Pharm Unit 2

Special concepts r/t Antimicrobials• Selective toxicity

– Ability to target without harming host• Susceptibility• Prophylaxis

– Neutropenia, Surgery, Endocarditis• Combination Therapy• Misuse – non-specific fevers, viruses

Resistance

Ch. 86

Aminoglycosides: Background• Resistance is beginning to limit use

– Gentamicin – cheaper but commonly used

– 20 diff aminoglycoside-inactivating enzymes– Reserve amikacin

• Bactericidal– concentration dependent– Post-antibiotic effect – several hours (prolonged)– NOT effective against anaerobes

Gentamicin (Garamycin)

MOA/ Use Narrow spectrum for gram negative bacilli- especially pseudo. Aerugenosa, E. coli, Klebs, Serratia

ADME Poor CSF Not absorbed orally Toxicity with wound irrigation Binds tightly to renal tissue Excretion primarily renal Dosage varies widely (.5 mg/kg to 25 mg/kg)

Adverse Effects Ototoxic R/t excess trough levels- sensory hairs HA, N, vertigo then high- pitched tinnitus (action?) Vestibules of ears and absorbs into tissues to kidney Nephrotoxic Total cumulative dose ATN (acute tubular necrosis- leads to renal failure) -- proteinuria, casts

(slough or big particles), increased BUN, increased Creatinine Elderly and children at risk Neuromuscular blockade Flaccid, weak muscles Dosage based Neurotoxic with peripheral muscles Hypersenditivity & blood dyscrasias (rare)

D = D – PCNs, Cephs, Vanco used in combo– PCNs inactivate – schedule issue?– Ethacrynic Acid – ototoxicity– Other nephrotoxics– Skeletal Muscle relaxants

Aminoglycosides: Special concerns• Neomycin most nephrotoxic• Scheduling once daily – Safer?

– Post-antibiotic effect– Washout – esp. in vestibule and kidneys– Typically only measure trough – up to 1hr prior to next dose – level should be ?

Ch. 91 Antifungal Agents

Systemic mycotic infections

• Opportunistic (host is immunocompromised, malnourished, ill): candidiasis, aspergillosis, cryptococcosis, mucormycosis

• Nonopportunistic: sporotrichosis, blastomycosis, histoplasmosis, coccidioidomycosisSuperficial mycotic infections

• Candidiasis• Dermatophytes

Major Classes of Antifungals• Polyenes• Azoles• Pyrimidine analogs• Echinocandins

Amphotericin B (Fungizone)MOA/ TE – Broad spectrum antifungal agent binds to ergosterol component of

fungal cell wall and increases permeability. – DOC for most progressive, potentially fatal systemic mycoses

ADME – Highly toxic (sterols)– Poor GI absorption - SLOW IV USE ONLY– Poor CSF– Break down human sterols and bug sterols

Adverse effects – almost 100% - varying

– Phlebitis– Fever, chills, nausea – pre-treat w benadryl / acetaminophen– Nephrotoxicity – residual if 4 g/day, 1 L NS, Monitor q 3-4 days– Hypokalemia– Bone marrow suppression

DDD nephrotoxics - flucytosine

Itraconazole (Sporanox)MOA/ TE – Azole group of antifungal agents that inhibits sythesis of

ergosterol – fungistatic to treat histoplamosis, meningitis of cryptococcus neoformans & disseminated candidiasis

ADME – PO or IV– Food abs. capsules, ¯ abs. of suspension– Metabolized in liver– 40% excreted unchanged in urine

Adverse Effects – Common – N, V, and D, rash, HA, edema– Rare - Hepatic necrosis, transient cardiosuppression

DDD – Inhibits cytochrome P450 isozymes– Increases levels of warfarin, digoxin, sulfonylureas, cyclosporine,

quinidine and many other drugs– Acid reduces decrease drug levels

**if system is impaired, drug levels will rise (cytochrome P450 isozymes)

Azoles: Special Considerations• Fluconazole [Diflucan]

– Lower toxicity level– Can be taken orally– SJS syndrome (Stephen Johnson syndrome)

• Ketoconazole [Nizoral]– Effect on sex hormones – inhibits production

Drugs for Superficial Mycoses• Dermatophytic infections (e.g., ringworm)

– Tinea pedis, tinea corporis, t. cruris, & t. capitis• Drugs

– Clotrimazole (Gyne-Lotrimin) – DOC for topical dermatophytic and candida infections of skin, mouth, vagina

• Vulvovaginal candidiasis– Griseofulvin (Grifulvin) - oral

• onychomycosis

Griseofulvin (Grifulvin V)MOA/ TE Superficial mycoses only – inhibits fungal mitosis – incorporates into keratin

Adverse Effects – Transient headache, rash, GI– Contraindicated in hepatocellular disease

DDD – Decreases warfarin

Ch. 92 Drugs fro Non-HIV Viral Infections

Viral Infections• Dilemma• Types

– HSV (Herpes-simplex)• Genitalia, mouth, face (HSV-2)• More sensitive to antivirals, less resistant

– VZV (Varicella Zoster)• Chicken pox – Shingles• Moderate sensitive

– CMV (Cytomegalovirus)• Less sensitive and more resistant

Acyclovir (Zovirax)MOA/ TE Suppress synthesis of viral DNA and is useful in treating HSV1,2 & VZV – no

cure

Adverse Effects – Intravenous: reversible nephrotoxicity, phlebitis• Infuse slowly – hydration – during & 2 hr after

– Oral: GI, vertigo– Topical: stinging

Nursing Implications – Resistance – type of clients– IV indicated for oral lesions in – STI control– Treatment for VZV in elderly and children (w/in 24 hr)– ONLY give po (low availability), topically or IV

– NO IV bolus, NO IM, or NO SubQ injections– Valacyclovir [Valtrex] – prodrug that increases oral

bioavailability by 55%– Without regard to meals

*check to see if admin is correct in bookBolus- def.

Ganciclovir (Cytovene, Vitrasert)MOA/ TE – Suppresses replication of viral DNA to treat CMV retinitis of

immune compromised clients & prevent CMV in transplant patients

Adverse Effects – Granulocytopenia & thrombocytopenia – Mutagenesis, carcinogenesis– Teratogenisis and infertility – (90d following cessation)

Valganciclovir (Valcyte) – prodrug for oral use

– Take intact – with food

Hepatitis C (HCV)• Transmission—blood and semen• Typically asymptomatic • Leading cause for liver transplants• Among most common causes of liver cancer• Not curable, only suppressible• Drugs

– Pegylated interferon alfa combined with ribavirin

Interferon alfa (Peg-Intron) Immune modulatory, antineoplastic, antiviralMOA/ TE – Blocks entry of virus, synthesis of viral m-RNA and proteins,

and viral assembly. Tx of chronic Hep B & C

ADME – Pegylated - makes drug longer acting– Only parenterally (SubQ)

Adverse Effects – Flu-like (fever, myalgia, HA, fatigue) & depression– Long/High dose – thyroid dysfunction, heart damage, bone

marrow suppression– Alopecia, GI, injection site pain, bruising

Ribavirin (Rebetol)MOA unclear – Used with Interferon A - together are DOC for

Hep C (HCV). – Therapy 24 to 48 weeks. Goal is SVR – sustained

virologic response (loss of detectable viral RNA)

Adverse Effects – Hemolytic anemia (a lot of RBCs that are broken)– Teratogenic (Category X) – two forms of BC

Dosage Based on weight

Teratogenic Can kill fetus

Hepatitis B - HBV • Transmission—blood and semen• Drugs

– HBV vaccine – Interferon alfa-2b [PEG-Intron]– Lamivudine [Epivir-HBV]- already developing resistance– Adefovir [Hepsera]

• Duration of treatment and relapse

Flu Vaccines• 3 strains – selected by CDC, FDA, & WHO• Inactivated

– IM• Live attenuated – LAIV (Flumist) – 2003

– Intranasally – MUST BE FROZEN– Only ages 5-49

• Efficacy – Who should receive it?– 1-2 wks before exposure & lasts for 6 mo

• Adverse effects– Fever, malaise, myalgia– Guillain-Barré syndrome – Swine flu vac. 1976– LAIV – runny nose, HA, cough – rare GBS, anaphylaxis

• Precautions and contraindications– Acute febrile illness, hypersensitivity to eggs

• Who should NOT without MD approval?– Allergy to egg– Previous severe reaction– GBS– Moderate, severe illness w/ fever– Children under 6 months– LAIV not for: adults over 50, children under 5, pregnants, children or adolescents on long-term

ASA therapy, chronic heart, lung disease

Drugs for Influenza

Oseltamivir (Tamiflu)MOA/ TE inhibit viral replication of Inf A&B and is used to prevent and treat same –

effective if implemented within 2 days of sxms

Adverse Effects – N&V– Confusion, self injury

Expensive Must be started prior to 48 hr

ATI p. 220 Ch. 32 Antidepressants

General Points• Most common psychiatric disorder• Major treatment method - medications

– Five major groups• Goal? • Sxms

– Depressed mood, loss of pleasure / interest in all or nearly all of one’s usual activities• Under-treated • More prevalent in women• Suicidal thoughts may increase w Rx

Tricyclic Antidepressants (TCAs)Imipramine (Tofranil)MOA/ TE/ Use – Blocks reuptake of the MAO transmitters NE (norepinephrine)

and serotonin. Elevates mood, thereby treating depression.– Other uses: bipolar disorder, neuropathic pain, insomnia,

fibromyalgia, OCD

Adverse Effects – Orthostatic hypotension, sedation, anticholinergic effects, diaphoresis, cardiotoxicity, seizures, hypomania, “yawngasm”- orgasm that occurs when they yawn

Glands (Table 14-1) Salivary glands- decreased secretionSweat glands- decreased secretionBronchial glands-

Precautions/ Interactions – TCAs w MAOI can lead to severe HTN– Potentiates drugs like NE (norepinephrine)– Potentiate CNS depressants

Antidote – Activated charcoal after gavageDosing – Based on clinical response – don’t give more than a week

supplys– Dose at bedtime once levels achieved – EXCEPT in elderly

(cardiac reasons)

SSRI AntidepressantsFluoxetine (Prozac)

MOA/ TE/ Use – Selective serotonin re-uptake inhibitor resulting in elevated

serotonin levels – elevating mood and relieving depression.– Helps in bulimia nervosa

Adverse Effects – Impotence, weight gain, Serotonin syndrome, withdrawal syndrome, EPS, bruxism (clenching teeth and jaw), bleeding, hyponatremia.

– Some people have w/draw symptoms with this

Interactions MAOIs, Warfarin, & TCAs

MAOI AntidepressantsPhenelzine (Nardil)MOA/ TE/ Use – Enzyme – deactivates NE, serotonin, dopamine, and tyramine

(NE stimulator) from foods– NOT 1st CHOICE– Relevant P-kinetics

• Tyramine

Adverse Effects – CNS stimulation – agitation – hypomania – mania – hypotension – HTN crisis – meperidine (hyperpyrexia)

Deactivates tyramine which deactivates the transmitter

Atypical AntidepressantsBupropion (Wellbutrin)MOA Action unclear

Effect Stimulant ergo no wt gain No sexual dysfunction – may augment

Adverse Effects agitation, HA, dry mouth, constipation, wt loss, insomnia, tachycardia, seizure

Note St. John’s Wort (Box 32-2)

Other

(ATI p. 203 or 220??)

Used in smoking cessation Known to bring on seizures Can enhance sexual functions Consider this a vitamin (herbal supplement) May have an impact with BCP

Ch. 34 Classification: Sedative- Hypnotics

Overview• Venacular

– Anti-anxiety, anti-anxiolytics, tranquilizers– Hypnotics

• Major Categories – Benzodiazepines, Barbiturates, Barbiturate–Like– Miscellaneous

• Major Effects– CNS depression

• Therapeutic Uses– Relieve anxiety, facilitate sleep, manage muscle spasms, seizure and panic disorders, augment

anesthesia, and manage ETOH withdrawal

Benzodiazepines (CIV) Category DDiazepan (Valium) – self limiting

Others: clonazepam, lorazepam, clorazepateMOA – Depress neuronal function at multiple CNS sites by potentiating

endogenous GABA (gamma-aminobutyric acid) and is limited because GABA is finite®safer

Cardiac PO effect - heart & blood vessels (not a huge effect) IV effect – potentially ? (huge effect)

Respiratory Minimal alone, serious if combo or IV

Pharmacokinetics – Readily absorbed – Differ in respect to time - course of action

• (main indicator for which one chosen for which job)

Adverse Effects CNS – daytime vs. nighttime impacts– Amnesia– Paradoxical- opposite effect– Abuse– Malnutrition, liver disease and blood levels

DDD w/ other CNS depressants

Dosage varies by agent

Low Albumin Low circulation of drug (malnutrition)Nursing Implications ATI p. 218

Benzodiazapine-likesZolpidem (Ambien) CIVMOA/ TE/ Use – Agonists at benzodiazepine receptor

site on GABA channel prolonging sleep duration and helps relieve insomnia

– Low potential for tolerance or abuse

Adverse Effects Causes sleep walking, or not safe effects for the person

– Similar to benzodiazepines (daytime drowsiness / dizziness)

– Can intensify CNS depressants

Dosage/ Administration Before bedtime?- about 1 hr before bedtime

Melatonin AgonistRamelteon (Rozerem)MOA/ TE/ Use Activates melatonin receptors and rapidly induces

sleep to treat insomnia

Adverse Effects Somnolence, dizziness, and fatigue, reduced libido

Precautions ETOH, liver impairment, dangerous activities

BarbituratesSecobarbital (Seconal)MOA/ TE/ Use Mimics GABA and depresses CNS directly causing

relaxation and anxiety reduction. Other uses: seizure management, anesthesia, sleep disorders, mania

ADME NO CEILING TO LIMITS OF CNS depression (mimics GABA)

Adverse Effects Resp. depression, hypotension in toxic doses, can readily cause death

Precautions – Highly addictive - physical dependence – withdrawal can be severe

– Caution in elderly– Caution with other CNS agents– Caution with IM injection

Ch. 37 Drug Abuse

Terms• Drug abuse- using a drug in a fashion inconsistent with medical or social norms• Addiction- a disease process characterized by the continued use of a specific psychoactive substance

despite physical, psychologic, or social harm• Cross-tolerance- is a state in which tolerance to one drug confers tolerance to another • Psychological dependence- an intense subjective need for a particular psychoactive drug• Physical dependence- a state in which an abstinence syndrome will occur if drug use is discontinued• Cross-dependence- refers to the ability of one drug to support physical dependence on another drug• Withdrawal syndrome- a constellation of signs and symptoms that occurs in physically dependent

individuals when they discontinue drug use

Table 37-1 Diagnostic Criteria for Substance Abuse and Dependence

Ch. 28 Classifications: Opioid (Narcotic) Analgesics, Opioid Antagonists, Non-opioid Centrally Acting Analgesics

Intro to Opioids• Chemical class: Opioid vs. opiate• Functional class: Narcotic Analgesic• MOA – body peptides (3) enkephalins, endorphins, dynorphins• Opioid receptors - mu, kappa, and delta

– Agonist, partial agonist, antagonist• Partial agonist- partially mimics, if give with drug can compete with another drug and

negate it or antagonize it--- produces low to moderate activation alone– Strong and moderate to strong

Table 28-1 Important Responses to Activation of Mu and Kappa Receptors

Opioid AgonistsSTRONG: Morphine (Duramorph) CIIMODERATE to STRONG: Codeine (Paveral) CIIIMOA/ TE – Mimics action of endogenous opioid receptors (mu) to produce

analgesia and thereby relieve pain– Other effects include drowsiness, mental clouding, anxiety reduction,

sense of well-being

Adverse Effects – Resp. depression• Diminished by “tolerance” • Most common cause of OD death

– Others • Constipation, orthostatic hypotension, urinary retention /

urgency, cough suppression, biliary colic, emesis (usually with codeine), elevated ICP (intracranial pressure), dysphoria, sedation, miosis, neurotixicity, immune and hormone suppression with prolonged use

– Toxicity • Classic triad (coma, resp. depression, pinpoint pupils)

DON’T USE Caution: don’t use morphine with head injuries – if there is pressure in the head, the vessels constrict

ADME (pharmacokinetics) Nursing Implications

– Given by several routes– Slowest to fastest– Time-frame for TE varies by mode of administration – Denatured in liver– Hard to cross blood-brain barrier

Precautions/ Contraindictions

– Decreased resp reserve, pregnancy, head injury, infants / elderly, hypotension, liver disease

Interactions – CNS depressants, antihistamines, antihypertensives, MOAIs*, antiemetics, amphetamines, agonist-antagonist, antagonists

Dosage Highly individualized (Table 28-5)Administration – po, IM, IV, SQ, topical

– Oral associated with chronic– Preferably fixed schedule– Site specific – hazards- epidural- effects delayed

Miosis- pinpoint eyes (constriction)

Mydriasis- linked to dialated eyes

Other strong opioidsFentanyl (Sublimaze) – Anesthesia primary use (injectable)

– 100 X mg potency of morphine– Commonly seen as transdermal

• No children under 2 / none for under 18 less than 100 lbs.

Transmucosal (popsicle) • Breakthrough cancer pain• Store carefully• very large amts of drug

Meperidine (Demerol) – Interacts with several drugs– Toxic metabolite

• Avoid use past 48 hrs and not to exceed 600mg/24hr.

Hydromorphone (Dilaudid)MethadoneHeroin Crosses blood-brain easier

Moderate to Strong Opioid AgonistsCodeine – Usual dose of 30 mg = about same relief as 325 mg

of ASA or Tylenol– Combo meds more effective– Extremely effective cough suppressant at 10 mg

dose range

Oxycodone (OxyContin) & CR formsHydrocodone (Lortab, Norco) CIIIProproxyphene (Darvon, Darvocet) CIV

Special Clinical Concepts r/t Use of Opioids• Pain assessment – including evaluation!• Dosing amt and schedule• Fear of addiction in clinical setting• Avoiding withdrawal – 20 days or more• Patient controlled anesthesia (PCA)• Morphine: DOC - heart attack (MI)• Meperidine [Demerol]: DOC OB in delivery• Avoid opioids in Head Injury…

Nursing Implications (ATI p. 133 or 150)

Class: Opioid Agonist- Antagonists (Partial agonist)Pentazocine (Talwin) Others: nalbuphine (Nubain), butorphanol (Stadol)MOA • act mostly at mu, kappa receptor to produce

analgesia and relieve pain– Alone = agonist action– With agonist = can antagonize (blocks

mu receptor)

Adverse effects Similar to opioidsADME (Pharmacokinetics) – Less respiratory depression, low abuse

potential– Less effective pain relief– *Can start withdrawal sxms in opioid

addiction

Class: Opioid AntagonistsNaloxone (Narcan)MOA/ TE/ Use – competes for opiate site and blocks effects of opioid agonists /

agonist-antagonists – no significant effect given alone – resulting in REVERSAL of narcotic

ADME – Rebound effect – if you give morphine and narcan- the narcan may wear off first

Adverse effects Acute withdrawalDosage/ Admin 0.4 mg IM, IV, SubQOthers Naltrexone (ReVia) ETOH/ Opioid abuse

Non-Opioid: Centrally Acting AnalgesicsTramadol (Ultram) Others: clonidine (Duraclon) – pain/ HTN

MOA/ TE/ Use – Analog of codeine – binds w mu receptor producing analgesia to relieve pain- also blocks re-uptake of norepi (fight or flight or increase BP)

ADME (Pharmacokinetics) – Minimal potential for dependence or resp depression

Adverse effects Rare – most common: sedation, dizziness, HA, dry mouth, constipation

Precautions Can intensify other CNS dep. – ABSOLUTELY avoid MAOIs

Ch. 77 Laxatives

Bulk-formingMethylcellulose, phyllium (Metamucil)MOA/ Use – Behave like dietary fiber – nonabsorbable – swell to form viscous

solution / gel and softening fecal mass and increasing transit.– Temp relief of constipation, diarrhea, irritable bowel, ostomies

Adverse effects Esophageal & intestinal obstruction if not enough fluid ® ?(If this, then?)

Can obstruct (build a brick) the gut and won’t move through, therefore causing surgeryEsophagus- if you don’t drink enough to get pill down it can cling to walls and get stuck causing tears

SurfactantsDocusate sodium (Colace)MOA/ Use – Lower surface tension of stool and softens by facilitating

penetration of water into the feces– Act on intestinal wall to inhibit fluid absorption and stimulate

secretion of water and electrolytes into the intestinal lumen.

ADME – Full glass of water– Sit upright for 30 min– Effectiveness dose related (min 200 mg/day)

Dosage 50-500 mg dailyAdverse reactions RareOther – Bring water to the stool to soften it

– Typically see someone getting 200+ mg/day– New EBP says that anything under 200 is not effective

StimulantsBisacodyl (Dulcolax), Senna (Senekot)MOA/ Legitimate Uses – Directly stimulate gut motility, increase secretion of water and

ions into intestine, and reduce water and electrolyte absorption.– Uses: Treatment of (1) opioid-induced constipation and (2) slow

transit constipation

Dosage • related to formulation administered– Take bisacodyl no sooner than 1 hour after ingesting milk or

antacids – do not crush

Adverse reactions bowel rupture can occur

Osmotics (Salt prototypes)Sodium phosphate (Fleet) & Magnesium saltsMOA/ Uses Non-absorbable and retains water in the colon

Adverse reaction – Dehydration, diarrhea and loss of water (more with salts than with glycol)

– Magnesium can accumulate to toxic levels in renal failure– Sodium can retain fluid – so…. Contraindicated in patients with

heart failure HTN and edema

Other • glycol (MiraLax) – fewer side effects / safer

Miscellaneous• Lactulose- sugar base

– Action / Uses• Poorly absorbed and cannot be digested – by product of breakdown results in osmotic

diuresis• Enhances excretion of ammonia in liver failure

– SEs – flatulence, cramping• Glycerin Suppository• Polyethylene Glycol-Electrolyte (GoLytely)

– Safe in dehydrated or electrolyte sensitive

Additional Nursing Implications• High risk patients

– Contraindicated in abdominal pain, nausea, cramps, regional enteritis, diverticulitis, ulcerative colitis, acute surgical abdomen, fecal impaction, bowel obstruction.

• Abuse• Castor oil (powerful stimulant – avoid at night – not to children) p. 908

Ch. 69 Antihistamines

Background• Histamines – (Predominantly H1)

– Endogenous – Vessel effects – Bronchi effects – Stomach effects – Greatest interest

• Allergic reactions (mild / anaphylaxis)• PUD

Histamine Release• Allergic response

– Requires IgE antibodies– Prior exposure to allergen

• Non-allergic – direct stimulation of cells– Some drugs, chemicals, radiocontrast media, plasma expanders - require no prior exposure– Cell injury

Physio/ Pharm Effects• H1 Stimulation

– Vasodilation (If this, then?)– Vessel wall cells contract (If this, then?)– Bronchoconstriction (If this, then?)– Itching & pain– Mucus secretion– CNS effect – cognition / memory / sleep

• H2 Stimulation– Secretion of gastric acid (If this, then?)

• H2 blocker, block secretion of acid

Allergies & Pharmacology• Mild Allergy

– Hay fever, urticaria, mild transfusion rx.– Sxms caused by ? TX?

• Severe– Anaphylactic shock (bronchocontriction, hypotension, & edema of glottis)– Sxms caused by? TX? (ch 17)

• Other Uses– Common cold – runny nose

Antihistamines: 1st GenerationH1 Antagonists (classic antihistamines)

– No single prototype • dyphenhydramine [Benadryl]

– Highly sedating

MOA – Blockers (1st Gen)• Selectively bind to histaminic receptors• Can also bind to nonhistaminic receptor (muscarinic)

TE – Vessels (If blocks histamine, then ?)– Capillaries (If blocks, then ?)– Sensory nerves (If, then) – itching relief– Mucous membranes (If, then)

• If you block mucous production, then you get dryness– CNS

• Therapeutic doses (If, then) - sedation• Overdose – stimulation, seizures – esp. in young

– Other: relieve N & V, motion sickness

Clinical uses – Mild allergies, seasonal rhinitis, acute urticaria, allergic conjunctivitis, mild transfusion reactions

– Some block muscarinic & H1 receptor sites – useful for motion sickness

• promethazine [Phenergan] and dimenhydrinate [Dramamine]

– Insomnia (diphenhydramine [Benadryl])

Adverse effects – CNS• Sedation = to excess ETOH (If this, then?)• Dizziness, lack of coordination, confusion• Paradoxical: insomnia, excitation, tremors, convulsions

– GI• N, V, Diarrhea / constipation, loss of appetite

– Anticholinergic effects (memorize)– Cardiac Dysrhythmias w some 2nd Gen.

• Torsades de pointes, V-fib • terfenadine [Seldane] & astemizole [Hismanal] (neither

one is on market anymore)• Contraindications – third trimester• Precautions: asthma (bronchoconstriction- spasms), children/elderly,

urinary retention, HTN, OA glaucoma, prostatic hypertrophy Dry mouth, throat, nasal passages, thickened secretions, (cautions?), urinary histiancy, constipation, palpitations

D D D – ETOH, barbs/benzos/ opioids

Toxiciy – Sxms similar to atropine poisoning (anticholinergic), hyperpyrexia (fever)

– Can lead to death in children via excitation, hallucinations, convulsion, coma, CV collapse, death.

– Tx: remove and support – may use charcoal followed with cathartics

Antihistamines: 2nd GenerationPrototypes Fexofenadine (Allegra) – ExpensiveMOA/ TE Antagonists of histamine to relieve sxms of allergic rhinitis and urticarias

ADME Do not readily cross B-B barrier therefore non-sedating w minimized anticholinergic SEs

Precautions ETOH, drowsiness, liver, kidneys

Ch. 75 Drugs for Treating Allergic Rhinitis, Coughs, Colds

Allergic RhinitisReview of Sxms Sneezing, itching, runny nose, congestion

Common- conjunctivitis, sinusitis, asthma• Commonly associated disorders• Seasonal vs. Perennial

• Outdoor vs. indoor

Antihistamines• First line - oral• Prophylaxis first• No use against cold• Adverse effects

– 1st gen - sedation, anticholinergic– 2nd gen - rare

Intranasal GlucocorticoidsFluticasone (Flonase)MOA/ Use – Predominantly local anti-inflammatory

– First line - Most effective against all sxms

Adverse effects – Drying, burning, or itching– Rare - sore throat, epistaxis and HA– Rare - systemic – adrenal suppression / slowed growth in children

Dose • Adults – 2 sprays of 50 mcg. once daily

Intranasal CromolynCromolyn (NasalCrom)MOA/ Use – Suppresses release of histamine

– Best suited for prophylaxis– May not see results for week or more

Adverse effects Negligible

Sympathomimetics (Decongestants)Phenylephrine (Neo-Synephrine)MOA/ Use – Topical - rapid and intense

– Oral - prolonged, moderate, systemic effects– Also used in sinusitis and colds

Adverse effects – Rebound congestion– CNS stimulation– Cardiovascular– Hemorrhagic stroke w/ phenylporpanolamine (not on market

anymore)– Abuse (pseudoephedrine and ephedrine)– Cocaine

Mimics the syntheseticsNasal sprays – 2 – 3 sprays every 4 hours needed – not to exceed 5 consecutive

days– Use temporarily– Don’t want tissues to become dependant on it

• Don’t want them to think they have to have it for tissues to function

AnticholinergicsIpratropium bromide (Atrovent)MOA/ Use – Blocks cholinergic receptors and inhibits secretions to relieve

rhinorrea in allergic rhinitis and asthma– No systemic effects

SEs Drying, irritation

Leukotriene AntagonistMontelukast (Singulair)MOA/ Use – Blocks binding of leukotrienes to receptors thereby relieving

nasal congestion

Adverse effects None significant

Treatment of Coughs

Antitussives• Antitussives (cough suppressants)

– Actions / use: elevate cough threshold in common cold and URTI• Opioid (codeine and hydrocodone) - best

– Dosage: codeine 10 to 20 mg up to 6 times daily• Nonopioid (dextromethorphan) - best

– Opioid derivative w/o euphoria or dependence– Can lead to mind-body dissociation equal to PCP

ExpectorantsGuaifenesin (Mucinex)MOA/ Use Increases flow of respiratory tract secretions

MucolyticsAcetlcysteine (Mucomyst)MOA/ Use Directly thins secretions

ADME Inhalation delivery

Adverse effects Can trigger bronchospasm

Other antidote for Tylenol

Colds• Drug regimen

– Symptomatic– Combination products

• Decongestants• Antitussives• Analgesics• Antihistamines - anticholinergic to suppress mucus• Caffeine

Ch. 17 Treatment of Severe Allergy

Adrenergic AgonistEpinephrineMOA/ Use – Direct receptor binding (a 1&2, b1&2) mimicing the sympathetic

nervous system • Also known as sympathomimetic & catecholamine

ADME – Broken down quickly in stomach & significant 1st pass effect (can’t take by mouth)

– Can’t cross blood-brain– Discolors (pink/brownish) as it degrades (If, then?)

TE – Vasoconstriction (most common use)• Hemostasis• Augments local anesthetic via vascontriction• Elevates blood pressure• Restores beating heart• Bronchodilates

– TOC for anaphylactic shock– Mydriasis (rare use)

Adverse effects – HTN, necrosis, bradycardia w/ HTN, tachycardia, tremor, chest pain, elevated blood sugar

D D D – MAOIs– TCAs– General anesthestics (myocardial effects)

Precautions – IV admin can cause potentially fatal effect – check concentrations!

– Insure patent and healthy IV site

EpiPen • Anaphylactic deaths– PCN, venoms & foods

• Device: EpiPen & EpiPen Jr.• Storage & Replacement

– Room temp – dark – do NOT refrigerate• Injection

– Dose dependant on weight• Duration

– Around 20 min and monitor for 6 hours• SEs- heart rate increase

Ch. 76 Selected Drugs for Peptic Ulcer Disease (PUD)

Histamine2 – Receptor AntagonistsCemetadine (Tagamet) First choice for gastric / duodenal ulcersMAO/ Use Promote healing through acid reduction

GERD, Aspiration Pneumonitis in obese & gyne prior to anesthesia

Adverse effects – Low incidence of gynecomastia, reduced libido, impotence, CNS depression / excitement, pneumonia

D D D – Inhibits hepatic drug metabolism – therefore?– Major Drugs of concern – warfarin, phenytoin, theophylline,

lidocaine

Table 76-1 (use for histamine and rest of outline)

Famotadine (Pepcid)• For heartburn, acid indigestion, sour stomach• Cut dose in renal compromise/ failure• No antiandrogenic effects• No effect on hepatic metabolism of other drugs

Proton Pump InhibitorsOmeprazole (Prilosec)MOA/ Uses • suppress secretion of gastric acid

– Irreversible - days - up to weeks after cessation– Superior to H2RAs

Adverse effects – HA, diarrhea, N & V– Long term may increase risk of CA

ADME give 30 min before meal – once daily

DDD, DDF – Reduced absorption of atazanavir, ketocanazole and itracanazole – NOT recommended concurrently with atazanavir

AntacidsMagnesium hydroxide/ Aluminum hydroxideMOA/ Uses • alkaline agents that neutralize acid & decrease destruction of gut wall

– And prophylactically to prevent aspiration pneumonia

ADME – Take regularly to promote healing– In PUD: 1 and 3 hr after each meal & at bedtime– Goal is gastric pH greater than 5

Adverse effects – Constipation (aluminum base) / Diarrhea (magnesium base)– Sodium “loading”– High levels in renal failure clients

DDD May interfere with absorption of other drugs