神经系统药理—吴希美(解热镇痛药.pptVIP

Chapter 27Antipyretic-Analgesic and Antiinflammatory Drugs A. General Pharmacological properties 1. Inhibition of prostaglandin synthesis inhibiting cyclooxygenase (COX，环氧酶), decreasing the synthesis of PGs and TXA2, resulting antipyretic, analgesic, and anti-inflammatory effects non-steroidal anti-inflammatory drugs (NSAIDs, 非甾体抗炎药）。 2. Antipyretic effects Inhibition of PGE2 production in the hypothalamus induced by endogenous pyregens after pathological stimuli ? temperature ? notes: symptomatic control only, not be indicated in all patients with fever. The effect on body temperature is different from that of chlorpromazine. A. General Pharmacological properties 3. Analgesic effects Analgesic effect is resulted from inhibition of PGE2 production. Effective on the pain of low to moderate intensity related to inflammatory responses. PGE2: a pain stimulant and hyperalgesic agent The analgesic effect is different from opioid analgesics. A. General Pharmacological properties Comparison of properties of two types of drugs 4. Anti-inflammatory effects PGs induce inflammatory responses. Inhibition of PG production can relieve inflammatory responses, such as congestion, exudation, pain. The effect is different from that of glucocorticosteroids. A. General Pharmacological properties Comparison of properties of two types of drugs 5. COX-1 / COX-2 and selectivity of the drugs COX-1: constructive; involved in physiologic regulatory functions in GI tract, kidney, etc.; inhibition of COX-1 is related to the adverse effects. COX-2: inducible; involved in pathological responses such as inflammation, and pregnancy; inhibition of COX-2 is related to the therapeutic effects. A. General Pharmacological properties （－） （＋） （＋） （－） B. Salicylates Aspirin 阿司匹林 Acetylsalicylic acid 乙酰水杨酸 Aspirin 阿司匹林 Salicylic acid 水杨酸 Salicylic sodium 水杨酸钠 Aspirin 阿司匹林 1. ADME transformed to salicylic acid form in the body hepatic metabolism is primaril