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physostigmine

A parasympathomimetic alkaloid, specifically, a reversible acetylcholinesterase inhibitor. It occurs naturally in the Calabar bean and manchineel tree. Parasympathomimetic activates the parasympathetic nervous system by mimicking or modifying the effects of acetylcholine. • muscarinic receptor agonists (direct-acting parasympathomimetics) • acetylcholinesterase inhibitors (indirect-acting parasympathomimetics) Acetylcholinesterase is the enzyme responsible for the breakdown of acetylcholine in the synaptic cleft of the neuromuscular junction. It acts by interfering with the metabolism of acetylcholine, so indirectly stimulates both nicotinic and muscarinic acetylcholine receptors. (Indications) • myasthenia gravis: It has a miotic function, causing pupillary constriction. • glaucoma: It increases outflow of the aqueous humor in the eye. • delayed gastric emptying: Parasympathetic nervous system exerts both excitatory and inhibitory control over gastric and intestinal tone and motility. • orthostatic hypotension (Functions) • Treats anticholinergic poisoning (e.g. atropine, scopolamine, other anticholinergic drug overdoses, Datura stramonium, Atropa belladonna, gamma-hydroxybutyric acid, dimenhydrinate poisoning). • Improves the memory of Alzheimer's patients. • Reverses the effects of benzodiazepines and barbiturates. (Side effects) • Nausea, vomiting, diarrhea, anorexia, dizziness, headache, stomach pain, sweating, dyspepsia, and seizures. • Overdose can cause cholinergic crisis. Its metabolite or eseroline may be neurotoxic. Death can occur rapidly following overdose as a result of respiratory arrest and paralysis of the heart. It is replaced by donepezil, galantamine, and rivastigmine for its poor tolerability.