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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
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