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Tizanidine: Difference between revisions
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Tizanidine is an [[imidazoline]] derivative and centrally acting α2 [[adrenergic]] [[agonist]] closely related to Clonidine. Tizanidine inhibits the release of excitatory amino acids from spinal interneurons. As a result, Tizanidine enhances the presynaptic inhibition of motor neurons. | Tizanidine is an [[imidazoline]] derivative and centrally acting α2 [[adrenergic]] [[agonist]] closely related to Clonidine. Tizanidine inhibits the release of excitatory amino acids from spinal interneurons. As a result, Tizanidine enhances the presynaptic inhibition of motor neurons. | ||
Tizanidine also has some affinity for the α1 receptors, but to a lesser than Clonidine, which may explain why its cardiovascular effects are so much milder than that of Clonidine<ref> S | Tizanidine also has some affinity for the α1 receptors, but to a lesser than Clonidine, which may explain why its cardiovascular effects are so much milder than that of Clonidine<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 also been found to have [[anticonvulsant]] effects against strychnine-induced seizures but not against [[GABA]]-induced seizures. The α2 receptor mediated inhibition of inter-neuronal activity appears to be the cause of Tizanidine's anti-convulsant properties. | Tizanidine has also been found to have [[anticonvulsant]] effects against strychnine-induced seizures but not against [[GABA]]-induced seizures. The α2 receptor mediated inhibition of inter-neuronal activity appears to be the cause of Tizanidine's anti-convulsant properties. | ||
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> | 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> | ||
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>S | 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>. | ||
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