esrisone

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Eperisone
Clinical data
Trade namesMyonal
AHFS/Drugs.comInternational Drug Names
Routes of
administration		O
ATC code
  • M03BX09 (WHO)
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers

IUPAC name

Bạn đang xem: esrisone

  • (2RS)-1-(4-Ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one

CAS Number
  • 64840-90-0 check
  • HCl: 56839-43-1 check
PubChem CID
DrugBank
  • DB08992 ☒
ChemSpider
  • 3123 check
UNII
  • 2M2P0551D3
  • HCl: U38O8U7P6X check
KEGG
  • D01671 check
ChEBI
  • CHEBI:77069 ☒
ChEMBL
  • ChEMBL1902981 ☒
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H25NO
Molar mass259.393 g·mol−1
3D model (JSmol)
  • Interactive image

SMILES

  • CCc1ccc(cc1)C(=O)C(C)CN2CCCCC2

InChI

  • 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 check

  • Key:SQUNAWUMZGQQJD-UHFFFAOYSA-N check

 ☒check (what is this?)  (verify)

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.

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Indications[edit]

  • Spastic paralysis in conditions such as cerebrovascular disease[2]
  • Spastic spinal paralysis
  • Cervical spondylosis[3]
  • Postoperative sequelae (including from cerebrospinal tumour)[4]
  • Sequelae vĩ đại trauma (e.g. spinal trauma or head injury)[4]
  • Amyotrophic lateral sclerosis
  • Cerebral palsy
  • Spinocerebellar degeneration
  • Spinal vascular diseases and other encephalomyelopathies
  • Cervical syndrome, periarthritis of the shoulder, and lumbago.[5]

Presentation[edit]

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 sườn 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[edit]

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 physiological hypofunction during treatment.[6]

Safety during pregnancy and breast-feeding[edit]

Eperisone has not been established vĩ đại be safe for use by pregnant women; therefore the drug should not 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 vĩ đại stop breast-feeding for the duration of treatment. Eperisone has been reported vĩ đại be excreted in breast milk in an animal study (in rats).

Pharmacology[edit]

  • Skeletal muscle relaxation
  • Relaxation of hypertonic skeletal muscles
  • Improves intramuscular blood flow
  • Suppression of spinal reflex potentials
  • Reduction of muscle spindle sensitivity via motor neurons
  • Vasodilatation and augmentation of blood flow
  • Analgesic action and inhibition of the pain reflex in the spinal cord

Contraindications[edit]

Eperisone is contraindicated in patients with known hypersensitivity vĩ đại 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[edit]

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

Weakness, light-headedness, sleepiness or other symptoms may occur. In the sự kiện 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 xế hộp.[6]

Side effects[edit]

  • Shock and anaphylactoid reactions: In the sự kiện of symptoms such as redness, itching, urticaria, oedema of the face[10] and other parts of the body toàn thân, dyspnoea, etc., treatment should be discontinued and appropriate measures taken.
  • Other side effects: anaemia, rash, pruritus, sleepiness, insomnia, headache, nausea and vomiting, anorexia, abdominal pain, diarrhoea, constipation, urinary retention or incontinence.[citation needed]

Drug interactions[edit]

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[edit]

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

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Future developments[edit]

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 vĩ đại one vĩ đại two hours following oral administration.

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

Brand names[edit]

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

See also[edit]

  • Chemically and mechanistically related drugs: inaperisone, lanperisone, silperisone, tolperisone

Notes[edit]

  1. ^ a b Yang SI, Park HY, Lee SH, et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation kêu ca oral eperisone". Pharmacology. 71 (3): 150–6. doi:10.1159/000077449. PMID 15161997. S2CID 24474033.
  2. ^ "eperisone Summary Report - CureHunter". www.curehunter.com.
  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. doi:10.1358/mf.1999.21.3.534831. 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. ^ 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 kêu ca oral eperisone". Pharmacology. 71 (3): 150–6. doi:10.1159/000077449. PMID 15161997. 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. ^ Ueno T, Kawana S (July 2007). "[A case of eperisone hydrochloride (myonal)--induced drug eruption leading vĩ đại erythema and angioedema]". Arerugi (in Japanese). 56 (7): 709–13. PMID 17671415. Archived from the original on 2014-12-19. Retrieved 2008-09-28.
  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". Am J Emerg Med. 25 (4): 481–2. doi:10.1016/j.ajem.2006.09.002. PMID 17499672.
  12. ^ EP 0310259 Eperisone as a hypotensive agent
  13. ^ Drugs.com International eperisone brands Page accessed March 10, năm nhâm thìn.

References[edit]

  • 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. PMID 3935775.
  • Inoue S, Bian K, Okamura T, Okunishi H, Toda N (July 1989). "Mechanisms of action of eperisone on isolated dog saphenous arteries and veins". Jpn. J. Pharmacol. 50 (3): 271–82. doi:10.1254/jjp.50.271. PMID 2761129.
  • Viveksarathi, K., et al. "Dosage sườn 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