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解热镇痛抗炎药 Antipyretic analgesic and anti-inflammatory drugs. 北京协和医学院基础医学院药理学系 叶菜英. Antipyretic analgesic and anti-inflammatory drugs. These drugs relieve the pain associated with inflammation, including that from arthritis and gout. Antipyretic, analgesic, and antiinflammatory drugs.
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These drugs relieve the pain associated with inflammation, including that from arthritis and gout.
Antipyretic, analgesic, and antiinflammatory drugs.
They produce their anti-inflammatory action through a different mechanism, not as glucocorticoid.
Classed into non-steroidal anti-inflammatordrugs (NSAIDs) in 1974.
unsaturated fatty acid
TEMP SET cells
endogenous pyrogen→CNS→release PG↑ →thermotaxic center → Febrile
antipyretic analgesic painstimulusPG
Effect on periphery, inhibit the synthesis of prostaglandins and prevent bradykinin from stimulating pain receptors, also inhibit the recognition of pain impulses centrally and peripherally.
in PG synthesis.
analgesic and anti-inflammatory
Oral, absorbed from gut→distribution, metabolism→kenosis(enter articular cavity, CSF)
【 Clinical Indications 】
Antipyretic analgesic and anti –inflammatory
【Pharmacological action & Clinical Indications】
Inhibit cycloxygenase cyclo-oxygenase，reduce TXA2 synthesis
Inhibit PA effect on thromboxane synthesis
PM phospholipid AA endoperoxide↓ TXA2↓
thrombosis↓ PA↓ platelet releasion↓
CHDthrombosis, cerebral thrombosis
dizziness, tinnitus, acouesthesia↓
Paracetamol & Phenacetin
(inhibition for center epoxidase is
stronger than that for external
Oral, absorb→hepatic metabolism →kenosis
↗ 60％combine with GA
de-ET（70％－80％）→Paracetamol→35％combine with H2SO4,fail
de-Ac→P-aminophenetole→hydroxide→hemoglobin →oxidationmetahemoglobin ↓
Strong anti-inflammatory, anti-rheumatic effects, but weak atipyretil, analgesic effects.
Primary used to rheumatism and rheumatoid arthritis
Oral to absorb, penetration synovia membrane→the concentration in synovia intermembrance space is 50% of that in blood (high concentration in joint tissue)
analgesic and rheumatism significantly;
Lots of untoward reaction, high incidence rate,
Stomach intestine reaction (ulcer), CNS reaction,
Inhibit hematopoietic system, anaphylactic response