医学PPT课件CholinoceptorBlocking .ppt

Classification Base on specific receptor affinities Antimuscarinic agents Antinicotinic agents( consist of ganglion-blockers and neuromuscular junction blockers) Atropine and its alkaloids Atropine Anisodamine Acopolamine chemistry and pharmacokinetics Tertiary amine alkaloid esters of tropic acid Well absorbed from the gut and across the conjunctival membrane Widely distributed Metabolism and excretion Pharmacological Effects Glands Sweat, salivary gland secretion are greatly reduced Bronchial secretion decreased Reduction in gastric secretion and total acid content, especially at doses greater than 1 mg Pharmacological Effects Eye Mydriasis ocular pressure increase cycloplegia Pharmacological Effects Smooth muscle Gastrointestinal tract: relax Genitourinary tract: relax, void slowly Pharmacological Effects Cardiovascular system: Heart rate:Lower doses: Presynaptic receptor blocked bradycardia At moderate to high therapeutic doses: tachycardia Atrioventricular conduction In toxic concentrations: intraventricular conduction block Pharmacological Effects blood vessel and pressure Vasodilation and hypopiesis caused by cholinnergic nerve can be blocked At toxic doses, cutaneous vasodilation Pharmacological Effects CNS At normal doses, minimal stimulant effect In toxic doses, excitement, agitation, hallucinations and coma Clinical uses Relieve hyperkinesia Inhibit secretion Ophthalmology: iritis, optometry Arrhythmia shock Cholinergic poisoning Clinical uses 2001年 1月11日 羊城晚报（成都消息） 37岁男性，因家庭纠纷喝乐果中毒。昏迷，每30分钟用5支阿托品，无效 每10分钟用5支，无效 每5分钟用10支，连续使用72小时，总共用了1700支，850 mg 病人清醒，生命体征趋向平稳。（阿托品的 最低致死量为成人80-130 mg ，儿童10 mg ）。 Adverse effects Dry mouth, mydriasis, tachycardia, hot and flushed skin, agitation and delirium Hyperthermic effects: dangerous when overdose in infants/children CNS: hallucinations, coma Rescue Catharsis Physostigmine CNS: diazepam Anisodamine Pharmacodynamics: similar to atropine Clinical uses: shock Scopolamine CNS