Pharmacolgy Flashcards by Mark Sutherland

Briefly describe additive, synergistic and permissive effects

Additive - A w/ B = A + B. Synergistic - A w/ B > A + B. Permissive - B = 0 but A w/ B > A

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Formula for volume of distribution

[Amount of drug in body] / [plasma dug concentration]

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Formula for half life

(0.7 x Vd) / CL

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Formula for loading dose

Cp x Vd/F. Cp is desired peak concentration, Vd is volume of distribution. F is bioavailability

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Drugs that undergo zero order elimination

Phenytoin, Ethanol, Aspirin (very high dosese)

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What type of compounds preferentially get metabolized by the liver?

Lipophilic compounds

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On a dose response curve, which axis is potency and which is efficacy?

Potency is x axis, efficacy is y axis

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What relationship do norepinephrine and phenoxybenzamine have at alpha receptors?

Noncompetitive antagonist

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What type of receptors are nicotinic receptors?

Ligand-gated Na/K channels

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G protein class for the sympathetic receptors

A1 - q, A2 - i, B1 - s, B2 - s

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G protein class for the parasympathetic receptors

M1 - q, M2 - i, M3 - q

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G protein class for dopamine, histamine, and vasopressin receptors

D1 - s, D2 - i. H1 - q, H2 - s. V1 - q, V2 - s

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Gq receptors

Use phospholipase C to create PIP2 which creates DAG (PKC) and IP3 (Ca influx)

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Gs receptors

Stimulate adenylyl cyclase to increase cAMP levels, which increases PKA levels, which increases Ca influx (heart) and inhibits MLCK (SM)

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Gi receptors

Inhibit adenylyl cyclase levels, decreasing cAMP

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Which sympathetic receptor does NE not act much on?

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How can you tell the difference between an alpha agonist and a muscarinic antagonist?

Alpha agonism causes mydriasis, muscarinic antagonism causes mydriasis AND FLUSHING

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Direct cholinomimetic agents

Bethanechol, carbachol, pilocarpine, methacholine

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Indirect cholinomimetics (AChE-Is)

Neostigmine, pyridostigmine, edrophonium, physostigmine, echothiophate, donepezil

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What do organophosphates do biochemically?

Shut down AChE

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Treatment for organophosphate poisoning and rationale

Atropine to help muscarinic receptors, pralidoxime to help nicotinic receptors (muscle paralysis)

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Pralidoxime

Regenerates active AChE. Give with atropine in cholinesterase poisoning

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Muscarinic antagonists

Eye - atropine, homatropine, tropicamide. CNS - benztropine, scopolamine. Respiratory - ipratropium. GU - oxybutynin, glycopyrrolate. GI - methscopolamine, pirenzepine, propantheline

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Tiotropium

Trade name spiriva. Muscarinic antagonist used in asthma and COPD

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Which sympathetic receptors does epi act at?

A1, A2, B1, B2 (all of them except D1)

Isoproterenol

B1 and B2 agonist. Used in AV block

Which sympathetic receptors does dopamine act at?

High dose - A1 and A2. Medium dose - B1 and B2. Low dose - D1. Use in shock to increase renal perfusion

Dobutamine

B1 agonist with some activity at A1, A2, and B2. Inotropic but not chronotropic

Phenylephrine

A1 and A2 agonist (more activity at A1 than A2)

Ritodrine

Selective B2 agonist. Reduces premature uterine contractions

Action of amphetamine and ephedrine

Indirect sympathetic agonists. Release stored catecholamines

Action of cocaine

Indirect general sympathetic agonist. Uptake inhibitor

Clonidine, alpha-methyldopa

Centrally acting alpha 2 agonists. Decrease adrenergic outflow. Use in HTN with renal disease

Phenoxybenzamine

Nonselective irreversible alpha blocker. Use in pheochromocytoma

Phentolamine

Reversible nonselective alpha blocker. Give to patients on MAOIs who eat tyramine-containing foods

Prazosin, terazosin, doxasin

Alpha-1 blockers. Use in HTN, BPH

Mirtazapine

Alpha-2 blocker. Use in depression

What neurologic disorder is propanolol used in and in what concurrent conditions might it be contraindicated?

Migraine prophylaxis. Do not use if pt has COPD or asthma

B1-selective antagonist with partial agonist activity

Acebutolol

B1-selective antagonists

Acebutolol (partial agonist), Betaxolol, Esmolol, Atenolol, Metoprolol

Carvedilol and Labetalol

Nonselective (vasodilatory) alpha and beta antagonists

Partial Beta Agonists

Pindolol, Acebutolol

Salicylate antidote

NaHCO3, dialysis

Amphetamine antidote

NH4Cl (to acidify urine)

Beta-blocker antidote

Glucagon

Lead, Mercury, Arsenic, Gold, Copper, and Cyanide antidotes

LEad - CaEDTA, dimercaprol, succimer and penicillamine. Mercury, Arsenic and Gold - Dimercaprol, succimer. Copper, arsenic and gold - Penicillamine. Cyanide - Nitrite, hydroxycobalamin, thiosulfate

TCA antidote

NaHCO3 (plasma alkalinization)

tPA, streptokinase, and urokinase antidote

Aminocaproic acid

Theophylline antidote

Beta-blocker

Hexamethonium

Essentially blocks the entire ANS (sympathetic and parasympathetic)

Drugs that cause cutaneous flushing

Vancomycin, Adenosine, Niacin, Ca channel blockers

Drugs that cause dilated cardiomyopathy

Doxorubicin, daunorubicin

Anti-arrhythmic drugs that cause torsades de pointes

Class 3 (sotalol), class 1A (quinidine) antiarrhythmics

Drugs that cause agranulocytosis

Clozapine, Carbamazepine, Colchicine, PTU, Methimazole, Dapsone

Drugs that cause aplastic anemia

Chloramphenicol, benzene, NSAIDs, PTU, methimazole

Drugs that cause direct coombs positive hemolytic anemia

Methyldopa

Drugs that cause hemolysis in G6PD patients

INH, Sulfonamides, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin

Drugs that cause megaloblastic anemia

Phenytoin, Methotrexate, Sulfa drugs

Drugs that cause pulmonary fibrosis

Bleomycin, Amiodarone, Busulfan

Drugs that cause acute cholestatic hepatitis

Macrolides

Drugs that cause focal to massive hepatic necrosis

Halothane, acetaminophen, valproic acid, amanita phalloides (mushroom)

Drugs that cause hepatitis

INH

Drugs that cause pseudomembranous colitis

Clindamycin, ampicillin

Drugs that cause gynecomastia

Spironolactone, Digitalis, Cimetidine, chronic alcohol use, Estrogens, Ketoconazole

Drugs that cause hypothyroidism

Lithium, amiodarone, sulfonamides

Drugs that cause hyperglycemia

Niacin, tacrolimus, protease inhibitors

Drugs that cause fat redistribution

Glucocorticoids and protease inhibitors

Drugs that cause gingival hyperplasia

Phenytoin, verapamil

Drugs that cause gout

Furosemide, thiazides, niacin, cyclosporine, pyrazinamide

Drugs that cause myopathy

Fibrates, Niacin, Colchicine, Hydroxychloroquine, Interferon-a, Penicillamine, Statins, Glucocorticoids

Drugs that cause osteoporosis

Corticosteroids, heparin

Drugs that cause photosensitivity

Sulfonamides, Amiodarone, Tetracycline

Drugs that cause stevens-johnson

Penicillin, Ethosuximide, Carbamazepine, Sulfa drugs, Lamotrigine, Allopurinol, Phenytoin, Phenobarbital

Drugs that cause SLE-like syndrome

Hydralazine, INH, Procainamide, Phenytoin

Who tends to get drug induced lupus?

Slow acetylators. The drugs that cause this all required n-acetylation in the liver

Drugs that cause tendonitis, tendon rupture, and cartilage damage in kids

Fluoroquinolones

Drugs that cause DI

Lithium, demeclocycline

Drugs that cause fanconis syndrome

Expired tetracycline

Drugs that cause interstitial nephritis

Methicillin, NSAIDs, furosemide

Drugs that cause hemorrhagic cystitis

Cyclophosphamide, ifosfamide (give with mesna)

Drugs that cause SIADH

Carbamazepine, cyclophosphamide

Drugs that cause cinchonism (flushed and sweaty skin, tinnitus, blurred vision, confusion, headache, abdominal pain, rashes, photosensitivity, vertigo, dysphoria, nausea, vomiting and diarrhea)

Quinidine, quinine

Drugs that cause Parkinsonism

Antipsychotics, reserpine, metoclopramide

Drugs that cause seizures

Bupropion, imipenem/cilastatin, INH

Drugs that cause disulfiram-like reaction

Metronidazole, cephalosporins, procarbazine, sulfonylureas

Drugs that cause nephrotoxicity/ototoxicity

Aminoglycosides, vancomycin, loop diuretics, cisplatin

List the P-450 inducers (7)

Barbiturates, St. Johns wort, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, Alcohol (chronic)

List the P-450 inhibitors (11)

Quinidine, Macrolides, Amiodarone, Grapefruit juice, INH, Cimetidine, Ritonavir, Alcohol (acute), Ciprofloxacin, Ketoconazole, Sulfonamides

Sulfa drugs (8)

Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine, Sulfonylureas

POMC derivatives

ACTH, MSH, B-endorphins

High CYP activity is associated with increased susceptibility to what?

Cancer. Most carcinogens come in as pro-carcinogens and are metabolized by the CYP-450 system (monooxygenases)