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

Stem definitionDrug idCAS RN
2713 1197-18-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tranexamic acid
  • amchafibrin
  • amikapron
  • cyclocapron
  • tranol
  • transamin
  • zataranax
Antifibrinolytic hemostatic used in severe hemorrhage.
  • Molecular weight: 157.21
  • Formula: C8H15NO2
  • CLOGP: -1.80
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 63.32
  • ALOGS: -0.94
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2 g O
2 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 34 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.38 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.97 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.30 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 31 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -2.788 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.694 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.964 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.692 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 81.850 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 75.380 % High 1
herg hERG pIC50 5.143 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.472 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.614 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 81.430 % High 1
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PRKDC,SYK,TEK,TGFBR1 25
kinase-selectivity-class EIF2AK3,MAP2K6 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.262 High 1
mh-clint Mouse hepatocyte intrinsic clearance 1.563 High 1
mppb Mouse plasma protein binding (% unbound) 87.570 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.279 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 83.560 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.972 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 81.710 % High 1
rppb Rat plasma protein binding (% unbound) 94.320 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 843.335 uM High 1

Approvals:

DateAgencyCompanyOrphan
Dec. 30, 1986 FDA PHARMACIA AND UPJOHN

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
Myoclonus 134.99 14.98 65 14840 19103 90594439
Aplastic anaemia 131.26 14.98 57 14848 13212 90600330
Renal cortical necrosis 130.52 14.98 25 14880 278 90613264
Wrong product administered 124.40 14.98 47 14858 7618 90605924
Pulmonary embolism 106.37 14.98 119 14786 130701 90482841
Generalised tonic-clonic seizure 98.61 14.98 65 14840 34838 90578704
Anaphylactic reaction 96.99 14.98 94 14811 87430 90526112
Vaginal haemorrhage 95.12 14.98 61 14844 31210 90582332
Melaena 91.56 14.98 62 14843 34735 90578807
Hereditary angioedema 88.62 14.98 39 14866 9326 90604216
Haemorrhage 83.50 14.98 78 14827 69291 90544251
Purpura 80.17 14.98 42 14863 14736 90598806
Heavy menstrual bleeding 74.98 14.98 45 14860 20485 90593057
Platelet count decreased 73.28 14.98 101 14804 136868 90476674
Seizure 72.02 14.98 106 14799 152523 90461019
Maternal exposure during delivery 71.27 14.98 26 14879 3820 90609722
Status epilepticus 67.97 14.98 41 14864 18833 90594709
Deep vein thrombosis 55.79 14.98 72 14833 91548 90521994
Hypotension 55.35 14.98 147 14758 325250 90288292
Cerebral venous sinus thrombosis 55.20 14.98 19 14886 2357 90611185
Rash maculo-papular 53.08 14.98 48 14857 40885 90572657
Cerebral infarction 52.94 14.98 40 14865 26556 90586986
Vasodilatation 51.60 14.98 19 14886 2865 90610677
Cardiac arrest 51.10 14.98 74 14831 104861 90508681
Tachycardia 50.58 14.98 92 14813 157581 90455961
Joint swelling 49.75 14.98 11 14894 503289 90110253
Thrombocytopenia 49.15 14.98 107 14798 208618 90404924
Febrile neutropenia 47.79 14.98 90 14815 158259 90455283
Anaphylactic shock 44.82 14.98 39 14866 31578 90581964
Alopecia 44.73 14.98 13 14892 495058 90118484
Fatigue 44.68 14.98 76 14829 1153947 89459595
Angioedema 44.30 14.98 54 14851 64822 90548720
Drug hypersensitivity 44.09 14.98 11 14894 463598 90149944
Acute myocardial infarction 43.45 14.98 40 14865 34850 90578692
Transfusion 43.24 14.98 30 14875 17458 90596084
Off label use 43.21 14.98 319 14586 1101933 89511609
Uterine haemorrhage 42.42 14.98 19 14886 4733 90608809
Systemic lupus erythematosus 42.23 14.98 5 14900 361891 90251651
Ovarian vein thrombosis 41.93 14.98 8 14897 87 90613455
Drug intolerance 41.83 14.98 11 14894 447580 90165962
Myoclonic epilepsy 41.68 14.98 14 14891 1613 90611929
Incorrect route of product administration 41.00 14.98 46 14859 50580 90562962
Biliary sepsis 39.82 14.98 12 14893 974 90612568
Hepatic function abnormal 39.10 14.98 43 14862 46245 90567297
Epistaxis 38.51 14.98 58 14847 85067 90528475
Enterococcal sepsis 37.84 14.98 13 14892 1603 90611939
Shock haemorrhagic 37.50 14.98 24 14881 12221 90601321
Brain oedema 36.50 14.98 27 14878 17358 90596184
Contraindicated product administered 35.96 14.98 5 14900 320134 90293408
Rheumatoid arthritis 35.66 14.98 8 14897 362606 90250936
Neutropenic sepsis 35.49 14.98 27 14878 18103 90595439
Haemoptysis 35.41 14.98 35 14870 33285 90580257
Product packaging confusion 34.77 14.98 8 14897 225 90613317
Rash erythematous 34.77 14.98 48 14857 65056 90548486
Mucosal inflammation 34.62 14.98 45 14860 57580 90555962
Abdominal discomfort 34.12 14.98 18 14887 477310 90136232
Retinal artery occlusion 33.53 14.98 13 14892 2258 90611284
Pericarditis 33.40 14.98 3 14902 270148 90343394
Sepsis 33.37 14.98 84 14821 179730 90433812
Haemoglobin decreased 32.53 14.98 78 14827 161878 90451664
Infusion related reaction 32.41 14.98 14 14891 416766 90196776
Ureteric perforation 31.89 14.98 5 14900 14 90613528
Puncture site haematoma 31.46 14.98 6 14899 65 90613477
Blood pressure decreased 31.02 14.98 49 14856 74846 90538696
Drug ineffective for unapproved indication 30.98 14.98 46 14859 66598 90546944
Haemorrhage intracranial 30.61 14.98 23 14882 15139 90598403
Tri-iodothyronine free decreased 30.42 14.98 8 14897 395 90613147
Tonic clonic movements 29.54 14.98 11 14894 1711 90611831
Pain 28.97 14.98 77 14828 996264 89617278
Toxic epidermal necrolysis 28.84 14.98 31 14874 32497 90581045
Ischaemic stroke 28.74 14.98 26 14879 22140 90591402
Acute left ventricular failure 28.70 14.98 10 14895 1286 90612256
Nosocomial infection 28.42 14.98 11 14894 1902 90611640
Alanine aminotransferase increased 28.21 14.98 61 14844 118277 90495265
Acute generalised exanthematous pustulosis 28.14 14.98 21 14884 13682 90599860
Infusion site scar 27.19 14.98 8 14897 598 90612944
Haemorrhagic disorder 27.08 14.98 9 14896 1003 90612539
Stridor 27.07 14.98 14 14891 4779 90608763
Psoriatic arthropathy 27.01 14.98 3 14902 228332 90385210
Pulmonary alveolar haemorrhage 26.82 14.98 15 14890 5983 90607559
Anaemia 26.09 14.98 121 14784 352681 90260861
Coronary artery thrombosis 26.02 14.98 9 14896 1133 90612409
Basophil count increased 25.95 14.98 9 14896 1142 90612400
Puncture site haemorrhage 25.77 14.98 7 14898 391 90613151
Mobility decreased 25.73 14.98 5 14900 250729 90362813
Uterine disorder 25.70 14.98 12 14893 3289 90610253
Factor VII deficiency 25.45 14.98 5 14900 64 90613478
Urine ketone body present 25.35 14.98 11 14894 2541 90611001
Multiple organ dysfunction syndrome 24.64 14.98 42 14863 68294 90545248
Perforation 24.51 14.98 10 14895 1984 90611558
Asthma 24.49 14.98 5 14900 242155 90371387
Platelet count increased 24.21 14.98 23 14882 20836 90592706
Haemodynamic instability 24.13 14.98 18 14887 11721 90601821
Weight increased 24.12 14.98 20 14885 417907 90195635
Electrocardiogram PR shortened 23.65 14.98 7 14898 534 90613008
Poor venous access 23.56 14.98 22 14883 19505 90594037
Cancer pain 23.44 14.98 12 14893 4013 90609529
Atrial thrombosis 23.36 14.98 10 14895 2235 90611307
Embolic stroke 23.30 14.98 12 14893 4060 90609482
Uterine leiomyoma 23.09 14.98 17 14888 10847 90602695
Premature delivery 22.86 14.98 30 14875 38732 90574810
Postpartum haemorrhage 22.72 14.98 10 14895 2391 90611151
Circulatory collapse 22.54 14.98 24 14881 24880 90588662
Thrombosis 22.53 14.98 42 14863 73209 90540333
Platelet transfusion 22.36 14.98 8 14897 1112 90612430
Product dose omission issue 22.34 14.98 10 14895 291677 90321865
Wound 22.26 14.98 11 14894 302969 90310573
Urinary tract disorder 21.42 14.98 11 14894 3700 90609842
Rectal haemorrhage 21.27 14.98 44 14861 82700 90530842
Type 2 diabetes mellitus 20.96 14.98 4 14901 203240 90410302
Extravasation 20.70 14.98 10 14895 2954 90610588
Pulmonary haemorrhage 20.41 14.98 14 14891 7999 90605543
Infusion site warmth 20.38 14.98 9 14896 2169 90611373
Hypoventilation 20.35 14.98 12 14893 5284 90608258
Coagulopathy 20.30 14.98 22 14883 23267 90590275
Memory impairment 20.09 14.98 4 14901 197240 90416302
Meningitis aseptic 20.06 14.98 13 14892 6760 90606782
Stress cardiomyopathy 19.99 14.98 17 14888 13338 90600204
Hepatic enzyme increased 19.92 14.98 18 14887 360718 90252824
Gastrointestinal haemorrhage 19.79 14.98 45 14860 90203 90523339
Blood cholesterol increased 19.62 14.98 5 14900 208007 90405535
Impaired healing 19.61 14.98 7 14898 234192 90379350
Fibroma 19.59 14.98 7 14898 969 90612573
Arterial thrombosis 19.58 14.98 8 14897 1592 90611950
Stevens-Johnson syndrome 19.31 14.98 24 14881 29352 90584190
Disinhibition 18.97 14.98 7 14898 1061 90612481
Infusion site discomfort 18.60 14.98 8 14897 1808 90611734
Lower respiratory tract infection 18.56 14.98 9 14896 250650 90362892
Drug interaction 18.38 14.98 92 14813 276361 90337181
Injury 18.13 14.98 5 14900 197344 90416198
Sinusitis 17.91 14.98 18 14887 343070 90270472
Ischaemia 17.77 14.98 11 14894 5284 90608258
Cerebral haemorrhage 17.75 14.98 25 14880 34497 90579045
Toxic skin eruption 17.56 14.98 17 14888 15757 90597785
Fibromyalgia 17.56 14.98 6 14899 206263 90407279
Uterine atony 17.41 14.98 5 14900 343 90613199
Venous thrombosis 17.32 14.98 11 14894 5526 90608016
Ventricular fibrillation 17.28 14.98 16 14889 14028 90599514
Asthenia 17.22 14.98 39 14866 533712 90079830
Allergic reaction to excipient 17.14 14.98 6 14899 782 90612760
Enterocolitis 17.04 14.98 14 14891 10476 90603066
Caesarean section 16.99 14.98 18 14887 18559 90594983
PCO2 abnormal 16.98 14.98 4 14901 125 90613417
Drug ineffective 16.90 14.98 320 14585 1383978 89229564
Hyperaesthesia 16.80 14.98 14 14891 10688 90602854
Acute respiratory distress syndrome 16.60 14.98 22 14883 28664 90584878
Nasopharyngitis 16.42 14.98 26 14879 407078 90206464
Ill-defined disorder 16.40 14.98 5 14900 184886 90428656
Dry mouth 16.29 14.98 5 14900 184054 90429488
Infusion site rash 16.21 14.98 8 14897 2475 90611067
Pancytopenia 16.18 14.98 50 14855 120213 90493329
Arterial haemorrhage 16.09 14.98 8 14897 2515 90611027
Discomfort 15.98 14.98 13 14892 274322 90339220
HER2 positive breast cancer 15.93 14.98 5 14900 465 90613077
Thoracotomy 15.69 14.98 3 14902 33 90613509
Upper respiratory tract inflammation 15.66 14.98 8 14897 2664 90610878
False negative investigation result 15.50 14.98 4 14901 183 90613359
Upper gastrointestinal haemorrhage 15.47 14.98 19 14886 22957 90590585
Acute myeloid leukaemia 15.43 14.98 18 14887 20622 90592920
Adnexal torsion 15.30 14.98 5 14900 529 90613013
Blood lactate dehydrogenase increased 15.18 14.98 20 14885 25912 90587630
Colitis ischaemic 15.07 14.98 14 14891 12332 90601210
Psoriasis 15.04 14.98 3 14902 147751 90465791
Shock 15.03 14.98 21 14884 28757 90584785

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
Anaphylactic reaction 147.92 16.84 109 11374 42634 42567218
Haemorrhage 142.27 16.84 123 11360 60440 42549412
Myoclonus 111.93 16.84 65 11418 17000 42592852
Factor VIII inhibition 88.91 16.84 20 11463 302 42609550
Mechanical ventilation complication 87.57 16.84 23 11460 681 42609171
Febrile neutropenia 86.14 16.84 168 11315 185535 42424317
Haemothorax 75.66 16.84 34 11449 5202 42604650
Wrong product administered 73.06 16.84 35 11448 6191 42603661
Haemarthrosis 67.61 16.84 29 11454 3969 42605883
Generalised tonic-clonic seizure 66.81 16.84 56 11427 26323 42583529
Anaphylactic shock 66.01 16.84 53 11430 23464 42586388
Aplastic anaemia 62.75 16.84 40 11443 12344 42597508
Inspiratory capacity decreased 58.47 16.84 24 11459 2943 42606909
Shock haemorrhagic 52.94 16.84 40 11443 16202 42593650
Vasodilatation 49.66 16.84 17 11466 1260 42608592
Adverse reaction 48.53 16.84 23 11460 3970 42605882
Status epilepticus 47.78 16.84 37 11446 15541 42594311
Post procedural haemorrhage 46.98 16.84 30 11453 9282 42600570
Post procedural hypotension 45.45 16.84 9 11474 70 42609782
Muscle haemorrhage 44.81 16.84 22 11461 4103 42605749
Vascular stent thrombosis 43.51 16.84 20 11463 3222 42606630
Cerebral infarction 42.41 16.84 47 11436 31122 42578730
Angiopathy 42.06 16.84 23 11460 5354 42604498
Epistaxis 41.82 16.84 69 11414 66757 42543095
Mucosal inflammation 39.33 16.84 57 11426 49317 42560535
Tachycardia 39.12 16.84 85 11398 101002 42508850
Platelet count decreased 39.05 16.84 103 11380 138478 42471374
Urticaria 35.45 16.84 68 11415 73968 42535884
Face oedema 34.56 16.84 29 11454 13637 42596215
Myoclonic epilepsy 34.55 16.84 14 11469 1660 42608192
Emphysema 33.89 16.84 27 11456 11808 42598044
Hypovolaemia 32.46 16.84 26 11457 11459 42598393
Haemophilia 32.16 16.84 5 11478 6 42609846
Fatigue 31.44 16.84 43 11440 435598 42174254
Pneumothorax 31.16 16.84 35 11448 23508 42586344
Mesenteric vascular insufficiency 31.10 16.84 7 11476 106 42609746
Coronary artery thrombosis 30.36 16.84 14 11469 2272 42607580
Incorrect route of product administration 30.25 16.84 35 11448 24270 42585582
Upper respiratory tract inflammation 29.60 16.84 13 11470 1883 42607969
Interstitial lung disease 29.24 16.84 65 11418 78397 42531455
Product dose omission issue 28.28 16.84 4 11479 154361 42455491
Haemoptysis 25.35 16.84 45 11438 46122 42563730
Platelet transfusion 24.47 16.84 11 11472 1683 42608169
Gingival bleeding 23.53 16.84 19 11464 8466 42601386
Hypotension 23.08 16.84 133 11350 257498 42352354
Hepatic function abnormal 23.01 16.84 46 11437 51521 42558331
Pulmonary haemorrhage 22.46 16.84 21 11462 11376 42598476
Inhibiting antibodies positive 21.66 16.84 3 11480 0 42609852
Tryptase decreased 21.10 16.84 4 11479 24 42609828
Immune thrombocytopenia 20.83 16.84 20 11463 11196 42598656
Gastrointestinal haemorrhage 20.14 16.84 65 11418 97661 42512191
Haemoglobin increased 19.62 16.84 14 11469 5192 42604660
Chronic pulmonary histoplasmosis 19.58 16.84 3 11480 3 42609849
Clonus 19.41 16.84 12 11471 3508 42606344
Toxicity to various agents 19.27 16.84 20 11463 229116 42380736
Bronchospasm 18.51 16.84 20 11463 12865 42596987
Acute myocardial infarction 18.18 16.84 45 11438 58120 42551732
Labile blood pressure 18.08 16.84 7 11476 736 42609116
Pneumonia 17.98 16.84 183 11300 421966 42187886
Haemorrhagic diathesis 17.91 16.84 11 11472 3178 42606674
Pleural effusion 17.69 16.84 62 11421 97104 42512748
Hepatic cyst ruptured 17.50 16.84 3 11480 9 42609843
Death 17.29 16.84 67 11416 471118 42138734
Fibrin degradation products increased 16.95 16.84 5 11478 228 42609624
Nystagmus 16.94 16.84 13 11470 5383 42604469

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
Anaphylactic reaction 233.37 13.62 199 24846 114101 110450153
Myoclonus 212.57 13.62 117 24928 32881 110531373
Haemorrhage 208.14 13.62 181 24864 106511 110457743
Wrong product administered 196.97 13.62 79 24966 10881 110553373
Aplastic anaemia 184.10 13.62 96 24949 24212 110540042
Generalised tonic-clonic seizure 167.43 13.62 121 24924 54559 110509695
Renal cortical necrosis 108.89 13.62 25 25020 499 110563755
Status epilepticus 108.52 13.62 75 24970 31496 110532758
Febrile neutropenia 107.87 13.62 228 24817 316539 110247715
Anaphylactic shock 107.67 13.62 91 24954 51455 110512799
Platelet count decreased 104.21 13.62 187 24858 230256 110333998
Vasodilatation 99.82 13.62 36 25009 3708 110560546
Mechanical ventilation complication 89.44 13.62 23 25022 748 110563506
Shock haemorrhagic 87.29 13.62 62 24983 27185 110537069
Cerebral infarction 87.29 13.62 81 24964 51757 110512497
Haemothorax 84.17 13.62 38 25007 6993 110557261
Hereditary angioedema 83.74 13.62 38 25007 7076 110557178
Myoclonic epilepsy 79.79 13.62 28 25017 2663 110561591
Factor VIII inhibition 79.74 13.62 18 25027 332 110563922
Tachycardia 76.93 13.62 163 24882 226482 110337772
Vaginal haemorrhage 73.35 13.62 54 24991 25020 110539234
Melaena 71.56 13.62 83 24962 68674 110495580
Epistaxis 71.04 13.62 115 24930 130257 110433997
Fatigue 69.72 13.62 105 24940 1215853 109348401
Pulmonary embolism 69.05 13.62 151 24894 214323 110349931
Inspiratory capacity decreased 65.63 13.62 24 25021 2571 110561683
Mucosal inflammation 65.36 13.62 94 24951 96047 110468207
Maternal exposure during delivery 61.64 13.62 25 25020 3540 110560714
Haemarthrosis 61.42 13.62 31 25014 7298 110556956
Incorrect route of product administration 61.15 13.62 74 24971 63987 110500267
Seizure 60.46 13.62 146 24899 221039 110343215
Heavy menstrual bleeding 58.89 13.62 40 25005 16325 110547929
Hypotension 57.60 13.62 253 24792 523596 110040658
Acute myocardial infarction 57.08 13.62 82 24963 83695 110480559
Coronary artery thrombosis 56.95 13.62 23 25022 3221 110561033
Post procedural hypotension 56.32 13.62 11 25034 96 110564158
Hepatic function abnormal 55.92 13.62 84 24961 89211 110475043
Drug intolerance 55.74 13.62 12 25033 406500 110157754
Haemoptysis 54.82 13.62 74 24971 71280 110492974
Purpura 52.86 13.62 44 25001 24344 110539910
Joint swelling 51.51 13.62 18 25027 442827 110121427
Synovitis 50.05 13.62 3 25042 274089 110290165
Arthropathy 50.03 13.62 4 25041 287518 110276736
Rash maculo-papular 49.61 13.62 72 24973 74150 110490104
Post procedural haemorrhage 48.99 13.62 35 25010 15477 110548777
Drug hypersensitivity 47.04 13.62 22 25023 454068 110110186
Platelet transfusion 45.94 13.62 19 25026 2827 110561427
Deep vein thrombosis 45.58 13.62 99 24946 139788 110424466
Cardiac arrest 44.55 13.62 121 24924 196632 110367622
Alopecia 43.85 13.62 14 25031 364739 110199515
Drug ineffective 43.59 13.62 530 24515 1520010 109044244
Muscle haemorrhage 43.23 13.62 24 25021 6845 110557409
Cerebral venous sinus thrombosis 42.29 13.62 18 25027 2877 110561377
Uterine haemorrhage 42.19 13.62 19 25026 3475 110560779
Product packaging confusion 42.19 13.62 11 25034 378 110563876
Product dose omission issue 41.15 13.62 11 25034 321771 110242483
Rheumatoid arthritis 40.74 13.62 9 25036 299604 110264650
Angiopathy 40.42 13.62 25 25020 8705 110555549
Blood pressure decreased 39.27 13.62 83 24962 115008 110449246
Upper respiratory tract inflammation 38.13 13.62 19 25026 4352 110559902
Systemic lupus erythematosus 38.08 13.62 6 25039 254332 110309922
Vascular stent thrombosis 36.04 13.62 18 25027 4143 110560111
Pericarditis 35.59 13.62 4 25041 219110 110345144
Asthma 35.09 13.62 7 25038 250284 110313970
Pain 34.93 13.62 106 24939 954849 109609405
Infusion related reaction 34.33 13.62 22 25023 381140 110183114
Ovarian vein thrombosis 34.29 13.62 7 25038 78 110564176
Pulmonary haemorrhage 34.24 13.62 29 25016 16427 110547827
Thrombocytopenia 34.19 13.62 163 24882 348722 110215532
Transfusion 33.89 13.62 35 25010 25437 110538817
Immune thrombocytopenia 33.77 13.62 33 25012 22461 110541793
Gastrointestinal haemorrhage 33.74 13.62 98 24947 165420 110398834
Drug ineffective for unapproved indication 33.74 13.62 73 24972 102765 110461489
Hypovolaemia 32.92 13.62 32 25013 21642 110542612
Retinal artery occlusion 32.79 13.62 17 25028 4232 110560022
Stridor 32.57 13.62 20 25025 6875 110557379
Face oedema 32.49 13.62 39 25006 33430 110530824
Pneumothorax 32.43 13.62 40 25005 35245 110529009
Tonic clonic movements 32.33 13.62 15 25030 2937 110561317
Dry mouth 31.61 13.62 4 25041 199944 110364310
Cerebral haemorrhage 30.96 13.62 54 24991 64914 110499340
Enterococcal sepsis 30.69 13.62 15 25030 3297 110560957
Mesenteric vascular insufficiency 30.62 13.62 7 25038 137 110564117
Mobility decreased 30.57 13.62 8 25037 237414 110326840
Shock 30.16 13.62 48 24997 53540 110510714
Asthenia 30.07 13.62 70 24975 688929 109875325
Haemodynamic instability 29.64 13.62 31 25014 22857 110541397
Ureteric perforation 29.56 13.62 5 25040 17 110564237
Acute generalised exanthematous pustulosis 29.24 13.62 30 25015 21634 110542620
Off label use 28.91 13.62 488 24557 1499697 109064557
Abdominal discomfort 28.83 13.62 28 25017 393830 110170424
Drug eruption 28.75 13.62 47 24998 53612 110510642
Biliary sepsis 28.72 13.62 12 25033 1831 110562423
Neutropenic sepsis 28.50 13.62 35 25010 30711 110533543
Weight increased 28.28 13.62 32 25013 419612 110144642
Angioedema 27.94 13.62 66 24979 98434 110465820
Interstitial lung disease 27.92 13.62 82 24963 139252 110425002
Platelet count increased 27.74 13.62 32 25013 26302 110537952
Haemoglobin increased 27.43 13.62 20 25025 9127 110555127
Infusion site scar 27.26 13.62 8 25037 428 110563826
Factor VII deficiency 27.04 13.62 6 25039 102 110564152
Injury 26.95 13.62 4 25041 177261 110386993
Tri-iodothyronine free decreased 26.85 13.62 8 25037 451 110563803
Brain oedema 26.59 13.62 34 25011 31064 110533190
Haemoglobin decreased 26.41 13.62 119 24926 248608 110315646
Blood cholesterol increased 26.25 13.62 5 25040 184780 110379474
Haemorrhagic diathesis 26.18 13.62 18 25027 7490 110556764
Contraindicated product administered 25.73 13.62 12 25033 248255 110315999
Rash erythematous 25.60 13.62 57 24988 81775 110482479
Thrombotic microangiopathy 25.13 13.62 32 25013 29117 110535137
Circulatory collapse 24.87 13.62 39 25006 42954 110521300
Anaemia 24.33 13.62 209 24836 546877 110017377
Alanine aminotransferase increased 24.26 13.62 94 24951 183679 110380575
Emphysema 24.24 13.62 26 25019 19730 110544524
Musculoskeletal stiffness 24.05 13.62 17 25028 279805 110284449
Haemorrhage intracranial 23.71 13.62 31 25014 28938 110535316
Fibromyalgia 23.50 13.62 5 25040 170904 110393350
Arterial haemorrhage 23.10 13.62 13 25032 3806 110560448
Uterine disorder 22.96 13.62 11 25034 2315 110561939
Depression 22.71 13.62 23 25022 317312 110246942
Basophil count increased 22.36 13.62 10 25035 1800 110562454
Perforation 22.36 13.62 10 25035 1800 110562454
Multiple organ dysfunction syndrome 22.02 13.62 80 24965 151630 110412624
Lower respiratory tract infection 21.92 13.62 14 25031 243092 110321162
Sinusitis 21.81 13.62 21 25024 296667 110267587
Helicobacter infection 21.81 13.62 7 25038 181870 110382384
Tryptase decreased 21.65 13.62 4 25041 25 110564229
Toxicity to various agents 21.61 13.62 48 24997 480507 110083747
Embolic stroke 21.54 13.62 17 25028 8726 110555528
Puncture site haematoma 21.49 13.62 6 25039 268 110563986
Gastrooesophageal reflux disease 21.45 13.62 7 25038 179969 110384285
Procedural haemorrhage 21.29 13.62 14 25031 5413 110558841
Peripheral swelling 21.06 13.62 37 25008 403997 110160257
Ill-defined disorder 20.74 13.62 5 25040 156848 110407406
Night sweats 20.42 13.62 3 25042 133980 110430274
Chronic pulmonary histoplasmosis 20.10 13.62 3 25042 3 110564251
Inhibiting antibodies positive 20.10 13.62 3 25042 3 110564251
Acute left ventricular failure 20.07 13.62 10 25035 2291 110561963
Neurotoxicity 20.00 13.62 35 25010 42172 110522082
Enterocolitis 19.91 13.62 23 25022 18926 110545328
Acute myeloid leukaemia 19.90 13.62 33 25012 38077 110526177
Pyrexia 19.77 13.62 299 24746 897966 109666288
Nosocomial infection 19.65 13.62 11 25034 3188 110561066
Impaired healing 19.63 13.62 10 25035 196707 110367547
Therapeutic product effect decreased 19.51 13.62 16 25029 244300 110319954
Coagulopathy 19.48 13.62 34 25011 40877 110523377
Clonus 19.46 13.62 16 25029 8700 110555554
Loss of personal independence in daily activities 19.41 13.62 5 25040 150015 110414239
Condition aggravated 19.41 13.62 93 24952 734743 109829511
Infusion site warmth 19.39 13.62 9 25036 1764 110562490
Puncture site haemorrhage 19.37 13.62 7 25038 725 110563529
Type 2 diabetes mellitus 19.26 13.62 8 25037 177224 110387030
Gingival bleeding 19.06 13.62 23 25022 19816 110544438
Atrial thrombosis 19.00 13.62 12 25033 4334 110559920
Hepatic enzyme increased 18.98 13.62 27 25018 320865 110243389
Pleural effusion 18.84 13.62 85 24960 177624 110386630
Thoracotomy 18.69 13.62 5 25040 190 110564064
Haemophilic arthropathy 18.16 13.62 5 25040 212 110564042
Parenteral nutrition 17.96 13.62 7 25038 893 110563361
Wound 17.93 13.62 16 25029 234421 110329833
Extravasation 17.81 13.62 12 25033 4833 110559421
Urine ketone body present 17.77 13.62 11 25034 3835 110560419
Liver injury 17.66 13.62 6 25039 150407 110413847
Therapeutic product effect incomplete 17.45 13.62 15 25030 223790 110340464
Nasopharyngitis 17.23 13.62 40 25005 394321 110169933
Osteoarthritis 17.18 13.62 10 25035 182613 110381641
Pain in extremity 17.10 13.62 55 24990 487063 110077191
Heparin resistance 17.06 13.62 5 25040 266 110563988
Fibroma 17.03 13.62 7 25038 1025 110563229
Mouth haemorrhage 16.99 13.62 18 25027 13470 110550784
Urticaria 16.98 13.62 127 24918 318730 110245524
Cholestasis 16.97 13.62 42 25003 64476 110499778
Venoocclusive liver disease 16.90 13.62 19 25026 15188 110549066
Gastrointestinal disorder 16.78 13.62 18 25027 241934 110322320
Disseminated intravascular coagulation 16.73 13.62 32 25013 41254 110523000
Intracardiac thrombus 16.72 13.62 11 25034 4257 110559997
Intentional product use issue 16.59 13.62 19 25026 247887 110316367
Arthralgia 16.58 13.62 106 24939 779526 109784728
Blood bilirubin increased 16.46 13.62 46 24999 75926 110488328
Anti factor VIII antibody positive 16.38 13.62 4 25041 105 110564149
Haemophilia 16.34 13.62 4 25041 106 110564148
Cancer pain 16.32 13.62 13 25032 6759 110557495
Weight decreased 16.32 13.62 53 24992 468004 110096250
Bronchial artery embolisation 16.21 13.62 3 25042 19 110564235
Hospitalisation 16.19 13.62 6 25039 142487 110421767
Haemorrhagic disorder 16.17 13.62 8 25037 1805 110562449
Sepsis 16.10 13.62 128 24917 327218 110237036
Hepatic cyst ruptured 16.07 13.62 3 25042 20 110564234
Infusion site discomfort 16.07 13.62 8 25037 1829 110562425
Traumatic haemorrhage 16.04 13.62 8 25037 1836 110562418
Spontaneous haemorrhage 15.97 13.62 7 25038 1201 110563053
Postpartum haemorrhage 15.86 13.62 8 25037 1881 110562373
Swelling 15.83 13.62 35 25010 351006 110213248
Urinary tract disorder 15.78 13.62 12 25033 5832 110558422
Pulmonary alveolar haemorrhage 15.63 13.62 21 25024 20129 110544125
Rectal haemorrhage 15.57 13.62 61 24984 119772 110444482
Fall 15.56 13.62 77 24968 603405 109960849
PCO2 abnormal 15.47 13.62 4 25041 133 110564121
Pulseless electrical activity 15.40 13.62 19 25026 16738 110547516
Premature delivery 15.30 13.62 26 25019 30606 110533648
HER2 positive breast cancer 15.23 13.62 5 25040 388 110563866
Allergic reaction to excipient 15.19 13.62 6 25039 793 110563461
Myelodysplastic syndrome 15.13 13.62 29 25016 37455 110526799
Sinus tachycardia 15.06 13.62 32 25013 44461 110519793
Platelet count abnormal 15.01 13.62 12 25033 6270 110557984
Ischaemia 14.91 13.62 14 25031 9069 110555185
Neuromuscular blocking therapy 14.90 13.62 3 25042 31 110564223
Adnexal torsion 14.72 13.62 5 25040 431 110563823
Uterine leiomyoma 14.72 13.62 13 25032 7787 110556467
Fibrin degradation products increased 14.71 13.62 5 25040 432 110563822
Arterial thrombosis 14.61 13.62 9 25036 3110 110561144
Cyanosis 14.53 13.62 25 25020 29716 110534538
Memory impairment 14.40 13.62 14 25031 196930 110367324
Haematoma 14.27 13.62 37 25008 58439 110505815
Obesity 14.24 13.62 4 25041 113347 110450907
Infusion site rash 14.24 13.62 8 25037 2335 110561919
Psoriasis 14.14 13.62 7 25038 139986 110424268
Device related infection 14.05 13.62 29 25016 39490 110524764
Intentional self-injury 13.94 13.62 28 25017 37401 110526853
Pneumonia 13.91 13.62 277 24768 876437 109687817
Neutrophil count decreased 13.69 13.62 59 24986 120882 110443372
Ventricular tachycardia 13.63 13.62 33 25012 49976 110514278

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B02AA02 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
ANTIFIBRINOLYTICS
Amino acids
MeSH PA D000933 Antifibrinolytic Agents
MeSH PA D003029 Coagulants
MeSH PA D006401 Hematologic Agents
MeSH PA D006490 Hemostatics
FDA PE N0000175632 Decreased Fibrinolysis
FDA EPC N0000175634 Antifibrinolytic Agent
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:48675 antifibrinolytic drug
CHEBI has role CHEBI:50248 hematologic agent
CHEBI has role CHEBI:55324 gastrointestinal drug
CHEBI has role CHEBI:62868 hepatoprotective agent
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:73336 vulnerary
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

B02AA Amino acids 2 drugs

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

DiseaseRelationSNOMED_IDDOID
Contraception indication 13197004
Female hypogonadism syndrome indication 16041008
Endometriosis indication 129103003
Menorrhagia indication 386692008
Hemorrhaging in Hemophilia indication
Refractory melasma off-label use 36209000
Epistaxis off-label use 249366005
Hyperfibrinolysis Induced Hemorrhage off-label use
Prevention of Hemorrhage with Cardiovascular Instability from Cardiopulmonary Bypass - CABG off-label use
Postsurgical Hemorrhage off-label use
Heart valve disorder contraindication 368009 DOID:4079
Cerebral edema contraindication 2032001
Hypercholesterolemia contraindication 13644009
Subarachnoid intracranial hemorrhage contraindication 21454007
Myocardial infarction contraindication 22298006 DOID:5844
Depressive disorder contraindication 35489007
Migraine contraindication 37796009 DOID:6364
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Body fluid retention contraindication 43498006
Thrombosis of retinal vein contraindication 46085004
Hyperlipidemia contraindication 55822004 DOID:1168
Benign mammary dysplasia contraindication 57993004
Obstructive hyperbilirubinemia contraindication 59848001
Thrombophlebitis contraindication 64156001 DOID:3875
Intermenstrual bleeding - irregular contraindication 64996003
Cerebral arterial thrombosis contraindication 71444005
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Malignant neoplasm of liver contraindication 93870000 DOID:3571
Deep venous thrombosis contraindication 128053003
Angina pectoris contraindication 194828000
Impaired renal function disorder contraindication 197663003
Cerebrovascular accident contraindication 230690007
Pulmonary thromboembolism contraindication 233935004
Thrombophilia contraindication 234467004 DOID:2452
Disease of liver contraindication 235856003 DOID:409
Cholestasis of pregnancy contraindication 235888006
Endometrial carcinoma contraindication 254878006 DOID:2871
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Malignant tumor of cervix contraindication 363354003 DOID:4362
Thromboembolic disorder contraindication 371039008
Cardiovascular event risk contraindication 395112001
Ligneous conjunctivitis contraindication 403435005
Disorder of coronary artery contraindication 414024009
Obesity contraindication 414916001 DOID:9970
Estrogen receptor positive tumor contraindication 416053008
Porphyria contraindication 418470004
Thrombosis contraindication 439127006
Hypertensive urgency contraindication 443482000
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002
Major Surgery with Prolonged Post-Operative Immobilization contraindication
Nonspecific Abnormal Papanicolaou Smear of Cervix contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.31 acidic
pKa2 10.7 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
Plasminogen Enzyme INHIBITOR Kd 5.96 CHEMBL CHEMBL

External reference:

IDSource
4020569 VUID
N0000148271 NUI
D01136 KEGG_DRUG
4020569 VANDF
C0040613 UMLSCUI
CHEBI:48669 CHEBI
CHEMBL877 ChEMBL_ID
DB00302 DRUGBANK_ID
D014148 MESH_DESCRIPTOR_UI
5526 PUBCHEM_CID
2060 INN_ID
6573 IUPHAR_LIGAND_ID
6T84R30KC1 UNII
10691 RXNORM
5607 MMSL
80873 MMSL
d00529 MMSL
002073 NDDF
109006003 SNOMEDCT_US
386960009 SNOMEDCT_US
6T84R30KC1 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cyklokapron HUMAN PRESCRIPTION DRUG LABEL 1 0013-1114 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 30 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 0517-0960 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 30 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 0591-3720 TABLET, FILM COATED 650 mg ORAL ANDA 25 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 14593-318 INJECTION, SOLUTION 1 g INTRAVENOUS ANDA 2 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 14789-115 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 26 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 23155-166 INJECTION, SOLUTION 1 g INTRAVENOUS ANDA 26 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 23155-524 INJECTION, SOLUTION 1 g INTRAVENOUS ANDA 23 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 23155-909 INJECTION 100 mg INTRAVENOUS ANDA 18 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 23155-910 INJECTION 100 mg INTRAVENOUS ANDA 18 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 25021-415 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 25021-415 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 25021-418 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 27 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 39822-1000 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 31 sections
TRANEXAMIC ACID HUMAN PRESCRIPTION DRUG LABEL 1 42571-189 INJECTION 100 mg INTRAVENOUS ANDA 28 sections
TRANEXAMIC ACID HUMAN PRESCRIPTION DRUG LABEL 1 42571-314 INJECTION 100 mg INTRAVENOUS ANDA 28 sections
TRANEXAMIC ACID HUMAN PRESCRIPTION DRUG LABEL 1 43066-008 INJECTION 100 mg INTRAVENOUS ANDA 27 sections
TRANEXAMIC ACID HUMAN PRESCRIPTION DRUG LABEL 1 43066-008 INJECTION 100 mg INTRAVENOUS ANDA 27 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 50090-4530 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 30 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 50268-772 TABLET 650 mg ORAL NDA authorized generic 28 sections
TRANEXAMIC ACID HUMAN PRESCRIPTION DRUG LABEL 1 51662-1532 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 16 sections
TRANEXAMIC ACID IN SODIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51754-0108 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 25 sections
Tranexamic Acid Human Prescription Drug Label 1 55150-188 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
TRANEXAMIC ACID Human Prescription Drug Label 1 59651-839 TABLET 650 mg ORAL ANDA 27 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 60505-6169 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 60687-750 TABLET 650 mg ORAL ANDA 29 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 62559-265 TABLET 650 mg ORAL ANDA 29 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 63629-8599 TABLET, FILM COATED 650 mg ORAL ANDA 26 sections
Tranexamic Acid HUMAN PRESCRIPTION DRUG LABEL 1 63629-8838 TABLET, FILM COATED 650 mg ORAL ANDA 26 sections
Tranexamic Acid Human Prescription Drug Label 1 65145-106 INJECTION 100 mg INTRAVENOUS ANDA 27 sections
TRANEXAMIC ACID IN SODIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 65219-534 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 26 sections