Methscopolamine

Methscopolamine reduces the secretions of certain organs in the body, such as the stomach.

Methscopolamine is used to reduce stomach acid secretion to help control peptic ulcers.

This medication does not help heal a stomach ulcer.

Methscopolamine may also be used for other purposes not listed in this medication guide.

You should not take this medication if you have glaucoma, urination problems due to a bladder obstruction, myasthenia gravis, a stomach disorder called paralytic ileus, or a blockage in your intestines, or severe ulcerative colitis with toxic megacolon.

Before taking methscopolamine, tell your doctor if you are allergic to any drugs, or if you have ulcerative colitis, kidney or liver disease, a thyroid disorder, high blood pressure or heart disease, a heart rhythm disorder, an enlarged prostate, or if you have had an ileostomy or colostomy.

To be sure this medication is helping your condition, you may need blood tests and x-rays or other scans of your stomach or intestines on a regular basis. Your stools may also need to be tested for the presence of blood. Do not miss any scheduled appointments.

Methscopolamine can cause side effects that may impair your vision, thinking, or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Cold or allergy medicine, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression or anxiety can add to sleepiness caused by methscopolamine. Tell your doctor if you regularly use any of these medicines.

Avoid drinking alcohol. It can increase some of the side effects of methscopolamine.

Avoid becoming overheated or dehydrated during exercise and in hot weather. Methscopolamine can decrease perspiration and you may be more prone to heat stroke.

Stop using this medication and call your doctor at once if you diarrhea, fast or pounding heartbeats, or if you are urinating less than usual or not at all.

Older adults may be more sensitive to the side effects of methscopolamine.

You should not take this medication if you are allergic to methscopolamine, or if you have:

• glaucoma;
• if you are unable to urinate due to a bladder obstruction;
• myasthenia gravis;
• a stomach disorder called paralytic ileus; or
• a blockage in your intestines, or severe ulcerative colitis with toxic megacolon.

Before taking methscopolamine, tell your doctor if you are allergic to any drugs, or if you have:

• ulcerative colitis;
• kidney disease;
• liver disease;
• a thyroid disorder;
• high blood pressure (hypertension);
• heart disease, congestive heart failure;
• a heart rhythm disorder;
• an enlarged prostate and problems with urination; or
• if you have had an ileostomy or colostomy.

If you have any of these conditions, you may need a dose adjustment or special tests to safely use methscopolamine.

FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

It is not known whether methscopolamine passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Older adults may be more sensitive to the side effects of methscopolamine.

You should not take this medication if you have glaucoma, urination problems due to a bladder obstruction, myasthenia gravis, a stomach disorder called paralytic ileus, or a blockage in your intestines, or severe ulcerative colitis with toxic megacolon.

Before taking methscopolamine, tell your doctor if you are allergic to any drugs, or if you have ulcerative colitis, kidney or liver disease, a thyroid disorder, high blood pressure or heart disease, a heart rhythm disorder, an enlarged prostate, or if you have had an ileostomy or colostomy.

To be sure this medication is helping your condition, you may need blood tests and x-rays or other scans of your stomach or intestines on a regular basis. Your stools may also need to be tested for the presence of blood. Do not miss any scheduled appointments.

Methscopolamine can cause side effects that may impair your vision, thinking, or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Cold or allergy medicine, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression or anxiety can add to sleepiness caused by methscopolamine. Tell your doctor if you regularly use any of these medicines.

Avoid drinking alcohol. It can increase some of the side effects of methscopolamine.

Avoid becoming overheated or dehydrated during exercise and in hot weather. Methscopolamine can decrease perspiration and you may be more prone to heat stroke.

Stop using this medication and call your doctor at once if you diarrhea, fast or pounding heartbeats, or if you are urinating less than usual or not at all.

Older adults may be more sensitive to the side effects of methscopolamine.

• If you have an allergy to methscopolamine or any other part of methscopolamine.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you have any of these health problems: Bleeding problems, bowel block, enlarged colon, glaucoma, myasthenia gravis, slow-moving GI (gastrointestinal) tract, trouble passing urine, or ulcerative colitis.

This is not a list of all drugs or health problems that interact with this medicine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take methscopolamine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

• Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert or have clear eyesight until you see how methscopolamine affects you.
• Talk with your doctor before you drink alcohol or use other drugs and natural products that slow your actions.
• Be careful in hot weather or while being active. Drink lots of fluids to stop fluid loss.
• Talk with your doctor before you take antacids while you are taking this medicine.
• If you are 65 or older, use methscopolamine with care. You could have more side effects.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Use methscopolamine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take 30 minutes before meals and at bedtime.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

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 of 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

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.

1. General precautions

Use Methscopolamine Bromide Tablets USP, 2.5 mg and 5 mg 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 patient

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

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.

8. Pediatric use

Safety and efficacy in children have not been established.

Methscopolamine is a quaternary ammonium derivative of scopolamine that exerts anticholinergic effects, which include reducing the volume and total acid content of gastric secretion, inhibiting gastrointestinal motility and salivary secretion, dilation of the pupil, and inhibition of accommodation that results in blurring of vision.

Absorption

Poorly and unreliably absorbed

Excretion

Bile and urine; feces (as unabsorbed drug)

Consult your pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Notes

Missed Dose

Consult your pharmacist.

Storage

Consult your pharmacist.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2016. Copyright(c) 2016 First Databank, Inc.

Adjunctive therapy:
Average dose: 2.5 mg orally one-half hour before meals and 2.5 to 5 mg at bedtime

If patients are experiencing symptoms such as severe abdominal pain or cramping which demand prompt relief, methscopolamine may be started on a daily dosage of 20 mg, administered in doses of 5 mg orally one-half hour before meals and at bedtime.

Summary of Use during Lactation

No information is available on the use of methscopolamine bromide during breastfeeding. Because methscopolamine bromide is a quaternary ammonium compound, it is not likely to be absorbed and reach the bloodstream of the infant. Long-term use of methscopolamine bromide might reduce milk production or milk letdown, but a single dose is unlikely to interfere with breastfeeding. During long-term use, observe for signs of decreased lactation (e.g., insatiety, poor weight gain).

To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.

Drug Levels

Maternal Levels. Relevant published information was not found as of the revision date. br>

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information in nursing mothers was not found as of the revision date. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion.[1][2][3][4][5] Anticholinergic drugs can also reduce serum prolactin in nonnursing women.[6] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

References

1. Aaron DK, Ely DG, Deweese WP et al. Reducing milk production in ewes at weaning using restricted feeding and methscopolamine bromide. J Anim Sci. 1997;75:1434-42. PMID: 9250502

2. Powell MR, Keisler DH. A potential strategy for decreasing milk production in the ewe at weaning using a growth hormone release blocker. J Anim Sci. 1995;73:1901-5. PMID: 7592071

3. Daniel JA, Thomas MG, Powell MR, Keisler DH. Methscopolamine bromide blocks hypothalmic-stimulated release of growth hormone in ewes. J Anim Sci. 1997;75:1359-62. PMID: 9159285

4. Bizzarro A, Iannucci F, Tolino A et al. Inhibiting effect of atropine on prolactin blood levels after stimulation with TRH. Clin Exp Obstet Gynecol. 1980;7:108-11. PMID: 6788407

5. Svennersten K, Nelson L, Juvnas-Moberg K. Atropinization decreases oxytocin secretion in dairy cows. Acta Physiol Scand. 1992;145:193-4. PMID: 1636447

6. Masala A, Alagna S, Devilla L et al. Muscarinic receptor blockade by pirenzepine: effect on prolactin secretion in man. J Endocrinol Invest. 1982;5:53-5. PMID: 6808052

Substance Name

Methscopolamine Bromide

CAS Registry Number

13265-10-6

Drug Class

Muscarinic Antagonists

Parasympatholytics