Chapter 44-Antiinflammatory and Antigout Drugs Flashcards
NSAIDS
Large and chemically diverse group of drugs with the following properties
NSAIDS are:
- Analgesic
- Antiinflammatory
- Antipyretic
- Antirheumatic
NSAIDS: Mechanism of Action
Activation of the arachidonic acid pathway causes: Pain, headache, fever, inflammation
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
Antipyretic
Reduce fever
-inhibit prostaglandin E2 within the area of the brain that controls temperature
Chemical Categories of NSAIDS
- Salicylates
- Acetic acid derivatives
- Cyclooxygenase-2 (COX-2) inhibitors
- 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: celecoxib (Celebrex)
- First and only remaining COX-2 inhibitor
- Indicated for osteoarthritis, rheumatoid 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)
- Relief of mild to moderate pain
- Acute gout
- Various bone, joint, and muscle pain
- Osteoarthritis
- Rheumatoid arthritis
- Juvenile rheumatoid arthritis
- Dysmenorrhea
- Fever
NSAIDS: Salicylates (aspirin)
- More potent effect on platelet aggregation
- analgesic
- antipyretic
- anti-inflammatory
- 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)
NSAIDS: Adverse Effects Renal
- Reductions in creatinine clearance
* Acute tubular necrosis with renal failure