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Eperisone
Systematic (IUPAC) name
(2RS)-1-(4-ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
Identifiers
CAS number 56839-43-1
ATC code M03BX09
PubChem 3236
Chemical data
Formula C 17H25NO 
Mol. mass 259.387 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status not licensed
Routes O

Eperisone (formulated as the eperisone hydrochloride salt) is an antispasmodic drug, sold in Bangladesh, China, India, Indonesia, Japan, United Arab Emirates, Malaysia, the Philippines and Thailand, under the brand name Myonal.

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 cycle 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 anti-spasmodic drugs; this simplifies the clinical application of the drug and makes it an attractive choice for patients who require anti-spasmodic therapy without a reduction in alertness.

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

Presentation

Eperisone hydrochloride is available as the brand name preparation Myonal as 50 mg enteric 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] (see Future developments, below).

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, it is recommended that a reduced dose is used, and the patient 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 that the drug is not used during lactation (breast-feeding). If eperisone must be used, it is recommended that the patient stops breast-feeding for the duration of treatment. (It has been reported that Eperisone is excreted in breast milk in an animal study (in rats).

Pharmacology

Contraindications

Eperisone is contraindicated in patients with known hypersensitivity to the drug.[8]

Cautions

Eperisone should be administered with care in patients with a history of hypersensitivity to any medication, or with disorders of liver function (Eperisone 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

  • Shock and Anaphylactoid reactions: In the event of symptoms such as redness, itching, urticaria, oedema of the face[9] and other parts of the body, dyspnoea etc, treatment should be discontinued and appropriate measues taken.
  • Oculo-muco-cutaneous syndrome (Stevens Johnson Syndrome) and Toxic Epidermal Necrolysis:[10] Serious dermatopathy such as oculo-muco-cutaneous syndrome (Stevens-Johnson syndrome) or toxic epidermal necrolysis may occur. Patients should be carefully observed, treatment discontinued and appropriate measures taken, in the event of symptoms such as fever, erythema, blistering, itching, ocular congestion or stomatitis, etc.[9]

Drug interactions

There have been reports of disturbances in ocular accommodation occurring after the concomitant use of 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 antispasmodic effect lasting over 24 hours, compared with 1–2 hours following oral administration.

Eperisone is also under investigation as an anti-hypertensive agent, with promising results from trials on beagles.[12]

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. doi:10.1159/000077449. PMID 15161997.  
  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. doi:10.1358/mf.1999.21.3.534831. PMID 10389124. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=6&p_RefId=534831&p_IsPs=N.  
  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, and Lee Seok-Yong (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone". Pharmacology 71 (3): 150–6. doi:10.1159/000077449. PMID 15161997.  
  8. ^ ClinicalTrials.gov NCT00327730 Evaluation of Eperisone HCl in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain
  9. ^ a b Ueno T, Kawana S (July 2007). "[A case of eperisone hydrochloride (myonal)--induced drug eruption leading to erythema and angioedema"] (in Japanese). Arerugi 56 (7): 709–13. PMID 17671415. http://jja.jsaweb.jp/2007/056070709e.html.  
  10. ^ Takeshi K, et al. (2004). "Severe Drug Eruption Due to Eperisone Hydrochloride and Fluconazole Supposed to be Accompanied with Viral Infection" (in Japanese). Rinsho Derma 46 (7): 995–8. http://sciencelinks.jp/j-east/article/200423/000020042304A0532555.php.  
  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. doi:10.1016/j.ajem.2006.09.002. PMID 17499672. http://linkinghub.elsevier.com/retrieve/pii/S0735675706003615.  
  12. ^ EP patent 0310259 Eperisone as a hypotensive agent

References








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