Mepenzolate

Uses

Mepenzolate is a postganglionic parasympathetic inhibitor that was previously approved for improving the healing of gastric ulcers, but has been discontinued.

For use as adjunctive therapy in the treatment of peptic ulcer. It has not been shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or preventing complications.

Mepenzolate is also used to associated treatment for these conditions: Peptic Ulcer

How Mepenzolate works

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.

Toxicity

The signs and symptoms of overdosage are headache; nausea; vomiting; blurred vision; dilated pupils; hot, dry skin; dizziness; dryness of the mouth; difficulty in swallowing; and CNS stimulation. A curare-like action may occur (i.e., neuromuscular blockade leading to muscular weakness and possible paralysis). The oral LD₅₀ is greater than 750 mg/kg in mice and greater than 1000 mg/kg in rats.

Mepenzolate Alcohol interaction

[Moderate] GENERALLY AVOID:

Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.

In addition, the potential for abuse may be increased with the combination.

The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.

No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.

However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.

Alcohol should generally be avoided during therapy with anticholinergic agents.

Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.

Mepenzolate Hypertension interaction

[Minor] Cardiovascular effects of anticholinergics may exacerbate hypertension.

Therapy with anticholinergic agents should be administered cautiously in patients with hypertension.

Mepenzolate Drug Interaction

Moderate: tiotropium, tiotropiumMinor: acetaminophen, acetaminophenUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, glucose, glucose

Mepenzolate Disease Interaction

Major: arrhythmias, autonomic neuropathy, GI obstruction, glaucoma, obstructive uropathy, tardive dyskinesia, infectious diarrheaModerate: psychosesMinor: hypertension, fever

Elimination Route

Between 3 and 22% of an orally administered dose is excreted in the urine over a 5-day period, with the majority of the radioactivity appearing on Day 1. The remainder appears in the next 5 days in the feces and presumably has not been absorbed.

Elimination Route

Between 3 and 22% of an orally administered dose is excreted in the urine over a 5-day period, with the majority of the radioactivity appearing on Day 1.

Innovators Monograph

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