antimuscarinic

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

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.

Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB).

Cyclopentolate Hydrochloride is a muscarinic acetylcholine receptors antagonist with Kis of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. It is a selective antagonist of mycotoxins M1 receptors, exhibiting high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity, with a 20-fold difference. Oxomemazine is an antihistamine and anticholinergic agent used in cough studies[1][2].

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).

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.

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.

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.

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).

Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with notable antimuscarinic activity. As a selective antagonist of the muscarinic M1 receptor, Oxomemazine demonstrates a 20-fold difference in affinity at high (histamine H1-receptor=84 nM, M1 receptor) and low (histamine H1-receptor=1.65 μM, M2 receptor) affinity sites. It serves as an antihistamine and anticholinergic agent used in cough-related research studies.

AD109 is composed of the selective norepinephrine reuptake inhibitor Atomoxetine and the antimuscarinic agent Aroxybutynin. It demonstrates significant oral bioactivity and effectively reduces the apnea-hypopnea index (AHI).

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.