QuickView for Tizanidine (compound)

Summary
General Info

PubChem

PubChem Compound 114869

Name:	tizanidine
PubChem Compound ID:	114869
Molecular formula:	C₉H₉Cl₂N₅S
Molecular weight:	290.173 g/mol
Synonyms:	5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole monohydrochloride; DS-103282 ch; Sirdalud; Ternelin; 51322-75-9; 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole hydrochloride; Tizanidine hydrochloride (JP15/USAN); AN-021A; Zanaflex; D00776. show more » 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole monohydrochloride; DS-103282 ch; Sirdalud; Ternelin; 51322-75-9; 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole hydrochloride; Tizanidine hydrochloride (JP15/USAN); AN-021A; Zanaflex; D00776; LS-40461; DS-103282; DS 103-282; Tizanidine hydrochloride [USAN:JAN]; 64461-82-1; Zanaflex (TN); Tizanidine hydrochloride; 2,1,3-Benzothiadiazol-4-amine, 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-, monohydrochloride show less «

DrugBank

Identification

Name:	tizanidine
Name (isomeric):	DB00697
Drug Type:	small molecule
Synonyms:	Tizanidine Hcl; Tizanidina [INN-Spanish]; Tizanidinum [INN-Latin]
Brand:	Sirdalud, Zanaflex, Ternelin
Category:	Parasympatholytics, Adrenergic alpha-Agonists, Muscle Relaxants, Central, Muscle Relaxants, Analgesics, Anticonvulsants, Skeletal Muscle Relaxants
CAS number:	51322-75-9

Pharmacology

Indication:	For the management of increased muscle tone associated with spasticity
Pharmacology:	Tizanidine is a short-acting drug for the management of spasticity. Tizanidine is an agonist at a2-adrenergic receptor sites and presumably reduces spasticity by increasing presynaptic inhibition of motor neurons. In animal models, tizanidine has no direct effect on skeletal muscle fibers or the neuromuscular junction, and no major effect on monosy... show more » Tizanidine is a short-acting drug for the management of spasticity. Tizanidine is an agonist at a2-adrenergic receptor sites and presumably reduces spasticity by increasing presynaptic inhibition of motor neurons. In animal models, tizanidine has no direct effect on skeletal muscle fibers or the neuromuscular junction, and no major effect on monosynaptic spinal reflexes. The effects of tizanidine are greatest on polysynaptic pathways. The overall effect of these actions is thought to reduce facilitation of spinal motor neurons. show less «
Mechanism of Action:	Tizanidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.
Protein binding:	30%
Route of elimination:	Approximately 95% of an administered dose is metabolized.
Half Life:	2.5 hours
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Ethinyl Estradiol	Ethinyl estradiol may increase the serum concentration of tizanidine. Monitor for changes in the therapeutic and adverse effects of tizanidine if ethinyl estradiol is initiated, discontinued or dose changed.
Benazepril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Ofloxacin	Ofloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Cimetidine	Cimetidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Gemfibrozil	Gemfibrozil may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.

Ethinyl Estradiol	Ethinyl estradiol may increase the serum concentration of tizanidine. Monitor for changes in the therapeutic and adverse effects of tizanidine if ethinyl estradiol is initiated, discontinued or dose changed.
Benazepril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Ofloxacin	Ofloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Cimetidine	Cimetidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Gemfibrozil	Gemfibrozil may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Trandolapril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Fluoxetine	Fluoxetine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Triprolidine	The CNS depressants, Triprolidine and Tizanidine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Propofol	Propofol may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Donepezil	Possible antagonism of action
Captopril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Lidocaine	Lidocaine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Thiabendazole	The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Tizanidine by decreasing Tizanidine metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Tizanidine if Thiabendazole is initiated, discontinued or dose changed.
Spirapril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Ramipril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Norethindrone	The contraceptive increases the effect of tizanidine
Diclofenac	Diclofenac may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Amlodipine	Amlopidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Perindopril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Moxifloxacin	Moxifloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Quinapril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Enalapril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Ciprofloxacin	Ciprofloxacin inhibits the metabolism and clearance of Tizanidine. Concomitant therapy is contraindicated.
Amiodarone	Amiodarone may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Tranylcypromine	Tranylcypromine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Propafenone	Propafenone may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Methoxsalen	Methoxsalen may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Ethanol	Ethanol increases the adverse effects of Tizanidine. The CNS depressant effects of these agents are additive.
Moexipril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Galantamine	Possible antagonism of action
Ticlopidine	Ticlopidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Ketoconazole	Ketoconazole may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Quinupristin	This combination presents an increased risk of toxicity
Nifedipine	Nifedipine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Norfloxacin	Norfloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Cilazapril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Miconazole	Miconazole may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Rivastigmine	Possible antagonism of action
Primaquine	Primaquine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Fluvoxamine	Fluvoxamine inhibits the metabolism and clearance of tizanidine. Concomitant therapy is contraindicated.
Trimipramine	Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Tizandine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Tizandine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Mexiletine	Mexilitene may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Lisinopril	Tizanidine increases the risk of hypotension with the ACE inhibitor
Mestranol	Oral contraceptives decrease the clearance of Tizanidine.
Fosinopril	Tizanidine increases the risk of hypotension with the ACE inhibitor

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Targets

Alpha-2A adrenergic receptor

Alpha-2B adrenergic receptor

Alpha-2C adrenergic receptor

Nischarin

Enzymes

Cytochrome P450 1A2