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Eperisone

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Antispasmodic and muscle relaxant drug
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Pharmaceutical compound
Eperisone
Clinical data
Trade namesMyonal
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • (2RS)-1-(4-Ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC17H25NO
Molar mass259.393 g·mol−1
3D model (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 theeperisone hydrochloride salt) is anantispasmodic drug.

Eperisone acts by relaxing bothskeletal muscles andvascular smooth muscles, and demonstrates a variety of effects such as reduction ofmyotonia, improvement ofcirculation, and suppression of the pain reflex. The drug inhibits the vicious circle of myotonia by decreasing pain,ischaemia, andhypertonia in skeletal muscles, thus alleviating stiffness andspasticity, and facilitating muscle movement[1]

Eperisone also improvesdizziness andtinnitus associated withcerebrovascular disorders orcervical spondylosis.

Eperisone has a relatively low incidence ofsedation when compared with other antispasmodic drugs; this simplifies theclinical application of the drug and makes it an attractive choice for patients who require antispasmodic therapy without a reduction inalertness.

Japanese package of eperisone

Eperisone also facilitates voluntary movement of the upper and lowerextremities without reducing muscle power; it is therefore useful during the initial stage ofrehabilitation and as a supporting drug during subsequent rehabilitativetherapy.

Indications

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Presentation

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Eperisone hydrochloride is available as the brand name preparations Myonal and Epry as 50 mgsugar-coated tablets, or as 10% granules for oral administration.[6] An experimental form of the drug, as atransdermal 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

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In adults, the usual dose of eperisone is 50–150 mg per day, in divided doses, after meals. However, the dosage is adjusted by theprescribingclinician depending on factors such as severity ofsymptoms, patient age and response.

Eperisone has not been established as definitely safe forpaediatric use, therefore its use in paediatrics cannot be recommended without further study.[6]

Ifelderly 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

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Eperisone has not been established to be safe for use bypregnant women; therefore the drug should not be used in pregnant women, or women who may be pregnant, if the expectedtherapeutic benefits will outweigh the possible risks associated with treatment. The manufacturers of Myonal recommend the drug not be used duringlactation (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

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Contraindications

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Eperisone iscontraindicated in patients with knownhypersensitivity 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

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

Weakness,light-headedness,sleepiness or othersymptoms 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

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Drug interactions

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There have been reports of disturbances inocularaccommodation occurring after the concomitant use of the related drugtolperisone hydrochloride andmethocarbamol.

Safety in overdose

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

Future developments

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Eperisone suffers from a very lowbioavailability when taken orally, as a result of highfirst pass intestinalmetabolism; atransdermal patch containing eperisone is currently in development inSouth 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 anantihypertensive agent, with promising results from trials onbeagles.[12]

Brand names

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

See also

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Chemically and mechanistically related drugs:

References

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  1. ^abYang SI, Park HY, Lee SH, Lee SJ, Han OY, Lim SC, et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone".Pharmacology.71 (3):150–156.doi:10.1159/000077449.PMID 15161997.S2CID 24474033.
  2. ^"eperisone Summary Report - CureHunter".www.curehunter.com.
  3. ^Bose K (April 1999). "The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial".Methods and Findings in Experimental and Clinical Pharmacology.21 (3):209–213.doi:10.1358/mf.1999.21.3.534831.PMID 10389124.
  4. ^ab"Myonil®"(PDF). Archived fromthe original(PDF) on 2009-02-06. Retrieved2008-09-01.
  5. ^"Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study".europeanreview.org. 17 October 2012.
  6. ^abcd"Myonal Tablets 50 mg"(PDF). Archived fromthe original(PDF) on 2009-12-29. Retrieved2008-09-01.
  7. ^Yang SI, Park HY, Lee SH, Lee SJ, Han OY, Lim SC, et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone".Pharmacology.71 (3):150–156.doi:10.1159/000077449.PMID 15161997.S2CID 24474033.
  8. ^Clinical trial numberNCT00327730 for "Evaluation of Eperisone HCl in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain" atClinicalTrials.gov
  9. ^"Myonil®"(PDF). Archived fromthe original(PDF) on 2010-11-28. Retrieved2010-06-12.
  10. ^Ueno T, Kawana S (July 2007)."[A case of eperisone hydrochloride (myonal)--induced drug eruption leading to erythema and angioedema]".Arerugi = [Allergy] (in Japanese).56 (7):709–713.PMID 17671415. Archived fromthe original on 2014-12-19. Retrieved2008-09-28.
  11. ^Tanno K, Narimatsu E, Takeyama Y, Asai Y (May 2007). "Infantile case of seizure induced by intoxication after accidental consumption of eperisone hydrochloride, an antispastic agent".The American Journal of Emergency Medicine.25 (4):481–482.doi:10.1016/j.ajem.2006.09.002.PMID 17499672.
  12. ^EP 0310259  Eperisone as a hypotensive agent
  13. ^"International eperisone brands".Drugs.com. Retrieved10 March 2016.

Further reading

[edit]
Peripherally acting
(primarilyantinicotinic,
NMJ block)
Non-depolarizing
Curarealkaloids
4° ammonium agents
Depolarizing
ACh release inhibitors
Centrally acting
Carbamic acid esters
Benzodiazepines
Nonbenzodiazepines
Thienodiazepines
Quinazolines
Anticholinergics
(Antimuscarinics)
Other
Directly acting
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