NSAIDS/DMARDS/GOUT Flashcards
(53 cards)
MOA PARACETAMOL
Selectively inhibits COX-3. Weak COX-1 and COX-2
inhibitor. Inhibits prostaglandin synthesis
Preferred antipyretic in children
Paracetamol
Mechanism of Paracetamol Overdose
Oxidation to a cytotoxic intermediate called N-acetyl-p-benzoquinoneimine
(NAPQI) by phase I CYP450 enzymes (CYP2E1)
Antidote of Paracetamol toxicity?
antidote is N-acetylcysteine (NAC), a sulfhydryl donor necessary
for detoxification of paracetamol.
Development of Paracetamol Overdose 24-48 hrs, what manifestation?
Hepatic injury
Development of Paracetamol Overdose 3-5 days, what manifestation?
Extremely high liver enzymes (>10,000 IU/L)
Maximal abnormalities and hepatic failure
Jaundice, hepatic encephalopathy, renal failure,
myocardial injury
MOA ASPIRIN (Acetylsalicylic acid, ASA), Salsalate,
Sodium salicylate, Choline salicylate, Magnesium salicylate
Nonselective, IRREVERSIBLE COX 1&2 inhibitor.
Reduces platelet production of thromboxane A2, a
potent stimulator of platelet aggregation.
Associated with Reye’s syndrome in children
Prevents uric acid excretion (don’t use in gout)
SALICYLATES
ASPIRIN (Acetylsalicylic acid, ASA), Salsalate,
Sodium salicylate, Choline salicylate, Magnesium salicylate
Dose range of aspirin
* low range (<300 mg/d)
for?
o effective in reducing platelet aggregation
o follows first-order elimination kinetics
Dose range of aspirin
* intermediate doses (300–2400 mg/d)
for?
o antipyretic and analgesic effects
Dose range of aspirin
- high doses (2400–4000 mg/d)
for?
o anti-inflammatory effects
o follows zero-order elimination kinetics
MOA?
IBUPROFEN, Diclofenac, Diflunisal, Etodolac, Fenoprofen,
Flurbiprofen, KETOPROFEN, Nabumetone, Naproxen,
Oxaprozin, PIROXICAM, Sulindac, Tolmetin, MEFENAMIC ACID,
Bromfenac, Meclofenamate, Suprofen, Aceclofenac
NON SELECTIVE NSAIDS
- Reversible COX 1 and 2 Inhibition.
prevents NSAIDinduced
gastritis
MISOPROSTOL
NSAIDs (in general) may cause premature closure of
DUCTUS ARTERIOSUS
used to close PDA
Ibuprofen and Indomethacin
Post-surgical analgesic control (moderate to severe,
short-term), mainly used for analgesia not for antiinflammatory
effect
Ketorolac, Dexketoprofen
MOA?
CELECOXIB, Etoricoxib,
Rofecoxib, Valdecoxib, Parecoxib [X],
Selective COX-2 inhibitor.
which cox2 selective inhibitors are withdrawn from the
market due to increased incidence of thrombosis
Rofecoxib and Valdecoxib
Parecoxib is pregnancy category
Category X
MOA: Inhibits AICAR (5-Aminoimidazole-4-Carboxamide
Ribonucleotide) transformylase and thymidylate
synthetase, with secondary effects on
polymorphonuclear chemotaxis
METHOTREXATE
DMARD of first choice to treat rheumatoid arthritis
Methotrexate
MOA? Forms phosphoramide mustard, which cross-links
DNA to prevent cell replication. Suppresses T-cell and Bcell
function
Cyclophosphamide [D]
RESCUE AGENT FOR CYCLOPHOSPHAMIDE?
MESNA
MOA: Forms 6-Thioguanine, suppressing inosinic acid
synthesis, B-cell and T-cell function, immunoglobulin
production, and interleukin-2 secretion
AZATHIOPRINE
