Antipyretic-Analgesic and Antinflammatory Drugs
Antipyretic-Analgesic and Antiinflammatory Drugs
A. General Pharmacological properties D 1. Inhibition ofprostaglandin synthesis inhibiting cyclooxygenase(COX,环氧酶 d decreasing the synthesis of PGs and TXA% I resulting antipyretic, analgesic, and anti inflammatory effects O non-steroidal anti-inflammatory drugs MAIDS,非甾体抗炎药)
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 antiinflammatory effects non-steroidal anti-inflammatory drugs (NSAIDs, 非甾体抗炎药）
Phospholipid 儿( from cell membran。), ∞5 corticosteroids mm)CO BradykInin Angiotensin Phospholipase A2 Arachidonic acid Cyclooxygenase NSAD8mm③ Pr。 stacyclIn(PGl2) PGG 2 ydro- PGE. 5-Lipoxygena PGF PGH Thromboxane a Dipyridamole 5-HPETE (see Chapter 20 Leukotrienes
膜磷脂 皮质斗 PLA2 激素 匚Ir-Dx花生四烯酸 炎性刺激 生理刺激}5c0X1c0x2 非甾体 抗炎药 中间体 PGE2 PGI2 炎症介质 TXA2
A. General Pharmacological properties 口2. Antipyretic effects u Inhibition of PGE, production in the hypothalamus induced by endogenous pyregens after pathological stimuli temperature I notes. symptomatic control only, not be indicated in all patients with fever u The effect on body temperature is different from that of chlorpromazine
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
Comparison of properties of two types of drugs 解热镇痛药 氯丙嗪 作用机制|抑制前列腺素合成,使|抑制下丘脑体温调节中枢, 散热增加而解热 使其调节功能减弱,不能随 外界温度变化而调节体温 作用 只能使升高的体温降到氯丙嗪配合物理降温,不仅 正常 可使升高的体温降到正常, 也可使正常体温降到正常以 下 用途用于各种发热 用于低温麻醉、人工冬眠 不良反应胃肠道反应等 锥体外系统反应等
解热镇痛药 氯丙嗪 作用机制 抑制前列腺素合成，使 散热增加而解热 抑制下丘脑体温调节中枢， 使其调节功能减弱，不能随 外界温度变化而调节体温 作用 只能使升高的体温降到 正常 氯丙嗪配合物理降温，不仅 可使升高的体温降到正常， 也可使正常体温降到正常以 下 用途 用于各种发热 用于低温麻醉、人工冬眠 不良反应 胃肠道反应等 锥体外系统反应等 Comparison of properties of two types of drugs
A. General Pharmacological properties 口3. Analgesic effects D Analgesic effect is resulted from inhibition of PGE, production. D Effective on the pain of low to moderate intensity related to inflammatory responses. D PGE2: a pain stimulant and hyperalgesic agen ent u The analgesic effect is different from opioid analgesics
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 解热镇痛药 阿片类镇痛药 作用 抑制前列腺素合成起效;兴奋阿片受体起效 对慢性钝痛有效,对剧烈对各种疼痛均有效 疼痛或内脏绞痛无效 用途 头痛、牙痛、神经痛、肌|用于其他药物无效的急性 肉或关节痛、痛经等 锐痛,晚期肿瘤的剧烈疼 痛 不良反应胃肠道反应等,但无成瘾有成瘾性 性
解热镇痛药 阿片类镇痛药 作用 抑制前列腺素合成起效； 对慢性钝痛有效，对剧烈 疼痛或内脏绞痛无效 兴奋阿片受体起效； 对各种疼痛均有效 用途 头痛、牙痛、神经痛、肌 肉或关节痛、痛经等 用于其他药物无效的急性 锐痛，晚期肿瘤的剧烈疼 痛 不良反应 胃肠道反应等，但无成瘾 性 有成瘾性 Comparison of properties of two types of drugs
A. General Pharmacological properties D 4. Anti-inflammatory effects u PGs induce inflammatory responses I Inhibition of PG production can relieve inflammatory responses, such as congestion exudation, pain. a The effect is different from that of glucocorticosteroids
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 非甾体抗炎药 糖皮质激素 作用 抑制前列腺素合成起效;|抑制炎症细胞、炎症分 缓解软组织、骨骼、关节子,多环节炎症炎症病变 的炎症 用途 风湿性、类风湿性炎症,可用于多种炎症,作用强 外伤损伤 不良反应胃肠道反应等 抑制机体防御反应,干扰 代谢,不良反应广泛
非甾体抗炎药 糖皮质激素 作用 抑制前列腺素合成起效； 缓解软组织、骨骼、关节 的炎症 抑制炎症细胞、炎症分 子，多环节炎症炎症病变 用途 风湿性、类风湿性炎症， 外伤损伤 可用于多种炎症，作用强 不良反应 胃肠道反应等 抑制机体防御反应，干扰 代谢，不良反应广泛 Comparison of properties of two types of drugs