Mepenzolate

Mepenzolate is a Postganglionic parasympathetic inhibitor/antimuscarinic agent belonging to Anti-ulcer agent.

Mepenzolate is a postganglionic parasympathetic inhibitor that was previously approved for improving the healing of gastric ulcers.

Incompletely absorbed from the GI tract. Mepenzolate is excreted between 3 and 22% via urine when administered orally.

Mepenzolate shows common side effects like dry mouth, decreased sweating, dizziness, drowsiness, blurred vision, widened pupils, nausea, vomiting, and constipation.

Mepenzolate is available in the form of an Oral Tablet.

Mepenzolate is available in India, Malaysia, Singapore, and Philippines.

Mepenzolate is an Anti-ulcer agent belonging to the class Postganglionic parasympathetic inhibitor/antimuscarinic agent.

Mepenzolate is a post-ganglionic parasympathetic inhibitor. It specifically antagonizes muscarinic receptors. This leads to decreases in gastric acid and pepsin secretion and suppression of spontaneous contractions of the colon.

The Data of Onset and Duration of action of Mepenzolate clinically not established.

The Tmax was found to be approximately 1-3 hours (fasted state) and 1-4 hours (after meal).

Mepenzolate is available in the form of an Oral Tablet.

Mepenzolate Tablet is usually taken orally, four times a daily.

Mepenzolate is a prescription medicine used to treat the symptoms of Peptic Ulcers and Irritable Bowel Syndrome.

Mepenzolate is a Postganglionic parasympathetic inhibitor/ antimuscarinic agent belonging to Anti-ulcer agent.

Mepenzolate is a post-ganglionic parasympathetic inhibitor. It specifically antagonizes muscarinic receptors. This leads to decreases in gastric acid and pepsin secretion and suppression of spontaneous contractions of the colon.

Mepenzolate is approved for use in the following clinical indications

• Adjunct in peptic ulcer

Mepenzolate is a postganglionic parasympathetic inhibitor that was previously approved for improving the healing of gastric ulcers.

• Adjunct in peptic ulcer

Adult: 25-50 mg 4 times daily, titrated to the lowest effective dose and adjust accordingly to patient's response.

Mepenzolate is available in various strengths as 25 and 50mg.

Mepenzolate is available in the form of Oral Tablet.

Mepenzolate is contraindicated in patients with

• Hypersentivity.
• Glaucoma
• obstructive uropathy and GI disease
• paralytic ileus
• myasthenia gravis
• unstable CV status in acute GI haemorrhage
• intestinal atony
• toxic megacolon complicating ulcerative colitis.

• In the presence of high environmental temperature, heat prostration (fever and heat stroke due to decreased sweating) can occur with use of Mepenzolate.
• Diarrhea may be an early symptom of incomplete intestinal obstruction especially in patients with ileostomy or colostomy. In this instance, treatment with this drug would be inappropriate and possibly harmful.
• Mepenzolate may produce drowsiness or blurred vision. The patient should be cautioned regarding activities requiring mental alertness such as operating a motor vehicle or other machinery or performing hazardous work while taking this drug.
• With over dosage, a curare-like action may occur i.e., neuromuscular blockage leading to muscular weakness and possible paralysis.
• It should be noted that the use of anticholinergic drugs in the treatment of gastric ulcer may produce a delay in gastric emptying time and may complicate such therapy (antral stasis).
• Psychosis has been reported in sensitive individuals given anticholinergic drugs. CNS signs and symptoms include confusion, disorientation, short-term memory loss, hallucinations, dysarthria, ataxia, coma, euphoria, decreased anxiety, fatigue, insomnia, agitation and mannerisms and inappropriate affect.
• These CNS signs and symptoms usually resolve within 12 to 24 hours after discontinuation of the medication.

It is not known whether Mepenzolate is secreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Mepenzolate is administered to a nursing woman.

Pregnancy Category B

Reproduction studies have been performed in rats and rabbits at doses up to 30 times the human dose (based on 50 kg weight) and have shown no evidence of impaired fertility or harm to the animal fetus. There are, however, no adequate and well-controlled studies with Mepenzolate in pregnant women. Because animal reproduction studies are not always predictive of human response, Mepenzolate should be used during pregnancy only if clearly needed.

Common

Drowsiness, blurred vision, diarrhoea, heat prostration, psyschosis, Dizziness, headache, nervousness, confusion, insomnia, weakness, Tachycardia, palpitations. Vomiting, nausea, constipation, ageusia, bloating, xerostomia, decreased lactation, Urinary retention, urinary hesitancy, impotence, Increased ocular tension, cycloplegia, mydriasis, Urticaria, hypohidrosis.

Potentially Fatal:

Anaphylaxis.

• The following agents may increase certain actions or side effects of anticholinergic drugs: amantadine, antiarrhythmic agents of class I (quinidine), antihistamines, antipsychotic agents (e.g., phenothiazines), benzodiazepines, MAO inhibitors, narcotic analgesics (e.g., meperidine), nitrates and nitrites, sympathomimetic agents, tricyclic antidepressants, and other drugs having anticholinergic activity.
• Anticholinergics antagonize the effects of antiglaucoma agents. Anticholinergic drugs in the presence of increased intraocular pressure may be hazardous when taken concurrently with agents such as corticosteroids.
• Anticholinergic agents may affect gastrointestinal absorption of various drugs, such as slowly dissolving dosage forms of digoxin; increased serum digoxin concentrations may result. Anticholinergic drugs may antagonize the effects of drugs that alter gastrointestinal motility, such as metoclopramide. Because antacids may interfere with the absorption of anticholinergic agents, simultaneous use of these drugs should be avoided.
• The inhibiting effects of anticholinergic drugs on gastric hydrochloric acid secretion are antagonized by agents used to treat achlorhydria and those used to test gastric secretion.

The common side effects of Mepenzolate include the following

Common side effects

Dry mouth, decreased sweating, dizziness, drowsiness, blurred vision, widened pupils, nausea, vomiting, and constipation.

Rare side effects

Hives, difficulty breathing, swelling of your face, lips, tongue, or throat, mental or mood changes, eye pain or pressure, fast or pounding heartbeat, difficulty urination, decreased sexual ability, rash, itching, and severe dizziness.

• Pregnancy

Pregnancy Category B

Reproduction studies have been performed in rats and rabbits at doses up to 30 times the human dose (based on 50 kg weight) and have shown no evidence of impaired fertility or harm to the animal fetus. There are, however, no adequate and well-controlled studies with Mepenzolate in pregnant women. Because animal reproduction studies are not always predictive of human response, Mepenzolate should be used during pregnancy only if clearly needed.

• Nursing Mothers

It is not known whether Mepenzolate is secreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Mepenzolate is administered to a nursing woman.

• Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Studies in newborn animals (rats) show that younger animals are more sensitive to the toxic effects of Mepenzolate than are older animals.

• Geriatric Use

Clinical studies of Mepenzolate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.

Mepenzolate is contraindicated in intestinal atony of the elderly. Mepenzolate should be used with caution in the elderly.

Symptoms: Curare-like effects (e.g. neuromuscular blockade leading to weakness and possible paralysis), headache, nausea, vomiting, blurred vision, mydriasis, hot and dry skin, xerostomia, difficulty in swallowing, dizziness, CNS stimulation.

Management: Employ gastric lavage, admin of emetics and activated charcoal. May use sedatives (e.g. short-acting barbiturates, benzodiazepines) for overt signs of excitement. If indicated, may also use parenteral cholinergic agent as antidote.

• Pharmacodynamic

Mepenzolate diminishes gastric acid and pepsin secretion. Mepenzolate also suppresses spontaneous contractions of the colon. Pharmacologically, it is a post-ganglionic parasympathetic inhibitor.

• Pharmacokinetics

Absorption

Incompletely absorbed from the GI tract.

Distribution

Information not available.

Metabolism and Excretion

Mepenzolate is excreted between 3 and 22% via urine when administered orally.

• https://www.rxlist.com/cantil-drug.htm
• https://www.mims.com/india/drug/info/mepenzolate bromide?type=full
• https://go.drugbank.com/drugs/DB04843
• https://www.drugs.com/ppa/mepenzolate.html