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药品详细

Tizanidine(替扎尼定)

化学结构式图
中文名
替扎尼定
英文名
Tizanidine
分子式
C9H8ClN5S
化学名
5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
分子量
Average: 253.711
Monoisotopic: 253.018893678
CAS号
51322-75-9
ATC分类
M03B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

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.

生产厂家
  • Acorda therapeutics inc
  • Actavis elizabeth llc
  • Actavis totowa llc
  • Alphapharm party ltd
  • Apotex inc
  • Barr laboratories inc
  • Caraco pharmaceutical laboratories ltd
  • Corepharma llc
  • Dr reddys laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzene and Derivatives
  • Halobenzenes
  • Anilines
Substructures
  • Imidazolines
  • Thiadiazoles
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Imidazoles
  • Heterocyclic compounds
  • Guanidines
  • Aromatic compounds
  • Carboxamidines
  • Anilines
适应症
药理
Indication For the management of increased muscle tone associated with spasticity
Pharmacodynamics 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.
Mechanism of action Tizanidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.
Absorption Not Available
Volume of distribution
  • 2.4 L/kg
Protein binding 30%
Metabolism
Not Available

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Tizanidine
5-chloro-4-(guanidino)-2,1,3-benzothiadiazole Details
Tizanidine
5-chloro-4-(2-imidazolin-4-on-2-ylamino)-2,1,3-benzothiadiazole Details
Route of elimination Approximately 95% of an administered dose is metabolized.
Half life 2.5 hours
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 1.4 Not Available
Predicted Properties
Property Value Source
water solubility 1.33e-01 g/l ALOGPS
logP 1.6 ALOGPS
logP 2.02 ChemAxon
logS -3.3 ALOGPS
pKa (strongest basic) 7.49 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 62.2 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 64.77 ChemAxon
polarizability 23.97 ChemAxon
药物相互作用
Drug Interaction
Amiodarone Amiodarone 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.
Benazepril Tizanidine increases the risk of hypotension with the ACE inhibitor
Captopril Tizanidine increases the risk of hypotension with the ACE inhibitor
Cilazapril Tizanidine increases the risk of hypotension with the ACE inhibitor
Cimetidine Cimetidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Ciprofloxacin Ciprofloxacin inhibits the metabolism and clearance of Tizanidine. Concomitant therapy is contraindicated.
Diclofenac Diclofenac may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Donepezil Possible antagonism of action
Enalapril Tizanidine increases the risk of hypotension with the ACE inhibitor
Ethanol Ethanol increases the adverse effects of Tizanidine. The CNS depressant effects of these agents are additive.
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.
Fluoxetine Fluoxetine 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.
Fosinopril Tizanidine increases the risk of hypotension with the ACE inhibitor
Galantamine Possible antagonism of action
Gemfibrozil Gemfibrozil 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.
Lidocaine Lidocaine 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.
Methoxsalen Methoxsalen may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Mexiletine Mexilitene may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Miconazole Miconazole may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Moexipril 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.
Nifedipine Nifedipine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Norethindrone The contraceptive increases the effect of tizanidine
Norfloxacin Norfloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Ofloxacin Ofloxacin 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
Primaquine Primaquine 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.
Propofol Propofol may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Quinapril Tizanidine increases the risk of hypotension with the ACE inhibitor
Quinupristin This combination presents an increased risk of toxicity
Ramipril Tizanidine increases the risk of hypotension with the ACE inhibitor
Rivastigmine Possible antagonism of action
Spirapril Tizanidine increases the risk of hypotension with the ACE inhibitor
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.
Ticlopidine Ticlopidine 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
Tranylcypromine Tranylcypromine 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.
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.
Triprolidine The CNS depressants, Triprolidine and Tizanidine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
食物相互作用
Not Available

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