Tìm theo
Tizanidine
Các tên gọi khác (5 ) :
  • 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
  • Tizanidin
  • Tizanidina
  • Tizanidine
  • Tizanidinum
Thuốc giãn cơ và tăng trương lực cơ
Thuốc Gốc
Small Molecule
CAS: 51322-75-9
ATC: M03BX02
ĐG : Acorda Therapeutics , http://www.acorda.com
CTHH: C9H8ClN5S
PTK: 253.711
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H8ClN5S
Phân tử khối
253.711
Monoisotopic mass
253.018893678
InChI
InChI=1S/C9H8ClN5S/c10-5-1-2-6-8(15-16-14-6)7(5)13-9-11-3-4-12-9/h1-2H,3-4H2,(H2,11,12,13)
InChI Key
InChIKey=XFYDIVBRZNQMJC-UHFFFAOYSA-N
IUPAC Name
5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
Traditional IUPAC Name
tizanidine
SMILES
ClC1=C(NC2=NCCN2)C2=NSN=C2C=C1
Độ hòa tan
1.33e-01 g/l
logP
1.4
logS
-3.3
pKa (Strongest Basic)
7.49
PSA
62.2 Å2
Refractivity
64.77 m3·mol-1
Polarizability
23.97 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. Tizanidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.
Dược Động Học :

▧ Volume of Distribution :
* 2.4 L/kg
▧ Protein binding :
30%
▧ Route of Elimination :
Approximately 95% of an administered dose is metabolized.
▧ Half Life :
2.5 hours
Chỉ Định : For the management of increased muscle tone associated with spasticity
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
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    Sản phẩm biệt dược : Zanaflex
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00697
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5487
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505373
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07452
ChemSpider
http://www.chemspider.com/Chemical-Structure.5287.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240671
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0722-01
PharmGKB
http://www.pharmgkb.org/drug/PA451701
Wikipedia
http://en.wikipedia.org/wiki/Tizanidine
RxList
http://www.rxlist.com/cgi/generic/tizanidine.htm
Drugs.com
http://www.drugs.com/tizanidine.html
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