Pitofenone is a spasmolytic agent. It exerts anticholinesterase and antimuscarinic activities. Pitofenone is used to relieve pain and spasms of smooth muscles. Pitofenone is also used for the treatment of back pain, sprains, and strains. Pitofenone is used in combination along with fenpiverinium bromide, and metamizole sodium. The drug is currently sold in Eastern Europe and India under various trade names. The combined preparation possesses strong analgesic, spasmolytic, cholinolytic and anti-inflammatory effects on the smooth muscles predominantly of the gastrointestinal and urogenital tract. Indications are strong pain in gastric or intestinal colic, kidney and gallstones, and for painful menstruation. Pitofenone hydrochloride present in the combination exerts papaverin-like spasmolytic effect on the vascular and extra-vascular smooth muscles of the stomach, intestines, urinary tract, biliary tract, and uterus.

Alizapride is a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting. The anti-emetic action of Alizapride is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS)—this action prevents nausea and vomiting triggered by most stimuli. Structurally similar to metoclopramide and, therefore, shares similar other attributes related to emesis and prokinetics.

Alosetron, marketed under the brand name Lotronex, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only. Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of the enteric nervous system. Alosetron is used for the treating women with severe irritable bowel syndrome (IBS) accompanied by severe diarrhea (usually lasting for 6 months or more). It is only prescribed to women who do not respond to other medicines and is not to be used by women whose main IBS problem is constipation.

Carbachol is a potent cholinergic (parasympathomimetic) agent which produces constriction of the iris and ciliary body resulting in reduction in intraocular pressure.

Dicyclomine is an anticholinergic tertiary amine used frequently by oral and parenteral route as an effective anti-spasmodic agent. Dicyclomine hydrochloride salt is approved under brand name bentyl for the treatment of functional bowel/irritable bowel syndrome. In addition is known, that dicyclomine is also used in morning and motion sickness, dysmenorrheal, intestinal hypermotility. It was shown, that Dicyclomine is a selective M1 and M3 muscarinic receptors antagonist, but os shown pharmacological activity via the M1 receptor.

Cisapride is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be expected to compromise the beneficial effects of cisapride.

Pipenzolate bromide (JB-323), an anticholinergic agent, which binds to muscarinic acetylcholine receptors as an antagonist. Pipenzolate bromide was studied as an antispasmodic agent, and to treat peptic ulcer.

Cimetropium bromide (cimetropium) is a semi-synthetic belladonna alkaliod, a quaternary derivatives of scopolamine. Cimetropium was used in Italy under the name Alginor for the treatment of painful gastrointestinal conditions, such as irritant bowel syndrome or infant colics as well as in preparation for diagnostic procedures. The drug exerts its action by binding to muscarinic receptors and inhibiting their activity.

Difemerine is antimuscarinic agent. It is used in the symptomatic treatment of visceral spasms. It may have anticholinergic side effects like dry mouth, dizziness, blurred vision and drowsiness. Anticholinergics must be used with caution in glaucoma and prostate hypertrophy patients.