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1、Zhi-guo SongDepartment of PharmacologyCholinoceptor blocking drugs Cholinoceptor blocking drugs M-receptor blocking drugs N-receptor blocking drugs M-R blocking drugs颠茄曼陀罗M-R blocking drugsM-R blocking drugs茛 菪Atropine Mechanism of action:competitively antagonist for M-receptorPharmacological action

2、Glands: inhibits glands secretion: salivary, sweat glandsEye: Mydriasis increases intraocular pressureparalysis of accommodationSmooth muscle: relaxes splanchnic smooth muscleHeart: decrease heart rate (blocking M1-R) higher doses: increase heart rate (blocking M2-R) antagonize atrioventricular bloc

3、k and arrhythmiaBlood vessel and pressure: dilation Central nervous system: excite depressPharmacological actionClinical usesAntispasmodic: GI tract, ureter and urinary bladderAntisecretory: preanesthetic medication, slavers, night sweatOphthalmologic: iritis, retina examinationAntiarrhythmia: sinus

4、 bradycardia, atrioventricular blockShock: infective shockRescue of organophosphates intoxicationDry mouth, blurred vison, tachycardia, mydriasisCNS: restlessness, hallucinations depressionPoisoning rescue: physostigmineContraindication:glaucoma, prostatic hypertrophyUntoward effectsynthetic mydriat

5、ic Homatropine (后马托品)mydriasis occurs more rapidly and has a shorter duration than atropinesynthetic antispasmodicIpratropium bromide(异丙托溴铵)Bronchial asthmaselective M1-R antagonist Pirenzepine (哌仑西平), Telenzepine (替仑西平)Gastric ulcer treatmentN-cholinoceptor blocking drugs N1-R blocking drugs (gangl

6、ionic blocking drugs)N2-R blocking drugs (skeletal muscular relaxants)Depolarizing neuromuscular blockers succinycholineNondepolarizing neuromuscular blockers curareSkeletal muscular relaxantsDepolarizing neuromuscular blockersFeatures: short time tremor tachyphylaxis 快速耐受性 overdosage can not be rev

7、ersed by neostigmine no ganglionic blocking actionSuccinycholine (琥珀胆碱, scoline) Clinical use:rapid endotracheal intubation Adverse effects:apneamuscle acheshyperkalemia hyperthermiaNondepolarizing neuromuscular blockersFeatures no muscular tremor effect can be increased by other nondepolarizing agent and other drugs effect can be resisted by neostigmine has autonomic ganglionic blocking effect increase histamine releaseTubocurarine(筒箭毒碱)

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