Drug Disposition II

Question 1

Effects of Biotransformation

Answer 1

Changes the response of the body to drugs

Question 2

Prodrugs

Answer 2

A medication or compound that is metabolized into a pharmacologically active drug after administration

Question 3

Sites of drug biotransformation

Answer 3

LIVER
Kidneys
Respiratory Tissues (nose, lungs)
Brain
Skin
Heart

Question 4

Two phases of Drug Metabolism

Answer 4

Phase I: (non-synthetic)
Oxidation and Reduction to add or unmask functional groups

Phase II: (synthetic)
Conjugation and coupling to endogenous molecules to increase polarity, making it more water soluble, and bulky moiety, usually rendering it inactive

Question 5

MFOs

Answer 5

Mixed Function Oxidases:

Inclusive of Flavin Monooxygenases and Cytochrome P450s (CYPs)

Use 2 electrons from NADPH plus molecular oxygen to metabolize drugs

Question 6

Glucuronidation

Answer 6

Most common Phase II congugation pathway often excreted in the bile

Question 7

Types of congugation pathways

Answer 7

Acetylation
Sulfation
Methylation
Glutathion Congugation (to keep from reactivity)

Question 8

Enzyme CYP2A6

Answer 8

Inactivates Nicotine
Not used clinically
Increases tolerance

Question 9

Enzyme CYP2C9

Answer 9

Inativates