Drug intelligence / Profile preview

methantheline

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Parenteral
01

Overview

Methantheline is a synthetic quaternary ammonium antimuscarinic agent used primarily as an antispasmodic to relieve cramps or spasms of the stomach, intestines, and bladder. It is indicated for the treatment of peptic ulcer disease, irritable bowel syndrome, pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, reflex neurogenic bladder in children, overactive bladder syndrome, hypersalivation (sialorrhea), and hyperhidrosis. Methantheline acts as a non-selective muscarinic antagonist by competitively inhibiting acetylcholine at muscarinic receptors on postganglionic parasympathetic neuroeffector sites in smooth muscle (including gastrointestinal and urogenital tracts), cardiac muscle (sinoatrial and atrioventricular nodes), exocrine glands (salivary and sweat glands), and other tissues. This results in reduced motility and secretory activity of the gastrointestinal system as well as relaxation of smooth muscles. Compared to atropine, methantheline has a longer duration of action for certain effects such as reduction in salivation. It can be administered orally or parenterally; clinical effects last about 6 hours after single therapeutic doses[2][3][5][8].

Brand names
Vagantin
Other names
methantheline bromide
02

Targets

CHRM5 (M5)CHRM2 (M2)CHRM4 (M4)CHRM3 (M3)M1 (Muscarinic acetylcholine receptor M1)

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