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

Stem definition	Drug id	CAS RN
	2750	5011-34-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: kyurinett trimetazidine vastarel trimetazidine hydrochloride trimetazidine dihydrochloride trimetazidine HCl	A vasodilator used in angina of effort or ischemic heart disease. Molecular weight: 266.34 Formula: C14H22N2O3 CLOGP: 1.27 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 42.96 ALOGS: -2.55 ROTB: 5

Molecule

Description

Molfile Inchi Smiles

Synonyms:

kyurinett
trimetazidine
vastarel
trimetazidine hydrochloride
trimetazidine dihydrochloride
trimetazidine HCl

A vasodilator used in angina of effort or ischemic heart disease.

Molecular weight: 266.34
Formula: C14H22N2O3
CLOGP: 1.27
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 42.96
ALOGS: -2.55
ROTB: 5

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	62 %	Benet LZ, Broccatelli F, Oprea TI

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1978	YEAR INTRODUCED

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
Tachypnoea	65.95	30.81	24	2114	17278	63469606
Cardiac failure	49.32	30.81	33	2105	89109	63397775
Apraxia	46.17	30.81	11	2127	1810	63485074
Perseveration	46.12	30.81	8	2130	267	63486617
Lipohypertrophy	45.01	30.81	9	2129	656	63486228
Hydrothorax	41.99	30.81	9	2129	922	63485962
Ocular hypertension	40.91	30.81	9	2129	1041	63485843
Angina pectoris	40.76	30.81	20	2118	30058	63456826
Immune-mediated myositis	38.70	30.81	9	2129	1334	63485550
Product substitution error	37.71	30.81	5	2133	24	63486860
Drug interaction	37.16	30.81	42	2096	229089	63257795
Cardiac ventricular disorder	35.37	30.81	6	2132	175	63486709
Disorientation	32.95	30.81	19	2119	39433	63447451
Oedema peripheral	32.87	30.81	36	2102	189475	63297409
Stenosis	32.83	30.81	8	2130	1446	63485438
Angina unstable	31.39	30.81	11	2127	7084	63479800

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
Cardiac failure	170.15	26.51	112	3712	91136	34861971
Rales	143.10	26.51	50	3774	9833	34943274
Dyspnoea at rest	133.91	26.51	38	3786	3790	34949317
Ejection fraction decreased	130.47	26.51	56	3768	19098	34934009
Tricuspid valve incompetence	117.22	26.51	43	3781	9717	34943390
Stenosis	101.35	26.51	25	3799	1448	34951659
Diastolic dysfunction	99.78	26.51	34	3790	6193	34946914
Pericardial disease	94.26	26.51	19	3805	431	34952676
Pulmonary valve disease	93.20	26.51	18	3806	325	34952782
Hepatic vein dilatation	80.78	26.51	15	3809	217	34952890
Bundle branch block left	77.94	26.51	28	3796	5951	34947156
Liver palpable	77.14	26.51	15	3809	281	34952826
Mitral valve incompetence	74.02	26.51	35	3789	14908	34938199
Physical examination abnormal	69.94	26.51	14	3810	306	34952801
Hyperlipidaemia	68.81	26.51	33	3791	14496	34938611
Coronary artery stenosis	68.34	26.51	29	3795	9587	34943520
Acute myocardial infarction	65.35	26.51	51	3773	53668	34899439
Atrial enlargement	64.88	26.51	15	3809	657	34952450
Angina pectoris	64.33	26.51	41	3783	31322	34921785
Inferior vena cava dilatation	63.04	26.51	15	3809	745	34952362
Cardiac discomfort	60.80	26.51	14	3810	602	34952505
Ventricular enlargement	59.76	26.51	14	3810	650	34952457
Electrocardiogram Q wave abnormal	59.59	26.51	13	3811	436	34952671
Ventricular arrhythmia	57.73	26.51	22	3802	5506	34947601
Hepatojugular reflux	55.82	26.51	13	3811	588	34952519
Left ventricular enlargement	53.81	26.51	13	3811	689	34952418
Cardiac failure chronic	53.46	26.51	23	3801	7856	34945251
Left ventricular dysfunction	51.27	26.51	24	3800	9983	34943124
Occult blood	51.07	26.51	13	3811	855	34952252
Base excess decreased	50.24	26.51	10	3814	212	34952895
Cardiomegaly	49.61	26.51	27	3797	15411	34937696
Mitral valve disease	49.21	26.51	14	3810	1405	34951702
Echocardiogram abnormal	48.46	26.51	13	3811	1050	34952057
Systolic dysfunction	48.16	26.51	16	3808	2692	34950415
Helicobacter gastritis	46.51	26.51	13	3811	1223	34951884
Supraventricular tachycardia	45.90	26.51	23	3801	11094	34942013
Carotid arteriosclerosis	45.48	26.51	14	3810	1844	34951263
Carotid artery stenosis	45.41	26.51	18	3806	5001	34948106
Cardiac murmur	43.90	26.51	20	3804	7817	34945290
Linear IgA disease	42.99	26.51	13	3811	1613	34951494
Oxygen consumption decreased	42.82	26.51	9	3815	252	34952855
Hypokinesia	41.51	26.51	20	3804	8860	34944247
Breath sounds abnormal	39.93	26.51	18	3806	6863	34946244
Ventricular hypokinesia	36.98	26.51	16	3808	5536	34947571
Aortic valve incompetence	36.03	26.51	16	3808	5888	34947219
Anaemia macrocytic	35.07	26.51	13	3811	3013	34950094
Left ventricular hypertrophy	34.08	26.51	17	3807	8113	34944994
Hypertrophy	32.59	26.51	8	3816	453	34952654
Angiopathy	31.02	26.51	13	3811	4160	34948947
Mean cell haemoglobin decreased	30.01	26.51	10	3814	1696	34951411
Renal cyst	29.47	26.51	16	3808	9077	34944030
Congestive cardiomyopathy	29.42	26.51	15	3809	7495	34945612
Wrong patient received product	29.29	26.51	11	3813	2643	34950464
Intestinal obstruction	28.42	26.51	22	3802	22800	34930307
International normalised ratio decreased	26.66	26.51	12	3812	4555	34948552

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
Cardiac failure	204.65	25.70	133	5823	154709	79583723
Rales	145.06	25.70	55	5901	19946	79718486
Stenosis	139.08	25.70	33	5923	2389	79736043
Dyspnoea at rest	128.19	25.70	39	5917	7263	79731169
Tricuspid valve incompetence	113.96	25.70	46	5910	19666	79718766
Ejection fraction decreased	112.98	25.70	54	5902	34523	79703909
Angina pectoris	103.22	25.70	58	5898	51674	79686758
Pulmonary valve disease	101.97	25.70	18	5938	290	79738142
Pericardial disease	96.43	25.70	19	5937	568	79737864
Diastolic dysfunction	94.07	25.70	34	5922	10777	79727655
Coronary artery stenosis	89.30	25.70	34	5922	12450	79725982
Hepatic vein dilatation	85.49	25.70	15	5941	233	79738199
Liver palpable	79.87	25.70	15	5941	346	79738086
Physical examination abnormal	75.75	25.70	14	5942	295	79738137
Bundle branch block left	73.96	25.70	29	5927	11484	79726948
Cardiac failure chronic	71.36	25.70	28	5928	11107	79727325
Hyperlipidaemia	71.03	25.70	36	5920	26057	79712375
Cardiomegaly	70.70	25.70	36	5920	26316	79712116
Ventricular arrhythmia	70.22	25.70	26	5930	8814	79729618
Left ventricular dysfunction	68.63	25.70	32	5924	19329	79719103
Acute myocardial infarction	68.41	25.70	52	5904	76984	79661448
Mitral valve incompetence	67.96	25.70	36	5920	28529	79709903
Inferior vena cava dilatation	66.69	25.70	15	5941	856	79737576
Atrial enlargement	64.00	25.70	15	5941	1028	79737404
Ventricular enlargement	63.71	25.70	14	5942	718	79737714
Electrocardiogram Q wave abnormal	60.14	25.70	13	5943	617	79737815
Hepatojugular reflux	59.78	25.70	13	5943	635	79737797
Left ventricular enlargement	57.95	25.70	13	5943	733	79737699
Cardiac discomfort	55.84	25.70	14	5942	1274	79737158
Systolic dysfunction	52.90	25.70	17	5939	3778	79734654
Ventricular hypokinesia	51.36	25.70	21	5935	9258	79729174
Tachypnoea	50.85	25.70	31	5925	32032	79706400
Oedema peripheral	49.11	25.70	76	5880	252212	79486220
Base excess decreased	48.53	25.70	10	5946	376	79738056
Occult blood	47.14	25.70	13	5943	1710	79736722
Carotid arteriosclerosis	45.81	25.70	14	5942	2642	79735790
Echocardiogram abnormal	43.84	25.70	13	5943	2215	79736217
Mitral valve disease	43.25	25.70	14	5942	3183	79735249
Supraventricular tachycardia	42.80	25.70	24	5932	21246	79717186
Helicobacter gastritis	42.63	25.70	13	5943	2436	79735996
Oxygen consumption decreased	41.16	25.70	9	5947	451	79737981
Atrial fibrillation	40.43	25.70	61	5895	197825	79540607
Linear IgA disease	39.48	25.70	13	5943	3119	79735313
Carotid artery stenosis	39.06	25.70	17	5939	8741	79729691
Hypertension	38.93	25.70	80	5876	330912	79407520
Cardiac murmur	37.78	25.70	20	5936	15804	79722628
Aortic valve incompetence	37.68	25.70	17	5939	9513	79728919
Congestive cardiomyopathy	37.24	25.70	18	5938	11762	79726670
Angina unstable	36.97	25.70	20	5936	16507	79721925
Perseveration	36.82	25.70	8	5948	389	79738043
Anaemia macrocytic	35.59	25.70	14	5942	5583	79732849
Coronary artery occlusion	35.56	25.70	19	5937	15296	79723136
Lipohypertrophy	35.31	25.70	9	5947	875	79737557
Breath sounds abnormal	34.80	25.70	19	5937	15965	79722467
Renal cyst	33.43	25.70	18	5938	14714	79723718
Apraxia	32.55	25.70	11	5945	2856	79735576
Arteriosclerosis	32.47	25.70	19	5937	18208	79720224
Left ventricular hypertrophy	32.09	25.70	16	5940	11175	79727257
Drug interaction	31.97	25.70	85	5871	415098	79323334
Hypokinesia	31.68	25.70	19	5937	19041	79719391
Hypertrophy	31.14	25.70	8	5948	802	79737630
Hydrothorax	30.79	25.70	9	5947	1459	79736973
Blood urea increased	30.76	25.70	27	5929	48763	79689669
Ocular hypertension	30.48	25.70	9	5947	1511	79736921
Product substitution error	30.44	25.70	5	5951	51	79738381
Angiopathy	29.17	25.70	13	5943	7069	79731363
Chronic kidney disease	29.10	25.70	30	5926	66124	79672308
Ventricular tachycardia	28.04	25.70	24	5932	41911	79696521
Coronary artery disease	27.56	25.70	29	5927	65445	79672987
Wrong patient received product	27.44	25.70	11	5945	4607	79733825
Blood creatinine increased	26.40	25.70	44	5912	155013	79583419
Cardiac ventricular disorder	26.38	25.70	6	5950	360	79738072
Electrocardiogram QT prolonged	26.18	25.70	33	5923	90353	79648079

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C01EB15	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Other cardiac preparations
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D014665	Vasodilator Agents

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

Disease	Relation	SNOMED_ID	DOID
Angina pectoris	indication	194828000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.61	Basic
pKa2	4.61	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])	Mechanism action	Bioact source	MoA source
Carnitine O-palmitoyltransferase 1, muscle isoform	Enzyme		CPT1B_RAT		IC50	5.89		CHEMBL

External reference:

ID	Source
N0000167121	NUI
D01606	KEGG_DRUG
C0041037	UMLSCUI
CHEBI:94789	CHEBI
CHEMBL203266	ChEMBL_ID
DB09069	DRUGBANK_ID
D014292	MESH_DESCRIPTOR_UI
21109	PUBCHEM_CID
1544	INN_ID
13171-25-0	SECONDARY_CAS_RN
N9A0A0R9S8	UNII
10826	RXNORM
003771	NDDF
003772	NDDF
1156140000	SNOMEDCT_US
703365009	SNOMEDCT_US
703366005	SNOMEDCT_US
CHEMBL3561076	ChEMBL_ID

Pharmaceutical products:

None