Metabolism Flashcards
Microsomal enzyme inducers
Examples of inducing agents:
1-phenytoin, phenobarbitone, carbamazepine, rifampicin,,
Example of inducing agent
• Clinical examples:
2- Phenytoin accelerates metabolism of cyclosporine-A (CS-A) leading to graft rejection
Examples of inhibiting agents
Examples of inhibiting agents:
1-macrolide antibiotics (eg erythromycin), ciprofloxacin, cimetidine,
Clinical examples of microsomal enzyme inhibitors
Clinical examples:
1-Ciprofloxacin inhibits metabolism of warfarin (anticoagulant) leading to accumulation of warfarin and bleeding
First pass metabolism is ……
Pre systemic elimination
Drug have complete first pasd metabolism
Lidocaine
Drug have patrial first pass metabolism
Propranolol, morphine ,nitroglycerine
Drugs don’t have first pass metabolism
Atenolol,mononitrates
Conversion of active drug into Inactive(example)
metabolites»>
ما النتائج ؟
termination of
drug effect.
انتهاء تأثير الدواء (most drugs)
Conversion of active drug into active metabolites→(name6 example,
Prodrugs,
Coidene to morphine
Conversion of inactive drug to active drug
Enalapril to enalaprilate
Conversion of non toxic drug to toxic drug
Paracetamol
Phase 1 metabolism (include - occured by )
Reduction
Hydrolysis
Cytochrome P450 (cyp450) enzyme
Genetic polymorphism
•Some drugs and environmental substances can induce or inhibit certain cyp450 enzymes G leading to significant drug interactions
Phase 2 include
Conjugation by glucuronic acid.
Paracetamol toxicity occur with
Glutathione