4th Flashcards
Where does drug metabolism occur
Liver,intestinal lumen,lung,plasma,skin,kidney
The most important reaction in metabolism phase 1
Oxidation by cytochrome p450
Most important conjure reaction
Glucuronide conjunction
Cytochrome p450 oxidases
Hepatic microsomal enzymes
Phase 1 oxidation reaction»_space;xanthine oxidase
Converts xanthine >uric acid
Phase 1 oxidation reaction monoamine oxidase
Oxidizes catecholamines & serotonin
Phase 1 reduction nitroreductase
> > chloramphenicol
Phase 1 reduction carbonyl reductase
> > naloxone
Phase 1 hydrolysis cholinestrase
Ach
Phase 1 hydrolysis peptidase
> > insulin
What consequence of phase 1 occurs with most drugs
Active drugs»>inactive drugs
E.g on converting inactive drug(prodrugs)»active drug
Cortisone»_space;cortisol (hydrocortisone)
Eg on converting active drug»another active drug
Codeine»morphine
E.g on converting active drug»_space;toxic metabolite
Methanol»_space;formaldehyde»_space;retinotoxic
Paracetamol»_space;NAPQI»hepatotoxic
Glucuronide conjunction:Drugs that enter the enterohepatic circulation
Estrogen (contraceptive pills are taken once daily)