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]
Pharmacology
Mechanism of Action
Mepenzolate is a postganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon.
Pharmacokinetics/Pharmacodynamics
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
Dosage and Administration
Dosing: Adult
Peptic ulcer disease: Oral: 25-50 mg 4 times/day
Dosing: Geriatric
Avoid use (Beers Criteria [AGS 2019]).
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
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
Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy
Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. 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. Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. 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
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. Monitor therapy
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. 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
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. 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
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Avoid combination
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of 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
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, fast heartbeat, arrhythmia, confusion, mood changes, sensing things that seem real but are not, trouble with memory, trouble sleeping, difficulty speaking, vision changes, diarrhea, sexual dysfunction, unable to pass urine, 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.
