Tolperisone: A typical representative of a class of centrally acting muscle relaxants with less sedative side effects

CNS Neuroscience and Therapeutics

Volumn 14, Issue 2, 2008, Pages 107-119

  Quasthoff, Stefan ^a   Möckel, Claudia ^b   Zieglgänsberger, Walter ^c   Schreibmayer, Wolfgang ^a  

^a MEDICAL UNIVERSITY OF GRAZ   (Austria)

^b Strathmann Research GmbH   (Germany)

^c MAX PLANCK INSTITUTE OF PSYCHIATRY   (Germany)

Author keywords

Behavioural neurology; Movement disorders; Neuromuscular disease; Neuropsychopharmacology; Painful muscle spasm; Parkinson's disease; Stroke

Indexed keywords

ABBSA; ARANTOICK; ATMOSGEN; BESNOLINE; CENTRAL MUSCLE RELAXANT; E 646; EPERISONE; INAPERISONE; ISOCALM; KINEORL; LANPERISONE; LIDOCAINE; MENOPATOL; METOSOMIN; MINACALM; MIONAL; MYDETON; MYONAL; N 553; NAISMERITIN; NONSTEROID ANTIINFLAMMATORY AGENT; PIPERIDINE DERIVATIVE; RGH 5002; SILPERISONE; TOLISARTINE; TOLPERISONE;

ANAPHYLACTIC SHOCK; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DIZZINESS; DRUG BIOAVAILABILITY; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG METABOLISM; DRUG STRUCTURE; FATIGUE; HUMAN; LATHYRISM; LOW BACK PAIN; MULTIPLE SCLEROSIS; MUSCLE SPASM; MYOTONIA; NEUROPATHIC PAIN; PERIPHERAL VASCULAR DISEASE; PHARMACODYNAMICS; REVIEW; SEDATION; SIDE EFFECT; SPASTICITY; SPINAL PAIN; TENSION HEADACHE; WEAKNESS;

ANIMALS; CLINICAL TRIALS AS TOPIC; HUMANS; HYPNOTICS AND SEDATIVES; MUSCLE RELAXANTS, CENTRAL; TOLPERISONE;

EID: 44049093471     PISSN: 17555930     EISSN: 17555949     Source Type: Journal    
DOI: 10.1111/j.1527-3458.2008.00044.x     Document Type: Review

References (87)

1. Abranyi I (1988) Study of the effect of 150 mg Mydocalm coated tablets in peripheral vascular diseases and in myotonias of various origin. Ther Hung 36 : 56 61.
2. Aleksandrov ISDLN (1974) Case of an allergic reaction to mydocalm. Klin Med (Mosk) 52 : 142.
3. Armstrong DW, Chang CD, Lee SH (1991) (R)-naphthylethylcarbamate- substituted and (S)-naphthylethylcarbamate-substituted beta-cyclo-dextrin bonded stationary phases for the reversed-phase liquid-chromatographic separation of enantiomers. J Chromatogr 539 : 83 90.
4. Bae JW, Kim MJ, Park YS, Myung CS, Jang CG, Lee SY (2007) Considerable interindividual variation in the pharmacokinetics of tolperisone HCl. Int J Clin Pharmacol Therapeutics 45 : 110 113.
5. Bae JW, Park YS, Sohn UD, Myung CS, Ryu BK, Jang CG, Lee SY (2006) HPLC determination of tolperisone in human plasma. Arch Pharmacal Res 29 : 339 342.
6. Bajaj P, Rendt-Nielsen L, Madeleine P, Svensson P (2003) Prophylactic tolperisone for post-exercise muscle soreness causes reduced isometric force - a double-blind randomized crossover control study. Euro J Pain 7 : 407 418.
7. Balint J, Egri G, Markovits I, Czugler M, Marthi K, Demeter A, Temesvari-Takacs K, Fogassy E (2002) Synthesis of some tolperisone metabolites in racemic and optically active form. Tetrahedron-Asymmetry 12 : 3417 3422.
8. Balint J, Hell Z, Markovits I, Parkanyi L, Fogassy E (2000) Synthesis and resolution of a Tolperisone metabolite. Tetrahedron-Asymmetry 11 : 1323 1329.
9. Balint J, Markovits I, Egri G, Tuza Z, Parkanyi L, Fogassy E (2001) Synthesis, resolution and absolute configuration of a tolperisone metabolite. Tetrahedron-Asymmetry 12 : 719 724.
10. Bean BP, Cohen CJ, Tsien RW (1983) Lidocaine block of cardiac sodium channels. J Gen Physiol 81 : 613 642.
11. Bohuslavizki KH, Kneip A, Koppenhofer E (1994) State-of-the-art potential clamp device for myelinated nerve-fibers using a new versatile input probe. Gen Physiol Biophys 13 : 357 376.
12. Briskin BS, Sakunova TI, Iakobishvili II (2000a) Role of midocalm in combined treatment of neuropathic diabetic foot syndrome. Khirurgiia (Mosk) 5 : 34 37.
13. Briskin BS, Sakunova TI, Iakobishvili II (2000b) Treatment of chronic arterial insufficiency of legs with midocalm in elderly. Khirurgiia (Mosk) 4 : 52-54.
14. Cappiello A, Mangani F, Palma P, Sisti E, Bruner F (1990) Sub Ppb level determination of eperison in human plasma by Gc/Ms. Chromatographia 30 : 357 360.
15. Chernysheva TV, Bagirova GG (2005) Midocalm in complex therapy of chronic low back pain syndrome. Klin Med (Mosk) 83 : 45 49.
16. Csanyi L (1989) High-dose Mydocalm therapy in certain myogenous headaches. Ther Hung 37 : 115 118.
17. Dalmadi B, Leibinger J, Borbas T, Szeberenyi S, Tihanyi K (2003a) Kinetic characterization of tolperisone hydroxylation by human microsomal enzymes. Drug Metabol Rev 35 : 118.
18. Dalmadi B, Leibinger J, Szeberenyi S, Borbas T, Farkas S, Szombathelyi Z, Tihanyi K (2003b) Identification of metabolic pathways involved in the biotransformation of tolperisone by human microsomal enzymes. Drug Metabol Dispos 31 : 631 636.
19. Davies J (1989) Effects of tizanidine, eperisone and afloqualone on feline dorsal horn neuronal responses to peripheral cutaneous noxious and innocuous stimuli. Neuropharmacology 28 : 1357 1362.
20. Dietrich A, Fels G (1999) Synthesis of H-3-tolperisone. J Label Comp Radiopharmaceut 42 : 1125 1134.
21. Ding L, Wei X, Zhang SQ, Sheng JP, Zhang YD (2004) Rapid and sensitive liquid chromatography-electrospray ionization-mass spectrometry method for the determination of eperisone in human plasma: Method and clinical applications. J Chromatogr Sci 42 : 254 258.
22. Dobi S (1961) Mydocalm and muscle tone. Ther Hung 9 : 15 18.
23. Dulin J, Kovacs L, Ramm S, Horvath F, Ebeling L, Kohnen R (1998) Evaluation of sedative effects of single and repeated doses of 50 mg and 150 mg tolperisone hydrochloride. Results of a prospective, randomized, double-blind, placebo-controlled trial. Pharmacopsychiatry 31 : 137 142.
24. Farkas S (2006) Silperisone: A centrally acting muscle relaxant. CNS Drug Rev 12 : 218 235.
25. Farkas S, Tarnawa I, Berzsenyi P (1989) Effects of some centrally acting muscle-relaxants on spinal root potentials - a comparative-study. Neuropharmacology 28 : 161 173.
26. Fels G (1996) Tolperisone: Evaluation of the lidocaine-like activity by molecular modeling. Arch Pharm 329 : 171 178.
27. Fujioka M, Kuriyama H (1985) Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery. J Pharmacol Exp Therapeutics 235 : 757 763.
28. Funakoshi M, Kawamura S (1986) Effects of tolperisone-Hcl on the silent period of the masseter. J Dental Res 65 : 592.
29. Funakoshi M, Nakashima M (1982) Effects of tolperisone hydrochloride on the jaw muscle activities in the rat. J Dental Res 61 : 596.
30. Furuta Y, Ishii Y (1977) Effect of Tolperisone on Insitu blood-perfused dog trachea. Jap J Pharmacol 27 : 71.
31. Furuta Y, Yoshikawa A (1976) Reversible adrenergic alpha-receptor blocking action of 2,4′-Dimethyl-3-Piperidino-propiophenone (Tolperisone). Jap J Pharmacol 26 : 543 550.
32. Gazdag M, Szepesi G, Nyiredy S (1978) Determination of tolperisone in pharmaceutical formulations by G. 1. C. Pharmazie 33 : 538 539.
33. Haginaka J, Kagawa C, Matsunaga H (1999) Separation of enantiomers on a chiral stationary phase based on ovoglycoprotein - VII. Comparison of chiral recognition ability of ovoglycoprotein from chicken and Japanese quail egg whites. J Chromatogr A 858 : 155 165.
34. Hinck D, Koppenhofer E (1997) Effects of tolperisone on the excitation process in myelinated axons. Pflugers Archiv-Euro J Physiol 433 : 503.
35. Hinck D, Koppenhofer E (2001) Tolperisone - a novel modulator of ionic currents in myelinated axons. Gen Physiol Biophys 20 : 413 429.
36. Hofer D, Lohberger B, Steinecker B, Schmidt K, Quasthoff S, Schreibmayer W (2006) A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms. Euro J Pharmacol 538 : 5 14.
37. Inoue S, Bian K, Okamura T, Okunishi H, Toda N (1989) Mechanisms of action of eperisone on isolated dog saphenous arteries and veins. Jap J Pharmacol 50 : 271 282.
38. Ishizuki M, Yanagisawa M (1992) Antinociceptive effects of tizanidine, diazepam and eperisone in isolated spinal-cord tail preparations of newborn rat. Pain 48 : 101 106.
39. Kato M, Yang YH (1990) Effects of eperisone on Renshaw Cells of cats. Neurosci Lett 112 : 246 250.
40. Kocsis P, Farkas S, Fodor L, Bielik N, Than M, Kolok S, Gere A, Csejtei M, Tarnawa I (2005) Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J Pharmacol Exp Therapeutics 315 : 1237 1246.
41. Kwasniewski AK-GBMS (2003) Mydocalm causing anaphylaxis. Pneumonol Alergol Pol 71 : 250 252.
42. Lashch NI, Avakian GN (2000) The use of midokalm in patients with multiple sclerosis. Zh Nevrol Psikhiatr Im S S Korsakova 100 : 24 28.
43. Lehoczky T (1961) Mydocalm, a new drug to relax spastic muscles in neurological diseases. Ther Hung 10 13.
44. Liawruangrath S, Liawruangrath B (1999) High performance thin layer chromatographic determination of tolperisone hydrochloride. J Pharmac Biomed Anal 20 : 401 404.
45. Liawruangrath S, Liawruangrath B, Pibool P (2001) Simultaneous determination of tolperisone and lidocaine by high performance liquid chromatography. J Pharmac Biomed Anal 26 : 865 872.
46. Liubishchev SA (1967) The use of mydocalm in the treatment of vascular diseases of the extremities. Klin Med (Moscow) 45 : 100 102.
47. Mao JR, Chen LL (2000) Systemic lidocaine for neuropathic pain relief. Pain 87 : 7 17.
48. Matsunaga H, Sadakane Y, Haginaka J (2003) Separation of basic drug enantiomers by capillary electrophoresis using chicken alpha(1)-acid glycoprotein: Insight into chiral recognition mechanism. Electrophoresis 24 : 2442 2447.
49. Melka A, TekleHaimanot R, Lambien F (1997) Symptomatic treatment of neurolathyrism with Tolperizone HCL (Mydocalm): A randomized double blind and placebo controlled drug trial. Ethiop Med J 35 : 77 91.
50. Mihara K, Matsumura M, Yoshioka E, Hanada K, Nakasa H, Ohmori S, Kitada M, Ogata H (2001) Intestinal first-pass metabolism of eperisone in the rat. Pharmac Res 18 : 1131 1137.
51. Miskolczi P, Vereczkey L, Frenkl R (1987) Gas-liquid-chromatographic method for the determination of tolperisone in human-plasma - pharmacokinetic and comparative bioavailability studies. J Pharmac Biomed Anal 5 : 695 700.
52. Miyazaki H, Ishibashi M, Izawa T, Takayama H, Idzu G (1975) Mass fragmentographic determination of 1-piperidino-2,4′-dimethyl- propiophenone(mydocalm) by use of 1/1 mixture technique. Chem Pharmac Bull 23 : 837 843.
53. Molnar L (1962) Successful use of mydocalm in peripheral arterial disease. Ther Hung 10 : 10 12.
54. Morikawa K, Oshita M, Yamazaki M, Ohara N, Mizutani F, Kato H, Ito Y, Kontani H, Koshiura R (1987) Pharmacological studies of the new centrally acting muscle-relaxant 4′-Ethyl-2-Methyl-3-Pyrrolidinopropiophenone hydrochloride 616. Arzneimittel-Forschung/Drug Res 37 : 331 336.
55. Nakajima Y, Wada N (1989) Effects of eperisone-Hcl on the stretch reflex in anesthetized cats. Jap J Pharmacol 51 : 572 578.
56. Novalesli P, Sun XP, Takeuchi H (1989) Suppression of calcium current in a snail neuron by eperisone and its analogs. Eur J Pharmacol 168 : 299 305.
57. Okada H, Honda M, Ono H (2001) Method for recording spinal reflexes in mice: Effects of thyrotropin-releasing hormone, DOI, tolperisone and baclofen on monosynaptic spinal reflex potentials. Jap J Pharmacol 86 : 134 136.
58. Ono H, Fukuda H, Kudo Y (1984) Mechanisms of depressant action of muscle-relaxants on spinal reflexes - participation of membrane stabilizing action 616. J Pharmacobio-Dyn 7 : 171 176.
59. Parfenov VA, Batysheva TT (2003) Spinal pain and its treatment with midocalm. Ter Arkh 75 : 82 83.
60. Porszasz J, Barankay T, Nador K, Gibiszer K (1961) Pharmakologie einer neuen interneuron-lahmenden substanz 1-Piperidino-2-Methyl-3-(P-Tolyl)-Propan-3- on. Arzneimittel-Forschung-Drug Res 11 : 257 260.
61. Pratzel HG, Alken RG, Ramm S (1996) Efficacy and tolerance of repeated oral doses of tolperisone hydrochloride in the treatment of painful reflex muscle spasm: Results of a prospective placebo-controlled double-blind trial. Pain 67 : 417 425.
62. Quasthoff S, Pojer C, Mori A, Hofer D, Liebmann P, Kieseier BC, Schreibmayer W (2003) No blocking effects of the pentapeptide QYNAD on Na+ channel subtypes expressed in Xenopus oocytes or action potential conduction in isolated rat sural nerve. Neurosci Lett 352 : 93 96.
63. + channels by local anesthetics. Science 265 : 1724 1728.
64. Ragsdale DS, McPhee JC, Scheuer T, Catterall WA (1996) Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels. Proc Natl Acad Sci U.S.A. 93 : 9270 9275.
65. Ribi C, Vermeulen C, Hauser C (2003) Anaphylactic reactions to tolperisone (Mydocalm (R)). Swiss Medical Weekly 133 : 369 371.
66. Saegusa K, Furukawa Y, Akahane K, Haniuda M, Chiba S (1991) Anti-nicotinic and anti-muscarinic actions of eperisone in the isolated canine atrium. Jap J Pharmacol 56 : 187 193.
67. Sakaue A, Honda M, Tanabe M, Ono H (2004) Antinociceptive effects of sodium channel-blocking agents on acute pain in mice. J Pharmacol Sci 95 : 181 188.
68. Sakitama K (1993) The effects of centrally acting muscle-relaxants on the intrathecal noradrenaline-induced facilitation of the flexor reflex mediated by group-Ii afferent-fibers in rats. Jap J Pharmacol 63 : 369 376.
69. Sakitama K, Ozawa Y, Aoto N, Nakamura K, Ishikawa M (1995) Pharmacological properties of Nk433: A new centrally acting muscle-relaxant. Euro J Pharmacol 273 : 47 56.
70. Sakitama K, Ozawa Y, Aoto N, Tomita H, Ishikawa M (1997) Effects of a new centrally acting muscle relaxant, NK433 (lanperisone hydrochloride) on spinal reflexes. Euro J Pharmacol 337 : 175 187.
71. Schreibmayer W, Lester HA, Dascal N (1994) Voltage clamping of xenopus-laevis oocytes utilizing agarose-cushion electrodes. Pflugers Archiv-Euro J Physiol 426 : 453 458.
72. Slusher BS, Tiffany CW, Olkowski JL, Jackson PF (1997) Use of identical assay conditions for cocaine analog binding and dopamine uptake to identify potential cocaine antagonists. Drug Alcohol Depen 48 : 43 50.
73. Solovieva AD, Akarachkova ES, Gordeev SA (2005) A study of mydocalm efficiency in the treatment of chronic headache of tension. Zh Nevrol Psikhiatr Im S S Korsakova 105 : 13 17.
74. Solozhenkin V (1999) Cavinton and mydocalm in combined therapy of anxiety disorders and tension headaches. Zh Nevrol Psikhiatr Im S S Korsakova 99 : 46.
75. Solti F (1961) Use of Mydocalm in influencing the effect of muscle tremor on the ECG. Ther Hung 9 : 31 32.
76. Stamenova P, Koytchev R, Kuhn K, Hansen C, Horvath F, Ramm S, Pongratz D (2005) A randomized, double-blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke. Euro J Neurol 12 : 453 461.
77. Stamenova P, Koytchev R, Kuhn K, Hansen C, Horvath F, Ramm S, Pongratz D (2006) A randomized, double blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke. Zh Nevrol Psikhiatr Im S S Korsakova 106 : 34 42.
78. Svensson P, Wang KL, Rendt-Nielsen L (2003) Effect of muscle relaxants on experimental jaw-muscle pain and jaw-stretch reflexes: A double-blind and placebo-controlled trial. Euro J Pain 7 : 449 456.
79. Sztankay C (1970) Treatment of vascular diseases with Mydocalm. Ther Hung 18 : 121 124.
80. Tsukamoto T, Ushio T, Haginaka J (1997) Separation of basic drug enantiomers by capillary electrophoresis with new glycosaminoglycan. Chem Lett 589 590.
81. Tsukamoto T, Ushio T, Haginaka J (1999) Chiral resolution of basic drugs by capillary electrophoresis with new glycosaminoglycans. J Chromatogr A 864 : 163 171.
82. Velmurugan T, Ching CB, Ng SC, Bai ZW, Ong TT (2002) Optimization of the reversed-phase high-performance liquid chromatographic separation of the enantiomers of a cationic chiral drug (tolperisone) on a heptakis(6-azido-6- deoxy) perphenylcarbamated beta-cyclodextrin column. Chromatographia 56 : 229 232.
83. Vorob'eva OV, Kozlova IM (2006) Comparative efficiency of bakloferon and tolperizon central muscle relaxants in complex therapy of back pain. Voen Med Zh 327 : 52 55.
84. Welch CJ, Szczerba T, Perrin SR (1997) Some recent high-performance liquid chromatography separations of the enantiomers of pharmaceuticals and other compounds using the Whelk-O 1 chiral stationary phase. J Chromatogr A 758 : 93 98.
85. Yang SI, Park HY, Lee SH, Lee SJ, Han OY, Lim SC, Jang CG, Lee WS, Shin YH, Kim JJ, et al. (2004) Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone. Pharmacology 71 : 150 156.
86. Yokoyama T, Fukuda K, Mori S, Ogawa M, Nagasawa K (1992) Determination of tolperisone enantiomers in plasma and their disposition in rats. Chem Pharmac Bull 40 : 272 274.
87. Youngvises N, Liawruangrath B, Liawruangrath S (2003) Simultaneous micellar LC determination of lidocaine and tolperisone. J Pharmac Biomed Anal 31 : 629 638.