(From Pharm book and lecture, 30 Jan 2001, by Brian Buschman)
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These drugs function by blocking cycloxygenase in the production of Pgs. This helps stop the inflammation at the source as well as function analgesically in the hypothalamus. NSAIDs do not undergo tolerance.
Salicylates are such as aspirin, acetylsalicylic acid, sodium salicylates and mesalamine. The decrease in Pg can be good but also bad. It’s effects include:
1) Decreased production of TxA2 causing thinner blood.
2) Loss of local protection in the stomach with excess HCl.
3) Liver damage occurs with time.
NSAIDs can either inhibit Cox I which is found in non-inflammatory cells or Cox II from inflammatory cells. Blocking Cox II messes up normal function like platelet formation. Aspirin does it irreversibly while the other are all reversible.
New NSAIDs are reversible Cox inhibitors so cells can revert back to the normal functions the body needs.
Aspirin is used at low dosages for reduction of platelet aggregation (an aspirin a day), intermediate doses for pain and high doses for inflammation.
People that have aspirin hypersensitivity can experience asthma with VERY low doses of the drug. At higher doses they fell tinnitus, vertigo, respiratory alkalosis, dehydration, collapse, coma and/or death.
Children, epically if virally infected, can develop Reye’s syndrome. It presents with a respiratory infection followed by nausea, vomiting and DLOC. Reye’s disease is a hepatic fatty degeneration and encephalopy.
Certain NSAIDs work better on inhibition of Cox I or II.
Cox I is preferentially hit by salicylates, indometacin and piroxican.
Both are hit by propanoic acid derivatives (ibuprofen and naproxen) as well as diclofenac.
Cox II is exclusively hit by celecoxib.
Ibuprofen and naproxen are both similar to aspirin but exhibit less gastric effects. Naproxen also has leukocyte chemotactic ability.
Diclofenac has very good anti-inflammatory ability compared to others. It is good chronic use.
Ketorolac, in the same class but exhibits better analgesic and poor anti-inflammatory.
Nabumexone is a good anti-inflammatory used for osteoarthritis.
Piroxicam is a very good anti-inflammatory.
Indometacin has very good anti-inflammatory effects.
Acetaminophen is not effective as an anti-inflammatory but rather works centrally a an analgesic. It is often used in patients with aspirin hypersensitivity or children with viral infections and are prone to develop Reye’s disease.
Misoprostol is a PgE2 analogue that can be used to help treat peptic ulcer that results form NSAID use.
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