Module 2-2 Antiinflammatory drugs Flashcards
NSAIDs
Large and chemically diverse group of drugs with the following properties: Analgesic Antiinflammatory Antipyretic Antirheumatic
NSAIDs: Mechanism of Action
Activation of the arachidonic acid pathway causes: Pain Headache Fever Inflammation
NSAIDs: Mechanism of
Action (cont’d)
Analgesia—treatment of headaches, mild to
moderate pain and inflammation
Block the chemical activity of either or both COX
enzymes (prostaglandin [PG] pathway)
Result: limits the undesirable inflammatory effect of PGs
NSAIDs: Mechanism of
Action (cont’d
Antipyretic: reduce fever
Inhibit prostaglandin E2 within the area of the brain
that controls temperature
ChemicaNSAIDs: Salicylatesl Categories of NSAIDs
Salicylates Acetic acid derivatives Cyclooxygenase 2 (COX 2) inhibitors Cyclooxygenase-COX- Enolic acid derivatives Propionic acid derivatives
NSAIDs: Salicylates
Salicylates also have antiplatelet activity
Inhibit platelet aggregation
Examples: aspirin, diflunisal (Dolobid)
NSAIDs: Acetic Acids
indomethacin (Indocin) ketorolac (Toradol) diclofenac sodium (Voltaren) sulindac (Clinoril) tolmetin (Tolectin) etodolac (Lodine)
NSAIDs: COX-2 Inhibitor
celecoxib (Celebrex)
First and only remaining COX-2 inhibitor
Indicated for osteoarthritis rheumatoid arthritis
osteoarthritis, arthritis,
acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea
NSAIDs: Enolic Acid Derivatives
piroxicam (Feldene)
meloxicam ( Mobic)
nabumetone (Relafen)
NSAIDs: Propionic Acids
fenoprofen (Nalfon) flurbiprofen (Ansaid) ibuprofen (Motrin, Advil) ketoprofen (Orudis KT) naproxen (Naprosyn, Aleve) oxaprozin (Daypro)
NSAIDs: Indications
Analgesia (mild to moderate) Antigout effects Antiinflammatory effects Antipyretic effects Relief of vascular headache Platelet inhibition (ASA)
NSAIDs: Indications (cont’d)
Relief of mild to moderate pain Acute gout Various bone, joint, and muscle pain Osteoarthritis Rheumatoid arthritis
NSAIDs: Indications (cont’d)
Juvenile rheumatoid arthritis
Dysmenorrhea
Fever
NSAIDs: Salicylates
salicylates (aspirin)
More potent effect on platelet aggregation
Analgesic
Antipyretic
Antiinflammatory
Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders
NSAIDs: Adverse Effects
Gastrointestinal Dyspepsia, heartburn, epigastric distress, nausea GI bleeding*
Mucosal lesions* (erosions or ulcerations)Renal
Reductions in creatinine clearance
Acute tubular necrosis with renal failure