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

FDA Adverse Event Reporting System (Male)

MedDRA adverse event 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	112.96	13.24	70	14569	11977	31670728
Multiple sclerosis	102.51	13.24	57	14582	7980	31674725
Completed suicide	94.40	13.24	159	14480	91355	31591350
Drug withdrawal syndrome	72.78	13.24	64	14575	18686	31664019
Muscle spasticity	69.23	13.24	39	14600	5596	31677109
Potassium wasting nephropathy	65.37	13.24	14	14625	91	31682614
Muscle spasms	64.23	13.24	114	14525	68204	31614501
Failure to suspend medication	59.25	13.24	17	14622	403	31682302
Back pain	52.45	13.24	139	14500	109274	31573431
Depression	44.14	13.24	116	14523	90699	31592006
Febrile neutropenia	39.26	13.24	5	14634	121844	31560861
Intervertebral disc protrusion	39.24	13.24	33	14606	9067	31673638
Neuralgia	39.18	13.24	37	14602	11829	31670876
Serotonin syndrome	37.82	13.24	45	14594	18728	31663977
Pain	36.05	13.24	176	14463	186583	31496122
Anxiety	34.21	13.24	106	14533	90927	31591778
Urinary tract infection	32.18	13.24	93	14546	76776	31605929
Accidental death	31.80	13.24	17	14622	2200	31680505
Fall	31.46	13.24	169	14470	185920	31496785
Suspected suicide	31.40	13.24	21	14618	4086	31678619
Perineal infection	29.97	13.24	11	14628	578	31682127
Scrotal infection	29.78	13.24	11	14628	589	31682116
Anaemia	29.64	13.24	33	14606	213489	31469216
Wrong patient received product	29.52	13.24	17	14622	2542	31680163
Road traffic accident	29.33	13.24	37	14602	16344	31666361
Optic nerve operation	29.17	13.24	10	14629	430	31682275
Drug dependence	26.98	13.24	42	14597	22537	31660168
Infected dermal cyst	26.56	13.24	11	14628	800	31681905
Progressive multiple sclerosis	26.15	13.24	8	14631	238	31682467
Gait disturbance	24.40	13.24	85	14554	77410	31605295
General physical health deterioration	24.28	13.24	11	14628	113424	31569281
Neutropenia	23.84	13.24	18	14621	140346	31542359
Hypoaesthesia	23.64	13.24	68	14571	55954	31626751
Inadequate analgesia	23.60	13.24	15	14624	2678	31680027
Tooth injury	23.02	13.24	11	14628	1123	31681582
Intracranial aneurysm	22.41	13.24	12	14627	1558	31681147
Thrombocytopenia	22.14	13.24	20	14619	142727	31539978
Memory impairment	21.96	13.24	52	14587	38078	31644627
Motor dysfunction	21.37	13.24	20	14619	6319	31676386
Arteriovenous fistula	20.93	13.24	10	14629	1020	31681685
Drug abuser	20.83	13.24	16	14623	3864	31678841
Spinal cord injury cauda equina	20.76	13.24	6	14633	146	31682559
Somatosensory evoked potentials abnormal	20.46	13.24	6	14633	154	31682551
Autonomic dysreflexia	19.96	13.24	5	14634	69	31682636
False positive investigation result	19.80	13.24	7	14632	330	31682375
Vitamin B6 deficiency	19.47	13.24	6	14633	183	31682522
Pancytopenia	19.42	13.24	8	14631	87308	31595397
Dysdiadochokinesis	19.17	13.24	6	14633	193	31682512
Urobilinogen urine increased	19.07	13.24	7	14632	368	31682337
Muscular weakness	19.07	13.24	70	14569	65378	31617327
Unemployment	17.84	13.24	4	14635	33	31682672
Kidney enlargement	17.66	13.24	8	14631	723	31681982
Blood folate increased	17.64	13.24	6	14633	252	31682453
Urine uric acid decreased	17.37	13.24	5	14634	120	31682585
Insomnia	17.27	13.24	88	14551	94748	31587957
Urinary sediment abnormal	17.21	13.24	5	14634	124	31682581
Drug tolerance	17.14	13.24	12	14627	2515	31680190
Burning sensation	17.08	13.24	29	14610	16718	31665987
Movement disorder	16.79	13.24	23	14616	10996	31671709
Pain in extremity	16.61	13.24	101	14538	116102	31566603
Respiratory arrest	16.42	13.24	37	14602	26220	31656485
Malignant neoplasm progression	16.37	13.24	8	14631	78990	31603715
Off label use	16.31	13.24	94	14545	347180	31335525
Lipomatosis	16.26	13.24	6	14633	320	31682385
Dermal cyst	16.17	13.24	10	14629	1701	31681004
Fear of falling	16.05	13.24	6	14633	332	31682373
Hyponatraemia	16.03	13.24	7	14632	73792	31608913
Sedation	15.71	13.24	30	14609	18935	31663770
Respiratory paralysis	15.48	13.24	4	14635	63	31682642
Decreased vibratory sense	15.38	13.24	6	14633	373	31682332
Anal haemorrhage	15.28	13.24	11	14628	2407	31680298
Implant site infection	15.21	13.24	8	14631	1002	31681703
Migraine	15.05	13.24	25	14614	14155	31668550
Secondary progressive multiple sclerosis	15.00	13.24	6	14633	399	31682306
Back injury	15.00	13.24	13	14626	3719	31678986
Feeling abnormal	14.98	13.24	59	14580	56943	31625762
Muscle strength abnormal	14.93	13.24	4	14635	73	31682632
Musculoskeletal stiffness	14.47	13.24	47	14592	41278	31641427
Gait inability	14.30	13.24	29	14610	19115	31663590
Cardio-respiratory arrest	13.96	13.24	54	14585	51672	31631033
Lumbar radiculopathy	13.93	13.24	7	14632	797	31681908
Tendon pain	13.79	13.24	11	14628	2804	31679901
Fine motor skill dysfunction	13.79	13.24	9	14630	1681	31681024
Overdose	13.66	13.24	76	14563	84588	31598117
Umbilical hernia	13.64	13.24	13	14626	4201	31678504
Headache	13.60	13.24	137	14502	183515	31499190
Somnolence	13.31	13.24	85	14554	99360	31583345

FDA Adverse Event Reporting System (Geriatric)

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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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