Tizanidine
Identification
- Summary
Tizanidine is an alpha-2 adrenergic agonist used for the short-term treatment of muscle spasticity.
- Brand Names
- Zanaflex
- Generic Name
- Tizanidine
- DrugBank Accession Number
- DB00697
- Background
Tizanidine is a fast-acting drug used for the management of muscle spasm, which may result from the effects of multiple sclerosis, stroke, an acquired brain injury, or a spinal cord injury 9. It may also be caused by musculoskeletal injury 5. Regardless of the cause, muscle spasticity can be an extremely painful and debilitating condition.
Initially approved by the FDA in 1996, tizanidine is an Alpha-2 adrenergic receptor agonist reducing spasticity by the presynaptic inhibition of excitatory neurotransmitters that cause firing of neurons promoting muscle spasm Label.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 253.711
Monoisotopic: 253.018893678 - Chemical Formula
- C9H8ClN5S
- Synonyms
- 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
- Tizanidin
- Tizanidina
- Tizanidine
- Tizanidinum
- External IDs
- AN 021
- DS 103-282
Pharmacology
- Indication
Tizanidine is indicated for the relief of muscle spasticity, which can interfere with daily activities. The general recommendation is to reserve tizanidine use for periods of time when there is a particular need for relief, as it has a short duration of action Label,11.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute low back pain ••• ••••• Treatment of Drug withdrawal headache ••• ••••• Treatment of Insomnia ••• ••••• Treatment of Migraine ••• ••••• Management of Muscle spasticity •••••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
A note on spasticity
Spasticity is an increase in muscle accompanied by uncontrolled, repetitive contractions of skeletal muscles which are involuntary. The patient suffering from muscle spasticity may have reduced mobility and high levels of pain, contributing to poor quality of life and problems performing activities of personal hygiene and care 7.
General effects
Tizanidine is a rapidly acting drug used for the relief of muscle spasticity when it is required for performing specific activities. It acts as an agonist at Alpha-2 adrenergic receptor sites and relieves symptoms of muscle spasticity, allowing the continuation of normal daily activities. In animal models, tizanidine has not been shown to exert direct effects on skeletal muscle fibers or the neuromuscular junction, and has shown no significant effect on monosynaptic spinal reflexes (consisting of the communication between only 1 sensory neuron and 1 motor neuron) 10. The frequency of muscle spasm and clonus are shown to be decreased by tizanidine 9. Tizanidine shows a stronger action on polysynaptic reflexes, which involve several interneurons (relay neurons) communicating with motor neurons stimulating muscle movement 10.
Effects on blood pressure and heart rate
This drug decreases heart rate and blood pressure in humans 4,6. Despite this, rebound hypertension and tachycardia along with increased spasticity can occur when tizanidine is abruptly discontinued 8.
- Mechanism of action
Tizanidine reduces spasticity by causing presynaptic inhibition of motor neurons via agonist actions at Alpha-2 adrenergic receptor sites. This drug is centrally acting and leads to a reduction in the release of excitatory amino acids like glutamate and aspartate, which cause neuronal firing that leads to muscle spasm. The above reduction and excitatory neurotransmitter release results in presynaptic inhibition of motor neurons. The strongest effect of tizanidine has been shown to occur on spinal polysynaptic pathways. The anti-nociceptive and anticonvulsant activities of tizanidine may also be attributed to agonist action on Alpha-2 receptors. Tizanidine also binds with weaker affinity to the Alpha-1 receptors, explaining its slight and temporary effect on the cardiovascular system 9.
Target Actions Organism NNischarin agonistHumans UAlpha-1 adrenergic receptors agonistHumans UAlpha-2 adrenergic receptors agonistHumans - Absorption
This drug undergoes significant first-pass metabolism. After the administration of an oral dose, tizanidine is mostly absorbed. The absolute oral bioavailability of tizanidine is measured to be about 40% Label.
Effect of food on absorption
Food has been shown to increase absorption for both the tablets and capsules. The increase in absorption with the tablet (about 30%) was noticeably higher than the capsule (~10%). When the capsule and tablet were administered with food, the amount absorbed from the capsule was about 80% of the amount absorbed from the tablet Label. It is therefore advisable to take this drug with food for increased absorption, especially in tablet form.
- Volume of distribution
Extensively distributed throughout the body. The average steady-state volume of distribution is 2.4 L/kg Label.
- Protein binding
About 30% bound to plasma proteins Label.
- Metabolism
About 95% of the ingested dose of tizanidine is metabolized. The main enzyme involved in the hepatic metabolism of tizanidine is CYP1A2 Label.
Hover over products below to view reaction partners
- Route of elimination
This drug is mainly eliminated by the kidney Label.
- Half-life
Approximately 2.5 hours Label.
- Clearance
A note on renal impairment
Tizanidine clearance is found to be decreased by more than 50% in elderly patients with renal insufficiency (creatinine clearance < 25 mL/min) compared to healthy elderly subjects; this would be expected to lead to a longer duration of clinical effect. This drug should be used with caution in patients with renal impairment Label.
- Adverse Effects
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- Toxicity
LD50 information
Oral LD50 (rat): 414 mg/kg; Subcutaneous LD50 (rat): 282 mg/kg; Oral LD50 (mouse): 235 mg/kg MSDS
Use in pregnancy
Animal studies have determined that this drug causes fetal harm Label. Studies have not been performed in humans, and it is advisable to ensure that tizanidine use in pregnant women should be reserved for cases in which possible benefit clearly outweighs the possible risk to mother and unborn child 11.
Use in breastfeeding
In studies of rat models, this tizanidine was found excreted in the breastmilk with a milk-to-blood ratio of 1.8:1 Label. In young nursing rats, abnormal results were obtained in tests indicative of central nervous system function. Various developmental changes that may have been attributable to the drug were observed. It is unknown whether tizanidine is excreted in human milk. It is a lipid-soluble drug, however, and likely to be excreted into breast milk 11.
Carcinogenesis and mutagenesis
No signs of carcinogenicity were observed in two dietary studies performed in rodent models. Tizanidine was given to mice for 78 weeks at doses reaching a maximum 16 mg/kg (equivalent to twice the maximum recommended human dose). In addition, the drug was given to rats for 104 weeks at doses reaching 9 mg/kg (equivalent to 2.5 times the maximum recommended human dose). There was a lack of a statistically significant increase in the occurrence of tumors in either study group 11.
Tizanidine was not found to be mutagenic or clastogenic in several laboratory essays, including the bacterial Ames test, the mammalian gene mutation test, in addition to the chromosomal aberration test in Chinese hamster cells and several other assays 11.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Tizanidine is combined with 1,2-Benzodiazepine. Abaloparatide The risk or severity of adverse effects can be increased when Tizanidine is combined with Abaloparatide. Abametapir The serum concentration of Tizanidine can be increased when it is combined with Abametapir. Abatacept The metabolism of Tizanidine can be increased when combined with Abatacept. Abiraterone The serum concentration of Tizanidine can be increased when it is combined with Abiraterone. - Food Interactions
- Avoid alcohol.
- Take with or without food. Maintain the same schedule with regard to meals, as concentrations increase in the fasted state and decrease in the fed state.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Tizanidine hydrochloride B53E3NMY5C 64461-82-1 ZWUKMNZJRDGCTQ-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Cimbrar (Euroetika) / Musant (Actavis) / Myores (Meprofarm) / Navizan (Caber) / Relaxkov (Blaskov) / Sirdalid (Novartis) / Sirdalud (Novartis) / Sirdalud MR (Novartis) / Sizolan (Dr. Reddy's) / Spaslax (Panion & BF) / Telzanine (Nisshin Seiyaku) / Ternelin (Novartis) / Tizadin (ACL) / Tizaflex (Actavis) / Tizalud (Opsonin) / Tizan (Sun) / Zanpeak (Tatsumi Kagaku) / Zitanid (Novell)
- Brand Name Prescription Products
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-tizanidine Tablet 4 mg Oral Apotex Corporation 2004-11-17 Not applicable Canada Apo-tizanidine Tablet 2 mg Oral Apotex Corporation Not applicable Not applicable Canada Comfort Pac with Tizanidine Kit; Tablet 4 mg/1 Oral PD-Rx Pharmaceuticals, Inc. 2013-07-09 2018-12-17 US Mint-tizanidine Tablet 4 mg Oral Mint Pharmaceuticals Inc 2023-09-07 Not applicable Canada Mylan-tizanidine Tablet 4 mg Oral Mylan Pharmaceuticals 2006-02-16 2017-01-09 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ALGI - B® TABLETAS Tizanidine hydrochloride (2 mg) + Acetaminophen (325 mg) Tablet, coated Oral 2010-05-27 Not applicable Colombia FLECTADOL CAPSULAS Tizanidine hydrochloride (2 mg) + Ibuprofen (400 mg) Capsule, coated Oral C.I. FARMACAPSULAS S.A.S. - PLANTA NO. 2 2006-11-10 2015-09-03 Colombia MIALGILOX Tizanidine (2 mg) + Ibuprofen (400 mg) Capsule, coated Oral SEVERIANO FERNÁNDEZS.A.S 2017-12-01 Not applicable Colombia MYOS -NOR F TABLETAS Tizanidine hydrochloride (2 mg) + Ibuprofen (200 mg) Tablet, coated Oral BLISTECO S.A.S. 2008-11-07 Not applicable Colombia TIZAFEN® TABLETA RECUBIERTA Tizanidine hydrochloride (2 mg) + Acetaminophen (350 mg) Tablet, coated Oral LABORATORIOSSIEGFRIED S.A.S 2006-11-10 Not applicable Colombia
Categories
- ATC Codes
- M03BX02 — Tizanidine
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic alpha-2 Receptor Agonists
- Adrenergic alpha-Agonists
- Agents producing tachycardia
- Analgesics
- Anticonvulsants
- Autonomic Agents
- Bradycardia-Causing Agents
- Central alpha-2 Adrenergic Agonist
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Hypotensive Agents
- Imidazoles
- Imidazolines
- Muscle Relaxants
- Muscle Relaxants, Centrally Acting Agents
- Musculo-Skeletal System
- Narrow Therapeutic Index Drugs
- Neuromuscular Agents
- Neurotransmitter Agents
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Sensory System Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzothiadiazoles. These are heterocyclic aromatic compounds containing a benzene ring fused to a thiadiazole ring. Thiadiazole is a five-membered aromatic heterocycle made up of one sulfur atom and two nitrogen atoms.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzothiadiazoles
- Sub Class
- Not Available
- Direct Parent
- Benzothiadiazoles
- Alternative Parents
- Benzenoids / Aryl chlorides / Thiadiazoles / Imidazolines / Heteroaromatic compounds / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Organopnictogen compounds show 2 more
- Substituents
- 2,1,3-benzothiadiazole / 2-imidazoline / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Azole / Benzenoid / Carboximidamide / Guanidine show 10 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- imidazoles, benzothiadiazole (CHEBI:63629)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6AI06C00GW
- CAS number
- 51322-75-9
- InChI Key
- XFYDIVBRZNQMJC-UHFFFAOYSA-N
- 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)
- IUPAC Name
- 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
- SMILES
- ClC1=C(NC2=NCCN2)C2=NSN=C2C=C1
References
- Synthesis Reference
Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny, "METHOD FOR THE PREPARATION OF TIZANIDINE HYDROCHLORIDE." U.S. Patent US20110263863, issued October 27, 2011.
US20110263863- General References
- Henney HR 3rd, Runyan JD: A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients. Int J Clin Pract. 2008 Feb;62(2):314-24. doi: 10.1111/j.1742-1241.2007.01660.x. [Article]
- Malanga G, Reiter RD, Garay E: Update on tizanidine for muscle spasticity and emerging indications. Expert Opin Pharmacother. 2008 Aug;9(12):2209-15. doi: 10.1517/14656566.9.12.2209 . [Article]
- 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. [Article]
- Mathias CJ, Luckitt J, Desai P, Baker H, el Masri W, Frankel HL: Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury. J Rehabil Res Dev. 1989 Fall;26(4):9-16. [Article]
- Mense S: Muscle pain: mechanisms and clinical significance. Dtsch Arztebl Int. 2008 Mar;105(12):214-9. doi: 10.3238/artzebl.2008.0214. Epub 2008 Mar 21. [Article]
- Taittonen M, Raty H, Kirvela O, Aantaa R, Kanto J: The metabolic effects of oral tizanidine in healthy volunteers. Acta Anaesthesiol Scand. 1995 Jul;39(5):628-32. [Article]
- Chang E, Ghosh N, Yanni D, Lee S, Alexandru D, Mozaffar T: A Review of Spasticity Treatments: Pharmacological and Interventional Approaches. Crit Rev Phys Rehabil Med. 2013;25(1-2):11-22. doi: 10.1615/CritRevPhysRehabilMed.2013007945. [Article]
- Suarez-Lledo A, Padulles A, Lozano T, Cobo-Sacristan S, Colls M, Jodar R: Management of Tizanidine Withdrawal Syndrome: A Case Report. Clin Med Insights Case Rep. 2018 Feb 13;11:1179547618758022. doi: 10.1177/1179547618758022. eCollection 2018. [Article]
- Shirin Ghanavatian; Armen Derian (2019). Tizanidine. StatPearls.
- Reflexes: Components of a Reflex Arc [Link]
- Canadian monograph, Tizanidine [File]
- External Links
- Human Metabolome Database
- HMDB0014835
- KEGG Compound
- C07452
- PubChem Compound
- 5487
- PubChem Substance
- 46505373
- ChemSpider
- 5287
- BindingDB
- 50240671
- 57258
- ChEBI
- 63629
- ChEMBL
- CHEMBL1079
- ZINC
- ZINC000019702309
- Therapeutic Targets Database
- DAP000234
- PharmGKB
- PA451701
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Tizanidine
- FDA label
- Download (329 KB)
- MSDS
- Download (24.2 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Back Pain Lower Back 1 4 Completed Treatment Thyroidectomy 1 4 Completed Treatment Unilateral Inguinal Hernia 1 4 Completed Treatment Upper Limb Spasticity 1 4 Recruiting Treatment Shoulder Arthropathy / Shoulder Pain 1
Pharmacoeconomics
- Manufacturers
- 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
- Packagers
- Acorda Therapeutics
- Aidarex Pharmacuticals LLC
- Alphapharm Party Ltd.
- Altura Pharmaceuticals Inc.
- Amerisource Health Services Corp.
- Amneal Pharmaceuticals
- Apotex Inc.
- A-S Medication Solutions LLC
- Bryant Ranch Prepack
- Caraco Pharmaceutical Labs
- Cardinal Health
- Corepharma LLC
- Deca Pharmaceuticals LLC
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Elan Pharmaceuticals Inc.
- Eon Labs
- Genpharm LP
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Ivax Pharmaceuticals
- Keltman Pharmaceuticals Inc.
- Lake Erie Medical and Surgical Supply
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patheon Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepak Systems Inc.
- Rebel Distributors Corp.
- Redpharm Drug
- Resource Optimization and Innovation LLC
- Southwood Pharmaceuticals
- St Mary's Medical Park Pharmacy
- Stat Rx Usa
- Torpharm Inc.
- UDL Laboratories
- Vangard Labs Inc.
- Dosage Forms
Form Route Strength Tablet, coated Oral Capsule, extended release Oral 6 mg Kit; tablet Oral 4 mg/1 Capsule Oral 15.000 mg Solution / drops Tablet Oral 400000 mg Capsule, coated Oral Tablet Oral 0.002 g Tablet, film coated Oral 4 mg Tablet, film coated Oral 400000 mg Solution / drops; tablet Ophthalmic Capsule, delayed release 6 mg Tablet Oral 2.288 mg Tablet Oral Tablet Oral 6 MG Capsule Oral 6 mg Tablet Oral 200000 mg Tablet Oral 2 mg/1 Capsule Oral 2 mg/1 Capsule, gelatin coated Oral 2 mg/1 Capsule, gelatin coated Oral 6 mg/1 Tablet Oral 4 mg/1 Tablet, film coated Oral Capsule Oral 4 mg/1 Capsule Oral 6 mg/1 Capsule, gelatin coated Oral 4 mg/1 Tablet Oral 2 mg Tablet Oral 4 mg - Prices
Unit description Cost Unit Zanaflex 6 mg capsule 4.79USD capsule Zanaflex 4 mg capsule 3.2USD capsule Zanaflex 2 mg capsule 2.52USD capsule Zanaflex 4 mg tablet 2.29USD tablet Tizanidine hcl 4 mg tablet 1.49USD tablet Zanaflex 2 mg tablet 1.42USD tablet Tizanidine hcl 2 mg tablet 1.25USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6455557 No 2002-09-24 2021-11-28 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 280 https://www.lookchem.com/Tizanidine-hydrochloride/ boiling point (°C) 391.2 https://www.lookchem.com/Tizanidine/ water solubility slightly soluble FDA label logP 1.72 https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1079/ pKa 7.48 https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1079/ - Predicted Properties
Property Value Source Water Solubility 0.133 mg/mL 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 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 64.77 m3·mol-1 Chemaxon Polarizability 23.97 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.8592 Caco-2 permeable + 0.5323 P-glycoprotein substrate Substrate 0.6545 P-glycoprotein inhibitor I Non-inhibitor 0.8365 P-glycoprotein inhibitor II Non-inhibitor 0.7953 Renal organic cation transporter Inhibitor 0.6577 CYP450 2C9 substrate Non-substrate 0.7953 CYP450 2D6 substrate Non-substrate 0.8018 CYP450 3A4 substrate Non-substrate 0.5795 CYP450 1A2 substrate Non-inhibitor 0.5248 CYP450 2C9 inhibitor Non-inhibitor 0.7117 CYP450 2D6 inhibitor Non-inhibitor 0.7867 CYP450 2C19 inhibitor Non-inhibitor 0.6353 CYP450 3A4 inhibitor Non-inhibitor 0.781 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5 Ames test Non AMES toxic 0.6538 Carcinogenicity Non-carcinogens 0.8915 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6573 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6935 hERG inhibition (predictor II) Non-inhibitor 0.8907
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 147.6872461 predictedDarkChem Lite v0.1.0 [M-H]- 147.9733461 predictedDarkChem Lite v0.1.0 [M-H]- 144.97597 predictedDeepCCS 1.0 (2019) [M+H]+ 148.6281461 predictedDarkChem Lite v0.1.0 [M+H]+ 148.5304461 predictedDarkChem Lite v0.1.0 [M+H]+ 147.37154 predictedDeepCCS 1.0 (2019) [M+Na]+ 148.0153461 predictedDarkChem Lite v0.1.0 [M+Na]+ 147.7531461 predictedDarkChem Lite v0.1.0 [M+Na]+ 153.41367 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Agonist
- General Function
- Phosphatidylinositol binding
- Specific Function
- Acts either as the functional imidazoline-1 receptor (I1R) candidate or as a membrane-associated mediator of the I1R signaling. Binds numerous imidazoline ligands that induces initiation of cell-si...
- Gene Name
- NISCH
- Uniprot ID
- Q9Y2I1
- Uniprot Name
- Nischarin
- Molecular Weight
- 166627.105 Da
References
- Tanabe M, Hashimoto M, Ono H: Imidazoline I(1) receptor-mediated reduction of muscle rigidity in the reserpine-treated murine model of Parkinson's disease. Eur J Pharmacol. 2008 Jul 28;589(1-3):102-5. doi: 10.1016/j.ejphar.2008.06.013. Epub 2008 Jun 7. [Article]
- Talakoub R, Abbasi S, Maghami E, Zavareh SM: The effect of oral tizanidine on postoperative pain relief after elective laparoscopic cholecystectomy. Adv Biomed Res. 2016 Feb 8;5:19. doi: 10.4103/2277-9175.175905. eCollection 2016. [Article]
- Canadian monograph, Tizanidine [File]
- FDA label, Zanaflex [File]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Components:
Name | UniProt ID |
---|---|
Alpha-1A adrenergic receptor | P35348 |
Alpha-1B adrenergic receptor | P35368 |
Alpha-1D adrenergic receptor | P25100 |
References
- Takayanagi I, Konno F, Ishii C, Takemasa T, Yanagida Y, Shimizu M, Mori H, Sugane H: Actions of tizanidine on alpha 1-and alpha 2-adrenoceptors in the peripheral tissues. Gen Pharmacol. 1984;15(3):239-41. [Article]
- Takayanagi I, Harada M, Koike K, Satoh M: Differences in alpha 1-adrenoceptor mechanisms for phenylephrine and tizanidine in rabbit thoracic aorta and common iliac artery. Can J Physiol Pharmacol. 1991 Dec;69(12):1819-24. [Article]
- Shirin Ghanavatian; Armen Derian (2019). Tizanidine. StatPearls.
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Components:
Name | UniProt ID |
---|---|
Alpha-2A adrenergic receptor | P08913 |
Alpha-2B adrenergic receptor | P18089 |
Alpha-2C adrenergic receptor | P18825 |
References
- Piletz JE, Zhu H, Chikkala DN: Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J Pharmacol Exp Ther. 1996 Nov;279(2):694-702. [Article]
- Giovannitti JA Jr, Thoms SM, Crawford JJ: Alpha-2 adrenergic receptor agonists: a review of current clinical applications. Anesth Prog. 2015 Spring;62(1):31-9. doi: 10.2344/0003-3006-62.1.31. [Article]
- Leiphart JW, Dills CV, Levy RM: Alpha2-adrenergic receptor subtype specificity of intrathecally administered tizanidine used for analgesia for neuropathic pain. J Neurosurg. 2004 Oct;101(4):641-7. doi: 10.3171/jns.2004.101.4.0641. [Article]
- Fairbanks CA, Stone LS, Wilcox GL: Pharmacological profiles of alpha 2 adrenergic receptor agonists identified using genetically altered mice and isobolographic analysis. Pharmacol Ther. 2009 Aug;123(2):224-38. doi: 10.1016/j.pharmthera.2009.04.001. Epub 2009 Apr 23. [Article]
- Zanaflex FDA label [File]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [Article]
- Shellenberger MK, Groves L, Shah J, Novack GD: A controlled pharmacokinetic evaluation of tizanidine and baclofen at steady state. Drug Metab Dispos. 1999 Feb;27(2):201-4. [Article]
- Karjalainen MJ, Neuvonen PJ, Backman JT: Rofecoxib is a potent, metabolism-dependent inhibitor of CYP1A2: implications for in vitro prediction of drug interactions. Drug Metab Dispos. 2006 Dec;34(12):2091-6. doi: 10.1124/dmd.106.011965. Epub 2006 Sep 19. [Article]
- Flockhart Table of Drug Interactions [Link]
- Tizanidine FDA label [File]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54