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Tizanidine: Difference between revisions
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==Pharmacology== | ==Pharmacology== | ||
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 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. | ||
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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. | 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. | ||
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>. | |||
{| class="wikitable" | |||
|- | |||
! Drug | |||
! Imidazoline receptors Ki (nM) | |||
! α2 Receptors Ki (nM) | |||
|- | |||
| Tizanidine | |||
| 4.17 ± 1.81 | |||
| 91.5 ± 9.1 | |||
|- | |||
| Clonidine | |||
| 9.20 ± 1.23 | |||
| 9.20 ± 1.23 | |||
|- | |||
| Oxymethazoline | |||
| 2.28 ± 0.36 | |||
| 25.9 ± 5.5 | |||
|- | |||
| Naphazoline | |||
| 309 ± 26 | |||
| 25.9 ± 5.5 | |||
|- | |||
| Adrenaline | |||
| > 10000 | |||
| 3.18 ± 0.41 | |||
|- | |||
|} | |||
==Subjective effects== | ==Subjective effects== | ||
{{Preamble/SubjectiveEffects}} | {{Preamble/SubjectiveEffects}} | ||