* Transport of choline blocked by – hemicholine * Release blocked by - Botulinum
Cholinergic Agonist * Direct acting 1. Acetylcholine 2. Bethanacol 3. Carbachol 4. Pilocarpine a. Bethanacol i. Strong muscarinic ii. Used to stimulate atonic bladder, post op. b. Methacholine iii. Used as a diagnostic tool for bronchial hyperactivity c. Carbachol iv. Mitotic agent (rarely used) v. Highly potent vi. No side effects when used in eye d. Pilocarpine vii. DOC for closed angle Galucoma (also used for wide) (opens trabecular meshwork), More muscarinic viii. Potent stimulation of all secretions ix. To increase sweat when doing a sweat chloride test for CF * Indirect Acting 1. Edrophonium 2. Neostigmine 3. Pyridostigmine 4. Physiostigmine a. Physostigmine i. Enters CNS ii. Used to treat over dose of anti-cholinergic actions iii. Glaucoma, Atonic bladder iv. SE: Convulsions, Paralysis of skeletal muscle b. Neostigmine v. No CNS vi. Used for Myasthenia Gravis vii. Antidote for tubocurarine c. Edrophonium viii. Diagnosis of Myasthenia Gravis (tensilone test) ix. 10-20 mins x. Antidote – Atropine d. Pyridostigmine xi. Myasthenia long term management e. Donepezil and tacrine xii. Lipid soluble xiii. Used for Alzheimers (maynerfs nucleus)

* Irreversible Blockers (AchE) (parathion, malathion – insecticides-inactivate Cp450) 1. Echothiophate a. Causes intense miosis (one week) b. Open angle glaucoma 2. Isoflurophate c. Aging – no cure (isopropyl group) d. Antidote PAM – pyrilodoxime e. No use – is in serine gas – Causes multiple sclerosis
Cholinergic Antagonist * Antimuscarinic (cardiotoxicity, convulsions, coma in high doses) 1. Atropine 2. Scopalamine 3. Ipratropium a. Atropine i. Long lasting Mydriasis ii. Encycloplegia iii. Low dose bradycardia, High tachycardia, Hallucinations iv. Used for pre op. to decrease secretions v. Relax ureter in renal colic vi. SE: xerostomia vii. To treat OP poisoning viii. Lasts up to 15 days b. Scopalamine (ine = CNS) ix. Motion Sickness x. Short term amnesia c. Ipratropium (pium = No CNS) xi. Inhalation agent for COPD for bronchodilation xii. Only anti cholinergic used for asthma d. Homatropine e. Tropacamide and Cyclopentanate
Ganglionic Blockers a. Nicotine b. Trimethaphan xiii. Short Acting xiv. Used for HTN Emergency c. Mecamlamine xv. Long Acting xvi. Chronic HTN
Neuro Muscular Blockers
a. Succinyl Choline and Rocuronium i. Tracheal Intubation ii. Dantrolene – Antidot iii. Succynyl choline for Malignant HTN a. Vecuronium xiv. Short Surgical Pressure b. Pancuronium xv. Vagolytic – Increase heart Rate c. Atracurium xvi. Mechanical Ventilation xvii. Safe with renal Failure
Adrenergic Agonist I. Isoproterenol a. B1 and B2 b. Used for acute CF c. Short term treatment of pump fail after surgery d. Post MI e. Management of torsades II. Phenylephrine and Methoxamine (paroxysmal SVT) f. Nasal Decongestant g. A1 selective III. Clonidine and Guanficine h. A2 selective i. Used for essential HTN j. SE: sexual dysfunction k. Used for withdrawal for opiates and benzodiazepines IV. Alpha methyl dopa l. Used for HTN m. Blocks Norepi release