Toxicokinetics and Metabolism Flashcards
6 cards from real ABT practice questions. Tap to flip, then mark Knew It or Still Learning — missed cards come back until you master them.
Read the first 6 Toxicokinetics and Metabolism flashcards as text
Which pharmacokinetic parameter describes the fraction of an administered dose that reaches systemic circulation unchanged?
Answer: Bioavailability (F)
Bioavailability (F) is the fraction of an administered dose that reaches the systemic circulation unchanged, accounting for absorption and first-pass metabolism.
Which cytochrome P450 enzyme is responsible for metabolizing the largest number of pharmaceutical drugs (approximately 30–40%)?
Answer: CYP3A4
CYP3A4 is the most abundant hepatic and intestinal CYP enzyme and metabolizes approximately 30–40% of clinically used drugs, making it a key site of drug-drug interactions.
A chemical with a high volume of distribution (Vd > 10 L/kg) is most likely to be:
Answer: Highly lipophilic and distributed into peripheral tissues
A high volume of distribution indicates the drug is extensively distributed into peripheral tissues (fat, muscle), suggesting high lipophilicity or strong tissue protein binding.
First-order elimination kinetics means that:
Answer: The rate of elimination is directly proportional to the drug concentration
In first-order kinetics, a constant fraction (not amount) of drug is eliminated per unit time; the rate of elimination is proportional to drug concentration, resulting in a constant half-life.
The hepatic extraction ratio (ER) of a drug determines whether its clearance is sensitive to changes in:
Answer: Hepatic blood flow for high-ER drugs and protein binding for low-ER drugs
High extraction ratio (ER > 0.7) drugs have flow-limited clearance sensitive to hepatic blood flow, while low ER drugs (< 0.3) have capacity-limited clearance sensitive to enzyme activity and protein binding.
Which phase II biotransformation reaction is most important for detoxifying reactive electrophilic metabolites via conjugation with a tripeptide?
Answer: Glutathione conjugation (GST)
Glutathione S-transferases (GSTs) conjugate reactive electrophilic metabolites with glutathione (γ-Glu-Cys-Gly), detoxifying them and preventing cellular damage.