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Tizanidine: Difference between revisions

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{{SubstanceBox/Tizanidine}}
{{SubstanceBox/Tizanidine}}


'''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 [[chemical class::arylaminoimidazoline]] 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 α<sub>2</sub> adrenergic agonist. The relationship between the α<sub>2</sub> 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> .
Tizanidine is a central α<sub>2</sub> adrenergic agonist. The relationship between the α<sub>2</sub> 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> .
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==Pharmacology==
==Pharmacology==
Tizanidine is an [[imidazoline]] derivative and centrally acting α<sub>2</sub> [[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 α<sub>2</sub> [[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 <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 also has some affinity for the α<sub>1</sub> 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 α<sub>1</sub> 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> .
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*'''[[Effect::Muscle relaxation]]'''
*'''[[Effect::Muscle relaxation]]'''
*'''[[Effect::Physical euphoria]]''' - This effect is very mild and may not be pronounced at all in some users.
*'''[[Effect::Physical euphoria]]''' - This effect is very mild and may not be pronounced at all in some users.
*'''[[Effect::Lip numbing]]''' - Numbing of the lips only occurs at higher doses as a result of low blood pressure.
*'''[[Effect::Spontaneous bodily sensations]]''' - It only occurs at higher doses as a result of low blood pressure and mostly at lips.  
*'''[[Effect::Perception of bodily heaviness]]'''
*'''[[Effect::Perception of bodily heaviness]]'''
*'''[[Effect::Decreased blood pressure]]'''  
*'''[[Effect::Decreased blood pressure]]'''  
*'''[[Effect::Decreased heart rate]]'''
*'''[[Effect::Decreased heart rate]]'''
*'''[[Effect::Abnormal heartbeat]]'''
*'''[[Effect::Abnormal heartbeat]]'''
*'''[[Effect::Dizziness]]''' - Because of the cardiovascular effects of tizanidine, users can become dizzy or lightheaded.
*'''[[Effect::Dizziness]]''' - Because of the cardiovascular effects of Tizanidine, users can become dizzy or lightheaded.
*'''[[Effect::Headache]]''' - When taking excessive doses, headaches are a common side effect.
*'''[[Effect::Headache]]''' - When taking excessive doses, headaches are a common side effect.
*'''[[Effect::Watery eyes]]'''
*'''[[Effect::Watery eyes]]'''
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*'''[[Effect::Pupil constriction]]'''
*'''[[Effect::Pupil constriction]]'''
*'''[[Effect::Dry mouth]]'''
*'''[[Effect::Dry mouth]]'''
}}


}}
{{effects/visual|
{{effects/visual|
 
*'''[[Effect::Acuity suppression]]''' - This effect typically presents itself at higher doses.
 
 
*'''[[Effect::Blurred vision]]''' - This effect typically presents itself at higher doses.
*'''[[Effect::Acuity suppression]]'''


====Distortions====
====Distortions====
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*'''[[Effect::Scenarios and plots]]'''
*'''[[Effect::Scenarios and plots]]'''
}}
}}


|{{effects/cognitive|
|{{effects/cognitive|
*'''[[Effect::Cognitive fatigue]]'''
*'''[[Effect::Cognitive fatigue]]'''
*'''[[Effect::Dream potentiation]]''' - Some users of tizanidine notice strange or increasingly vivid dreams after continuous use of tizanidine.
*'''[[Effect::Dream potentiation]]''' - Some users of tizanidine notice strange or increasingly vivid dreams after continuous use of tizanidine.
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*'''[[Effect::Delirium]]''' - At extremely high doses, delirium can be induced.
*'''[[Effect::Delirium]]''' - At extremely high doses, delirium can be induced.
*'''[[Effect::Sleepiness]]''' - This is the most prevalent cognitive effect of Tizanidine
*'''[[Effect::Sleepiness]]''' - This is the most prevalent cognitive effect of Tizanidine
}}
}}


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===Lethal dosage===
===Lethal dosage===
The [[LD50]] of oral tizanidine in rats was found to be 414mg/kg in rats and 235 mg/kg in mice<ref> https://www.drugbank.ca/drugs/DB00697 </ref>.
The [[LD50]] of oral tizanidine in rats was found to be 414mg/kg in rats and 235 mg/kg in mice<ref> https://www.drugbank.ca/drugs/DB00697 </ref>.
In some cases, Tizanidine overdose can be reversed with naloxone; however, this is not the case with everyone <ref> Bader D, Adam A, Shaban M, Alyahya B. Pediatric tizanidine toxicity reversed with naloxone: a case report. Int J Emerg Med. 2021 Dec 14;14(1):73. doi: 10.1186/s12245-021-00397-y. PMID: 34906071; PMCID: PMC8903539. </ref> <ref> Spiller HA, Bosse GM, Adamson LA. Retrospective review of Tizanidine (Zanaflex) overdose. J Toxicol Clin Toxicol. 2004;42(5):593-6. doi: 10.1081/clt-200026978. PMID: 15462150. </ref>.
===Tolerance and addiction potential===
===Tolerance and addiction potential===
While dependence is rare, use of Tizanidine exceeding 36mg daily over an extended period of time can lead to hypertensive withdrawals. In cases where dependence has been built, a user should taper to avoid a hypertensive crisis<ref> "Tizanidine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019. </ref>.
While dependence is rare, use of Tizanidine exceeding 36mg daily over an extended period of time can lead to hypertensive withdrawals. In cases where dependence has been built, a user should taper to avoid a hypertensive crisis<ref> "Tizanidine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019. </ref>.
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==Legal status==
==Legal status==
{{LegalStub}}
{{LegalStub}}
* '''Austria:''' Tizanidine is available by prescription only.
* '''Turkey:''' Tizanidine is available in pharmacies without prescription.
* '''United States:''' Tizanidine is available by prescription only.
* '''United States:''' Tizanidine is available by prescription only.
* '''United Kingdom:''' Tizanidine is available by prescription only.
* '''United Kingdom:''' Tizanidine is available by prescription only.
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==External links==
==External links==
* [https://en.wikipedia.org/wiki/Tizanidine (Wikipedia)]
*[https://en.wikipedia.org/wiki/Tizanidine Tizanidine (Wikipedia)]
* [https://erowid.org/experiences/subs/exp_Tizanidine.shtml Tizanidine (Erowid Vault)]
*[https://isomerdesign.com/pihkal/explore/15021 Tizanidine (IsomerDesign)]
* [https://druginfo.nlm.nih.gov/drugportal/name/tizanidine "Tizanidine"]. Drug Information Portal. U.S. National Library of Medicine.
*[https://erowid.org/experiences/subs/exp_Tizanidine.shtml Tizanidine (Erowid Vault)]
*[https://go.drugbank.com/drugs/DB00697 Tizanidine (DrugBank)]


==References==
==References==
<references />
<references />


[[Category:Psychoactive substance]][[Category:Proofread]][[Category:Approval]]
[[Category:Psychoactive substance]]
[[Category:Arylaminoimidazoline]]
[[Category:Depressant]]
Retrieved from "http://psy.st/wiki/Tizanidine"