Comprehensive Questions (Frequently
Tested) with Verified Answers Graded
A+
Prodrug - Answer: An inactive drug dosage form that is converted to an active metabolite by
various biochemical reactions once it is inside the body.
-Cytochrome P450
-Ex. Aspirin, psilocybin, heroin
Bioavailability - Answer: the rate at and the extent to which a nutrient is absorbed and used
-Affected by route of administration and drug dosage
-Drug clearance (rate drug leaves circulation)
-Steady state concentration
-Affected by chemical stability, solubility, and first pass
Steady state (of a drug) - Answer: stable level of drug in the body, occurs in 5 half lives of the
drug
-rate of drug being added to system is equal to amount being eliminated from system
Pharmacokinetics - Answer: The process by which drugs are absorbed, distributed within the
body, metabolized, and excreted.
-what the body does to the drug
,First pass - Answer: the fact that a medication in the GI tract passes through the liver before
entering other organs
does not - Answer: bioequivalence does/does not affect bioavailability
Bioequivalence - Answer: relative therapeutic effectiveness of chemically equivalent drugs.
Bioavailability (is affected by) - Answer: -chemical instability
-solubility
-first pass metabolism
Cytochrome P450 - Answer: -enzymes that function to metabolize potentially toxic compounds,
including drugs and products of endogenous metabolism such as bilirubin, principally in the
liver.
-genetics influence presence of enzymes
-affects metabolism of warfarin, antidepressants, antiepileptics, and statins.
-the levels of these drugs are higher when taken with certain drugs that are inhibitors (ex.
warfarin with omeprazole) because there is competition for enzyme metabolism.
-inducers lead to decreased plasma concentration of drug.
cytochrome p450 inducer - Answer: An inducer increases the metabolism of a substrate
resulting in a decreased level or effect of the substrate
cytochrome p450 inhibitor - Answer: An inhibitor decreases the metabolism of a substrate
resulting in an increased level or effect of the substrate.
Clopidogrel - Answer: prodrug that must be activated by hepatic CYP2C19 metabolism;
individuals who are poor metabolizers may not form the active metabolite and have reduced
antiplatelet response
, half-life (determines) - Answer: how often a drug is administered
4-5 - Answer: steady state is reached in _-_ times the half-life
Warfarin (MOA) - Answer: -Vitamin K antagonist
-Factors II, VII, IX, X
-takes several days to take effect
-monitor INR
Vitamin K - Answer: warfarin antidote
Heparin (MOA) - Answer: -rapid anticoagulation by binding with antithrombin III and inhibits
factors IXa, Xa, XIIa, and XIII
-aPTT monitoring (low dose SQ does not require monitoring)
Apixaban (MOA) - Answer: direct factor Xa inhibitor
parenteral administration - Answer: -directly into systemic circulation
-poor absorption or unstable in GI tract (ex. heparin, insulin), rapid absorption, unable to take
meds PO
-IV, IM, SQ, ID
IV - Answer: -into the vein
-can be given through bolus (rapid peak) or infusion (lower peak, longer duration)
-ex. rocuronium (neuromuscular blocker)