Musc Pharm Flashcards
Aspirin: mech
Irreversibly inhibits COX1 and COX2 by covalent acetylation, which decreases synthesis of TXA2 and prostaglandins.
Increases bleeding time until new platelets are produces (~7days)
No effect on PT, PTT.
Aspirin: uses
Low dose (
Aspirin: tox
Gastric ulceration, tinnitus (CN VIII)
Chronic use can lead to acute renal failure, intersitial nephritis, and upper GI bleeding.
Risk of Reye syndrome in children treated with aspirin for viral infection.
Stimulates respiratory centers, causing hyperventilation and respiratory alkalosis
Aspirin: tox
Gastric ulceration, tinnitus (CN VIII)
Chronic use can lead to acute renal failure, intersitial nephritis, and upper GI bleeding.
Risk of Reye syndrome in children treated with aspirin for viral infection.
Stimulates respiratory centers, causing hyperventilation and respiratory alkalosis
NSAIDS:
Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac
NSAIDS mech:
Reversibly inhibit COX1 and COX2. Block PG synthesis
NSAIDS use:
antipyretic, analgesic, anti-inflammatory.
Indomethacin - used to close a PDA
NSAIDS tox:
Interstitial nephritis, gastric ulcer (PG’s protect gastric mucosa), renal ischemia (PGs vasodilate afferent arteriole)
COX-2 Inhibitors (celecoxib) mech:
Reversibly inhibit COX2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain;
spares COX1, which helps maintain gastric mucosa
Should not have corrosive effects of other NSAIS on GI lining. Spares platelet function as TXA2 production is dependent on COX-1
Celecoxib uses:
RA and osteoarthritis; pts with gastritis or ulcers
Celecoxib tox:
increased risk of thrombosis.
Sulfa allergy
Acetaminophen mech:
Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally
Acetaminophen use:
Antipyretic, analgesic, but not anti-inflammatory. Used instead of aspirin to avoid Reye syndrome in children with viral infection
Acetaminophen tox:
Overdose produces hepatic necrosis; acetaminophen metabolite (NAPQI) depletes glutathione and forms toxic tissue adducts in liver.
N-acetylcysteine is antidote - regenerates glutathione
Bisphosphonates:
Alendronate, other -dronates
Alendronate: mech
Pyrophosphate analog; bind hydroxyapatite in bone, inihibiting osteoclast activity
Alendronate: uses
Osteoporosis, hypercalcemia, Paget disease of bone
Alendronate toxx:
Corrosive esophagitis (pts advised to take with water and remain upright for 30 min), osteonecrosis of jaw
Alendronate toxx:
Corrosive esophagitis (pts advised to take with water and remain upright for 30 min), osteonecrosis of jaw
Allopurinol: mech
Chronic gout (preventative) Inhibits xanthine oxidase, decreasing the conversion of xanthine to uric acid
Allopurinol: uses
Chronic gout
Lymphoma and leukemia (to prevent tumor lysis syndrome associated urate nephropathy)
Allopurinol: tox
Increases concentrations of Azathioprine and 6-MP (both normally metabolized by xanthine oxidase)
Do not give salicylates; all but highest doses depress uric acid clearance. Even high doses (5-6 g/day) have only minor uricosuric activity
Febuxostat: mech
Inhibits xanthine oxidase
Febuxostat: uses
Chronic gout (preventative)
Probenecid: mech
Inhibits reaborption of uric acid in PCT (also inhibits secretion of penicillin)
Probenecid: uses
Chronic gout (preventative)
NSAIDS for Acute Gout:
Naproxen, indomethacin
Glucocorticoids for acute gout:
oral or intraarticular
Colchicine: mech
Binds and stabilizes tubulin to inihibit microtubule polymerization, impairing leukocyte chemotaxis and degranulation.
Colchicine: uses
Acute and prophylactic Gout use
Colchicine: tox
GI side effects
Colchicine: mech
Binds and stabilizes tubulin to inihibit microtubule polymerization, impairing leukocyte (neutrophil) chemotaxis and degranulation (anti-inflammatory)
Colchicine: tox
GI side effects
Teriparatide: mech
Recombinant PTH analog given subQ daily.
Increases osteoblastic activity
Teriparatide: uses
Osteoporosis. Causes increased bone growht compared to anti resorptive therapies (bisphosphonates)
Teriparatide: tox
Transient hypercalcemia. May increase risk of osteosarcoma (seen in rodent studies)
TNF alpha inhibitors: general
All TNF alpha inhibitors predispose to infection, including reactivation of latent TB, since TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes.
Etanercept: mech
Fusion protein (receptor for TNF-alpha + IgG1 Fc), produced by recombinant DNA EtanerCEPT is a TNF decoy reCEPTor
Etanercept uses:
RA, psoriasis, ankylosing spondylitis
Infliximab mech:
Anti-TNF-alpha monoclonal Ab
Infliximab use:
IBD, RA, ankylosing spondylitis, psoriasis
Adalimumab: mech
Anti-TNF-alpha monoclonal Ab
Adalimumab: use
IBD, RA, ankylosing spondylitis, psoriasis
Adalimumab: use
IBD, RA, ankylosing spondylitis, psoriasis
Pegloticase: mech
Recombinant uricase that catalyzes metabolism of uric acid to allantoin (more H20-soluble product)
Pegloticase: use
Chronic gout (prevention
