Tizanidine: Difference between revisions

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Tizanidine is an imidazoline derivative and centrally acting α2 receptor 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.

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;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/ </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 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.

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> S;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. 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>S;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/ </ref>.

@@ Line 16: / Line 16: @@
 Tizanidine is an imidazoline derivative and centrally acting α2 receptor 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.
+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;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/  </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 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.
+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> S;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. 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>S;, M. I. K. (n.d.). Tizanidine may discriminate between imidazoline-receptors and alpha 2-adrenoceptors. Japanese journal of pharmacology. Retrieved from https://pubmed.ncbi.nlm.nih.gov/1331591/ </ref>.