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26 Cards in this Set

  • Front
  • Back
what is the duration of the drug effect dependent on?
rates of absorption and elimination
what is a consequence of saturated zero-order elimination?
little to no metabolic reserve is available
what compounds are described by michaelis-menten kinetics?
phenytoin and ethanol
what describes kinetics of limiting capacity?
michaelis-menten kinetics
what is characteristic of first order kinetics?
rate depends on concentration
what describes absorption of drug solutions and elimination of most drugs at therpeutic doses?
first order kinetics
how is bioavailability calculated?
AUC values for oral relative to IV or relative bioavailability of product X versus product Y
why are drugs that are acids or bases often provided as pharmaceutical salts?
salt forms are more stable for storage and more soluble for absorption
does clearance of a drug change as concentration drops?
clearance is independent of drug concentration and remains constant with first-order changes in plasma levels
which takes longer to reach steady state, a drug with a short or long half life?
long half life reach steady state slowly
what are disadvantages of a loading dose?
high transient blood levels producing toxicity, no similar means to remove drug once given
what is a rule of thumb for dosing intervals?
use of dosing intervals equal to the half-life of the drug will result in a two-fold concentration fluctuation (maximum level equals twice the minimum)
when is blood drug level monitoring useful?
drug response is difficult to quantify, small therapeutic window, response inadequately predicted from dose due to variability in blood concentrations in the population, relationship between concentration and effect must be known
why blood drug concentration monitoring rather than use dose-response relationships?
when drug response is difficult to monitor directly, concentration-response relationships usually are less variable
where is variability generated in looking at dose-response relationships?
differences in absorption, distribution, metabolism, excretion
what are indications for serum concentration measurements?
evaluate concentration-related toxicity, analyze lack of therapeutic efficacy, ensure dose regimen is adequate, use pharmacokinetics to guide dose adjustments
what could cause concentration-related toxicity?
unexpectedly slow drug elimination, overdose, surreptitious drug use, dispensing errors
what could cause lack of therapeutic efficacy?
noncompliance, poor absorption or bioavailability, unexpectedly rapid drug elimination
what are important factors in interpreting blood drug levels?
timing with respect to time of drug administration, patient physiological state, presence of active metabolites
for what drugs is concentration monitoring useful?
psychotropic drugs, digoxin, anti-arrhythmics, anti-seizure, aminoglycosides, immunosuppressive anti-rejection drugs
psychotropic drugs for which concentration monitoring is useful?
lithium; antidepressants: amitriptyline/nortiptyline, imipramine/desipramine, doxepin/nordoxepin
anti-arrhythmic drugs for which concentration monitoring is useful?
lidocaine, procainamide, and N-acetylprocainamide (active metabolite)
anti-seizure drugs for which concentration monitoring is useful?
phenytoin, carbamazepine, primidone and metabolic phenobarbital (active metabolite)
aminoglycoside antibacterial drugs for which concentration monitoring is useful and what is a possible consequence of toxicity?
amikacin and tobramycin; ototoxicity
immunosuppressive anti-rejection drugs for which concentration monitoring is useful?
cyclosporine, tacrolimus, sirolimus
which drugs for which concentration monitoring is useful have a active metabolite that needs to be taken into account and what is it?
procainamide (N-acetylprocainamide) and primidone (phenobarbital)