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Neuromuscular Drugs

Pharmacology Exam 2

DrugMOASOASE / ADRsEK
Acetylcholine Nicotinic & Muscarinic Depolarizing agent All over body DUMBBELSS Diarrhea, Urination, Miosis, Bradycardia, Bronchial constriction, Emesis, Lacrimation, Salivation, Stimulation (CNS)
Varenicline (Chantix) a4/B2 Nn partial agonist CNS (Nn) Headache, insomnia, suicidal thoughts, depression, flatulence FDA warning of mood and behavioral changes; used for smoking cessation
Succinylcholine Depolarizing agent (Neuromuscular blockade – nicotinic) NMJ (Nm) Can affect autonomic (PNS / SNS) ganglia NMJ Paralysis Hyperkalemia, HTN & arrhythmias, muscle pain (myalgia), hyperthermia Phase 1: binds to Ach binding space and keeps all Na+ channels open (cannot repolarize) Phase 2: blocks Na+ channels (cannot depolarize)
Physostigmine Cholinesterase Inhibitor (AChE Antagonist) CNS & periphery DUMBBELSS Penetrates CNS / cross BBB Treatment for anti-muscarinic poisoning (Atropine)
Donepezil (Aricept) Rivastigmine (Exelon) Galantamine Cholinesterase Inhibitor (AChE Antagonist) CNS & periphery DUMBBELSS Lipophilic > cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine
PyriDOstigmine Neostigmine Cholinesterase Inhibitor (AChE Antagonist) NMJ DUMBBELS No CNS effects DO NOT cross BBB Reverse the effects of Curare / treatment of myasthenia gravis
Edrophonium Cholinesterase Inhibitor (AChE Antagonist) NMJ DUMBBELS No CNS effects Used for diagnosis of myasthenia gravis or medication dose adjustments Short duration of action/reversible
Echothiophate Organophosphate inhibitor of acetylcholinesterase enzyme M3 receptor in ciliary muscle (eye) Miosis and blurred vision, lacrimation, stinging / redness of eye Ophthalmology treatment glaucoma
Botulinum Toxin (Botox) Prevent ACh release Presynaptic terminal Muscle relaxation Cleaves sites on SNARE protein
Curare & Curare like Mivacurium Vecuronium Rocuronium Pancuronium Tubocurarine NON-depolarizing agent Direct competitive antagonist >Binds to Ach binding space NMJ NMJ Paralysis Histamine release, hypotension & tachycardia No CNS effect Doesn’t allow Ach to bind; Ach is required for muscle contraction
Created by: PharmacistJulian
 

 



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