259
Views
0
CrossRef citations to date
0
Altmetric
Pharmacology

Tizanidine: Advances in Pharmacology & Therapeutics and Drug Formulations

, & ORCID Icon
Pages 1257-1271 | Received 23 Jan 2024, Accepted 16 Mar 2024, Published online: 21 Mar 2024

References

  • Zygmunt M, Sapa J. Muscle relaxants-the current position in the treatment of spasticity in orthopedics. Ortop Traumatol Rehabil. 2015;17:423–430. doi:10.5604/15093492.1173500
  • Witenko C, Moorman-Li R, Motycka C, et al. Considerations for the appropriate use of skeletal muscle relaxants for the management of acute low back pain. P T. 2014;39:427–435. PMID: 25050056. doi:10.1002/jcph.247
  • By the 2023 American Geriatrics Society Beers Criteria® Update Expert Panel. American Geriatrics society 2023 updated AGS beers criteria® for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2023;71:2052–2081. doi:10.1111/jgs.18372
  • RxList [homepage on the Internet]. ZANAFLEX; 2022. Available from: https://www.rxlist.com/zanaflex-drug.htm#indications. Accessed October 3, 2023.
  • Su Zhang VR, Niu F, Lee EA, et al. Safety of baclofen versus tizanidine for older adults with musculoskeletal pain. J Am Geriatr Soc. 2023;71:2579–2584. doi:10.1111/jgs.18349
  • Hwang YJ, Chang AR, Brotman DJ, Inker LA, Grams ME, Shin JI. Baclofen and the risk of encephalopathy: a real-world, active-comparator cohort study. Mayo Clin Proc. 2023;98:676–688. doi:10.1016/j.mayocp.2022.11.004
  • Khan NF, Bykov K, Barnett ML, Glynn RJ, Vine SM, Gagne JJ. Comparative risk of opioid overdose with concomitant use of prescription opioids and skeletal muscle relaxants. Neurology. 2022;99:e1432–e1442. doi:10.1212/WNL.0000000000200904
  • Hwang YJ, Chang AR, Brotman DJ, Inker LA, Grams ME, Shin JI. Baclofen and the risk of fall and fracture in older adults: a real-world cohort study. J Am Geriatr Soc. 2024;72(1):91–101. doi:10.1111/jgs.18665
  • Rahkonen A, Taipale H, Koponen M, et al. The cumulative use of muscle relaxants and the risk of Alzheimer’s disease: a nationwide case-control study. J Alzheimers Dis. 2023;91:1283–1290. doi:10.3233/JAD-220409
  • Chaugai S, Dickson AL, Shuey MM, et al. Co-prescription of strong CYP1A2 inhibitors and the risk of tizanidine-associated hypotension: a retrospective cohort study. Clin Pharmacol Ther. 2019;105(3):703–709. doi:10.1002/cpt.1233
  • Aezi G, Shafizad M, Firouzian A, Mirani A, Hassanzadeh Kiabi F. Effects of tizanidine and clonidine on postoperative pain after lumbar fusion surgery. Interdiscip Neurosurg. 2023;31:101680. doi:10.1016/j.inat.2022.101680
  • Meskar H, Aezzi G, Kiyasari AZ, Shafizad M, Jalalian F, Alderraji M. The effect of tizanidine on postoperative pain management after lumbar fusion surgery. Exp Appl Biomed Res. 2023;24:49–56.
  • Sane S, Sayyadi S, Abbasivash R, Rezaei S, Azadfar A, Salimi S. Comparison of the effect of preoperative oral tizanidine and pregabalin on shoulder pain in laparoscopic cholecystectomy under general anesthesia. Adv Biomed Res. 2023;12:58. doi:10.4103/abr.abr_222_22
  • Dadmehr S, Shooshtari Z, Alipour M, et al. Is preemptive oral tizanidine effective on postoperative pain intensity after bimaxillary orthognathic surgery? A triple-blind randomized clinical trial. World J Plast Surg. 2022;11:37–45. doi:10.52547/wjps.11.2.37
  • Yazicioğlu D, Caparlar C, Akkaya T, Mercan U, Kulaçoğlu H. Tizanidine for the management of acute postoperative pain after inguinal hernia repair: a placebo-controlled double-blind trial. Eur J Anaesthesiol. 2016;33:215–222. doi:10.1097/EJA.0000000000000371
  • Semenchuk MR, Sherman S. Effectiveness of tizanidine in neuropathic pain: an open-label study. J Pain. 2000;1:285–292. doi:10.1054/jpai.2000.9435
  • Pareek A, Chandurkar N, Chandanwale AS, Ambade R, Gupta A, Bartakke G. Aceclofenac-tizanidine in the treatment of acute low back pain: a double-blind, double-dummy, randomized, multicentric, comparative study against aceclofenac alone. Eur Spine J. 2009;18:1836–1842. doi:10.1007/s00586-009-1019-4
  • Berry H, Hutchinson DR. Tizanidine and ibuprofen in acute low-back pain: results of a double-blind multicentre study in general practice. J Int Med Res. 1988;16:83–91. doi:10.1177/030006058801600202
  • O’Rourke MJ, Keshock MC, Boxhorn CE, et al. Preoperative management of opioid and nonopioid analgesics: Society for Perioperative Assessment and Quality Improvement (SPAQI) consensus statement. Mayo Clin Proc. 2021;96:1325–1341. doi:10.1016/j.mayocp.2020.06.045
  • Tiansheng S, Jianxiong S, Zhongjun L, et al. Expert consensus in enhanced recovery after spinal surgery in China: perioperative management. Chin J Bone Joint Surg. 2017:271–279. doi:10.3969/j.issn.2095-9958.2017.04-01
  • The Group of Minimally Invasive Spinal Surgery and Enhanced Recovery, Professional Committee of Orthopaedic Surgery and Enhanced Recovery, Association of China Rehabilitation Technology Transformation and Promotion. Expert consensus on the implementation of enhanced recovery after surgery in percutaneous endoscopic interlaminar lumbar decompression/discectomy (2020). Zhongguo Xiu Fu Chong Jian Wai Ke Za Zhi. 2020;34:1497–1506. doi:10.7507/1002-1892.202011021
  • Rodríguez-Palma EJ, Castelo-Flores DG, Caram-Salas NL, et al. Sex-dependent antiallodynic effect of α2 adrenergic receptor agonist tizanidine in rats with experimental neuropathic pain. Eur J Pharmacol. 2022;920:174855. doi:10.1016/j.ejphar.2022.174855
  • Pei W, Zou Y, Wang W, Wei L, Zhao Y, Li L. Tizanidine exerts anti-nociceptive effects in spared nerve injury model of neuropathic pain through inhibition of TLR4/NF-κB pathway. Int J Mol Med. 2018;42:3209–3219. doi:10.3892/ijmm.2018.3878
  • Smrke A, Anderson PM, Gulia A, Gennatas S, Huang PH, Jones RL. Future directions in the treatment of osteosarcoma. Cells. 2021;10:172. doi:10.3390/cells10010172
  • Xing XW, Sun YF, Zhao J, Pan ZX, Jiang WX. Tizanidine hydrochloride exhibits a cytotoxic effect on osteosarcoma cells through the PI3K/AKT signaling pathway. J Int Med Res. 2019;47:3792–3802. doi:10.1177/0300060519850395
  • Zhao L, Zhao G, Xue Q. Tizanidine (hydrochloride) inhibits A549 lung cancer cell proliferation and motility through regulating Nischarin. Onco Targets Ther. 2020;13:291–298. doi:10.2147/OTT.S228317
  • Zhu J, Naulaerts S, Boudhan L, Martin M, Gatto L, Van den Eynde BJ. Tumour immune rejection triggered by activation of α2-adrenergic receptors. Nature. 2023;618(7965):607–615. doi:10.1038/s41586-023-06110-8
  • Patiño-Camacho SI, Déciga Campos M, Beltrán-Villalobos K, Castro-Vidal DA, Montiel-Ruiz RM, Flores-Murrieta FJ. Low doses of tizanidine synergize the anti-nociceptive and anti-inflammatory effects of ketorolac or naproxen while reducing of side effects. Eur J Pharmacol. 2017;805:51–57. doi:10.1016/j.ejphar.2017.03.021
  • Rodriguez-Silverio J, Sanchez-Mendoza ME, Arrieta-Valencia J, Rocha-Gonzalez HI, Flores-Murrieta FJ. Tizanidine increases antinociceptive effect and prevents gastric damage induced by ketorolac in the rat. Drug Dev Res. 2013;74:38–42. doi:10.1002/ddr.21054
  • Arpa MD, Nü O, Gök MK, Özgümüş S, Cevher E. Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine. Int J Pharm. 2023;642:123168. doi:10.1016/j.ijpharm.2023.123168
  • El-Mahrouk GM, El-Gazayerly ON, Aboelwafa AA, Taha MS. Chitosan lactate wafer as a platform for the buccal delivery of tizanidine HCl: in vitro and in vivo performance. Int J Pharm. 2014;467:100–112. doi:10.1016/j.ijpharm.2014.03.049
  • Zaman M, Hanif M, Shaheryar ZA, Xu B. Development of tizanidine HCl-meloxicam loaded mucoadhesive buccal films: in-vitro and in-vivo evaluation. PLoS One. 2018;13:e0194410. doi:10.1371/journal.pone.0194410
  • Dsouza L, Chaudhari P, Brahmam B, Lewis SA. Derma roller mediated transdermal delivery of tizanidine invasomes for the management of skeletal muscle spasms. Eur J Pharm Sci. 2021;165:105920. doi:10.1016/j.ejps.2021.105920
  • Thakkar H, Pandya K, Patel B. Microneedle-mediated transdermal delivery of tizanidine hydrochloride. Methods Mol Biol. 2020;2059:239–258. doi:10.1007/978-1-4939-9798-5_13
  • Khalil RM, Abdelbary A, Arini SKE, Basha M, El-Hashemy HA, Farouk F. Development of tizanidine loaded aspasomes as transdermal delivery system: ex-vivo and in-vivo evaluation. J Liposome Res. 2021;31:19–29. doi:10.1080/08982104.2019.1684940
  • Vitale DC, Piazza C, Sinagra T, et al. Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm. Clin Drug Investig. 2013;33:885–891. doi:10.1007/s40261-013-0137-2
  • Thakkar H, Modi B, Patel B. Intranasal spray of cubosomal tizanidine hydrochloride for brain targeting: in vitro and in vivo characterisation. J Microencapsul. 2023;40:366–383. doi:10.1080/02652048.2023.2209651
  • Moawad FA, Ali AA, Salem HF. Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance. Drug Deliv. 2017;24:252–260. doi:10.1080/10717544.2016.1245369
  • Zhang W, McIntyre C, Riehl T, et al. Effect of vemurafenib on the pharmacokinetics of a single dose of tizanidine (a CYP1A2 Substrate) in patients with BRAFV600 mutation-positive malignancies. Clin Pharmacol Drug Dev. 2020;9:651–658. doi:10.1002/cpdd.788
  • Ji Q, Yi D, Wang JY, et al. Expert consensus on management of chronic musculoskeletal pain in older adults (2019). Chin J Geriatr. 2019:500–507. doi:10.3760/cma.j.issn.0254-9026.2019.05.008
  • Chinese Association for the Study of Pain. Expert consensus on spinal degenerative nerve root pain treatment. Natl Med J China. 2019;1133–1137. doi:10.3760/cma.j.issn.0376-2491.2019.15.003
  • Kang PD, Huang ZY, Li T, et al. Expert consensus on chronic pain management in the musculoskeletal system. Chin J Bone Joint Surg. 2020:8–16. doi:10.3969/j.issn.2095-9958.2020.01.02
  • Gui R, Wang Y, Chen BH. Clinical guidelines for nonspecific low back pain in China. Chin J Spine Spinal Cord. 2022;32:258–268. doi:10.3969/j.issn.1004-406X.2022.03.09
  • Spinal pain Group Affiliated to Pain Society of Chinese Medical Association. Chinese expert consensus on diagnosis and treatment of sacroiliac joint pain. Chin J Pain Med. 2021;87–93. doi:10.3969/j.issn.1006-9852.2021.02.002
  • Smith H, Elliott J. Alpha(2) receptors and agonists in pain management. Curr Opin Anaesthesiol. 2001;14:513–518. doi:10.1097/00001503-200110000-00009
  • Piletz JE, Zhu H, Chikkala DN. Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J Pharmacol Exp Ther. 1996;279:694–702.
  • López-Córdoba G, Martínez-Lorenzana G, Lozano-Cuenca J, Condés-Lara M, González-Hernández A. The differential in vivo contribution of spinal α2A- and α2C-adrenoceptors in tonic and acute evoked nociception in the rat. Front Pharmacol. 2022;13:1023611. doi:10.3389/fphar.2022.1023611
  • Gyires K, Müllner K, Rónai AZ. Functional evidence that gastroprotection can be induced by activation of central alpha(2B)-adrenoceptor subtypes in the rat. Eur J Pharmacol. 2000;396:131–135. doi:10.1016/s0014-2999(00)00231-4
  • Zádori ZS, Shujaa N, Brancati SB, Hein L, Gyires K. Both α2B- and α2C-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. Eur J Pharmacol. 2011;669:115–120. doi:10.1016/j.ejphar.2011.07.018
  • Maeda-Hagiwara M, Watanabe H, Kanaoka R, Watanabe K. Influence of clonidine and a new related imidazoline derivative (tizanidine) on rat gastric mucosa. Pharmacology. 1986;32:109–113. doi:10.1159/000138158
  • Jain NK, Kulkarni SK, Singh A. Modulation of NSAID-induced antinociceptive and anti-inflammatory effects by alpha2-adrenoceptor agonists with gastroprotective effects. Life Sci. 2002;70:2857–2869. doi:10.1016/s0024-3205(02)01549-7
  • Emre M. The gastroprotective effects of tizanidine: an overview. Curr Therap Res. 1998;59:2–12. doi:10.1016/S0011-393X(98)85018-2
  • Kroin JS, McCarthy RJ, Penn RD, Lubenow TJ, Ivankovich AAD. Continuous intrathecal clonidine and tizanidine in conscious dogs: analgesic and hemodynamic effects. Anesth Analg. 2003;96:776–782. doi:10.1213/01.ANE.0000048087.57487.0C
  • Kawamata T, Omote K, Yamamoto H, Toriyabe M, Wada K, Namiki A. Antihyperalgesic and side effects of intrathecal clonidine and tizanidine in a rat model of neuropathic pain. Anesthesiology. 2003;98:1480–1483. doi:10.1097/00000542-200306000-00027
  • Zhang SJ, Lai G, Griffis CA, Schiltz M, Aroke EN. α2-Adrenergic receptor agonist, an attractive but underused ERAS component in improving fast-track recovery and surgical outcomes. AANA J. 2021;89:529–537.
  • Wolf E, Kothari NR, Roberts JK, Sparks MA. Baclofen toxicity in kidney disease. Am J Kidney Dis. 2018;71(2):275–280. doi:10.1053/j.ajkd.2017.07.005
  • Chou R, Peterson K, Helfand M. Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review. J Pain Symptom Manage. 2004;28(2):140–175. doi:10.1016/j.jpainsymman.2004.05.002
  • Li Y, Delcher C, Reisfield GM, Wei Y-J, Brown JD, Winterstein AG. Utilization patterns of skeletal muscle relaxants among commercially insured adults in the United States from 2006 to 2018. Pain Med. 2021;22(10):2153–2161. doi:10.1093/pm/pnab088
  • Wang RW, Liu L, Cheng H. Identification of human liver cytochrome P450 isoforms involved in the in vitro metabolism of cyclobenzaprine. Drug Metab Dispos. 1996;24(7):786–791.
  • See S, Ginzburg R. Choosing a skeletal muscle relaxant. Am Fam Physician. 2008;78(3):365–370.
  • Spence MM, Shin PJ, Lee EA, Gibbs NE. Risk of injury associated with skeletal muscle relaxant use in older adults. Ann Pharmacother. 2013;47(7–8):993–998. doi:10.1345/aph.1R735
  • Cherrington B, Englich U, Niruntari S, Grant W, Hodgman M. Monoamine oxidase A inhibition by toxic concentrations of metaxalone. Clin Toxicol. 2020;58(5):383–387. doi:10.1080/15563650.2019.1648815
  • RxList [homepage on the Internet]. VANADOM; 2023. Available from: https://www.rxlist.com/vanadom-drug.htm#clinpharm. Accessed February 29, 2024.
  • CPIC [hompage on the Internet]. Prioritization of CPIC guidelines. Available from: https://cpicpgx.org/prioritization-of-cpic-guidelines/. Accessed February 2, 2024.
  • Zubiaur P, Figueiredo-Tor L, Villapalos-García G, et al. Association between CYP2C19 and CYP2B6 phenotypes and the pharmacokinetics and safety of diazepam. Biomed Pharmacother. 2022;155:113747. doi:10.1016/j.biopha.2022.113747
  • Almansa C, Frampton CS, Vela JM, Whitelock S, Plata-Salamán CR. Co-crystals as a new approach to multimodal analgesia and the treatment of pain. J Pain Res. 2019;12:2679–2689. doi:10.2147/JPR.S208082
  • Beltrán-Villalobos KL, Ramírez-Marín PM, Cruz CA, Déciga-Campos M. Coadministration of tramadol and tizanidine in an experimental acute pain model in rat. Drug Dev Res. 2014;75:473–478. doi:10.1002/ddr.21229
  • ClinicalTrials.gov [hompage on the Internet]. Study to assess the efficacy and safety of tizaspray® Versus Sirdalud®, in patients with acute low back pain; 2018. Available from: https://clinicaltrials.gov/study/NCT02934061. Accessed January 21, 2024.
  • Nalamachu S, Pergolizzi J, Kaye R. Tolperisone for the treatment of acute muscle spasm of the back: results from the dose-ranging Phase 2 STAR Study (NCT03802565). J Pain Res. 2020;13:3059–3069. doi:10.2147/JPR.S278857
  • Byeon JY, Cho CK, Kang P, et al. Effects of CYP2D6 and CYP2C19 genetic polymorphisms and cigarette smoking on the pharmacokinetics of tolperisone. Arch Pharm Res. 2023;46:713–721. doi:10.1007/s12272-023-01462-1
  • McLaughlin MJ, He Y, Brunstrom-Hernandez J, et al. Pharmacogenomic variability of oral baclofen clearance and clinical response in children with cerebral palsy. PM R. 2018;10:235–243. doi:10.1016/j.pmrj.2017.08.441
  • Jogiraju VK, Heimbach T, Toderika Y, Taft DR. Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: impact of drug-drug interactions and cigarette consumption. Drug Metab Pharmacokinet. 2021;37:100375. doi:10.1016/j.dmpk.2020.100375