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Antispasmodics and anticholinergics

21 articles

Anisodamine

Anisodamine (山莨菪碱, code 654; synthetic racemate 654-2) is a tropane alkaloid M-anticholinergic from Anisodus tanguticus, isolated in China in the 1960s and used for smooth-muscle spasm, microcirculatory shock, and organophosphate poisoning.

Anisotropine

Anisotropine methylbromide (octatropine methylbromide), a quaternary ammonium antimuscarinic tropane derivative once sold as Valpin 50 for peptic ulcer; discontinued, replaced by more effective agents.

Cimetropium

Cimetropium (cimetropium bromide) is a quaternary ammonium antimuscarinic antispasmodic, a semisynthetic scopolamine derivative (ATC A03BB05) studied for irritable bowel syndrome and infantile colic; never approved in the US or Canada.

Clidinium

Clidinium (clidinium bromide, brand Quarzan) is a synthetic anticholinergic muscarinic M1/M3 antagonist that reduces stomach acid and bowel spasms; combined with chlordiazepoxide as Librax (FDA approved 1966) for peptic ulcer, IBS, and enterocolitis.

Difemerine

Difemerine (difemerin, Luostyl) is a synthetic tertiary-amine anticholinergic antispasmodic, ATC A03AA09, formula C20H25NO3, withdrawn in Germany in 1986 for frequent adverse effects.

Diphemanil

Diphemanil, sold as Prantal, is a synthetic quaternary ammonium anticholinergic drug that blocks muscarinic receptors to reduce stomach acid, saliva, and sweat; it was used for peptic ulcer and is now discontinued.

Fenoverine

Fenoverine, marketed as Spasmopriv, is a phenothiazine-derived antispasmodic drug that modulates calcium flow across gastrointestinal smooth muscle membranes to treat spasmodic conditions including irritable bowel syndrome.

Flavoxate

Flavoxate (Urispas, W-61) is a synthetic flavone urinary tract spasmolytic and competitive muscarinic antagonist, FDA-approved in 1970, used for symptomatic relief of dysuria, urgency, and bladder spasms.

Hexocyclium

Hexocyclium (Tral) is a discontinued quaternary amine muscarinic acetylcholine receptor antagonist, methylsulfate salt, ATC A03AB10, formerly used for gastric ulcers and diarrhea, with about 5-fold ileal over cardiac receptor selectivity.

Isopropamide

Isopropamide (isopropamide iodide, Darbid) is a long-acting quaternary ammonium antimuscarinic drug, first FDA-approved 1957, used orally for peptic ulcer and GI spasm; now discontinued for humans but retained in veterinary prochlorperazine combinations.

Mepenzolate

Mepenzolate (Cantil, mepenzolate bromide) is a quaternary ammonium antimuscarinic antispasmodic, ATC A03AB12, FDA-approved November 14, 1956 and later discontinued; used in Japan for IBS and studied for COPD.

Methantheline

Methantheline (methanthelinium bromide; Banthine, Vagantin) is a quaternary ammonium antimuscarinic drug used in Europe since the 1950s for overactive bladder, hypersalivation, and hyperhidrosis; not available in the US.

Methylhomatropine

Methylhomatropine, sold as homatropine methylbromide (CAS 80-49-9), is a quaternary ammonium muscarinic antagonist derived from homatropine, used in antacid antispasmodic combinations and formerly with hydrocodone in Hycodan.

Otilonium

Otilonium bromide (Spasmomen, Spasmoctyl), a poorly absorbed quaternary ammonium antispasmodic blocking L-type calcium channels, muscarinic and tachykinin receptors; used at 40 mg three times daily for irritable bowel syndrome, superior to placebo with placebo-like tolerability.

Oxyphencyclimine

Oxyphencyclimine (Daricon) is a synthetic tertiary amine antimuscarinic anticholinergic drug, ATC A03AA01, C20H28N2O3, introduced 1958, used for peptic ulcer and gastrointestinal smooth muscle spasm, reducing gastric acid secretion.

Oxyphenonium

Oxyphenonium (Antrenyl, oxyphenonium bromide) is a synthetic quaternary ammonium anticholinergic, first US-approved 1952, used for visceral spasms and peptic ulcer adjunct therapy; dual antimuscarinic and musculotropic action, targets CHRM3/CHRM1, now discontinued in the US.

Pinaverium

Pinaverium (pinaverium bromide, Dicetel, Pinverin) is a GI-selective quaternary ammonium calcium channel blocker antispasmodic, poorly absorbed orally, used mainly for irritable bowel syndrome symptoms.

Piperidolate

Piperidolate (Dactil) is a racemic tertiary amine antimuscarinic antispasmodic, ATC A03AA30, C21H25NO2, CAS 82-98-4, approved in Japan in 1967 for spasm and premature labor, banned in US racing.

Propantheline

Propantheline (Pro-Banthine) is a synthetic quaternary ammonium antimuscarinic approved by the FDA in 1953, used as adjunctive peptic ulcer therapy and for hyperhidrosis; US brand discontinued.

Tiropramide

Tiropramide (CR 605, ATC A03AC05) is a racemic tyrosine-derivative antispasmodic that relaxes smooth muscle by raising cAMP and shifting calcium into the sarcoplasmic reticulum; used for abdominal spasm and IBS, non-inferior to octylonium.

Trimebutine

Trimebutine (trimebutine maleate; brands Modulon, Debridat) is a non-FDA-approved spasmolytic for IBS and postoperative paralytic ileus, acting via opioid receptors, peptide release, and calcium channels; ATC A03AA05, up to 600 mg/day.