Propantheline Bromide

(British Approved Name, rINN)

What Is Propantheline Bromide?

Propantheline bromide is a medication classified as an antimuscarinic agent or anticholinergic. It works by blocking the effects of acetylcholine, a neurotransmitter that plays a role in various bodily functions. Propantheline is primarily used to treat certain gastrointestinal conditions, such as irritable bowel syndrome (IBS) and other gastrointestinal motility disorders.

Propantheline works by inhibiting the action of acetylcholine at muscarinic receptors, which are present in the smooth muscles of the gastrointestinal tract. By doing so, it helps to reduce smooth muscle contractions and modify gastrointestinal motility.

Propantheline is typically taken orally, usually before meals. The healthcare provider determines the dosage and frequency of administration based on the individual’s condition.

Common side effects may include dry mouth, blurred vision, constipation, and urinary retention. These are typical anticholinergic side effects.

Propantheline is contraindicated in individuals with certain conditions, such as glaucoma, obstructive urinary disorders, and myasthenia gravis.

Propantheline should be used cautiously in elderly individuals, as they may be more prone to specific side effects, such as confusion and constipation.

Propantheline may interact with other medications, including antacids, certain antidiarrheal medications, and drugs with antimuscarinic effects.

As with any medication, it’s crucial to use propantheline under the guidance of a healthcare professional. Inform your healthcare provider about your complete medical history and all the medications and supplements you are taking to ensure safe and effective use.

Pharmacokinetics

Propantheline bromide is incompletely absorbed from the gastrointestinal tract, and bioavailability is reported to be reduced by the food; it is extensively metabolized in the small intestine before absorption. The plasma elimination half-life after a single oral dose has been reported to be about 2 to 3 hours. Propantheline is eliminated mainly in the urine as metabolites and less than 10% as an unchanged drug. The duration of action is about 6 hours.

Uses

• Irritable Bowel Syndrome (IBS): Propantheline alleviates symptoms associated with IBS, including abdominal pain, cramps, and changes in bowel habits.
• Gastrointestinal Motility Disorders: It may be prescribed for other conditions characterized by abnormal gastrointestinal motility.
• Symptom Relief: Propantheline helps to relieve symptoms related to increased gastrointestinal motility, such as spasms and cramps. It is not a cure for underlying conditions but can provide symptomatic relief.

Administration

Propantheline bromide is a quaternary ammonium antimuscarinic with peripheral effects similar to atropine. It has been used as an antispasmodic for conditions associated with gastrointestinal spasms and as an adjunct in treating peptic ulcer disease. The initial oral dose is 15 mg thrice daily, 30 to 60 minutes before meals, and 30 mg at bedtime. Doses of up to 120 mg daily may be needed in some patients.

In elderly patients, doses of 7.5 mg three times daily may be sufficient. Doses of 300 micrograms/kg (to a maximum of 15 mg) given 3 or 4 times daily have been used to relieve gastrointestinal spasms in children aged one month to 12 years. Older children may be given the adult dose. Propantheline bromide has been used in treating adult enuresis or urinary incontinence and hyper-hidrosis in doses similar to those described above.

Hyperhidrosis

Some antimuscarinics, including propantheline, have been applied topically in treating hyperhidrosis. Adverse effects of oral antimuscarinics generally preclude their use by this route. However, oral propantheline was used successfully to control excessive sweating in 2 patients with spinal cord injuries, and it is sometimes used in palliative care to control night sweats. The BNF notes that propantheline may be used for gustatory sweating in patients with diabetic neuropathy.

Urinary incontinence

In the UK, guidelines issued by NICE suggest that propantheline should not be recommended for treating urinary incontinence or overactive bladder in women; other antimuscarinics are preferred.

Adverse Effects, Treatment, and Precautions

Like many medications, Propantheline bromide can cause side effects in some individuals. It’s important to note that not everyone will experience these side effects, and the severity and occurrence can vary. Common side effects are often related to the medication’s antimuscarinic (anticholinergic) effects. Here are some potential side effects of propantheline bromide:

1. Dry Mouth: Anticholinergic medications, including propantheline, can reduce saliva production, leading to a dry mouth sensation.
2. Blurred Vision: Propantheline may cause blurred vision or difficulty focusing, especially near distances.
3. Constipation: Antimuscarinic medications can slow down the movement of the digestive tract, leading to constipation.
4. Urinary Retention: Propantheline can affect the urinary tract muscles, potentially causing difficulty emptying the bladder and urinary retention.
5. Confusion: In some cases, especially in elderly individuals, anticholinergic medications may lead to confusion or cognitive impairment.
6. Dizziness: Propantheline may cause dizziness or lightheadedness, particularly when standing up from a sitting or lying position.
7. Increased Heart Rate (Tachycardia): Some individuals may experience increased heart rate as a side effect.
8. Sensitivity to Light: Propantheline can lead to increased sensitivity to light (photophobia) in some individuals.
9. Allergic Reactions: While rare, allergic reactions such as rash, itching, or swelling can occur. Seek medical attention if you experience severe allergic reactions.
10. Contact dermatitis has been reported after topical application of propantheline bromide.
11. Buccal and oesophageal ulceration: Severe buccal mucosal ulceration has been reported in a 95-year-old woman due to retaining emepronium bromide tablets in her mouth, and she has recurred on giving propantheline bromide tablets.

It is essential to notify your healthcare provider if you experience any side effects, especially if they are persistent, severe, or affecting your quality of life. Additionally, inform your healthcare provider before starting propantheline or any other antimuscarinic medication if you have a history of certain medical conditions, such as glaucoma, urinary retention, or myasthenia gravis.

Always take medications as prescribed and follow your healthcare provider’s instructions. Consult your healthcare provider for personalized guidance if you have concerns about side effects or interactions.

Interactions

Propantheline bromide may interact with other medications and substances, potentially affecting its effectiveness or increasing the risk of side effects. To ensure safe and appropriate use, you must inform your healthcare provider about all your medications, supplements, and over-the-counter drugs. Here are some potential interactions with propantheline bromide:

1. Antacids: Concurrent use of propantheline with antacids may reduce the absorption of propantheline. It is advisable to separate the administration of propantheline and antacids by at least 2 hours.
2. Antidiarrheal Medications: Concurrent use with other antimuscarinic or anticholinergic medications, including antidiarrheal medications, may increase the risk of side effects such as dry mouth, constipation, and blurred vision.
3. Other Anticholinergic Medications: Using propantheline with other anticholinergic medications may lead to additive antimuscarinic effects. This includes medications for allergies, motion sickness, and certain psychiatric conditions.
4. Phenothiazines (Antipsychotic Medications): Propantheline may enhance the antimuscarinic effects of phenothiazine medications, increasing the risk of side effects.
5. Tricyclic Antidepressants: Concurrent use with tricyclic antidepressants may increase antimuscarinic effects, leading to dry mouth, blurred vision, and constipation.
6. Amantadine: Propantheline may reduce the effectiveness of amantadine, an antiviral and antiparkinsonian medication.
7. Ketoconazole: Propantheline may reduce the absorption of ketoconazole, an antifungal medication. It is advisable to separate the administration of propantheline and ketoconazole by at least 2 hours.
8. Potassium Supplements: Concurrent use of propantheline with potassium supplements may increase gastrointestinal side effects, such as constipation.
9. Digoxin: Propantheline may increase the absorption of digoxin, a medication used for heart conditions. Monitoring and adjustment of digoxin dosage may be necessary.

It’s important to note that this is not an exhaustive list of interactions, and individual responses may vary. Always inform your healthcare provider about your medications and substances for personalized advice and guidance. Do not start, stop, or change the dosage of any medication without consulting your healthcare provider.

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Bromuro de propantelina; Propanteliinibromidi; Propantelin-bromid; Propantelina, bromuro de; Propantelinbromid; Propantelino bromidas; Propanthelini Bromidum; Propanthelinii Bromidum; Propanthelinium-bromid

BAN: Propantheline Bromide

INN: Propantheline Bromide [rINN (en)]

INN: Bromuro de propantelina [rINN (es)]

INN: Propanthéline, Bromure de [rINN (fr)]

INN: Propanthelini Bromidum [rINN (la)]

INN: Пропантелина Бромид [rINN (ru)]

Chemical name: Di-isopropylmethyl[2-(xanthen-9-ylcarbonyloxy)ethyl]ammonium bromide

Molecular formula: C23H30BrNO3 =448.4

CAS: 298-50-0 (propantheline); 50-34-0 (propantheline bromide)

ATC code: A03AB05

Read code: y01On [Antispasmodic]

Pharmacopoeias. In China, Europe, Japan, and the US.

European Pharmacopoeia, 6th ed. (Propantheline Bromide). A white or yellowish-white, slightly hygroscopic powder. It is very soluble in water, alcohol, and dichloromethane. Store in airtight containers.

The United States Pharmacopeia 31, 2008 (Propantheline Bromide). White or practically white, odorless crystals. Very soluble in water, alcohol, and chloroform, practically insoluble in ether and benzene.

Preparations

BP 2008: Propantheline Tablets

The United States Pharmacopeia 31, 2008: Propantheline Bromide Tablets

Proprietary Preparations

Australia:: Pro-Banthine

Canada: Propanthel

Denmark: Ercoril

India: Pro-Banthine

Indonesia: Pro-Banthine

Mexico: Propantel

New Zealand: Pro-Banthine

South Africa: Pro-Banthine

United Kingdom: Pro-Banthine

USA: Pro-Banthine

Multi-ingredient

Indonesia: Methaphyllin

Italy: Lexil