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Chemical Compound Review

Sirdalud     3-chloro-N-(4,5-dihydro-1H- imidazol-2-yl)...

Synonyms: Ternelin, Tizanidina, tizanidine, Tizanidinum, Sirdalud (TN), ...
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Disease relevance of Ternelin


Psychiatry related information on Ternelin


High impact information on Ternelin


Chemical compound and disease context of Ternelin


Biological context of Ternelin


Anatomical context of Ternelin

  • It was concluded that, overall, tizanidine is effective in reducing spasticity in patients with spinal cord injury [2].
  • 6. Two hours after the ingestion of tizanidine, an alpha(2)-adrenergic receptor agonist known to selectively depress the transmission in the group II afferent pathway, the medium latency reflex was strongly depressed (P = 0.007), whereas the short latency component was unchanged (P = 0.653) [23].
  • On the basis of the present results, taken together with previous observations that tizanidine transiently inactivates neurons of the nucleus locus coeruleus, it is proposed that the reflex depression may be caused by a removal of a descending noradrenergic facilitation exerted on spinal reflex transmission [24].
  • This interpretation leaves open further possible actions of tizanidine exerted directly on spinal interneurons [24].
  • Tizanidine but not placebo decreased the quadriceps muscle and global lower limb Ashworth scores (2.9 (0.2) to 1.9 (0.3), p<0.001; and 12 (0.7) to 9.5 (0.8), p<0.0001, respectively) [25].

Associations of Ternelin with other chemical compounds


Gene context of Ternelin

  • METHODS: The effect of CYP isoform inhibitors on the elimination of tizanidine was studied using pooled human liver microsomes [31].
  • CONCLUSIONS: Tizanidine reduces spasticity in MS, and both therapeutic effects and side effects are related to the plasma drug levels [27].
  • In spinalized preparations, a net facilitatory alpha 1-mediated action may be revealed by the higher doses of tizanidine that would be unopposed by the alpha 2-mediated disfacilitation [32].
  • Aspirin (150 mg/kg i.v.), proacetaminophen (300 mg/kg i.v.) and tizanidine, a centrally acting myorelaxant (0.25-1 mg/kg i.v.), had no effect on the number of Fos-like immunoreactivity neurons induced by heat stimulation [33].
  • RESULTS: Incubation of tizanidine (80 nm) with human liver microsomes resulted in time- and NADPH-dependent substrate consumption with a half-life of 50 min, initial reaction velocity of 1.1 pmol x min-1 x mg-1 protein and intrinsic clearance of 17 ml x min-1 x kg-1 [31].

Analytical, diagnostic and therapeutic context of Ternelin

  • Summary of combined clinical analysis of controlled clinical trials with tizanidine [34].
  • This multicenter study (14 sites) assessed the efficacy and safety of oral tizanidine in patients who had spinal cord injury of > 12 months' duration [2].
  • Experiments were performed in rats to determine if the alpha 2-adrenergic agonist tizanidine has an antinociceptive effect when injected intrathecally, and whether the analgesia is accompanied by changes in blood pressure [20].
  • Wide interpatient variability in the effective plasma concentrations of tizanidine means that the optimal dosage must be titrated over 2 to 4 weeks for each patient (dosages of 2 to 36 mg/day have been used in clinical trials) [4].
  • In a double blind, placebo controlled, cross over study the correlations between single doses (2, 4, and 8 mg), plasma concentrations, and antispastic action of tizanidine were investigated in 16 patients with extensor spasticity of the legs due to multiple sclerosis [35].


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  2. Efficacy and safety of tizanidine in the treatment of spasticity in patients with spinal cord injury. North American Tizanidine Study Group. Nance, P.W., Bugaresti, J., Shellenberger, K., Sheremata, W., Martinez-Arizala, A. Neurology (1994) [Pubmed]
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  6. Effects of tizanidine administration on precipitated opioid withdrawal signs in rats. Pinelli, A., Trivulzio, S., Spezia, R. Drug and alcohol dependence. (1998) [Pubmed]
  7. Effects of tizanidine administration on exteroceptive suppression of the temporalis muscle in patients with chronic tension-type headache. Nakashima, K., Tumura, R., Wang, Y., Shimoda, M., Sakuma, K., Takahashi, K. Headache. (1994) [Pubmed]
  8. The effect of tizanidine on maximal electroshock seizures (MES) in mice. Denizbaşi, A., Berkman, K., Ozyazgan, S., Eşkazan, E. Gen. Pharmacol. (1999) [Pubmed]
  9. Assessment of efficacy and psychomotor performances of thiocolchicoside and tizanidine in patients with acute low back pain. Ketenci, A., Ozcan, E., Karamursel, S. International journal of clinical practice. (2005) [Pubmed]
  10. Drug interaction of tizanidine and ciprofloxacin: Case report. Momo, K., Homma, M., Kohda, Y., Ohkoshi, N., Yoshizawa, T., Tamaoka, A. Clin. Pharmacol. Ther. (2006) [Pubmed]
  11. Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism. Granfors, M.T., Backman, J.T., Neuvonen, M., Neuvonen, P.J. Clin. Pharmacol. Ther. (2004) [Pubmed]
  12. Fluvoxamine drastically increases concentrations and effects of tizanidine: a potentially hazardous interaction. Granfors, M.T., Backman, J.T., Neuvonen, M., Ahonen, J., Neuvonen, P.J. Clin. Pharmacol. Ther. (2004) [Pubmed]
  13. Antihyperalgesic and side effects of intrathecal clonidine and tizanidine in a rat model of neuropathic pain. Kawamata, T., Omote, K., Yamamoto, H., Toriyabe, M., Wada, K., Namiki, A. Anesthesiology (2003) [Pubmed]
  14. Systemic tizanidine hydrochloride (Zanaflex) partially decreases experimental postoperative pain in rats. Hord, A.H., Denson, D.D., Azevedo, M.I. Anesth. Analg. (2001) [Pubmed]
  15. Oral tizanidine, an alpha2-adrenoceptor agonist, reduces the minimum alveolar concentration of sevoflurane in human adults. Wajima, Z., Yoshikawa, T., Ogura, A., Imanaga, K., Shiga, T., Inoue, T., Ogawa, R. Anesth. Analg. (2002) [Pubmed]
  16. A multi-centre, double-blind trial of tizanidine, a new antispastic agent, in spasticity associated with hemiplegia. Bes, A., Eyssette, M., Pierrot-Deseilligny, E., Rohmer, F., Warter, J.M. Current medical research and opinion. (1988) [Pubmed]
  17. Hypotension due to interaction between lisinopril and tizanidine. Kao, C.D., Chang, J.B., Chen, J.T., Wu, Z.A., Shan, D.E., Liao, K.K. The Annals of pharmacotherapy. (2004) [Pubmed]
  18. Pharmacokinetics and pharmacodynamics of tizanidine. Roberts, R.C., Part, N.J., Pokorny, R., Muir, C., Leslie, G.C., Emre, M. Neurology (1994) [Pubmed]
  19. Tizanidine: neuropharmacology and mechanism of action. Coward, D.M. Neurology (1994) [Pubmed]
  20. Effect of intrathecal tizanidine on antinociception and blood pressure in the rat. McCarthy, R.J., Kroin, J.S., Lubenow, T.R., Penn, R.D., Ivankovich, A.D. Pain (1990) [Pubmed]
  21. Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. Piletz, J.E., Zhu, H., Chikkala, D.N. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  22. Intrathecal clonidine and tizanidine in conscious dogs: comparison of analgesic and hemodynamic effects. Kroin, J.S., McCarthy, R.J., Penn, R.D., Lubenow, T.R., Ivankovich, A.D. Anesth. Analg. (1996) [Pubmed]
  23. Group II muscle afferents probably contribute to the medium latency soleus stretch reflex during walking in humans. Grey, M.J., Ladouceur, M., Andersen, J.B., Nielsen, J.B., Sinkjaer, T. J. Physiol. (Lond.) (2001) [Pubmed]
  24. Tizanidine-induced depression of polysynaptic cutaneous reflexes in nonanesthetized monkeys is mediated by an alpha 2-adrenergic mechanism. Corboz, M., Palmer, C.I., Palmeri, A., Wiesendanger, M. Exp. Neurol. (1991) [Pubmed]
  25. Modulation of the transmission in group II heteronymous pathways by tizanidine in spastic hemiplegic patients. Maupas, E., Marque, P., Roques, C.F., Simonetta-Moreau, M. J. Neurol. Neurosurg. Psychiatr. (2004) [Pubmed]
  26. Antinociceptive effects of tizanidine, diazepam and eperisone in isolated spinal cord-tail preparations of newborn rat. Ishizuki, M., Yanagisawa, M. Pain (1992) [Pubmed]
  27. Relationship of the antispasticity effect of tizanidine to plasma concentration in patients with multiple sclerosis. Nance, P.W., Sheremata, W.A., Lynch, S.G., Vollmer, T., Hudson, S., Francis, G.S., O'Connor, P., Cohen, J.A., Schapiro, R.T., Whitham, R., Mass, M.K., Lindsey, J.W., Shellenberger, K. Arch. Neurol. (1997) [Pubmed]
  28. The effect of centrally acting myorelaxants on NMDA receptor-mediated synaptic transmission in the immature rat spinal cord in vitro. Siarey, R.J., Long, S.K., Evans, R.H. Br. J. Pharmacol. (1992) [Pubmed]
  29. Inhibitory effects of clonidine and tizanidine on release of substance P from slices of rat spinal cord and antagonism by alpha-adrenergic receptor antagonists. Ono, H., Mishima, A., Ono, S., Fukuda, H., Vasko, M.R. Neuropharmacology (1991) [Pubmed]
  30. Selective antinociceptive effects of tizanidine (DS 103-282), a centrally acting muscle relaxant, on dorsal horn neurones in the feline spinal cord. Davies, J., Johnston, S.E. Br. J. Pharmacol. (1984) [Pubmed]
  31. Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. Granfors, M.T., Backman, J.T., Laitila, J., Neuvonen, P.J. British journal of clinical pharmacology. (2004) [Pubmed]
  32. The adrenergic agonist tizanidine has differential effects on flexor reflexes of intact and spinalized rat. Chen, D.F., Bianchetti, M., Wiesendanger, M. Neuroscience (1987) [Pubmed]
  33. Effects of opioids and non-opioids on c-Fos-like immunoreactivity induced in rat lumbar spinal cord neurons by noxious heat stimulation. Abbadie, C., Honoré, P., Fournié-Zaluski, M.C., Roques, B.P., Besson, J.M. Eur. J. Pharmacol. (1994) [Pubmed]
  34. Summary of combined clinical analysis of controlled clinical trials with tizanidine. Wallace, J.D. Neurology (1994) [Pubmed]
  35. Correlations between dose, plasma concentrations, and antispastic action of tizanidine (Sirdalud). Emre, M., Leslie, G.C., Muir, C., Part, N.J., Pokorny, R., Roberts, R.C. J. Neurol. Neurosurg. Psychiatr. (1994) [Pubmed]
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