antimuscarinic

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment.

Tiquizium has effective Antimuscarinic effect, and causes significant bronchodilation in patients with chronic obstructive pulmonary disease.

Homatropine Methylbromide is the methyl bromide salt of homatropine, a synthetic tertiary amine alkaloid with antimuscarinic properties.

Clidinium bromide (Ro 2-3773) , a synthetic anticholinergic agent, has been shown in experimental and clinical researchers to have a pronounced antisecretory and antispasmodic effect on the gastrointestinal tract. It can inhibit muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve cramps or stomach spasms or abdominal due to colicky abdominal diverticulitis, pain, and irritable bowel syndrome.

Diphenidol hydrochloride (Difenidol hydrochloride), a muscarinic antagonist, is employed as an anti-vertigo and as an antiemetic drug.

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not an FDA-Approved Clinical drug, but it is available in Canada and several other international countries.

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects. Trimebutine is an agonist of peripheral mu, delta, and kappa opiate receptors served as a spasmolytic drug for therapy of both chronic and acute abdominal pain.

Otilonium bromide (SP63) , an antimuscarinic, is utilized as a spasmolytic agent.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

Carbinoxamine Maleate Salt (Lergefin) is an ethanolamine class of H1 antihistamines with mild antimuscarinic and sedative properties.

Trihexyphenidyl hydrochloride (Benzhexol hydrochloride) is an antiparkinsonian agent of the antimuscarinic class.

Prifinium bromide is a quaternary ammon antimuscarinic. It inhibits hyperkinesia of the digestive organs and urinary tract and has a spasmolytic action.

Piperidolate hydrochloride is an antimuscarinic, could restrain the abnormal activity caused by acetylcholine. inhibits intestinal cramp induced by acetylcholine (rats and dogs).

Camylofine (Avacan) is an antimuscarinic, used for relaxing smooth muscle.

Flavoxate is an anticholinergic with antimuscarinic effects.

Fesoterodine L-mandelate is a efficacious antimuscarinic agent for the overactive bladder (OAB).

Oxyphencyclimine Hydrochloride (Ulcociclinina) is a synthetic tertiary amine and antimuscarinic agent with antispasmodic and antisecretory activities.

Caramiphen is an antimuscarinic and anticholinergic agent that acts as an antagonist of the NMDA receptor.

Dihexyverine HCl is an antimuscarinic with effects similar to those of atropine.

Revatropate, a selective muscarinic antagonist, is an antimuscarinic drug.

Telenzepine is a potent and selective M1 antimuscarinic.

Espatropate is a bronchodilator with antimuscarinic activity.

Tridihexethyl is an anticholinergic, antimuscarinic, and antispasmolytic drug, which can be used to treat acquired nystagmus or peptic ulcer disease.