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
NSAIDs: Salicylate Toxicity
Adults: tinnitus and hearing loss
Children: hyperventilation and CNS effects
Metabolic acidosis and respiratory alkalosis
may be present
NSAIDs: Interactions
Serious interactions can occur when given with:
Anticoagulants
Aspirin
Corticosteroids and other ulcerogenic drugs
Protein bound drugs
Antigout Drugs
Gout: condition that results from inappropriate
uric acid metabolism
decreased excretion of uric acid
excessive production of uric acid
Uric acid crystals are deposited in tissues and
joints, resulting in pain
Antigout Drugs: Indications
cont’d
allopurinol (Zyloprim)
Used to reduce production of uric acid
colchicine
Reduces inflammatory response to the deposits of urate
crystals in joint tissue
probenecid (Benemid), sulfinpyrazone (Anturane)
Increases excretion of uric acid in the urine