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Mepenzolate

Pronunciation

(me PEN zoe late)

Index Terms

  • Mepenzolate Bromide

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral, as bromide:

Cantil: 25 mg [DSC]

Brand Names: U.S.

  • Cantil [DSC]

Pharmacologic Category

  • Anticholinergic Agent
  • Antispasmodic Agent, Gastrointestinal

Pharmacology

Mepenzolate is a postganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon.

Absorption

Oral: Low

Excretion

Urine (3% to 22%); feces

Use: Labeled Indications

Adjunctive treatment of peptic ulcer disease; has not been shown to be effective in contributing to the healing of peptic ulcer, preventing complications, or decreasing the rate of recurrence

Contraindications

Allergic or idiosyncratic reactions to mepenzolate or related compounds; glaucoma; obstructive uropathy (ie, bladder neck obstruction due to prostatic hyperplasia); obstructive gastrointestinal disease (ie, pyloroduodenal stenosis, achalasia); paralytic ileus; intestinal atony of the debilitated or elderly patient; unstable cardiovascular status in acute GI hemorrhage; toxic megacolon complicating ulcerative colitis; myasthenia gravis

Dosing: Adult

Peptic ulcer disease: Oral: 25-50 mg 4 times/day

Dosing: Geriatric

Refer to adult dosing. Use caution or avoid; anticholinergics generally not tolerated in older adults.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Administration

Administration with meals and at bedtime is preferred.

Dietary Considerations

May be taken with meals.

Storage

Store below 30°C (86°F). Keep tightly sealed. Protect from heat.

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

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

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

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

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

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

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

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

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

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

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Adverse Reactions

Frequency not defined.

Cardiovascular: Palpitations, tachycardia

Central nervous system: Confusion, dizziness, drowsiness, headache, insomnia, nervousness

Dermatologic: Hypohidrosis, urticaria

Gastrointestinal: Ageusia, bloating, constipation, delayed gastric emptying, nausea, vomiting, xerostomia

Genitourinary: Decreased lactation, impotence, urinary hesitancy, urinary retention

Hypersensitivity: Anaphylaxis

Neuromuscular & skeletal: Weakness

Ophthalmic: Blurred vision, cycloplegia, increased intraocular pressure, mydriasis

Warnings/Precautions

Concerns related to adverse effects:

• 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, treatment should be discontinued if this occurs.

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

• Psychosis: Has been reported in patients with an extreme sensitivity to anticholinergic effects; usually resolves with discontinuation of treatment.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with coronary artery disease, tachycardia, arrhythmias, heart failure, or hypertension; evaluate tachycardia prior to administration.

• Gastric ulcer treatment: Use of anticholinergics in gastric ulcer treatment may cause a delay in gastric emptying due to antral stasis.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Hiatal hernia: Use with caution in patients with hiatal hernia with reflux esophagitis; may aggravate condition.

• Hyperthyroidism: Use with caution in patients with hyperthyroidism.

• Neuropathy: Use with caution in patients with autonomic neuropathy.

• Prostatic hyperplasia: Use with caution in patients with prostatic hyperplasia.

• Renal impairment: Use with caution in patients with renal impairment.

• Ulcerative colitis: Use with caution in patients with ulcerative colitis; may precipitate/aggravate toxic megacolon.

Special populations:

• Elderly: Use with caution in the elderly; increased risk for anticholinergic effects, confusion, and hallucinations.

Dosage form specific issues:

• Tartrazine: Some products may contain tartrazine.

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience lightheadedness, fatigue, blurred vision, headache, change in taste, nausea, vomiting, constipation, or dry mouth. Have patient report immediately to prescriber severe dizziness, passing out, severe loss of strength and energy, change in balance, tachycardia, arrhythmia, confusion, mood changes, hallucinations, memory impairment, insomnia, difficulty speaking, vision changes, diarrhea, sexual dysfunction, urinary retention, or lack of sweat (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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