非甾体抗炎药(nsaids).doc
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非甾体抗炎药(nsaids)
Prostaglandins and fever, pain, inflammation, have close relations, prostaglandin is the medium of inflammation, the majority of antipyretic analgesics (except acylation aniline) can affect the prostaglandin biosynthesis and anti-inflammatory effects. Clinically, the treatment of rheumatoid arthritis, rheumatoid arthritis. As the population ages, there will be greater demand for such drugs.
I. structure type
(1) 3, 5-pyrazolane diketone class
In 1946 found that pyrazole alkanes diketone drugs bute (phenylbutazone) has good anti-inflammatory analgesic action, used to treat rheumatoid arthritis, rheumatoid arthritis, but has toxicity to the liver, hematopoietic system, application of dwindling. But because it has a better uric acid effect, it can be used to treat acute gout (90% effective). In 1961, the body metabolite oxyphenbutazone was found to be antiinflammatory and anti-rheumatic, and less toxic.
Sulfonated pyrazole ketones (sulfur oxygen sanzuotong, benzene sulfonic cover is too loose, sulfinpyrazone) is confirmed too loose derivatives, almost no anti-inflammatory effects, but has a strong line of uric acid (can strong inhibiting renal tubular reabsorption of uric acid), as the powerful promotion of uric acid excretion agent. An oral administration was available for 10 hours, one day orally 0.5 g, serum uric acid decreased by 51 percent, and there were antithrombotic effects. The U.S.P and b.p. are loaded.
(2) adjacent aminobenzoic acid (acid)
The derivative of adjacent aminobenzoic acid is a non-steroidal antiphlogistic analgesic in the 1960s. Are: JiaFen the acid (a acid, flapping wet pain, mefenamic acid), chlorine Finn that acid (chlorine acid, anti-rheumatism spirit, clofenamic acid), a chlorine Finn that acid sodium (anti-inflammatory acid sodium, chlorine acid sodium, a chloramine sodium benzoate, meclofenamate sodium), fluorine Finn that acid (flufenamic acid, flufenamic acid), Nepal flufenamic acid (nitrogen flufenamic acid, niflumic aci
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