Anticholinesterase Agents

Anticholinesterase Agents


a group of medicinal substances that slow the activity of cholinesterase (an enzyme that decomposes acetylcholine, a substance that transmits stimuli in the nervous system). The mechanism of anticholinesterase activity consists in the intensification of the effect of acetycholine on the glands, heart, nerve ganglia, and smooth and skeletal musculature. Also significant is the direct effect of anticholinesterase remedies on tissue. Anticholinesterase agents are conventionally divided into substances of reversible or irreversible effect, according to the way they interact with cholinesterase. To those of the first group belong physostigmine (or eserine), galanthamine, proserine methyl sulfate, and others; to those of the second group belong phosphacol, “armine,” “pyrophos,” insecticides (for example, “chlorophos,” parathion), and also certain chemical warfare agents (tabun, “zarin,” and “zoman”). Anticholinesterase remedies intensify contractions of the smooth musculature of the eyes, bronchi, gastrointestinal tract, biliary and urinary tracts, and uterus. They increase secretion of the digestive and sweat glands and stimulate the autonomic nervous system, increasing the tonus of the sympathetic and parasympathetic nerves. Anticholinesterase agents that act on the eye cause extreme miosis, the decrease of intraocular pressure, and an accommodation cramp. Contraction of the striated (skeletal muscles is also intensified under the influence of anticholinesterase agents.

Certain anticholinesterase agents (phosphacol, “armine,” “pyrophos,” physostigmine) are used in ophthalmology to decrease intraocular pressure in the treatment of glaucoma; galanthamine and eserine in the treatment of myasthenia, myopathy, and other diseases accompanied by reduction in the strength of skeletal muscle contraction.

Anticholinesterase agents used as chemical warfare agents and also toxic doses of anticholinesterase agents in medical practice are capable of causing excitation of the central nervous system manifested by convulsions, which may be followed by paralysis. If the paralysis spreads to the respiratory center, death results. Atropine and other preparations are used for treatment of poisoning with anticholinesterase agents.


Zakusov, V. V. Farmakologiia, 2nd ed. Moscow, 1966.
Mashkovskii, M. D. Lekarstvennye sredstva, 6th ed., parts 1–2. Moscow, 1967.


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Reversal by atropine of tetanic fade induced in cats by antinicotinic and anticholinesterase agents.
In clinical practice, atropine, a nonselective muscarinic receptor blocker, is employed to prevent the parasympathomimetic effects induced by neostigmine when the anticholinesterase agent is clinically used to reverse the blockage of neuromuscular transmission caused by non-depolarizing muscular relaxants (Barrio, Miguel, Garcia, & Pelegrin, 2007).
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Thus, there are a variety of changes during aging that could affect sensitivity toward anticholinesterase agents (e.
Anticholinesterase agents, atropine, and [alpha]-agonists have been effective for cardiovascular instabilities.
Previous studies indicate that electrical stimulation of tube feet is potentiated by anticholinesterase agents and antagonized by cholinergic blocking agents (2, 3).
Common Side Effects Experienced With Anticholinesterase Agents Abdominal cramps Diarrhea Excessive salivation Nausea Vomiting Anorexia Pupil constriction Bronchial relaxation (collapse) Increased bronchial secretions Diaphoresis Tachycardia Hypotension Muscle twitching Muscle cramps Muscle weakness Headache Rash
One of these anticholinesterase agents is involved in the diagnostic test for myasthenia gravis.
In the cours eof those 8 days, she was introduced to another, and more durable, anticholinesterase agent, called, Mestinon, and an effective dosage (one 60-milligram tablet every four hours) was determined.