Mebeverine

Medical use

Mebeverine is used to alleviate some of the symptoms of irritable bowel syndrome (IBS) and related conditions; specifically stomach pain and cramps, persistent diarrhoea, and flatulence.

Historically data from controlled clinical trials have not found a difference from placebo or statistically significant results in the global improvement of IBS. However, more recent systematic reviews found Mebeverine is an effective treatment option in IBS, with a good safety profile and low frequency of adverse effects.

It has not been tested in pregnant women nor in pregnant animals so pregnant women should not take it; it is expressed at low levels in breast milk, while no adverse effects have been reported in infants, breastfeeding women should not take this drug.

Adverse effects

Adverse effects include hypersensitivity reactions and allergic reactions, immune system disorders, skin disorders including hives, oedema and widespread rashes.

Additionally, the following adverse effects have been reported: heartburn, indigestion, tiredness, diarrhoea, constipation, loss of appetite, general malaise, dizziness, insomnia, headache, and decreased pulse rate.

It does not have systemic anticholinergic side effects.

Mebeverine can, on highly rare occasions, cause drug-induced acute angle closure glaucoma.

In a urine drug-screening test, mebeverine can affect a false positive result for amphetamines.

Pharmacology

Mechanism of action

Mebeverine is an anticholinergic but its mechanism of action is not known; it appears to work directly on smooth muscle within the gastrointestinal tract and may have an anaesthetic effect, may affect calcium channels, and may affect muscarinic receptors.

Pharmacokinetics

It is metabolized mostly by esterases, and almost completely. The metabolites are excreted in urine.

Mebeverine exists in two enantiomeric forms. The commercially available product is a racemic mixture of them. A study in rats indicates that the two have different pharmacokinetic profiles.

The drug contains the psychoactive drugs moiety such as para-methoxy-N-ethylamphetamine (PMEA) and para-methoxyamphetamine (PMA) within its chemical structure and can form these drugs as minor active metabolites. This can result in false positives for "ecstasy" on drug tests.

History

It is a second generation papaverine analog, and was first synthesized around the same time as verapamil.

It was first registered in 1965.

Availability

Mebeverine is a generic drug and is available internationally under many brand names, such as Duspatalin as sold by Abbott or Mave and Mave SR by .

References

References

1. (14 June 2017). "Colofac data sheet". New Zealand Medicines and Medical Devices Safety Authority.
2. (26 August 2016). "Colofac Tablets 135mg - Summary of Product Characteristics (SPC)". UK Electronic Medicines Compendium.
3. (May 2014). "Role of antispasmodics in the treatment of irritable bowel syndrome". World Journal of Gastroenterology.
4. (February 2010). "A systematic review of efficacy and tolerability of mebeverine in irritable bowel syndrome". World Journal of Gastroenterology.
5. (February 2022). "The Efficacy of Mebeverine in the Treatment of Irritable Bowel Syndrome-A Systematic Review". Journal of Clinical Medicine.
6. (March 2007). "Drug-induced acute angle closure glaucoma". Current Opinion in Ophthalmology.
7. Optimisation, NECS Medicines. (2015-07-21). "Misuse of hyoscine butylbromide (Buscopan) {{!}}".
8. (August 2012). "Fiber-based liquid-phase micro-extraction of mebeverine enantiomers followed by chiral high-performance liquid chromatography analysis and its application to pharmacokinetics study in rat plasma". Chirality.
9. "Мебеверин (Mebeverine)".
10. (2005). "Drug Discovery: A History". John Wiley & Sons.
11. "Mebeverine". druginfosys.
12. "Mebeverine". drugs.com.