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27 Cards in this Set

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Drugs with narrow therapeutic indices:
aminoglycosides, anticoagulants, aspirin, carbamezapine, conjugated estrogens, cyclosporine, digoxin, esterified estrogens, hypoglycemic agents, levothyroxine, lithium, phenytoin, procainamide, quinidine, theophylline, TCAs, valproic acid
What is a common characteristic of drugs with narrow therapeutic indices?
-they usually exhibit high protein binding
-caution with kidney failure: uremia can decrease protein binding and increase their levels
Difference between phase 1 and phase 2 metabolism
-phase 1: Biotransformation (oxidation, hydroxylation, reduction, hydrolysis)
-phase 2: conjugation (glutathione s-transferaseds, UDP glucuronyltransferases, n-acetyl transferases, sulfotransferases)
Ketoconazole (azoles) + antacids=______
-ketoconazole and other aoles require gastric acid for absorption, so taking them with antacids decreases their availability
Quinolones + antacids=_______
Quinolones bind calcium and magnesium salts, which decreases their absorption, so taking them with antacids decreases their availbility
Tetracycline + antacids=_______
Tetracyline forms an insoluble chelate with aluminum salts, which decreases their absorption, so taking it with antacids decreases its avialibility
Warfarin + cholestyramine=______
Warfarin adsorbs to cholestyramine, so cholestyramine decreases its absorption
When are protein binding interactions most significant?
-Need greater than 90% binding (warfarin, phenytoin)
-small volumes of distribution (salicylic acid)
-zero order/saturable kinetics (phenytoin)
1. NSAIDs + phenytoin=_____
3. Uremia + NSAIDs + phenytoin=_____
1. NSAIDs displace phenytoin from protein binding only at high concentrations
3. Uremia and NSAIDs together can lead to an even greater displacement of phenytoin protein binding and an increase in phenytoin levels
Sulfonamides + warfarin=_____
Sufonamides displace warfarin from protein binding AND inhibit its clearance, causing an increase in free warfarin levels
Chloral hydrate + warfarin=_____
chloral hydrate displaces warfarin from protein binding, but free levels of warfarin only transiently increase because the clearance of free warfarin increases
What are the cyp450 enzymes that metabolize the greatest proportion of drugs?
#1 CYP3A4
#2 CYP2D6
#3 CYP2C
#4 CYP2E
#5 CYP1A2
How does Ritonavir effect the p450 system?
Ritonavir is a universal cyp450 inhibitor
Which drugs are major inducers of the cyp450 system?
-Rifampin (universal)
-phenytoin (universal; Rifampin is more powerful and will decrease phenytoin levels)
-Carbamezapine (universal)
-Phenobarbital (universal)
What are some inhibitors of cyp3A4?
-grapefruit juice
-azoles (fluconazole, itraconoazole, ketoconazole, omeprazole)
-protease inhibitors (Ritonavir, saquinavir)
What are some substrates of cyp3A4?
-benzodiazapines (sedation)
-statins (myopathy)
-estrogen (increased metabolism could ruin efficacy of oral contraceptives)
Azoles + fibrates + statins=_____
azoles inhibit cyp3A4 metabolism of statins, and fibrates increase statin levels, so together they increase the risk of myopathy
Protease inhibitors + clopidogrel=______
-protease inhibitors inhibit cyp2C19, increasing clopidogrel levels (bleeding)
What is the effect of smoking on the cyp450 system?
smoking induces cyp1A2, leading to increased warfarin, caffeine, theophyline, diazepam, etc. metabolism
What are the effects of cimetidine and ciprofloxacin on the cyp450 system
cimetidine and ciproflaxacin inhibit cyp1A2, leading to decreased warfarin, theophyline, diazepam, etc. metabolism
Diltiazem + cyclosporine=______
-diltiazem inhibits cyclosporine metabolism, increasing cyclosporine levels and its toxicity
grapefruit juice + terfenadine=_____
grapefruit juice inhibits terfenadine metabolism, increasing its levels and increasing the risk of torsades
How does the pH of urine effect drug excretion?
-Weak acids are ionized at an alkaline pH, which increases their excretion
-Weak bases are ionized at acidic pH, which increases their excretion
How does probenicid effect excretion of penicillin?
-probenecid inhibits the active tubular secretion of penicillin, thus decreasing its excretion
How does digoxin and its derivatives effect quinidine excretion?
-digoxin inhibits the active tubular secretion of quinidine, thus decreasing its excretion
How does bicarbonate administration effect amphetamine levels?
-Amphetamine is a weak base, which is best excreted when the urine is acidic
-Administration of bicarbonate causes alkinization, with more of the amphetamine in a non-ionized form
-therefore amphetamine excretion will be decreased
Zidovudine + Gangcyclovir=_____
additive bone marrow suppression