liquid gel forms may be more effective for absorption into fascia and muscle. Gastrointestinal irritation and bleeding occur less frequently than with aspirin. Use of aspirin and ibuprofen together may decrease overall anti-inflammatory effects. Therefore, treatment with ibuprofen in individuals with increased cardiovascular risks may limit the heart-protecting effects of aspirin. Aspirin is contraindicated in individuals with nasal polyps, angioedema, and bronchospastic reactivity to aspirin. It has also been associated with rash, pruritus, tinnitus, dizziness, headache, and fluid retention. Renal difficulties occur (as with all NSAIDs) but very rarely. ● Ketoprofen (Orudis) : Ketoprofen nonselectively inhibits COX and lipoxygenase but is similar to the other NSAIDs in its effectiveness for the treatment of rheumatoid arthritis and osteoarthritis. It adversely affects the gastrointestinal tract and central nervous system. ● Naproxen (Naprosyn, Aleve) : Naproxen availability is 41% higher in women than in men and is effective for rheumatologic conditions in a slow-release formula, as a topical preparation, and as an eye-wash. Over- the-counter use of naproxen is associated with two times greater incidence of gastrointestinal bleeding than that of over-the-counter use of ibuprofen. Beyond normal NSAID-associated effects, rare cases of allergic pneumonitis, leukocytoclastic vasculitis, and pseudopophyria are associated with use. ● Oxaprozin (Daypro) : The major difference between this drug and other NSAIDs like it is its very long half-life, permitting dosage in a once-a-day formulation (Farinde, 2023). Fenamate NSAIDs Meclofenamate sodium and mefenamic acid (Ponstel) inhibit both COX and phospholipase A2. Meclofenamate has similar side effects to other NSAIDS, with slightly higher incidence of abdominal pain and diarrhea. It also enhances the effect of oral anticoagulants and is contraindicated in pregnancy. Mefanamic acid is less effective than aspirin as an anti- inflammatory but is considerably more toxic. It should not be used for a period over one week (Farinde, 2023). Oxicam NSAIDs Piroxicam (Feldene): Has a long half-life, permitting once- a-day dosage. At high concentrations, this COX inhibitor also inhibits leukocyte migration, decreases oxygen radical production and inhibits lymphocyte function. Toxicity includes gastrointestinal symptoms in 20 percent of users, and other adverse effects including headache, dizziness, tinnitus, and rash. Peptic ulcer and bleeding can occur at higher dosages, at a rate more than nine times that of other NSAIDs. Salicylates NSAIDS ● Diflunisal (Dolobid) : Although it is derived from salicylic acid, it is not reduced to salicylic acid or salicylate. Clearance is dependent on renal function and hepatic metabolism, and dosages should be limited in users with renal impairment. It is considered particularly effective for pain in cases of bone metastases and dental surgery. NSAID side effects in general include (Eustice, 2022): ○ Gastrointestinal : Dyspepsia, heartburn, epigastric distress, and nausea; less frequently, vomiting, anorexia, abdominal pain, GI bleeding, and mucosal lesions. Misoprostol (Cytotec), a synthetic prostaglandin that inhibits gastric acid secretion, may be given to prevent GI intolerance. It prevents gastric ulcers and their associated GI bleeding in people receiving NSAIDs.
There are three types of NSAIDs: salicylates (acetylated and nonacetylated), the traditional NSAIDs, and COX-2 selective inhibitors. All NSAIDs are gastric irritants, although newer formulations cause less gastric acid, in general, than aspirin. All newer NSAIDS are analgesic, anti-inflammatory, and antipyretic, and most (except the COX-2-selective agents and non-acetylated salicylates, discussed subsequently below) inhibit platelet aggression (Ghlichloo & Gerriets, 2023). Acetic acid NSAIDs ● Diclofenac (Cataflam, Voltarren) : Relatively nonselective as a COX inhibitor, adverse effects occur in about 20% of users, include symptoms of gastrointestinal distress, bleeding, and ulceration. Used post-surgically in certain operations. ● Etodolac (Lodine) : Somewhat more COX-2 selective than most NSAIDs; may cause less gastric toxicity in relation to ulcer disease that other nonselective NSAIDs. ● Indomethacin (Indocin) : A powerful nonselective COX inhibitor that may also decrease T-cell proliferations. Useful for rheumatic conditions and can reduce gingival inflammation in an oral rinse administration. At higher dosages, one-third of users have reactions requiring discontinuing the drug. Side effects include abdominal pain, diarrhea, gastrointestinal hemorrhage, and pancreatitis. Headache is experienced in up to one-quarter of users and is associated with dizziness, confusion, and depression. May interact with other medications. Should not be used in individuals with nasal polyps or angioedema, as it may precipitate an asthma attack. ● Ketorolac (Toradol) : Used systemically primarily as an analgesic, rather than an anti-inflammatory, although it does have typical NSAID anti-inflammatory properties. Most typically given intramuscularly or intravenously after surgery, but an oral dose is available. When combined with an opioid, it can decrease the amount of opioid required by as much as 25-50%. Toxicities are similar to other NSAIDs, with renal toxicity perhaps more common with chronic use than that of other NSAIDs. ● Nabumetone (Relafen) : Nabumetone is the only nonacid NSAID currently available. Its half-life is greater than 24 hours, permitting a once-daily dose. It may be slightly less damaging to the stomach than other NSAIDs, but it is more expensive, which may be prohibitive in larger dosages. Like naproxen, nabumetone has been reported to cause photosensitivity and pseudoporphyria in some users. ● Sulindac (Clinoril) : Along with its use for rheumatic disease, it may have implications for inhibiting the growth of certain cancers. Like diclofenac, it may cause elevated serum aminotransferases more than most other NSAIDs (Farinde, 2023). Propionic acid NSAIDs ● Fenoprofen (Nalfon) : Most associated with rare toxicity of interstitial nephritis among all the NSAIDs. Other side effects include nausea, dyspepsia, peripheral edema, rash, central nervous system and cardiovascular effects, and tinnitus. Drug interactions. ● Flurbiprofen (Ansaid) : Extensive hepatic metabolism; comparable in strength to aspirin in studies with rheumatoid arthritis and osteoarthritis; available in a topical form; effective after surgery; side effects similar to other NSAIDS, with slightly more pronounced adverse effects including ataxia or tremors. ● Ibuprofen (Motrin, Advil) : Oral ibuprofen is often prescribed in low doses, at which it has analgesic but not anti-inflammatory effects. Topical cream and
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Book Code: MIL1226
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