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Tizanidine
drug data and news
Tizanidine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Tizanidine | ||
| Brand Names/Synonyms | CHEMBANK1846; Pramiracetam; Sirdalud; Ternelin; Tizanidina [Inn-Spanish]; Tizanidine; Tizanidine Hcl; Tizanidinum [Inn-Latin]; Zanaflex | ||
| Indication | For the management of increased muscle tone associated with spasticity | ||
| Sponsored links | Description | Not Available | |
| 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 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. | ||
| Tizanidine News (When available) |
Acorda Therapeutics Reports First Quarter 2006 Financial Results May 5, 2006 Acorda Therapeutics to Present at Two Upcoming Conferences May 8, 2006 Acorda Therapeutics Reports First Quarter 2006 Financial Results May 5, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Muscle Relaxants; Anticonvulsants; Analgesics; Skeletal Muscle Relaxants; ATC:M03BX02 | ||
| Absorption | Not Available | ||
| Interactions |
-->Interactions for Tizanidine: In vitro studies of cytochrome P450 isoenzymes using human liver microsomes indicate that neither tizanidine nor the major metabolites are likely to affect the metabolism of other drugs metabolized by cytochrome P450 isoenzymes. Acetaminophen: Tizanidine delayed the Tmax of acetaminophen by 16 minutes. Acetaminophen did not affect the pharmacokinetics of tizanidine. Alcohol: Alcohol increased the AUC of tizanidine by approximately 20% while also increasing its Cmax by approximately 15%. This was associated with an increase in side effects of tizanidine. The CNS depressant effects of tizanidine and alcohol are additive. Fluvoxamine: Clinically significant hypotension (decreases in both systolic and diastolic pressure) has been reported with concomitant administration of fluvoxamine following single doses of 4 mg. Caution is recommended when considering concomitant use of tizanidine with other inhibitors of CYP1A2, such as, antiarrhythmics (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones (ciprofloxacin, norfloxacin), rofecoxib, oral contraceptives, and ticlopidine. Oral Contraceptives: No specific pharmacokinetic study was conducted to investigate interaction between oral contraceptives and tizanidine, but retrospective analysis of population pharmacokinetic data following single and multiple dose administration of 4 mg tizanidine showed that women concurrently taking oral contraceptives had 50% lower clearance of tizanidine than women not on oral contraceptives. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-8-thia-7,9-diazabicyclo[4.3.0]nona-2,4,6,9-tetraen-5-amine | ||
| Chemical Formula | C9H8ClN5S | ||
| Molecular Weight | 253.712 g/mol | ||
| Smiles String | C1CN=C(N1)NC2=C(C=CC3=NSN=C32)Cl | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | -1.591 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 2.5 hours | ||
| Protein Binding [%] | 30% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Tizanidine.html http://www.rxlist.com/cgi/generic/tizanidine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00128 | ||
| CAS Registry Number | 51322-75-9 | ||
| KEGG Compound ID | C07452 | ||
| PubChem ID | SID:180932 | ||
| PharmGKB ID | Not Available | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2259893 |
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