tizanidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2683 51322-75-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • DS 103-282
  • tizanidine
  • tizanidine hydrochloride
  • tizanidine HCl
  • AN021
  • DS103-282
Tizanidine is an agonist at alpha2-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.
  • Molecular weight: 253.71
  • Formula: C9H8ClN5S
  • CLOGP: 2.32
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 62.20
  • ALOGS: -3.28
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
12 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 2.36 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 21 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.70 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.40 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 27, 1996 FDA ACORDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple sclerosis relapse 375.20 10.37 312 48822 44591 56198342
Pneumonia aspiration 237.59 10.37 209 48925 32202 56210731
Multiple sclerosis 168.12 10.37 161 48973 27641 56215292
Gastrooesophageal reflux disease 168.09 10.37 278 48856 82979 56159954
Somnolence 157.86 10.37 402 48732 163011 56079922
Completed suicide 148.15 10.37 347 48787 133486 56109447
Coma 146.51 10.37 218 48916 59437 56183496
Contraindicated product administered 124.95 10.37 10 49124 186276 56056657
Synovitis 122.74 10.37 4 49130 161301 56081632
Muscle spasms 114.44 10.37 320 48814 137051 56105882
Glossodynia 108.64 10.37 6 49128 152452 56090481
Depression 106.09 10.37 372 48762 179745 56063188
Hand deformity 103.52 10.37 3 49131 134489 56108444
Drug withdrawal syndrome 98.19 10.37 117 49017 25740 56217193
Migraine 98.10 10.37 227 48907 86570 56156363
Rheumatoid arthritis 97.92 10.37 114 49020 382490 55860443
Fall 94.82 10.37 584 48550 356926 55886007
Systemic lupus erythematosus 92.11 10.37 22 49112 180056 56062877
Maternal exposure during pregnancy 87.90 10.37 28 49106 189525 56053408
Drug intolerance 86.54 10.37 63 49071 264755 55978178
Pericarditis 78.48 10.37 4 49130 108919 56134014
Product dose omission issue 76.88 10.37 368 48766 204385 56038548
Treatment failure 75.81 10.37 27 49107 170365 56072568
Lower respiratory tract infection 74.66 10.37 7 49127 114787 56128146
Infusion related reaction 69.15 10.37 49 49085 208882 56034051
Hypoaesthesia 68.88 10.37 275 48859 141216 56101717
Urinary tract infection 64.33 10.37 394 48740 240119 56002814
Neutropenia 60.87 10.37 31 49103 158136 56084797
Suspected suicide 60.77 10.37 45 49089 5421 56237512
Joint swelling 59.46 10.37 101 49033 289699 55953234
Withdrawal syndrome 58.03 10.37 76 49058 18386 56224547
Gait disturbance 57.30 10.37 288 48846 163033 56079900
Exposure during pregnancy 56.67 10.37 24 49110 136318 56106615
Wound 52.23 10.37 28 49106 138776 56104157
Helicobacter infection 51.81 10.37 3 49131 73265 56169668
Neck pain 49.82 10.37 142 48992 61413 56181520
General physical health deterioration 49.81 10.37 45 49089 169965 56072968
Muscle spasticity 44.80 10.37 70 49064 19890 56223043
Autonomic dysreflexia 44.45 10.37 15 49119 318 56242615
Anxiety 41.65 10.37 300 48834 192872 56050061
Headache 41.02 10.37 700 48434 558344 55684589
Tremor 40.68 10.37 211 48923 120878 56122055
Febrile neutropenia 40.13 10.37 21 49113 105524 56137409
Thrombocytopenia 39.96 10.37 36 49098 136188 56106745
Stiff person syndrome 39.86 10.37 14 49120 336 56242597
Therapeutic product effect decreased 39.59 10.37 54 49080 169398 56073535
Memory impairment 39.52 10.37 165 48969 86392 56156541
Back pain 38.42 10.37 345 48789 236825 56006108
Folliculitis 36.69 10.37 3 49131 54976 56187957
Drug ineffective 36.58 10.37 574 48560 918415 55324518
Arthropathy 36.45 10.37 75 49059 200200 56042733
Off label use 35.39 10.37 313 48821 555867 55687066
Alopecia 34.83 10.37 135 48999 293323 55949610
Hypersensitivity 34.40 10.37 112 49022 256296 55986637
Muscular weakness 33.69 10.37 180 48954 104272 56138661
Feeling abnormal 33.24 10.37 215 48919 133387 56109546
Influenza like illness 32.46 10.37 122 49012 60866 56182067
Paraesthesia 32.45 10.37 210 48924 130304 56112629
Hepatic enzyme increased 32.19 10.37 63 49071 171321 56071612
Malignant neoplasm progression 32.13 10.37 12 49122 73575 56169358
Muscle injury 32.09 10.37 4 49130 52496 56190437
Pancytopenia 31.77 10.37 19 49115 88696 56154237
Sleep apnoea syndrome 31.45 10.37 70 49064 25991 56216942
Dysphoria 31.09 10.37 29 49105 4813 56238120
COVID-19 30.38 10.37 138 48996 74920 56168013
Rash 29.81 10.37 281 48853 492766 55750167
Vision blurred 29.57 10.37 147 48987 82796 56160137
Intervertebral disc protrusion 28.15 10.37 60 49074 21634 56221299
Insomnia 27.99 10.37 273 48861 191587 56051346
Product use issue 27.26 10.37 78 49056 185963 56056970
Sleep disorder due to general medical condition, insomnia type 27.24 10.37 3 49131 43335 56199598
Swelling 26.74 10.37 113 49021 239658 56003275
Therapy interrupted 26.73 10.37 65 49069 25560 56217373
Vitamin D deficiency 26.37 10.37 42 49092 12128 56230805
Spinal operation 25.83 10.37 32 49102 7324 56235609
Pain 25.02 10.37 756 48378 662428 55580505
Amnesia 24.93 10.37 93 49041 46229 56196704
Abdominal discomfort 24.41 10.37 142 48992 277132 55965801
Therapeutic response unexpected 24.30 10.37 49 49085 16995 56225938
C-reactive protein increased 24.03 10.37 20 49114 78664 56164269
Suicidal ideation 23.99 10.37 107 49027 57635 56185298
Cardiac failure 23.70 10.37 22 49112 82071 56160862
JC polyomavirus test positive 23.16 10.37 14 49120 1204 56241729
Neurogenic bladder 23.12 10.37 20 49114 3009 56239924
Blood pressure systolic increased 22.90 10.37 4 49130 40832 56202101
Hallucination 22.66 10.37 94 49040 49055 56193878
Visual impairment 22.66 10.37 126 49008 74076 56168857
Surgery 22.54 10.37 71 49063 32415 56210518
Pre-existing condition improved 22.54 10.37 30 49104 7368 56235565
Suspected product quality issue 22.32 10.37 8 49126 204 56242729
Respiratory arrest 22.24 10.37 68 49066 30557 56212376
Lumbar radiculopathy 22.15 10.37 16 49118 1855 56241078
Back disorder 22.05 10.37 35 49099 10078 56232855
Impaired healing 20.95 10.37 27 49107 86814 56156119
Balance disorder 20.80 10.37 126 49008 76394 56166539
Therapy cessation 20.23 10.37 61 49073 27203 56215730
Loss of consciousness 19.20 10.37 162 48972 109187 56133746
Intentional product misuse 18.86 10.37 92 49042 51412 56191521
Formication 18.53 10.37 20 49114 3950 56238983
Urinary incontinence 18.14 10.37 62 49072 29523 56213410
Nervousness 17.96 10.37 61 49073 28954 56213979
Cardio-respiratory arrest 17.60 10.37 95 49039 55226 56187707
Neuralgia 17.57 10.37 53 49081 23642 56219291
Progressive multiple sclerosis 17.54 10.37 10 49124 771 56242162
Mental status changes 17.51 10.37 72 49062 37429 56205504
Dizziness 17.28 10.37 440 48694 375700 55867233
Drug dependence 17.27 10.37 51 49083 22482 56220451
Decreased interest 17.20 10.37 17 49117 3029 56239904
Central nervous system lesion 17.16 10.37 31 49103 9907 56233026
Peroneal nerve palsy 16.62 10.37 20 49114 4441 56238492
Ankle fracture 16.46 10.37 41 49093 16362 56226571
Temperature intolerance 16.40 10.37 27 49107 8013 56234920
International normalised ratio increased 16.38 10.37 9 49125 44032 56198901
Blood creatinine increased 16.36 10.37 28 49106 80163 56162770
Asthenia 16.28 10.37 403 48731 342570 55900363
Dysarthria 16.21 10.37 73 49061 39477 56203456
Respiratory alkalosis 15.84 10.37 15 49119 2536 56240397
Intervertebral disc degeneration 15.77 10.37 37 49097 14217 56228716
Pyrexia 15.73 10.37 264 48870 418509 55824424
Discomfort 15.67 10.37 67 49067 141694 56101239
Underdose 15.64 10.37 51 49083 23706 56219227
Hyperhidrosis 15.27 10.37 137 48997 93951 56148982
Acute kidney injury 15.02 10.37 136 48998 240627 56002306
Impaired gastric emptying 14.87 10.37 28 49106 9235 56233698
Disease progression 14.74 10.37 45 49089 105128 56137805
Haemorrhagic diathesis 14.70 10.37 18 49116 4070 56238863
Nasopharyngitis 14.59 10.37 123 49011 220836 56022097
Secondary progressive multiple sclerosis 14.57 10.37 11 49123 1364 56241569
Gastrointestinal disorder 14.56 10.37 50 49084 112652 56130281
Panic attack 14.47 10.37 45 49089 20402 56222531
Cholestasis 14.32 10.37 3 49131 26910 56216023
Anaemia 14.24 10.37 157 48977 267354 55975579
Mucosal inflammation 14.19 10.37 10 49124 42800 56200133
Nausea 14.16 10.37 808 48326 763370 55479563
Head injury 14.05 10.37 51 49083 25015 56217918
Pneumonitis 14.02 10.37 5 49129 31559 56211374
Seizure 13.60 10.37 168 48966 124951 56117982
Thinking abnormal 13.48 10.37 28 49106 9913 56233020
Bone marrow failure 13.41 10.37 4 49130 28282 56214651
Appetite disorder 13.26 10.37 22 49112 6571 56236362
Device expulsion 13.23 10.37 5 49129 30444 56212489
Bronchitis 13.17 10.37 153 48981 112158 56130775
Hypertonia 13.10 10.37 17 49117 4075 56238858
Fibula fracture 12.97 10.37 15 49119 3195 56239738
Muscle tightness 12.95 10.37 29 49105 10807 56232126
Spinal fusion acquired 12.94 10.37 3 49131 14 56242919
Cervical spinal stenosis 12.92 10.37 12 49122 1980 56240953
Plasma cell myeloma 12.88 10.37 13 49121 46633 56196300
Diplopia 12.76 10.37 43 49091 20326 56222607
Spinal osteoarthritis 12.76 10.37 35 49099 14801 56228132
Disturbance in attention 12.55 10.37 59 49075 32481 56210452
Neutrophil count decreased 12.53 10.37 15 49119 49807 56193126
Loss of control of legs 12.48 10.37 10 49124 1353 56241580
Stress 12.38 10.37 91 49043 58819 56184114
Nerve compression 12.31 10.37 24 49110 8120 56234813
Spinal pain 12.24 10.37 30 49104 11854 56231079
Ascites 12.15 10.37 9 49125 37535 56205398
Hepatotoxicity 12.13 10.37 6 49128 31147 56211786
Hepatocellular injury 12.13 10.37 4 49130 26510 56216423
Multiple organ dysfunction syndrome 12.12 10.37 17 49117 52753 56190180
Hyperkalaemia 12.08 10.37 16 49118 50849 56192084
Cystitis interstitial 12.03 10.37 10 49124 1424 56241509
Autonomic nervous system imbalance 11.99 10.37 13 49121 2580 56240353
Blood pressure orthostatic 11.89 10.37 4 49130 84 56242849
Relapsing-remitting multiple sclerosis 11.85 10.37 7 49127 577 56242356
Product quality issue 11.84 10.37 57 49077 31679 56211254
Optic neuritis 11.80 10.37 23 49111 7781 56235152
Road traffic accident 11.78 10.37 52 49082 27875 56215058
Myalgia 11.76 10.37 171 48963 131854 56111079
Fluid replacement 11.76 10.37 4 49130 87 56242846
Blister 11.70 10.37 52 49082 108835 56134098
Upper respiratory tract infection 11.66 10.37 104 49030 71184 56171749
Stomatitis 11.64 10.37 60 49074 120750 56122183
Acute febrile neutrophilic dermatosis 11.46 10.37 13 49121 2712 56240221
Back injury 11.35 10.37 23 49111 8003 56234930
Drug dependence, antepartum 11.35 10.37 3 49131 26 56242907
Burning sensation 11.27 10.37 77 49057 48619 56194314
Pulmonary fibrosis 11.19 10.37 6 49128 29752 56213181
Liver injury 11.18 10.37 12 49122 41836 56201097
Urosepsis 11.11 10.37 36 49098 16680 56226253
Normocytic anaemia 11.09 10.37 10 49124 1589 56241344
Foetal exposure during pregnancy 11.08 10.37 8 49126 33815 56209118
Micturition urgency 11.06 10.37 24 49110 8757 56234176
Gastrointestinal haemorrhage 11.00 10.37 32 49102 75919 56167014
Fibromyalgia 10.83 10.37 89 49045 59514 56183419
Chills 10.82 10.37 137 48997 102467 56140466
Illness 10.80 10.37 59 49075 34452 56208481
Mucosa vesicle 10.79 10.37 3 49131 32 56242901
CSF immunoglobulin increased 10.74 10.37 4 49130 114 56242819
Pollakiuria 10.69 10.37 47 49087 25155 56217778
Crying 10.67 10.37 42 49092 21398 56221535
Injection site pain 10.55 10.37 152 48982 116966 56125967
Dysstasia 10.53 10.37 39 49095 19315 56223618
Infusion site swelling 10.38 10.37 22 49112 7899 56235034

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple sclerosis relapse 112.96 13.24 70 14569 11977 31670728
Multiple sclerosis 102.51 13.24 57 14582 7980 31674725
Completed suicide 94.40 13.24 159 14480 91355 31591350
Drug withdrawal syndrome 72.78 13.24 64 14575 18686 31664019
Muscle spasticity 69.23 13.24 39 14600 5596 31677109
Potassium wasting nephropathy 65.37 13.24 14 14625 91 31682614
Muscle spasms 64.23 13.24 114 14525 68204 31614501
Failure to suspend medication 59.25 13.24 17 14622 403 31682302
Back pain 52.45 13.24 139 14500 109274 31573431
Depression 44.14 13.24 116 14523 90699 31592006
Febrile neutropenia 39.26 13.24 5 14634 121844 31560861
Intervertebral disc protrusion 39.24 13.24 33 14606 9067 31673638
Neuralgia 39.18 13.24 37 14602 11829 31670876
Serotonin syndrome 37.82 13.24 45 14594 18728 31663977
Pain 36.05 13.24 176 14463 186583 31496122
Anxiety 34.21 13.24 106 14533 90927 31591778
Urinary tract infection 32.18 13.24 93 14546 76776 31605929
Accidental death 31.80 13.24 17 14622 2200 31680505
Fall 31.46 13.24 169 14470 185920 31496785
Suspected suicide 31.40 13.24 21 14618 4086 31678619
Perineal infection 29.97 13.24 11 14628 578 31682127
Scrotal infection 29.78 13.24 11 14628 589 31682116
Anaemia 29.64 13.24 33 14606 213489 31469216
Wrong patient received product 29.52 13.24 17 14622 2542 31680163
Road traffic accident 29.33 13.24 37 14602 16344 31666361
Optic nerve operation 29.17 13.24 10 14629 430 31682275
Drug dependence 26.98 13.24 42 14597 22537 31660168
Infected dermal cyst 26.56 13.24 11 14628 800 31681905
Progressive multiple sclerosis 26.15 13.24 8 14631 238 31682467
Gait disturbance 24.40 13.24 85 14554 77410 31605295
General physical health deterioration 24.28 13.24 11 14628 113424 31569281
Neutropenia 23.84 13.24 18 14621 140346 31542359
Hypoaesthesia 23.64 13.24 68 14571 55954 31626751
Inadequate analgesia 23.60 13.24 15 14624 2678 31680027
Tooth injury 23.02 13.24 11 14628 1123 31681582
Intracranial aneurysm 22.41 13.24 12 14627 1558 31681147
Thrombocytopenia 22.14 13.24 20 14619 142727 31539978
Memory impairment 21.96 13.24 52 14587 38078 31644627
Motor dysfunction 21.37 13.24 20 14619 6319 31676386
Arteriovenous fistula 20.93 13.24 10 14629 1020 31681685
Drug abuser 20.83 13.24 16 14623 3864 31678841
Spinal cord injury cauda equina 20.76 13.24 6 14633 146 31682559
Somatosensory evoked potentials abnormal 20.46 13.24 6 14633 154 31682551
Autonomic dysreflexia 19.96 13.24 5 14634 69 31682636
False positive investigation result 19.80 13.24 7 14632 330 31682375
Vitamin B6 deficiency 19.47 13.24 6 14633 183 31682522
Pancytopenia 19.42 13.24 8 14631 87308 31595397
Dysdiadochokinesis 19.17 13.24 6 14633 193 31682512
Urobilinogen urine increased 19.07 13.24 7 14632 368 31682337
Muscular weakness 19.07 13.24 70 14569 65378 31617327
Unemployment 17.84 13.24 4 14635 33 31682672
Kidney enlargement 17.66 13.24 8 14631 723 31681982
Blood folate increased 17.64 13.24 6 14633 252 31682453
Urine uric acid decreased 17.37 13.24 5 14634 120 31682585
Insomnia 17.27 13.24 88 14551 94748 31587957
Urinary sediment abnormal 17.21 13.24 5 14634 124 31682581
Drug tolerance 17.14 13.24 12 14627 2515 31680190
Burning sensation 17.08 13.24 29 14610 16718 31665987
Movement disorder 16.79 13.24 23 14616 10996 31671709
Pain in extremity 16.61 13.24 101 14538 116102 31566603
Respiratory arrest 16.42 13.24 37 14602 26220 31656485
Malignant neoplasm progression 16.37 13.24 8 14631 78990 31603715
Off label use 16.31 13.24 94 14545 347180 31335525
Lipomatosis 16.26 13.24 6 14633 320 31682385
Dermal cyst 16.17 13.24 10 14629 1701 31681004
Fear of falling 16.05 13.24 6 14633 332 31682373
Hyponatraemia 16.03 13.24 7 14632 73792 31608913
Sedation 15.71 13.24 30 14609 18935 31663770
Respiratory paralysis 15.48 13.24 4 14635 63 31682642
Decreased vibratory sense 15.38 13.24 6 14633 373 31682332
Anal haemorrhage 15.28 13.24 11 14628 2407 31680298
Implant site infection 15.21 13.24 8 14631 1002 31681703
Migraine 15.05 13.24 25 14614 14155 31668550
Secondary progressive multiple sclerosis 15.00 13.24 6 14633 399 31682306
Back injury 15.00 13.24 13 14626 3719 31678986
Feeling abnormal 14.98 13.24 59 14580 56943 31625762
Muscle strength abnormal 14.93 13.24 4 14635 73 31682632
Musculoskeletal stiffness 14.47 13.24 47 14592 41278 31641427
Gait inability 14.30 13.24 29 14610 19115 31663590
Cardio-respiratory arrest 13.96 13.24 54 14585 51672 31631033
Lumbar radiculopathy 13.93 13.24 7 14632 797 31681908
Tendon pain 13.79 13.24 11 14628 2804 31679901
Fine motor skill dysfunction 13.79 13.24 9 14630 1681 31681024
Overdose 13.66 13.24 76 14563 84588 31598117
Umbilical hernia 13.64 13.24 13 14626 4201 31678504
Headache 13.60 13.24 137 14502 183515 31499190
Somnolence 13.31 13.24 85 14554 99360 31583345

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple sclerosis relapse 377.86 11.10 282 49708 42735 70835719
Completed suicide 238.77 11.10 507 49483 226628 70651826
Multiple sclerosis 233.74 11.10 171 49819 25114 70853340
Pneumonia aspiration 161.30 11.10 209 49781 62080 70816374
Drug withdrawal syndrome 157.88 11.10 152 49838 32563 70845891
Gastrooesophageal reflux disease 146.80 11.10 244 49746 90595 70787859
Muscle spasms 134.91 11.10 320 49670 153726 70724728
Somnolence 129.17 11.10 389 49601 215217 70663237
Coma 106.84 11.10 214 49776 91630 70786824
Urinary tract infection 105.75 11.10 400 49590 248369 70630085
Depression 101.75 11.10 340 49650 198634 70679820
Migraine 99.66 11.10 181 49809 72057 70806397
Fall 99.07 11.10 592 49398 443504 70434950
Muscle spasticity 84.80 11.10 86 49904 19603 70858851
Hypoaesthesia 83.31 11.10 268 49722 153471 70724983
Suspected suicide 79.93 11.10 59 49931 8775 70869679
Neutropenia 79.50 11.10 41 49949 257115 70621339
Febrile neutropenia 77.14 11.10 24 49966 204294 70674160
General physical health deterioration 68.09 11.10 41 49949 235990 70642464
Gait disturbance 67.62 11.10 284 49706 184822 70693632
Pain 67.09 11.10 707 49283 628109 70250345
Back pain 66.54 11.10 371 49619 270781 70607673
Autonomic dysreflexia 60.15 11.10 19 49971 406 70878048
Intervertebral disc protrusion 56.95 11.10 73 49917 21430 70857024
Thrombocytopenia 56.70 11.10 51 49939 239059 70639395
Neck pain 55.62 11.10 136 49854 66521 70811933
Lower respiratory tract infection 54.97 11.10 7 49983 111906 70766548
Off label use 53.76 11.10 306 49684 742754 70135700
Potassium wasting nephropathy 52.77 11.10 14 49976 156 70878298
Product dose omission issue 51.63 11.10 295 49695 217173 70661281
Withdrawal syndrome 51.51 11.10 75 49915 24829 70853625
Headache 49.89 11.10 626 49364 579779 70298675
Pancytopenia 49.88 11.10 22 49968 151085 70727369
Hand deformity 48.95 11.10 3 49987 86479 70791975
Contraindicated product administered 48.71 11.10 17 49973 134595 70743859
Pericarditis 47.76 11.10 3 49987 84702 70793752
Failure to suspend medication 46.99 11.10 16 49974 436 70878018
Glossodynia 43.48 11.10 5 49985 86482 70791972
Stiff person syndrome 42.52 11.10 14 49976 343 70878111
Acute kidney injury 41.97 11.10 182 49808 474442 70404012
Drug intolerance 41.65 11.10 59 49931 225628 70652826
Malignant neoplasm progression 41.33 11.10 17 49973 121722 70756732
Treatment failure 40.21 11.10 26 49964 144116 70734338
Memory impairment 39.30 11.10 149 49841 92492 70785962
Maternal exposure during pregnancy 37.73 11.10 17 49973 115328 70763126
Anxiety 37.59 11.10 275 49715 220055 70658399
Feeling abnormal 37.05 11.10 198 49792 142121 70736333
Muscular weakness 35.02 11.10 191 49799 138145 70740309
Insomnia 34.98 11.10 268 49722 217538 70660916
Neuralgia 34.86 11.10 68 49922 28535 70849919
Cardiac failure 34.75 11.10 30 49960 143511 70734943
Anaemia 33.66 11.10 158 49832 403265 70475189
Lumbar radiculopathy 32.50 11.10 19 49971 1907 70876547
Road traffic accident 32.44 11.10 74 49916 34608 70843846
Influenza like illness 31.88 11.10 110 49880 65221 70813233
Progressive multiple sclerosis 31.11 11.10 14 49976 812 70877642
Drug dependence 30.97 11.10 76 49914 37245 70841209
Systemic lupus erythematosus 30.35 11.10 17 49973 101885 70776569
Respiratory arrest 30.06 11.10 95 49895 53838 70824616
Visual impairment 29.94 11.10 124 49866 80126 70798328
Infusion related reaction 29.63 11.10 59 49931 197475 70680979
Hypersensitivity 29.30 11.10 75 49915 229737 70648717
Joint swelling 29.04 11.10 87 49903 253124 70625330
Cardio-respiratory arrest 28.22 11.10 143 49847 100534 70777920
Rheumatoid arthritis 28.20 11.10 108 49882 291697 70586757
Blood creatinine increased 27.77 11.10 36 49954 142965 70735489
Neurogenic bladder 26.95 11.10 22 49968 3791 70874663
Scrotal infection 26.08 11.10 11 49979 545 70877909
Mucosal inflammation 25.53 11.10 8 49982 67842 70810612
Urinary incontinence 25.21 11.10 71 49919 37771 70840683
JC polyomavirus test positive 25.05 11.10 14 49976 1290 70877164
Optic nerve operation 25.05 11.10 10 49980 430 70878024
Mental status changes 24.73 11.10 99 49891 63002 70815452
Drug abuser 24.14 11.10 25 49965 5839 70872615
False positive investigation result 23.94 11.10 12 49978 886 70877568
Dysphoria 23.79 11.10 22 49968 4476 70873978
Platelet count decreased 23.62 11.10 57 49933 178165 70700289
Dizziness 23.09 11.10 457 49533 463684 70414770
Tremor 23.05 11.10 188 49802 155436 70723018
Perineal infection 22.88 11.10 11 49979 742 70877712
Hyperkalaemia 22.64 11.10 25 49965 106566 70771888
Vision blurred 21.95 11.10 128 49862 94856 70783598
Inadequate analgesia 21.49 11.10 20 49970 4102 70874352
Multiple organ dysfunction syndrome 21.39 11.10 27 49963 108488 70769966
Paraesthesia 21.11 11.10 175 49815 145362 70733092
Pyrexia 20.44 11.10 303 49687 606649 70271805
Spinal operation 20.43 11.10 25 49965 7003 70871451
Exposure during pregnancy 20.42 11.10 19 49971 87698 70790756
Back injury 20.41 11.10 28 49962 8774 70869680
C-reactive protein increased 20.26 11.10 29 49961 110488 70767966
Gait inability 20.10 11.10 76 49914 47099 70831355
Bone marrow failure 19.89 11.10 5 49985 49005 70829449
Peroneal nerve palsy 19.85 11.10 22 49968 5548 70872906
Surgery 19.71 11.10 56 49934 29933 70848521
Muscle tightness 19.52 11.10 32 49958 11730 70866724
Vitamin D deficiency 19.42 11.10 33 49957 12454 70866000
International normalised ratio increased 19.38 11.10 17 49973 80709 70797745
Panic attack 19.37 11.10 46 49944 22073 70856381
Back disorder 19.26 11.10 30 49960 10534 70867920
Secondary progressive multiple sclerosis 19.23 11.10 12 49978 1355 70877099
Ascites 19.08 11.10 12 49978 67535 70810919
Hyponatraemia 19.07 11.10 54 49936 160033 70718421
Disease progression 18.55 11.10 53 49937 156619 70721835
Accidental death 18.55 11.10 18 49972 3890 70874564
Urinary sediment abnormal 18.54 11.10 6 49984 139 70878315
Dysarthria 18.51 11.10 90 49900 62223 70816231
Hallucination 18.42 11.10 104 49886 76156 70802298
Infected dermal cyst 18.35 11.10 11 49979 1156 70877298
Spinal cord injury cauda equina 18.26 11.10 6 49984 146 70878308
Amnesia 18.22 11.10 79 49911 52076 70826378
Toxic epidermal necrolysis 18.20 11.10 3 49987 39554 70838900
Gastrointestinal haemorrhage 18.16 11.10 44 49946 137364 70741090
Spinal osteoarthritis 18.11 11.10 36 49954 15312 70863142
Pain in extremity 17.99 11.10 328 49662 327754 70550700
Atrial fibrillation 17.94 11.10 68 49922 184280 70694174
Burning sensation 17.65 11.10 79 49911 52791 70825663
COVID-19 17.44 11.10 131 49859 105626 70772828
Somatosensory evoked potentials abnormal 16.98 11.10 6 49984 183 70878271
Therapy interrupted 16.98 11.10 47 49943 24755 70853699
Loss of consciousness 16.92 11.10 176 49814 155540 70722914
Intervertebral disc degeneration 16.88 11.10 33 49957 13867 70864587
Balance disorder 16.81 11.10 115 49875 90013 70788441
Therapy cessation 16.68 11.10 57 49933 33619 70844835
Hepatic enzyme increased 16.54 11.10 56 49934 156934 70721520
Hepatocellular injury 16.36 11.10 6 49984 46085 70832369
Thinking abnormal 16.36 11.10 30 49960 12021 70866433
Renal impairment 16.10 11.10 50 49940 143887 70734567
Folliculitis 16.05 11.10 5 49985 42565 70835889
Angioedema 16.02 11.10 14 49976 66596 70811858
Melaena 15.94 11.10 10 49980 56345 70822109
Formication 15.92 11.10 18 49972 4639 70873815
Sleep disorder due to general medical condition, insomnia type 15.81 11.10 3 49987 35729 70842725
Asthenia 15.73 11.10 428 49562 457238 70421216
Serotonin syndrome 15.65 11.10 65 49925 42049 70836405
Head injury 15.38 11.10 56 49934 34085 70844369
Urine uric acid decreased 15.28 11.10 5 49985 120 70878334
Neutrophil count decreased 15.24 11.10 22 49968 83534 70794920
Arteriovenous fistula 15.15 11.10 10 49980 1243 70877211
Urobilinogen urine increased 15.04 11.10 8 49982 668 70877786
Productive cough 14.92 11.10 20 49970 78317 70800137
Movement disorder 14.84 11.10 44 49946 24085 70854369
Unemployment 14.81 11.10 4 49986 48 70878406
Plasma cell myeloma 14.65 11.10 18 49972 73183 70805271
Ankle fracture 14.64 11.10 33 49957 15311 70863143
Spinal fusion surgery 14.61 11.10 16 49974 3981 70874473
Drug hypersensitivity 14.59 11.10 263 49727 262196 70616258
Product quality issue 14.51 11.10 51 49939 30510 70847944
Cytomegalovirus infection 14.41 11.10 5 49985 39753 70838701
Bladder disorder 14.36 11.10 23 49967 8266 70870188
Intracranial aneurysm 14.34 11.10 16 49974 4064 70874390
Interstitial lung disease 14.25 11.10 33 49957 104652 70773802
Vitamin B6 deficiency 14.11 11.10 6 49984 303 70878151
Paraparesis 14.09 11.10 15 49975 3614 70874840
Tooth injury 14.00 11.10 11 49979 1794 70876660
Arterial perforation 13.96 11.10 3 49987 12 70878442
Loss of control of legs 13.95 11.10 11 49979 1803 70876651
Dysdiadochokinesis 13.93 11.10 6 49984 313 70878141
Blood pressure systolic increased 13.81 11.10 12 49978 57247 70821207
Respiratory paralysis 13.80 11.10 4 49986 63 70878391
Pneumonitis 13.71 11.10 11 49979 54586 70823868
Muscle injury 13.68 11.10 5 49985 38489 70839965
Circulatory collapse 13.68 11.10 4 49986 35470 70842984
Nausea 13.61 11.10 732 49258 851356 70027098
Hepatotoxicity 13.59 11.10 7 49983 43979 70834475
Fibula fracture 13.59 11.10 14 49976 3249 70875205
Motor dysfunction 13.47 11.10 29 49961 13041 70865413
Impaired gastric emptying 13.40 11.10 24 49966 9442 70869012
Sleep apnoea syndrome 13.36 11.10 52 49938 32661 70845793
Intentional product misuse 13.35 11.10 99 49891 79496 70798958
Septic shock 13.27 11.10 38 49952 112220 70766234
Nerve compression 13.23 11.10 22 49968 8156 70870298
Wrong patient received product 13.12 11.10 16 49974 4464 70873990
Haemorrhagic diathesis 13.10 11.10 18 49972 5649 70872805
Underdose 13.07 11.10 48 49942 29335 70849119
Bedridden 13.06 11.10 26 49964 11072 70867382
pH urine decreased 12.95 11.10 3 49987 18 70878436
Nerve injury 12.95 11.10 22 49968 8302 70870152
Appetite disorder 12.94 11.10 20 49970 6975 70871479
Haemoglobin decreased 12.93 11.10 88 49902 205071 70673383
Acute myeloid leukaemia 12.86 11.10 3 49987 30937 70847517
Lipomatosis 12.67 11.10 6 49984 391 70878063
Leukopenia 12.65 11.10 36 49954 106524 70771930
Concussion 12.60 11.10 22 49968 8487 70869967
Therapeutic product effect decreased 12.50 11.10 55 49935 142963 70735491
Bronchitis 12.49 11.10 132 49858 117111 70761343
Implant site infection 12.37 11.10 10 49980 1699 70876755
Nervousness 12.33 11.10 49 49941 31071 70847383
Lymphocyte percentage decreased 12.30 11.10 16 49974 4763 70873691
Tubulointerstitial nephritis 12.27 11.10 4 49986 33072 70845382
Limb injury 12.25 11.10 43 49947 25709 70852745
Neurotoxicity 12.18 11.10 3 49987 29823 70848631
Device allergy 12.09 11.10 3 49987 25 70878429
Disturbance in attention 12.06 11.10 61 49929 42833 70835621
Drug dependence, antepartum 11.99 11.10 3 49987 26 70878428
Osteonecrosis of jaw 11.98 11.10 7 49983 40995 70837459
Tibia fracture 11.96 11.10 16 49974 4894 70873560
Renal failure 11.96 11.10 81 49909 188989 70689465
Epistaxis 11.94 11.10 35 49955 102592 70775862
Product use issue 11.93 11.10 76 49914 179861 70698593
Implant site swelling 11.92 11.10 6 49984 447 70878007
Autonomic nervous system imbalance 11.91 11.10 15 49975 4324 70874130
Sinus bradycardia 11.72 11.10 40 49950 23583 70854871
White blood cells urine positive 11.68 11.10 17 49973 5623 70872831
Haematochezia 11.68 11.10 21 49969 73060 70805394
Stress 11.66 11.10 85 49905 67881 70810573
Medical device site pain 11.66 11.10 5 49985 258 70878196
Agranulocytosis 11.60 11.10 7 49983 40291 70838163
Crying 11.50 11.10 37 49953 21162 70857292
Mucosa vesicle 11.43 11.10 3 49987 32 70878422
Injection site bruising 11.34 11.10 55 49935 37977 70840477
Blood folate increased 11.34 11.10 6 49984 496 70877958
Intervertebral disc disorder 11.26 11.10 15 49975 4570 70873884
Decreased interest 11.25 11.10 13 49977 3428 70875026
Device failure 11.24 11.10 17 49973 5818 70872636
Umbilical hernia 11.21 11.10 16 49974 5200 70873254
Kidney enlargement 11.19 11.10 8 49982 1132 70877322
T-lymphocyte count decreased 11.17 11.10 6 49984 511 70877943

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03BX02 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
FDA MoA N0000009918 Adrenergic alpha2-Agonists
FDA EPC N0000175554 Central alpha-2 Adrenergic Agonist
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D000700 Analgesics
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35569 alpha-adrenergic agonists
CHEBI has role CHEBI:51371 muscle relaxants

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Spasticity indication 221360009
Muscle spasticity of spinal origin indication 416830008
Muscle Spasticity of Cerebral Origin indication
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Hepatic failure contraindication 59927004
Psychotic disorder contraindication 69322001
Kidney disease contraindication 90708001 DOID:557




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.01 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2A adrenergic receptor GPCR AGONIST EC50 7.07 CHEMBL CHEMBL
Alpha-2B adrenergic receptor GPCR AGONIST WOMBAT-PK CHEMBL
Alpha-2C adrenergic receptor GPCR AGONIST EC50 5.91 CHEMBL CHEMBL
Nischarin Membrane receptor Ki 7.55 CHEMBL
Alpha-1A adrenergic receptor GPCR EC50 6.58 CHEMBL
Alpha-1B adrenergic receptor GPCR EC50 6.49 CHEMBL

External reference:

IDSource
4021025 VUID
N0000148492 NUI
D00776 KEGG_DRUG
64461-82-1 SECONDARY_CAS_RN
4021025 VANDF
4021027 VANDF
C0146011 UMLSCUI
CHEBI:63629 CHEBI
CHEMBL1079 ChEMBL_ID
CHEMBL1200329 ChEMBL_ID
DB00697 DRUGBANK_ID
C023754 MESH_SUPPLEMENTAL_RECORD_UI
5487 PUBCHEM_CID
7308 IUPHAR_LIGAND_ID
4697 INN_ID
6AI06C00GW UNII
236460 RXNORM
22951 MMSL
44068 MMSL
5589 MMSL
d04102 MMSL
006021 NDDF
006022 NDDF
108461005 SNOMEDCT_US
108462003 SNOMEDCT_US
373440006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0034 TABLET 2 mg ORAL ANDA 27 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-4400 TABLET 4 mg ORAL ANDA 27 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2788 CAPSULE, GELATIN COATED 2 mg ORAL NDA 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2788 CAPSULE, GELATIN COATED 2 mg ORAL NDA 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2789 CAPSULE, GELATIN COATED 4 mg ORAL NDA 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2789 CAPSULE, GELATIN COATED 4 mg ORAL NDA 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2790 CAPSULE, GELATIN COATED 6 mg ORAL NDA 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2790 CAPSULE, GELATIN COATED 6 mg ORAL NDA 26 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-5574 TABLET 4 mg ORAL ANDA 25 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-6564 TABLET 2 mg ORAL ANDA 25 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-8274 TABLET 4 mg ORAL ANDA 27 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-8360 TABLET 2 mg ORAL ANDA 27 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0904-6418 TABLET 4 mg ORAL ANDA 18 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0904-6418 TABLET 4 mg ORAL ANDA 18 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0904-6898 TABLET 4 mg ORAL ANDA 27 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 10544-576 TABLET 4 mg ORAL ANDA 20 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 10544-587 TABLET 2 mg ORAL ANDA 18 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 10544-863 TABLET 2 mg ORAL ANDA 18 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 10544-890 TABLET 4 mg ORAL ANDA 22 sections
TIZANIDINE HUMAN PRESCRIPTION DRUG LABEL 1 16590-220 TABLET 2 mg ORAL ANDA 16 sections
TIZANIDINE HUMAN PRESCRIPTION DRUG LABEL 1 16590-221 TABLET 4 mg ORAL ANDA 16 sections
ZANAFLEX HUMAN PRESCRIPTION DRUG LABEL 1 16590-756 CAPSULE 6 mg ORAL NDA 24 sections
ZANAFLEX HUMAN PRESCRIPTION DRUG LABEL 1 16590-871 CAPSULE 4 mg ORAL NDA 24 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 16714-171 TABLET 2 mg ORAL ANDA 27 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 16714-172 TABLET 4 mg ORAL ANDA 27 sections
TIZANIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 21695-126 TABLET 2 mg ORAL ANDA 24 sections
TIZANIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 21695-127 TABLET 4 mg ORAL ANDA 24 sections
Zanaflex HUMAN PRESCRIPTION DRUG LABEL 1 21695-373 CAPSULE, GELATIN COATED 4 mg ORAL NDA 26 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 29300-168 TABLET 2 mg ORAL ANDA 26 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 29300-169 TABLET 4 mg ORAL ANDA 26 sections