Chpt 07 Cholinoceptor-activating drugs胆碱受体激动剂.pptVIP

Chapter 7 Cholinoceptor agonists N 胆碱受体激动药 Drug list Prototype: ?acetylcholine ?pilocarpine Major variants: ? carbachol ?methacholine ? Bethanechol 思考题 毛果芸香碱导致调节痉挛的原理及对视觉的影响？(提示：睫状肌、悬韧带、晶状体是如何改变的） * * Pharmacology Instructor : Lei Linsheng 雷林生 Cholinoceptor agonists are a large group of drugs that mimic acetylcholine and classified pharmacologically by their spectrum of action depending on the type of receptor that is activated. Classification 1. M Cholinoceptor agonists 1) Choline esters methacholine carbachol bethanechol 2) Alkaloids pilocarpine 2. N Cholinoceptor agonists nicotine Acetylcholine A. Muscarinic effect (M-effect) iv small dosage decreases heart rate and contractility dilation of blood vessels, decline of blood pressure constriction of bronchial muscle, gastrointestinal, urinary tract, uterus smooth muscle and pupil SLUD response --- Salivation --- Lacrimation --- Urination --- Defecation increases the secretion of gland (sweat, salivary, lacrimal, nasopharyngeal) B. Nicotinic effects (N-effect) Larger dosage activates N1 -- produces and activates all the autonomic ganglia -- resembles simultaneous discharge of both the parasympathetic and sympathetic nervous systems activates N1 receptor of pheochrome cells of adrenal medulla--- releases adr. activates N2, constriction of skeletal muscle C. Therapeutic use None---action is too transient Not effective orally Duration after IV-2 minutes Methacholine 醋甲胆碱 Selective for M receptor not easily hydrolyzed by cholinesterase--- effects are longer used to treat xerostomia Measurement of bronchial hyperactivity (hyperresponsiveness) (methacholine challenge激发test) 2.1 The methacholine challenge test is one method of assessing airway responsiveness. In this test, the patient inh