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Identification
NameTizanidine
Accession NumberDB00697  (APRD00128)
TypeSmall Molecule
GroupsApproved
Description

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.

Structure
Thumb
Synonyms
5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
Tizanidin
Tizanidina
Tizanidine
Tizanidinum
External Identifiers
  • AN 021
  • DS 103-282
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mylan-tizanidinetablet4 mgoralMylan Pharmaceuticals Ulc2006-02-16Not applicableCanada
Pal-tizanidinetablet4 mgoralPaladin Labs Inc1999-10-29Not applicableCanada
Tizanidinetablet4 mgoralAa Pharma Inc2004-11-17Not applicableCanada
Tizanidinetablet2 mgoralAa Pharma IncNot applicableNot applicableCanada
Tizanidine Hydrochloridecapsule, gelatin coated2 mg/1oralActavis Pharma, Inc.2012-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated6 mg/1oralbryant ranch prepack2012-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated6 mg/1oralActavis Pharma, Inc.2012-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated2 mg/1oralClinical Solutions Wholesale2012-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated4 mg/1oralActavis Pharma, Inc.2012-02-06Not applicableUs
Zanaflextablet4 mg/1oralPd Rx Pharmaceuticals, Inc.1997-01-01Not applicableUs
Zanaflexcapsule6 mg/1oralAcorda Therapeutics, Inc.2005-04-04Not applicableUs
Zanaflexcapsule6 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-28Not applicableUs
Zanaflexcapsule4 mg/1oralAcorda Therapeutics, Inc.2005-04-04Not applicableUs
Zanaflexcapsule4 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-28Not applicableUs
Zanaflexcapsule2 mg/1oralAcorda Therapeutics, Inc.2005-04-04Not applicableUs
Zanaflexcapsule2 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-28Not applicableUs
Zanaflextablet4 mg/1oralAcorda Therapeutics, Inc.1997-01-01Not applicableUs
Zanaflexcapsule, gelatin coated4 mg/1oralRebel Distributors Corp2002-08-29Not applicableUs
Zanaflexcapsule4 mg/1oralSTAT Rx USA LLC2002-08-29Not applicableUs
Zanaflexcapsule6 mg/1oralSTAT Rx USA LLC2002-08-29Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Comfort Pac With TizanidinekitPd Rx Pharmaceuticals, Inc.2013-07-09Not applicableUs
Tizanidinetablet2 mg/1oralBlenheim Pharmacal, Inc.2014-04-08Not applicableUs
Tizanidinetablet4 mg/1oralREMEDYREPACK INC.2013-02-19Not applicableUs
Tizanidinetablet4 mg/1oralSun Pharmaceutical Industries, Inc.2003-12-11Not applicableUs
Tizanidinetablet2 mg/1oralDIRECT RX2014-01-01Not applicableUs
Tizanidinetablet2 mg/1oralPreferred Pharmaceuticals, Inc2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralREMEDYREPACK INC.2013-05-23Not applicableUs
Tizanidinetablet2 mg/1oralSTAT Rx USA LLC2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralProficient Rx LP2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralPreferred Pharmaceuticals, Inc.2014-03-26Not applicableUs
Tizanidinetablet2 mg/1oralMedsource Pharmaceuticals2009-01-05Not applicableUs
Tizanidinetablet4 mg/1oralDr. Reddy's Laboratories Limited2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralAidarex Pharmaceuticals LLC2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralCore Pharma, Llc2007-02-06Not applicableUs
Tizanidinetablet4 mg/1oralMylan Institutional Inc.2003-06-15Not applicableUs
Tizanidinetablet2 mg/1oralSun Pharmaceutical Industries, Inc.2003-12-11Not applicableUs
Tizanidinetablet2 mg/1oralBlenheim Pharmacal, Inc.2014-01-13Not applicableUs
Tizanidinetablet4 mg/1oralMedsource Pharmaceuticals2008-12-08Not applicableUs
Tizanidinetablet2 mg/1oralDr. Reddy's Laboratories Limited2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralUnichem Pharmaceuticals (USA), Inc.2013-04-01Not applicableUs
Tizanidinetablet4 mg/1oralApotex Corp.2004-01-16Not applicableUs
Tizanidinetablet2 mg/1oralAltura Pharmaceuticals, Inc.2010-01-01Not applicableUs
Tizanidinetablet4 mg/1oralProficient Rx LP2003-12-11Not applicableUs
Tizanidinetablet2 mg/1oralREMEDYREPACK INC.2015-12-16Not applicableUs
Tizanidinetablet4 mg/1oralBlenheim Pharmacal, Inc.2014-01-22Not applicableUs
Tizanidinetablet4 mg/1oralUnit Dose Services2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralPd Rx Pharmaceuticals, Inc.2002-11-26Not applicableUs
Tizanidinetablet2 mg/1oralApotex Corp.2004-01-16Not applicableUs
Tizanidinetablet2 mg/1oralbryant ranch prepack2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralPreferred Pharmaceuticals Inc.2016-03-16Not applicableUs
Tizanidinetablet2 mg/1oralAphena Pharma Solutions Tennessee, Llc2003-05-06Not applicableUs
Tizanidinetablet2 mg/1oralPhysicians Total Care, Inc.2004-03-03Not applicableUs
Tizanidinetablet2 mg/1oralUnichem Pharmaceuticals (USA), Inc.2013-04-01Not applicableUs
Tizanidinetablet2 mg/1oralREMEDYREPACK INC.2015-09-03Not applicableUs
Tizanidinetablet2 mg/1oralAmerican Health Packaging2014-06-02Not applicableUs
Tizanidinetablet4.576 mg/1oralMajor Pharmaceuticals2014-10-01Not applicableUs
Tizanidinetablet2 mg/1oralUnit Dose Services2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralAv Kare, Inc.2015-07-23Not applicableUs
Tizanidinetablet4 mg/1oralGolden State Medical Supply, Inc.2004-01-16Not applicableUs
Tizanidinetablet4 mg/1oralbryant ranch prepack2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralMylan Pharmaceuticals Inc.2003-05-06Not applicableUs
Tizanidinetablet4 mg/1oralAphena Pharma Solutions Tennessee, Llc2003-05-06Not applicableUs
Tizanidinetablet4 mg/1oralPhysicians Total Care, Inc.2004-01-19Not applicableUs
Tizanidinetablet2 mg/1oralSt. Mary's Medical Park Pharmacy2015-08-18Not applicableUs
Tizanidinetablet4 mg/1oralAmerican Health Packaging2013-09-25Not applicableUs
Tizanidinetablet2 mg/1oralCardinal Health2013-03-21Not applicableUs
Tizanidinetablet2 mg/1oralAv Kare, Inc.2015-07-23Not applicableUs
Tizanidinetablet2 mg/1oralGolden State Medical Supply, Inc.2004-01-16Not applicableUs
Tizanidinetablet4 mg/1oralProficient Rx LP2013-04-01Not applicableUs
Tizanidinetablet4 mg/1oralMc Kesson Contract Packaging2012-02-23Not applicableUs
Tizanidinetablet2 mg/1oralMylan Pharmaceuticals Inc.2003-05-06Not applicableUs
Tizanidinetablet4 mg/1oralPd Rx Pharmaceuticals, Inc.2012-07-24Not applicableUs
Tizanidinetablet2 mg/1oralH.J. Harkins Company, Inc.2002-07-03Not applicableUs
Tizanidinetablet2 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralCardinal Health2011-01-28Not applicableUs
Tizanidinetablet4 mg/1oralDispensing Solutions, Inc.2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralBlenheim Pharmacal, Inc.2014-12-18Not applicableUs
Tizanidinetablet2 mg/1oralREMEDYREPACK INC.2013-05-15Not applicableUs
Tizanidinetablet2 mg/1oralClinical Solutions Wholesale2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralDIRECT RX2014-01-01Not applicableUs
Tizanidinetablet4 mg/1oralPreferred Pharmaceuticals, Inc2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
Tizanidinetablet4 mg/1oralProficient Rx LP2004-01-16Not applicableUs
Tizanidinetablet4 mg/1oralPreferred Pharmaceuticals, Inc.2014-03-05Not applicableUs
Tizanidinetablet4 mg/1oralH.J. Harkins Company, Inc.2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralSTAT Rx USA LLC2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralREMEDYREPACK INC.2014-11-21Not applicableUs
Tizanidinetablet4 mg/1oralCardinal Health2002-07-032016-03-22Us
Tizanidinetablet4 mg/1oralAidarex Pharmaceuticals LLC2002-07-03Not applicableUs
Tizanidinetablet4 mg/1oralCore Pharma, Llc2007-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated6 mg/1oralAv Kare, Inc.2014-06-20Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralEon Labs, Inc.2002-11-26Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralSTAT Rx USA LLC2002-06-27Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralClinical Solutions Wholesale2002-06-27Not applicableUs
Tizanidine Hydrochloridecapsule6 mg/1oralMylan Pharmaceuticals Inc.2013-03-01Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated2 mg/1oralApotex Corp.2012-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated4 mg/1oralAv Kare, Inc.2014-06-20Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralTIZANIDINE HYDROCHLORIDE2014-01-01Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralKeltman Pharmaceuticals Inc.2005-06-01Not applicableUs
Tizanidine Hydrochloridecapsule4 mg/1oralMylan Pharmaceuticals Inc.2013-03-01Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralKeltman Pharmaceuticals Inc.2005-06-01Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated2 mg/1oralAv Kare, Inc.2014-06-20Not applicableUs
Tizanidine Hydrochloridecapsule2 mg/1oralMylan Pharmaceuticals Inc.2013-03-01Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralPd Rx Pharmaceuticals, Inc.2002-06-27Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralAmerican Health Packaging2013-07-082015-12-29Us
Tizanidine Hydrochloridetablet4 mg/1oralRebel Distributors2007-02-06Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralMajor Pharmaceuticals2010-07-16Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-04-20Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralRebel Distributors2007-02-06Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-23Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-02-06Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated6 mg/1oralApotex Corp.2012-02-06Not applicableUs
Tizanidine Hydrochloridetablet2 mg/1oralSTAT Rx USA LLC2002-11-26Not applicableUs
Tizanidine Hydrochloridetablet4 mg/1oralEon Labs, Inc.2002-06-27Not applicableUs
Tizanidine Hydrochloridecapsule, gelatin coated4 mg/1oralApotex Corp.2012-02-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CimbrarEuroetika
MusantActavis
MyoresMeprofarm
NavizanCaber
RelaxkovBlaskov
SirdalidNovartis
SirdaludNovartis
Sirdalud MRNovartis
SizolanDr. Reddy's
SpaslaxPanion & BF
TelzanineNisshin Seiyaku
TernelinNovartis
TizadinACL
TizaflexActavis
TizaludOpsonin
TizanSun
ZanpeakTatsumi Kagaku
ZitanidNovell
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tizanidine Hydrochloride
Thumb
  • InChI Key: ZWUKMNZJRDGCTQ-UHFFFAOYSA-N
  • Monoisotopic Mass: 288.995571417
  • Average Mass: 290.172
DBSALT000550
Categories
UNII6AI06C00GW
CAS number51322-75-9
WeightAverage: 253.711
Monoisotopic: 253.018893678
Chemical FormulaC9H8ClN5S
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiadiazoles
Sub ClassNot Available
Direct ParentBenzothiadiazoles
Alternative Parents
Substituents
  • 2,1,3-benzothiadiazole
  • Benzenoid
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Thiadiazole
  • 2-imidazoline
  • Azole
  • Guanidine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of increased muscle tone associated with spasticity
PharmacodynamicsTizanidine 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 actionTizanidine reduces spasticity by increasing presynaptic inhibition of motor neurons through agonist action at a2-adrenergic receptor sites.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 2.4 L/kg
Protein binding30%
Metabolism
SubstrateEnzymesProduct
Tizanidine
5-chloro-4-(guanidino)-2,1,3-benzothiadiazoleDetails
Tizanidine
5-chloro-4-(2-imidazolin-4-on-2-ylamino)-2,1,3-benzothiadiazoleDetails
Route of eliminationApproximately 95% of an administered dose is metabolized.
Half life2.5 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8592
Caco-2 permeable+0.5323
P-glycoprotein substrateSubstrate0.6545
P-glycoprotein inhibitor INon-inhibitor0.8365
P-glycoprotein inhibitor IINon-inhibitor0.7953
Renal organic cation transporterInhibitor0.6577
CYP450 2C9 substrateNon-substrate0.7953
CYP450 2D6 substrateNon-substrate0.8018
CYP450 3A4 substrateNon-substrate0.5795
CYP450 1A2 substrateNon-inhibitor0.5248
CYP450 2C9 inhibitorNon-inhibitor0.7117
CYP450 2D6 inhibitorNon-inhibitor0.7867
CYP450 2C19 inhibitorNon-inhibitor0.6353
CYP450 3A4 inhibitorNon-inhibitor0.781
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5
Ames testNon AMES toxic0.6538
CarcinogenicityNon-carcinogens0.8915
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6573 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6935
hERG inhibition (predictor II)Non-inhibitor0.8907
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
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
Dosage forms
FormRouteStrength
Kit
Tabletoral4 mg
Tabletoral2 mg
Tabletoral4.576 mg/1
Capsuleoral2 mg/1
Capsuleoral4 mg/1
Capsuleoral6 mg/1
Capsule, gelatin coatedoral2 mg/1
Capsule, gelatin coatedoral4 mg/1
Capsule, gelatin coatedoral6 mg/1
Tabletoral2 mg/1
Tabletoral4 mg/1
Prices
Unit descriptionCostUnit
Zanaflex 6 mg capsule4.79USD capsule
Zanaflex 4 mg capsule3.2USD capsule
Zanaflex 2 mg capsule2.52USD capsule
Zanaflex 4 mg tablet2.29USD tablet
Tizanidine hcl 4 mg tablet1.49USD tablet
Zanaflex 2 mg tablet1.42USD tablet
Tizanidine hcl 2 mg tablet1.25USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6455557 No2001-11-282021-11-28Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.133 mg/mLALOGPS
logP1.6ALOGPS
logP2.02ChemAxon
logS-3.3ALOGPS
pKa (Strongest Basic)7.49ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area62.2 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity64.77 m3·mol-1ChemAxon
Polarizability23.97 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0udi-5490000000-5ee0610f321160b63c82View in MoNA
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 ReferencesNot Available
External Links
ATC CodesM03BX02
AHFS Codes
  • 12:20.00
PDB EntriesNot Available
FDA labelDownload (145 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Tizanidine can be increased when it is combined with Abiraterone.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Tizanidine.
AminophyllineThe serum concentration of Tizanidine can be increased when it is combined with Aminophylline.
AmiodaroneThe serum concentration of Tizanidine can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Tizanidine can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Tizanidine can be increased when it is combined with Amlodipine.
AnastrozoleThe serum concentration of Tizanidine can be increased when it is combined with Anastrozole.
ApomorphineThe serum concentration of Tizanidine can be increased when it is combined with Apomorphine.
AtazanavirThe serum concentration of Tizanidine can be increased when it is combined with Atazanavir.
AzelastineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzithromycinThe serum concentration of Tizanidine can be increased when it is combined with Azithromycin.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Tizanidine.
BenazeprilTizanidine may increase the hypotensive activities of Benazepril.
BortezomibThe serum concentration of Tizanidine can be increased when it is combined with Bortezomib.
BretyliumBretylium may increase the bradycardic activities of Tizanidine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
BromocriptineThe serum concentration of Tizanidine can be increased when it is combined with Bromocriptine.
BuprenorphineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalButabarbital may increase the hypotensive activities of Tizanidine.
ButethalButethal may increase the hypotensive activities of Tizanidine.
CaffeineThe serum concentration of Tizanidine can be increased when it is combined with Caffeine.
CaptoprilTizanidine may increase the hypotensive activities of Captopril.
CeritinibTizanidine may increase the bradycardic activities of Ceritinib.
CilazaprilTizanidine may increase the hypotensive activities of Cilazapril.
CimetidineThe serum concentration of Tizanidine can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Tizanidine can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Tizanidine can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Tizanidine can be increased when it is combined with Clarithromycin.
ClotrimazoleThe serum concentration of Tizanidine can be increased when it is combined with Clotrimazole.
ClozapineThe serum concentration of Tizanidine can be increased when it is combined with Clozapine.
DeferasiroxThe serum concentration of Tizanidine can be increased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Tizanidine can be increased when it is combined with Delavirdine.
DexmedetomidineThe serum concentration of Tizanidine can be increased when it is combined with Dexmedetomidine.
DiclofenacThe serum concentration of Tizanidine can be increased when it is combined with Diclofenac.
DisulfiramThe serum concentration of Tizanidine can be increased when it is combined with Disulfiram.
DofetilideTizanidine may increase the QTc-prolonging activities of Dofetilide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
DuloxetineTizanidine may increase the orthostatic hypotensive activities of Duloxetine.
EnalaprilTizanidine may increase the hypotensive activities of Enalapril.
EnalaprilatTizanidine may increase the hypotensive activities of Enalaprilat.
EntacaponeThe serum concentration of Tizanidine can be increased when it is combined with Entacapone.
EsmololEsmolol may increase the bradycardic activities of Tizanidine.
EstradiolThe serum concentration of Tizanidine can be increased when it is combined with Estradiol.
EthanolTizanidine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FluconazoleThe serum concentration of Tizanidine can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Tizanidine can be increased when it is combined with Fluoxetine.
FluphenazineThe serum concentration of Tizanidine can be increased when it is combined with Fluphenazine.
FlutamideThe serum concentration of Tizanidine can be increased when it is combined with Flutamide.
FluvastatinThe serum concentration of Tizanidine can be increased when it is combined with Fluvastatin.
FluvoxamineThe serum concentration of Tizanidine can be increased when it is combined with Fluvoxamine.
FosinoprilTizanidine may increase the hypotensive activities of Fosinopril.
GemfibrozilThe serum concentration of Tizanidine can be increased when it is combined with Gemfibrozil.
Glycerol PhenylbutyrateThe serum concentration of Tizanidine can be increased when it is combined with Glycerol Phenylbutyrate.
GoserelinTizanidine may increase the QTc-prolonging activities of Goserelin.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Tizanidine.
HexobarbitalHexobarbital may increase the hypotensive activities of Tizanidine.
HydrocodoneTizanidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
ImipramineThe serum concentration of Tizanidine can be increased when it is combined with Imipramine.
Interferon gamma-1bThe serum concentration of Tizanidine can be increased when it is combined with Interferon gamma-1b.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Tizanidine.
IsoniazidThe serum concentration of Tizanidine can be increased when it is combined with Isoniazid.
IvabradineTizanidine may increase the bradycardic activities of Ivabradine.
KetoconazoleThe serum concentration of Tizanidine can be increased when it is combined with Ketoconazole.
LacosamideTizanidine may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LeuprolideTizanidine may increase the QTc-prolonging activities of Leuprolide.
LevodopaTizanidine may increase the orthostatic hypotensive activities of Levodopa.
LidocaineThe serum concentration of Tizanidine can be increased when it is combined with Lidocaine.
LisinoprilTizanidine may increase the hypotensive activities of Lisinopril.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Tizanidine.
LosartanThe serum concentration of Tizanidine can be increased when it is combined with Losartan.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
MefloquineThe therapeutic efficacy of Tizanidine can be decreased when used in combination with Mefloquine.
MethimazoleThe serum concentration of Tizanidine can be increased when it is combined with Methimazole.
MethohexitalMethohexital may increase the hypotensive activities of Tizanidine.
MethotrimeprazineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethoxsalenThe serum concentration of Tizanidine can be increased when it is combined with Methoxsalen.
MetyrosineTizanidine may increase the sedative activities of Metyrosine.
MexiletineThe serum concentration of Tizanidine can be increased when it is combined with Mexiletine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Tizanidine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
MirtazapineThe serum concentration of Tizanidine can be increased when it is combined with Mirtazapine.
MoclobemideThe serum concentration of Tizanidine can be increased when it is combined with Moclobemide.
MoexiprilTizanidine may increase the hypotensive activities of Moexipril.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
NadololTizanidine may increase the atrioventricular blocking (AV block) activities of Nadolol.
NefazodoneThe serum concentration of Tizanidine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Tizanidine can be increased when it is combined with Nelfinavir.
NevirapineThe serum concentration of Tizanidine can be increased when it is combined with Nevirapine.
NicorandilNicorandil may increase the hypotensive activities of Tizanidine.
NifedipineThe serum concentration of Tizanidine can be increased when it is combined with Nifedipine.
NisoldipineThe serum concentration of Tizanidine can be increased when it is combined with Nisoldipine.
NorfloxacinThe serum concentration of Tizanidine can be increased when it is combined with Norfloxacin.
OctreotideOctreotide may increase the bradycardic activities of Tizanidine.
OfloxacinThe serum concentration of Tizanidine can be increased when it is combined with Ofloxacin.
OlanzapineThe serum concentration of Tizanidine can be increased when it is combined with Olanzapine.
OmeprazoleThe serum concentration of Tizanidine can be increased when it is combined with Omeprazole.
OndansetronThe serum concentration of Tizanidine can be increased when it is combined with Ondansetron.
OrlistatThe serum concentration of Tizanidine can be decreased when it is combined with Orlistat.
OrphenadrineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeTizanidine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe serum concentration of Tizanidine can be increased when it is combined with Paroxetine.
Peginterferon alfa-2aThe serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2a.
Peginterferon alfa-2bThe serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2b.
PentobarbitalPentobarbital may increase the hypotensive activities of Tizanidine.
PentoxifyllineThe serum concentration of Tizanidine can be increased when it is combined with Pentoxifylline.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
PerindoprilTizanidine may increase the hypotensive activities of Perindopril.
PerphenazineThe serum concentration of Tizanidine can be increased when it is combined with Perphenazine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Tizanidine.
PramipexoleTizanidine may increase the sedative activities of Pramipexole.
PrimaquineThe serum concentration of Tizanidine can be increased when it is combined with Primaquine.
PrimidonePrimidone may increase the hypotensive activities of Tizanidine.
PropafenoneThe serum concentration of Tizanidine can be increased when it is combined with Propafenone.
PropofolThe serum concentration of Tizanidine can be increased when it is combined with Propofol.
PropranololThe serum concentration of Tizanidine can be increased when it is combined with Propranolol.
QuinaprilTizanidine may increase the hypotensive activities of Quinapril.
RamiprilTizanidine may increase the hypotensive activities of Ramipril.
RanitidineThe serum concentration of Tizanidine can be increased when it is combined with Ranitidine.
RisperidoneTizanidine may increase the hypotensive activities of Risperidone.
RopiniroleThe serum concentration of Tizanidine can be increased when it is combined with Ropinirole.
RotigotineTizanidine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tizanidine.
RuxolitinibRuxolitinib may increase the bradycardic activities of Tizanidine.
SecobarbitalSecobarbital may increase the hypotensive activities of Tizanidine.
SelegilineThe serum concentration of Tizanidine can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Tizanidine can be increased when it is combined with Sertraline.
SimeprevirThe serum concentration of Tizanidine can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Sodium phenylbutyrateThe serum concentration of Tizanidine can be increased when it is combined with Sodium phenylbutyrate.
StiripentolThe serum concentration of Tizanidine can be increased when it is combined with Stiripentol.
SulconazoleThe serum concentration of Tizanidine can be increased when it is combined with Sulconazole.
SuvorexantTizanidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
TenofovirThe serum concentration of Tizanidine can be increased when it is combined with Tenofovir.
ThalidomideTizanidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe serum concentration of Tizanidine can be increased when it is combined with Theophylline.
ThioridazineThe serum concentration of Tizanidine can be increased when it is combined with Thioridazine.
TiclopidineThe serum concentration of Tizanidine can be increased when it is combined with Ticlopidine.
TioconazoleThe serum concentration of Tizanidine can be increased when it is combined with Tioconazole.
TofacitinibTofacitinib may increase the bradycardic activities of Tizanidine.
TrandolaprilTizanidine may increase the hypotensive activities of Trandolapril.
TranylcypromineThe serum concentration of Tizanidine can be increased when it is combined with Tranylcypromine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Tizanidine.
VemurafenibThe serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Tizanidine.
VerapamilThe serum concentration of Tizanidine can be increased when it is combined with Verapamil.
ZafirlukastThe serum concentration of Tizanidine can be increased when it is combined with Zafirlukast.
ZileutonThe serum concentration of Tizanidine can be increased when it is combined with Zileuton.
ZolpidemTizanidine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. 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. [PubMed:8930173 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Epinephrine 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 clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. 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. [PubMed:8930173 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. 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. [PubMed:8930173 ]
Kind
Protein
Organism
Human
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-signaling cascades triggering to cell survival, growth and migration. Its activation by the agonist rilmenidine induces an increase in phosphorylation of mitogen-activated protein kinases MAPK1 and MAPK...
Gene Name:
NISCH
Uniprot ID:
Q9Y2I1
Molecular Weight:
166627.105 Da
References
  1. Rolon PA: Myxoglobulosis of the appendix. Int Surg. 1977 Jun-Jul;62(6-7):355-6. [PubMed:893017 ]

Enzymes

Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. 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. [PubMed:19754423 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. 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. [PubMed:9929503 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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Drug created on June 13, 2005 07:24 / Updated on January 09, 2014 11:38