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Tizanidine: Difference between revisions
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'''Tizanidine''' (known by the trade names '''Zanaflex''' and '''Trinex''' among others) is a [[depressant]] substance of the imidazoline class closely related to [[clonidine]]. Tizanidine is primarily used primarily as an antispasmodic drug. Tizanidine's effectivness is similar to that of [[baclofen]] or [[diazepam]] <ref> Wagstaff AJ, Bryson HM. Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs. 1997 Mar;53(3):435-52. doi: 10.2165/00003495-199753030-00007. PMID: 9074844. </ref>. | '''Tizanidine''' (known by the trade names '''Zanaflex''' and '''Trinex''' among others) is a [[depressant]] substance of the imidazoline class closely related to [[clonidine]]. Tizanidine is primarily used primarily as an antispasmodic drug. Tizanidine's effectivness is similar to that of [[baclofen]] or [[diazepam]] <ref> Wagstaff AJ, Bryson HM. Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs. 1997 Mar;53(3):435-52. doi: 10.2165/00003495-199753030-00007. PMID: 9074844. </ref>. | ||
Tizanidine is a central α2 adrenergic agonist. The relationship between the α2 receptor agonism and the spasmolytic function of tizanidine is not fully understood. | Tizanidine is a central α2 adrenergic agonist. The relationship between the α2 receptor agonism and the spasmolytic function of tizanidine is not fully understood <ref> Katzung, Bertram G. (30 November 2017). Basic & clinical pharmacology. Katzung, Bertram G. (Fourteenth ed.). New York. p. 487. ISBN 9781259641152. OCLC 1015240036 </ref> . | ||
While recreational use is extremely rare, some users take tizanidine for its standalone sedative effects or to potentiate the effects of [[opiates]]. In higher doses, tizanidine is capable of inducing [[hallucinations]], [[psychosis]], and [[delirium]]. | While recreational use is extremely rare, some users take tizanidine for its standalone sedative effects or to potentiate the effects of [[opiates]]. In higher doses, tizanidine is capable of inducing [[hallucinations]], [[psychosis]], and [[delirium]]. | ||
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Tizanidine has an oral bioavailability of 20-34% and an elimination half-life of 2.5 hours. It attains steady-state concentration within 24-48 hours after administration <ref>Ghanavatian S, Derian A. Tizanidine. [Updated 2021 Aug 13]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK519505/ </ref> | Tizanidine has an oral bioavailability of 20-34% and an elimination half-life of 2.5 hours. It attains steady-state concentration within 24-48 hours after administration <ref>Ghanavatian S, Derian A. Tizanidine. [Updated 2021 Aug 13]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK519505/ </ref> | ||
Tizanidine has approximately one tenth to one fifteenth of the blood pressure lowering effect of clonidine <ref> Katzung, Bertram G. (30 November 2017). Basic & clinical pharmacology. Katzung, Bertram G. (Fourteenth ed.). New York. p. 487. ISBN 9781259641152. OCLC 1015240036 </ref> . | |||
The table below compares the selectivity of Tizanidine and other drugs to the imidzaoline-receptor and the α2 receptors in rats. Tizanidine has a significantly greater selectivity to the imidazoline receptor than clonidine. The imidazoline receptor selectivity of tizanidine may be responsible for its unique pharmacological profile<ref>Muramatsu I, Kigoshi S. Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Jpn J Pharmacol. 1992 Aug;59(4):457-9. doi: 10.1254/jjp.59.457. PMID: 1331591.. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/ </ref>. | The table below compares the selectivity of Tizanidine and other drugs to the imidzaoline-receptor and the α2 receptors in rats. Tizanidine has a significantly greater selectivity to the imidazoline receptor than clonidine. The imidazoline receptor selectivity of tizanidine may be responsible for its unique pharmacological profile<ref>Muramatsu I, Kigoshi S. Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Jpn J Pharmacol. 1992 Aug;59(4):457-9. doi: 10.1254/jjp.59.457. PMID: 1331591.. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/ </ref>. | ||