Term
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Definition
COX-2 selective inhibitor
-About 10-20 times more selective COX-2 than COX-1 isozyme inhibitor
-Better GI tolerated than nonselective NSAIDs, does not affect platelet aggregation
-Occasionally interact with warfarin
-May cause rashes probably due to sulfonamide structure |
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Term
| Aspirin (acetylsalicylic acid, ASA) |
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Definition
-irreversibly acetylates COX-1 and 2 to prevent arachidonate binding to enzyme
-Irreversible inhibits platelet COX so that its anti-platelet effect last 8-10 days (the life of the platelet)
-Decreases incidence of transient ischemic attacks, unstable angina, coronary artery thrombosis with myocardial infarction, and thrombosis after coronary artery bypass grafting
-Discontinue ASA 7-10 days before surgery (platelet’s lifetime)
-Not to be used in hemophilic patients
-ASA main adverse effect at antithrombic doses are GI intolerance and gastric and duodenal ulcers |
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Term
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Definition
COX-2 selective inhibitor
-Less selective COX-2 over COX-1 isozyme inhibitor than celecoxib
-Better GI tolerated than nonselective NSAIDs, does not affect platelet aggregation
-USA approved for treatment of osteoarthritis |
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Term
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Definition
-Less selective COX-2 over COX-1 isozyme inhibitor than celecoxib (“preferentially” selective)
-Better GI tolerated than nonselective NSAIDs, does not affect platelet aggregation
-USA approved for treatment of osteoarthritis |
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Term
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Definition
-nonselective NSAID
-Dosage over 150 mg/d impairs renal blood flow and GFR
-Serum aminotransferase increase more frequently than with other NSAIDs
-Topical gel (3%) effective for solar keratoses (rough scaly spots on sun-damaged skin- considered pre-cancerous) |
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Term
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Definition
-nonselective NSAID
-enterohepatic cycle with reabsorption
-Recommended for RA, cancer pain with bone metastases, pain control in dental surgery and oral lesions
-Clearance depends on renal function and hepatic metabolism, dosage limited in patients with significant renal impairment |
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Term
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Definition
-nonselective NSAID
-Only the (S)(-) enatiomere inhibits COX
-Topical ophthalmic preparation used to inhibit intraoperative miosis
*IV preparation effective for perioperative analgesia in minor, ear, neck, and nose surgery
-Lozenge preparation for sore throat
-SE profile similar to that of older NSAIDs; however this drug is also associated rarely with cogwheel rigidity, ataxia, tremor, and myoclonus |
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Term
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Definition
Low dose= analgesic
High does= analgesic+anti-inflam
• Ibuprofen rarely may produce agranulocytosis, aplastic anemia, and aseptic meningitis |
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Term
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Definition
-NS COX inhibitor
*also inhibit lipoxygenase
-At recommended levels clinical efficacy compared to other NSAIDs
-Major SE are GI and CNS |
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Term
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Definition
-NS COX inhibitor
-Commonly used for the treatment of gout and ankylosing spondylitis, and to accelerate closure of patent ductus arteriosus
-SE at higher doses ~ 1/3 of patients suffer from conditions requiring drug discontinuance e.g., pancreatitis, headaches, psychosis with hallucinations, thrombocytopenia, plastic anemia and renal papillary necrosis |
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Term
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Definition
-recommended for systemic use mainly as an analgesic, not as an anti-inflammatory drug.
-Effective analgesic often given IV or IM (oral preparations also available); used successfully to replace morphine in some conditions associated with mild to moderate postsurgical pain
-Ophthalmic preparation used for ocular inflammation
-When used with an opioid it may decrease opioid requirement by 25-50%
-Chronic use may result in renal toxicity |
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Term
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Definition
-NS COX inhibitor
-Prodrug, once daily dosing b/c T1/2 more than 24 hrs, expensive
*Like naproxen, in some patients this compound may cause pseudoporphyria and photosensitivity |
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Term
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Definition
-NS CoX inhibitor
-Naproxen’s free fraction in plasma is significantly higher in women than in men
-Effective in usual rheumatologic indications
-Rare cases of allergic pneumonitis, leukocytoclastic vasculatis, and pseudophorphyria have been reported |
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Term
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Definition
-NS COX inhibitor
-At high concentration inhibits polymorphonuclear leukocyte migration and lymphocyte function, and decreases oxygen radical production
-Recommended for the usual rheumatic indications
*EYE: Dosages > 20 mg/d greatly increase the incidence and severity of peptic ulcers and bleeding |
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Term
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Definition
-NS COX inhibitor
-Recommended for the usual rheumatic disease indications
- Also suppresses familial intestinal polyposis and it may inhibit the development of colon, breast, and prostate cancer
*Some severe SE include Stevens-Johnson epidermal necrolysis syndrome, various blood dyscrasias, and nephrotic syndrome |
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Term
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Definition
1.Active metabolite of the more toxic prodrug phenacetin
2.Phenacetin not available in the USA
3.*Weak COX-1 and COX-2 inhibitor; widely used for the treatment of mild to moderate pain when anti-inflammatory effects are not necessary
4.*****Large doses may lead to significant formation of N-Acetyl-p-benzoquinone, a minor but highly active metabolite showing liver and kidney toxicity |
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Term
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Definition
| for acetaminophen overdose |
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Term
| Nonacetylated Salicylates |
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Definition
-magnesium choline; sodium and salicyl salicylate
-effective anti-inflammatory drugs, however less effective analgesics than ASA
-may be prefered to ASA in asthma and kidney patients, and in those with bleeding tendencies |
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