Eperisone

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Eperisone
Clinical data
Trade namesMyonal
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Ora
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • (2RS)-1-(4-Ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
JSmol)
  • CCc1ccc(cc1)C(=O)C(C)CN2CCCCC2
  • InChI=1S/C17H25NO/c1-3-15-7-9-16(10-8-15)17(19)14(2)13-18-11-5-4-6-12-18/h7-10,14H,3-6,11-13H2,1-2H3 checkY
  • Key:SQUNAWUMZGQQJD-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Eperisone (formulated as the eperisone hydrochloride salt) is an antispasmodic drug.

Eperisone acts by relaxing both

ischaemia, and hypertonia in skeletal muscles, thus alleviating stiffness and spasticity, and facilitating muscle movement[1]

Eperisone also improves

cervical spondylosis
.

Eperisone has a relatively low incidence of

clinical application of the drug and makes it an attractive choice for patients who require antispasmodic therapy without a reduction in alertness
.

Japanese package of eperisone

Eperisone also facilitates voluntary movement of the upper and lower extremities without reducing muscle power; it is therefore useful during the initial stage of rehabilitation and as a supporting drug during subsequent rehabilitative therapy.

Indications

Presentation

Eperisone hydrochloride is available as the brand name preparations Myonal and Epry as 50 mg sugar-coated tablets, or as 10% granules for oral administration.[6] An experimental form of the drug, as a transdermal patch system, has shown promising results in laboratory tests on rodents; however, this product is not currently available for human use.[7]

Dosage and administration

In adults, the usual dose of eperisone is 50–150 mg per day, in divided doses, after meals. However, the dosage is adjusted by the

symptoms
, patient age and response.

Eperisone has not been established as definitely safe for

paediatric use, therefore its use in paediatrics cannot be recommended without further study.[6]

If

elderly patients are treated with eperisone, a reduced dose is recommended, and the patient should be closely monitored for signs of physiological hypofunction during treatment.[6]

Safety during pregnancy and breast-feeding

Eperisone has not been established to be safe for use by

breast-feeding
). If eperisone must be used, the patient is advised to stop breast-feeding for the duration of treatment. Eperisone has been reported to be excreted in breast milk in an animal study (in rats).

Pharmacology

Contraindications

Eperisone is

contraindicated in patients with known hypersensitivity to the drug.[8]
Side effects: 'very rare' excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhoea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation etc.[9]

Cautions

Eperisone should be administered with care in patients with a history of hypersensitivity to any medication, or with disorders of liver function (it may aggravate hepatic dysfunction).

symptoms may occur. In the event of such symptoms, the dosage should be reduced or treatment discontinued. Patients should be cautioned against engaging in potentially hazardous activities requiring alertness, such as operating machinery or driving a car.[6]

Side effects

Drug interactions

There have been reports of disturbances in

accommodation occurring after the concomitant use of the related drug tolperisone hydrochloride and methocarbamol
.

Safety in overdose

Seizures have been reported in an infant after accidental ingestion of eperisone.[11]

Future developments

Eperisone suffers from a very low

first pass intestinal metabolism; a transdermal patch containing eperisone is currently in development in South Korea.[1]
This has shown promise, with the antispasmodic effect lasting over 24 hours, compared to one to two hours following oral administration.

Eperisone is also under investigation as an

beagles.[12]

Brand names

Eperisone is marketed under many brand names worldwide.[13]

See also

Chemically and mechanistically related drugs:

References

  1. ^
    S2CID 24474033
    .
  2. ^ "eperisone Summary Report - CureHunter". www.curehunter.com.
  3. PMID 10389124
    .
  4. ^ a b "Myonil®" (PDF). Archived from the original (PDF) on 2009-02-06. Retrieved 2008-09-01.
  5. ^ "Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study". europeanreview.org. 17 October 2012.
  6. ^ a b c d "Myonal Tablets 50 mg" (PDF). Archived from the original (PDF) on 2009-12-29. Retrieved 2008-09-01.
  7. S2CID 24474033
    .
  8. ^ Clinical trial number NCT00327730 for "Evaluation of Eperisone HCl in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain" at ClinicalTrials.gov
  9. ^ "Myonil®" (PDF). Archived from the original (PDF) on 2010-11-28. Retrieved 2010-06-12.
  10. PMID 17671415. Archived from the original
    on 2014-12-19. Retrieved 2008-09-28.
  11. PMID 17499672
    .
  12. ^ EP 0310259  Eperisone as a hypotensive agent
  13. ^ "International eperisone brands". Drugs.com. Retrieved 10 March 2016.

Further reading
Retrieved from "https://en.wikipedia.org/w/index.php?title=Eperisone&oldid=1199777048"