Cyclobenzaprine: mechanisms of action. What is known?

August 7, 2024
521
УДК:  616.741
Specialities :
Resume

The treatment of acute muscle spasm of the back muscles is one of the most common reasons for consulting a neurologist, which requires a clear understanding of the pathogenesis of this phenomenon and the availability of an effective, standardized arsenal of therapeutic effects. The article summarizes the basic concepts of the mechanism of action of cyclobenaprine based on a ten-year clinical experience of its use in the treatment of acute muscle spasm and muscle-tonic syndromes. The effect of cyclobenzaprine on the serotonergic system, biotransformation depending on the route of administration into the body and comparative characteristics with the drugs most often used for the treatment of muscle spasm in back pain are considered. The advantages of using cyclobenzaprine prolonged action compared to immediate release are analyzed.

References

  • 1. Chou R., Peterson K., Helfand M. (2004) Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review. J. Pain Symptom Manage, 28(2): 140–175.
  • 2. See S., Ginzburg R. (2008) Choosing a skeletal muscle relaxant. Am. Fam. Physician., 78(3): 365–370.
  • 3. Міщенко О.Я., Бездітко Н.В. (2021) Міорелаксанти центральної дії: роль і місце в лікуванні болю у спині. https://umj.com.ua/uk/publikatsia-223377.
  • 4. Katz W.A., Dube J. (1988) Cyclobenzaprine in the treatment of acute muscle spasm: review of a decade of clinical experience. Clin. Ther., 10(2): 216–228.
  • 5. Kobayashi H., Hasegawa Y., Ono H. (1996) Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur. J. Pharmacol., 311(1): 29–35. doi: 10.1016/0014-2999(96)00402-5.
  • 6. Weil A.J., Ruoff G.E., Nalamachu S. et al. (2010) Efficacy and tolerability of cyclobenzaprine extended release for acute muscle spasm: a pooled analysis. Postgrad. Med., 122(4): 158–169. doi:10.3810/pgm.2010.07.2182.
  • 7. Till A.E., Constanzer M.L., Demetriades J. et al. (1982) Evidence for route dependent biotransformation of cyclobenzaprine hydrochloride. Biopharm. Drug Dispos., 3(1): 19–28.
  • 8. Toth P.P., Urtis J. (2004) Commonly used muscle relaxant therapies for acute low back pain: a review of carisoprodol, cyclobenzaprine hydrochloride, and metaxalone. Clin. Ther., 26(9): 1355–1367.
  • 9. Braschi E., Garrison S., Allan G.M. (2015) Cyclobenzaprine for acute back pain. Can. Fam. Physician., 61(12): 1074.
  • 10. Roelofs P.D., Deyo R.A., Koes B.W. et al. (2008) Non-steroidal anti-inflammatory drugs for low back pain. Cochrane Database Syst. Rev., 1: CD000396.
  • 11. Borenstein D.G., Korn S. (2003) Efficacy of a low-dose regimen of cyclobenzaprine hydrochloride in acute skeletal muscle spasm: results of two placebo-controlled trials. Clin. Ther., 25(4): 1056–1073.
  • 12. Canadian Agency for Drugs and Technologies in Health (2015) Long-term Use of Cyclobenzaprine for Pain: A Review of the Clinical Effectiveness. https://www.ncbi.nlm.nih.gov/books/NBK279660/
  • 13. Cimolai N. (2009) Cyclobenzaprine: a new look at an old pharmacological agent, Expert Review of Clinical Pharmacology, 2(3): 255–263.