Drug Metabolism Flashcards
Mention 5 consequence of metabolism ?
- Pharmacological inactivation
- Bioactivation or toxicological activation
- Pharmacological activation
- Change in pharmacological activity
- Lethal synthesis
Major organ of drug bio transformation?
Liver
Give an example of a drug that undergoes non enzymatic metabolism and explain how ?
Atracurium : through molecular re-arrangement
Microsomal enzymes activity requires?
NADPH and oxygen
Microsomal enzymes are located where ?
Smooth endoplasmic reticulum
Non Microsomal enzymes undergoes all phase 2 reactions except?
Glucoronidation
Functionalization reaction is what phase of metabolism ?
Phase 1
How many p450 enzymes are identified in human liver microsomes ?
15
Mention 2 examples of drugs that undergoes auto induction?
Carbamazepine and rifampicin
Mention 5 clinical importance of enzyme induction?
- Decease plasma level and therapeutic effect of a drug
- Reduce half life of a drug
- Reduce potency and efficacy of a drug
- Increase change of drug interactions
5.enhance drug tolerance - Increase drug toxicity
How does propranolol reduce the rate of metabolism of lignocaine ?
By reducing hepatic blood flow
Mention the 3 major factors affecting drug metabolism ?
- Physicochemical properties of drugs
- Chemical factors
- Biological factors
Explain how sex affect drug metabolism ?
Metabolism is higher in males due to high GFR
Explain the effect of of age in drug metabolism ?
Metabolism reduce with age cause of reduction in liver mass and liver blood flow which leads to reduction in first pass metabolism which lead to higher absorption but lower metabolism
Mention two properties of non Microsomal enzymes ?
- Non inducible
- May show genetic variation