SAR of Parasympathomimetic Agents: Direct acting agents: Acetylcholine, Carbachol, Bethanechol, Methacholine, Pilocarpine : Pharmaguideline -->

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SAR of Parasympathomimetic Agents: Direct acting agents: Acetylcholine, Carbachol, Bethanechol, Methacholine, Pilocarpine

A enzyme called choline acetyltransferase (CAT) catalyzes the synthesis of acetylcholine in nerve terminals by converting glucose to acetyl CoA.

Acetylcholine

A enzyme called choline acetyltransferase (CAT) catalyzes the synthesis of acetylcholine in nerve terminals by converting glucose to acetyl CoA (acetyl CoA).


USES:
Acetylcholine is the main and primary central neurotransmitter of the parasympathetic nervous system, this is the part of the autonomic sensory system (a part of the peripheral sensory system) that agreements smooth muscles, expands the veins, increments the real emissions, and eases back pulse as well.

SAR-
When the nitrogen of the quaternary ammonium group is replaced by arsenic, phosphorus, sulfur or selenium, their activity decreases.

It is required that the atom present in the nitrogen zone be positively charged with muscarinic activity.

When all three methyl groups are replaced by large alkyl groups of quaternary nitrogen, the drug loses its potency as an agonist.

Carbachol

There are exactly two steps may be needed to synthesize carbachol. By reacting 2-chloroethanol with urea, 2-chloroethyl-carbamate is formed, and by reacting trimethylamine with this compound, it is quaternised.


USES:
Through its ability to increase the amount of fluid draining from the eye, carbachol reduces eye strain. When taken ophthalmically, it is also known to be used to treat glaucoma as well.

SAR-
  • Carbachol stimulates both muscarinic and nicotinic receptors through parasympathomimetic action.
  • When applied to topical ocular or intraocular, it produces effects such as miosis and increased fluid flow.

Bethanechol

Bethanechol is a muscarinic agonist used to treat obstructive functional urinary retention, as well as neurogenic atony of the bladder, postoperatively or postnatally.


USES
Bethanechol is used to treat problems with peeing caused by suggested certain medical procedures, medicines, or other essential factors.

SAR-
  • Bethanechol directly stimulates the cholinergic receptors present in the parasympathetic nervous system.
  • It stimulates ganglia to a lesser extent.
  • It only works on muscarinic receptors.

Methacholine

In the parasympathetic nervous system, Acetyl-β-methylcholine functions as a non-selective muscarinic receptor agonist.


USES:
Methacholine is utilized as a test to decide if you might have asthma or inhaling problems. A cholinergic medication causes wheezing and windedness.

SAR-
Methacholine induces bronchoconstriction by suppressing muscarinic receptors.

Therefore, this is used during the diagnosis of asthma and bronchial hyperreactivity.

Pilocarpine

Plants in the genus Pilocarpus are the strongest and main known sources of pilocarpine, and commercial production is gotten altogether from the leaves of Pilocarpus microphyllus (Maranham Jaborandi). This variety grows just in South America, and Pilocarpus microphyllus is local to a few states in northern Brazil only.


USES:
Pilocarpine is usually used to treat dry mouth which may be caused by radiation in people with the head also with the deadliest disease like neck cancer, as well as dry mouth caused by Sjogren's illness (an immune system ailment that causes dryness in certain parts and muscles of the body, such as the eyes and mouth).

SAR-
Pilocarpine is a cholinergic parasympathomimetic agent.

In particular it stimulates muscarinic receptors.

Therefore, it increases the retention of exocrine glands and produces contraction of the iris, sphincture muscle and ciliary muscle.
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Ankur Choudhary is India's first professional pharmaceutical blogger, author and founder of Pharmaceutical Guidelines, a widely-read pharmaceutical blog since 2008. Sign-up for the free email updates for your daily dose of pharmaceutical tips.
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