Mebeverine Hydrochloride

What Is Mebeverine Hydrochloride?

Mebeverine, also known as mebeverine hydrochloride, falls under the category of antispasmodic medications designed to alleviate muscle spasms.

It effectively relieves painful stomach cramps associated with conditions such as irritable bowel syndrome (IBS). The mechanism involves the relaxation of specific muscles in the gastrointestinal tract.

Mebeverine is formulated in both tablet and slow-release capsule forms, the latter often referred to as modified release.

While it requires a prescription, mebeverine tablets tailored for IBS symptoms are also available over the counter at pharmacies.

Pharmacokinetics

Mebeverine is rapidly absorbed after oral doses, with peak plasma concentrations occurring in 1 to 3 hours. It is 75% bound to albumin in plasma. Mebeverine is completely metabolized by hydrolysis to veratric acid and mebeverine alcohol, the latter of which may then be conjugated. The metabolites are excreted in the urine.

British Pharmacopoeia 2008 (Mebevenne Hydrochlonde). A white or almost white crystalline powder. Very soluble in water, freely soluble in alcohol, practically insoluble in ether. A 2% solution in water has a pH of 4.5 to 6.5. Store in airtight containers at a temperature not exceeding 30°. Protect from light.

Uses and Administration

Mebeverine hydrochloride is an antispasmodic with a direct action on the smooth muscle of the gastrointestinal tract. It is used in conditions such as irritable bowel syndrome in a usual oral dose of 135 mg three times daily before meals; 100 mg three times daily has also been used.

A modified-release preparation is also available, taken as 200 mg twice daily. The embonate is also used for oral liquid preparations in a dose equivalent to 150 mg of hydrochloride thrice daily. The BNFC suggests that the following hydrochloride-equivalent doses may be given three times daily, based on age:

• 25 mg for those aged 3 to 4 years;
• 50 mg for those 4 to 8 years;
• 100 mg for those 8 to 10 years;
• 135 to 150 mg for those over 10 years.

Consume mebeverine approximately 20 minutes before your meal for optimal effectiveness. The onset of mebeverine’s action occurs approximately 1 hour after ingestion. Generally considered safe, the likelihood of experiencing side effects is low; however, a few individuals may encounter a mild, itchy rash known as hives.

Mebeverine is suitable for most adults and children aged 10 years and above. It may sometimes be prescribed for children three years or older.

Contraindications

Mebeverine may not be suitable for some individuals. To ensure its safety for you, inform a doctor or pharmacist before taking it if you:

• have experienced an allergic reaction to mebeverine or any other medication;
• suffer from constipation due to paralytic ileus (inactive gut);
• have a rare inherited condition preventing the digestion of galactose (a sugar in lactose);
• are pregnant, attempting to conceive, or breastfeeding.

If considering purchasing the medicine without a prescription, consult with a pharmacist or doctor first if you:

• are 40 years old or older;
• notice blood in your stool;
• experience nausea or vomiting;
• have a diminished appetite or recent weight loss;
• appear paler than usual and feel fatigued;
• encounter unusual vaginal bleeding or discharge;
• suspect or have symptoms of food poisoning, particularly after recent travel abroad.

Adverse Effects and Precautions

Although adverse effects appear rare, gastrointestinal disturbances, dizziness, headache, insomnia, anorexia, and decreased heart rate have been reported in patients receiving mebeverine. Cases of hypersensitivity, including erythematous rash, urticaria, and angioedema, have also been reported. Mebeverine should be avoided in patients with paralytic ileus. Based on theoretical concerns, it should be used with care in patients with marked hepatic or renal impairment and those with cardiac disorders such as heart block.

Any side effects that do arise are likely to be mild and transient.

Mild side effects are infrequent, but some individuals may develop a mild, itchy skin rash due to mebeverine. If this occurs, taking an antihistamine, available at pharmacies, may provide relief. Consult with a pharmacist to determine the most suitable type for you.

If the rash persists or becomes bothersome, it’s advisable to discontinue mebeverine. Seek advice from a pharmacist or doctor to explore alternative medication options.

In rare instances, mebeverine can trigger a severe allergic reaction known as anaphylaxis. If you suspect such a reaction, seek immediate medical attention.

Cystic fibrosis

A 24-year-old man with cystic fibrosis, given mebeverine hydrochloride for lower abdominal pain and constipation, was found to have a perforated stercoral ulcer with generalized peritonitis. It was suggested that mebeverine produced colonic stasis, predisposing the patient to ulceration. Still, the manufacturers considered that the development of constipation and distal intestinal syndrome (meconium ileus equivalent) in this patient precipitated the development of stercoral ulceration. It was recommended that antispasmodics such as mebeverine should not be used for the symptomatic treatment of distal intestinal syndrome in cystic fibrosis.

Porphyria

Mebeverine hydrochloride is considered to be unsafe in patients with porphyria because it is porphyrinogenic in in-vitro systems.

Interactions

Be cautious when combining mebeverine with other medications. Using it alongside most prescription drugs and common pain relievers like paracetamol and ibuprofen is generally safe.

However, it’s advisable to avoid simultaneous use of mebeverine with other treatments for irritable bowel syndrome (IBS) since they operate on the same principle.

Unless a doctor advises otherwise, refrain from taking more than one IBS remedy concurrently. Doing so is unlikely to provide additional symptom relief and may increase the risk of side effects.

When it comes to mixing mebeverine with herbal remedies and supplements, exercise caution. There is insufficient information to confirm the safety of combining complementary medicines and herbal remedies with mebeverine. These substances are not subjected to the same rigorous testing as pharmacy and prescription medications, especially regarding their potential interactions with other drugs.

Drug Approvals

(BANM, US Adopted Name, rINNM)

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

Synonyms: CSAG-144; Mebeverina, hidrocloruro de

BAN: Mebeverine Hydrochloride [BANM]

USAN: Mebeverine Hydrochloride

INN: Mebeverine Hydrochloride [rINNM (en)]

INN: Hidrocloruro de mebeverina [rINNM (es)]

INN: Mébévérine, Chlorhydrate de [rINNM (fr)]

INN: Mebeverini Hydrochloridum [rINNM (la)]

INN: Мебеверина Гидрохлорид [rINNM (ru)]

Chemical name: 4-[Ethyl(4-methoxy-αmethylphenethyl)amino]butyl veratrate hydrochloride

Molecular formula: C25H35NO5,HCl =466.0

CAS: 3625-06-7 (mebeverine); 2753-45-9 (mebeverine hydrochloride)

ATC code: A03AA04

Read code: y01Ov

Pharmacopoeias. In British.

Manufacturer

British Pharmacopoeia 2008: Mebeverine Tablets.

Other Brand Names in Different Countries

Argentina: Duspatalin

Australia: Colese Colofac

Austria: Colofac

Belgium: Duspatalin Spasmonal

Brazil: Duspatalin

Chile: Doloverina Duspatal Evadol Meditoina

Czech Republic: Duspatalin

Denmark: Duspatalin

France: Colopriv Duspatalin Spasmopriv

Germany: Duspatal Mebemerck

Greece: Duspatalin Gastromins

Hong Kong: Duspatalin

Hungary: Duspatalin

India: Colospa

Indonesia: Duspatalin Irbosyd

Ireland: Colofac

Israel: Colotal

Italy: Duspatal

Malaysia: Duspatalin Lezpain Mebetin

Mexico: Arluy

The Netherlands: Duspatal

New Zealand: Colofac

Philippines: Duspatalin

Poland: Duspatalin

Portugal: Duspatal

Russia: Duspatalin

South Africa: Bevispas Colofac

Singapore: Duspatalin Mebetin

Spain: Duspatalin

Switzerland: Duspatalin

Thailand: Colofac Duspatin Menosor

Turkey: Duspatalin Duspaverin

UK: Colofac Equilon IBS Relief

Multi-ingredient

Hong Kong: Fybogel Mebeverine

Ireland: Fybogel Mebeverine

UK: Fybogel Mebeverine