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

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

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

FDA Adverse Event Reporting System (Male)

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

FDA Adverse Event Reporting System (Geriatric)

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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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	D000927	Anticonvulsants
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D000322	Adrenergic Agonists
MeSH PA	D058647	Adrenergic alpha-2 Receptor Agonists
MeSH PA	D000316	Adrenergic alpha-Agonists
MeSH PA	D000700	Analgesics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D009125	Muscle Relaxants, Central
MeSH PA	D009465	Neuromuscular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D010276	Parasympatholytics
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
CHEBI has role	CHEBI:35569	alpha-adrenergic agonists
CHEBI has role	CHEBI:51371	muscle relaxants

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

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	0591-2788	CAPSULE, GELATIN COATED	2 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2789	CAPSULE, GELATIN COATED	4 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2789	CAPSULE, GELATIN COATED	4 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2789	CAPSULE, GELATIN COATED	4 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2790	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2790	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	26 sections
tizanidine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2790	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	26 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-5574	TABLET	4 mg	ORAL	ANDA	25 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-6564	TABLET	2 mg	ORAL	ANDA	25 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8274	TABLET	4 mg	ORAL	ANDA	27 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8274	TABLET	4 mg	ORAL	ANDA	27 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8360	TABLET	2 mg	ORAL	ANDA	27 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8360	TABLET	2 mg	ORAL	ANDA	27 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8468	TABLET	2 mg	ORAL	ANDA	26 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8469	TABLET	4 mg	ORAL	ANDA	26 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6418	TABLET	4 mg	ORAL	ANDA	18 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6418	TABLET	4 mg	ORAL	ANDA	18 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6898	TABLET	4 mg	ORAL	ANDA	27 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	10544-576	TABLET	4 mg	ORAL	ANDA	20 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	10544-587	TABLET	2 mg	ORAL	ANDA	18 sections
tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	10544-863	TABLET	2 mg	ORAL	ANDA	18 sections
Tizanidine	HUMAN PRESCRIPTION DRUG LABEL	1	10544-890	TABLET	4 mg	ORAL	ANDA	22 sections
TIZANIDINE	HUMAN PRESCRIPTION DRUG LABEL	1	16590-220	TABLET	2 mg	ORAL	ANDA	16 sections
TIZANIDINE	HUMAN PRESCRIPTION DRUG LABEL	1	16590-221	TABLET	4 mg	ORAL	ANDA	16 sections
ZANAFLEX	HUMAN PRESCRIPTION DRUG LABEL	1	16590-756	CAPSULE	6 mg	ORAL	NDA	24 sections
ZANAFLEX	HUMAN PRESCRIPTION DRUG LABEL	1	16590-871	CAPSULE	4 mg	ORAL	NDA	24 sections