MSK

Question 1

Allopurinol

[MOA, use]

Answer 1

For chronic gout; also lymphoma, leukemia.
>Inhibits xanthine oxidase – dec. conversion of xanthine to uric acid
>Can inc. azathioprine and 6-MP concentrations (metabolized by xanthine oxidase).

Question 2

Febuxostat

[MOA, use]

Answer 2

For chronic gout.
>Inhibits xanthine oxidase – dec. conversion of xanthine to uric acid.
>Can Inc. conc. of azathioprine, 6-MP.

Question 3

Pegloticase

[MOA, use]

Answer 3

For chronic gout.
Recombinant uricase (uric acid --> allantoin --> more H20-soluble).

Question 4

Probenecid

[MOA, use]

Answer 4

For chronic gout.
>Inhibits reabsorption of uric acid in PCT.
>Precipitates uric acid calculi.

Question 5

NSAIDs

Drug names

Answer 5

Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac

Question 6

NSAIDs

MOA

Answer 6

Reversibly inhibits COX-1, COX-2 – blocks PG synthesis

Question 7

NSAIDs

Clinical use

Answer 7

Antipyretic, analgesic, anti-inflammatory.
>Indomethacin: close PDA.
>Ibuprofen, naproxen: acute gout.

Question 8

NSAIDs

Toxicity

Answer 8

Interstitial nephritis.
Gastric ulcers (PGs protect gastric mucosa).
Renal ischemia (PGs vasodilate afferent arteriole).

Question 9

Acetaminophen

[MOA, clinical use]

Answer 9

> Reversibly inhibits COX (mostly in CNS).
Antipyretic, analgesic; Not anti-inflammatory.
Use in kids w/ viral infxn to avoid Reye syndrome (aspirin).

Question 10

Aspirin

MOA

Answer 10

> Irreversibly inhibits COX-1, COX-2 via acetylation.

>Dec. synthesis of TXA2, PGs – Inc. bleeding time.

Question 11

Aspirin

Clinical use

Answer 11

> Low dose (300mg/day): dec. platelet aggregation.
Intermediate (300-2400): analgesic, antipyretic.
High (2400-4000): anti-inflammatory.

Question 12

Aspirin

Toxicity

Answer 12

Gastric ulcer
Tinnitus (CNVIII)
>Chronic use: ARF, interstitial nephritis, GI bleed.
*Risk Reye syndrome in kids w/ viral infxn.

Question 13

Celecoxib

MOA

Answer 13

> Reversibly inhibits COX-2 (inflammatory cells, vascular endothelium) – Mediates inflammation, pain.
Spares COX-1 – gastric mucosal protection.
Spares TXA2 – platelet function.

Question 14

Celecoxib

Clinical use

Answer 14

Rheumatoid arthritis

osteoarthritis

Question 15

Celecoxib

Toxicity

Answer 15

> Increase risk of thrombosis – dec. PGI2, w/c normally dec. platelet aggregation; normal TXA2, w/c inc. platelet aggregation.
Sulfa allergy.

Question 16

Bisphosphonates

Drug names

Answer 16

Alendronate, other -dronates

Question 17

Bisphosphonates

MOA

Answer 17

Pyrophosphate analogs

Bind hydroxyapatite in bone – inhibits osteoclast activity.

Question 18

Bisphosphonates

Clinical use

Answer 18

Osteoporosis
Hypercalcemia
Paget disease of bone

Question 19

Bisphosphonates

Toxicity

Answer 19

> Corrosive esophagitis (take water and remain upright for 30 mins).
Osteonecrosis of jaw.

Question 20

Colchicine

[clinical use, MOA, CI]

Answer 20

> For acute gout.
Inhibits microtubule polymerization – impairs neutrophil chemotaxis and degranulation.
CI: Don’t give salicylates – depress uric acid clearance.

Question 21

Etanercept

[Use, MOA, SE]

Answer 21

> For Rheumatoid arthritis, psoriasis, ankylosing spondylitis.
Fusion protein (Receptor for TNF-alpha + IgG1-Fc) – TNF decoy receptor.
SE: predispose to infection (reactivated TB).

Question 22

Teriparatide (PTH analog)

[MOA, use]

Answer 22

> Inc. osteoblastic activity.
For osteoporosis – inc. bone growth.
SE: transient hypercalcemia

Question 23

Infliximab, Adalimumab

[MOA, use]

Answer 23

> Anti-TNF-alpha monoclonal antibody.

>For IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis.