trimetazidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2750 5011-34-7

Description:

MoleculeDescription

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:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
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
BA (Bioavailability) 89 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 54
kinase-selectivity-class AKT3,ALK,AXL,BRAF,CAMK2D,CDK9,DDR1,EPHB4,ERBB2,FLT3,IRAK3,JAK1,MAP3K21,MAP4K1,MAPK7,PDK4,PIK3CB,PRKDC,SIK2,SIK3,TTK,ULK1 22
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1978 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tachypnoea 90.19 28.59 31 2683 21278 90604455
Cardiac failure 79.11 28.59 46 2668 109450 90516283
Ventricular hypokinesia 53.32 28.59 15 2699 5326 90620407
Cardiac failure chronic 52.49 28.59 15 2699 5631 90620102
Lipohypertrophy 51.17 28.59 10 2704 729 90625004
Orthopnoea 49.66 28.59 15 2699 6820 90618913
Perseveration 46.77 28.59 8 2706 277 90625456
Apraxia 45.08 28.59 11 2703 2251 90623482
Ocular hypertension 42.99 28.59 10 2704 1670 90624063
Hydrothorax 42.10 28.59 9 2705 1024 90624709
Drug interaction 41.43 28.59 46 2668 276407 90349326
Immune-mediated myositis 39.36 28.59 10 2704 2411 90623322
Angina pectoris 37.97 28.59 20 2694 39140 90586593
Product substitution error 36.57 28.59 5 2709 36 90625697
Cardiac ventricular disorder 36.34 28.59 6 2708 167 90625566
Acute kidney injury 34.37 28.59 45 2669 320342 90305391
Oedema peripheral 33.70 28.59 40 2674 257875 90367858
Lactic acidosis 33.23 28.59 20 2694 50443 90575290
Disorientation 33.03 28.59 19 2695 44095 90581638
Angina unstable 32.58 28.59 11 2703 7132 90618601
Congestive cardiomyopathy 32.26 28.59 11 2703 7343 90618390
Stenosis 30.90 28.59 8 2706 2076 90623657
Left ventricular hypertrophy 30.16 28.59 10 2704 6134 90619599
Hyperreflexia 29.37 28.59 10 2704 6647 90619086
Lipid metabolism disorder 28.90 28.59 5 2709 185 90625548

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 184.01 27.21 124 4453 106732 42510026
Dyspnoea at rest 157.69 27.21 44 4533 4205 42612553
Rales 155.82 27.21 55 4522 11345 42605413
Tricuspid valve incompetence 138.22 27.21 50 4527 11063 42605695
Ejection fraction decreased 136.58 27.21 60 4517 22027 42594731
Diastolic dysfunction 123.99 27.21 41 4536 6942 42609816
Pericardial disease 121.55 27.21 24 4553 498 42616260
Pulmonary valve disease 114.22 27.21 22 4555 399 42616359
Stenosis 102.49 27.21 27 4550 2074 42614684
Mitral valve incompetence 96.12 27.21 43 4534 16446 42600312
Physical examination abnormal 94.14 27.21 19 4558 442 42616316
Coronary artery stenosis 93.85 27.21 37 4540 10342 42606416
Electrocardiogram Q wave abnormal 91.36 27.21 19 4558 515 42616243
Bundle branch block left 91.33 27.21 32 4545 6444 42610314
Acute myocardial infarction 89.20 27.21 63 4514 58102 42558656
Hepatojugular reflux 86.81 27.21 19 4558 660 42616098
Hepatic vein dilatation 81.12 27.21 15 4562 216 42616542
Echocardiogram abnormal 79.94 27.21 20 4557 1250 42615508
Cardiac discomfort 79.80 27.21 18 4559 719 42616039
Occult blood 79.75 27.21 19 4558 967 42615791
Liver palpable 77.31 27.21 15 4562 283 42616475
Hyperlipidaemia 76.52 27.21 40 4537 21476 42595282
Helicobacter gastritis 73.72 27.21 19 4558 1338 42615420
Carotid arteriosclerosis 72.31 27.21 21 4556 2311 42614447
Systolic dysfunction 71.10 27.21 22 4555 3006 42613752
Angina pectoris 70.69 27.21 44 4533 32852 42583906
Ventricular arrhythmia 69.70 27.21 26 4551 6253 42610505
Carotid artery stenosis 69.58 27.21 25 4552 5411 42611347
Mitral valve disease 66.97 27.21 18 4559 1492 42615266
Atrial enlargement 63.93 27.21 15 4562 714 42616044
Left ventricular hypertrophy 63.04 27.21 27 4550 9292 42607466
Inferior vena cava dilatation 62.18 27.21 15 4562 805 42615953
Left ventricular dysfunction 60.70 27.21 28 4549 11473 42605285
Ventricular enlargement 59.62 27.21 14 4563 669 42616089
Linear IgA disease 56.72 27.21 17 4560 2086 42614672
Cardiomegaly 56.28 27.21 30 4547 16736 42600022
Cardiac failure chronic 55.80 27.21 25 4552 9576 42607182
Anaemia macrocytic 55.66 27.21 19 4558 3536 42613222
Supraventricular tachycardia 55.64 27.21 27 4550 12381 42604377
Aortic valve incompetence 54.50 27.21 22 4555 6526 42610232
Ventricular hypokinesia 53.44 27.21 22 4555 6862 42609896
Left ventricular enlargement 51.85 27.21 13 4564 819 42615939
Base excess decreased 50.98 27.21 10 4567 200 42616558
Angiopathy 47.99 27.21 19 4558 5358 42611400
Hypokinesia 42.81 27.21 21 4556 9850 42606908
Oxygen consumption decreased 41.41 27.21 9 4568 302 42616456
Cardiac murmur 35.00 27.21 20 4557 12755 42604003
Coronary artery disease 33.96 27.21 35 4542 53685 42563073
Intestinal obstruction 33.86 27.21 26 4551 27132 42589626
Hypertrophy 31.89 27.21 8 4569 505 42616253
Renal cyst 30.99 27.21 17 4560 10022 42606736
Breath sounds abnormal 30.65 27.21 18 4559 12075 42604683
Chronic kidney disease 30.26 27.21 31 4546 47210 42569548
Electrocardiogram QT prolonged 29.87 27.21 31 4546 47914 42568844
Skin lesion 29.54 27.21 24 4553 27150 42589608
Ventricular tachycardia 29.38 27.21 25 4552 30135 42586623
Mean cell haemoglobin decreased 28.30 27.21 10 4567 2060 42614698
Ill-defined disorder 28.09 27.21 19 4558 16277 42600481
Congestive cardiomyopathy 27.49 27.21 15 4562 8749 42608009

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cardiac failure 251.23 22.80 156 7234 187470 110394439
Rales 168.26 22.80 63 7327 24676 110557233
Dyspnoea at rest 153.27 22.80 45 7345 8301 110573608
Tricuspid valve incompetence 148.64 22.80 57 7333 23816 110558093
Stenosis 142.12 22.80 35 7355 3316 110578593
Pulmonary valve disease 128.12 22.80 22 7368 337 110581572
Ejection fraction decreased 125.23 22.80 59 7331 40821 110541088
Pericardial disease 125.08 22.80 24 7366 699 110581210
Diastolic dysfunction 123.81 22.80 42 7348 12362 110569547
Coronary artery stenosis 123.39 22.80 43 7347 13715 110568194
Cardiac failure chronic 111.79 22.80 40 7350 13771 110568138
Mitral valve incompetence 104.84 22.80 49 7341 33280 110548629
Angina pectoris 104.46 22.80 60 7330 62235 110519674
Physical examination abnormal 100.26 22.80 19 7371 517 110581392
Acute myocardial infarction 100.21 22.80 65 7325 83712 110498197
Ventricular hypokinesia 96.53 22.80 34 7356 11180 110570729
Hepatojugular reflux 94.28 22.80 19 7371 716 110581193
Electrocardiogram Q wave abnormal 94.05 22.80 19 7371 725 110581184
Bundle branch block left 88.25 22.80 33 7357 12855 110569054
Hepatic vein dilatation 87.40 22.80 15 7375 229 110581680
Ventricular arrhythmia 84.60 22.80 30 7360 10057 110571852
Hyperlipidaemia 83.67 22.80 43 7347 35805 110546104
Liver palpable 81.95 22.80 15 7375 336 110581573
Left ventricular dysfunction 81.57 22.80 37 7353 23456 110558453
Cardiomegaly 79.94 22.80 39 7351 29091 110552818
Systolic dysfunction 77.52 22.80 23 7367 4392 110577517
Occult blood 76.75 22.80 19 7371 1837 110580072
Carotid arteriosclerosis 76.52 22.80 21 7369 3036 110578873
Cardiac discomfort 76.43 22.80 18 7372 1410 110580499
Helicobacter gastritis 75.00 22.80 20 7370 2596 110579313
Echocardiogram abnormal 74.56 22.80 20 7370 2654 110579255
Inferior vena cava dilatation 66.79 22.80 15 7375 952 110580957
Left ventricular hypertrophy 66.22 22.80 27 7363 13217 110568692
Tachypnoea 66.16 22.80 38 7352 39357 110542552
Ventricular enlargement 65.41 22.80 14 7376 710 110581199
Mitral valve disease 65.21 22.80 19 7371 3406 110578503
Carotid artery stenosis 64.44 22.80 24 7366 9239 110572670
Atrial enlargement 64.19 22.80 15 7375 1136 110580773
Chronic kidney disease 60.40 22.80 46 7344 76245 110505664
Supraventricular tachycardia 59.03 22.80 30 7360 24392 110557517
Left ventricular enlargement 57.38 22.80 13 7377 858 110581051
Aortic valve incompetence 57.00 22.80 23 7367 10958 110570951
Anaemia macrocytic 54.78 22.80 20 7370 7283 110574626
Linear IgA disease 52.33 22.80 17 7373 4372 110577537
Oedema peripheral 52.27 22.80 85 7305 328575 110253334
Congestive cardiomyopathy 51.28 22.80 23 7367 14196 110567713
Base excess decreased 49.18 22.80 10 7380 394 110581515
Angina unstable 48.10 22.80 23 7367 16409 110565500
Angiopathy 47.79 22.80 19 7371 8711 110573198
Atrial fibrillation 47.28 22.80 67 7323 229575 110352334
Coronary artery disease 43.50 22.80 37 7353 71653 110510256
Blood creatinine increased 41.59 22.80 56 7334 182833 110399076
Oxygen consumption decreased 40.92 22.80 9 7381 519 110581390
Lipohypertrophy 40.10 22.80 10 7380 996 110580913
Perseveration 37.12 22.80 8 7382 419 110581490
Orthopnoea 37.12 22.80 17 7373 11004 110570905
Coronary artery occlusion 37.02 22.80 19 7371 15753 110566156
Drug interaction 36.87 22.80 94 7296 500089 110081820
Ventricular tachycardia 34.90 22.80 28 7362 49981 110531928
Renal cyst 34.49 22.80 19 7371 18153 110563756
Hypokinesia 33.85 22.80 20 7370 21806 110560103
Blood urea increased 32.59 22.80 28 7362 54929 110526980
Electrocardiogram QT prolonged 32.13 22.80 38 7352 108922 110472987
Cardiac murmur 31.62 22.80 20 7370 24608 110557301
Arteriosclerosis 31.52 22.80 20 7370 24747 110557162
Apraxia 31.48 22.80 11 7379 3529 110578380
Ocular hypertension 31.46 22.80 10 7380 2398 110579511
Hypertrophy 30.89 22.80 8 7382 927 110580982
Hydrothorax 30.69 22.80 9 7381 1649 110580260
Arrhythmia 30.63 22.80 30 7360 69545 110512364
Myocardial ischaemia 30.15 22.80 20 7370 26664 110555245
Product substitution error 29.34 22.80 5 7385 73 110581836
Intestinal obstruction 29.31 22.80 26 7364 53201 110528708
Hypertension 28.80 22.80 87 7303 509997 110071912
Breath sounds abnormal 28.61 22.80 19 7371 25385 110556524
Drug ineffective 28.55 22.80 36 7354 1520504 109061405
Diverticulum intestinal haemorrhagic 28.30 22.80 11 7379 4752 110577157
Cardiac ventricular disorder 27.29 22.80 6 7384 345 110581564
Splenomegaly 26.81 22.80 18 7372 24480 110557429
Diabetes mellitus 26.60 22.80 33 7357 99348 110482561
Skin lesion 26.03 22.80 24 7366 51607 110530302
Sideroblastic anaemia 25.82 22.80 6 7384 443 110581466
International normalised ratio decreased 25.54 22.80 12 7378 8224 110573685
Brain natriuretic peptide increased 24.86 22.80 13 7377 11196 110570713
Wrong patient received product 24.71 22.80 11 7379 6663 110575246
Myocardial infarction 24.36 22.80 45 7345 192038 110389871
Arteriosclerosis coronary artery 24.06 22.80 17 7373 25101 110556808
Blood glucose increased 23.40 22.80 36 7354 132460 110449449
Blood bicarbonate decreased 22.90 22.80 10 7380 5787 110576122

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01EB15 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
OTHER CARDIAC PREPARATIONS
Other cardiac preparations
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

C01EB Other cardiac preparations 15 drugs
acadesineacoramidisadenosinecamphorcreatinolfosfateibuprofenindomethacinivabradinemavacamtenmeldoniumphosphocreatineranolazine show all 15 →

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

DiseaseRelationSNOMED_IDDOID
Angina pectoris indication 194828000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Carnitine O-palmitoyltransferase 1, muscle isoform Enzyme IC50 5.89 CHEMBL

External reference:

IDSource
N0000167121 NUI
D01606 KEGG_DRUG
C0041037 UMLSCUI
CHEBI:94789 CHEBI
CHEMBL203266 ChEMBL_ID
DB09069 DRUGBANK_ID
CHEMBL3561076 ChEMBL_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
N9A0A0R9S8 INXIGHT DRUGS

Pharmaceutical products:

None