Pharm study guide 1:

Concepts:

Special population considerations- Elderly - they can have multiple chronic conditions, polypharmacy, adherence issues,

functional limitations, use 31% of the drugs even though they represent 12% of population. Issues in All parts of ADME

- A: ↓ GI motility and gastric emptying, ↑ gastric pH- D: ↑ body fat %, ↓ body H2O, Lean body mass, albumin- M: ↓ hepatic (Liver) mass, blood flow, and metabolism.- E: Renal issues will cause excretion issues and can lead to toxicity and negative

drug effects - African population responds poorly to ACE inhibitors, but responds better to calcium

channel blockers and Diuretics. - Kiddos, but I did not find information about this population in the slides except do not

recommend over the counter cough meds to a child less than 6 yo. (per the American Academy of Pediatrics)

Scheduled vs. legend drugs- Look in davis/online

Half-life- (t ½ )The amount of time it takes for the body to eliminate half of the drug.

Pregnancy categories (old and new) Davis Drug Guide for Nurses Appendix I.- A: have not shown an increased risk of fetal abnormalities- B: Studies in animals show no negative effects, but there are no studies in pregnant

women, or there are animal studies that show adverse effects and studies in pregnant women are not adequate

- C: animals have shown adverse effect, and there are no adequate and well-controlled studies in pregnant women, OR no animal studies have been conducted and there are no adequate and well controlled studies in pregnant women

- D: studies, adequate well-controlled or observational, in pregnant women have demonstrated a risk to the fetus. however, the benefits of therapy may outweigh the potential risk.

- X: Studies, adequate well-controlled or observational, in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. the use of the product is contradicated in women who are or may be pregnant.

Concepts of potentiation and interference in CYP 450 system- System overview: 12 channels, 50 isoenzymes, 90% of drugs go through 6 channels. If

2 or more drugs need one channel there can be interference. - Interference: one drug can increase or decrease the excretion or metabolism of another

drug. - ex. Erythromycin taken w/ increases serum digoxin levels, and increases action

of Coumadin - potentiation: when two similar drugs have an effect that adds on one another.

- ex. Coumadin + aspirin can = excessive bleeding- ex. sedatives + ETOH can = excessive sedation

How other organ system issues impact drug dosing (i.e. renal)- The renal system if not working well or in a disease state, will cause drug accumulation.

this is an extremely important and common cause of toxicity and adverse med effects.Protein binding

- a drug is competing to bind a protein in the blood and will end in a “drug reservoir” and allows accumulation to occur.

- the drug must be unbound to be useful or work.- the most common protein that a drug binds to is albumin- two similar drug molecules will have compete for binding sites on serum proteins

Therapeutic index- is a ratio between the lethal dose and the effective dose. TI=LD/ED- Therapeutic range: the area between the ED and LD, so effective but not lethal or toxic.

First pass effect- for most oral or enteral drugs will be metabolized by the liver on the first pass through

the liver. - Some drugs could be 90% metabolized on the first pass.

Nursing interventions to reduce adverse effects- Monitor for drug interactions - know pt allergies history- monitor patient for s/s

Drug interactions- interference - one drug stops or slows the action of a second drug.

- cyp450 system- can be used on purpose

- HIV meds: ritonavir inhibits metabolism of lopinavir so the second drug can be effective.

- Potentiation: similar meds have effects that add to each other- displacement is when two drugs are fighting for the same binding sites and only one can

win. this leads to a drug with a higher affinity for the site or higher serum levels to displace the lesser drug.

Different forms of meds and how fast into the system- Oral: swallowed, sublingual, buccal: 30 mins to and hour?- enternal: NG, gastric tubes, rectal:- Parental: SC, IM, IV, intrathecal, epidural:

- from slow to fast: ID, SC, IM, IV (IV is almost instantaneous in some cases) - Pulmonary: gas, mist:

- fast due to the large amount of capillaries - topical: local effect usually, must be lipid soluble.

Loading doses- initial dose that is larger than maintenance dose that brings the levels of the drug up to

the desired range.Duration of action and minimal effective concentration

- measurable action of the drug from the beginning to end- lowest serum levels that produce the desired effect.

BBB and drugs- the Blood-brain barrier is a barrier that is harder to pass through than normal endothelial

cells. this is due to the fatty sheath that covers the endothelial columns- only lipid soluble meds can pass through (also drugs that are compatible with specific

active transport site but this was not covered in class soooo) What is ADME?

- Absorption, Distribution, Metabolism, Excretion - This is all a part of pharmacokinetics

What is included in patient education?- How, when, why, how much, how long, for what reason, diet, when not to take it, side

effects, adverse effects, s/s of toxicity, when to notify HCP---Emergency care (Appendix T) of Davis Drug Guide for Nurses Appendix T.

- Early management of anaphylactic reactions1. Stop the administration of the drug2. Maintain airway: bronchodilators and Aminophylline may be needed to keep the

airways open in severe resp. distress.3. Administer epinephrine:

a. IM, SubQ; adults 0.3-0.5 mg q5-15 mins, Kiddos 0.01mg/kg or 0.1 q5-15 mins

b. IV: Adults 0.1mg over 5mins or 1-4 mcg/min infusion, Kiddos 0.01mg/kg or 0.1-0.2 mg over 5 mins q 30 mins, infusion 0.1-1.5 mcg max/ kg/min

4. Administer antihistamines: diphenhydramine (Benadryl) IM, IV: 50-100 mg initial, kiddos 5mg/kg/day divided into doses q6-8hr do not exceed 300mg/day (so child >15kg should not get the maximum dose)5. Support BP w/ fluids and vasopressors 6. Administer corticosteroids: hydrocortisone (Sulo-cortef) IV 100-1000mg mg followed by 7mg/kg/day IV for 1-2 days 7. Document the reaction in medical reaction and have the pt/family to carry ID

Side effects of anti-HTN meds and digoxin - Thiazides cause a shift of K out of the body causing Digoxin toxicity - Furosemide can cause ototoxicity - Spironolactone (K sparing diuretic) will increase the half life of digoxin

---Inotrope, chronotrope, dromotrope - Cardiac drug effects- inotropic ↑ contractility - Chronotropic ↑ HR- dromotropic ↑ conduction velocity of the heart

Selecting a BP medication - Step I: A diuretic, calcium channel blocker, or ACE inhibitor - Step II: increase dose of the first med, or ad another- Step III: Pick another drug from a different class

- Step IV: Add another one or two meds, three or four total. ---Labs and HTN meds

- Labs:- Urinalysis for kidney function, lipid panel, electrolytes, Basic metabolic panel

- Meds: Beta blockers, ACE inhibitors, Diuretics

Bibliography

Deglin, J., Vallerand, A., & Sanoski, C. (2015). Davis's drug guide for nurses (14th ed.). Philadelphia, Pennsylvania: F.A. Davis.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. (2015, September 1). Pharmacokinetics & Pharmacodynamics. Lecture presented in Anschutz Medical campus, Aurora.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. (2015, September 8). Antihypertensives and Diuretics. Lecture presented in Anschutz Medical campus, Aurora.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. Nino, T. (2015, September 15). Respretory Pharmacology Fall 2015 Updates. Lecture presented in Anschutz Medical campus, Aurora.

Meds:Drugs listed in the test by Name/Family

ACE inhibitors, -pril, Angiotensin converting enzyme inhibitors- captopril (Capoten) PO 12.5-25mg 2-3 times per day- Action

- Decrease BP- Decrease vascular tone- Inhibit RAAS system

- Stops angiotensin I from converting to angiotensin II(a vasoconstrictor)- reduces the amount of aldosterone in the body

- Report Chest pain to HCP- Take BP before administration, Monitor I’s & O’s, look for signs of CHF and angioedema

Acetylcysteine (mucomyst): Mucolytic - PO 140mg/kg, then 70mg/kg q4hr- Action: Decreases viscosity of mucus to expectorate

- inhaled through nebulizer - DX that need this are COPD and cystic fibrosis- Onset > 1 min Peak 5-10 min

- Bad odor- side effects are runny nose, throat and lung irritation, rash and stomatitis

Albuterol: Bronchodilator Beta2-Agonist- Action: relaxes smooth muscle in the bronchioles by binding to the Beta2 adrenergic

receptors- used in asthma or COPD- side effects are not common but increase in sympathetic nervous system(nervous,

tremors, hyperactivity, headache), and chest pn, palpitations, angina, arrhythmias, hypertension.

- Spacer doubles the effective dose- These are used before the steroid inhalers to increase the area that the second

medication can affect. - Wait one minute between doses, and rinse out mouth afterward to avoid THRUSH

Anithistamines H1 antagonists - Generations:

- Gen 1: Diphenhydramine (Benadryl)causes sedation and crosses the blood brain barrier

- Gen 2: Loratadine (Claritin) is non sedating

- Action: binds H1 sites and blocks the effects of histamines, Also binds Ach (muscarinic) receptors

- Routes: IV, PO, Nasal, Topical- effects:

- peripheral: decreased itching, pain, flushing, mucus secretions - CNS: depression is the therapeutic effect and excitement is the over dose effect.

- Caution: anti-cholinergic side effects, use with caution in patients with glaucoma, hyperthyroidism (tachycardia), HTN or BPH/urinary retention

- Sedation: do not take with ETOH, no driving - Children: some become hyperactive—unpredictable - Drug interactions: CNS effects with ETOH, hypnotics, antipsychotics, anxiolytics,

narcotics - Anticholinergic effects: antipsychotics, TCAs

ARBs Angiotensin II receptor blocker - losartan (Cozaar)

- Management of HTN, and CHF in people that cannot take ACE inhibitors- Disables Raas system, by blocking the receptor for angiotensin II

- Assess for signs of CHF and angioedema - more specific than ACE inhibitors, - Action - smooth muscle dilation to reduce BP, reduce salt and H2O in body- Retains less K than ACE

Atropine(Lomotil): antidiarrheals

- treatment of chronic diarrhea often caused by inflammatory bowel disease - Action: inhibits GI motility and peristalsis, by direct nerve effect on the muscle wall

- decrease the loss of fluid and electrolytes - side effects: Anticholinergic effects Drowsiness, dizziness, nervousness, constipation,

abdominal pain, distention, discomfort, dry mouth, nausea, vomiting, ileus “hot as a hare, dry as a bone,red as a beet, mad as a hatter, and blind as a bat”

Beta 2 agonists (albuterol)- Action: relaxes smooth muscle in the bronchioles by binding to the Beta2 adrenergic

receptors- used in asthma or COPD- side effects are not common but increase in sympathetic nervous system(nervous,

tremors, hyperactivity, headache), and chest pn, palpitations, angina, arrhythmias, hypertension.

- Spacer doubles the effective dose- These are used before the steroid inhalers to increase the area that the second

medication can affect. - Wait one minute between doses, and rinse out mouth afterward to avoid THRUSH

Beta blockers metoprolol (Lopressor) - Antihypertensives, antiarrhythmics- treatment of HTN, prevention of MI and decrease of mortality in people that have had an

MI- Blocks the stimulation of beta1-adrenergic receptors- side effects: Bradycardia, CHF, pulmonary edema- teach the pt to call HCP if slow HR or Dyspnea occurs

Calcium Salts: Ca carbonate, Ca gluconate, Ca Citrate, Ca Acetate- electrolyte replacement supplement, Acid buffer/ electrolyte - treat osteoporosis, antacid, treat electrolyte imbalance - activates nerve impulses of muscle, buffers acid, essential for bone formation- Side effects: cardiac arrest through IV therapy, arrhythmias, bradycardia- monitor BP pulse and ECG frequently

Calcium channel blockers: verapamil (Calan)- Antihypertensive agent, antiarrhythmic agent, - treat HTN, angina, arrhythmias - inhibits the transport of calcium into muscles (cardiac muscles are the most

delicate/important) - this makes the excitation of the muscle inhibited or blocked

- side effects: arrhythmias, CHF, peripheral edema, bradycardia, chest pain, hypotension, palpitations, syncope, tachycardia

----------------Chlorpheniramine (Chlor-Trimeton)- antihistamine, antitussive- Like benadryl but non drowsy- treats s/s not the cause of the problem

----------CodeineCorticosteroids

Cromolyn sodium (Intal) ----------DextromethorphanDigoxin---------Digoxin Immune FabEnalaprilEpinephrine-Ethambutol-Furosemide (Lasix)Guiafenesen (Mucinex)Hydroclorothiazide (HCTZ)Ipratropium-Isoniazid-Lisinopril-Leukotriene inhibitors-Loratadine (Claritin)-----Mannitol------Methyldopa-Montelukast (Singulair)Order of giving inhalation medsOTC cold medsPotassiumPotassium supplements-------Propranolol (Inderal)--------Pseudoephedrine-Pyrazinamide-Rifampin-Salmeterol-Spironolactone (Aldactone)--------Steroids--------Zinc for colds

Deglin, J., Vallerand, A., & Sanoski, C. (2015). Davis's drug guide for nurses (14th ed.). Philadelphia, Pennsylvania: F.A. Davis.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. (2015, September 1). Pharmacokinetics & Pharmacodynamics. Lecture presented in Anschutz Medical campus, Aurora.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. (2015, September 8). Antihypertensives and Diuretics. Lecture presented in Anschutz Medical campus, Aurora.

Robinson PhD, FNP, M., & Gilbert DNP ARNP-BC, M. Nino, T. (2015, September 15). Respretory Pharmacology Fall 2015 Updates. Lecture presented in Anschutz Medical campus, Aurora.

ACE Inhibitor - Angiotensin converting enzyme inhibitors

- stops RAAS system stop hypertension- step 1 for HTN meds- African population tend to respond poorly to ACE inhibitors

adenosine (Adenocard)

- slows AV node conduction- for PSVT Paroxysmal supraventricular tachycardia- rate of delivery is over 3 seconds by an MD, Very unique

Alpha blocker - Block the Alpha receptors which cause vessels to dilate

- Lower BP

alprazolam (Xanax) - Anti anxiety

- schedule IV, pregnancy class D- S/E: Dizzy, Lethargy, Drowsiness, CNS depression- grapefruit increases increases effects and the measurable levels of the drug

amiodarone (Cordarone) - Group III K channel blockers: delay repolarization - delays ventricular repol at qt- prolongs action potential- increases effective refractory period- Pulmonary toxicity- grapefruit interaction- Side effects: thyroid issues, blue grey skin, - D/D interactions: increase effect Digoxin, anticoags, statins, dilantin- life threatening dysrhythmias

Angiotensin Receptor Blocker - for HTN - blocks angiotensin II receptor from binding and causing vasoconstriction- ex.

- Losartan (Cozaar)- Actions - more specific than ACE

Antacids

Antacids that can be bought over the counter (the goal is to bring pH of the stomach to about 3.5): Tums, Caltrate, OsCal, Viactiv(not w/ coumadin), Citracal (not w/ KD)● Action: increase stomach pH

● indications: Peptic ulcer, GERD, hernia

● ADME:

● onset: 20-40 min (give 1-3hr before meal + night)● not meant to absorb, just buffer the acid● excreted in the feces

● reduces Absorption of other drugs (chelation) due to the raise in

stomach pH

● S/E: constipation, bone deg, increased acid secretion, Kidney failure,

Diarrhea

● increased Ca, K and NA, decreased Mg● Kidney failure in chronic use

Antibiotics - used to treat H.pylori with bismuth and proton pump inhibitors

- lasts for 2, and then the Antibiotics and bismuth drop off and the PPI is prescribed for 4 more weeks, about 90% of people are recovered after this treatment.

- antibiotic- induced Diarrhea for the elimination of C. diff with the antibiotic fidaxomicin (Dificid)

antidysrhythmic drugs Antidysrhythmic drug classes or group (listen to heart for 1 min)

● I – quck Na channel blockers (broken up into three classes, but do not need to know that

for the test

○ Ia - quinidine

■ procainamide (more side effects)

○ Ib - lidocaine

○ Ic - flecainide

● II – Beta Blockers

○ Propanolol

○ metoprolol

● III – K channel blockers

○ Amiodarone

● IV – Ca channel blockers

○ Verapamil

○ Dilitiazem

● V - variable mechanism

○ Adenosine

○ Digoxin

○ Magnesium sulfate

Antiemetics - Action: Block CTZ (chemoreceptor trigger zone)

- relieve nausea and vomiting- Anticholinergic: Scopolamine (Transderm-Scop)

- for motion sickness- Side effects: Blurred vision, dry mouth and CNS depression

- Antihistamines

- Diphenhydramine (Benadryl)- Dimenhydrinate (Dramamine)

- H1 blocker (antihistamine), CNS depression- Phenothiazine:

- Prochlorperazine (compazine)- similar to atropine

- Dopamine receptor blocker

- Metoclopramide (Reglan)- Drousie, extrapyramidal effects, Diarrhea

- Cannabinoid

- Dronabinol (Marinol)- Made from THC

Anti-inflammatory- NSAID’s- Steriods- C-reactive protein levels reflect inflammation

- high levels associated w/ increased risk of CV problemsAntiseasickness pills Antiemetics will help, but not all.

● Action: Block CTZ (chemoreceptor trigger zone)

● relieve nausea and vomiting● Anticholinergic: Scopolamine (Transderm-Scop)

● for motion sickness● Side effects: Blurred vision, dry mouth and CNS depression

● Antihistamines

● Diphenhydramine (Benadryl)● Dimenhydrinate (Dramamine)

● H1 blocker (antihistamine), CNS depression

Atorvastatin (Lipitor) - Class: HMG-CoA reductase inhibitors

- Action:block the synthesis of cholesterol - inhibits HMG-CoA reductase: so the pathway for cholesterol synthesis is

blocked.- Indications: Hypercholesterolaemia, Coronary heart disease, Stroke, MI and

chest pain- S/E: Rhabdomyolysis (ask about muscle pain and tell the patient to report any

pain or weakness), Angioneurotic edema- stronger than simvastatin, not as strong and Rosuvastatin

Atropine - Anticholinergic/antiarrhythmic

- Action: blocks vagal stimulation, which increases (HR) SNS- blocks Acetylcholine at prostaglandin sites

- Tachy arrhythmias, Pulmonary edema, physostigmine is the antidote for an OD- side effects: red as a beet, mad as a hatter, hot as a hare,

Benzodiazepine drugs - for insomnia, anxiety, seizures, alcohol withdrawals

- for acute use not chronic (does not cure Dx, can develop tolerance and dependence)

- 14 days tops- schedule IV (most) - may be related - patho: increases the effect of GABA, calming, sedative

- GABA receptors are dense in the limbic system, which messes with your emotions

- abnormal non-REM sleep- BZ1 receptor: cerebellum: controls anxiety- BZ2 receptor: basal ganglia, and hippocampus: MM relaxation

- side effects and interactions: Smoking decreases effectiveness, parental rout can cause cardiovascular issues and must adhere strictly to the rate, hypotension depression of RR(with IV), and CNS, Pregnancy risks.

- IV, give slowly, needs to be monitored - make resp issues worse

- will not cure, or meant to cure the symptoms- used for conscious sedation (colonoscopy)- Withdrawal: starts in 1 to 3 days and peaks in 1 to 2 weeks (depends if short or

long acting drug) - weight loss, anxiety, weakness, insomnia, and tremors

- ex: diazepam (Valium), - used for: Calms a person down so they don’t puke as much before

chemo, alcohol withdrawal- the metabolites can collect over time and cause CNS depression

- Resp. ↓ and hypotension- when given IV the vessel gets irritated

- burns in IV so dilute or slow down the rate of admin- #1 drug in the US

- ex: lorazepam (Ativan) - similar to diazepam- for status epilepticus- dosing too fast can lead to bradycardia, RR depression, and apnea

about 2 mg/minBeta blockers

● reduces heart rate and force of contraction and therefore O2 demand

● long term only

● makes vasospastic angina worse (prinzmetal)

● Non-selective – decrease Cardiac contractility, drops bp and renin release

○ HTN, tachycardia, and angina● Some are more lipid soluble and more water soluble

● Education – don’t change the regimen

○ OTC cold meds with pseudoephedrine/ phenylephrine○ HR <45 don’t give○ orthostatic hypotension

● don’t stop the regime or the opposite effects happen, HTN, rapid HR

Bile acid sequestrants ● Colesevelam (Welchol)

● binds bile acid so it cannot reabsorb● does not decrease vitamin absorption and not many other meds● Not absorbed● for hyperlipidemia and high LDL● take with lots of fluids

● cholestyramine (Questran)

● Binds bile so it cannot be reabsorbed● used with statins● take with lots of fluids

Bismuth subsalicylate (Pepto-Bismol) - Antidiarrheal

- promotes absorption in the intestines to decrease diarrhea - bismuth is not absorbed, subsalicylate is - S/E constipation, grey stool, - OTC- if taken with ASA increases toxicity risk

Bulk-laxatives psyllium (metamucil)

● encreases stool size and softens by absorbing water, this increases the size of the

bolus and pushes against the wall of the intestine to stimulate peristalsis

● takes 12hr -3 days work

● excreted in stool

● NEED fluid for it to work!

Calcium carbonate (TUMS) ● Action: increase stomach pH

● indications: Peptic ulcer, GERD, hernia

● ADME:

● onset: 20-40 min (give 1-3hr before meal + night)● not meant to absorb, just buffer the acid● excreted in the feces

● reduces Absorption of other drugs (chelation) due to the raise in

stomach pH

● S/E: constipation, bone deg, increased acid secretion, Kidney failure,

Diarrhea

● increased Ca, K and NA, decreased Mg● Kidney failure in chronic use

CCBs - Diltiazem (Cardizem)- Verapamil (Calan)- Calcium channel blockers

- used in stable vasospastic angina, Arrhythmias, HTN- Slows HR

Cimetidine (Tagamet) - Peptic ulcer Drug

● Acid-Neutralizing Drugs

● H2 receptor blocker

digoxin – positive inotropic, negative chronotrope, neg dromotrope

● increased cardiac contractility

● decreased conduction

● indications: CHF, AFIB

● use loading doses

● SE: bradycardia, av block, anorexia, vision issues, green- yellow tint, halo around

lights, gynecomastia with long term use.

dopamine (Intropin) ● catecholamine (sympathomimetic)

● increase BP, CO, vasoconstriction (B1, A2)● Very toxic to tissues● need large bore IV● For Cardiogenic shock primarily and vasoconstriction (neurogenic shock)

epinephrine - catecholamine (sympathomimetic)- Bronchodilation, vasoconstriction

● A1, vaso constriction

● Beta1, increase BP

● can have a paradoxical bronchospasm

Eszopiclone (Lunesta) - Benzo-like drug

- for sleep only, not anxiety- for increasing the duration of sleep - S/E sleepwalking, driving and such

- Bitter after taste Flumazenil

- Benzo antagonist - no effect on a person not on a benzodiazepine - antidote for benzo OD or excessive effect- short half life so it is given through a drip or multiple IVP- S/E: hypotension, decreased respers, and cardiac arrest

H2 Blockers ● Cimetidine (tagamet)

● ranitidine (Zantac) fewer side effects and strogerew

● Better value to prevent ulcer than PPI● Action: Lowers H2 secretion by stopping histamine from stimulating H2

receptors● Prevents PUD, acid reflux, hypersecretion

IV fluids

Lactulose - Osmotic Laxatives

- and milk of magnesia

● sugar, and salt that don’t absorb well and then attract water to induce peristalsis.

● ↓serum Ammonia in people with chronic liver disease● works in 1-3 days and not much is absorbed into the body

Lidocaine (Xylocaine)- Group IB Na channel blockers

● ↓ depol of mm contraction (decreases the time of action potential)

● monitor on EKG● works first on the tissues with the issues● for Ventricular dysrhythmias acutely ● narrow therapeutic range

● the maximum dose is 3mg/kg● Side effects – CARDIAC ARREST, confusion, tremors, twitching, blurry

vision, tinnitus, dizziness, fainting, Bradycardia● D/D interactions with propranolol and cimetidine increase the drug levels

Lovastatin (Mevacor) ● HMG-CoA reductase inhibitors

● Stops the pathway for the synthesis of cholesterol

● for hyperlipidemia when diet is not enough● Side effects: MYALGIA, can lead to mm damage, Kidney injury

● more risky when taken w/ niacin or gemfibrozil● Grapefruit interaction, increase the level of the med

Melatonin - remelton (Rozerem)

- activates melatonin receptors - hypnotic, for falling asleep- effect in 30mins, ok for chronic use- no dependence symptoms when stopped- safe for long term use

Metoclopramide ( Reglan)Dopamine receptor blocker

● gastric stimulant

● Drousie, extrapyramidal effects, Diarrhea● S/E: Gynecomastia, bone marrow suppression

Misoprostol (Cytotec)- Prostaglandin

- cytoprotective agent

- PG E1 analog – ↓Acid secretion, ↑ Bicarb (HCO3) and mucus

secretion

- Category X, miscarriage- Prevents NSAID ulcers

Mylanta or Maalox liquids

- Aluminum and magnesium antacid - neutralizes acid in the stomach increasing pH- may affect absorption of some drugs and foods

Narcan- Opiate Antagonist

- Antidote for opiates- reverses the CNS and Respiratory effects of opioids

- S/E V. fibNiacin

- nicotinic agent, lipid lowering agent- coenzymes for lipid metabolism- increased risk of myopathy with Statins - Flushing occurs- Vitamin B 3

Nitrates

Nitroglycerin SL, ointment, patch (NTG)- Organic Nitrate Vasodilators

- nitroglycerin- both short and long term- vasodilates peripheral and coronary arteries

- does not dilate the atherosclerotic vessels (so the elderly may not respond well)

- Hypotension Fall risk- will get a headache and that’s OK- taken sublingual(minutes), ointment (half hour to hour and can

cause tolerance)- wear gloves when applying the patch to avoid headache

● Use for chest pain emergency

● one SL wait 5mins● if after second dose pain is still happening call 911● take no more than 3 doses

● Capsules● sustained release

● Ointment● apply to hairless chest wall and cover with plastic

● transdermal patch● don’t soak in water

● rotate placement of patch

● 10-12 hr time w/out patch

● D/D interactions: any hypertension meds

● nicotine● Phosphodiesterase

● Light and heat will break down the drug and make it ineffective● Others for chronic angina

● Beta blockers● reduces heart rate and force of contraction and therefore O2

demand● long term only● makes vasospastic angina worse (prinzmetal)

● Calcium channel blockers● used in stable vasospastic angina

NSAIDs- Non steroidal anti inflammatory

- Ibuprofen, ASA, acetaminophen - can cause ulcers

- misoprostol and sucralfate can prevent these ulcersOmega 3 fatty acids

● fish oil● RX is Lovaza● not complete evidence in: dementia, Diabetes

Omeprasole (Prilosec)- Proton pump inhibitor

● better at repairing ulcers than H2 blocker

● Blocks acid secretion

● Blocks ATPase at the parietal cells that would produce H2● treats: esophagitis from GERD, Duodenal ulcer, long term HTN● quick onset, 2h to peak, and ends effectiveness at 3-4 days● Side effects are: Heartburn, weakness, dizziness, C.diff risk increases,

also cannot absorb Ca as efficiently● Ulcers can heal in a matter of weeks

Ondansteron (Zofran)● Block serotonin 5 HT3 receptors, antiemetic

○ D-D interaction with apomorphine causing hypotension

○ monitor EKG in patients with hypoK and Mg, HF, brady arrhythmias

○ can be hepatotoxic over 8mg for day

Osmotic laxatives● lactulose and milk of magnesia

● sugar, and salt that don’t absorb well and then attract water to induce peristalsis.

● ↓serum Ammonia in people with chronic liver disease● works in 1-3 days and not much is absorbed into the body

● polyethylene glycol (Golytely) (Glycerin sup in children)

● draws water into intestine (sugar, salt, and PEG)● Cleansing before colonoscopy● (Other) metoclopramide (Reglan)

● ↑ ACH, stim PSNS

● ↑secretions, and motility

● for GERD, risk of ileus, and to eliminate barium

● Contra indicated in patient with intestinal blockage

Oxygen

Pancreatic enzymes (Prancrelipase)● ind: Pancreas insufficiency (pancreatitis, cystic fibrosis, Pancreatectomy)● Act: increased digestion in GI (enzymatic)● Enteric coated● S/E all abdominal, Fibrosing● hold if NPO, give before meals (dose based on calories)

Phenobarbital- Barbiturate- patho: increases the effect of GABA, calming, sedative- used in addition to anesthesia- for insomnia, seizures, anxiety (acutely) - develop tolerance to the therapeutic effect, but not to the side effects

- liver makes more enzymes to break down the drug, and lowers the therapeutic half life.

- used to treat neonatal kiddos to use this increased metabolic effect w/ hyperbilirubinemia.

- S/E: ↓ CNS, cardiovascular function, and RR. - hangover, porphyria (werewolf?), suicide

- withdrawal: seizures (if they have epilepsy), anorexia, weakness, chills, poor sleep

- This is called abstinence syndrome Phenothiazine antiemetics

- Prochlorperazine (compazine)- antiemetic- management of nausea and vom. - depresses the CTZ, changes the effect of dopamine - S/E: Neuroleptic malignant syndrome, and med leads to Reye’s syndrome in kids

younger than 16- dry eyes and mouth, pink or reddish brown urine, agranulocytosis

● similar to atropine

Phenytoin (Dylantin)- For tonic clonic seizures

- blocks Na channels selectively- take often (tid)- low therapeutic index

- half life is variable even in the same patient: 8-60 hr- S/E: gingival hyperplasia, CV effects, cognition issues, steven johnson

syndrome and toxic epidermal necrolysis (like being burned inside out)- screws up Vitamins: deficiencies Folic acid, D and k

Pravastatin (Pravachol)- HMG-CoA reductase inhibitor, lipid lowering agent

- Blocks synthesis of cholesterol - additive med for the prevention of CV disease in people that already have CHD- S/E: Rhabdomyolysis, - least impactful to most impactful

- Lova-, Prava-, Simva-, Atorva-, Rosuva-- rosuvastatin newest, strongest, most side effects- HDL changes start at simvastatin

Promethazine (Phenergan)- Antiemetic

- CTZ depression, changes the effect of dopamine - S/E: agranulocytosis, neuroleptic malignant syndrome

- dry eyes and mouth, blurry vision, and constipation Propranolol

● propranolol(only one that is not beta 1 selective), acebutolol, esmolol, sotalol

● Decreases contractility, automaticity in SA, and slows conduction● cardioprotective for post MI and HF? this is now uncertain, and may not be

true● slows conduction, HR, renin, BP,● increases cardiac output

Proton Pump Inhibitors (PPIs)omeprazole (Prilosec) -prazole

● better at repairing ulcers than H2 blocker

● Blocks acid secretion

● Blocks ATPase at the parietal cells that would produce H2● treats: esophagitis from GERD, Duodenal ulcer, long term HTN● quick onset, 2h to peak, and ends effectiveness at 3-4 days● Side effects are: Heartburn, weakness, dizziness, C.diff risk increases,

also cannot absorb Ca as efficiently● Ulcers can heal in a matter of weeks

Ramelteon (Rozerem)- Hypnotic

- melatonin agonist (activates receptors)- for insomnia, works in 30mins - more selective and effective than supplement of melatonin- D/D interactions: Fluvoxamine, Liver Dx’s, and alcohol- S/E: basically getting too sleepy, also amenorrhea -

Ranitidine (Zantac)ranitidine (Zantac) fewer side effects and strogerew

- H2 receptor blocker● Better value to prevent ulcer than PPI

● Action: Lowers H2 secretion by stopping histamine from stimulating H2

receptors

● Prevents PUD, acid reflux, hypersecretion

Rosuvastatin (Crestor)- Strongest Statin

- this means that it also has the most severe side effects - HMG-CoA reductase inhibitors

Sildenafil (Viagra)- erectile dysfunction and vasodilation

- can treat pulmonary artery HTN- contraindicated use with Nitrates (nitroglycerin)

- causes hypotension - S/E: MI, hepatic toxicity

Sodium Nitroprusside (Nipride)- vasodilation

- breaks down into Nitrous oxide

Statins● HMG-CoA reductase inhibitors

● Not all statins are alike

● least impactful to most impactful● Lova-, Prava-, Simva-, Atorva-, Rosuva-● rosuvastatin newest, strongest, most side effects● HDL changes start at simvastatin

Stimulant laxativesbisacodyl (Dulcolax)

● stimulate peristalsis by affecting the muscle and mucus secreting cells

● works in 6-8hr

● can cause fluid loss (watery discharge), cramping, and dependence

Stool softeners- Docusate sodium

- absorbent, water is pulled into fecal matter- causes the retention of water and electrolytes not letting them be absorbed into

the body- takes 12 hours to 3 days-

Sucralfate (Carafate)- anti ulceral, GI protectant

● Protects ulcer by forming a barrier with the ulcer cells from acid in the

stomach.

● For PUD, and protect other ulcers from forming. (NSAID’s)

Tetanus- Caused muscle spasms including high HR and HTN

- vaccination is Tdap

Zaleplon (Sonata)- Benzo-like drug

- for sleep only, not anxiety- for falling asleep- S/E: sleepwalking, driving and such- rebound insomnia after tolerance is built over a time of longer than a week- Motor Paralysis “locked in”

Zolpidem (Ambien)- Benzo-like drug

- for sleep only, not anxiety- for falling asleep and asleep and staying asleep - S/E: sleepwalking, driving and such- rebound insomnia after tolerance is built over a time of longer than a week

Hints Sheet Exam #3 – NURS 3150 Pharmacology

Anesthesia and analgesia

- Acetaminophen (Tylenol)- anti-prostaglandin- metabolized in liver (watch out for this)

- 3 g per day is the most dose per day- works in CNS- low GI irritation- can be used with kids- s/e: liver damage with ETOH is a high risk,- toxicity: 25 grams for adult

- top cause of acute liver failure- the OD patient will die in 3-5 days from the liver damage

- Acetylsalicylic acid Aspirin (ASA) – COX 1- gen 1 NSAID- inhibits platelet aggregation until there is a reproduction of more

platelets- irreversible in the platelets that it affects

- anti prostaglandin (inflammation)- do not use in kiddos- s/e: salicylism (ringing in ears points towards OD), reye’s syndrome,

Renal impairment- Too Much? Tinnitus, respiratory depression, HypERthermia, can

cause metabolic acidosis, then resp alkalosis to compensate.- COX inhibitors

- COX 1: promotes Platelet aggregation, GI protection, renal fxn, (GOOD)

- COX 2: promote inflammation (bad)- Anticholinergics

- Can be used in pre anesthesia to reduce secretions- “Caine” drugs for numbing

- local anesthesia

- for: fingers, ears, nose, toes, and those- Codeine

- Narcotic- *1/10th power of morphine- 5x power of aspirin, or acetaminophen

- Epinephrine with Lidocaine- keeps the lidocaine local due to the vasoconstrictive properties of epi

- Celecoxib (Celebrex) – COX 2 - similar strength to ibuprofen- less stomach ulcers than other NSAIDs (some evidence)

- Fentanyl- narcotic- **one hundred times stronger than morphine- Lollipop form in some cases for chronic pain (cancer)

- will kill a kiddo!- -fluranes

- Isoflurane- Strong anesthetic

- weak analgesic - Volatile liquids mixes with O2 and inhaled- Resp depression, HYPOtension, arrhythmias, Hyperthermia- ***can be mixed with Nitrous oxide

- for the strong analgesic properties - allows for a lower amount of each inhalant to get the desired effect, which

lowers the risk for depression of resp. and the heart- Ibuprofen (Motrin, Advil) – COX 1

- S/E: can cause renal damage, and GI bleeding, Retention of NA and H2O (watch out for HF patients)

- Inhaled anesthetic agents- Works very quickly

- IV anesthesia agents - lasts longer than inhaled

- Methadone- narcotic- longest duration of action- long QT interval- for coming off of narcotics and given in clinics

- Meperidine (Demerol)- narcotic- same action as morphine with a shorter action- treats post anesthesia shivers or rigors that can occur- no cough suppression effect

- Morphine- narcotic

- moderate to severe pain- can be given through almost all routes- cross BBB- S/E: resp depression, constipation, nausea, Miosis(pinpoint

pupils)- morpheus god of sleep

- give before the pain occurs if possible- PCA pump allows for the patient to not fall out of the TPR

- is better than PRN, or fixed schedule- decreases overdose- can use smaller doses- empowers patient

- cross tolerance to other opiates- Naloxone (Narcan)

- opiate antidote- also given when there is an OD of unknown cause

- NSAIDS- gen 1: inhibit COX one and two

- inhibit inflammation- inhibits prostaglandins in the stomach, so there is a higher

chance for ulcers- Gen 2:- some studies show slowed healing of muscle, bone and ligament

injuries.- Propofol

- Anesthetic- rapid onset and short duration- no analgesic effect- s/e: resp depression, rhabdo

- Tramadol (Ultram)- Non opiate CNS acting analgesic- schedule 4- not an opiate but binds to the receptor

- Pyridium (Phenazopyridine)- Treats pain from lower UTI’s- do not take if the pt has DM, or liver Dx- can cause a bright red or orange urine,take with food or there may be a

Headache after dose- OTC

HA and migraines

All of these drugs vaso constrict except the beta blockers and CCB. OTC is the most effective, and Ergot is not prescribed often

- Beta-blockers and Calcium Channel Blockers- are prophylactic and chronically dilate and cause the vessels to be less spastic

- Ergot Alkaloid- Ergotamine

- for prophylaxis of migraines, - Alpha blocker vasoCONstriction - Rebound HA- S/E: HTN, MI trigger- increased risk of stillborn pregnancy increased uterine stim, and

decreases the blood flow to the placenta

- separate 24hrs between the use of ergotamine and sumatriptan.- related to ACID

- Excedrin Migraine - OTC- one of the best if not the best remedy for HA and migraines- formulation: ASA, ibuprofen, and some caffeine - basic and effective

- Triptans- Serotonergic - sumatriptan and zolmitriptan- stim 5 – HT in the brain- it vasoconstricts and inhibits inflammation- not for prophylaxis of migraines only treat - S/E: stroke, MI, cerebral hemorrhage- WAIT 2 weeks to use a MAO-I med- DON’T take within 24 hours of ergotamine

- toxicity w/ other 5-ht blockers, prozac,paxil, zoloftParkinson'stoo much ACH and not enough DA causing dyskinesia and Akinesia. Drugs do not cure but only slow the decline of symptoms, and treat the Bradykinesia, Gait, and improve daily activities. Comes from the degeneration in the extrapyramidal system which controls posture and gait (and others)

- Anticholinergic- reduce ACH to bring balance to the Dopamine/ACH teeter totter- Benzotropine (Cogentin) and trihexyphenidyl (Artane)

- similar to atropine, antimuscarinic - Dopaminergic

- MAO-B inhibitors are used in patients with mild symptoms- Selegiline and rasagiline

- inhibit DA breakdown - when the symptoms are increased, given meds change to levodopa and

Dopamine agonist- S/E: drooling, constipation

- Levodopa- DA prodrug - best effect in the first two years- take time off the drug “holiday”- many d/d interactions- vitamin B6 allows less levodopa to get to the CNS

- Carbidopa- no bad effects on its own- increase usable levels of levodopa in the CNS

- Is the CAR that drives levodopa to the CNS- COMT inhibitors:

- blocks breakdown of Levodopa- Entacapone, and Tolcapone

- CAPONE “protects” levodopa, like the mob- Levodopa/Carbidopa (Sinemet)- Levodopa/Carbidopa/Entacapone (Stalevo)

- increase TP effects by stopping the breakdown of Levodopa

- more convenient than taking 3 pills- Pramipexole (Mirapex)

- dopamine agonist- first given alone in early parkinson’s then added to Levodopa in late. - S/E: sexy grandpa/grandma

- MAO Inhibitors - 2 kinds

- MAOA helps metabolize norepinephrine and serotonin- MAOB metabolizes dopamine

- Selegiline (Eldepryl) inhibits this so DA is not metabolized.

- food interactions: aged cheeses and meats, yeast, bread, BEER

- stop antidepressants 2-7 weeks befor using- Selegiline

- MAOI- look MAOI’s- many s/e and dd interactions

- Tricyclic antidepressants (Amitriptyline) - Are the only antidepressants that should be used in PA- Do not use is ALZ

- blocks ACHAlzheimers progression can only be slowed not cured. Medicine is creating new treatments, and there is a link to chromosome 21 (like in down’s). Tangles in the brain may be related to cholesterol so statins may be useful for prophylaxis. Know the lifestyle risk factors: low activity and education, smoking, DM, HTN, depression.

- Memantine (Namenda) NMDA antagonist- Regulates calcium influx into the neuron- Indication is moderate to severe AD, but some neurologists start it early with

Aricept- SE: dizzy, HA, confusion, constipation, hallucination

- donepezil (Aricept) Acetylcholinesterase inhibitors - stop ACHesterase, increasing ACH- treatment of early dementia

Antimicrobials

- Antivirals

- Acyclovir (Zocirax)- similar to a purine nucleoside, and suppresses protein synthesis- S/E: phlebitis, nephrotoxic, stinging sensations.

- Flu drugs:- Amantadine- Oseltamivir (Tamiflu)

- Interferon alpha-2b

- For hep B, also C if combined with Ribavirin and a PI - causes flu like symptoms, and Hep causes flu like symptoms….

- Ribavirin- Treats hep C with pegylated interferon-Alpha and a PI

- HIV drugs- Reverse transcriptase, protease, and integrase are main targets of

treatment to disrupt the virus.- HAART therapy – highly active antiretroviral therapy. two nucleoside

reverse transcriptase inhibitors, and a protease inhibitor.- six classes of drugs to treat HIV

- Non-nucleoside reverse transcriptase inhibitors (NNRTIs) Nucleoside reverse transcriptase inhibitors (NRTIs) Protease inhibitors (PIs) Fusion inhibitors, CCR5 antagonists or entry inhibitors (CCR5s) Integrase strand transfer inhibitors (INSTIs)

- focus on the first three plus the fusion inhibitors- examples

- NRTI: Zidovudine (Retrovir)- stops replication, slows the Dx, and

increases the white blood cell (CD4) levels- Two of these are in the First set of Meds

given along with on of the following: INSTI, NNRTI, or PI

- NNRTI: Nevirapine (Viramune) Efavirenz (sustiva)- binds reverse transcriptase and stops the

transcription- Can be a part of the first line of meds along

with two NRTI’s- PI: Indinavir (Crixivan)

- very effective- Can be a part of the first line of meds along

with two NRTI’s- FI: Fuzeon, T-20

- fusion inhibitors - stops HIV envelope from fusing with a CD4

cell membrane. - INSTI (HIV)- Integrase strand transfer inhibitors

- Can be a part of the first line of meds along with two NRTI’s

- CCR5 Antagonist (HIV) - Maraviroc (selzentry)- Entry inhibitors- Blocks HIV from binding to the CD4 cell

(similar to the FI) - Can have an allergic rxn, cough, nausea,

dizzy

- Antibiotics

- Aminoglycosides- Inhibit protein synthesis and are bactericidal - Causes injury to the inner ear and Kidneys

- Nephro, and Ototoxic that is permanent

- Narrow spectrum - draw drug levels

- Peak thirty minutes after IV- Trough an hour before the next dose- given once a day

- Amoxicillin - Broad spectrum - Aminopenicillins - disrupt cell wall with beta lactam ring- Amoxicillin and Clavulanic acid is Augmentin

- This increases the effectiveness by breaking down the PenASE enzyme

- Antibiotic resistance - Bacteria can adapt to a drug and create defences from a drug such as the

PenicillinASE enzyme. - Carbapenems:

- Imipenem (primaxin)- broad spectrum- resistant to beta lactam break down (penASE resistant)- used in Pseudomonas aeruginosa- Superinfections are an adverse effect as well and an allergic RXN

- Cephalosporins - break down cell wall, for G+ and an increasing effectiveness with G-- bactericidal, and more resistant to PenASE than penicillin- spectrum broadens from gen 1 and 2 (narrow) to gen 3 and 4 are broad- ADME: poorly absorbed through PO route, no metabolism, excreted in

kidneys and stool- allergy in 10% of people w/ the pen allergy- four generations: they all have the Cef- or Ceph- prefix.

- Clindamycin- inhibits protein synthesis, Bacteriostatic - Narrow spectrum- Given with Tetracycline and Bactrim in MRSA - only for anaerobic infections such as in the gums, colon, sepsis

- not effective in the CNS- Can give orally (IM,IV as well)- S/E: pseudomembranous colitis severe bloody diarrhea, Hepatic and

renal toxicity, hypersensitivity- Erythromycin (macrolides)

- Broad spectrum- inhibits bacterial protein synthesis- use is allergic to penicillin- for G+- long QT interval- S/E: GI upset, cholestatic hepatitis, superinfection- D/D: interacts with CCB, HIV protease inhibitors, and antifungal increase

the serum levels of erythromycin- So HIV drugs and antifungals.

- Fluoroquinolones (Ciprofloxacin) Metronidazole (Flagyl)- Broad spectrum- inhibits DNA gyrase in bacteria

- Tendon rupture!!! do not give to kiddos under 18- undergo chelation just like tetracycline

- Gentamycin - Aminoglycoside, Inhibits protein synthesis - for G- serious (aerobic) infections - nephro and ototoxicity

- draw peak and trough levels to avoid toxicity

- Penicillins- bactericidal in gram positive bacteria- safe to humans b/c we do not have cell walls- D/D interactions with anticoags increase bleeding, contraceptives with

estrogen can cause PEN to no be effective- beta lactam ring weakens the cell wall

- beta lactamASE is used by some bacteria, breaks up the ring in the drug to make the drug ineffective

- unstable absorption when taken orally- very thick and viscous IM needs to be givin Z track. it is thick and a lot of

pressure is needed to administer.- few side effects, but 5% of the population has an allergic reaction- PenASE (beta lactamase) makes bacteria resistant to Penicillins- Classes of Pen. - Maybe just skim this, the individual drugs are not

on the review list. - Pen G

- Benzylpenicillin● narrow specturom, and sensitive to penASE● Bac-cidal to G+● prophylaxis in dental/invasive procedures

for endocarditis and syphilis● Dicloxacillin

● Narrow, PenASE resistant● Treat staph

● Aminopenicillins● Ampicillin, Amoxicillin (broad spectrum)● G+ and some G- are treated● S/E: rash and Diarrhea

● Extended spectrum Penicillins● Ticarcillin● Piperacillin● less important Carbenicillin indanyl, and mezlocillin

- Ampicillin and sulbactam is Unasyn- Amoxicillin and Clavulanic acid is Augmentin

- Sulfa drugs (sulfonamides) - Trimethoprim-Sulfamethoxazole (Bactrim)- Broad spectrum- inhibits folic acid to slow down growth

- folic acid is used in the synthesis of Nucleic acid (DNA RNA and other nucleic acid strands)

- (this is also why pregnant women should take folic acid supplements)

- collect urine sample before giving any antibiotic- used in UTI G+ or G-

- UTI is usually caused by e. coli- some elderly pts can have bacteria in the bladder

and be asymptomatic and done not necessarily need to be treated.

- Hypersensitivity reaction results in stevens- johnson syndrome- Bc it is a sulfa drug

- Tetracyclines - Broad spectrum- Inhibit protein synthesis - Effective through PO route- for acne, lyme Dx, H. pylori, Cholera, Riskettsia, cholera

- Can treat MRSA with Clindamycin, and Bactrim - chelation occurs when calcium, Iron, and magnesium

containing supplements and foods inactivate the tetracycline and cause it to be inactive

- do not take with meals!- one hour before or two hours after meals to avoid

chelation- S/E: photosensitivity, brown teeth, not ok for mothers pregnant

and breastfeeding moms, do not give to kiddos.- Vancomycin***

- inhibit Cell wall synthesis- most used antibiotic in the US- for severe G+ infections: MRSA, C diff, prophylaxis endocarditis- ADME: PO is ok with this drug, - S/E:**altered taste, OTOTOXICITY**, redneck syndrome if given

to quick IV

- Antifungals - Amphotericin B

- Broad spectrum - Cell wall/membrane permeability is disrupted

- humans have cell membranes… - binds -sterols which are also found in the human body

(cholesterol) which causes the renal damage.- it is very toxic

- used for SYSTEMIC mycoses that are potentially fatal, admin parentera/E: infusion reaction fever and chills, nephrotoxic

- ADME: can be found up to a year later in the pt body- Griseofulvin

- still in the -azole class- just for SUPERFICIAL (skin infections), not systemic- inhibits fungal mitosis- s/e: Insomnia, Rash and headache

- Ketoconazole - used in less severe fungal reactions (fungistatic) - MOA is it inhibits the synthesis of ergosterol which is a part of the fungal

cell membrane- this also affects the body’s sterols (sex hormones)

- -conazols are all less toxic- Mycostatin (Nystatin)

- Candidiasis only- It is in the form of a mouth wash- alters the permeability of the membrane- used for infant thrush often due to the low side effects.

Extras:

- alprazolam (Xanax)- Anti anxiety

- schedule IV, pregnancy class D- S/E: Dizzy, Lethargy, Drowsiness, CNS depression- grapefruit increases increases effects and the measurable levels of the

drug- Estrogens

- may increase risk of ALZ- inactivated with Gentamicin - contraceptives with estrogen can cause penicillin to be ineffective

- Food and meds - Antacids, Fe, Ca, and Mg Causes chelation in tetracyclines and

Fluoroquinolones all the previous + Alu, Zn, and sucralfate - Pre-op medication

- reduce the bad effects of anesthesia - Atropine

- Lomotil treats diarrhea from the use of anesthetics- also decreases secretions

- Baclofen- Anti-spastic- treats MM spasms from cerebral palsy, or Multiple sclerosis- Can cause seizures!- Increase CNS depression with opiates and MAO’s

- MAO’s with this can also cause HYPOtension- Preg category C

- Narcotics (pain), Benzos and barbs (anxiety), phenothiazines (nausea), MM relaxers

OD Reversal Drugs

- NARCAN- Opiate antidote

- given even if there is an OD of unknown cause- Flumazenil

- Antidote for benzos- Amyl Nitrate

- For Chest pain- cyanide antidote

- Ipecac- To Puke- mallory weiss tear from violent puking- vomiting like the exorcist

- Atropine- to stop cholinergic effects - It is an anticholinergic

- Charcoal - Binds med in the gut so it cannot be absorbed then is passed in the stool. - Powder form mixed in water and sucked through a straw to prevent reddining of

the teeth. - Vitamin K

- Antidote for Warfarin - Protamine Sulfate

- Antidote for heparin

Cancer

Antimetabolite- 5FU (fluorouracil)

- Pyrimidine analog (disrupts nucleic acid fxn)- IV or topical admin (topical for skin cancer and we may not need to know this)- Cell cycle S-phase specific, prevents thymidine production- bone marrow depression- High alert medication

- MTX methotrexate - Folic acid analog (prevents folic acid conversion)- Sphase specific- PREG category X- High alert med- dose limiting bone marrow suppression- Kills rapidly dividing cells, and causes immunosuppression- SE: Pulmonary fibrosis, Hepatotoxicity, nephrotoxic, Steven-Johnson’s

syndrome, and aplastic anemia- for the pulmonary toxicity, early signs are a dry nonproductive cough- for SJS, assess for rash as an early sign- for nephrotoxicity low back and flank pain is an early sign as well as changes in

urination patterns or pain.

Alkylating agentsalkylates DNA and binds 2 guanines together to prevent the helix from becoming unbound, therefore inhibiting replication. The dose is limited by bone marrow suppression, but can be given in a bolus.

- Mustargen (mechlorethamine) - inhibits DNA and RNA protein synthesis- for hodgkin’s disease and malignant lymphomas. - Cell cycle phase nonspecific- Contraindicated in pregnancy- SE: thrombocytopenia, Leukocytopenia, Seizures- monitor for bleeding and bone marrow suppression- notify provider for sore throat, neph-toxic s/s, bruising, bleeding, red stools- DO not drink alcohol, or take NSAIDs, or ASPIRIN, this will increase bleeding risk

- Mustard Gas- similar to the nitrogen mustards, but for warfare.

- Cytoxan (cyclophosphamide)- High alert med- most common alkylating agent - cell cycle phase nonspecific- SE: Pulmonary fibrosis, myocardial fibrosis, hemorrhagic cystitis(increase fluid

intake to 3000ml/day), leukopenia(monitor for , thrombocytopenia(monitor for bleeding), anemia.

- increases effects of warfarin, phenobarb and rifampin increase toxicity of this drug. Prolongs the effects of cocaine.

- monitor for edema, crackles, cardio/resp distress, HF s/s. - crosses BBB

Antibody Anti-tumor- Doxorubicin (Adriamycin)

- antitumor antibiotic - binds directly to DNA and stops replication- High alert med- dose limiting heart failure, and bone - cell cycle S phase specific- SE: CARDIO TOXIC, dark urine stools, palms and nails, alopecia, leukopenia, - monitor uric acid levels, bleeding and CBC, I’s and O’s

Platinum- Cisplatin

- produces crosslinks in DNA and is cell cycle nonspecific- dose limiting kidney failure- metastatic, head and neck, testicular, ovarian, bladder ,lung, and colon cancer

- tubular necrosis in the kidney, ototoxic, bone marrow suppression, severe nausea and vomiting in the first hour after administration.

- MOA similar to alkylating agents - Kidney Failure is a dose limiting factor.

Mitotic Inhibitors- Vincristine

- prevents cell division (m-phase specific)- SE: peripheral neuropathy (Neurotoxic), barely and bone suppression!!

- vinblastine causes bone marrow suppression and not peripheral neuropathy, so when used together there is not stacking of those side effects.

AntiHormones- Tamoxifen

- antiestrogen- for treatment and PREVENTION of estrogen related cancers ie. breast - SE: causes CANCER, birth defects, vaginal discharge w/ bleeding. - DD: carbamazepine = rapid metabolism. and erythromycin = slowed metabolism.

- prednisone- use in high doses- glucocorticoids- toxic to lymphocytes and lymph tissues

- progestin (megace) - used in AIDS pt for anorexia, weight gain and stim of appetite

Anticoagulants

- Aspirin- suppress platelet aggregation for the platelet’s life span through cyclooxygenase

inhibition. - doubles bleeding time for up to seven days- can be used for prophylaxis of MI in men and questionable in women. - risk of GI hemorrhage

- Heparin - Interrupt coag pathway in factor X and thrombin - prevents thrombosis, post op thrombus, and more clots forming- SE: HEMORRHAGE, HIT, Sensitivity reaction bc it is animal product, All kinds of

bleeding (gums, bruises, petechiae, hematoma, red or black stool)

- HIT heparin induced thrombocytopenia - antibodies develop against Heparin, and the person can NEVER GET THE DRUG AGAIN, there will also be long term bleeding issues associated with this

- RAPID acting, and only given IV never PO or IM- Made from animals- normal aPTT is 40 seconds- therapeutic aPTT with heparin is 60-80 seconds- PROTAMINE SULFATE is the antidote

- Lovenox- LMW Heparin - low molecular weight heparin- only stops factor X not thrombin - for prevention and treatment of DVT, prevents complications with unstable

angina- do not need to check aPTT- never givin IM

- Argatroban- direct thrombin inhibitor- Use this drug if the patient is experiencing HIT

- also bivalirudin does this (monitor with ACT test) - monitor with aPTT- no reversal agent - expensive

- Streptokinase- Thrombolytic: Dissolves clot after formation- stick all IV’s before giving drug- converts plasminogen to plasmin- for acute MI, pulmonary emboli, to break up a clot in a central line- can cause bleeding, Allergic RXN,

- tPA alteplase- thrombolytic: Dissolves clot after formation- stick all IV’s before giving drug- major bleeding issues. but not as much of an allergy risk- very similar to streptokinase

- Dabigatran (Pradaxa)- direct thrombin inhibitor- for HIT- ORAL anti coag for stroke PT’s w/ non valvular Afib- very expensive, - bleeding problems as well

- clopidogrel (Plavix)- ADP receptor antagonist- given with ASA sometimes, but do not take ASA- for PAD and CVA- these are contraindicated with HERBALS

- proton pump inhibitors makes plavix not effective- Warfarin (coumadin)

- indirectly decreases many clotting factors- works in the LIVER not the blood- normal tests while on warfarin are INR(2-3sec) and PT (12sec)- Pregnancy category X- decreases production of factors IIV, IX, X and prothrombin- for long term treatment of thrombosis, or pulmonary embolism, also prophylaxis

of clot formation(TIA, Prosthetic valve, Afib)- Lasts much longer than heparin- SE: bleeding like the rest- keep Vit K levels consistent throughout treatment- Vit K is the antidote- d/d interactions increase clotting: quinidine, antibiotics, NSAIDs, cimetidine,

thyroid hormones, ASA, Tylenol even

Musculoskeletal chapter 25

- Diazepam (Valium)- Centrally acting MM relaxants - flumazenil is the antidote for this- used to treat spasticity- CNS depression, sedation- benzo

- Selegiline (Eldepryl)- for parkinson's and for pt’s taking levodopa - spasticity as well

- Baclofen- for spasticity- analog for GABA- SE: sedation and HA, dizziness, diplopia and weakness- do not stop the administration of this drug suddenly- taper over 2 weeks or: hallucinations, fever rigidity, paranoia, seizures- DO NOT mix with ALCOHOL - given 2-3 times/day - herbal interactions: kava-kava, valerian root, or chamomile these can cause CNS

depression- no antidote

- Carbamazepine (tegretol)- SZ med- nerve pain and bipolar disorder- grapefruit interaction

- steven johnson’s syndrome- suicidal thoughts- do not take with warfarin

- cyclobenzaprine (Flexeril)- Centrally acting MM relaxants - do not use in:hyperthyroidism, heart conduction difficulties, heart failure, recent

MI.- serotonin syndrome - agitation, tachy, hyperthermia, (madams TIPS) - urine color change- do not use with other SSRI’s

- Metaxalone (Skelaxin)- Centrally acting MM relaxants - Can cause liver damage- test liver function before and throughout- ACH effects, caution in sedation w/ elderly

- methocarbamol (Robaxin)- Central acting MM relaxant- unknown MOA- for acute injuries- give ¾ x/day, urine color change, dizzy, drowsy, metallic taste. - intensifies with ETOH- chemically similar to tricyclic antidepressants

- Tizanidine (Zanaflex)- Centrally acting MM relaxants- acts at presynaptic A-2 - ACH effects, caution in sedation w/ elderly - do not take with alcohol

- NM Blocker in general- Bisphosphonates (alendronate)

- decrease bone resorption- SE: esophageal irritation, Heartburn, osteonecrosis of the jaw, atypical femur

fracture- SEVERE esophagitis, stand for 30 MINUTES after swallowing with water only- do not take with other drugs

- Teriparatide- STIMULATES bone formation- SQ injection- can be taken for up to 2 years

- NSAIDs (COX 1 and 2)- used in RA until the DMARDS kick in, (this is changing from NSAIDS to

glucocorticoids though)- 1st line treatment for gout

- DMARDs (MTX, Arava, Plaquenil)- Disease-modifying anti-rheumatic drugs

- given first for RA- take glucocorticoids until DMARD’s take effect- suppress autoimmune inflammatory process

- TNF is a part of the inflammatory process...- Synvisc

- injectable directly into the joint- cartilage and synovial fluid synthesis

- Indomethacin- NSAID for gout- inhibits prostaglandins- only give for 3-6 days

- colchicine- older gout drug- stops inflammation cycle, by decreasing mobility of granulocytes - treats acute gout attack

- Allopurinol- febuxostat (Uloric)- Xanthine oxidase inhibitor, stops production of uric acid- for chronic gout- Drink 3 liters of water per day

Diabetes Mellitus

Proinsulin is the prohormone to insulin, and is bound to a C-peptide. The peptide will be found in T2DM, but not T1DM.type 1 can have Ketoacidosis (DKA), and type 2 can have Hyperosmolar hyperglycemic non ketotic state (HHNK)

incretins stimulate insulin release, suppresses glucagon, slows GI emptying, as well as suppress appetite.

prediabetesImpaired fasting glucose (IFG) 100-125impaired glucose tolerance (IGT) 140 - 199 two hours after the oral glucose tolerance test6.5% > HgA1c > 5.7%

Diabetes DiagnosisHgA1c > 6.5%FBG > 126glucose tolerance > 200

Insulin(also promotes K uptake by the cells, so can also be given for hyperK)

- Lantus- no peak, duration of 24 hours

- Detemir- no peak, duration of 24 hours

- NPH- O: 60-120 P: 6-14 D: 16-24- cloudy solution

- 70/30- 70% NPH, 30% Regular- roll gently to mix

- Regular- O: 30-60 min P: 1-5hr D: 6-10hr

- Lispro- O: 5-10 min P: 30min-2.5hr D: 3-6.5hr

Orals- Biguanide (Metformin)

- stops liver glucose production in liver, increases glucose uptake in the periphery skeletal muscles.

- Will NOT cause insulin production. this means that this drug does NOT put a person at risk for hypoglycemia.

- Can be used with regular insulin and sulfonylureas - SE: Renal issues from LACTIC ACIDOSIS. If a person has renal insufficiency

they are put at a much higher mortality rate. - MONITOR renal fxn.

- Sulfonylureas (glipizide, Amaryl)- First line, promotes insulin secretion, - SE: HYPOGLYCEMIA- similar structure to a sulfonamide antibiotic - these are 2nd gen. and have longer durations than the 1st gen and fewer d/d

interactions. - D/D: all cause HypoGLY: ETOH, sulfonamides, Cimetidine, NSAIDs, beta

blockers- Glitazones (pioglitazone)

- decrease insulin resistance, and decreases liver glucose production- SE: HYPOGLYCEMIA- Not a first line med- D/D interactions: CIMETIDINE, ketoconazole, rifampin, Atorvastatin

- Glinides- stimulates pancreatic secretion of insulin - SE: HYPOGLYCEMIA

- Can be used with metformin- DD: Gemfibrozil

- A-Glucosidase inhibitors (acarbose, miglitol)- Delays carb absorption - 2% of drug is absorbed orally - SE: abb cramps, borborygmus bowel sounds, flatulence

- DPP-4 inhibitors (Sitagliptin)- Stops DPP-4 from breaking down incretin - the hormone Incretin increases insulin release, decreases hepatic glu production

and release. - Few SE and DD

Injectable noninsulin

- INcretin mimetics (exenatide - Byetta)- increase release of insulin, decrease glucagon secretion, makes you feel full, and

slows GI emptying- SQ INJECTION at breakfast and supper- from Gila monster spit- Nausea and vomiting- Hypoglycemia possible WITH sulfonylureas - a new formulation is once a week SQ injection!- SE: weight loss

- Amylin mimetics (pramlintide - Symlin)- Slows GI emptying, decrease glucagon release, pt will feel more full, decrease

postprandial glucose levels- SE: HYPOGLYCEMIA

Antianemics (heme)

- Iron sulfate- use a straw- toxic in kids- Makes RA worse - for iron deficiency anemia

- B12- treats b12 or pernicious anemia- b12 is needed to synthesize folic acid for cell growth and development- can cause hypoK - Cyanocobalamin

- Folic Acid (folate)- for folic acid anemia- essential for cell replication- anemia can be from alcoholism, liver damage.

- Deferoxamine- high affinity for ferric iron- do not take with oj

- Erythropoietin - stimulates RBC production- mimics a natural hormone produced in the kidney- needs the supplies to make RBC’s: iron, folate, and B12- indications: chronic renal failure, anemia from chemo, or a chronic anemic patient

having surgery. - can cause HTN- if HGB increases above 11 MI, CVA, and HF chances are increased dt increased

clotting