Drug Metabolism Flashcards
(12 cards)
What’s the purpose of Drug metabolism?
To convert compounds into polar molecules that can be easily excreted
What is the primary goal of Phase 1 metabolism
To prepare the drug for phase 2 metabolism by creating sites for conjugation with endogenous molecules
What enzymes are involved in Phase 1 metabolism
Cytochrome P450 enzymes
What types of reactions occur in phase 1 metabolism?
Oxidation, Reduction and hydrolysis
What’s the result of Phase 1 metabolism
Formation of active metabolites, inactive metabolites and toxic intermediates
What does the formation of phase 1 metabolism depend on
nature of the drug and specific reactions involved
What is phase 2 metabolism also known as ?
Conjugation
What is Phase 2 metabolism
It’s the conjugation of phase 1 molecules with endogenous molecules to increase water solubility
What are the 2 enzyme systems that take place in phase 1 reactions
Microsomal mixed Function oxidases
Non-cytochrome oxidising enzymes
What are the CYP biotransformations?
Cytochrome P450 enzymes
What reactions take place with CYP biotransformations?
Dealkylation
N and S-oxidations
Deamination
Dehalogenation
Aliphatic and aromatic hydroxylation