Mebeverine

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1 : 1 mixture (racemate)Mebeverine
Systematic (IUPAC) name
(RS)-4-(ethyl[1-(4-methoxyphenyl)propan-2-yl]amino)butyl 3,4-dimethoxybenzoate
Identifiers
CAS number 2753-45-9
ATC code A03AA04
PubChem 4031
Chemical data
Formula C25H35NO5 
Mol. mass 429,6[g/mol]
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status

P(UK)

Routes Oral

Mebeverine is a drug whose major therapeutic role is in the treatment of irritable bowel syndrome (IBS) and the associated abdominal cramping. It works by relaxing the muscles in and around the gut. It is a musculotropic antispasmodic drug without anticholinergic side-effects. The drug is also indicated for treatment of gastrointestinal spasm secondary to organic disorder.

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Indications

Spastic functional disturbances of the colon:

  • Irritable bowel syndrome in its primary form
  • Irritable bowel syndrome associated with organic lesions of the gastrointestinal tract such as; diverticulosis and diverticulitis, regional enteritis, disease of the gall bladder and gall ducts, gastric and duodenal ulcers, dysentery, and aspecific or specific inflammation of the digestive tract.
  • Mebeverine should be taken 20 minutes before meals.

Mechanism of action

Mebeverine is an antimuscarinic. It belongs to a group of compounds called musculotropic antispasmodics. These compounds act directly on the gut muscles at the cellular level to relax them. This relieves painful muscle spasms of the gut, without affecting its normal motility. Mebeverine is used to relieve symptoms of irritable bowel syndrome and related intestinal disorders that are the result of spasms in the intestinal muscles. These include colicky abdominal pain and cramps, diarrhoea alternating with constipation and flatulence (wind).

Mebeverine is also an inhibitor of calcium-depot replenishment. Therefore, it has dual mode of action which normalizes the small bowel motility.

Adverse effects

Side effects may include:[1]

  • Indigestion or heartburn
  • Constipation
  • Dizziness
  • Insomnia (difficulty sleeping)
  • anorexia (loss of appetite)
  • Headache
  • Tiredness
  • Slow heart beat
  • Rash and/or itchy skin

Since 1978, 21 cases of severe adverse reactions to mebeverine were reported in the Netherlands.[2] Most reactions consisted of urticaria or maculopapular rash, sometimes accompanied by fever, polyarthritis, thrombopenia or angioedema.

Very rarely, people taking this medicine may develop allergic reactions.[3]

Pregnancy and breastfeeding

Mebeverine passes into breast milk, but the amount is considered too small to be harmful to a nursing infant.[1]

Driving and using machines

Mebeverine is unlikely to affect the ability to operate machinery or to drive, yet not completely out of the question. [4] [5]

History

It was first registered in 1965.[6]

Availability

Mebervine is a generic drug and is available internationally under many brand names.[7]

References

  1. 1.0 1.1 Colofac Data Sheet (PDF) http://www.medsafe.govt.nz/profs/datasheet/c/colofactab.pdf
  2. in 't Veld BA, van Puyenbroek E, Stricker BH. (1997). Hypersensitivity reactions to use of mebeverine. pp. 1392–5.  Ned Tijdschr Geneeskd. 1997 July 12;141(28):1392-5. Hypersensitivity reactions to use of mebeverine [1] pubmed: 9380201
  3. Colofac Patient leaflet sheet http://emc.medicines.org.uk/medicine/2531/PIL/Colofac+Tablets+135mg/
  4. http://www.drugs.com/uk/mebeverine-50mg-5ml-sugar-free-oral-suspension-leaflet.html
  5. http://www.nhs.uk/medicine-guides/pages/MedicineOverview.aspx?condition=Irritable%20bowel&medicine=mebeverine%20hydrochloride&preparation=Mebeverine%20135mg%20tablets
  6. Mebeverine page at druginfosys Page accessed Feb 1, 2015
  7. International page at drugs.com for Mebeverine Page accessed Feb 1, 2015

External links

Template:Cholinergics


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