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Flashcards in MSK Deck (23)
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1

Allopurinol
[MOA, use]

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).

2

Febuxostat
[MOA, use]

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

3

Pegloticase
[MOA, use]

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

4

Probenecid
[MOA, use]

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

5

NSAIDs
Drug names

Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac

6

NSAIDs
MOA

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

7

NSAIDs
Clinical use

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

8

NSAIDs
Toxicity

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

9

Acetaminophen
[MOA, clinical use]

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

10

Aspirin
MOA

>Irreversibly inhibits COX-1, COX-2 via acetylation.
>Dec. synthesis of TXA2, PGs -- Inc. bleeding time.

11

Aspirin
Clinical use

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

12

Aspirin
Toxicity

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

13

Celecoxib
MOA

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

14

Celecoxib
Clinical use

Rheumatoid arthritis
osteoarthritis

15

Celecoxib
Toxicity

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

16

Bisphosphonates
Drug names

Alendronate, other -dronates

17

Bisphosphonates
MOA

Pyrophosphate analogs
Bind hydroxyapatite in bone -- inhibits osteoclast activity.

18

Bisphosphonates
Clinical use

Osteoporosis
Hypercalcemia
Paget disease of bone

19

Bisphosphonates
Toxicity

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

20

Colchicine
[clinical use, MOA, CI]

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

21

Etanercept
[Use, MOA, SE]

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

22

Teriparatide (PTH analog)
[MOA, use]

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

23

Infliximab, Adalimumab
[MOA, use]

>Anti-TNF-alpha monoclonal antibody.
>For IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis.