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Eperisone

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Eperisone

Eperisone
Systematic (IUPAC) name
(2RS)-1-(4-ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
Clinical data
AHFS/Drugs.com
Legal status
  • not licensed
Routes of
administration
O
Identifiers
CAS Registry Number  N
ATC code M03
PubChem CID:
DrugBank  N
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  N
ChEMBL  N
Chemical data
Formula C17H25NO
Molecular mass 259.387 g/mol
 N   

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

Eperisone acts by relaxing both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. The drug inhibits the vicious circle of myotonia by decreasing pain, ischaemia, and hypertonia in skeletal muscles, thus alleviating stiffness and spasticity, and facilitating muscle movement[1]

Eperisone also improves dizziness and tinnitus associated with cerebrovascular disorders or cervical spondylosis.

Eperisone has a relatively low incidence of sedation when compared with other antispasmodic drugs; this simplifies the 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.

Contents

  • Indications 1
  • Presentation 2
  • Dosage and administration 3
  • Safety during pregnancy and breast-feeding 4
  • Pharmacology 5
  • Contraindications 6
  • Cautions 7
  • Side effects 8
  • Drug interactions 9
  • Safety in overdose 10
  • Future developments 11
  • Brand names 12
  • See also 13
  • Notes 14
  • References 15

Indications

Presentation

Eperisone hydrochloride is available as the brand name preparation Myonal 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] It is also available as the brand name Epry as 50 mg as sugar coated tablets.

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 prescribing clinician depending on factors such as severity of 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 psychological hypofunction during treatment.[6]

Safety during pregnancy and breast-feeding

Eperisone has not been established to be safe for use by pregnant women; therefore the drug should only be used in pregnant women, or women who may be pregnant, if the expected therapeutic benefits will outweigh the possible risks associated with treatment. The manufacturers of Myonal recommend the drug not be used during lactation (breast-feeding). If eperisone must be used, the patient is advised to stop breast-feeding for the duration of treatment. Eperisone has beed 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).

Weakness, light-headedness, sleepiness or other 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 ocular 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 bioavailability when taken orally, as a result of high 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 antihypertensive agent, with promising results from trials on beagles.[12]

Brand names

Eperisone is sold in Bangladesh, China, India, Indonesia, Japan, United Arab Emirates, Qatar, Malaysia, the Philippines, Thailand, Sudan and Pakistan under the brand name Myonal[13] and in Italy under the brand name Expose.[14]

See also

Notes

  1. ^ a b Yang SI, Park HY, Lee SH; et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone". Pharmacology 71 (3): 150–6.  
  2. ^ http://www.curehunter.com/public/keywordSummaryC030848--4--ethyl-2-methyl-3-piperidino-propiophenone.do
  3. ^ Bose K (1999). "The efficacy and safety of eperisone in patients with cervical spondylosis: Results of a randomized, double-blind, placebo-controlled trial". Methods Find Exp Clin Pharmacol 21 (3): 209–13.  
  4. ^ a b http://squarepharma.com.bd/SPL_PI_PDF/myonil226.pdf
  5. ^ http://www.europeanreview.org/articolo.php?id=502
  6. ^ a b c d http://di.eisai.co.jp/di/EPI/MYO_T-G_EPI.pdf
  7. ^ Yang Sang-In; Park Ha-Young; Lee Sang-Ho; Lee Seung-Jin; Han Ok-Yeun; Lim Sung-Cil; Jang Choon-Gon; Lee Wan-Suk; Shin Young-Hee; Kim Jung-Ju; Lee Seok-Yong (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone". Pharmacology 71 (3): 150–6.  
  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. ^ http://www.squarepharma.com.bd/SPL_PI_PDF/myonil226.pdf
  10. ^ Ueno T, Kawana S (July 2007). "[A case of eperisone hydrochloride (myonal)--induced drug eruption leading to erythema and angioedema]". Arerugi (in Japanese) 56 (7): 709–13.  
  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". Am J Emerg Med 25 (4): 481–2.  
  12. ^ EP 0310259  Eperisone as a hypotensive agent
  13. ^ http://goliath.ecnext.com/coms2/gi_0199-451231/Tokyo-pharma-stocks-week-to.html
  14. ^ http://www.torrinomedica.it/farmaci/schedetecniche/Expose.asp

References

  • Fujioka M, Kuriyama H (December 1985). "Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery". J. Pharmacol. Exp. Ther. 235 (3): 757–63.  
  • Inoue S, Bian K, Okamura T, Okunishi H, Toda N (July 1989). "Mechanisms of action of eperisone on isolated dog saphenous arteries and veins" (– Scholar search). Jpn. J. Pharmacol. 50 (3): 271–82.  
  • Viveksarathi, K., et al. "Dosage form design and evaluation of eperisone hydrochloride matrix film coated extended release tablets." Int J Pharm Pharm Sci 4.2 (2012): 575-581. http://www.ijppsjournal.com/Vol4Issue2/3559.pdf
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