23 Questions
What is the main mechanism of drug elimination through biotransformation?
Either phase I or phase II reactions
Where are the specific enzyme systems that catalyze metabolism located?
Liver
What is the effect of biotransformation on the pharmacologic action of the parent drug?
It terminates the action
What is the term for the process where a more toxic metabolite is produced?
Lethal synthesis
What is the term for a drug that is biotransformed into a pharmacologically active metabolite?
Prodrug
What is the effect of biotransformation on the biological half-life of a drug?
It decreases the half-life
What is the reason for the increased incidence of toxicity with propranolol and lignocaine in elderly?
Decreased hepatic metabolism
What is the term for the study of genetically determined variation in drug response?
Pharmacogenetics
What is the result of chronic diseases of liver on hepatic metabolism of some drugs?
Decreased metabolism
Why do neonates conjugate chloramphenicol more slowly?
Due to decreased activity of hepatic microsomal enzymes
What is the characteristic of fast acetylators of isoniazid?
Hepatotoxicity and require larger dose of the drug
What is the result of atypical pseudocholinesterase metabolizing succinylcholine?
Prolonged apnea due to paralysis of respiratory muscles
What is the effect of poor nutrition on enzyme function?
Decrease enzyme function
What is the importance of G6PD activity in RBCs?
To maintain the integrity of RBCs
What is the effect of simultaneous administration of drugs on drug metabolism?
Can result in increased or decreased metabolism
Where are the drug-metabolizing enzyme systems localized?
In the liver microsomes
What is the effect of enzyme induction and enzyme inhibition on drug interactions?
They represent the major sites of drug interactions
What type of factors play an important role in regulating the activity of drug-metabolizing enzyme systems?
Environmental factors
What is a known factor that stimulates the activity of drug-metabolizing enzymes in the liver microsomes?
Hormonal changes in the body
What is the purpose of pretreating the second mouse with phenobarbitone in Experiment 1?
To induce the enzyme responsible for thiopental biotransformation
What is the effect of starvation on the biotransformation of thiopental?
It inhibits the biotransformation
What is the outcome of pretreating the mouse with an enzyme inducer such as phenobarbitone?
It decreases the duration of action of thiopental
What is the dose of thiopental administered to the mice in Experiment 1?
100 mg/kg
This quiz covers the process of drug biotransformation, its effects on drug activity, and the impact of environmental factors on metabolism. It also explores the simultaneous administration of drugs and their effects on microsomal enzymes, including enzyme induction and inhibition.
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