Tizanidine: Difference between revisions

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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 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> .
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 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> .


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 <ref> Denizbaşi A, Berkman K, Ozyazgan S, Eşkazan E. The effect of tizanidine on maximal electroshock seizures (MES) in mice. Gen Pharmacol. 1999 Apr;32(4):513-6. doi: 10.1016/s0306-3623(98)00249-3. Erratum in: Gen Pharmacol 2000 Jun;34(6):443. PMID: 10323494. </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 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>