Test 3 Flashcards
Why can’t lipophilic drugs be excreted by the kidney?
Liver converts lipophilic drugs to hydrophobic metabolites that can be easily excreted by the kidney.
What are xenobiotics?
Toxins, foreign/unwanted molecules
What are enzymes?
Proteins in nature, speeds up reaction
What is a co-enzyme?
Non-protien, helper
Is prodrug active or inactive?
Inactive
Hydrolase
Hydrolysis of substrate
Ligases
Bond formation
Transferases
Transfer of group between molecules
Lyases
Elimination and addition reaction
Isomerases
Rearrangement reactions
Oxidoreductases
Oxidation or reduction
Steps of drug metabolism in liver?
- Toxic substances are presented to liver via portal circulation
- Liver modifies these substances by “first pass metabolism”
- Phase 1 reactions are catalyzed by cytochrome P-450 enzymes
- This includes oxidation, reduction, and hydrolysis
- Phase 2 reactions conjugate the substances. Once conjugated, the substance can be easily excreted.
What phase of drug metabolism is affected in old age?
Phases 1
What is intrinsic activity?
Drug’s ability to initiate response after binding to a receptor
What is an agonist?
Drug has an affinity for a receptor and stimulates it
What is an antagonist?
Drug has an affinity for a receptor but displays little or no intrinsic activity.
Two types of antagonist?
Competitive,non-competitive
Competitive Antagonist
Competes with agonist for receptor sites, occupies the receptor site = NO activity
Non-competitive antagonist
Binds to the site other than receptor site and changes the shape of receptor = NO activity
Phase 1 reaction
Oxidation, reduction, and hydrolysis
Phase 2 reactions
Conjugate the substances
Metabolic pathway
Sequence of chemical reactions
What happens during a metabolic pathway?
- Each reaction is catalyzed by a different enzyme
- he product of one reaction serves as the substrate for the next
Enzyme activity is regulated and can be inhibited.
True
How do feedback inhibition hinder metabolic pathways?
Inhibits an enzyme in the pathway so no product is available to feed the next reaction
How is drugs eliminated from plasma?
Urine/Bile, chemically converting to metabolites