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83 Cards in this Set
- Front
- Back
Enzyme kinetics
Michaelis-Menten eqn? Km rep? = [S] when? Vmax proportional to? Chart: Y-axis? X-axis? Y-int? X-int? Slope? Competitive inh change? Noncompetitive inh change? |
v = vmax[S]/Km + [S]
Affinity of enzyme for substrate (inverse) When 1/2 vmax, Km = [S] Enzyme concentration Y-axis: 1/V; X-axis: 1/[S] Y-int: 1/Vmax; X-int: 1/-Km Slope = Km/Vmax Comp inh change Km (dec potency) Noncomp inh change Vmax (dec efficacy) |
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amount of drug in body/_______ = Vd
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plasma drug concentration (note: Vd is Volume of Distribution)
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rate of elimination of drug/[plasma drug] = ?
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CL (Clearance)
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(.7)(Vd)/CL = ?
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T 1/2
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A drug infused at a constant rate reaches about 94% of steady state after _______ t 1/2s.
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4-5
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A loading dose is calculated using this formula.
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(Cp)(Vd)/F (note: Cp = target plasma concentration, and F = bioavailability)
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A maintenance dose is calculated using this formula.
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(Cp)(CL)/F
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Rate of elimination is proportional to _______ ______ in 1st order elimination.
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drug concentration (constant fraction of drug eliminate/time)
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In the case of EtOH, which is elimated by _____ order elimination, a constant amount of drug is eliminated per unit time.
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zero
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Phase ____ (I or II) reactions yield slightly polar metabolites that are often _____ (active or inactive)
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I, active
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Phase ____ (I or II) reactions yield very polar metabolites that are often _____ (active or inactive) and are excreted by the _______.
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II, inactive, kidney
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Phase II reactions are often of this type.
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conjugation
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Cytochrome P-450 is involved in _____ phase (I or II) reactions.
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I
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Drugs are first tested in patients in phase _____ of clinical testing, pharmacokinetic safety is determined in phase ______ of clinical testing, double blind tests are done in phase ____ and post-market surveillance is done in phase _____.
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2,1,3,4
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In a dose response curve, a competitive antagonist shifts the curve _____, while a non-competitive antagonist shifts the curve ______.
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right, down
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What pharmacologic relationship would determine the existence of spare receptors?
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EC50 < Kd
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What does it mean if EC50 and Kd are equal?
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The system does not have spare receptors
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A partial agonist acts on the same receptor system as a full agonist? True or false
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T
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What's the main difference between a partial agonist and a full agonist?
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A partial agonist has a lower maximal efficacy.
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Is a partial agonist less potent than a full agonist?
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Not necessarily. It can be less, more or equally potent as a full agonist.
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In renal or liver dz, how do you change maintenance dose?
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Dec
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In renal or liver dz, how do you hange loading dose?
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Unchanged
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Which 3 drugs show zero order metabolism?
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Phenytoin, Ethanol, Aspirin (PEA)
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Efficacy is defined as
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maximal effect a drug can produce
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Potency is defined as
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amount of drug needed for a given effect
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Drug reactions
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Pulmonary fibrosis (3)
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bleomycin, amiodarone, busulfan
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Hepatitis (2)
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isoniazid, halothane
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Focal to massive hepatic necrosis (4)
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halothane, valproic acid, acetaminophen, amanita phalloides
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Anaphylaxis (1)
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penicillin
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SLE-like syndrome (4). [mnemonic: it's not HIPP to have lupus]
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hydralazine, INH, procainamide, phenytoin
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Hemolysis in G6PD-deficient patients (8)
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sulfonamides, INH, aspirin, ibuprofen, primaquine, nitrofurantoin, pyrimethamine, chloramphenicol
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Thrombotic complications (1 class)
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OCPs (e.g. estrogens and progestins)
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Adrenocortical insufficiency (withdrawal of what class of drugs causes adrenocortical insufficiency?)
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withdrawal of glucocorticoids causes hypothalamic-pituitary-axis suppression
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Photosensitivity reactions (3) [mnemonic: SAT for a photo]
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Sulfonamides, amiodarone, tetracycline
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Induce P-450 system (6)
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barbiturates, phenytoin, carbamazepine, rifampin, griseofulvin, quinidine
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Inhibit P-450 system (6, including one fruit)
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cimetidine, ketoconazole, grapefruit, erythromycin, INH, sulfonamides
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Tubulointerstitial nephritis (5)
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sulfonamides, furosemide, methicillin, rifampin, NSAIDs (except aspirin)
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Hot flashes (1)
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Tamoxifen
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Cutaneous flushing (4)
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niacin, Ca++ channel blockers, adenosine, vancomycin
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Cardiac toxicity (2)
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doxorubicin (adriamycin), daunorubicin
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Agranulocytosis (3, all start with letter C)
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clozapine, carbamazepine, colchicine
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Stevens-Johnson syndrome (3)
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ethosuximide, sulfonamides, lamotrigine
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Cinchonism (2)
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quinidine, quinine
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Tendonitis, tendon rupture and cartilage damage (kids) (1)
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fluoroquinolones
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Disulfiram-like reaction (4)
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metronidazole, certain cephalosporins, procarbazine, sulfonylureas
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Otoxicity and nephrotoxicity (3)
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aminoglycosides, loop diuretics, cisplatin
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Drug-induced Parkinson's (4)
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haloperidol, chlorpromazine, resperine, MPTP
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Torsades de pointes (two subclasses of antiarrhythmics)
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Class III (sotalol), class IA (quinidine) antiarrhythmics
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Aplastic anemia (3)
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chloramphenicol, benzene, NSAIDs
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Neuro/nephrotoxicity (1)
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polymyxins
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Pseudomembranous colitis (2)
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clindamycin, ampicillin
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Gynecomastia (5) [mnemonic: Some Drugs Create Awesome Knockers]
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spironolactone, digitalis, cimetidine, chronic Alcohol use, estrogens, ketoconazole
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Atropine-like side effects (1)
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tricyclics
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Cough (1)
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ACE inhibitors (losartan --> no cough)
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Gingival hyperplasia (1)
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phenytoin
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Diabetes insipidus (1)
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lithium
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Tardive dyskinesia (1)
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antipsychotics
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Fanconi's syndrome (1)
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tetracycline
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Gray baby syndrome (1)
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chloramphenicol
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Extrapyramidal side effects (3)
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chlorpromazine, thioridazine, haloperidol
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Osteoporosis (2)
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corticosteroids, heparin
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Drug name
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ane
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inhalational general anesthetic. Halothane
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azepam
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benzodiazepine. Diazepam
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azine
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phenothiazine (neuroleptic, antiemetic). Chlorpromazine
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azole
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antifungal. Ketoconazole
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barbital
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barbiturate. Phenobarbital
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caine
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local anesthetic. Lidocaine
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cillin
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penicillin. Methicillin
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cycline
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antibiotic, protein synthesis inhibitor. Tetracycline
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ipramine
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tricyclic antidepressant. Imipramine
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navir
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protease inhibitor. Saquinavir
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olol
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beta antagonist. Propranolol
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operidol
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butyrophenone (neuroleptic). Haloperidol
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oxin
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cardiac glycoside (inotropic agent). Digoxin
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phylline
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methylxanthine. Theophylline
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pril
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ACE inhibitor. Captopril
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terol
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beta-2 agonist. Albuterol
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tidine
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H2 antagonist. Cimetidine
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triptyline
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tricyclic antidepressant. Amitriptyline
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tropin
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pituitary hormone. Somatotropin
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zosin
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alpha-1 antagonist. Prazosin
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