Methscopolamine

METHSCOPOLAMINE- methscopolamine bromide tablet
Golden State Medical Supply, Inc.

Rx Only

DESCRIPTION

Methscopolamine Bromide Tablets USP, 2.5 mg and 5mg contain methscopolamine bromide, an anticholinergic, which occurs as white crystals, or as a white odorless crystalline powder. Methscopolamine bromide melts at about 225°C with decomposition. The drug is freely soluble in water, slightly soluble in alcohol, and insoluble in acetone and in chloroform.

The chemical name for methscopolamine bromide is 3-Oxa-9-azoniatricyclo [3.3.1.02,1ronane, 7-(3-hydroxy-1-000-2-phenyl-propoxy)-9, 9-dimethyl-, bromide, [7(5)-(1., 26, 46, 5., 76) ]-and the molecular weight is 398.30.

The structural formula is represented below:

Chemical Structure -- Methscopolamine
(click image for full-size original)

Methscopolamine Bromide Tablets USP, 2.5 mg for oral administration contain 2.5 mg of methscopolamine bromide.

Methscopolamine Bromide Tablets USP, 5 mg for oral administration contain 5mg of methscopolamine bromide.

Inactive ingredients: microcrystalline cellulose, pregelatinized starch, magnesium stearate.

Contains no lactose.

CLINICAL PHARMACOLOGY

Methscopolamine bromide is an anticholinergic agent which possesses most of the pharmacological actions of that drug class. These include reduction in volume and total acid content gastric secretion, inhibition of gastrointestinal motility, inhibition of salivary excretion, dilation of the pupil and inhibition of accommodation with resulting blurring of vision. Large doses may result in tachycardia.

PHARMACOKINETICS

Methscopolamine bromide is quaternary ammonium derivative of scopolamine. As a class, these agents are poorly and unreliably absorbed. 1, 2 Total absorption of quaternary ammonium derivatives of the alkaloids is 10-25%. Rate of absorption is not available. Quaternary ammonium salts have limited absorption from intact skin, and conjunctival penetration is poor.1 Little is known of the fate and excretion of most of these agents .1 Following oral administration, drug effects appear in about one hour and persist for 4 to 6 hours.2 Methscopolamine bromide has limited ability to cross the blood-brain-barrier.3,4,5 The drug is excreted primarily in the urine and bile, or as unabsorbed drug in feces.2 There is no data on the presence of methscopolamine in breast milk; traces of atropine have been found after administration of atropine .1

INDICATIONS AND USAGE

Adjunctive therapy for the treatment of peptic ulcer.

METHSCOPOLAMINE BROMIDE HAS NOT BEEN SHOWN TO BE EFFECTIVE IN CONTRIBUTING TO THE HEALING OF PEPTIC ULCER, DECREASING THE RATE OF RECURRENCE OR PREVENTING COMPLICATIONS.

CONTRAINDICATIONS

Glaucoma; obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy); obstructive disease of the gastrointestinal tract (e.g., pyloroduodenal stenosis); paralytic ileus; intestinal atony of the elderly or debilitated patient; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis; toxic megacolon complicating ulcerative colitis; myasthenia gravis. Methscopolamine bromide tablets USP, 2.5 mg and 5 mg are contraindicated in patients who am hypersensitive to methscopolamine bromide or related drugs.

WARNINGS

In the presence of high environmental temperature, heat prostration (fever and heat stroke due to decreased sweating) can occur with drug use. 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. Methscopolamine bromide 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 overdosage, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and possible paralysis.

PRECAUTIONS

1. General

Use methscopolamine bromide tablets USP, 2.5 mg and 5mg with caution in the elderly and in all patients with: autonomic neuropathy; hepatic or renal disease; or ulcerative colitis-large doses may suppress intestinal motility to the point of producing a paralytic ileus and for this reason precipitate or aggravate “toxic megacolon,” a serious complication of the disease.

The drug also should be used with caution in patients having hyperthyroidism, coronary heart disease, congestive heart failure, tachyrhythmia, tachycardia, hypertension, or prostatic hypertrophy.

2. Information for Patients

See statement under WARNINGS.

3. Laboratory Tests

Progress of the peptic ulcer under treatment should be followed by upper gastrointestinal contrast radiology or endoscopy to insure healing. Stool tests for occult blood and blood hemoglobin or hematocrit values should be followed to rule out bleeding from the ulcer.

4. Drug Interactions

Additive anticholinergic effects may result from concomitant use with antipsychotics, tricyclic antidepressants, and other drugs with anticholinergic effects. Concomitant administration with antacids may interfere with the absorption of methscopolamine bromide.

5. Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term studies in animals have been performed to evaluate carcinogenic potential.

6. Pregnancy Teratogenic Effects

Pregnancy Category C

Animal reproduction studies have not been conducted with methscopolamine bromide. It is also not known whether methscopolamine bromide can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Methscopolamine bromide should be given to a pregnant woman only if clearly needed.

7. Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when methscopolamine bromide is administered to a nursing woman. Anticholinergic drugs may suppress lactation.

9. Pediatric Use

Safety and efficacy in children have not been established.

ADVERSE REACTIONS

The following adverse reactions have been observed, but there is not enough data to support an estimate of frequency.

Cardiovascular. Tachycardia, palpitation.

Allergic: Severe allergic reaction or drug idiosyncrasies including anaphylaxis.

CNS: Headaches, nervousness, mental confusion, drowsiness, dizziness.

Special Senses: Blurred vision, dilatation of the pupil, cycloplegia, increased ocular tension, loss of taste.

Renal: Urinary hesitancy and retention.

Gastrointestinal: Nausea, vomiting, constipation, bloated feeling.

Dermatologic: Decreased sweating, urticaria and other dermal manifestations.

Miscellaneous: Xerostomia, weakness, insomnia, impotence, suppression of lactation.

DRUG ABUSE AND DEPENDENCE

Not applicable.

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