tizanidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.739 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.167 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 15.631 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.519 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 68.580 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 77.250 % High 1
herg hERG pIC50 4.667 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.054 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 7.096 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 60.770 % High 1
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK7,MARK4,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK,TTK 34
kinase-selectivity-class CDK9,GRK2,MAPK7,PDK1 4
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.466 High 1
mh-clint Mouse hepatocyte intrinsic clearance 13.183 High 1
mppb Mouse plasma protein binding (% unbound) 70.910 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.199 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 70.050 % High 1
rh-clint Rat hepatocyte intrinsic clearance 8.375 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 93.360 % High 1
rppb Rat plasma protein binding (% unbound) 66.310 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 872.971 uM High 1

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 458.16 10.74 342 63379 51963 90512763
Completed suicide 450.19 10.74 532 63189 144526 90420200
Pneumonia aspiration 260.59 10.74 222 63499 40718 90524008
Multiple sclerosis 232.51 10.74 177 63544 27663 90537063
Somnolence 222.92 10.74 469 63252 208615 90356111
Synovitis 200.75 10.74 7 63714 329745 90234981
Hand deformity 192.98 10.74 3 63718 296359 90268367
Glossodynia 191.88 10.74 8 63713 321771 90242955
Coma 172.00 10.74 233 63488 72399 90492327
Pericarditis 170.77 10.74 4 63717 270147 90294579
Systemic lupus erythematosus 162.87 10.74 29 63692 361867 90202859
Suspected suicide 160.68 10.74 94 63627 9474 90555252
Contraindicated product administered 152.26 10.74 22 63699 320117 90244609
Lower respiratory tract infection 150.19 10.74 6 63715 250653 90314073
Infusion related reaction 148.16 10.74 54 63667 416726 90148000
Product dose omission issue 144.26 10.74 492 63229 291195 90273531
Helicobacter infection 140.95 10.74 4 63717 226846 90337880
Fall 139.17 10.74 688 63033 481122 90083604
Maternal exposure during pregnancy 136.07 10.74 42 63679 360021 90204705
Drug withdrawal syndrome 134.23 10.74 131 63590 28592 90536134
Folliculitis 122.04 10.74 5 63716 204348 90360378
Urinary tract infection 120.39 10.74 479 63242 305153 90259573
Drug intolerance 120.17 10.74 84 63637 447507 90117219
Gastrooesophageal reflux disease 113.37 10.74 314 63407 166023 90398703
Wound 113.27 10.74 36 63685 302944 90261782
Depression 112.73 10.74 464 63257 300137 90264589
General physical health deterioration 111.77 10.74 55 63666 355060 90209666
Muscle injury 100.13 10.74 6 63715 176648 90388078
Treatment failure 92.74 10.74 49 63672 303879 90260847
Exposure during pregnancy 89.67 10.74 28 63693 238382 90326344
Withdrawal syndrome 89.30 10.74 94 63627 22430 90542296
Back pain 85.14 10.74 444 63277 316731 90247995
Hepatic enzyme increased 85.09 10.74 77 63644 360659 90204067
Joint swelling 84.41 10.74 140 63581 503160 90061566
Tremor 84.23 10.74 268 63453 152905 90411821
Impaired healing 78.76 10.74 33 63688 234166 90330560
Liver injury 78.13 10.74 13 63708 170554 90394172
Arthropathy 77.42 10.74 86 63635 366156 90198570
Sleep disorder due to general medical condition, insomnia type 77.33 10.74 3 63718 128691 90436035
Surgery 66.61 10.74 116 63605 44771 90519955
Migraine 65.17 10.74 286 63435 190106 90374620
COVID-19 64.28 10.74 262 63459 168581 90396145
C-reactive protein increased 61.88 10.74 25 63696 181364 90383362
Feeling abnormal 61.69 10.74 257 63464 166978 90397748
Therapeutic product effect decreased 61.07 10.74 63 63658 277508 90287218
Gait disturbance 60.69 10.74 351 63370 260145 90304581
Toxicity to various agents 60.15 10.74 377 63344 287469 90277257
Irritable bowel syndrome 59.58 10.74 36 63685 207412 90357314
Neutropenia 59.24 10.74 43 63678 224861 90339865
Hypersensitivity 57.94 10.74 148 63573 454529 90110197
Type 2 diabetes mellitus 57.36 10.74 36 63685 203208 90361518
Off label use 57.36 10.74 498 63223 1101754 89462972
Ill-defined disorder 56.09 10.74 30 63691 184861 90379865
Dysphoria 55.54 10.74 41 63680 6113 90558613
Febrile neutropenia 52.13 10.74 23 63698 158326 90406400
Headache 51.63 10.74 872 62849 861874 89702852
Stomatitis 51.21 10.74 71 63650 274627 90290099
Thrombocytopenia 51.05 10.74 43 63678 208682 90356044
Seizure 50.49 10.74 227 63494 152402 90412324
Muscle spasms 50.20 10.74 326 63395 251557 90313169
Therapy interrupted 49.38 10.74 109 63612 49999 90514727
Illness 49.28 10.74 148 63573 81821 90482905
Swelling 49.17 10.74 142 63579 418916 90145810
Facet joint syndrome 48.54 10.74 6 63715 98383 90466343
Vision blurred 48.36 10.74 179 63542 110114 90454612
Anxiety 47.85 10.74 377 63344 309395 90255331
Pulmonary fibrosis 47.47 10.74 9 63712 107494 90457232
Cardio-respiratory arrest 46.79 10.74 123 63598 63017 90501709
Product use issue 46.29 10.74 102 63619 329817 90234909
Stiff person syndrome 45.63 10.74 16 63705 478 90564248
Autonomic dysreflexia 45.46 10.74 15 63706 371 90564355
Alopecia 45.10 10.74 187 63534 494884 90069842
Injury 44.29 10.74 44 63677 197305 90367421
Live birth 43.88 10.74 3 63718 79104 90485622
Sleep apnoea syndrome 43.20 10.74 79 63642 31668 90533058
Vitamin D deficiency 42.56 10.74 57 63664 17499 90547227
Influenza like illness 42.43 10.74 139 63582 80472 90484254
Blister 41.69 10.74 72 63649 254926 90309800
Hypercholesterolaemia 41.37 10.74 10 63711 100882 90463844
Intervertebral disc protrusion 41.29 10.74 71 63650 27125 90537601
Product administration interrupted 40.63 10.74 47 63674 12445 90552281
Gastrointestinal disorder 40.59 10.74 74 63647 256613 90308113
Balance disorder 40.44 10.74 155 63566 96925 90467801
Injection site pain 40.39 10.74 234 63487 173465 90391261
Neuralgia 39.88 10.74 76 63645 31424 90533302
Abdominal discomfort 39.42 10.74 187 63534 477141 90087585
Neck pain 38.06 10.74 170 63551 113793 90450933
Loss of consciousness 38.03 10.74 197 63524 140041 90424685
Pre-existing condition improved 37.66 10.74 39 63682 9130 90555596
Suicidal ideation 35.90 10.74 124 63597 73731 90490995
Respiratory arrest 35.73 10.74 75 63646 33236 90531490
Stress 35.59 10.74 132 63589 81263 90483463
Discomfort 35.13 10.74 89 63632 274246 90290480
Peripheral venous disease 35.04 10.74 8 63713 83913 90480813
Bursitis 34.88 10.74 25 63696 131629 90433097
Malignant neoplasm progression 34.42 10.74 16 63705 106854 90457872
Joint range of motion decreased 34.34 10.74 27 63694 135616 90429110
Lung disorder 34.11 10.74 33 63688 149850 90414876
Hallucination 34.05 10.74 113 63608 65846 90498880
Blood cholesterol increased 33.75 10.74 59 63662 207953 90356773
Therapeutic response unexpected 33.05 10.74 57 63664 21823 90542903
Grip strength decreased 32.82 10.74 12 63709 92564 90472162
Wound infection 32.65 10.74 17 63704 106385 90458341
Hypotension 32.57 10.74 361 63360 325036 90239690
Spinal operation 32.55 10.74 38 63683 10158 90554568
Inflammation 32.43 10.74 47 63674 178545 90386181
Liver disorder 32.16 10.74 23 63698 121246 90443480
JC polyomavirus test positive 31.04 10.74 18 63703 1784 90562942
Pain 29.74 10.74 913 62808 995428 89569298
Myalgia 29.73 10.74 218 63503 174907 90389819
Nausea 29.67 10.74 1004 62717 1109312 89455414
Adjustment disorder with depressed mood 29.15 10.74 3 63718 56750 90507976
Panic attack 29.02 10.74 60 63661 26305 90538421
Pyrexia 28.48 10.74 312 63409 660173 89904553
Muscle spasticity 28.43 10.74 71 63650 35251 90529475
Chills 28.23 10.74 174 63547 131807 90432919
Mental status changes 28.11 10.74 82 63639 44597 90520129
Nervousness 27.99 10.74 69 63652 33987 90530739
Pancytopenia 27.92 10.74 26 63695 120237 90444489
Spinal osteoarthritis 27.78 10.74 49 63672 19099 90545627
Nasopharyngitis 27.77 10.74 170 63551 406934 90157792
Blood pressure systolic increased 27.72 10.74 4 63717 58341 90506385
Neurogenic bladder 27.69 10.74 22 63699 3656 90561070
Urinary incontinence 27.64 10.74 73 63648 37493 90527233
Appetite disorder 27.44 10.74 33 63688 9100 90555626
Haemorrhagic diathesis 27.32 10.74 26 63695 5498 90559228
Impaired gastric emptying 27.17 10.74 39 63682 12770 90551956
Autoimmune disorder 27.12 10.74 10 63711 76734 90487992
Epilepsy 26.95 10.74 12 63709 82194 90482532
Skin warm 26.83 10.74 30 63691 7657 90557069
Visual impairment 26.76 10.74 172 63549 132193 90432533
Disturbance in attention 26.39 10.74 83 63638 47026 90517700
Hypoaesthesia 26.33 10.74 337 63384 313873 90250853
Decreased interest 26.21 10.74 23 63698 4384 90560342
Therapy cessation 26.09 10.74 70 63651 36291 90528435
Bronchitis 25.75 10.74 190 63531 152737 90411989
Ankle fracture 25.60 10.74 49 63672 20321 90544405
Thinking abnormal 25.30 10.74 36 63685 11696 90553030
Lumbar radiculopathy 25.05 10.74 18 63703 2573 90562153
Rheumatoid arthritis 24.95 10.74 151 63570 362463 90202263
Intervertebral disc degeneration 24.79 10.74 44 63677 17230 90547496
Peroneal nerve palsy 24.60 10.74 25 63696 5723 90559003
Dysarthria 24.36 10.74 89 63632 54393 90510333
Serotonin syndrome 24.28 10.74 70 63651 37817 90526909
Central nervous system lesion 24.04 10.74 35 63686 11611 90553115
Drug dependence 23.66 10.74 59 63662 29268 90535458
Drug interaction 23.37 10.74 297 63424 276156 90288570
Temperature intolerance 23.17 10.74 35 63686 11995 90552731
Red blood cell sedimentation rate increased 22.78 10.74 15 63706 82580 90482146
Formication 22.66 10.74 22 63699 4769 90559957
Head injury 22.33 10.74 60 63661 31128 90533598
Crying 22.19 10.74 53 63668 25592 90539134
Suspected product quality issue 21.80 10.74 9 63712 423 90564303
Prescribed overdose 21.63 10.74 22 63699 97603 90467123
Blepharospasm 19.97 10.74 7 63714 55438 90509288
Lupus-like syndrome 19.72 10.74 5 63716 48841 90515885
Blood potassium decreased 19.70 10.74 76 63645 47651 90517075
Cardiac failure 19.69 10.74 29 63692 109467 90455259
Hepatic cirrhosis 19.56 10.74 10 63711 63243 90501483
Diplopia 19.33 10.74 54 63667 28660 90536066
Coeliac disease 19.13 10.74 4 63717 44606 90520120
Muscle tightness 18.99 10.74 34 63687 13405 90551321
Bladder disorder 18.87 10.74 30 63691 10742 90553984
Dry skin 18.76 10.74 116 63605 87957 90476769
Insomnia 18.72 10.74 334 63387 333140 90231586
Burning sensation 18.50 10.74 91 63630 63361 90501365
Photophobia 18.45 10.74 44 63677 21225 90543501
Disease progression 18.39 10.74 53 63668 156562 90408164
Cervical spinal stenosis 18.23 10.74 15 63706 2620 90562106
Injection site bruising 18.19 10.74 79 63642 52228 90512498
Nerve injury 18.19 10.74 30 63691 11076 90553650
Rash 18.12 10.74 424 63297 795676 89769050
Injection site erythema 18.09 10.74 125 63596 98377 90466349
Sinus bradycardia 17.98 10.74 38 63683 16914 90547812
Nerve compression 17.93 10.74 29 63692 10537 90554189
Psoriatic arthropathy 17.92 10.74 91 63630 228244 90336482
Liver function test increased 17.82 10.74 20 63701 84835 90479891
Initial insomnia 17.81 10.74 27 63694 9283 90555443
Areflexia 17.70 10.74 17 63704 3636 90561090
Secondary progressive multiple sclerosis 17.68 10.74 12 63709 1567 90563159
Dermatitis atopic 17.66 10.74 46 63675 23426 90541300
Pollakiuria 17.44 10.74 57 63664 32948 90531778
Irritability 17.43 10.74 60 63661 35602 90529124
Progressive multiple sclerosis 17.33 10.74 11 63710 1283 90563443
Dizziness 17.24 10.74 539 63182 588745 89975981
Bradycardia 16.97 10.74 109 63612 83738 90480988
Pneumonitis 16.93 10.74 5 63716 44165 90520561
Sinus disorder 16.88 10.74 58 63663 34389 90530337
Decorticate posture 16.78 10.74 7 63714 338 90564388
Paraesthesia 16.73 10.74 258 63463 250068 90314658
Intentional product misuse 16.63 10.74 114 63607 89490 90475236
Delirium 16.56 10.74 30 63691 104329 90460397
Mucosal inflammation 16.53 10.74 10 63711 57615 90507111
Arthritis infective 16.47 10.74 24 63697 7968 90556758
Product dose omission in error 16.28 10.74 41 63680 20462 90544264
Foot deformity 16.23 10.74 11 63710 59640 90505086
Muscular weakness 16.19 10.74 219 63502 206447 90358279
Loss of control of legs 16.19 10.74 11 63710 1439 90563287
Hypertonia 16.10 10.74 19 63702 5136 90559590
Cholestasis 16.10 10.74 3 63718 36296 90528430
Fatigue 16.07 10.74 977 62744 1153046 89411680
Neutrophil count decreased 15.98 10.74 16 63705 71516 90493210
Nail disorder 15.92 10.74 11 63710 59056 90505670
Dysstasia 15.78 10.74 46 63675 25006 90539720
Syncope 15.53 10.74 152 63569 132511 90432215
Blood pressure increased 15.45 10.74 209 63512 197008 90367718
Memory impairment 15.44 10.74 209 63512 197035 90367691
Hyperhidrosis 15.39 10.74 155 63566 136150 90428576
Intervertebral disc disorder 15.23 10.74 19 63702 5441 90559285
Respiratory alkalosis 14.76 10.74 15 63706 3433 90561293
Somnambulism 14.76 10.74 20 63701 6208 90558518
Jejunectomy 14.74 10.74 4 63717 49 90564677
Nephrolithiasis 14.74 10.74 71 63650 49014 90515712
Thrombosis 14.68 10.74 95 63626 73156 90491570
Influenza 14.60 10.74 156 63565 139108 90425618
Conduction disorder 14.41 10.74 11 63710 1724 90563002
Urosepsis 14.36 10.74 40 63681 21192 90543534
Concussion 14.33 10.74 27 63694 11064 90553662
Cervical radiculopathy 14.16 10.74 10 63711 1392 90563334
Breakthrough pain 14.12 10.74 10 63711 1397 90563329
Intentional product use issue 14.03 10.74 92 63629 216800 90347926
Mobility decreased 13.98 10.74 111 63610 250623 90314103
Aberrant aortic arch 13.96 10.74 3 63718 12 90564714
Fibula fracture 13.88 10.74 16 63705 4221 90560505
Withdrawal hypertension 13.82 10.74 5 63716 164 90564562
Bedridden 13.79 10.74 28 63693 12120 90552606
Premature delivery 13.78 10.74 5 63716 38757 90525969
Asthenia 13.75 10.74 481 63240 533270 90031456
Shrinking lung syndrome 13.65 10.74 5 63716 170 90564556
Frequent bowel movements 13.58 10.74 12 63709 56923 90507803
Breast cancer stage II 13.54 10.74 4 63717 35330 90529396
Drug tolerance decreased 13.54 10.74 3 63718 32127 90532599
Constipation 13.39 10.74 274 63447 280121 90284605
Vaginitis gardnerella 13.37 10.74 4 63717 71 90564655
Dyspepsia 13.36 10.74 83 63638 198077 90366649
Device expulsion 13.35 10.74 6 63715 40880 90523846
Post-traumatic stress disorder 13.34 10.74 20 63701 6808 90557918
Dysphagia 13.31 10.74 129 63592 112149 90452577
Emotional distress 13.23 10.74 56 63665 36606 90528120
Therapeutic product effect incomplete 13.18 10.74 81 63640 193815 90370911
Blood pressure orthostatic 13.06 10.74 4 63717 77 90564649
Fungal infection 13.02 10.74 62 63659 42599 90522127
Lymphocyte count decreased 13.01 10.74 54 63667 34996 90529730
Spinal pain 13.01 10.74 32 63689 15735 90548991
Tenderness 12.96 10.74 45 63676 26823 90537903
Vitamin D decreased 12.88 10.74 27 63694 11952 90552774
Abnormal dreams 12.84 10.74 26 63695 11231 90553495
Dehydration 12.83 10.74 200 63521 194247 90370479
Unresponsive to stimuli 12.82 10.74 57 63664 38064 90526662
Therapy non-responder 12.81 10.74 51 63670 136653 90428073
Pregnancy 12.62 10.74 15 63706 62032 90502694
Ligament sprain 12.44 10.74 30 63691 14569 90550157
Taste disorder 12.39 10.74 15 63706 61531 90503195
Skin burning sensation 12.34 10.74 36 63685 19575 90545151
Speech disorder 12.32 10.74 64 63657 45521 90519205
Impaired quality of life 12.25 10.74 40 63681 23104 90541622
Urinary tract disorder 12.13 10.74 14 63707 3697 90561029
Finger deformity 12.11 10.74 4 63717 32893 90531833
Drug ineffective 12.10 10.74 825 62896 1383473 89181253
Night sweats 12.09 10.74 48 63673 128718 90436008
Limb injury 12.06 10.74 49 63672 31459 90533267
Vitamin B12 deficiency 11.96 10.74 20 63701 7466 90557260
Spinal stenosis 11.95 10.74 33 63688 17391 90547335
Musculoskeletal pain 11.92 10.74 71 63650 171180 90393546
Hand fracture 11.86 10.74 19 63702 6846 90557880
Sleep disorder 11.82 10.74 86 63635 197944 90366782
Optic neuritis 11.82 10.74 23 63698 9655 90555071
Colitis ulcerative 11.80 10.74 15 63706 60251 90504475
Urticaria 11.80 10.74 152 63569 312582 90252144
Bone marrow failure 11.72 10.74 4 63717 32217 90532509
Knee operation 11.72 10.74 19 63702 6917 90557809
Micturition urgency 11.71 10.74 25 63696 11208 90553518
Injection site swelling 11.62 10.74 77 63644 59762 90504964
Adverse event 11.52 10.74 43 63678 117375 90447351
Paranoia 11.52 10.74 27 63694 12881 90551845
Nerve conduction studies abnormal 11.43 10.74 3 63718 32 90564694
Neuromyelitis optica spectrum disorder 11.40 10.74 9 63712 1481 90563245
CSF immunoglobulin increased 11.39 10.74 4 63717 120 90564606
Paraplegia 11.37 10.74 13 63708 3399 90561327
Enuresis 11.36 10.74 13 63708 3401 90561325
Application site erythema 11.26 10.74 16 63705 5192 90559534
International normalised ratio increased 11.25 10.74 10 63711 47306 90517420
Autonomic nervous system imbalance 11.25 10.74 13 63708 3437 90561289
Brain death 11.23 10.74 14 63707 4007 90560719
Autoimmune thyroiditis 11.14 10.74 17 63704 5876 90558850
Magnetic resonance imaging abnormal 11.14 10.74 13 63708 3473 90561253
CD4 lymphocytes decreased 11.11 10.74 9 63712 1538 90563188
Progressive multifocal leukoencephalopathy 11.09 10.74 30 63691 15625 90549101
Spinal disorder 11.05 10.74 25 63696 11654 90553072
Acute febrile neutrophilic dermatosis 10.97 10.74 13 63708 3532 90561194
Hyperkalaemia 10.92 10.74 18 63703 64946 90499780
Neurodermatitis 10.85 10.74 12 63709 3026 90561700
Neck surgery 10.81 10.74 10 63711 2040 90562686
Increased tendency to bruise 10.75 10.74 25 63696 11865 90552861

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
Completed suicide 164.89 13.87 206 18286 96259 42506584
Multiple sclerosis relapse 110.99 13.87 72 18420 14192 42588651
Multiple sclerosis 108.84 13.87 57 18435 7541 42595302
Drug withdrawal syndrome 101.22 13.87 80 18412 21469 42581374
Potassium wasting nephropathy 67.49 13.87 14 18478 82 42602761
Failure to suspend medication 61.03 13.87 17 18475 385 42602458
Febrile neutropenia 59.14 13.87 6 18486 185697 42417146
Intervertebral disc protrusion 53.91 13.87 42 18450 11030 42591813
Muscle spasticity 51.99 13.87 34 18458 6788 42596055
Serotonin syndrome 50.24 13.87 59 18433 25786 42577057
Suspected suicide 49.96 13.87 32 18460 6167 42596676
Muscle spasms 49.64 13.87 113 18379 85931 42516912
Anxiety 46.89 13.87 135 18357 118425 42484418
Back pain 44.54 13.87 149 18343 141627 42461216
Depression 41.34 13.87 124 18368 111239 42491604
Pain 41.02 13.87 212 18280 244636 42358207
Urinary tract infection 38.22 13.87 112 18380 99172 42503671
Fall 35.15 13.87 197 18295 234323 42368520
Road traffic accident 34.50 13.87 42 18450 19051 42583792
Protein S decreased 34.02 13.87 8 18484 89 42602754
Optic nerve operation 32.58 13.87 11 18481 481 42602362
Anaemia 32.03 13.87 45 18447 280233 42322610
Accidental death 30.14 13.87 18 18474 3065 42599778
Perineal infection 29.55 13.87 11 18481 641 42602202
Neutropenia 29.37 13.87 26 18466 199405 42403438
General physical health deterioration 28.55 13.87 15 18477 151231 42451612
Hypoaesthesia 26.90 13.87 80 18412 71383 42531460
Scrotal infection 26.81 13.87 11 18481 832 42602011
Progressive multiple sclerosis 26.24 13.87 8 18484 251 42602592
Kidney enlargement 26.08 13.87 11 18481 892 42601951
Spinal fusion surgery 25.90 13.87 12 18480 1217 42601626
Infected dermal cyst 25.73 13.87 11 18481 922 42601921
Thrombocytopenia 25.46 13.87 27 18465 190252 42412591
Wrong patient received product 25.23 13.87 17 18475 3566 42599277
Hyponatraemia 24.19 13.87 7 18485 101455 42501388
Drug abuser 23.07 13.87 16 18476 3515 42599328
Tooth injury 22.64 13.87 11 18481 1240 42601603
Secondary progressive multiple sclerosis 22.48 13.87 8 18484 410 42602433
Neuralgia 22.33 13.87 40 18452 25607 42577236
Inadequate analgesia 22.11 13.87 15 18477 3182 42599661
Intracranial aneurysm 21.77 13.87 12 18480 1756 42601087
Motor dysfunction 21.77 13.87 22 18470 8124 42594719
Muscular weakness 21.27 13.87 82 18410 83416 42519427
Withdrawal syndrome 21.20 13.87 29 18463 14746 42588097
Persistent depressive disorder 21.10 13.87 8 18484 491 42602352
Off label use 20.98 13.87 177 18315 638158 41964685
Spinal cord injury cauda equina 20.98 13.87 6 18486 150 42602693
Sedation 20.96 13.87 43 18449 30432 42572411
Somatosensory evoked potentials abnormal 20.54 13.87 6 18486 162 42602681
Arteriovenous fistula 20.46 13.87 10 18482 1142 42601701
Drug dependence 19.95 13.87 41 18451 29053 42573790
Urobilinogen urine increased 19.80 13.87 7 18485 352 42602491
Albuminuria 19.59 13.87 8 18484 598 42602245
Back disorder 19.55 13.87 20 18472 7494 42595349
Pancytopenia 19 13.87 14 18478 117729 42485114
Feeling abnormal 18.99 13.87 70 18422 69716 42533127
Insomnia 18.78 13.87 101 18391 118152 42484691
Memory impairment 18.68 13.87 56 18436 50166 42552677
Toxicity to various agents 18.64 13.87 166 18326 228970 42373873
Hypotension 18.64 13.87 182 18310 257449 42345394
Gait disturbance 18.59 13.87 88 18404 97912 42504931
Movement disorder 18.35 13.87 27 18465 14671 42588172
Respiratory arrest 18.25 13.87 39 18453 28385 42574458
Unemployment 17.78 13.87 4 18488 36 42602807
Dysdiadochokinesis 17.67 13.87 6 18486 267 42602576
Urine uric acid decreased 17.48 13.87 5 18487 125 42602718
Therapy interrupted 17.23 13.87 33 18459 22217 42580626
Urinary sediment abnormal 17.22 13.87 5 18487 132 42602711
Umbilical hernia 16.97 13.87 16 18476 5431 42597412
Blood folate increased 16.74 13.87 6 18486 314 42602529
Lipomatosis 16.72 13.87 6 18486 315 42602528
Gait inability 16.63 13.87 33 18459 22800 42580043
Vitamin B6 deficiency 16.43 13.87 6 18486 331 42602512
Back injury 15.95 13.87 14 18478 4334 42598509
Balance disorder 15.75 13.87 51 18441 47594 42555249
Fear of falling 15.73 13.87 6 18486 374 42602469
False positive investigation result 15.63 13.87 7 18485 656 42602187
Disease progression 15.46 13.87 24 18468 143632 42459211
Dermal cyst 15.30 13.87 10 18482 1993 42600850
Drug tolerance 14.98 13.87 12 18480 3278 42599565
Autonomic dysreflexia 14.93 13.87 4 18488 78 42602765
Decreased vibratory sense 14.88 13.87 6 18486 434 42602409
Mental status changes 14.76 13.87 46 18446 42069 42560774
Implant site infection 14.63 13.87 8 18484 1153 42601690
Cardio-respiratory arrest 14.45 13.87 57 18435 58579 42544264
Dizziness 14.25 13.87 168 18324 249086 42353757
Anal haemorrhage 14.20 13.87 11 18481 2862 42599981
Spinal osteoarthritis 13.92 13.87 18 18474 8668 42594175
Emotional distress 13.88 13.87 25 18467 16068 42586775

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
Completed suicide 627.30 10.99 740 63951 241641 110282967
Multiple sclerosis relapse 436.24 10.99 304 64387 49936 110474672
Multiple sclerosis 274.71 10.99 177 64514 25521 110499087
Drug withdrawal syndrome 212.43 10.99 177 64514 37877 110486731
Suspected suicide 198.68 10.99 119 64572 15080 110509528
Pneumonia aspiration 175.76 10.99 227 64464 81006 110443602
Urinary tract infection 158.84 10.99 485 64206 325797 110198811
Somnolence 156.98 10.99 455 64236 296994 110227614
Synovitis 138.18 10.99 5 64686 274087 110250521
Fall 133.15 10.99 700 63991 602782 109921826
General physical health deterioration 115.69 10.99 52 64639 425243 110099365
Coma 115.03 10.99 229 64462 117640 110406968
Hand deformity 113.68 10.99 3 64688 218503 110306105
Pericarditis 107.07 10.99 5 64686 219109 110305499
Febrile neutropenia 106.49 10.99 27 64664 316740 110207868
Lower respiratory tract infection 105.80 10.99 10 64681 243096 110281512
Glossodynia 102.54 10.99 7 64684 221997 110302611
Depression 100.11 10.99 409 64282 316926 110207682
Back pain 94.88 10.99 449 64242 370547 110154061
Product dose omission issue 93.15 10.99 404 64287 321378 110203230
Helicobacter infection 92.77 10.99 3 64688 181874 110342734
Gastrooesophageal reflux disease 91.67 10.99 272 64419 179704 110344904
Off label use 89.10 10.99 515 64176 1499670 109024938
Toxicity to various agents 85.15 10.99 526 64165 480029 110044579
Systemic lupus erythematosus 84.85 10.99 22 64669 254316 110270292
Withdrawal syndrome 82.88 10.99 97 64594 31283 110493325
Neutropenia 80.33 10.99 61 64630 374559 110150049
Infusion related reaction 76.81 10.99 66 64625 381096 110143512
Maternal exposure during pregnancy 76.08 10.99 27 64664 254856 110269752
Drug intolerance 73.05 10.99 78 64613 406434 110118174
Folliculitis 72.66 10.99 7 64684 167646 110356962
Intervertebral disc protrusion 72.13 10.99 85 64606 27613 110496995
Gait disturbance 66.96 10.99 331 64360 277877 110246731
Contraindicated product administered 66.46 10.99 31 64660 248236 110276372
Pain 66.09 10.99 850 63841 954105 109570503
Migraine 65.38 10.99 235 64456 171417 110353191
Thrombocytopenia 64.87 10.99 65 64626 348820 110175788
Muscle spasms 63.46 10.99 326 64365 277831 110246777
Muscle injury 63.41 10.99 5 64686 140802 110383806
Autonomic dysreflexia 60.64 10.99 19 64672 480 110524128
Serotonin syndrome 60.19 10.99 117 64574 59036 110465572
Feeling abnormal 60.19 10.99 237 64454 180474 110344134
Cardio-respiratory arrest 57.94 10.99 174 64517 115662 110408946
Potassium wasting nephropathy 54.19 10.99 14 64677 171 110524437
Surgery 53.91 10.99 91 64600 41192 110483416
Muscle spasticity 52.07 10.99 83 64608 35832 110488776
Anxiety 50.91 10.99 361 64330 344717 110179891
Sleep disorder due to general medical condition, insomnia type 49.75 10.99 3 64688 105640 110418968
Tremor 49.62 10.99 242 64449 201990 110322618
Failure to suspend medication 48.77 10.99 16 64675 470 110524138
Headache 48.73 10.99 755 63936 881622 109642986
C-reactive protein increased 48.61 10.99 34 64657 217885 110306723
Neck pain 46.38 10.99 168 64523 122962 110401646
Hepatic enzyme increased 45.87 10.99 73 64618 320819 110203789
Treatment failure 45.66 10.99 57 64634 277177 110247431
COVID-19 45.06 10.99 271 64420 244789 110279819
Respiratory arrest 44.99 10.99 103 64588 58196 110466412
Exposure during pregnancy 44.65 10.99 21 64670 167403 110357205
Dysphoria 44.63 10.99 34 64657 6394 110518214
Joint swelling 44.58 10.99 123 64568 442722 110081886
Stiff person syndrome 43.98 10.99 16 64675 644 110523964
Pancytopenia 43.80 10.99 35 64656 209578 110315030
Impaired healing 43.47 10.99 31 64660 196686 110327922
Liver injury 43.08 10.99 17 64674 150396 110374212
Mental status changes 42.55 10.99 119 64572 76003 110448605
Hypoaesthesia 41.93 10.99 321 64370 313902 110210706
Wound 40.95 10.99 46 64645 234391 110290217
Hypersensitivity 40.81 10.99 112 64579 403886 110120722
Facet joint syndrome 39.53 10.99 5 64686 96823 110427785
Hypotension 38.98 10.99 473 64218 523376 110001232
Product administration interrupted 38.65 10.99 40 64651 11252 110513356
Influenza like illness 37.96 10.99 126 64565 88286 110436322
Neuralgia 37.80 10.99 86 64605 48392 110476216
Malignant neoplasm progression 36.65 10.99 29 64662 174538 110350070
Visual impairment 35.98 10.99 165 64526 134263 110390345
Inflammation 35.89 10.99 36 64655 193202 110331406
Lung disorder 35.24 10.99 32 64659 180015 110344593
Therapy interrupted 35.15 10.99 85 64606 49737 110474871
JC polyomavirus test positive 34.95 10.99 20 64671 2327 110522281
Balance disorder 34.93 10.99 148 64543 116412 110408196
Stomatitis 34.50 10.99 66 64625 270176 110254432
Ill-defined disorder 34.28 10.99 25 64666 156828 110367780
Spinal osteoarthritis 33.99 10.99 50 64641 20133 110504475
Irritable bowel syndrome 33.58 10.99 28 64663 164187 110360421
Injection site pain 33.49 10.99 198 64493 177724 110346884
Lumbar radiculopathy 33.21 10.99 20 64671 2558 110522050
Drug dependence 32.82 10.99 83 64608 49937 110474671
Mucosal inflammation 32.66 10.99 8 64683 96133 110428475
Urinary incontinence 32.27 10.99 81 64610 48506 110476102
Pulmonary fibrosis 31.84 10.99 10 64681 102032 110422576
Hallucination 31.34 10.99 130 64561 101302 110423306
Neurogenic bladder 31.22 10.99 25 64666 5054 110519554
Pyrexia 31.08 10.99 356 64335 897909 109626699
Cardiac failure 30.44 10.99 39 64652 187587 110337021
Progressive multiple sclerosis 30.23 10.99 15 64676 1309 110523299
Disease progression 29.94 10.99 61 64630 243973 110280635
Loss of consciousness 29.87 10.99 207 64484 196099 110328509
Drug abuser 29.84 10.99 25 64666 5384 110519224
Type 2 diabetes mellitus 29.63 10.99 36 64655 177196 110347412
Sinus bradycardia 29.60 10.99 58 64633 29425 110495183
Accidental death 29.41 10.99 24 64667 4985 110519623
Liver disorder 29.40 10.99 24 64667 142219 110382389
Dysarthria 29.35 10.99 112 64579 84009 110440599
Optic nerve operation 29.32 10.99 11 64680 483 110524125
Panic attack 29.14 10.99 57 64634 28883 110495725
Peripheral venous disease 28.57 10.99 7 64684 84110 110440498
Vision blurred 28.55 10.99 150 64541 128872 110395736
Intervertebral disc degeneration 27.89 10.99 43 64648 18042 110506566
Protein S decreased 27.73 10.99 8 64683 151 110524457
Anaemia 27.56 10.99 197 64494 546889 109977719
Illness 27.52 10.99 108 64583 82063 110442545
Spinal operation 27.46 10.99 33 64658 10939 110513669
Arthropathy 27.34 10.99 82 64609 287440 110237168
Cholestasis 27.15 10.99 3 64688 64515 110460093
Appetite disorder 27.14 10.99 31 64660 9738 110514870
Insomnia 26.96 10.99 326 64365 360264 110164344
Seizure 26.77 10.99 221 64470 220964 110303644
Bursitis 26.75 10.99 22 64669 129896 110394712
Peroneal nerve palsy 26.72 10.99 27 64664 7387 110517221
Dizziness 26.32 10.99 563 64128 697630 109826978
Acute kidney injury 25.55 10.99 243 64448 635187 109889421
Nausea 25.53 10.99 922 63769 1234768 109289840
Therapeutic product effect decreased 25.20 10.99 67 64624 244249 110280359
Thinking abnormal 24.76 10.99 37 64654 15103 110509505
Haemorrhagic diathesis 24.63 10.99 26 64665 7482 110517126
Scrotal infection 24.47 10.99 11 64680 769 110523839
Wound infection 24.36 10.99 13 64678 96452 110428156
Product use issue 24.17 10.99 97 64594 311598 110213010
Gastrointestinal disorder 23.73 10.99 68 64623 241884 110282724
False positive investigation result 23.64 10.99 13 64678 1401 110523207
Perineal infection 23.35 10.99 11 64680 856 110523752
Back disorder 23.28 10.99 43 64648 20879 110503729
Multiple organ dysfunction syndrome 23.12 10.99 33 64658 151677 110372931
Vitamin D deficiency 23.04 10.99 40 64651 18512 110506096
Muscle tightness 22.62 10.99 35 64656 14727 110509881
Secondary progressive multiple sclerosis 22.38 10.99 13 64678 1556 110523052
Hyponatraemia 22.21 10.99 60 64631 217593 110307015
Head injury 21.86 10.99 65 64626 42952 110481656
Burning sensation 21.61 10.99 89 64602 69123 110455485
Grip strength decreased 21.46 10.99 10 64681 80164 110444444
Bronchitis 21.24 10.99 161 64530 156871 110367737
Joint range of motion decreased 21.16 10.99 24 64667 121808 110402800
Ankle fracture 21.14 10.99 40 64651 19779 110504829
Therapy cessation 21.13 10.99 66 64625 44791 110479817
Inadequate analgesia 21.12 10.99 20 64671 5057 110519551
Muscular weakness 20.96 10.99 230 64461 248238 110276370
Neutrophil count decreased 20.82 10.99 24 64667 120917 110403691
Toxic epidermal necrolysis 20.73 10.99 4 64687 56723 110467885
Dermatitis atopic 20.68 10.99 46 64645 25495 110499113
Crying 20.57 10.99 46 64645 25582 110499026
Frequent bowel movements 20.55 10.99 8 64683 71382 110453226
Blood creatinine increased 20.54 10.99 48 64643 182841 110341767
Skin warm 20.41 10.99 26 64665 9144 110515464
Disturbance in attention 20.37 10.99 81 64610 61914 110462694
Platelet count decreased 20.30 10.99 68 64623 230375 110294233
Emotional distress 20.22 10.99 65 64626 44782 110479826
Nerve injury 20.19 10.99 28 64663 10685 110513923
Drug interaction 20.02 10.99 407 64284 499776 110024832
Urobilinogen urine increased 19.85 10.99 9 64682 642 110523966
Intracranial aneurysm 19.35 10.99 19 64672 5021 110519587
Urinary sediment abnormal 19.32 10.99 6 64685 147 110524461
Formication 19.32 10.99 20 64671 5628 110518980
Bone marrow failure 19.29 10.99 5 64686 57843 110466765
Spinal cord injury cauda equina 19.21 10.99 6 64685 150 110524458
Hypercholesterolaemia 19.18 10.99 15 64676 90822 110433786
Psoriatic arthropathy 18.78 10.99 56 64635 196705 110327903
Infected dermal cyst 18.78 10.99 11 64680 1337 110523271
Concussion 18.59 10.99 28 64663 11510 110513098
Nervousness 18.08 10.99 55 64636 36796 110487812
Intervertebral disc disorder 17.93 10.99 19 64672 5493 110519115
Decreased interest 17.92 10.99 18 64673 4890 110519718
Bladder disorder 17.91 10.99 27 64664 11110 110513498
Nerve compression 17.91 10.99 27 64664 11110 110513498
Memory impairment 17.87 10.99 185 64506 196759 110327849
Influenza 17.87 10.99 164 64527 168937 110355671
Injection site erythema 17.83 10.99 105 64586 94071 110430537
Blepharospasm 17.80 10.99 5 64686 54846 110469762
Paraplegia 17.78 10.99 20 64671 6180 110518428
Sleep apnoea syndrome 17.68 10.99 58 64633 40389 110484219
Respiratory rate decreased 17.62 10.99 20 64671 6238 110518370
Neuromyelitis optica spectrum disorder 17.59 10.99 11 64680 1504 110523104
Somatosensory evoked potentials abnormal 17.37 10.99 6 64685 207 110524401
Kidney enlargement 17.36 10.99 11 64680 1540 110523068
Temperature intolerance 17.22 10.99 30 64661 13920 110510688
Blood potassium decreased 17.22 10.99 70 64621 54044 110470564
Fibula fracture 17.04 10.99 17 64674 4581 110520027
Bradycardia 17.03 10.99 152 64539 155365 110369243
Impaired gastric emptying 16.98 10.99 29 64662 13246 110511362
Pneumonitis 16.98 10.99 12 64679 76519 110448089
Injection site bruising 16.86 10.99 67 64624 51196 110473412
Stress 16.56 10.99 112 64579 105236 110419372
Red blood cell sedimentation rate increased 16.44 10.99 13 64678 78289 110446319
Ascites 16.43 10.99 18 64673 92790 110431818
Photophobia 16.12 10.99 42 64649 25729 110498879
Dysdiadochokinesis 16.11 10.99 7 64684 451 110524157
Agranulocytosis 16.07 10.99 8 64683 61752 110462856
Suicidal ideation 16.06 10.99 102 64589 93835 110430773
Urine uric acid decreased 16.01 10.99 5 64686 125 110524483
Jejunectomy 15.95 10.99 4 64687 43 110524565
Blood pressure systolic increased 15.94 10.99 15 64676 82976 110441632
Coeliac disease 15.88 10.99 3 64688 43184 110481424
Tooth injury 15.86 10.99 12 64679 2234 110522374
Nail disorder 15.86 10.99 7 64684 57928 110466680
Circulatory collapse 15.78 10.99 3 64688 42990 110481618
Sedation 15.40 10.99 81 64610 69602 110455006
Neurotoxicity 15.37 10.99 3 64688 42204 110482404
Pre-existing condition improved 15.31 10.99 19 64672 6507 110518101
Arteriovenous fistula 15.30 10.99 10 64681 1475 110523133
Myalgia 15.30 10.99 198 64493 222183 110302425
Pain in extremity 15.29 10.99 383 64308 486735 110037873
Blood cholesterol increased 15.29 10.99 56 64635 184729 110339879
Leukopenia 15.19 10.99 41 64650 148750 110375858
Therapeutic response unexpected 15.06 10.99 39 64652 23804 110500804
Haematochezia 14.92 10.99 28 64663 115496 110409112
Autoimmune disorder 14.88 10.99 10 64681 65473 110459135
Movement disorder 14.84 10.99 51 64640 36353 110488255
Colitis ulcerative 14.84 10.99 14 64677 77349 110447259
Unemployment 14.72 10.99 4 64687 60 110524548
White blood cells urine positive 14.68 10.99 20 64671 7504 110517104
Irritability 14.55 10.99 61 64630 47748 110476860
Chills 14.53 10.99 173 64518 190407 110334201
Blister 14.50 10.99 76 64615 227300 110297308
Shrinking lung syndrome 14.46 10.99 5 64686 173 110524435
Vaginitis gardnerella 14.26 10.99 4 64687 68 110524540
Cytomegalovirus infection 14.25 10.99 7 64684 54437 110470171
Bedridden 14.20 10.99 27 64664 13398 110511210
Loss of control of legs 14.20 10.99 11 64680 2121 110522487
Swelling 14.19 10.99 134 64557 350907 110173701
Hyperkalaemia 14.18 10.99 37 64654 135759 110388849
Tubulointerstitial nephritis 14.17 10.99 7 64684 54277 110470331
International normalised ratio increased 14.11 10.99 18 64673 86754 110437854
Hepatocellular injury 14.05 10.99 6 64685 50636 110473972
Diplopia 13.98 10.99 55 64636 41839 110482769
Lumbar spinal stenosis 13.94 10.99 18 64673 6415 110518193
Progressive multifocal leukoencephalopathy 13.93 10.99 39 64652 24917 110499691
Liver function test increased 13.75 10.99 19 64672 88529 110436079
Melaena 13.71 10.99 12 64679 68745 110455863
Tibia fracture 13.61 10.99 18 64673 6567 110518041
Intentional product misuse 13.59 10.99 128 64563 132776 110391832
Paraparesis 13.56 10.99 15 64676 4551 110520057
Magnetic resonance imaging abnormal 13.55 10.99 14 64677 3931 110520677
Albuminuria 13.43 10.99 8 64683 1003 110523605
Hyperhidrosis 13.40 10.99 168 64523 187130 110337478
Withdrawal hypertension 13.38 10.99 6 64685 417 110524191
Lymphocyte percentage decreased 13.34 10.99 16 64675 5294 110519314
Acute myeloid leukaemia 13.28 10.99 3 64688 38107 110486501
Dysstasia 13.26 10.99 46 64645 32940 110491668
Dry skin 13.25 10.99 108 64583 107545 110417063
Ligament sprain 13.08 10.99 29 64662 16039 110508569
Foot deformity 13.04 10.99 6 64685 48474 110476134
Limb injury 13.04 10.99 50 64641 37586 110487022
Persistent depressive disorder 12.96 10.99 9 64682 1468 110523140
Dysphagia 12.86 10.99 142 64549 153458 110371150
Lipomatosis 12.86 10.99 6 64685 457 110524151
Cystitis 12.74 10.99 74 64617 65962 110458646
Lupus-like syndrome 12.72 10.99 4 64687 40788 110483820
Umbilical hernia 12.71 10.99 18 64673 7004 110517604
Asthenia 12.70 10.99 508 64183 688491 109836117
Angioedema 12.61 10.99 24 64667 98476 110426132
Renal impairment 12.57 10.99 62 64629 188383 110336225
Syncope 12.56 10.99 177 64514 202359 110322249
Urosepsis 12.53 10.99 43 64648 30632 110493976
Gastrointestinal haemorrhage 12.51 10.99 52 64639 165466 110359142
Rash maculo-papular 12.48 10.99 15 64676 74207 110450401
Drug eruption 12.46 10.99 8 64683 53651 110470957
Overdose 12.43 10.99 199 64492 233595 110291013
Injection site swelling 12.42 10.99 70 64621 61720 110462888
Myofascial pain syndrome 12.39 10.99 11 64680 2562 110522046
Initial insomnia 12.38 10.99 22 64669 10367 110514241
Device failure 12.35 10.99 18 64673 7189 110517419
Arthritis infective 12.32 10.99 22 64669 10407 110514201
Torsade de pointes 12.30 10.99 35 64656 22565 110502043
Implant site swelling 12.26 10.99 6 64685 508 110524100
Dermal cyst 12.21 10.99 12 64679 3174 110521434
Implant site infection 12.19 10.99 10 64681 2093 110522515
Urinary tract disorder 12.11 10.99 16 64675 5828 110518780
Abdominal discomfort 12.09 10.99 160 64531 393698 110130910
Device allergy 11.98 10.99 3 64688 32 110524576
Obstructive airways disorder 11.98 10.99 6 64685 46143 110478465
Spinal nerve stimulator implantation 11.96 10.99 4 64687 125 110524483
Pneumocystis jirovecii pneumonia 11.96 10.99 5 64686 42730 110481878
Palpitations 11.91 10.99 144 64547 159068 110365540
Spinal stenosis 11.86 10.99 31 64660 19025 110505583
Tenderness 11.79 10.99 41 64650 29396 110495212
Vitamin B12 deficiency 11.61 10.99 21 64670 10034 110514574
Rectal haemorrhage 11.51 10.99 34 64657 119799 110404809
Central nervous system lesion 11.47 10.99 27 64664 15526 110509082
Vitamin B6 deficiency 11.42 10.99 6 64685 590 110524018
Respiratory paralysis 11.42 10.99 4 64687 144 110524464
Blood folate increased 11.40 10.99 6 64685 592 110524016
CSF immunoglobulin increased 11.23 10.99 3 64688 42 110524566
Hyporeflexia 11.22 10.99 13 64678 4147 110520461
Stress cardiomyopathy 11.18 10.99 27 64664 15779 110508829
T-lymphocyte count decreased 11.15 10.99 6 64685 620 110523988
Zinc deficiency 11.06 10.99 5 64686 354 110524254
Arterial perforation 11.04 10.99 3 64688 45 110524563
CD4 lymphocytes decreased 11.03 10.99 11 64680 2963 110521645

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 D000316 Adrenergic alpha-Agonists
MeSH PA D000322 Adrenergic 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 D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35569 ฮฑ-adrenergic agonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:51371 muscle relaxant

Related Drugs by ATC class:

M03BX Other centrally acting agents 9 drugs

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 2MG BASE/5ML ONTRALFY FIDELITY BIOPHARMA N216190 Dec. 12, 2024 RX SOLUTION ORAL 12042484 May 7, 2042 TREATMENT OF SPASTICITY
EQ 2MG BASE/5ML ONTRALFY FIDELITY BIOPHARMA N216190 Dec. 12, 2024 RX SOLUTION ORAL 12263158 May 7, 2042 TREATMENT OF SPASTICITY

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 IC50 7.80 IUPHAR 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
37185 MMSL
44068 MMSL
5589 MMSL
d04102 MMSL
006021 NDDF
006022 NDDF
108461005 SNOMEDCT_US
108462003 SNOMEDCT_US
373440006 SNOMEDCT_US
6AI06C00GW INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2788 CAPSULE, GELATIN COATED 2 mg ORAL NDA authorized generic 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2789 CAPSULE, GELATIN COATED 4 mg ORAL NDA authorized generic 26 sections
tizanidine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2790 CAPSULE, GELATIN COATED 6 mg ORAL NDA authorized generic 26 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 19 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 27 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 29300-169 TABLET 4 mg ORAL ANDA 27 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 33261-103 TABLET 2 mg ORAL ANDA 22 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 33261-104 TABLET 4 mg ORAL ANDA 22 sections
Tizanidine HUMAN PRESCRIPTION DRUG LABEL 1 35356-662 TABLET 2 mg ORAL ANDA 27 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-810 CAPSULE, GELATIN COATED 2 mg ORAL ANDA 19 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-810 CAPSULE, GELATIN COATED 2 mg ORAL ANDA 19 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-811 CAPSULE, GELATIN COATED 4 mg ORAL ANDA 19 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-811 CAPSULE, GELATIN COATED 4 mg ORAL ANDA 19 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-812 CAPSULE, GELATIN COATED 6 mg ORAL ANDA 19 sections
Tizanidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-812 CAPSULE, GELATIN COATED 6 mg ORAL ANDA 19 sections