Cholinergic presynaptic modifiers Flashcards
Acetylcholine synthesis
Acetyl-CoA + choline → Acetylcholine via Choline Acetyltransferase (ChAT)
Presynaptic inhibitors
Hemicholinium
Vesamicol
Botulinum toxin
Latrotoxins
Hemicholinium
inhibits choline uptake presynaptically
Vesamicol
Inhibits VMAT
Botulinum toxins
Cleave SNAREs and SNAPs, inhibits release
Latrotoxins
Increase presynaptic release, spider toxins.
Ganglion blockers
Nicotine at high doses
Hexamethoinum and Tetraethylammonium
Mecamylamine and Trimethaphan
Hexamethonium and Tetraethylammonium
Quaternary amines, poorly absorbed
Mecamylamine and Tetraethylammonium
Tertiary amines, better absorbed, also more penetration to CNS.
Effects of ganglion blockers
nonspecific inhibition of both the sympathetic and parasympathetic
Vasodilation and hypotension
Tachycardia
mydriasis
constipation, urinary retention,
xerostomia, and anhydrosis.