Eperison

Structural formula
	Structural formula without stereochemistry
General
Non-proprietary name	Eperison
other names	( RS ) -4'-ethyl-2-methyl-3-piperidinopropiophenone ( IUPAC ) ; Eperisonum ( Latin ) ;
Molecular formula	C 17 H 25 NO (eperisone) ; C 17 H 25 NO HCl (eperisone hydrochloride) ;
Brief description	Eperisone hydrochloride is a white, crystalline powder
External identifiers / databases
PubChem	3236
ChemSpider	3123
DrugBank	DB08992
Wikidata	Q426401
Drug information
ATC code	M03 BX09
Drug class	Muscle relaxants
properties
Molar mass	259.39 g · mol -1
Physical state	firmly
Melting point	167 ° C (eperisone hydrochloride) (decomposition)
solubility	Easily soluble in water, methanol and acetic acid ; soluble in ethanol (eperisone hydrochloride)
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
Toxicological data	129 mg kg −1 ( LD 50 , mouse , ip , hydrochloride)
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Eperisone is an orally active drug from the group of centrally acting muscle relaxants and is chemically structurally related to tolperisone . Eperisone is particularly used in numerous Asian countries including China, India, Indonesia, South Korea, and Japan to treat muscular tension, lumbago, and spastic paralysis .

pharmacology

Mode of action (pharmacodynamics)

Eperisone is a centrally acting muscle relaxant drug. It also has an active analgesic component. At the molecular level, these effects are associated with a local anesthetic- like inhibition of voltage-dependent sodium and calcium channels on motor neurons and primary afferents and thus associated with an inhibition of the release of transmitters .

Clinical information

application areas

There are currently no drug approvals in Europe or North America. A possible application for the treatment of spastic paralysis, back pain and spondylosis has been investigated in smaller clinical studies . The results of these clinical studies were interpreted by the authors as an indication of effectiveness.

Side effects

During the clinical studies, drowsiness, dizziness, balance disorders, nausea, vomiting and abdominal pain were observed as adverse drug side effects that may be related to the use of eperisone.

Trade names and dosage forms

Eperison is marketed in Asia under the brand name Myonal.

Web links

A. Cappiello, F. Mangani, P. Palma, E. Sisti, F. Bruner: Sub PPB level determination of eperison in human plasma by GC / MS . In: Chromatographia October 1990, Volume 30, Number 7-8, pp. 357-360 doi: 10.1007 / BF02328497
eisai.jp: Myonal
medical-explorer.com: Myonal

Individual evidence

^ ^A ^b ^c Society of Japanese Pharmacopoeia (Ed.): The japanese pharmacopoeia: JP XV: German version . 15th edition. Yakuji Nippo, Tokyo 2006, OCLC 474705025 , p. 618 ( Monographs D to K [PDF]).
↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Entry on eperisone in the ChemIDplus database of the United States National Library of Medicine (NLM) .
↑ Ono H, Fukuda H, Kudo Y: Mechanisms of depressant action of muscle relaxants on spinal reflexes: participation of membrane stabilizing action . In: J Pharmacobio-dyn . 7, No. 3, March 1984, pp. 171-6. PMID 6747808 .
↑ Kocsis P, Farkas S, Fodor L, et al. : Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels . In: J Pharmacol Exp Ther . 315, No. 3, December 2005, pp. 1237-46. doi : 10.1124 / jpet.105.089805 . PMID 16126840 .
↑ Farkas S: Silperisone: a centrally acting muscle relaxant . In: CNS Drug Rev . 12, No. 3-4, 2006, pp. 218-35. doi : 10.1111 / j.1527-3458.2006.00218.x . PMID 17227288 .
↑ Bresolin N, Zucca C, Pecori A: Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial . In: Adv Ther . 26, No. 5, May 2009, pp. 563-73. doi : 10.1007 / s12325-009-0031-8 . PMID 19458926 .
↑ ^a ^b Cabitza P, Randelli P: Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study . In: Eur Rev Med Pharmacol Sci . 12, No. 4, 2008, pp. 229-35. PMID 18727454 .
Jump up ↑ Bose K: The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial . In: Methods Find Exp Clin Pharmacol . 21, No. 3, April 1999, pp. 209-13. PMID 10389124 .
↑ Sartini S, Guerra L: Open experience with a new myorelaxant agent for low back pain . In: Adv Ther . 25, No. 10, October 2008, pp. 1010-8. doi : 10.1007 / s12325-008-0108-9 . PMID 18836866 .

[JP15-1] A ^b ^c Society of Japanese Pharmacopoeia (Ed.): The japanese pharmacopoeia: JP XV: German version . 15th edition. Yakuji Nippo, Tokyo 2006, OCLC 474705025 , p. 618 ( Monographs D to K [PDF]).

[NV-2] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[ChemIDplus-3] Entry on eperisone in the ChemIDplus database of the United States National Library of Medicine (NLM) .

[pmid6747808-4] Ono H, Fukuda H, Kudo Y: Mechanisms of depressant action of muscle relaxants on spinal reflexes: participation of membrane stabilizing action . In: J Pharmacobio-dyn . 7, No. 3, March 1984, pp. 171-6. PMID 6747808 .

[pmid16126840-5] Kocsis P, Farkas S, Fodor L, et al. : Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels . In: J Pharmacol Exp Ther . 315, No. 3, December 2005, pp. 1237-46. doi : 10.1124 / jpet.105.089805 . PMID 16126840 .

[pmid17227288-6] Farkas S: Silperisone: a centrally acting muscle relaxant . In: CNS Drug Rev . 12, No. 3-4, 2006, pp. 218-35. doi : 10.1111 / j.1527-3458.2006.00218.x . PMID 17227288 .

[pmid19458926-7] Bresolin N, Zucca C, Pecori A: Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial . In: Adv Ther . 26, No. 5, May 2009, pp. 563-73. doi : 10.1007 / s12325-009-0031-8 . PMID 19458926 .

[pmid18727454-8] Cabitza P, Randelli P: Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study . In: Eur Rev Med Pharmacol Sci . 12, No. 4, 2008, pp. 229-35. PMID 18727454 .

[pmid10389124-9] Jump up ↑ Bose K: The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial . In: Methods Find Exp Clin Pharmacol . 21, No. 3, April 1999, pp. 209-13. PMID 10389124 .

[pmid18836866-10] Sartini S, Guerra L: Open experience with a new myorelaxant agent for low back pain . In: Adv Ther . 25, No. 10, October 2008, pp. 1010-8. doi : 10.1007 / s12325-008-0108-9 . PMID 18836866 .