tizanidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2683	51322-75-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
12	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.36 µM/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:

Date	Agency	Company	Orphan
Nov. 27, 1996	FDA	ACORDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	361.18	10.92	307	46498	42657	50515662
Pneumonia aspiration	223.30	10.92	203	46602	30801	50527518
Multiple sclerosis	187.77	10.92	154	46651	20339	50537980
Gastrooesophageal reflux disease	160.27	10.92	268	46537	76160	50482159
Somnolence	141.34	10.92	387	46418	154598	50403721
Coma	136.35	10.92	212	46593	56667	50501652
Completed suicide	136.20	10.92	345	46460	131544	50426775
Contraindicated product administered	107.18	10.92	8	46797	148950	50409369
Depression	104.09	10.92	363	46442	165060	50393259
Synovitis	97.28	10.92	4	46801	123861	50434458
Drug withdrawal syndrome	95.61	10.92	117	46688	24964	50533355
Migraine	87.28	10.92	206	46599	75074	50483245
Fall	85.03	10.92	565	46240	334367	50223952
Glossodynia	83.72	10.92	6	46799	115563	50442756
Maternal exposure during pregnancy	82.16	10.92	23	46782	159755	50398564
Muscle spasms	75.04	10.92	271	46534	125282	50433037
Systemic lupus erythematosus	69.09	10.92	22	46783	140600	50417719
Hypoaesthesia	68.00	10.92	265	46540	126992	50431327
Drug intolerance	67.43	10.92	62	46743	219042	50339277
Lower respiratory tract infection	63.40	10.92	7	46798	95194	50463125
Product dose omission issue	62.50	10.92	335	46470	183503	50374816
Neutropenia	61.45	10.92	30	46775	147935	50410384
Treatment failure	60.11	10.92	26	46779	137611	50420708
Infusion related reaction	59.63	10.92	42	46763	169515	50388804
Suspected suicide	59.26	10.92	45	46760	5312	50553007
Pericarditis	57.23	10.92	4	46801	78685	50479634
Urinary tract infection	56.17	10.92	377	46428	223643	50334676
Exposure during pregnancy	55.88	10.92	21	46784	120994	50437325
Withdrawal syndrome	54.40	10.92	74	46731	17516	50540803
Gait disturbance	54.16	10.92	278	46527	149727	50408592
Joint swelling	45.12	10.92	100	46705	245186	50313133
Stiff person syndrome	44.77	10.92	14	46791	217	50558102
Autonomic dysreflexia	43.69	10.92	15	46790	316	50558003
Neck pain	42.77	10.92	133	46672	56934	50501385
Thrombocytopenia	41.83	10.92	34	46771	127639	50430680
General physical health deterioration	39.57	10.92	44	46761	142390	50415929
Anxiety	39.27	10.92	290	46515	177316	50381003
Febrile neutropenia	38.75	10.92	21	46784	97646	50460673
Muscle spasticity	38.31	10.92	62	46743	17122	50541197
Memory impairment	37.38	10.92	159	46646	79201	50479118
Wound	34.87	10.92	28	46777	105766	50452553
Helicobacter infection	34.80	10.92	3	46802	49699	50508620
Tremor	33.46	10.92	201	46604	114702	50443617
Drug ineffective	33.31	10.92	546	46259	818787	49739532
Headache	32.69	10.92	653	46152	505882	50052437
Pancytopenia	31.99	10.92	19	46786	84011	50474308
Muscular weakness	31.46	10.92	172	46633	94841	50463478
Back pain	31.28	10.92	326	46479	219704	50338615
Malignant neoplasm progression	31.14	10.92	12	46793	68112	50490207
Sleep apnoea syndrome	30.60	10.92	68	46737	23800	50534519
Influenza like illness	30.12	10.92	119	46686	57340	50500979
Feeling abnormal	30.09	10.92	209	46596	125283	50433036
Dysphoria	30.01	10.92	29	46776	4745	50553574
Paraesthesia	29.26	10.92	201	46604	120042	50438277
Alopecia	29.20	10.92	122	46683	244925	50313394
Intervertebral disc protrusion	28.31	10.92	60	46745	20333	50537986
Insomnia	28.20	10.92	266	46539	174599	50383720
Off label use	28.10	10.92	292	46513	474134	50084185
Therapeutic product effect decreased	27.94	10.92	52	46753	135998	50422321
Rash	27.68	10.92	265	46540	437206	50121113
Hypersensitivity	26.33	10.92	106	46699	215055	50343264
Folliculitis	25.81	10.92	3	46802	39222	50519097
Vision blurred	25.11	10.92	141	46664	78506	50479813
Amnesia	25.02	10.92	91	46714	42169	50516150
Pain	23.60	10.92	701	46104	578202	49980117
Therapy interrupted	23.17	10.92	55	46750	20097	50538222
Neurogenic bladder	23.13	10.92	20	46785	2837	50555482
Cardiac failure	22.79	10.92	22	46783	76018	50482301
Vitamin D deficiency	22.56	10.92	39	46766	11363	50546956
Arthropathy	22.48	10.92	73	46732	157833	50400486
Lumbar radiculopathy	22.31	10.92	16	46789	1730	50556589
Visual impairment	22.19	10.92	123	46682	68152	50490167
Suspected product quality issue	22.13	10.92	8	46797	197	50558122
Muscle injury	21.74	10.92	4	46801	37107	50521212
Hallucination	21.59	10.92	93	46712	46564	50511755
Hepatic enzyme increased	21.35	10.92	61	46744	137319	50421000
JC polyomavirus test positive	21.04	10.92	13	46792	1096	50557223
Suicidal ideation	20.90	10.92	104	46701	55281	50503038
Blood pressure systolic increased	20.38	10.92	4	46801	35445	50522874
Balance disorder	20.23	10.92	123	46682	70467	50487852
COVID-19	20.07	10.92	91	46714	46571	50511748
Sleep disorder due to general medical condition, insomnia type	19.28	10.92	3	46802	31444	50526875
Swelling	19.27	10.92	108	46697	200764	50357555
Pre-existing condition improved	19.19	10.92	28	46777	7069	50551250
C-reactive protein increased	19.04	10.92	20	46785	66454	50491865
Formication	18.98	10.92	20	46785	3626	50554693
Therapeutic response unexpected	18.91	10.92	44	46761	15871	50542448
Therapy cessation	18.91	10.92	60	46745	25951	50532368
Spinal operation	18.85	10.92	26	46779	6234	50552085
Back disorder	18.64	10.92	32	46773	9273	50549046
Drug dependence	18.61	10.92	50	46755	19709	50538610
Rheumatoid arthritis	18.31	10.92	111	46694	202439	50355880
Respiratory arrest	18.08	10.92	65	46740	29944	50528375
Product use issue	18.04	10.92	74	46731	149401	50408918
International normalised ratio increased	17.52	10.92	9	46796	43143	50515176
Progressive multiple sclerosis	17.32	10.92	10	46795	745	50557574
Intentional product misuse	17.10	10.92	87	46718	46647	50511672
Surgery	17.00	10.92	64	46741	30141	50528178
Nervousness	16.75	10.92	60	46745	27591	50530728
Decreased interest	16.71	10.92	17	46788	2959	50555360
Acute kidney injury	16.66	10.92	133	46672	227925	50330394
Blood creatinine increased	16.63	10.92	28	46777	76132	50482187
Abdominal discomfort	16.50	10.92	136	46669	231505	50326814
Neuralgia	16.41	10.92	51	46754	21812	50536507
Peroneal nerve palsy	16.35	10.92	20	46785	4263	50554056
Anaemia	16.32	10.92	152	46653	252304	50306015
Urinary incontinence	16.07	10.92	60	46745	28148	50530171
Central nervous system lesion	15.66	10.92	30	46775	9459	50548860
Dysarthria	15.38	10.92	72	46733	37331	50520988
Disease progression	15.31	10.92	42	46763	95824	50462495
Respiratory alkalosis	15.27	10.92	15	46790	2504	50555815
Fibromyalgia	15.26	10.92	82	46723	44896	50513423
Temperature intolerance	15.20	10.92	26	46779	7513	50550806
Loss of consciousness	14.98	10.92	155	46650	104198	50454121
Secondary progressive multiple sclerosis	14.81	10.92	11	46794	1255	50557064
Intervertebral disc degeneration	14.68	10.92	36	46769	13425	50544894
Dizziness	14.48	10.92	421	46384	345948	50212371
Haemorrhagic diathesis	14.37	10.92	18	46787	3930	50554389
Cholestasis	14.32	10.92	3	46802	25398	50532921
Cardio-respiratory arrest	14.25	10.92	92	46713	53800	50504519
Neutrophil count decreased	14.16	10.92	13	46792	46013	50512306
Bone marrow failure	14.14	10.92	4	46801	27620	50530699
Impaired healing	14.03	10.92	27	46778	69759	50488560
Ankle fracture	14.02	10.92	39	46766	15683	50542636
Mucosal inflammation	14.02	10.92	10	46795	40132	50518187
Hyperhidrosis	13.88	10.92	135	46670	89291	50469028
Pneumonitis	13.81	10.92	5	46800	29505	50528814
Mental status changes	13.61	10.92	68	46737	36204	50522115
Appetite disorder	13.55	10.92	22	46783	6092	50552227
Pyrexia	13.54	10.92	259	46546	379944	50178375
Device expulsion	13.29	10.92	5	46800	28817	50529502
Hyperkalaemia	13.18	10.92	15	46790	48074	50510245
Thinking abnormal	13.11	10.92	28	46777	9539	50548780
Fibula fracture	13.04	10.92	15	46790	2997	50555322
Illness	13.00	10.92	51	46754	24489	50533830
Nasopharyngitis	12.96	10.92	115	46690	192812	50365507
Optic neuritis	12.90	10.92	23	46782	6867	50551452
Hepatocellular injury	12.84	10.92	4	46801	25943	50532376
Nerve compression	12.82	10.92	24	46781	7438	50550881
Spinal fusion acquired	12.77	10.92	3	46802	14	50558305
Hypertonia	12.72	10.92	17	46788	3956	50554363
Relapsing-remitting multiple sclerosis	12.66	10.92	7	46798	480	50557839
Panic attack	12.61	10.92	43	46762	19299	50539020
Cervical spinal stenosis	12.58	10.92	12	46793	1931	50556388
Impaired gastric emptying	12.51	10.92	26	46779	8692	50549627
Multiple organ dysfunction syndrome	12.44	10.92	17	46788	50320	50507999
Ascites	12.44	10.92	9	46796	35852	50522467
Loss of control of legs	12.38	10.92	10	46795	1291	50557028
Normocytic anaemia	12.21	10.92	10	46795	1317	50557002
Head injury	11.98	10.92	49	46756	23971	50534348
Blood pressure orthostatic	11.84	10.92	4	46801	80	50558239
Gastrointestinal haemorrhage	11.80	10.92	32	46773	73289	50485030
Muscle tightness	11.75	10.92	28	46777	10252	50548067
Spinal osteoarthritis	11.64	10.92	34	46771	14058	50544261
Road traffic accident	11.62	10.92	49	46756	24303	50534016
Urosepsis	11.54	10.92	36	46769	15429	50542890
Underdose	11.44	10.92	43	46762	20235	50538084
Drug dependence, antepartum	11.28	10.92	3	46802	25	50558294
Gastrointestinal disorder	11.24	10.92	47	46758	94409	50463910
Seizure	11.21	10.92	162	46643	117712	50440607
Back injury	11.20	10.92	22	46783	7063	50551256
Acute febrile neutrophilic dermatosis	11.17	10.92	13	46792	2629	50555690
Loss of bladder sensation	11.08	10.92	3	46802	27	50558292
Bronchitis	11.06	10.92	146	46659	104013	50454306
Tremor neonatal	11.05	10.92	4	46801	99	50558220
Diplopia	11.00	10.92	41	46764	19219	50539100

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	113.95	13.42	69	13567	11350	29549541
Multiple sclerosis	110.24	13.42	53	13583	5501	29555390
Completed suicide	96.27	13.42	159	13477	90087	29470804
Drug withdrawal syndrome	73.16	13.42	63	13573	17921	29542970
Potassium wasting nephropathy	65.39	13.42	14	13622	91	29560800
Muscle spasticity	57.89	13.42	33	13603	4850	29556041
Failure to suspend medication	55.92	13.42	16	13620	376	29560515
Depression	46.99	13.42	114	13522	85033	29475858
Muscle spasms	46.98	13.42	97	13539	64985	29495906
Back pain	43.25	13.42	124	13512	102160	29458731
Intervertebral disc protrusion	38.59	13.42	32	13604	8638	29552253
Febrile neutropenia	35.15	13.42	5	13631	112235	29448656
Pain	35.01	13.42	164	13472	171268	29389623
Urinary tract infection	33.80	13.42	91	13545	72263	29488628
Suspected suicide	31.84	13.42	21	13615	3999	29556892
Accidental death	29.73	13.42	16	13620	2102	29558789
Wrong patient received product	28.61	13.42	16	13620	2266	29558625
Anxiety	28.18	13.42	95	13541	85270	29475621
Drug dependence	27.92	13.42	41	13595	20940	29539951
Fall	27.47	13.42	157	13479	177021	29383870
Progressive multiple sclerosis	26.56	13.42	8	13628	226	29560665
Anaemia	25.72	13.42	33	13603	200918	29359973
Gait disturbance	25.43	13.42	83	13553	73266	29487625
Hypoaesthesia	24.71	13.42	67	13569	53400	29507491
Inadequate analgesia	23.82	13.42	15	13621	2639	29558252
Motor dysfunction	22.54	13.42	20	13616	5910	29554981
Memory impairment	22.45	13.42	51	13585	36419	29524472
Neuralgia	21.82	13.42	26	13610	10848	29550043
Drug abuser	21.05	13.42	16	13620	3811	29557080
Neutropenia	20.91	13.42	18	13618	131693	29429198
Spinal cord injury cauda equina	20.77	13.42	6	13630	146	29560745
Somatosensory evoked potentials abnormal	20.54	13.42	6	13630	152	29560739
General physical health deterioration	20.40	13.42	11	13625	102846	29458045
Autonomic dysreflexia	19.97	13.42	5	13631	69	29560822
Vitamin B6 deficiency	19.74	13.42	6	13630	175	29560716
Thrombocytopenia	19.55	13.42	20	13616	134803	29426088
Dysdiadochokinesis	19.21	13.42	6	13630	192	29560699
Urobilinogen urine increased	19.14	13.42	7	13629	365	29560526
Drug tolerance	18.90	13.42	12	13624	2141	29558750
Road traffic accident	18.70	13.42	29	13607	15532	29545359
Movement disorder	18.16	13.42	23	13613	10214	29550677
Kidney enlargement	17.93	13.42	8	13628	699	29560192
Unemployment	17.85	13.42	4	13632	33	29560858
Pancytopenia	17.84	13.42	8	13628	83160	29477731
Blood folate increased	17.65	13.42	6	13630	252	29560639
Sedation	17.60	13.42	30	13606	17375	29543516
Insomnia	17.40	13.42	84	13552	88677	29472214
Urine uric acid decreased	17.37	13.42	5	13631	120	29560771
Urinary sediment abnormal	17.22	13.42	5	13631	124	29560767
Pain in extremity	17.17	13.42	98	13538	110335	29450556
Respiratory arrest	16.87	13.42	37	13599	25796	29535095
Burning sensation	16.82	13.42	28	13608	15910	29544981
Lipomatosis	16.38	13.42	6	13630	314	29560577
Fear of falling	16.10	13.42	6	13630	330	29560561
Secondary progressive multiple sclerosis	15.63	13.42	6	13630	358	29560533
Muscle strength abnormal	15.61	13.42	4	13632	61	29560830
Decreased vibratory sense	15.50	13.42	6	13630	366	29560525
Respiratory paralysis	15.49	13.42	4	13632	63	29560828
Implant site infection	15.40	13.42	8	13628	978	29559913
Musculoskeletal stiffness	15.39	13.42	45	13591	37413	29523478
Gait inability	15.17	13.42	29	13607	18346	29542545
Mobility decreased	14.70	13.42	35	13601	25745	29535146
Headache	14.56	13.42	133	13503	173874	29387017
Fine motor skill dysfunction	14.51	13.42	9	13627	1542	29559349
Malignant neoplasm progression	14.49	13.42	8	13628	73851	29487040
Osteochondrosis	13.92	13.42	7	13629	800	29560091
Cardio-respiratory arrest	13.85	13.42	53	13583	50548	29510343
Muscular weakness	13.83	13.42	61	13575	61991	29498900
Hyponatraemia	13.75	13.42	7	13629	67626	29493265
Back injury	13.74	13.42	12	13624	3472	29557419
Spinal fusion surgery	13.58	13.42	7	13629	842	29560049

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	369.40	11.09	278	47179	40857	64410418
Multiple sclerosis	254.49	11.09	164	47293	18777	64432498
Completed suicide	227.00	11.09	506	46951	223908	64227367
Drug withdrawal syndrome	156.19	11.09	151	47306	31140	64420135
Pneumonia aspiration	153.07	11.09	203	47254	59068	64392207
Gastrooesophageal reflux disease	140.08	11.09	233	47224	82910	64368365
Somnolence	118.47	11.09	374	47083	203271	64248004
Depression	104.18	11.09	334	47123	182957	64268318
Urinary tract infection	99.69	11.09	385	47072	231211	64220064
Coma	99.16	11.09	207	47250	87408	64363867
Migraine	96.76	11.09	169	47288	62508	64388767
Muscle spasms	93.22	11.09	271	47186	140752	64310523
Fall	89.46	11.09	568	46889	416258	64035017
Hypoaesthesia	81.29	11.09	256	47201	138852	64312423
Suspected suicide	78.75	11.09	59	47398	8595	64442680
Neutropenia	77.17	11.09	40	47417	239584	64211691
Febrile neutropenia	72.22	11.09	24	47433	187633	64263642
Muscle spasticity	71.31	11.09	74	47383	16595	64434680
Gait disturbance	67.43	11.09	278	47179	171877	64279398
Pain	63.68	11.09	654	46803	552857	63898418
Autonomic dysreflexia	59.88	11.09	19	47438	394	64450881
Intervertebral disc protrusion	58.11	11.09	73	47384	20118	64431157
Thrombocytopenia	56.42	11.09	49	47408	223752	64227523
General physical health deterioration	56.25	11.09	41	47416	204384	64246891
Back pain	54.82	11.09	343	47114	249828	64201447
Potassium wasting nephropathy	52.68	11.09	14	47443	150	64451125
Neck pain	50.38	11.09	128	47329	61405	64389870
Withdrawal syndrome	49.48	11.09	73	47384	23419	64427856
Pancytopenia	49.04	11.09	22	47435	143287	64307988
Lower respiratory tract infection	46.58	11.09	7	47450	94607	64356668
Stiff person syndrome	46.19	11.09	14	47443	248	64451027
Failure to suspend medication	44.08	11.09	15	47442	390	64450885
Headache	44.06	11.09	588	46869	528879	63922396
Product dose omission issue	43.25	11.09	268	47189	194479	64256796
Off label use	42.56	11.09	282	47175	632524	63818751
Acute kidney injury	42.00	11.09	179	47278	449061	64002214
Contraindicated product administered	39.40	11.09	15	47442	107814	64343461
Malignant neoplasm progression	39.13	11.09	17	47440	112854	64338421
Memory impairment	38.89	11.09	145	47312	85537	64365738
Insomnia	37.10	11.09	261	47196	197575	64253700
Infusion related reaction	35.70	11.09	41	47416	164426	64286849
Feeling abnormal	34.93	11.09	192	47265	133410	64317865
Anxiety	34.93	11.09	262	47195	202387	64248888
Pericarditis	34.83	11.09	3	47454	62513	64388762
Cardiac failure	34.54	11.09	28	47429	132345	64318930
Drug dependence	34.54	11.09	76	47381	33236	64418039
Maternal exposure during pregnancy	33.94	11.09	14	47443	95870	64355405
Anaemia	33.48	11.09	154	47303	378526	64072749
Lumbar radiculopathy	33.36	11.09	19	47438	1738	64449537
Glossodynia	31.35	11.09	5	47452	64691	64386584
Influenza like illness	31.04	11.09	108	47349	61594	64389681
Progressive multiple sclerosis	31.02	11.09	14	47443	782	64450493
Visual impairment	30.05	11.09	121	47336	73956	64377319
Muscular weakness	30.00	11.09	178	47279	127160	64324115
Drug intolerance	29.98	11.09	58	47399	187934	64263341
Treatment failure	28.90	11.09	26	47431	116790	64334485
Blood creatinine increased	27.20	11.09	36	47421	135746	64315529
Neurogenic bladder	27.12	11.09	22	47435	3597	64447678
Respiratory arrest	26.01	11.09	92	47365	52893	64398382
Road traffic accident	24.17	11.09	63	47394	30682	64420593
Cardio-respiratory arrest	24.12	11.09	139	47318	98254	64353021
Mucosal inflammation	24.06	11.09	8	47449	62576	64388699
Platelet count decreased	24.00	11.09	55	47402	167656	64283619
Dysphoria	23.45	11.09	22	47435	4366	64446909
Drug abuser	23.44	11.09	25	47432	5783	64445492
Urinary incontinence	23.39	11.09	69	47388	36082	64415193
Hyperkalaemia	23.28	11.09	24	47433	101105	64350170
Hypersensitivity	23.13	11.09	71	47386	196381	64254894
JC polyomavirus test positive	22.24	11.09	13	47444	1249	64450026
Neuralgia	21.98	11.09	55	47402	26129	64425146
Inadequate analgesia	21.37	11.09	20	47437	3958	64447317
Mental status changes	21.01	11.09	95	47362	61067	64390208
Tremor	20.83	11.09	183	47274	148047	64303228
Exposure during pregnancy	20.80	11.09	16	47441	77659	64373616
Bone marrow failure	20.52	11.09	5	47452	47947	64403328
International normalised ratio increased	20.33	11.09	17	47440	79150	64372125
Dizziness	20.31	11.09	436	47021	429727	64021548
Multiple organ dysfunction syndrome	20.20	11.09	27	47430	101386	64349889
Joint swelling	19.96	11.09	86	47371	215296	64235979
Paraesthesia	19.91	11.09	168	47289	134354	64316921
Peroneal nerve palsy	19.90	11.09	22	47435	5299	64445976
Vision blurred	19.84	11.09	124	47333	90192	64361083
Secondary progressive multiple sclerosis	19.81	11.09	12	47445	1231	64450044
Systemic lupus erythematosus	19.52	11.09	17	47440	77595	64373680
Gait inability	19.46	11.09	72	47385	42296	64408979
Back injury	19.14	11.09	26	47431	7731	64443544
Hallucination	18.60	11.09	104	47353	72684	64378591
Muscle tightness	18.49	11.09	31	47426	11084	64440191
Gastrointestinal haemorrhage	18.44	11.09	44	47413	132268	64319007
Disease progression	18.29	11.09	49	47408	141631	64309644
Urinary sediment abnormal	18.29	11.09	6	47451	139	64451136
Back disorder	18.16	11.09	29	47428	9961	64441314
Amnesia	18.12	11.09	77	47380	48192	64403083
Dysarthria	18.02	11.09	89	47368	59317	64391958
Spinal cord injury cauda equina	18.01	11.09	6	47451	146	64451129
Pyrexia	18.00	11.09	296	47161	558348	63892927
Toxic epidermal necrolysis	17.72	11.09	3	47454	37163	64414112
Ascites	17.61	11.09	12	47445	61989	64389286
Panic attack	17.57	11.09	44	47413	20909	64430366
Spinal osteoarthritis	17.53	11.09	35	47422	14306	64436969
Vitamin D deficiency	17.35	11.09	31	47426	11661	64439614
Drug hypersensitivity	17.23	11.09	258	47199	237557	64213718
Intervertebral disc degeneration	17.22	11.09	33	47424	13087	64438188
Hyponatraemia	17.18	11.09	54	47403	148285	64302990
Balance disorder	17.06	11.09	113	47344	83813	64367462
Hepatocellular injury	17.01	11.09	6	47451	45229	64406046
Somatosensory evoked potentials abnormal	16.79	11.09	6	47451	181	64451094
Accidental death	16.77	11.09	17	47440	3708	64447567
Surgery	16.52	11.09	52	47405	28161	64423114
Renal impairment	16.46	11.09	48	47409	134969	64316306
Thinking abnormal	16.33	11.09	30	47427	11526	64439749
Formication	16.27	11.09	18	47439	4339	64446936
Atrial fibrillation	16.04	11.09	68	47389	171021	64280254
Neutrophil count decreased	15.94	11.09	20	47437	77176	64374099
Pain in extremity	15.86	11.09	312	47145	302773	64148502
Melaena	15.70	11.09	10	47447	53538	64397737
Therapy interrupted	15.69	11.09	41	47416	19995	64431280
Cytomegalovirus infection	15.68	11.09	4	47453	37195	64414080
Therapy cessation	15.59	11.09	56	47401	32433	64418842
Burning sensation	15.49	11.09	75	47382	49589	64401686
C-reactive protein increased	15.37	11.09	29	47428	94880	64356395
Urobilinogen urine increased	15.23	11.09	8	47449	624	64450651
Movement disorder	15.21	11.09	43	47414	21957	64429318
Urine uric acid decreased	15.07	11.09	5	47452	120	64451155
Angioedema	15	11.09	14	47443	61807	64389468
Renal failure	14.80	11.09	76	47381	181612	64269663
Bladder disorder	14.74	11.09	23	47434	7744	64443531
Unemployment	14.64	11.09	4	47453	48	64451227
Spinal operation	14.29	11.09	20	47437	6113	64445162
Vitamin B6 deficiency	14.21	11.09	6	47451	285	64450990
Motor dysfunction	14.19	11.09	28	47429	11345	64439930
Loss of control of legs	14.17	11.09	11	47446	1688	64449587
Productive cough	14.06	11.09	20	47437	73183	64378092
Nerve compression	14.03	11.09	22	47435	7439	64443836
Paraparesis	14.00	11.09	15	47442	3487	64447788
Bedridden	13.98	11.09	26	47431	10083	64441192
Leukopenia	13.84	11.09	34	47423	101208	64350067
Arterial perforation	13.83	11.09	3	47454	12	64451263
Fibula fracture	13.73	11.09	14	47443	3074	64448201
Dysdiadochokinesis	13.72	11.09	6	47451	311	64450964
Respiratory paralysis	13.63	11.09	4	47453	63	64451212
Circulatory collapse	13.52	11.09	4	47453	33728	64417547
Appetite disorder	13.49	11.09	20	47437	6441	64444834
Interstitial lung disease	13.22	11.09	33	47424	97699	64353576
Product quality issue	13.15	11.09	50	47407	29749	64421526
Wrong patient received product	13.12	11.09	15	47442	3747	64447528
Concussion	13.02	11.09	22	47435	7916	64443359
Haemoglobin decreased	13.01	11.09	87	47370	194976	64256299
Asthenia	12.92	11.09	409	47048	427635	64023640
Haemorrhagic diathesis	12.88	11.09	18	47439	5496	64445779
pH urine decreased	12.82	11.09	3	47454	18	64451257
Head injury	12.80	11.09	53	47404	32789	64418486
Intentional product misuse	12.73	11.09	94	47363	72201	64379074
Pneumonitis	12.70	11.09	11	47446	50354	64400921
Fibromyalgia	12.64	11.09	56	47401	35675	64415600
Epistaxis	12.61	11.09	34	47423	98097	64353178
Lipomatosis	12.54	11.09	6	47451	383	64450892
Septic shock	12.47	11.09	38	47419	105399	64345876
Ankle fracture	12.45	11.09	31	47426	14679	64436596
Hepatotoxicity	12.36	11.09	7	47450	39955	64411320
Device allergy	12.30	11.09	3	47454	22	64451253
Osteonecrosis of jaw	12.29	11.09	7	47450	39818	64411457
Nerve injury	12.21	11.09	21	47436	7664	64443611
Implant site infection	12.20	11.09	10	47447	1659	64449616
Lymphocyte percentage decreased	12.11	11.09	16	47441	4633	64446642
Implant site swelling	12.07	11.09	6	47451	417	64450858
Stress	12.00	11.09	81	47376	60453	64390822
CSF immunoglobulin increased	11.96	11.09	3	47454	25	64451250
Drug dependence, antepartum	11.96	11.09	3	47454	25	64451250
Hepatic enzyme increased	11.96	11.09	52	47405	129891	64321384
Tibia fracture	11.85	11.09	16	47441	4729	64446546
Spinal fusion surgery	11.80	11.09	14	47443	3637	64447638
Tubulointerstitial nephritis	11.79	11.09	4	47453	30905	64420370
Nervousness	11.76	11.09	48	47409	29508	64421767
White blood cells urine positive	11.69	11.09	17	47440	5381	64445894
Loss of consciousness	11.54	11.09	163	47294	148202	64303073
Medical device site pain	11.51	11.09	5	47452	255	64451020
Acute myeloid leukaemia	11.49	11.09	3	47454	27460	64423815
Neurotoxicity	11.45	11.09	3	47454	27401	64423874
Kidney enlargement	11.43	11.09	8	47449	1048	64450227
Agranulocytosis	11.40	11.09	7	47450	38222	64413053
Injection site bruising	11.39	11.09	55	47402	36318	64414957
Impaired gastric emptying	11.38	11.09	22	47435	8782	64442493
Muscle strength abnormal	11.38	11.09	4	47453	115	64451160
Mucosa vesicle	11.30	11.09	3	47454	32	64451243
Blood folate increased	11.29	11.09	6	47451	479	64450796
T-lymphocyte count decreased	11.27	11.09	6	47451	481	64450794
Bronchitis	11.25	11.09	126	47331	108617	64342658
Acute febrile neutrophilic dermatosis	11.15	11.09	13	47444	3316	64447959
Temperature intolerance	11.13	11.09	21	47436	8234	64443041
Intervertebral disc disorder	11.09	11.09	15	47442	4442	64446833

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.01	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	EC50	7.07	CHEMBL	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	AGONIST			WOMBAT-PK	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	AGONIST	EC50	5.91	CHEMBL	CHEMBL
Nischarin	Membrane receptor	Q9Y2I1	NISCH_HUMAN		Ki	7.55	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		EC50	6.58	CHEMBL
Alpha-1B adrenergic receptor	GPCR		G3HDX1_CRIGR		EC50	6.49	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	0591-2789	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	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
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