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Flashcards in Pharm MS Deck (18):
1

Describe the formation/pathway and function of:
LTC,D,E4:
LTB4
PGI2:
PGE1:
PGE2:
PGF2:
TXA2:

Phospholipase A2 converts membrane phospholipids into Arachidonic acid.
Lipoxygenase converts AA into 5-HPETE then into LTC,D,E4 and LTB4
COX-1,2 convert AA into prostacyclin, prostaglandins, and thromboxane.

LTC,D,E4: Incr. bronchial tone
LTB4: Incr. neutrophil chemotaxis
PGI2: Decr. platelet aggregation, decr. vasc. tone
PGE1: Decr. vascular tone
PGE2: incr. uterine tone
PGF2: incr. uterine tone
TXA2: Incr. platelet aggregation, incr. vascular tone

2

What is the mechanism of acetaminophen? Where is it inactivated? Clinical use? Toxicity? Antidote?

Reversibly inhibits COX, mostly in CNS
Inactivated peripherally

Antipyretic, analgesic
Not antiinflammatory
Used instead of aspirin to avoid Reye syndrome

Overdose leads to hepatic necrosis; NAPQI depletes glutathione and forms toxic tissue byproducts in liver

N-acetylcysteine: regenerates glutathione

3

What ist he mechanism of aspirin? Clinical use/doses? Toxicity? Chronic toxicity? Overdose?

Irreversibly inhibits COX via acetylation
Decr. synth of TXA2 and PGs
Incr. bleeding time
No effect on PT/PTT

Low dose=decr. platelet aggregation
Intermediate=antipyretic, analgesic
High=antiinflammatory

Gastric ulceration, tinnitus

Acute renal failure, interstitial nephritis
Reye syndrome

Resp alk early, the to mixed.

4

What is the mechanism of celecoxib? How does it differ from NSAIDs in affects? Clinical use? toxicity?

Reversibly inhibits COX 2, found in inflammatory cells and vasc endothelium and mediates inflammation and pain; spares COX-1 which helps maintain the gastric mucosa.
No corrosive effects on GI lining and spares platelet function.

RA, osteoarthritis

Incr. risk of thrombosis, sulfa allergy

5

What type of drugs are ibuprofen, naproxen, indomethacin (1), ketorolac, diclofenac? mechanism? Clinical use ? Of 1? Toxicity?

NSAIDS

Reversibly inhibit COX. Block PG synth

Antipyretic, analgesic, antiinflammatory
1=used to close PDA

Interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate afferent arteriole)

6

What type of drug is alendronate? Mechanism? Clinical use? Toxicity?

Bisphosphonate

Pyrophosphate analog; bind hydroxyapatite in bone, inhibiting osteoclast activity

Osteoporosis, Hypercalcermia, Paget disease of bone

Corrosive esophagitis (take with water, remain upright for 30 min)
Osteonecrosis of jaw

7

What is the mechanism of teriparatide? clincal use? Toxicity?

Recombinant PTH analog given subQ daily.
Incr. osteoblast activity

Osteoporosis
Incr. bone growth compared to antiresorptive therapies

Transient hypercalcemia. May increase risk of osteosarcoma

8

What are the chronic gout drugs? Acute gout drugs? What should be avoided in acute gout?

Allopurinol
Febuxostat
Pegloticase
Probenecid

NSAIDS
Glucocorticoids
Colchicine

Salicylates

9

What is the mechanism of allopurinol? Clinical uses? Drug interactions?

Inhibits XO after being converted to alloxanthine
Decr. conversion of xanthine to uric acid

Chronic gout
Lymphoma and leukemia to avoid lysis associated urate nephropathy

Incr. conc. of azathioprine and 6MP (metabolized by XO)

10

What is the mechanism of febuxostat? Clinical use?

Inhibits XO

Chronic gout

11

What is the mechanism of pegloticase? Use?

Recombinant uricase that catalyzes metabolism of uric acid to allantoin (more water soluble)

Chronic gout

12

What is the mech of probenecid? Use? sx?

Inhibits absorption of uric acid in PCT (also secretion of penicillin)

Can precipitate uric acid calculi

13

What are the NSAIDS used for acute gout?

Naproxen, indomethacin

14

What is admin of glucocorticoids like in acute gout?

oral or intra articular

15

What is the mechanism of colchicine? Sx? Uses?

Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation.

Acute and prophylactic value

16

What is the mechanism of colchicine? Sx? Uses?

Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation.

Acute and prophylactic value

17

What type of drug is etanercept? Mechanism? Clinical use? Side effects?

TNF-alpha inhib

Fusion protein (TNF-alpha receptor +IgG Fc) produced by recombinant DNA
TNF decoy receptor

RA, psoriasis, ankylosing spondylitis

Predispose to infection, especially reactivation of latent TB.
TNF important in granuloma formation and stabilization.

18

What type of drug is infliximab and adalimumab? Clinical use? Toxicity?

Anti TNF alpha monoclonal antibody

IBD, RA, ankylosing spondylitis, psoriasis

Predispose to infection, especially reactivation of latent TB.
TNF important in granuloma formation and stabilization.