Other, Similar AgentsValacyclovir (Valtrex)Famciclovir (Famvir)

Topical AgentsPenciclovir (Denavir)Docosanol (Abbreva)

Ocular AgentsTrifluridine (Viroptic)

Vidarabine ointment (Vira-A)

ANTIVIRAL DRUGSPrototype: Acyclovir (Zovirax)

Mechanism of ActionSuppresses synthesis of viral DNA

UsesHerpes simplex genitalis

Mucocutaneous herpes simplex infectionsVaricella-zoster infections

Adverse EffectsIV administration can lead to phlebitis and nephrotoxicity

Infuse slowly over 1 hour and maintain hydrationOral therapy may lead to nausea, vomiting, diarrhea

Headache and vertigo

Ch91

AntifungalA

gentsCh

92A

ntiviralAgents

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DRUGS FOR HEPATITISPrototype: Interferon Alpha

DRUGS FOR HEPATITISPrototype: Interferon Alpha

Mechanism of ActionDecreases viral replication

UsesHepatitis B and hepatitis C

Adverse EffectsFlulike syndrome

Neuropsychiatric effects—depression and suicidal ideationFatigue, thyroid dysfunction, heart damage

Bone marrow suppression

DRUGS FOR HEPATITISPrototype: Ribavirin (Rebetol, Copegus)

DRUGS FOR HEPATITISPrototype: Ribavirin (Rebetol, Copegus)

Mechanism of ActionUnclear

UsesUsed with interferon for treatment of hepatitis C

Adverse EffectsHemolytic anemia

Fetal harm (FDA Pregnancy Risk Category X)Use a second reliable form of birth control during treatment

and for 6 months after treatment

Ch92

AntiviralA

gentsI

Ch92

AntiviralA

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NUCLEOSIDE/NUCLEOTIDE REVERSE TRANSCRIPTASEINHIBITORS (NRTIs) Antiretroviral Drugs

Prototype: Zidovudine (Retrovir)

Other NRTIs and CombinationsDidanosine (Videx)

Stavudine (Zerit)Lamivudine (Epivir)Abacavir (Ziagen)

Tenofovir disoproxil fumarate (Viread)Emtricitabine (Emtriva)

Zalcitabine (Hivid)Abacavir/zidovudine/lamivudine (Trizivir)

Abacavir/lamivudine (Epzicom)Emtricitabine/tenovir (Truvada)

Lamivudine/zidovudine (Combivir)Emtricitabine/tenofovir/efavirenz (Atripla)

NUCLEOSIDE/NUCLEOTIDE REVERSE TRANSCRIPTASEINHIBITORS (NRTIs)Antiretroviral Drugs

Prototype: Zidovudine (Retrovir)Mechanism of Action

Suppress the synthesis of viral DNA by blocking transcriptasePenetrates the CNS better than most antiretrovirals

UsesHIV infection

Adverse EffectsAnemia and neutropenia from bone marrow suppressionLactic acidosis with hepatomegaly and hepatic steatosis

Gastrointestinal effectsCNS reactions (headache, insomnia, confusion, anxiety, and seizures)

Myopathy

NON-NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NNRTIs)Antiretroviral Drugs

Prototype: Efavirenz (Sustiva)

Other NNRTIsNevirapine (Viramune)

Delavirdine (Rescriptor)Etravirine (Intelence)

NON-NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NNRTIs)Antiretroviral Drugs

Prototype: Efavirenz (Sustiva)Mechanism of Action

Binds directly to HIV reverse transcriptaseInhibits reverse transcriptase

UsesHIV infection

Adverse EffectsCNS symptoms

Rash, Stevens-Johnson syndromeFetal harm

Liver damageMany drug-drug reactions

Ch93

AntiviralA

gentsII

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PROTEASE INHIBITORSAntiretroviral Drugs

Prototype: Ritonavir (Norvir)

Other Protease InhibitorsLopinavir/ritonavir (Kaletra)

Indinavir (Crixivan)Saquinavir (Invirase)Nelfinavir (Viracept)

Amprenavir (Agnerease)Fosamprenavir (Lexiva)

Atazanavir (Reyataz)Tipranavir (Aptivus)

Darunavir/ritonavir (Prezista)

PROTEASE INHIBITORSAntiretroviral Drugs

Prototype: Ritonavir (Norvir)Mechanism of Action

Inhibits the enzyme protease, which HIV requires to mature

UsesHIV infection

Adverse EffectsHyperglycemia/diabetes, fat maldistribution, hyperlipidemia

Increased bleeding in hemophiliac patientsReduced bone mineral density

Elevation of serum transaminasesCan increase or decrease levels of other drugs

Many drug-drug interactions

INTEGRASE INHIBITORSAntiretroviral Drugs

Prototype: Raltegravir (Isentress)

Other Drugs for HIV

HIV Fusion InhibitorEnfuvirtide (Fuzeon)

Chemokine Receptor CCR5 AntagonistMaraviroc (Selzentry)

INTEGRASE INHIBITORSAntiretroviral Drugs

Prototype: Raltegravir (Isentress)Mechanism of Action

Inhibits integrase to stop HIV replication

UsesHIV infection

Adverse EffectsDiarrhea, nausea, fatigue, headache, and itching

Possible myopathy and rhabdomyolysis

Ch93

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gentsII

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Dietary Supplement

Black cohosh

Coenzyme Q-10

Cranberry juice

EchinaceaFeverfew

Flaxseed

Garlic

Ginger root

Uses

Menopausal symptoms

May reduce myalgias associated with statins

Prevents bacteria from adhering to urinary tract

Stimulates immune systemMigraine prophylaxis

Dyslipidemia and constipation

Dyslipidemia and hypertension

Vertigo, nausea, and vomitingAnti-inflammatory effects

Potential Problems

Liver toxicityComes mixed with St. John’s

wort; many drug-drug reactionsMay antagonize the effects of

warfarinGI upset and formation of uric

acid kidney stonesAllergic reactionsSuppresses platelet

aggregation-risk of bleedingSuppresses platelet



aggregation-risk of bleedingHigh doses can cause

spontaneous abortion

Commonly Used Dietary Supplements Ch107

Dietary

Supplements

Dietary Supplement

Ginkgo bilobaGlucosamineGreen tea

KavaMa huangProbiotics

Saw palmetto

Soy

St. John’s wort

Valerian root

Uses

Improves age-related memoryOsteoarthritisImproves mental clarity,

weight loss, cancer preventionAnxietyStimulantIrritable bowel syndrome,

antibiotic-associated diarrheaBenign prostatic hypertrophy

Prevention of cancerMenopausal symptomsMild to moderate depression

Sedative, promotes sleep

Potential Problems

May suppress coagulationIncreased risk of bleedingIncreased heart rate, hepatotoxicityReduces effects of warfarinHepatotoxicity, sedationStroke, MI, and deathFlatulence

Suppresses platelet aggregation-risk of bleeding

Fetal harm in womenIncreased risk of oxalateKidney stonesPhotosensitivityAccelerates metabolism of

many drugsSerotonin syndromeDrowsiness

Commonly Used Dietary Supplements

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