Drug metabolism and renal excretion of drugs

Question 1

describe in outline phase 1 and phase 2 of drug metabolism?

Answer 1

phase 1-oxidation, reduction, and hydrolysis-

phase 2-conjugation

Question 2

what is the main organ of drug metabolism?

Answer 2

the liver -but the GI tract, lungs, and plasma also have activity

Question 3

What factors affect the tubular reabsorption of drugs and their metabolites?

Answer 3

Lipid solubility
polarity
urinary flow rate
urinary ph

Question 4

what is phase 1 and 2 of drug metabolism in detail?

Answer 4

Phase 1-oxidation, reduction and hydrolysis makes drugs more polar, adds a chemically reactive group (a handle) permitting conjugation (fictionalization)

Phase 2- Conjugation- adding an endogenous compound increasing polarity- with glucuonyl, sulphate, methyl, acetyl, glycyl, or glutathione groups

Question 5

does phase 1 and 2 of drug metabolism make drug compounds more/less polar? how does the resulting outcome affect the processing of the drug?

Answer 5

Phase 1 and 2 of drug metabolism makes the drug more polar thus decreasing lipid solubility and increasing elimination

Question 6

Phase 1 is catabolic or anabolic?

Answer 6

catabolic

Question 7

Phase 2 is anabolic. T/F?

Answer 7

True

Question 8

Where does phase 1 and phase 2 reactions take place?

Answer 8

in the liver

Question 9

What superfamily of microsomal proteins perform phase 1?

Answer 9

CYP450 -Cytochrome P 450

Question 10

What are the main gene families in the human liver?

Answer 10

CYP1, CYP2, CYP3

Question 11

What are the 3 phases involved in renal excretion?

Answer 11

1- glomerular filtration
2- active tubular secretion
3-passive reabsorption by diffusion across the tubular epithelium

Question 12

T/F- only unbound proteins can enter the filtrate via glomerular filtration?

Answer 12

True

Question 13

True or false? Clinically relevant urinary alkalinisation can be used to accelerate the excretion of aspirin (weak acid) in cases of overdose

Answer 13

True