Anti-Inflammatory drugs Flashcards
Tissue injury causes the release of..
Prostaglandins
Autacoids (local mediators) cause:
Vasodilation
Increased vascular permeability
Chemotaxis
Pain
Is cox-1 or cox-2 responsible for platelet function?
COX-1
COX-1 Is responsible for..
Homeostatic functions
GI tract
Renal
Platelet function
Vessels
COX-2 Is responsible for..
Inflammation
NSAIDS mechanism of action
Blocking either or both cyclooxygenase (COX) enzymes
•COX-1 and COX-2
Limits the undesirable inflammatory effect of prostaglandins and related substances
Cyclooxygenase purpose
COX is the enzyme that converts arachidonic acid into prostanoids (prostaglandins and related compounds)
COX-1 and COX-2
Properties of NSAID drugs
Analgesic
Anti-inflammatory
Antipyretic
NSAID indications
Relief for mild to moderate pain
Non-Selective NSAIDS
Inhibit both COX-1 and COX-2
•Alleviate mild - moderate pain
•Inflammatory disorders (rheumatoid arthritis, bursitis, osteoarthritis)
•Suppress inflammation but pose risk of serious harm
Non-Selective NSAID drugs
Acetylsalicylic Acid (ASA): Aspirin
Ibuprofen (motrin, advil)
Ketoralac
Acetylsalicylic Acid (ASA) - Aspirin
Anti-inflammatory
Analgesic
Antipyretic
Antiplatelet
Different to other NSAIDS
Irreversibly inhibits COX
(all other NSAIDS reversibly inhibit COX)
80-160 mg daily prophylactic for MI, stroke.
CI’s:
Pregnancy, bleeding disorders, caution in renal dysfunction
Adverse:
•GI bleeding
•Reye’s syndrome in kids
•Renal: reductions in creatinine clearance
•Salicylate toxicity: Tinnitus/hearing loss in adults, hyperventilation in kids
Non-ASA NSAIDS
ASA-like drugs with fewer GI, renal, and hemorrhagic effects than aspirin (ASA)
•Inhibit COX-1 and COX-2: Inhibition is reversible unlike with ASA
DO NOT protect against MI and stroke like ASA does
Selective COX-2 Inhibitors
COX-2: Responsible for inflammatory mediators
Just as effective as NSAIDS in suppressing inflammation and pain. Possible lower risk for GI adverse effects.
Can impair renal function, cause hypertension and edema.
Increased risk of MI and stroke
Celecoxib
•Sulfa drug allergies CI
Drug used to reduce GI ulceration with NSAIDS
Misoprostol
Synthetic prostaglandin
Used in combination with NSAIDs to reduce ulceration