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WorksheetsPharmacology Quiz
Total questions: 20
Worksheet time: 10mins
Biotransformation means:
Drug elimination by kidney
Conversion of drug to active/inactive metabolites
Drug distribution
Protein binding
Primary site of drug metabolism:
Kidney
Liver
Skin
Lungs
Phase 1 reactions mainly involve:
Conjugation
Oxidation–reduction–hydrolysis
Glucuronidation
Sulfation
Most common Phase 1 enzyme system:
MAO
CYP450
Cyclooxygenase
Tyrosine kinase
Phase 2 reactions involve:
Hydrolysis only
Conjugation reactions
Oxidation only
Deamination
Example of Phase 2 reaction:
Oxidation
Glucuronidation
Hydrolysis
O-dealkylation
Prodrug is:
Inactive compound converted to active form in body
Active drug with long half-life
Only topical drug
Non-metabolized drug
Example of a prodrug:
Morphine
L-Dopa
Lidocaine
Aspirin
Purpose of prodrug:
Increase toxicity
Improve pharmacokinetics & absorption
Block receptors
Increase protein binding
CYP450 induction leads to:
Reduced metabolism
Increased metabolism
No change in metabolism
Immediate toxicity
Enzyme induction effect on other drugs:
Increases their half-life
Decreases their action
Prevents clearance
Has no effect
Typical enzyme inducer:
Erythromycin
Rifampicin
Cimetidine
Ketoconazole
Typical enzyme inhibitor:
Rifampicin
Carbamazepine
Cimetidine
Phenobarbital
Phase 1 reaction outcome:
Usually makes drug more lipophilic
Usually makes drug more polar
Always inactivates drug
Always activates drug
Phase 2 conjugation increases:
Lipid solubility
Water solubility
Protein binding
Receptor affinity
First-pass metabolism primarily affects:
IV drugs
Oral drugs
Topical drugs
Inhalational drugs
Microsomal enzymes are located in:
Mitochondria
Nucleus
Rough ER
Smooth ER
Enzyme induction may lead to:
Drug toxicity
Enhanced clearance of drugs
Prolonged drug effect
Reduced metabolism
Drug most affected by microsomal enzyme induction:
Warfarin
Heparin
Amoxicillin
Insulin
Phase 2 reaction requiring acetylation occurs with:
Aspirin
Isoniazid
Morphine
Digoxin
