Slide 6 GI

What is the relationship between bulky structure/double bonds and potency? A. More bulky/double bonds decrease potency B. More bulky/double bonds increase potency C. Bulky structure has no effect on potency D. Only single bonds affect potency

B. More bulky/double bonds increase potency

What is the effect of bulky structure/double bonds on activity? A. They increase activity B. They have no effect on activity C. They decrease activity D. They convert compounds into inactive metabolites

C. They decrease activity

What is the effect of a halogen substitution at carbon 9 on activity? A. Decreases activity B. Has no effect C. Increases activity D. Causes rapid metabolism

C. Increases activity

High-activity steroids are associated with which physiological effect? A. Decreased glucose levels B. Increased Na⁺ and water retention C. Increased potassium excretion only D. Decreased blood pressure

B. Increased Na⁺ and water retention

What are the two components derived from the prodrug Sulfasalazine? A. Methotrexate and mesalamine B. Sulfapyridine and 5-ASA C. Prednisolone and prednisone D. Azathioprine and mercaptopurine

B. Sulfapyridine and 5-ASA

How is Prednisolone activated in the body? A. By hydrolysis in the stomach B. By renal excretion C. By Cytochrome P450 dehydrogenation D. By bacterial metabolism in the colon

C. By Cytochrome P450 dehydrogenation

Cyp-mediated metabolism corresponds to which phase of drug metabolism? A. Phase 0 B. Phase 1 C. Phase 2 D. Phase 3

B. Phase 1

How does having two double bonds in the A ring of steroids like Prednisone/Prednisolone affect the drug? A. Decreases potency B. Has no effect C. Decreases specificity D. Increases potency and specificity

D. Increases potency and specificity

What is the effect of having a ketone instead of a hydroxyl group in steroid structure? A. Decreases potency B. Increases potency C. Eliminates activity D. Prevents metabolism

B. Increases potency

Which 5-ASA compound is NOT a prodrug? A. Mesalamine B. Sulfapyridine C. Sulfasalazine D. Prednisolone

A. Mesalamine

What is the mechanism of action of 5-ASA compounds like Mesalamine? A. Protein synthesis inhibition B. DNA replication inhibition C. Prostaglandin synthesis inhibition D. Purine synthesis inhibition

C. Prostaglandin synthesis inhibition

What is the mechanism of action of sulfapyridine (a metabolite of Sulfasalazine)? A. Folate synthesis inhibition B. Purine synthesis inhibition C. DNA polymerase inhibition D. Calcineurin inhibition

B. Purine synthesis inhibition

What is the mechanism of action of Methotrexate? A. Inhibits calcineurin B. Inhibits dihydrofolate reductase (DHFR) C. Inhibits HGPRT D. Inhibits prostaglandin synthesis

B. Inhibits dihydrofolate reductase (DHFR)

What is the mechanism of action of Cyclosporin? A. Inhibits DHFR B. Inhibits HGPRT C. Inhibits calcineurin → decreases IL-2 activation D. Inhibits purine synthesis directly

C. Inhibits calcineurin → decreases IL-2 activation

What is the mechanism of action of Mercaptopurine? A. Inhibits calcineurin B. Inhibits HGPRT C. Inhibits DHFR D. Inhibits prostaglandin synthesis

B. Inhibits HGPRT

What is the mechanism of action of Azathioprine? A. Folate antagonist B. Calcineurin inhibitor C. Purine antagonist (antimetabolite affecting AMP and GMP synthesis) D. Prostaglandin inhibitor

C. Purine antagonist (antimetabolite affecting AMP and GMP synthesis)