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Questions and Answers
Which CYP enzyme is involved in the metabolism of clopidogrel and proton pump inhibitors?
Which CYP enzyme is involved in the metabolism of clopidogrel and proton pump inhibitors?
- CYP 2C19 (correct)
- CYP 3A4
- CYP 2A
- CYP 2B
Which of the following statements is true about protein binding of drugs?
Which of the following statements is true about protein binding of drugs?
- Drugs having higher affinity for a plasma protein can displace another drug from the same protein (correct)
- Acidic drugs bind to alpha-1 acid glycoprotein in plasma
- Basic drugs bind to albumin in plasma
- Sex steroid hormones do not bind to any protein in plasma
What is the pH at which a drug is 50% ionized?
What is the pH at which a drug is 50% ionized?
- pH of the plasma
- pKa of the drug (correct)
- pH of the solution
- pH of the gut
What is the primary factor that determines the extent of ionization of a drug?
What is the primary factor that determines the extent of ionization of a drug?
What happens to the degree of ionization of a weak acidic drug when the pH is near its pKa?
What happens to the degree of ionization of a weak acidic drug when the pH is near its pKa?
What is the ionization state of phenobarbitone at an acid pH?
What is the ionization state of phenobarbitone at an acid pH?
Which of the following statements about bioavailability is false?
Which of the following statements about bioavailability is false?
What is the significance of knowing the pKa of a drug?
What is the significance of knowing the pKa of a drug?
What is the volume of plasma completely cleared of a specimen compound per unit time and measured as a test of kidney function?
What is the volume of plasma completely cleared of a specimen compound per unit time and measured as a test of kidney function?
What is the formula to calculate the volume of distribution of a drug?
What is the formula to calculate the volume of distribution of a drug?
What is the conjugation reaction involved in the metabolism of sulphonamides?
What is the conjugation reaction involved in the metabolism of sulphonamides?
Which anesthetic is associated with the redistribution phenomenon?
Which anesthetic is associated with the redistribution phenomenon?
Which of the following is a nonsynthetic phase I reaction for drug detoxification?
Which of the following is a nonsynthetic phase I reaction for drug detoxification?
What is the primary role of the kidney in pharmacokinetics?
What is the primary role of the kidney in pharmacokinetics?
What is bioavailability?
What is bioavailability?
What is the primary role of conjugation reactions in drug metabolism?
What is the primary role of conjugation reactions in drug metabolism?
What is an example of physiological antagonism?
What is an example of physiological antagonism?
Which of the following drugs does not act on ionic channels?
Which of the following drugs does not act on ionic channels?
What does efficacy of a drug refer to?
What does efficacy of a drug refer to?
Which of the following drugs is known to cause an SLE-like reaction?
Which of the following drugs is known to cause an SLE-like reaction?
What is the term for a drug that binds to a receptor and causes an action opposite to that of an agonist?
What is the term for a drug that binds to a receptor and causes an action opposite to that of an agonist?
What is the study of how variation in the human genome affects the response to medications known as?
What is the study of how variation in the human genome affects the response to medications known as?
What is the term for a drug that has a high affinity for a receptor but does not activate it?
What is the term for a drug that has a high affinity for a receptor but does not activate it?
Which of the following is an example of a partial agonist?
Which of the following is an example of a partial agonist?
What type of dose-response curve provides information on variation in sensitivity of response to increasing doses of the drug in different individuals?
What type of dose-response curve provides information on variation in sensitivity of response to increasing doses of the drug in different individuals?
What is the primary goal of Phase 1 in drug development?
What is the primary goal of Phase 1 in drug development?
What is the effect on Vmax and Km in competitive inhibition?
What is the effect on Vmax and Km in competitive inhibition?
Which of the following drugs is contraindicated in acute intermittent porphyria?
Which of the following drugs is contraindicated in acute intermittent porphyria?
What is drug efficacy defined as?
What is drug efficacy defined as?
What is the purpose of Phase 2 in drug development?
What is the purpose of Phase 2 in drug development?
What is the effect on Vmax and Km in non-competitive inhibition?
What is the effect on Vmax and Km in non-competitive inhibition?
What is the goal of Phase 3 in drug development?
What is the goal of Phase 3 in drug development?
What is the most common cytochrome P450 enzyme involved in drug metabolism?
What is the most common cytochrome P450 enzyme involved in drug metabolism?
Which of the following drugs is known to bind to albumin?
Which of the following drugs is known to bind to albumin?
Which of the following is an enzyme inhibitor?
Which of the following is an enzyme inhibitor?
Which of the following antiepileptics is NOT a microsomal enzyme inducer?
Which of the following antiepileptics is NOT a microsomal enzyme inducer?
What is the effect of grapefruit juice on drug metabolism?
What is the effect of grapefruit juice on drug metabolism?
Which of the following can result in oral contraceptive failure?
Which of the following can result in oral contraceptive failure?
Which of the following is a substrate for CYP3A4?
Which of the following is a substrate for CYP3A4?
Which of the following statements about drug metabolism is TRUE?
Which of the following statements about drug metabolism is TRUE?
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Study Notes
Enzymes and Metabolism
- CYP 2C19 is the mitochondrial enzyme involved in the metabolism of clopidogrel and proton pump inhibitors.
- A drug's extent of ionization depends on its pKa and the pH of the solution it is dissolved in.
Drug-Protein Binding
- Acidic drugs bind to albumin in plasma.
- Basic drugs bind to alpha-1 acid glycoprotein in plasma.
- Drugs with higher affinity for a plasma protein can displace other drugs from the same protein.
Bioavailability
- Bioavailability is the percentage of a drug detected in the systemic circulation after its administration.
- Volume of plasma completely cleared of a specific compound per unit time is a measure of kidney function.
Volume of Distribution
- Volume of distribution (Vd) is the ratio of the dose administered IV to the plasma concentration.
Redistribution Phenomenon
- Redistribution phenomenon is seen in Thiopentone.
Conjugation Reactions
- Sulphonamide is conjugated with Acetylation.
- Oxidation is a nonsynthetic phase I reaction for drug detoxification.
Cytochrome P450 Enzymes
- CYP3A4 is the cytochrome P450 enzyme most commonly involved in drug metabolism.
- Ketoconazole is an enzyme inhibitor.
- Rifampicin is an enzyme inducer.
Drug Metabolism
- Grapefruit juice is an enzyme inhibitor.
- Phenobarbitone and Phenytoin are microsomal enzyme inducers.
- Valproate is not an enzyme inducer.
Pharmacodynamics
- Efficacy of a drug refers to the maximum response it can produce.
- Inverse agonist is a drug that binds to a receptor and causes an action opposite to that of an agonist.
Pharmacogenomics
- Pharmacogenomics is the study of how variations in the human genome affect the response to medications.
Dose-Response Curve
- A graded DRC shows the variation in sensitivity of response to increasing doses of a drug in different individuals.
- In competitive inhibition, Km increases, and Vmax remains unchanged.
- In non-competitive inhibition, Vmax decreases, and Km remains unchanged.
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