Propantheline

Propantheline is an Anticholinergic / antimuscarinic Agent belonging to Anti-ulcer agent.

Propantheline is an antimuscarinic agent used to treat urinary incontinence, hyperhidrosis, as well as cramps and spasms of the stomach, intestines, and bladder.

Propantheline is incompletely absorbed from the gastrointestinal tract. Time taken to reach peak plasma concentration is approximately 1 hour. Propantheline is extensively metabolized in the liver via hydrolysis into inactive metabolites. Propantheline is mainly excreted Via urine (approximately 70% as metabolites).

Propantheline shows common side effects like Dry mouth, nose, or throat, blurred vision, constipation, headache, dizziness, drowsiness;, confusion or feeling nervous, decreased sweating, nausea, vomiting, bloating, decreased sense of taste, impotence, sexual problems, sleep problems (insomnia).

Propantheline is available in the form of an Oral Tablet.

Propantheline is available in India, Germany, Bangladesh, Australia, China, South Africa, Malaysia, Singapore, and Philippines.

Propantheline is an Anti-ulcer agent belonging to the class Anticholinergic / antimuscarinic Agent.

Propantheline, a quaternary ammonium antimuscarinic agent, competitively blocks the action of acetylcholine at the postganglionic parasympathetic receptor sites leading to suppressed parasympathetic activity. This results in decreased gastric acid secretion and gastrointestinal motility. It also has spasmolytic properties.

The Onset and Duration of action of Propantheline is approximately 30-45 minutes and 6 hours respectively.

The Tmax was found to be approximately 1 hour.

Propantheline is available in the form of an Oral tablet.

Propantheline tablet is taken orally, usually 3 times a day.

Propantheline is used for the treatment of peptic ulcers. It is also used to relieve muscle spasms in the stomach or intestines.

Propantheline is an Anticholinergic / antimuscarinic Agent belonging to Anti-ulcer agent.

Propantheline competitively blocks the action of acetylcholine at the postganglionic parasympathetic receptor sites leading to suppressed parasympathetic activity, resulting in decreased gastric acid secretion and gastrointestinal motility. It also has spasmolytic properties.

Propantheline is approved for use in the following clinical indications

Adult Indication:

• Peptic ulcer

Pediatric Indication:

• GI or bladder spasm, irritable bowel syndrome

Off - Label Indication:

• It has also been used for hyperhidrosis, and cramps or spasms of the stomach, intestines or bladder.

Adult Dose:

• Peptic ulcer: Oral: 15 mg 3 times daily before meals or food and 30 mg at bedtime; adjust dosage according to patient response and tolerance.

Pediatric Dose:

• GI or bladder spasm, irritable bowel syndrome

Children and Adolescents: Oral: 1.5 to 3 mg/kg/day in divided doses every 4 to 6 hours; maximum daily dose: 75 mg/day.

Propantheline is available in various strengths as 15 mg and 7.5 mg.

Propantheline is available in the form of Oral tablet.

Propantheline is contraindicated in patients with

• Enuresis.
• Glaucoma
• Obstructive disease of the gastrointestinal tract (eg, pyloro duodenal stenosis, achalasia, paralytic ileus)
• Obstructive uropathy (eg, bladder-neck obstruction due to prostatic hypertrophy); intestinal atony of elderly or debilitated patients
• Severe ulcerative colitis or toxic megacolon complicating ulcerative colitis
• Unstable cardiovascular adjustment in acute hemorrhage
• Myasthenia gravis.

• CNS effects

May cause drowsiness and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Diarrhea

May be a sign of incomplete intestinal obstruction; discontinue treatment if this occurs.

• Heat prostration

May occur in the presence of increased environmental temperature; use caution in hot weather and/or exercise.

• Cardiovascular disease

Use with caution in patients with coronary artery disease, tachyarrhythmias, heart failure, or hypertension.

• Hepatic impairment

Use with caution in patients with hepatic impairment.

• Hiatal hernia

Use with caution in patients with hiatal hernia with reflux esophagitis.

• Hyperthyroidism

Use with caution in patients with hyperthyroidism.

• Neuropathy

Use with caution in patients with autonomic neuropathy.

• Renal impairment

Use with caution in patients with renal impairment.

• Ulcerative colitis

Use with caution in patients with ulcerative colitis; large doses may suppress intestinal motility.

Consumption of alcohol during treatment with Propantheline may increase the risk of severe side effects such as severe gastrointestinal bleeding, dizziness, drowsiness, etc.

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Common

Drowsiness, blurred vision, diarrhea, heat prostration (in presence of high environmental temperature), reduced bronchial secretions, Bradycardia followed by tachycardia, palpitations, arrhythmias, Dilatation of pupils with loss of accommodation and sensitivity to light, increased intraocular pressure, Dryness of the mouth, difficulty in swallowing, constipation, nausea, vomiting, ageusia, Thirst, weakness, Hypersensitivity reactions, Dizziness, headache, Nervousness, insomnia, mental confusion, Urinary hesitancy and retention, Suppression of lactation, impotence, Dryness of the skin, decreased sweating, Flushing.

• Acetylcholinesterase Inhibitors:

May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors.

• Aclidinium:

May enhance the anticholinergic effect of Anticholinergic Agents.

• Amantadine:

May enhance the anticholinergic effect of Anticholinergic Agents.

• Anticholinergic Agents:

May enhance the adverse/toxic effect of other Anticholinergic Agents.

• Digoxin:

Propantheline may increase the serum concentration of Digoxin.

• Eluxadoline:

Anticholinergic Agents may enhance the constipating effect of Eluxadoline.

• Gastrointestinal Agents (Prokinetic):

Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic).

• Glucagon:

Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased.

• Glycopyrrolate (Oral Inhalation)

Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation).

• Glycopyrronium (Topical):

May enhance the anticholinergic effect of Anticholinergic Agents.

• Ipratropium (Oral Inhalation)

May enhance the anticholinergic effect of Anticholinergic Agents.

• Itopride

Anticholinergic Agents may diminish the therapeutic effect of Itopride.

• Levosulpiride

Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride.

• Mianserin

May enhance the anticholinergic effect of Anticholinergic Agents.

• Mirabegron

Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron.

• Nitroglycerin

Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption.

• Opioid Agonists

Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination.

• Oxatomide

May enhance the anticholinergic effect of Anticholinergic Agents.

• Potassium Chloride

The common side effects of Propantheline include the following

• Common side effects

Dry mouth, nose, or throat, blurred vision, constipation, headache, dizziness, drowsiness;, confusion or feeling nervous, decreased sweating, nausea, vomiting, bloating, decreased sense of taste, impotence, sexual problems, sleep problems (insomnia).

• Rare side effects

Diarrhea, fast or pounding heartbeats, fluttering in your chest, eye pain or redness, seeing halos around lights, painful or difficult urination.

• Pregnancy

Pregnancy Category C

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Symptoms: Intensification of usual adverse effects (e.g. nausea, vomiting); CNS disturbances (e.g. excitement, restlessness, delirium, hallucinations), hyperthermia, respiratory depression, circulatory changes (e.g. flushing, fall in blood pressure, circulatory failure), coma; curare-like action (e.g. neuromuscular blockade resulting in muscular weakness and possible paralysis).

Management: Supportive and symptomatic treatment. Perform gastric lavage or induce emesis. The administrator activated charcoal.

• Pharmacodynamic

Propantheline is an anticholinergic drug, a medication that reduces the effect of acetylcholine, a chemical released from nerves that stimulates muscles, by blocking the receptors for acetylcholine on smooth muscle (a type of muscle). It also has a direct relaxing effect on smooth muscles. Propantheline is used to treat or prevent spasm in the muscles of the gastrointestinal tract in the irritable bowel syndrome. In addition, Propantheline inhibits gastrointestinal propulsive motility and decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretions.

• Pharmacokinetics

Absorption

Propantheline is incompletely absorbed from the gastrointestinal tract. Time taken to reach peak plasma concentration is approximately 1 hour.

Distribution

Information not available.

Metabolism and Excretion

Propantheline is extensively metabolized in the liver via hydrolysis into inactive metabolites. Propantheline is mainly excreted Via urine (3%; approximately 70% as metabolites).

• https://www.mims.com/india/drug/info/propantheline bromide?type=full
• https://go.drugbank.com/drugs/DB00782
• https://www.drugs.com/mtm/propantheline.html
• https://www.uptodate.com/contents/propantheline-united-states-and-canada-not-available-drug-information?search=propantheline&source=panel_search_result&selectedTitle=1~9&usage_type=panel&kp_tab=drug_general&display_rank=1
• https://www.practo.com/medicine-info/propantheline-2448-api