NSAIDS, DMARDS and Hyperuricemia drugs Flashcards
Examples of DMARDs
- Methotrexate
- Azathioprine
- Penicillamine
- Hydroxychloroquine
- Chloroquine
- Organic gold compounds
- Sulfasalazine
Therapeutic goal of DMARDs
-Reduce disease activity
-Retard progression of arthritic tissue destruction
Effects of DMARDs may take how long to be evident
6weeks - 6months
Methotrexate is contraindicated in
Pregnancy and breastfeeding
Therapeutic action of sulfasalazine
- metabolised to sulfapyridine and 5-aminosalicylic acid
- decrease IgA and IgM rheumatoid factor production
- absorption is 10 - 20%
Actions of NSAIDs
Anti-inflammatory
Analgesic
Antipyretic
Antithrombotic
Prostanoids include
Prostaglandins
Prostacycline
Thromboxane A2
Prostanoids are synthesized from
Arachidonic acids derived from phospholipids
Enzyme responsible for synthesis of prostanoids
Prostaglandin endoperoxidase G/H synthase (cyclooxygenase)
Isoforms of COX
COX-1: housekeeping functions, expressed constitutively in most cells
COX-2: Principal source of prostanoid formation in inflammation and cancer
Function of PGI2
Inhibits platelet aggregation, vasodilation, vascular permeability
Function of PGE2
Pain, hyperalgia, heat, vasodilation, bronchoconstriction, synergist with pro inflammatory mediators like Histamine
Function of TXA2
Promote platelet aggregation
Vasoconstriction
Bronchoconstriction
Classify NSAIDs based on chemical structure
Salicylates eg aspirin
Acetic Acid eg indomethacin
Fenamic Acid eg meclofenamate
Enolic acids eg piroxicam
Proprionic Acids eg ibuprofen
Ketones eg nabumetone
Classify NSAIDs based on enzyme selectivity
Non selective COX enzyme inhibitor (aspirin)
COX-2 Selective inhibitors (‘coxibs’)