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