Anticholinergic drugs /‘ænti,kəuli’nə:dʒik/ 抗胆碱的 Chapter 7 Anticholinergic drugs /‘ænti,kəuli’nə:dʒik/ 抗胆碱的

Subtypes and effects of cholinergic receptors Nicotine receptor N1 receptor: excitation of nerve ganglion N2 receptor promoting the contracting of skeletal muscle M1 receptor M3 receptor M2 receptor: inhibition of heart promoting the contracting of smooth muscle  [‘gæŋglɪən] 神经节  Muscarine receptor promoting the secretion of glands

Atropine ['ætrəpiːn]（阿托品）

Mechanism of action Competitively preventing the effects of ACh by blocking its binding to muscarinic [,mʌskə‘rinik]毒蕈碱的 cholinergic receptors at neuroeffector神经效应器的 sites on smooth muscle, cardiac muscle, and gland cells; in peripheral ganglia ['ɡæŋɡliə]神经节; and in the CNS. In general, muscarinic receptor antagonists cause little blockade at nicotinic /,nikə'tinik/ 烟碱的receptor sites.

Pharmacological effects (Dose dependently) 1 Inhibiting glandular [‘glændjʊlə] 腺体的secretion 2 Relaxing smooth muscle e.g. reduces gastrointestinal motility运动性 3 Producing the dilatation of pupil, increase of intraocular pressure, and paralysis of accommodation扩瞳、升高眼内压、调节麻痹

4 Causing heart stimulation; 5 Causing small artery relaxation 6 Causing central excitation

Clinical uses: 1 Relief of gastrointestinal smooth muscle spasm 2 Inhibition of glandular secretion (1) Preanesthetic [,pri:ænis'θetik] medication (2) Severe night sweat and salivation [,sælə'veʃən]流涎症

3 Bradycardia[brædi‘kɑ:diə] 心动过缓 and heart block 传导阻滞 4 Toxicity induced by organophosphates /, ɔ:ɡænəu'fɔsfeit/ 有机磷酸酯类 5 Eye (1) Prevent synechia[si‘nekiə] 黏连 formation in iritis 虹膜炎) (2) Optical ['ɔptikəl]光学的 examination

(1) dilates the spasm arteriole[ɑ:‘tiəriəul]小动脉； 6 Anti-shock抗休克 (1) dilates the spasm arteriole[ɑ:‘tiəriəul]小动脉； (2) improves microcirculation微循环, increases the blood supply of important organs; (3) rises blood pressure.

Side effects 1 Dry mouth and skin, tachycardia [,tækɪ'kɑːdɪə]心动过速, dilation of pupil, blurred vision, central excitation 2 Toxic (5~10 mg), lethal dosage: adults 80~130 mg, children 10 mg.

Dose dependent side effects 0.5 mg 轻微心率减慢，略有口干及少汗 1 mg 口干、心率加快、瞳孔轻度扩大 2 mg 心悸、显著口干、瞳孔扩大，有时出现视力模糊 5 mg 上述症状加重，并有语言不清、烦躁不安、皮肤干燥发热、小便困难、肠蠕动减少 >10 mg 呼吸加深加快，出现谵妄、幻觉、惊厥等中枢兴奋症状，并可转为抑制，即昏迷、呼吸麻痹，甚至死亡

Contraindication: Hypertrophy /hai'pə:trəufi/肥大 of the prostate /'prɔsteit/前列腺; Glaucoma

Anisodamine [ænɪ‘sədəmi:n] 山莨菪碱 Effects: Similar to but weaker than that of atropine; Lack of central excitatory effect;

Clinical uses: 1 Relief of gastrointestinal smooth muscle spasm; 2 Infectious shock / Septic shock

Scopolamine /skəu'pɔləmi:n/ 东莨菪碱 Effects: 1 Peripheral effects: 1) Inhibiting glandular secretion: stronger than atropine; 2) Producing the dilatation of pupil, increase of intraocular pressure, and paralysis of accommodation: weaker than atropine; 3) Causing heart stimulation: weaker than atropine

2 Central inhibitory effects: Sedation (/si'deiʃən/镇静); Hypnosis (/hip'nəusis/催眠); Anesthesia ([,ænɪs'θiːzɪə]麻醉) Clinical uses: 1 Parkinson’s disease; 2 Preanesthetic medication; 3 Motion sickness晕动病; Side effects: Similar to that of atropine

大纲要求 Objective and requirements Master the characteristics, actions, and adverse reactions of atropine. Teaching contents Atropine’s competitive blocking functions on M-cholinergic receptors, and its function characteristics,clinical applications, adverse reactions, toxic symptoms, and rescue principles.

Essential vocabulary Anticholinergic drugs Paralysis of accommodation Gastrointestinal smooth muscle spasm Microcirculation Hypertrophy Preanesthetic medication Infectious shock /septic shock