镇静药--幻灯片.pptVIP

Chapter 13 Anxiolytics Hypnotics抗焦虑药和催眠药 失眠的诱因 1 环境因素 强光、噪声 2 生活习惯因素 睡前饮咖啡 3 躯体因素 咳嗽、疼痛 4 精神心理因素　焦虑、紧张 5 精神疾病　焦虑症 、抑郁症 6 药物原因　咖啡因、阿托品 7 年龄因素　 8 与睡眠相关疾病　睡眠呼吸暂停综合征? Anxiolytics (抗焦虑药）：the medicine for relief anxiety, tense and dread § 2 Benzodiazepines,BDZ Diazepam 地西泮（t1/2：30~60h） Triazolam 三唑仑（t1/2：2~3h） Nitrazepam 硝西泮（t1/2：6~8h） Lorazepam 劳拉西泮 Alprazolam 阿普唑伦 Nordiazepam 去甲安定 Halazepam 哈拉西泮 Clonazepam 氯硝西泮 Oxazepam 奥沙西泮 Prazepam 普拉西泮 Pharmacokinetics of Benzodiazepines absorbed well from GI tract distributed widely some also given parenterally all metabolized in liver, excreted primarily in urine Biotransformation of Benzodiazepines Effects of Benzodiazepines Relief of anxiety and tension Sedative-hypnotic or sleep inducement effects Anticonvulsant activity Skeletal muscle relaxation 苯二氮 受体 分布: 皮层（最多） 、边缘系统、中脑（次之）、脑干、脊髓（最少)。 相似于γ–氨基丁酸（GABA）亚型受体GABAA的分布 与配体-门控性Clˉ通道 (ligand-gated Cl- channel)有关 Cl ˉ通道周围含有5个结合位点 (GABA, BDZ,巴比妥类, 印防己毒素，神经甾体化合物) GABAergic SYNAPSE Buspirone 丁螺环酮/布司匹隆 absorbed rapidly metabolized to at least 1 active metabolite eliminated in urine and feces mechanism of action unclear May be a partial agonist of 5-HT1A receptor 用于抗焦虑和伴有焦虑的失眠、抑郁症，对恐怖症无效 巴比妥类 Barbiturates Phenobarbital 苯巴比妥 Pentobarbital 戊巴比妥 Amobarbital 异戊巴比妥 Mephobarbital 甲苯比妥 Secobarbital 司可巴比妥 Aprobarbital 阿普比妥 Thiopentone 硫喷妥 Pharmacokinetics of Barbiturates Rapid absorption following oral administration Rapid onset of central effects Extensively metabolized in liver, however, there are no active metabolites Phenobarbital is excreted unchanged. Its excretion can be increased by alkalinization of the urine Pharmacokinetics of Barbiturates In the elderly and in those with limited hepatic function, dosages should be reduced. Phenobarbital cause autometabolism by induction of liver enzymes. Pharmacology Effects of Barbituates daytime sedation (short periods only) hypnotic effects (insomnia) preop sedation and anesthesia relief of anxiet