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Flashcards in MSS drugs Deck (21):
1

Acetaminophen

REVERSIBLE COX inhibitor; CNS action;
inactivated peripherally

Use: Antipyretic, analgesic but not inflammatory
Used in place of Aspirin to prevent Reye syndrome in children with viral infection

Tox: Hepatic necrosis.
metabolite (NAPQI) depletes glutathione and forms toxic tissue byproducts in liver

Antidote for acetaminophen tox: N-Acetylcysteine - regenerates glutathione

2

Aspirin

IRREVERSIBLE inhibition of COX (1 and 2) by acetylation
-> decreased synthesis of TXA2(increases platelet aggregation and vasoconstricts) and PGs
Increased bleeding time; No effect on PT, PTT
Type of NSAID

Use: low dose: decrease platelet aggregation
intermediate dose: antipyretic and analgesic
High dose: anti-inflammatory

3

Aspirin toxicity

Gastric ulceration, tinnitis (CNVIII)
Chronic: Acute Renal failure, interstitial nephritis, GI bleeding

Risk of Reye in children with viral infection
Causes Resp alkalosis early but transitions to metabolic acidosis - respiratory alkalosis

4

Celecoxib

Reversible COX2 inhibitor
COX2 found in inflammatory cells and vascular endothelium and mediates inflammation and pain
Spares COX-1 -> helps maintain gastric mucosa
Spares platelet function; TXA2 produced by COX1

Use: RA, OA

Tox: increased risk of thrombosis; sulfa allergy

5

NSAIDs

Ibuprofen, Ketolorac, Indomethacin, naproxen, diclofenac

REVERSIBLY inhibits COX1 and 2
Blocks PG synthesis
Antipyretic, analgesic, anti-inflammatory
Indomethacin - closes PDA

6

PG functions

PGE1 - decrease vascular tone
PGE2 and F2 - increases uterine tone

PGI2 (prostacyclin) - inhibits platelet aggregation, vasodilation

7

NSAID toxicity

Interstitial nephritis, gastric ulcer (PGE1 protects gastric mucosa by stimulating bicarb secretion), renal ischemia (PGs vasodilate afferent arteriole)

8

AT2 and PG effect on renal arterioles

AT2 constricts efferent arteriole -> increases GFR

PGs dilates afferent arteriole

9

Bisphosphonates

Alendronate, dronates - Pyrophosphate analog

Inhibit osteoclast activity by binding hydroxyapatite in bone
Use: Osteoporosis, Hypercalcemia, Paget's disease

10

Teriparatide

Recombinant PTH analog (SubQ) -> increases osteoblast activity
Use: Osteoporosis (causes more bone growth than antiresorptive meds - bisphosphonates)

Tox: Transient hypercalcemia; increase risk for osteosarcoma

11

Uric acid prodcution

Nucleic acid/ Diet -> purines -> Hypoxanthine -> Xanthine via XO;
Xanthine -> plasma Uric acid via XO

12

Allopurinol

Inhibits Xanthine Oxidase -> decreased conversion of Hypoxanthine or xanthine to Uric acid

Use: lymphoma/leukemia -> prevent tumor lysis urate nephropathy

SE: increases concentration of 6MP and azathioprine (both metabolized by XO)

13

Febuxostat

Inhibit XO

14

Pegloticase

Uricase -> metabolizes Uric acid to allantoin (more water soluble product than uric acid)

15

Probenicid

Inhibits Uric acid and salicyclate (penicillin) reabsorption in PCT
Can precipitate uric acid calculi

16

Chronic gout drugs - preventive

Allopurinol, febuxostat, Pegloticase, Probenicid

17

Acute Gout drugs

NSAIDs - naproxn, indomethacin
Glucocorticoids - Oral or intra-articular
Colchicine

salicyclates CI!!! Because they depress uric acid clearance
except for high dose

18

Colchicine

Binds and stabilizes tubulin -> inhibit polymerization of microtubule-> impair neutrophil chemotaxis and degranulation
Acute and prophylactic

19

TNF alpha inhibitors

predispose to infection - esp reactivation of latent TB
since TNF is important in forming and stabilizing granuloma

20

Etanercept

Fusion protein of TNF-a and IgG1Fc - made by recombinant DNA
Decoy receptor
Use: RA, psoriasis, ankylosing spondylitis

21

Infliximab, adamlimumab

Anti-TNFa monoclonal antibody

Use: inflammatory bowel disease, RA, Ankylosing spondylitis, psoriasis