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

Stem definitionDrug idCAS RN
alpha-2 adrenoreceptor agonists 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) 1 Bocci G, Oprea TI, Benet LZ
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
S (Water solubility) 18.25 mg/mL Bocci G, Oprea TI, Benet LZ

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 383.72 10.72 321 52915 48157 63387629
Pneumonia aspiration 237.29 10.72 211 53025 34329 63401457
Multiple sclerosis 204.45 10.72 167 53069 24205 63411581
Somnolence 168.65 10.72 425 52811 178260 63257526
Gastrooesophageal reflux disease 156.98 10.72 285 52951 95354 63340432
Completed suicide 152.88 10.72 361 52875 145312 63290474
Coma 151.91 10.72 226 53010 64138 63371648
Contraindicated product administered 140.88 10.72 11 53225 217637 63218149
Synovitis 138.28 10.72 4 53232 186914 63248872
Glossodynia 121.73 10.72 7 53229 178869 63256917
Hand deformity 119.48 10.72 3 53233 159454 63276332
Depression 109.56 10.72 388 52848 196104 63239682
Drug intolerance 104.36 10.72 65 53171 308596 63127190
Systemic lupus erythematosus 103.69 10.72 24 53212 208894 63226892
Drug withdrawal syndrome 102.17 10.72 120 53116 27074 63408712
Fall 102.06 10.72 619 52617 391715 63044071
Maternal exposure during pregnancy 100.25 10.72 30 53206 220032 63215754
Pericarditis 93.17 10.72 4 53232 131575 63304211
Migraine 88.32 10.72 237 52999 103109 63332677
Product dose omission issue 87.77 10.72 409 52827 233904 63201882
Urinary tract infection 82.82 10.72 439 52797 264245 63171541
Lower respiratory tract infection 82.00 10.72 8 53228 132299 63303487
Treatment failure 80.58 10.72 33 53203 199010 63236776
Infusion related reaction 78.49 10.72 55 53181 245466 63190320
Muscle spasms 77.45 10.72 297 52939 155853 63279933
Withdrawal syndrome 66.56 10.72 83 53153 19914 63415872
Joint swelling 65.24 10.72 109 53127 327557 63108229
Helicobacter infection 65.09 10.72 3 53233 92782 63343004
Suspected suicide 63.63 10.72 49 53187 6519 63429267
General physical health deterioration 63.20 10.72 46 53190 201356 63234430
Wound 63.00 10.72 29 53207 163234 63272552
Exposure during pregnancy 62.60 10.72 26 53210 155521 63280265
Hypoaesthesia 62.31 10.72 293 52943 168100 63267686
Neutropenia 60.27 10.72 36 53200 174969 63260817
Gait disturbance 57.35 10.72 304 52932 182874 63252912
Therapeutic product effect decreased 47.69 10.72 55 53181 193132 63242654
Folliculitis 47.06 10.72 3 53233 70314 63365472
Febrile neutropenia 45.75 10.72 21 53215 118428 63317358
Neck pain 45.75 10.72 145 53091 69173 63366613
Anxiety 45.31 10.72 325 52911 217216 63218570
Autonomic dysreflexia 44.91 10.72 15 53221 321 63435465
Tremor 44.51 10.72 224 53012 132015 63303771
Back pain 44.17 10.72 375 52861 263770 63172016
Arthropathy 44.06 10.72 81 53155 234711 63201075
COVID-19 43.43 10.72 199 53037 112904 63322882
Thrombocytopenia 43.05 10.72 38 53198 151119 63284667
Headache 42.57 10.72 756 52480 632485 62803301
Hepatic enzyme increased 42.40 10.72 65 53171 202263 63233523
Off label use 41.54 10.72 364 52872 674098 62761688
Stiff person syndrome 41.13 10.72 14 53222 318 63435468
Alopecia 40.56 10.72 146 53090 337390 63098396
Feeling abnormal 38.97 10.72 235 53001 148157 63287629
Muscle spasticity 38.34 10.72 67 53169 21727 63414059
Hypersensitivity 38.29 10.72 122 53114 292563 63143223
Influenza like illness 36.34 10.72 131 53105 66693 63369093
Drug ineffective 35.65 10.72 640 52596 1044125 62391661
Seizure 34.16 10.72 209 53027 132425 63303361
Product use issue 33.94 10.72 85 53151 220435 63215351
Spinal operation 33.58 10.72 38 53198 8233 63427553
Dysphoria 33.41 10.72 30 53206 4936 63430850
Muscle injury 33.41 10.72 7 53229 65338 63370448
Pancytopenia 33.27 10.72 20 53216 96913 63338873
Intervertebral disc protrusion 33.10 10.72 66 53170 23643 63412143
Sleep disorder due to general medical condition, insomnia type 32.76 10.72 3 53233 52214 63383572
Malignant neoplasm progression 32.59 10.72 14 53222 82107 63353679
Memory impairment 32.57 10.72 173 53063 104085 63331701
Therapy interrupted 32.43 10.72 79 53157 32376 63403410
Abdominal discomfort 32.14 10.72 149 53087 320736 63115050
Vision blurred 31.83 10.72 157 53079 91767 63344019
Sleep apnoea syndrome 31.37 10.72 73 53163 29060 63406726
Swelling 30.55 10.72 123 53113 275255 63160531
Rash 30.50 10.72 312 52924 560559 62875227
Muscular weakness 29.75 10.72 190 53046 122163 63313623
C-reactive protein increased 29.20 10.72 22 53214 94685 63341101
Surgery 28.30 10.72 80 53156 35832 63399954
Vitamin D deficiency 27.48 10.72 45 53191 13847 63421939
Paraesthesia 27.35 10.72 225 53011 156741 63279045
Pre-existing condition improved 27.08 10.72 34 53202 8210 63427576
Insomnia 26.71 10.72 287 52949 214965 63220821
Impaired healing 26.60 10.72 28 53208 102514 63333272
Blood pressure systolic increased 26.57 10.72 4 53232 47393 63388393
Suspected product quality issue 25.97 10.72 9 53227 216 63435570
Suicidal ideation 25.58 10.72 112 53124 62309 63373477
Back disorder 24.99 10.72 38 53198 10979 63424807
Cardiac failure 24.66 10.72 23 53213 89119 63346667
Neurogenic bladder 24.42 10.72 21 53215 3264 63432522
JC polyomavirus test positive 23.88 10.72 15 53221 1438 63434348
Therapeutic response unexpected 23.57 10.72 50 53186 18709 63417077
Pain 23.16 10.72 797 52439 739831 62695955
Rheumatoid arthritis 23.02 10.72 122 53114 253697 63182089
Balance disorder 22.98 10.72 135 53101 84287 63351499
Therapy cessation 22.22 10.72 66 53170 30391 63405395
Loss of consciousness 22.03 10.72 172 53064 117949 63317837
Lumbar radiculopathy 21.99 10.72 16 53220 1953 63433833
Hallucination 21.43 10.72 97 53139 54720 63381066
Respiratory arrest 21.27 10.72 68 53168 32577 63403209
Visual impairment 21.06 10.72 132 53104 84314 63351472
Neuralgia 20.67 10.72 58 53178 25868 63409918
Urinary incontinence 20.23 10.72 66 53170 31948 63403838
Liver injury 20.06 10.72 13 53223 60507 63375279
Amnesia 20.00 10.72 96 53140 55489 63380297
Discomfort 19.67 10.72 73 53163 167301 63268485
Bronchitis 19.60 10.72 175 53061 124760 63311026
Ankle fracture 19.50 10.72 45 53191 17810 63417976
Dysarthria 19.33 10.72 79 53157 42632 63393154
Illness 19.32 10.72 87 53149 48972 63386814
Temperature intolerance 19.05 10.72 30 53206 8934 63426852
Drug dependence 18.77 10.72 54 53182 24429 63411357
Impaired gastric emptying 18.48 10.72 32 53204 10300 63425486
Disease progression 18.34 10.72 48 53188 122710 63313076
Formication 17.91 10.72 20 53216 4271 63431515
Central nervous system lesion 17.81 10.72 32 53204 10603 63425183
Mental status changes 17.73 10.72 73 53163 39526 63396260
Areflexia 17.44 10.72 17 53219 3101 63432685
Nervousness 17.06 10.72 61 53175 30918 63404868
Decreased interest 16.83 10.72 17 53219 3237 63432549
Intervertebral disc degeneration 16.47 10.72 39 53197 15693 63420093
Cardio-respiratory arrest 16.39 10.72 96 53140 59863 63375923
Cervical spinal stenosis 16.18 10.72 14 53222 2194 63433592
Peroneal nerve palsy 15.98 10.72 20 53216 4815 63430971
Panic attack 15.92 10.72 48 53188 22283 63413503
Spinal osteoarthritis 15.74 10.72 39 53197 16147 63419639
Intentional product misuse 15.67 10.72 96 53140 60821 63374965
Pyrexia 15.67 10.72 289 52947 470189 62965597
Pneumonitis 15.66 10.72 5 53231 35217 63400569
Blister 15.66 10.72 56 53180 129758 63306028
Respiratory alkalosis 15.63 10.72 15 53221 2686 63433100
Stress 15.52 10.72 103 53133 67064 63368722
Pulmonary fibrosis 15.45 10.72 7 53229 39802 63395984
Device expulsion 15.45 10.72 5 53231 34917 63400869
Cholestasis 15.36 10.72 3 53233 29431 63406355
International normalised ratio increased 15.34 10.72 10 53226 46415 63389371
Stomatitis 15.34 10.72 62 53174 138663 63297123
Thinking abnormal 15.30 10.72 30 53206 10613 63425173
Hepatotoxicity 15.20 10.72 6 53230 37035 63398751
Neutrophil count decreased 15.08 10.72 15 53221 56391 63379395
Underdose 15.07 10.72 54 53182 27402 63408384
Dizziness 15.01 10.72 469 52767 429456 63006330
Gastrointestinal disorder 14.93 10.72 58 53178 131181 63304605
Acute kidney injury 14.90 10.72 145 53091 263270 63172516
Ill-defined disorder 14.62 10.72 29 53207 81726 63354060
Secondary progressive multiple sclerosis 14.60 10.72 11 53225 1416 63434370
Nasopharyngitis 14.37 10.72 140 53096 254117 63181669
Mucosal inflammation 14.34 10.72 11 53225 46917 63388869
Asthenia 14.33 10.72 422 52814 383182 63052604
Haemorrhagic diathesis 14.17 10.72 18 53218 4397 63431389
Progressive multiple sclerosis 14.14 10.72 10 53226 1168 63434618
Nausea 14.07 10.72 862 52374 853609 62582177
Upper respiratory tract infection 13.95 10.72 117 53119 81930 63353856
Red blood cell sedimentation rate increased 13.84 10.72 10 53226 43972 63391814
Product quality issue 13.67 10.72 63 53173 35802 63399984
Nerve compression 13.54 10.72 26 53210 9061 63426725
Chills 13.50 10.72 150 53086 113228 63322558
Head injury 13.46 10.72 52 53184 27344 63408442
Infusion site swelling 13.40 10.72 27 53209 9743 63426043
Blood creatinine increased 13.39 10.72 34 53202 87810 63347976
Bone marrow failure 13.31 10.72 4 53232 29286 63406500
Irritable bowel syndrome 13.27 10.72 31 53205 82381 63353405
Ascites 13.16 10.72 9 53227 40719 63395067
Disturbance in attention 13.05 10.72 65 53171 38124 63397662
Muscle tightness 13.01 10.72 30 53206 11870 63423916
Spinal fusion acquired 12.89 10.72 3 53233 15 63435771
Hyperkalaemia 12.75 10.72 16 53220 54187 63381599
Loss of control of legs 12.62 10.72 10 53226 1386 63434400
Bladder disorder 12.60 10.72 25 53211 8921 63426865
Live birth 12.59 10.72 3 53233 25627 63410159
Injection site pain 12.52 10.72 165 53071 129635 63306151
Anaemia 12.52 10.72 172 53064 293258 63142528
Micturition urgency 12.52 10.72 26 53210 9585 63426201
Optic neuritis 12.40 10.72 24 53212 8411 63427375
Haematochezia 12.40 10.72 16 53220 53528 63382258
Burning sensation 12.31 10.72 83 53153 54324 63381462
Fibula fracture 12.26 10.72 15 53221 3527 63432259
Appetite disorder 12.22 10.72 22 53214 7299 63428487
Multiple organ dysfunction syndrome 12.10 10.72 18 53218 56734 63379052
Blood pressure orthostatic 12.05 10.72 4 53232 84 63435702
Relapsing-remitting multiple sclerosis 12.04 10.72 7 53229 583 63435203
Hepatocellular injury 11.97 10.72 4 53232 27377 63408409
Hypertonia 11.97 10.72 17 53219 4620 63431166
Foetal exposure during pregnancy 11.82 10.72 6 53230 31956 63403830
Stress cardiomyopathy 11.65 10.72 25 53211 9425 63426361
Myalgia 11.63 10.72 180 53056 146349 63289437
Autonomic nervous system imbalance 11.53 10.72 13 53223 2805 63432981
Drug dependence, antepartum 11.47 10.72 3 53233 26 63435760
Cystitis interstitial 11.39 10.72 10 53226 1598 63434188
Pollakiuria 11.34 10.72 50 53186 27887 63407899
Hypotension 11.32 10.72 304 52932 272300 63163486
Hyperhidrosis 11.21 10.72 139 53097 107697 63328089
Gastrointestinal haemorrhage 11.19 10.72 33 53203 81143 63354643
Hyponatraemia 11.15 10.72 52 53184 111848 63323938
Brain death 11.10 10.72 14 53222 3396 63432390
Therapy non-responder 11.09 10.72 30 53206 75871 63359915
Spinal pain 11.07 10.72 30 53206 13109 63422677
Sinus bradycardia 11.06 10.72 32 53204 14519 63421267
Haemoglobin decreased 11.02 10.72 74 53162 145411 63290375
Acute febrile neutrophilic dermatosis 10.96 10.72 13 53223 2961 63432825
Mucosa vesicle 10.91 10.72 3 53233 32 63435754
CSF immunoglobulin increased 10.90 10.72 4 53232 114 63435672
Concussion 10.88 10.72 24 53212 9220 63426566
Nerve injury 10.79 10.72 25 53211 9921 63425865

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 120.41 13.77 59 15567 6586 34934719
Multiple sclerosis relapse 117.01 13.77 73 15553 13060 34928245
Completed suicide 99.22 13.77 166 15460 98002 34843303
Drug withdrawal syndrome 73.46 13.77 65 15561 19769 34921536
Potassium wasting nephropathy 65.83 13.77 14 15612 91 34941214
Failure to suspend medication 59.09 13.77 17 15609 421 34940884
Muscle spasticity 55.66 13.77 34 15592 5854 34935451
Serotonin syndrome 46.94 13.77 51 15575 19882 34921423
Depression 46.65 13.77 121 15505 96977 34844328
Muscle spasms 46.29 13.77 103 15523 74898 34866407
Intervertebral disc protrusion 41.66 13.77 35 15591 9921 34931384
Urinary tract infection 41.64 13.77 106 15520 83975 34857330
Febrile neutropenia 41.34 13.77 6 15620 136843 34804462
Neuralgia 37.93 13.77 40 15586 15073 34926232
Back pain 37.78 13.77 130 15496 121659 34819646
Anxiety 34.27 13.77 110 15516 99318 34841987
Pain 33.55 13.77 180 15446 204495 34736810
Optic nerve operation 32.30 13.77 11 15615 479 34940826
Fall 32.29 13.77 177 15449 202708 34738597
Suspected suicide 31.58 13.77 22 15604 4726 34936579
Accidental death 30.68 13.77 17 15609 2439 34938866
Road traffic accident 30 13.77 38 15588 17412 34923893
Wrong patient received product 29.45 13.77 17 15609 2637 34938668
Perineal infection 29.45 13.77 11 15615 628 34940677
Scrotal infection 29.22 13.77 11 15615 642 34940663
General physical health deterioration 28.24 13.77 11 15615 128258 34813047
Neutropenia 27.70 13.77 18 15608 156760 34784545
Anaemia 27.07 13.77 39 15587 233296 34708009
Infected dermal cyst 25.87 13.77 11 15615 883 34940422
Progressive multiple sclerosis 25.76 13.77 8 15618 259 34941046
Hypoaesthesia 24.92 13.77 72 15554 61372 34879933
Gait disturbance 24.75 13.77 89 15537 85051 34856254
Drug dependence 24.45 13.77 41 15585 24176 34917129
Tooth injury 22.73 13.77 11 15615 1194 34940111
Inadequate analgesia 22.68 13.77 15 15611 2960 34938345
Thrombocytopenia 22.50 13.77 22 15604 156225 34785080
Motor dysfunction 22.19 13.77 21 15605 6953 34934352
Memory impairment 21.82 13.77 55 15571 43263 34898042
Intracranial aneurysm 21.76 13.77 12 15614 1706 34939599
Movement disorder 21.57 13.77 27 15599 12221 34929084
Spinal fusion surgery 21.33 13.77 10 15616 1011 34940294
Drug abuser 21.02 13.77 16 15610 3938 34937367
Spinal cord injury cauda equina 20.72 13.77 6 15620 152 34941153
Arteriovenous fistula 20.53 13.77 10 15616 1101 34940204
Somatosensory evoked potentials abnormal 20.26 13.77 6 15620 165 34941140
Off label use 20.14 13.77 108 15518 419416 34521889
Autonomic dysreflexia 19.68 13.77 5 15621 76 34941229
Muscular weakness 19.34 13.77 74 15552 72823 34868482
Vitamin B6 deficiency 19.18 13.77 6 15620 199 34941106
Urobilinogen urine increased 19.17 13.77 7 15619 375 34940930
Dysdiadochokinesis 18.93 13.77 6 15620 208 34941097
Hyponatraemia 18.34 13.77 7 15619 82684 34858621
False positive investigation result 17.98 13.77 7 15619 448 34940857
Unemployment 17.97 13.77 4 15622 33 34941272
Urine uric acid decreased 17.33 13.77 5 15621 125 34941180
Kidney enlargement 17.30 13.77 8 15618 784 34940521
Blood folate increased 17.16 13.77 6 15620 283 34941022
Urinary sediment abnormal 17.07 13.77 5 15621 132 34941173
Gait inability 16.91 13.77 32 15594 20726 34920579
Pain in extremity 16.60 13.77 105 15521 126408 34814897
Lipomatosis 16.31 13.77 6 15620 328 34940977
Fear of falling 16.09 13.77 6 15620 341 34940964
Drug tolerance 16.07 13.77 12 15614 2870 34938435
Insomnia 16.04 13.77 90 15536 103817 34837488
Burning sensation 15.79 13.77 29 15597 18365 34922940
Malignant neoplasm progression 15.68 13.77 10 15616 88036 34853269
Dermal cyst 15.67 13.77 10 15616 1857 34939448
Back disorder 15.62 13.77 17 15609 6634 34934671
Respiratory arrest 15.60 13.77 37 15589 28006 34913299
Pancytopenia 15.38 13.77 12 15614 95145 34846160
Secondary progressive multiple sclerosis 15.36 13.77 6 15620 387 34940918
Decreased vibratory sense 15.33 13.77 6 15620 389 34940916
Respiratory paralysis 15.06 13.77 4 15622 73 34941232
Feeling abnormal 15.00 13.77 62 15564 63173 34878132
Anal haemorrhage 14.97 13.77 11 15615 2567 34938738
Implant site infection 14.88 13.77 8 15618 1082 34940223
Back injury 14.47 13.77 13 15613 4028 34937277
Sedation 14.25 13.77 30 15596 20976 34920329
Balance disorder 14.00 13.77 45 15581 40609 34900696
Lumbar radiculopathy 13.82 13.77 7 15619 837 34940468

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 391.42 11.45 292 53469 46241 79644386
Multiple sclerosis 265.03 11.45 173 53588 22109 79668518
Completed suicide 252.03 11.45 529 53232 245238 79445389
Pneumonia aspiration 162.85 11.45 213 53548 66754 79623873
Drug withdrawal syndrome 159.70 11.45 154 53607 34564 79656063
Gastrooesophageal reflux disease 136.56 11.45 249 53512 103997 79586630
Somnolence 135.59 11.45 411 53350 238570 79452057
Urinary tract infection 132.01 11.45 446 53315 274066 79416561
Coma 109.22 11.45 222 53539 100427 79590200
Fall 106.76 11.45 626 53135 487003 79203624
Depression 103.07 11.45 351 53410 216439 79474188
Muscle spasms 92.07 11.45 293 53468 174437 79516190
Migraine 89.06 11.45 188 53573 87305 79603322
Febrile neutropenia 85.16 11.45 25 53736 230974 79459653
Suspected suicide 83.61 11.45 64 53697 10512 79680115
Neutropenia 81.97 11.45 46 53715 287664 79402963
General physical health deterioration 79.87 11.45 43 53718 275195 79415432
Hypoaesthesia 78.81 11.45 283 53478 179069 79511558
Muscle spasticity 71.27 11.45 80 53681 21395 79669232
Gait disturbance 67.48 11.45 298 53463 207208 79483419
Off label use 66.90 11.45 350 53411 906865 78783762
Pain 64.02 11.45 740 53021 703062 78987565
Product dose omission issue 63.50 11.45 332 53429 247205 79443422
Autonomic dysreflexia 60.00 11.45 19 53742 429 79690198
Back pain 59.75 11.45 380 53381 303800 79386827
Thrombocytopenia 59.12 11.45 55 53706 265204 79425423
Pericarditis 57.85 11.45 3 53758 104233 79586394
Lower respiratory tract infection 57.74 11.45 9 53752 129211 79561416
Hand deformity 57.65 11.45 3 53758 103916 79586711
Intervertebral disc protrusion 57.18 11.45 75 53686 23546 79667081
Withdrawal syndrome 57.01 11.45 80 53681 26774 79663853
Contraindicated product administered 56.33 11.45 18 53743 157520 79533107
Neck pain 53.74 11.45 141 53620 75276 79615351
Potassium wasting nephropathy 53.39 11.45 14 53747 156 79690471
Drug intolerance 50.78 11.45 62 53699 264057 79426570
Headache 49.74 11.45 665 53096 653107 79037520
Glossodynia 48.99 11.45 6 53755 103331 79587296
Failure to suspend medication 46.94 11.45 16 53745 458 79690169
Pancytopenia 46.46 11.45 27 53734 165718 79524909
Maternal exposure during pregnancy 44.73 11.45 18 53743 136520 79554107
Stiff person syndrome 44.55 11.45 14 53747 308 79690319
Feeling abnormal 41.81 11.45 215 53546 158984 79531643
Treatment failure 40.82 11.45 33 53728 170453 79520174
Anxiety 40.73 11.45 297 53464 248215 79442412
Malignant neoplasm progression 39.78 11.45 21 53740 135969 79554658
Neuralgia 37.81 11.45 75 53686 33309 79657318
Acute kidney injury 36.69 11.45 203 53558 519201 79171426
Systemic lupus erythematosus 35.00 11.45 19 53742 121130 79569497
Influenza like illness 34.80 11.45 117 53644 71590 79619037
Cardiac failure 34.60 11.45 32 53729 154810 79535817
Memory impairment 33.69 11.45 157 53604 111577 79579050
Insomnia 33.00 11.45 280 53481 244890 79445737
Serotonin syndrome 32.91 11.45 85 53676 44942 79645685
Lumbar radiculopathy 32.63 11.45 19 53742 1980 79688647
Anaemia 32.48 11.45 172 53589 444843 79245784
Muscular weakness 32.25 11.45 202 53559 160527 79530100
Hypersensitivity 31.12 11.45 83 53678 262156 79428471
Drug dependence 30.87 11.45 78 53683 40691 79649936
Joint swelling 30.86 11.45 96 53665 288550 79402077
Infusion related reaction 30.35 11.45 69 53692 230168 79460459
COVID-19 30.30 11.45 196 53565 157478 79533149
Neurogenic bladder 30.07 11.45 24 53737 4188 79686439
Respiratory arrest 28.90 11.45 95 53666 57455 79633172
Optic nerve operation 27.89 11.45 11 53750 479 79690148
Road traffic accident 27.47 11.45 78 53683 43586 79647041
Cardio-respiratory arrest 27.41 11.45 145 53616 108365 79582262
Tremor 26.55 11.45 201 53560 169882 79520745
Progressive multiple sclerosis 26.54 11.45 14 53747 1203 79689424
Mucosal inflammation 26.37 11.45 9 53752 75571 79615056
Mental status changes 26.32 11.45 102 53659 66857 79623770
Surgery 26.19 11.45 64 53697 32702 79657925
Visual impairment 25.99 11.45 127 53634 92004 79598623
Urinary incontinence 25.66 11.45 73 53688 40836 79649791
Dysphoria 25.62 11.45 23 53738 4711 79685916
JC polyomavirus test positive 25.55 11.45 15 53746 1587 79689040
Scrotal infection 25.51 11.45 11 53750 602 79690025
Platelet count decreased 25.12 11.45 59 53702 194605 79496022
Exposure during pregnancy 24.93 11.45 19 53742 101113 79589514
False positive investigation result 24.84 11.45 13 53748 1099 79689528
Drug abuser 24.54 11.45 25 53736 5988 79684639
Disease progression 24.49 11.45 55 53706 184307 79506320
C-reactive protein increased 24.03 11.45 31 53730 128996 79561631
Back disorder 23.84 11.45 34 53727 11544 79679083
Spinal operation 23.75 11.45 28 53733 7889 79682738
Blood creatinine increased 23.37 11.45 43 53718 155014 79535613
Multiple organ dysfunction syndrome 23.33 11.45 28 53733 120218 79570409
Hyponatraemia 22.87 11.45 54 53707 177794 79512833
Peroneal nerve palsy 22.64 11.45 24 53737 6018 79684609
Perineal infection 22.62 11.45 11 53750 796 79689831
Folliculitis 22.29 11.45 5 53756 55375 79635252
Vision blurred 21.80 11.45 134 53627 105764 79584863
Hepatic enzyme increased 21.50 11.45 58 53703 182552 79508075
Dizziness 21.21 11.45 484 53277 525957 79164670
Dysarthria 20.36 11.45 95 53666 67527 79623100
Spinal osteoarthritis 20.35 11.45 39 53722 16888 79673739
Inadequate analgesia 20.28 11.45 20 53741 4609 79686018
Ascites 20.20 11.45 13 53748 75549 79615078
Toxic epidermal necrolysis 20.15 11.45 3 53758 44578 79646049
Panic attack 20.10 11.45 48 53713 24168 79666459
Vitamin D deficiency 19.81 11.45 35 53726 14244 79676383
Bone marrow failure 19.81 11.45 5 53756 51102 79639525
Intervertebral disc degeneration 19.76 11.45 37 53724 15748 79674879
Balance disorder 19.67 11.45 124 53637 98733 79591894
Loss of consciousness 19.60 11.45 186 53575 167757 79522870
Pyrexia 19.54 11.45 331 53430 678378 79012249
Sleep disorder due to general medical condition, insomnia type 19.53 11.45 3 53758 43553 79647074
Secondary progressive multiple sclerosis 19.48 11.45 12 53749 1385 79689242
Seizure 19.08 11.45 203 53558 188631 79501996
Gastrointestinal haemorrhage 18.87 11.45 45 53716 147674 79542953
Urinary sediment abnormal 18.56 11.45 6 53755 145 79690482
Illness 18.40 11.45 71 53690 46440 79644187
Muscle tightness 18.37 11.45 32 53729 12882 79677745
International normalised ratio increased 18.35 11.45 18 53743 84703 79605924
Spinal cord injury cauda equina 18.29 11.45 6 53755 152 79690475
Pain in extremity 18.22 11.45 346 53415 364192 79326435
Burning sensation 18.12 11.45 83 53678 58549 79632078
Neutrophil count decreased 18.09 11.45 22 53739 93937 79596690
Infected dermal cyst 18.04 11.45 11 53750 1247 79689380
Hallucination 17.96 11.45 109 53652 85636 79604991
Therapy interrupted 17.81 11.45 54 53707 31287 79659340
Accidental death 17.80 11.45 18 53743 4273 79686354
Back injury 17.54 11.45 28 53733 10495 79680132
Movement disorder 17.44 11.45 49 53712 27210 79663417
Therapy cessation 17.09 11.45 60 53701 37502 79653125
Atrial fibrillation 17.04 11.45 72 53689 197814 79492813
Dysdiadochokinesis 17.03 11.45 7 53754 340 79690287
Bronchitis 16.92 11.45 148 53613 130496 79560131
Somatosensory evoked potentials abnormal 16.91 11.45 6 53755 194 79690433
Ankle fracture 16.72 11.45 36 53725 16933 79673694
Angioedema 16.64 11.45 16 53745 76019 79614608
Muscle injury 16.56 11.45 6 53755 48555 79642072
Hepatotoxicity 16.44 11.45 7 53754 51345 79639282
Bladder disorder 16.13 11.45 25 53736 9140 79681487
Hepatocellular injury 16.03 11.45 6 53755 47587 79643040
Blood pressure systolic increased 15.98 11.45 13 53748 66973 79623654
Nerve compression 15.98 11.45 25 53736 9214 79681413
Product use issue 15.89 11.45 80 53681 209742 79480885
Paraesthesia 15.74 11.45 185 53576 176138 79514489
Formication 15.46 11.45 18 53743 5005 79685622
Interstitial lung disease 15.44 11.45 33 53728 112567 79578060
Thinking abnormal 15.42 11.45 30 53731 13131 79677496
Haematochezia 15.37 11.45 22 53739 87623 79603004
Urine uric acid decreased 15.31 11.45 5 53756 125 79690502
Urobilinogen urine increased 15.30 11.45 8 53753 675 79689952
Product quality issue 15.26 11.45 54 53707 33886 79656741
Intracranial aneurysm 15.18 11.45 17 53744 4533 79686094
Impaired gastric emptying 15.18 11.45 26 53735 10327 79680300
Therapeutic product effect decreased 15.13 11.45 58 53703 163805 79526822
Gait inability 15.05 11.45 79 53682 58838 79631789
Unemployment 14.98 11.45 4 53757 48 79690579
Arteriovenous fistula 14.85 11.45 10 53751 1344 79689283
Spinal fusion surgery 14.85 11.45 18 53743 5220 79685407
Sinus bradycardia 14.82 11.45 44 53717 25203 79665424
Head injury 14.74 11.45 57 53704 37312 79653315
Haemoglobin decreased 14.47 11.45 89 53672 222030 79468597
Renal impairment 14.47 11.45 56 53705 157727 79532900
Amnesia 14.40 11.45 82 53679 62975 79627652
Nerve injury 14.31 11.45 24 53737 9368 79681259
Melaena 14.30 11.45 12 53749 60878 79629749
Pneumonitis 14.29 11.45 12 53749 60848 79629779
Arterial perforation 14.09 11.45 3 53758 12 79690615
Paraparesis 14.06 11.45 15 53746 3788 79686839
Circulatory collapse 14.01 11.45 4 53757 37664 79652963
Zinc deficiency 13.82 11.45 5 53756 171 79690456
Productive cough 13.75 11.45 24 53737 88307 79602320
Vitamin B6 deficiency 13.72 11.45 6 53755 340 79690287
Leukopenia 13.71 11.45 37 53724 116476 79574151
Hyperkalaemia 13.71 11.45 36 53725 114362 79576265
Asthenia 13.63 11.45 446 53315 511243 79179384
Loss of control of legs 13.61 11.45 11 53750 1954 79688673
Underdose 13.43 11.45 51 53710 33100 79657527
Injection site bruising 13.39 11.45 59 53702 40943 79649684
Wrong patient received product 13.31 11.45 16 53745 4602 79686025
Tooth injury 13.30 11.45 11 53750 2017 79688610
Toxicity to various agents 13.25 11.45 375 53386 421165 79269462
Agranulocytosis 13.09 11.45 7 53754 45023 79645604
pH urine decreased 13.08 11.45 3 53758 18 79690609
Neurotoxicity 12.96 11.45 3 53758 32515 79658112
Respiratory paralysis 12.90 11.45 4 53757 84 79690543
Wound 12.86 11.45 38 53723 116141 79574486
Concussion 12.81 11.45 23 53738 9480 79681147
Fibula fracture 12.73 11.45 14 53747 3660 79686967
Haemorrhagic diathesis 12.73 11.45 18 53743 6066 79684561
Upper respiratory tract infection 12.71 11.45 105 53656 91063 79599564
Lipomatosis 12.62 11.45 6 53755 413 79690214
Pulmonary fibrosis 12.62 11.45 7 53754 44105 79646522
Nausea 12.58 11.45 776 52985 956420 78734207
Stress cardiomyopathy 12.54 11.45 25 53736 11141 79679486
Drug hypersensitivity 12.38 11.45 276 53485 298640 79391987
Lymphocyte percentage decreased 12.35 11.45 16 53745 4960 79685667
Bedridden 12.33 11.45 26 53735 12053 79678574
Sleep apnoea syndrome 12.30 11.45 53 53708 36425 79654202
Drug dependence, antepartum 12.12 11.45 3 53758 26 79690601
Appetite disorder 12.09 11.45 20 53741 7719 79682908
Rash maculo-papular 12.04 11.45 12 53749 56066 79634561
Implant site swelling 12.02 11.45 6 53755 459 79690168
Acute myeloid leukaemia 12.01 11.45 3 53758 30882 79659745
Motor dysfunction 12.01 11.45 29 53732 14704 79675923
Implant site infection 11.99 11.45 10 53751 1855 79688772
Cytomegalovirus infection 11.87 11.45 7 53754 42637 79647990
Device allergy 11.83 11.45 3 53758 29 79690598
Hypotension 11.77 11.45 384 53377 439933 79250694
Autonomic nervous system imbalance 11.67 11.45 15 53746 4615 79686012
Inflammation 11.62 11.45 29 53732 93724 79596903
Limb injury 11.62 11.45 45 53716 29483 79661144
Nervousness 11.61 11.45 49 53712 33366 79657261
Lumbar spinal stenosis 11.60 11.45 16 53745 5266 79685361
Mucosa vesicle 11.56 11.45 3 53758 32 79690595
Disturbance in attention 11.56 11.45 66 53695 50735 79639892
Crying 11.53 11.45 38 53723 23005 79667622
Injection site pain 11.48 11.45 136 53625 129702 79560925

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 D000927 Anticonvulsants
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 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 0591-2788 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 0591-2789 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 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 0615-8274 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 0615-8360 TABLET 2 mg ORAL ANDA 27 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-8468 TABLET 2 mg ORAL ANDA 26 sections
tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 0615-8469 TABLET 4 mg ORAL ANDA 26 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