神经系统药理—魏尔清(传出药理概论拟胆碱药.pptVIP

* * Part 2Parasympathomimetics Cholinoceptor agonists: M, N Anticholinesterase inhibitors A Muscarinic receptor agonists A Muscarinic receptor agonists 1. Choline Esters (胆碱酯类) Acetylcholine 乙酰胆碱 Carbachol 卡巴胆碱 Methacholine 醋甲胆碱 Bethanechol chloride 氯贝胆碱 2. Natural Alkaloids (生物碱类) Pilocarpine 毛果芸香碱（匹罗卡品） Muscarine 毒蕈碱 Pilocarpine 毛果芸香碱（匹罗卡品） Pilocarpine 毛果芸香碱 A Muscarinic receptor agonists 1. Pharmacological effects （1）Eyes Miosis（缩瞳）: contraction of sphincter muscle of iris Lowing intraocular pressure（降低眼内压）: enlarging angle of anterior chamber, increasing drainage of aquous humor Spasm of accommodation（调节痉挛）: contraction of ciliary muscle, contraction for near vision A Muscarinic receptor agonists Iris, cilliary muscles, and Schelemm canal Aqueous humor drainage Pilocarpine Atropine （2） Promoting secretion of exocrine glands（外分泌腺体） especially in sweat, salivary and tear glands A Muscarinic receptor agonists 2. Clinical uses （1）Ophthamological uses Glaucoma: narrow- or wide-angles Iritis: miotics/mydriatics BOX Glaucoma Acute congestive glaucoma（narrow-angle） Chronic simple glaucoma（wide-angle） A Muscarinic receptor agonists （2）Systemic use Dry mouth: radiotherapy Antidote for atropine poisoning A Muscarinic receptor agonists 3. Adverse effects （1）Local (eye): pain, tears （2）Systemic: secretion of exocrine glands, treated with atropine A Muscarinic receptor agonists B Anticholinesterases 1. Reversible anticholinesterases 2. Irreversible anticholinesterases anionic site esteratic site Acetylcholinesterase is the mechanism of terminating ACh effects B-1 Reversible anticholinesterases Action of acetylcholinesterase Acetylcholinese: structure for interaction with substrate B-1 Reversible anticholinesterases Neostigmine 新斯的明 Neostigmine 新斯的明 1. Pharmacological effects binding to AChE, but slowly hydrolysis inhibiting AChE activity Properties