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Questions and Answers
What is the consequence of grapefruit juice on enzymes?
What is the consequence of grapefruit juice on enzymes?
- Inhibits enzymes (correct)
- Activates enzymes
- Has no effect on enzymes
- Degrades enzymes
What occurs in individuals classified as 'poor metabolizers'?
What occurs in individuals classified as 'poor metabolizers'?
- Increased CYP2D6 function
- Enhanced drug metabolism
- Little or no CYP2D6 function (correct)
- Normal CYP2D6 function
Which enzyme is responsible for metabolizing ethanol?
Which enzyme is responsible for metabolizing ethanol?
- Monooxygenase
- Alcohol dehydrogenase (correct)
- Xanthine oxidase
- Cytochrome P450
What happens in individuals classified as 'ultrarapid metabolizers'?
What happens in individuals classified as 'ultrarapid metabolizers'?
How does suxamethonium get metabolized?
How does suxamethonium get metabolized?
Which enzyme inactivates 6-mercaptopurine?
Which enzyme inactivates 6-mercaptopurine?
Which type of bonds are less readily susceptible to hydrolytic cleavage in drug metabolism?
Which type of bonds are less readily susceptible to hydrolytic cleavage in drug metabolism?
In glucuronide conjugation, which chemical group is inserted into the substrate?
In glucuronide conjugation, which chemical group is inserted into the substrate?
What is the endogenous substrate for glucuronide conjugation among the following?
What is the endogenous substrate for glucuronide conjugation among the following?
Which enzyme is involved in glutathione conjugation?
Which enzyme is involved in glutathione conjugation?
Which type of substrates require no activation in glutathione conjugation?
Which type of substrates require no activation in glutathione conjugation?
What is the product of a reaction between R-CH2-X and GSH in glutathione conjugation?
What is the product of a reaction between R-CH2-X and GSH in glutathione conjugation?
Which type of inhibition involves the complex formation with Fe3+ form of haem iron of CYP3A4?
Which type of inhibition involves the complex formation with Fe3+ form of haem iron of CYP3A4?
Which drug is an example of competitive inhibition in the context of P450 inhibition?
Which drug is an example of competitive inhibition in the context of P450 inhibition?
Which compound is known for its mechanism-based inhibition involving suicide inhibition by covalently binding to the enzyme?
Which compound is known for its mechanism-based inhibition involving suicide inhibition by covalently binding to the enzyme?
Which drug causes microsomal enzyme induction and has the effect of increasing activity with repeated administration?
Which drug causes microsomal enzyme induction and has the effect of increasing activity with repeated administration?
Which compound exemplifies the concept of pro-drugs with deliberate design in drug delivery?
Which compound exemplifies the concept of pro-drugs with deliberate design in drug delivery?
Which drug interaction scenario is characterized by slow onset of induction and slow recovery, posing clinical issues?
Which drug interaction scenario is characterized by slow onset of induction and slow recovery, posing clinical issues?
Which process does NOT account for renal drug excretion?
Which process does NOT account for renal drug excretion?
How can one drug affect the rate of renal excretion of another?
How can one drug affect the rate of renal excretion of another?
Which factor can contribute to individual variation in renal drug excretion?
Which factor can contribute to individual variation in renal drug excretion?
Which condition leads to increased renal elimination of drugs?
Which condition leads to increased renal elimination of drugs?
What genetic condition is associated with suxamethonium?
What genetic condition is associated with suxamethonium?
What mechanism can one drug use to affect the rate of renal excretion of another?
What mechanism can one drug use to affect the rate of renal excretion of another?
Which organ is primarily responsible for drug metabolism?
Which organ is primarily responsible for drug metabolism?
What is the main type of reaction involved in Phase 1 drug metabolism?
What is the main type of reaction involved in Phase 1 drug metabolism?
Which enzyme system is known as the CYP450 monooxygenase system?
Which enzyme system is known as the CYP450 monooxygenase system?
What type of reactions are Phase 2 reactions in drug metabolism primarily associated with?
What type of reactions are Phase 2 reactions in drug metabolism primarily associated with?
Which group acts as a point of attack for the conjugating system in Phase 1 reactions?
Which group acts as a point of attack for the conjugating system in Phase 1 reactions?
What is required for a mixed-function oxidation reaction catalyzed by cytochrome P450 enzymes?
What is required for a mixed-function oxidation reaction catalyzed by cytochrome P450 enzymes?
Drug metabolism and elimination primarily occur in the kidneys.
Drug metabolism and elimination primarily occur in the kidneys.
The route of drug metabolism can significantly impact its pharmacological activity.
The route of drug metabolism can significantly impact its pharmacological activity.
Most drugs are hydrophilic and easily eliminated by the body.
Most drugs are hydrophilic and easily eliminated by the body.
The first-pass effect refers to the metabolism of a drug after it has entered the systemic circulation.
The first-pass effect refers to the metabolism of a drug after it has entered the systemic circulation.
Phase 1 reactions in drug metabolism involve primarily conjugation reactions.
Phase 1 reactions in drug metabolism involve primarily conjugation reactions.
Liver plays a minor role in drug elimination compared to other organs like lungs and intestines.
Liver plays a minor role in drug elimination compared to other organs like lungs and intestines.
Phase 1 reactions in drug metabolism are primarily anabolic in nature.
Phase 1 reactions in drug metabolism are primarily anabolic in nature.
Cytochrome P450 enzymes are exclusively found in the kidneys for drug metabolism.
Cytochrome P450 enzymes are exclusively found in the kidneys for drug metabolism.
Phase 2 reactions mainly occur in the liver and involve attachment of glucuronic acid, sulphate, and amino acids.
Phase 2 reactions mainly occur in the liver and involve attachment of glucuronic acid, sulphate, and amino acids.
The handle for conjugation in drug metabolism can be a carboxyl group.
The handle for conjugation in drug metabolism can be a carboxyl group.
Phase 1 enzymes are mainly located in the smooth endoplasmic reticulum (ER) of cells.
Phase 1 enzymes are mainly located in the smooth endoplasmic reticulum (ER) of cells.
CYP450 enzymes are a homogenous superfamily with identical substrate specificities.
CYP450 enzymes are a homogenous superfamily with identical substrate specificities.
Gestodene is an example of a mechanism-based inhibitor involving suicide inhibition.
Gestodene is an example of a mechanism-based inhibitor involving suicide inhibition.
Rifampicin, ethanol, and carbamazepine are examples of substances that cause P450 inhibition.
Rifampicin, ethanol, and carbamazepine are examples of substances that cause P450 inhibition.
Pro-drugs like aspirin are designed to have different effects in their metabolized forms.
Pro-drugs like aspirin are designed to have different effects in their metabolized forms.
Methanol and ethylene glycol are examples of drugs with metabolites that have similar effects as the parent compound.
Methanol and ethylene glycol are examples of drugs with metabolites that have similar effects as the parent compound.
Slow onset of induction and slow recovery are not clinical issues associated with selective enzyme induction.
Slow onset of induction and slow recovery are not clinical issues associated with selective enzyme induction.
Microsomal enzyme induction by carcinogenic chemicals can be exploited therapeutically.
Microsomal enzyme induction by carcinogenic chemicals can be exploited therapeutically.
Thrombosis can be a side effect of enzyme induction.
Thrombosis can be a side effect of enzyme induction.
Disulfiram inhibits the metabolism of ethanol.
Disulfiram inhibits the metabolism of ethanol.
Proton pump inhibitors like omeprazole can enhance the activity of clopidogrel.
Proton pump inhibitors like omeprazole can enhance the activity of clopidogrel.
Clopidogrel is an antiplatelet drug that can potentiate the effects of disulfiram.
Clopidogrel is an antiplatelet drug that can potentiate the effects of disulfiram.
Organic cation transporters (OCTs) are primarily involved in hepatic excretion of drugs.
Organic cation transporters (OCTs) are primarily involved in hepatic excretion of drugs.
Glucuronides can be hydrolyzed in the intestine, regenerating the active drug in enterohepatic circulation.
Glucuronides can be hydrolyzed in the intestine, regenerating the active drug in enterohepatic circulation.
Renal clearance involves the volume of plasma containing the amount of substance that is added to the body by the kidneys in unit time.
Renal clearance involves the volume of plasma containing the amount of substance that is added to the body by the kidneys in unit time.
Active tubular secretion is one of the processes that account for renal drug excretion.
Active tubular secretion is one of the processes that account for renal drug excretion.
Passive reabsorption refers to diffusion from the dilute tubular fluid back across tubular epithelium.
Passive reabsorption refers to diffusion from the dilute tubular fluid back across tubular epithelium.
Ethnicity does not play a role in individual variation in renal drug excretion.
Ethnicity does not play a role in individual variation in renal drug excretion.
Genetic variation can lead to plasma cholinesterase deficiency, affecting drug metabolism.
Genetic variation can lead to plasma cholinesterase deficiency, affecting drug metabolism.
Pregnancy leads to decreased renal elimination of drugs due to reduced renal blood flow.
Pregnancy leads to decreased renal elimination of drugs due to reduced renal blood flow.
Study Notes
- Metabolism is the process of converting chemicals to more polar metabolites, primarily occurring in the liver but can happen in all organs.
- Drug metabolism consists of two phases: Phase 1 (catabolic) involves oxidation, reduction, and hydrolysis, where sometimes the metabolites can be more toxic than the parent drug due to the introduction of reactive groups for conjugation.
- Phase 2 of drug metabolism is synthetic ('anabolic') and involves conjugation with groups like glucuronic acid, sulfate, amino acids, glutathione, and acetyl groups to inactivate products.
- Cytochrome P450 enzymes are crucial in Phase 1 metabolism, with different CYP enzymes having distinct substrate specificities and roles in oxidizing drug molecules.
- Not all drug oxidation involves P450 enzymes; for example, suxamethonium is metabolized by plasma cholinesterase and ethanol by alcohol dehydrogenase and CYP2E1.
- Phase 2 reactions involve conjugation reactions such as glucuronide conjugation, sulfate conjugation, methyl conjugation, and acetyl conjugation to attach chemical groups and inactivate substances.
- Factors like species differences, dietary components, environmental influences, and polymorphisms can impact the expression and regulation of drug-metabolizing enzymes like CYP450.
- Drug interactions, individual variations (ethnicity, age, pregnancy), genetic variations, and mechanisms of renal excretion play significant roles in determining drug metabolism, efficacy, and potential toxicity.
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Description
Test your knowledge of drug metabolism Phase II enzymes and conjugation reactions with this quiz. Learn about the hydrolytic cleavage of ester and amide bonds, reduction of ketones to alcohols, and the insertion of chemical groups like glucuronyl, sulphate, methyl, and acetyl. This quiz is based on the book 'Introduction to Drug Metabolism' by Gordon & Skett.
