Antipyretic-Analgesic and Antiinflammatory Drugs 解热镇痛药 汤慧芳 浙江大学医学院 药理系 2018-11-7
汤慧芳 浙江大学医学院 药理系 2018-11-7 Antipyretic-Analgesic and Antiinflammatory Drugs 解热镇痛药
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 anti inflammatory effects Non-steroidal anti-inflammatory drugs NSAIDS,非甾体抗炎药)。 大亭院
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）。 A. General Pharmacological properties
Stimulus Disturbance of cell membranes Phospholipids Phospholipase inhibitors Corticosteroids Phospholipase Fatty acid substitution(diet) Arachidonic acid Lipoxygenase inhibitors Lipoxygenase Cyclooxygenase NSAID. ASA Leukotrienes eceptor antagonists LTBA LTC//DA/E4 ( Prostaglandins Thromboxane Prostacyclin Phagocyte Alteration of vascula permeability, bronchial activation constriction, increased Leukocyte modulation secretion Colchicine Inflammatio Bronchospasm Inflammation congestion, mucous plugging I
A.General Pharmacological properties 2. Antipyretic effects Inhibition of pce 2 production in the hypothalamus induced by endogenous pyregens after pathological stimuli -y temperature↓ notes: symptomatic control only, not be indicated in all patients with fever The effect on body temperature is different from that of chlorpromazine 大亭院
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 满大告学流
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 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 出大皆亭
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 出大皆亭
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 4. Anti-inflammatory effects PGs induce inflammatory responses Inhibition of PG production cal relieve inflammatory responses, sucl as congestion exudation, pain The effect is different from that of glucocorticosteroids 大亭院
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 出大皆亭
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
A.General Pharmacological properties 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 出大皆亭
5. COX-1 / COX-2 and selectivity of the drugs COX-1: constructive; i n v o l v e d i n p h y s i o l o g i c 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