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Flashcards in MSS Drugs Deck (33):
1

2

Aspirin MOA

irreversibly inhibits COX by covalent acetylation; this decreases synthesis of TXA2 and prostaglandins

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Decreased synthesis of TXA2 and prostaglandins leads to...

increased bleeding time until new platelets are produced (7 days).

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Low dose Aspirin (

decreased platelet aggregation

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Intermediate dose (300-2400) Aspirin use

antipyretic and analgesic

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High dose (2400-4000) Aspirin use

anti-inflammatory

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Aspirin toxicity

gastric ulceration and tinnitus

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Chronic use of Aspirin leads to...

acute renal failure, interstitial nephritis and upper GI bleeding.

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Aspirin can also stimulate respiratory centers leading to...

hyperventilation and respiratory alkalosis.

10

Indomethacin is..

an NSAID used to close a PDA.

11

NSAIDs cause gastric ulcer bc...

prostaglandins protect the gastric mucosa.

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NSAIDs cause... renal ischemia bc...

PGs vasodilate the afferent arteriole.

13

Celecoxib is...

a COX-2 inhibitor

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COX-2 is found in...

inflammatory cells and vascular endothelium. It mediates inflammation and pain.

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Celecoxib spares...

COX1 which helps maintain the gastric mucosa. And spares platelet fxn because TXA2 production is dependent on COX1.

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Use of Celecoxib

RA and osteoarthritis; pts with gastritis or ulcers

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Toxicity of Celecoxib

-increased risk of thrombosis -sulfa allergy

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Acetaminophen MOA

reversibly inhibits COX, mostly in CNS; inactivated peripherally

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Use of acetaminophne

antipyretic, analgesic, but not anti-inflammatory; use instead of aspirin to avoid Reye

20

Toxicity of Acetaminophen

hepatic necrosis - a metabolite (NAPQI) depletes glutathione and forms toxci tissue adducts in liver

21

Antidote to Acetaminophen induced Hepatotoxicity is...

N-acetylcysteine - it regenerates glutathione

22

Bisphosphonates (Aledronate) MOA

pyrophosphate analogs; binds hydroxyapatite in bone, inhibiting osteoclast activity

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Use of Bisphosphonates

-osteoporosis -hypercalcemia -Paget disease of bone

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Toxcity of Bisphosphonates

-corrosive esophagitis -osteonecrosis of the jaw

25

Allopurinol acts by...

inhibiting xanthine oxidase, which decreases the conversion of xanthine to uric acid.

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Additional use of Allopurinol

in lymphoma and leukemia to prevent tumor lysis-associated urate nephropathy

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Chronic gout drugs

-Allopurinol -Febuxostat -Probenecid

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Febuxostat

inhibits xanthine oxidase

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Probenecid

inhibits reabsorption of uric acid in the PCT

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Acute gout drugs

-NSAIDs (naproxen, indomethacin) -Glucocorticoids -Colchicine -TNF-alpha inhibitors (Etanercept, Infliximab, Adalimumab)

31

Colchicine acts by...

binding and stabilizing tubulin to inhibit microtuble polymerization, impairing leukocyte chemotaxis and degrunlation

32

Etanercept is a...

fusion protein (TNF-alpha inhibitor) used in RA, psoriasis, ankylosing spodylits and gout.

33

Infliximab/Adalimumab is an...

anti-TNFalpha monoclonal antibody used for IBD, RA, ankylosing spondylitis, psoriasis and gout