Mebeverine
Meverin®
Category:
Antispasmodic
(Martindale)
Chemistry:
4-[Ethyl(4-methoxy-α-methylphenethyl)amino]butyl veratrate hydrochloride. C25H35NO5.HCl , Mw= 466.0
Pharmacokinetic/Mechanism of Action:
Mebeverine has a direct non-specific relaxant effect on vascular, cardiac and other smooth muscle. This compound possesses a polyvalent spasmolytic action in which at least three types of mechanisms are involved:
- a direct musculotropic action involving calcium ion exchange and stabilization of excitable membranes.
- a competitive antimuscarinic activity of about 0.05-0.1 times that of atropine.
- a local anaesthetic activity together with potentiation of sympathetic inhibitory influences due to blockade of noradernaline uptake into sympathetic nerve endings.
(Vidal, Martindale)
Pharmacokinetic properties
Absorption Rapidly absorbed
Protein binding 75%
Biotransformation Completely metabolised by hydrolysis to veratric acid & mebeverine alcohol
Time to Peak Concentration 1-3 hours
Elimination The metabolites are excreted in the urine
(Martindale)
Indication:
Adjunct in gastrointestinal disorders characterized by smooth muscle spasm.
(BNF)
Contraindications:
- Hypersensitivity to Mebeverine or any components of the product.
- Children below 6 years.
(Vidal)
- Paralytic ileus
(BNF)
Warnings & Precautions:
1- Use with caution in patients with cardiac dysrhythmia, hepatic dysfunction and advanced renal disease.
(Vidal)
2- Avoid in porphyria.
(BNF)
Pregnancy:
Safe use in pregnancy has not been established relative to adverse effects on fetal development. Therefore mebeverine is not recommended during the first trimester of pregnancy, and otherwise risk-benefit must be considered in its use in pregnant women. Category B2.
(Vidal, Prescribing medicines in pregnancy 4th, edition TGA)
Breast-Feeding:
Mebeverine is secreted in breast milk. This drug should not be given to a woman who is breast feeding unless the anticipated benefits outweigh possible risks.
(Vidal, BNF)
Adverse Reactions:
Nausea, dizziness, headache, rare allergic reactions include: pruritus, urticaria, face oedema, angiodema.
Indigestion, heartburn, insomnia, anorexia, decrease in pulse rate, constipation, general malaise.
(Vidal, Martindale)
Overdose:
No data are available in regard to overdosage in humans. On theoretical grounds, it may be predicted that CNS excitability might occur in cases of overdosage.
No specific antidote is available. Treatment is symptomatic and supportive.
(Vidal)
Administration & Dosage:
Adults and children over 10 years:
- Tablet
135-150 mg 3 times daily preferably 20 minutes before meals.
- Extended release capsule
200 mg twice daily, to be given one in the morning and one in the evening preferably 20 minutes before meals.
Children under 10 years:
Is not recommended.
(BNF, Martindale)
Storage:
Store below 30oC.
How Supplied:
Mebeverine - Tedapharm are available as follows:
- 135 mg, biconvex, white and coated tablets. There are blisters of 5 × 10 in a box of 50's.
- 200 mg, white opaque capsule. There are blisters of 10's in a box of 30's.
References:
1- Martindale (36th edition)
2- BNF (57)
3- Vidal 2004
4- Colofac leaflet (solvay)