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Pharmacology test 2
Neuromuscular
Drug | MOA | SOA | Side effects/ADR | Extra/key information |
---|---|---|---|---|
Acetylcholine | nicotinic and muscarinic Depolarizing agent | all over body | DUMBELSS | Diarrhea, urination, miosis, bradycardia, bronchial constriction, emesis, lacrimation, salivation, stimulation (CNS) |
Chantix | a4/b2 Nn partial agonist | CNS (Nn) | headache, insomnia, suicidal thoughts, depression, flatuence | FDA black box warning of mood |
succinylcholine | depolarizing agent (neuromuscular blockade)-nictinic | NMJ (Nm) Can affect PNS/SNS ganglia (Nn) | NMJ Paralysis Hyperkalemia, HTN and arrythmias, muscle pain, hyperthermia | Phase 1: binds to ALL Ach binding space and keeps all Na channels open (cannot repolarize) Phase 2: blocks Na channels:gets stuck (can't depolarize) |
Physostigmine | Cholinesterase Inhibitor (AChE Antagonist) | CNS BBB | DUMBELSS | Penetrates CNS / cross BBB Antidote for anti-muscarinic poisoning (Atropine overdose) |
Donepezil (Aricept) Rivastigmine (Exelon) Galantamine | Cholinesterase Inhibitor (AChE Antagonist) | CNS BBB | DUMBELSS | Lipophilic cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine |
PyriDOstigmine Neostigmine | Cholinesterase Inhibitor (AChE Antagonist) | NMJ(targeting periphery) | DUMBELSS | DO NOT cross BBB stays in the periphery Reverse the effects of Curare / treatment of myasthenia gravis |
Edrophonium | Cholinesterase Inhibitor (AChE Antagonist) | NMJ(targeting periphery) | DUMBELSS | 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 Rocuronium | NON-depolarizing agent Direct competitive antagonist Binds to Ach binding space | NMJ-Nm | NMJ Paralysis Histamine release, hypotension & tachycardia No CNS effect | Doesn’t allow Ach to bind; keeps channels closed |