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Cholinergic

TermDefinition
Direct Acting Cholinergics Alkaloids and Ester Choline
Ester of Choline Carbachol, Acetylcholine, Bethanechol, and Methacholine.
Alkaloid Pilocarpine. Muscarine and Arecholine
Indirect Acting Cholinergics ( Reversibles) 1. Carbamates -->Physostigmine, Neostigmine, Pyridostigmine, Edrophonium, Rivastigmine, Donepezil, Galantamine. 2. Acridine -->Tacrine
Indirect Acting Cholinergics ( Irreversibles) 1. Organophosphates --> Parathion, Malathion, Sarin, Tabun, Echothiophate, Diazinon, Soman. 2. Carbamates --> Carbaryl and Propoxur.
Ester of Choline acts on which receptors? Muscarine and Nicotine
Muscarinic actions on the heart 1a. Increase in potassium current in the SA and AV nodes --> Gi protein 1b. Increase the outflow of K+ ions. 1c. This makes the cell more negative --> hyperpolarization--> Difficult to reach the threshold. 1d. Decreases the excitability and slow HR 2a. Decrease in the slow inward calcium current in heart cells. 2b. Decrease entry of calcium into the cells 2c. Decrease force of contraction.
Muscarinic actions on blood vessel Dilated -->decreased BP by the release of Endothelium dependent relaxing factor (EDRF) – Nitric oxide.
Muscarinic actions on Smooth muscles GIT --> : ↑Tone & peristalsis & sphincter relax Gallbladder: contraction Urinary bladder: Detrusor muscle--> contraction, Trigone & sphincter: relaxes. Bronchial muscle: Bronchospasm Ureter: contraction
Muscarinic actions on glands ↑ Sweating, salivation, lacrimation, tracheobronchial and gastric secretion
Muscarinic actions on eyes Contraction of circular fibers of sphincter pupillae-->Miosis Contraction the ciliary muscle-->Spasm of accommodation.
Muscarinic actions on Male sex organ Erection – muscarinic actions Ejaculation
Nicotinic actions on Autonomic ganglia ↑ release of Ach & NA.
Nicotinic actions on Skeletal muscle (NM junction) Initial contraction. High doses --> paralysis of skeletal muscles by persistant depolarization.
Nicotinic actions on Autonomic ganglia Stimulation then depression.
Interaction of Direct acting cholinergic Atropine – antagonizes muscarinic actions. Adrenaline – physiological antagonist. Anticholnesterases potentate Ach.
Adverse effects of Direct Acting cholinergic drugs. D--> Diarrhea U--> Urinary incontinence M--> Miosis B--> Bronchoconstriction E--> Electrical Changes L--> Lacrimation S--> Salivation.
Contra indications of ester of cholines Angina Bronchial asthma Peptic ulcer Hyperthyroidism
Uses of pilocarpine Tx: Narrow angle and Wide angle glaucoma to reduce IOP. Reverse mydriatic effect of atropine.
Antidote for acute pilocarpine poisoning Atropine
Absorption property of quaternary carbamates ( AchE) The conjunctiva, skin and lungs is poor. Relatively insoluble in lipids. Except Physostigmine
Malathion rapidly metabolized to inactive products in birds and mammals but not in insects; safe.
Parathion Not detoxified effectively in vertebrate; it is dangerous to man
Acetylcholinesterase inhibitors fall into three chemical groups. 1. Simple alcohols bearing a quaternary ammonium --> edrophoniun; 2. carbamic acid esters of alcohols bearing quaternary or tertiary ammonium groups-->neostigmine and physostigmine 3. organic derivatives of phosphoric acid-->echothiophate
Created by: Jameel D. Wilson
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