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

Stem definitionDrug idCAS RN
vasopressin receptor antagonists 4110 150683-30-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • OPC 41061
  • jinarc
  • tolvaptan
  • samsca
  • OPC-41061
  • tolvaptan sodium phosphate
A benzazepine derivative and selective VASOPRESSIN V2 RECEPTOR antagonist that is used to treat euvolemic and hypervolemic HYPONATREMIA. It is also used in the treatment of rapidly progressing AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE to slow the rate of cyst development and renal insufficiency.
  • Molecular weight: 448.95
  • Formula: C26H25ClN2O3
  • CLOGP: 3.91
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 69.64
  • ALOGS: -5.56
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
30 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.91 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.50 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) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.90 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 56 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,STK33,TTK 20
kinase-selectivity-class GRK2,PDK4,TTK 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1

Approvals:

DateAgencyCompanyOrphan
Oct. 27, 2010 PMDA Otsuka Pharmaceutical Co., Ltd
Feb. 26, 2015 EMA
May 19, 2009 FDA OTSUKA AMERICA PHARM

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
Thirst 649.57 21.90 194 14036 16101 90598116
Polyuria 463.51 21.90 134 14096 9906 90604311
Renal impairment 447.21 21.90 250 13980 105171 90509046
Hypernatraemia 409.92 21.90 120 14110 9267 90604950
Rapid correction of hyponatraemia 409.15 21.90 60 14170 94 90614123
Cardiac failure 344.16 21.90 214 14016 109282 90504935
Nocturia 314.83 21.90 100 14130 10155 90604062
Polydipsia 299.38 21.90 79 14151 4152 90610065
Hepatic function abnormal 293.96 21.90 144 14086 46144 90568073
Incorrect product administration duration 292.01 21.90 111 14119 19211 90595006
Glomerular filtration rate decreased 276.68 21.90 103 14127 16829 90597388
Underdose 225.68 21.90 127 14103 53890 90560327
Blood urea increased 221.54 21.90 104 14126 30309 90583908
Blood sodium decreased 209.10 21.90 97 14133 27516 90586701
Inappropriate schedule of product administration 174.69 21.90 162 14068 149771 90464446
Blood creatinine increased 161.49 21.90 131 14099 101255 90512962
Blood sodium increased 144.69 21.90 42 14188 3140 90611077
Alanine aminotransferase increased 138.03 21.90 128 14102 118210 90496007
Death 131.34 21.90 247 13983 456304 90157913
Cardiac failure chronic 128.76 21.90 44 14186 5602 90608615
Pollakiuria 122.80 21.90 72 14158 32933 90581284
Wrong technique in product usage process 121.42 21.90 96 14134 71475 90542742
Aspartate aminotransferase increased 121.30 21.90 112 14118 102825 90511392
Dehydration 116.63 21.90 148 14082 194299 90419918
Brain natriuretic peptide increased 114.67 21.90 41 14189 5964 90608253
Renal transplant 102.77 21.90 28 14202 1660 90612557
Platelet count decreased 96.27 21.90 113 14117 136856 90477361
Blood pressure decreased 93.10 21.90 84 14146 74811 90539406
Drug monitoring procedure incorrectly performed 86.68 21.90 18 14212 325 90613892
Pulmonary arterial hypertension 84.14 21.90 52 14178 26135 90588082
Dialysis 71.10 21.90 35 14195 11294 90602923
Polycystic liver disease 68.04 21.90 10 14220 16 90614201
Hyponatraemia 66.69 21.90 93 14137 133445 90480772
Drug ineffective 65.45 21.90 73 14157 1384225 89229992
Concomitant disease aggravated 64.68 21.90 33 14197 11485 90602732
Pulmonary congestion 63.47 21.90 39 14191 19394 90594823
Gallbladder polyp 63.30 21.90 17 14213 954 90613263
Pain 61.01 21.90 41 14189 996300 89617917
Therapy cessation 59.97 21.90 48 14182 36313 90577904
Blood uric acid increased 58.08 21.90 27 14203 7677 90606540
Urine output increased 57.44 21.90 18 14212 1744 90612473
Renal cyst ruptured 57.12 21.90 9 14221 28 90614189
Renal cyst haemorrhage 56.94 21.90 10 14220 69 90614148
Liver transplant 56.53 21.90 19 14211 2298 90611919
Hepatic encephalopathy 56.42 21.90 32 14198 13740 90600477
Pleural effusion 55.91 21.90 78 14152 111913 90502304
Liver disorder 55.45 21.90 81 14149 121188 90493029
Nephrogenic anaemia 55.37 21.90 19 14211 2447 90611770
Joint swelling 55.24 21.90 7 14223 503293 90110924
Cerebral infarction 54.60 21.90 40 14190 26556 90587661
Drug hypersensitivity 54.57 21.90 5 14225 463604 90150613
Hyperkalaemia 53.09 21.90 58 14172 64906 90549311
Hyperuricaemia 52.06 21.90 24 14206 6695 90607522
Defect conduction intraventricular 51.67 21.90 11 14219 225 90613992
Swelling 50.73 21.90 4 14226 419054 90195163
Drug titration error 50.40 21.90 15 14215 1222 90612995
Transplant 48.37 21.90 14 14216 1035 90613182
Ascites 46.83 21.90 47 14183 47693 90566524
Renal cyst infection 45.62 21.90 9 14221 124 90614093
Concomitant disease progression 45.50 21.90 16 14214 2216 90612001
Rash 44.47 21.90 36 14194 796064 89818153
Incorrect dose administered 43.98 21.90 58 14172 78872 90535345
Arthralgia 43.74 21.90 35 14195 778487 89835730
End stage renal disease 43.65 21.90 23 14207 8548 90605669
Product use in unapproved indication 42.91 21.90 133 14097 336103 90278114
Marasmus 42.51 21.90 12 14218 811 90613406
Right ventricular failure 41.96 21.90 30 14200 19175 90595042
Inability to afford medication 41.34 21.90 17 14213 3605 90610612
Alopecia 39.88 21.90 14 14216 495057 90119160
Rheumatoid arthritis 39.87 21.90 5 14225 362609 90251608
Hypersensitivity 38.12 21.90 12 14218 454665 90159552
Blood sodium abnormal 37.81 21.90 11 14219 828 90613389
Blood potassium increased 37.68 21.90 29 14201 20720 90593497
Blood alkaline phosphatase increased 37.67 21.90 42 14188 48037 90566180
Hepatic cyst 37.40 21.90 19 14211 6549 90607668
Drug intolerance 37.19 21.90 12 14218 447579 90166638
Hepatic failure 36.94 21.90 38 14192 39690 90574527
Treatment failure 36.49 21.90 3 14227 303925 90310292
Incorrect drug administration rate 35.37 21.90 17 14213 5206 90609011
Renal pain 34.42 21.90 19 14211 7740 90606477
Abdominal discomfort 34.36 21.90 16 14214 477312 90136905
Toxicity to various agents 34.12 21.90 3 14227 287843 90326374
Product dose omission issue 34.11 21.90 112 14118 291575 90322642
Blood bilirubin increased 34.10 21.90 38 14192 43432 90570785
Pulmonary hypertension 33.06 21.90 37 14193 42486 90571731
Urine output decreased 32.98 21.90 22 14208 12581 90601636
Discomfort 32.14 21.90 3 14227 274332 90339885
Transaminases increased 31.77 21.90 34 14196 37158 90577059
Contraindicated product administered 31.58 21.90 6 14224 320133 90294084
Osmotic demyelination syndrome 31.18 21.90 10 14220 1044 90613173
Altered state of consciousness 30.84 21.90 31 14199 31501 90582716
Insurance issue 30.79 21.90 20 14210 10938 90603279
Hospitalisation 29.11 21.90 63 14167 128037 90486180
Urticaria 28.53 21.90 7 14223 312727 90301490
Therapy interrupted 28.18 21.90 37 14193 50071 90564146
Hypokalaemia 28.11 21.90 63 14167 131053 90483164
Gamma-glutamyltransferase increased 27.77 21.90 32 14198 37920 90576297
Blood chloride increased 26.55 21.90 12 14218 3198 90611019
Low cardiac output syndrome 25.51 21.90 7 14223 426 90613791
Upper respiratory tract inflammation 25.36 21.90 11 14219 2661 90611556
Peripheral swelling 25.18 21.90 17 14213 413089 90201128
Immobilisation syndrome 24.90 21.90 7 14223 466 90613751
Anxiety 24.51 21.90 9 14221 309763 90304454
Transfusion 24.48 21.90 21 14209 17467 90596750
Alanine aminotransferase decreased 24.46 21.90 8 14222 889 90613328
Sinusitis 23.91 21.90 12 14218 343076 90271141
Therapeutic product effect decreased 23.83 21.90 7 14223 277564 90336653
Off label use 23.48 21.90 270 13960 1101982 89512235
Stomatitis 23.45 21.90 7 14223 274691 90339526
Aortic valve stenosis 23.37 21.90 12 14218 4228 90609989
Uraemic encephalopathy 23.15 21.90 6 14224 293 90613924
Hepatotoxicity 22.96 21.90 32 14198 45810 90568407
Pericarditis 22.85 21.90 7 14223 270144 90344073
Iron deficiency anaemia 22.66 21.90 23 14207 23639 90590578
Irritable bowel syndrome 22.45 21.90 3 14227 207445 90406772
Exposure during pregnancy 22.41 21.90 5 14225 238405 90375812
Cardiac failure acute 22.38 21.90 17 14213 11912 90602305
Decreased appetite 22.10 21.90 117 14113 376423 90237794
Paraesthesia 22.07 21.90 6 14224 250320 90363897
Ventricular fibrillation 22.01 21.90 18 14212 14026 90600191
Post transplant distal limb syndrome 21.93 21.90 6 14224 361 90613856

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
Hypernatraemia 557.90 19.32 180 12805 9852 42598498
Thirst 541.71 19.32 172 12813 8936 42599414
Renal impairment 395.49 19.32 301 12684 109927 42498423
Rapid correction of hyponatraemia 354.05 19.32 59 12926 118 42608232
Polyuria 302.33 19.32 114 12871 9897 42598453
Cardiac failure 279.74 19.32 243 12742 106613 42501737
Underdose 277.86 19.32 124 12861 16542 42591808
Incorrect product administration duration 276.43 19.32 93 12892 5787 42602563
Blood sodium increased 247.15 19.32 74 12911 3144 42605206
Hepatic function abnormal 211.69 19.32 153 12832 51414 42556936
Blood urea increased 208.98 19.32 128 12857 32665 42575685
Glomerular filtration rate decreased 190.37 19.32 95 12890 16256 42592094
Nocturia 163.89 19.32 78 12907 12034 42596316
Blood creatinine increased 162.03 19.32 183 12802 109820 42498530
Polydipsia 138.66 19.32 52 12933 4436 42603914
Cardiac failure chronic 115.31 19.32 57 12928 9544 42598806
Inappropriate schedule of product administration 99.73 19.32 134 12851 95768 42512582
Wrong technique in product usage process 97.43 19.32 90 12895 42545 42565805
Dehydration 94.57 19.32 161 12824 141606 42466744
Renal transplant 89.37 19.32 32 12953 2393 42605957
Hepatic encephalopathy 89.17 19.32 58 12927 16384 42591966
Blood sodium decreased 86.28 19.32 59 12926 18103 42590247
Low cardiac output syndrome 81.71 19.32 22 12963 632 42607718
Dialysis 76.81 19.32 47 12938 11939 42596411
Alanine aminotransferase increased 76.26 19.32 113 12872 88293 42520057
Death 74.87 19.32 312 12673 470873 42137477
Drug monitoring procedure incorrectly performed 73.74 19.32 18 12967 346 42608004
Osmotic demyelination syndrome 72.22 19.32 22 12963 990 42607360
Aspartate aminotransferase increased 71.44 19.32 102 12883 77061 42531289
Hyperuricaemia 68.29 19.32 40 12945 9384 42598966
Altered state of consciousness 63.42 19.32 60 12925 29199 42579151
Blood potassium increased 58.31 19.32 47 12938 18489 42589861
Pulmonary arterial hypertension 57.85 19.32 37 12948 10150 42598200
Blood pressure decreased 56.77 19.32 79 12906 58253 42550097
Urine output increased 56.36 19.32 20 12965 1456 42606894
Hyperkalaemia 55.70 19.32 93 12892 80365 42527985
Toxicity to various agents 49.24 19.32 6 12979 229130 42379220
Renal cyst haemorrhage 49.23 19.32 15 12970 675 42607675
Renal cyst ruptured 49.01 19.32 9 12976 38 42608312
Concomitant disease aggravated 45.22 19.32 27 12958 6559 42601791
Pollakiuria 44.71 19.32 44 12941 22461 42585889
Cerebral infarction 39.33 19.32 48 12937 31121 42577229
Liver disorder 39.02 19.32 54 12931 39590 42568760
Right ventricular failure 38.32 19.32 28 12957 9527 42598823
Pain 37.32 19.32 14 12971 244834 42363516
Product use issue 35.90 19.32 75 12910 76676 42531674
Urine osmolarity decreased 35.14 19.32 7 12978 49 42608301
Oedema 33.18 19.32 58 12927 51943 42556407
Urine output decreased 32.98 19.32 27 12958 10846 42597504
Product use in unapproved indication 32.94 19.32 127 12858 184329 42424021
Drug titration error 31.73 19.32 11 12974 747 42607603
Therapy cessation 31.67 19.32 35 12950 20415 42587935
Cardiac failure acute 31.54 19.32 29 12956 13604 42594746
Drug ineffective 31.24 19.32 94 12891 630103 41978247
Arthralgia 30.82 19.32 12 12973 205226 42403124
Liver injury 30.05 19.32 33 12952 19115 42589235
Renal cyst infection 29.94 19.32 7 12978 111 42608239
Incorrect drug administration rate 29.47 19.32 14 12971 2146 42606204
Neutropenia 29.39 19.32 12 12973 199419 42408931
Pulmonary congestion 28.02 19.32 29 12956 15701 42592649
Prescribed underdose 28.02 19.32 24 12961 10258 42598092
Procedural failure 27.78 19.32 6 12979 65 42608285
Cardiac failure congestive 26.27 19.32 71 12914 85531 42522819
Marasmus 26.25 19.32 10 12975 889 42607461
Gamma-glutamyltransferase increased 25.79 19.32 40 12945 32457 42575893
Hepatic failure 24.96 19.32 43 12942 38057 42570293
Disseminated intravascular coagulation 24.73 19.32 34 12951 24760 42583590
Febrile neutropenia 24.53 19.32 13 12972 185690 42422660
Hyponatraemia 24.27 19.32 77 12908 101385 42506965
Blood bilirubin increased 24.23 19.32 45 12940 42207 42566143
Fluid intake reduced 23.77 19.32 15 12970 4017 42604333
Blood chloride increased 22.92 19.32 14 12971 3542 42604808
Hepatic enzyme increased 22.88 19.32 46 12939 45738 42562612
Renal pain 22.66 19.32 14 12971 3613 42604737
Congestive hepatopathy 22.40 19.32 12 12973 2370 42605980
Transplant 22.19 19.32 9 12976 945 42607405
Pleural effusion 21.67 19.32 72 12913 97094 42511256
Nephrogenic anaemia 21.47 19.32 12 12973 2574 42605776
Neuropathy peripheral 21.05 19.32 3 12982 101850 42506500
Fatigue 20.79 19.32 66 12919 435575 42172775
Inability to afford medication 20.79 19.32 11 12974 2119 42606231
N-terminal prohormone brain natriuretic peptide increased 20.74 19.32 13 12972 3440 42604910
Carbon dioxide decreased 20.72 19.32 11 12974 2133 42606217
Rash 20.50 19.32 33 12952 276921 42331429
Drug monitoring procedure not performed 20.26 19.32 7 12978 471 42607879
Oesophageal varices haemorrhage 20.22 19.32 13 12972 3594 42604756
Pulmonary hypertension 20.10 19.32 30 12955 23539 42584811
Hepatocellular carcinoma 20.07 19.32 18 12967 8176 42600174
Haemorrhagic cyst 20.06 19.32 5 12980 105 42608245
Pulmonary vein occlusion 19.39 19.32 4 12981 34 42608316

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
Thirst 1107.92 19.01 339 24366 21368 110543226
Hypernatraemia 946.18 19.01 287 24418 17546 110547048
Renal impairment 731.78 19.01 479 24226 187966 110376628
Cardiac failure 592.77 19.01 420 24285 187206 110377388
Polyuria 577.26 19.01 197 24508 17541 110547053
Hepatic function abnormal 499.64 19.01 287 24418 89008 110475586
Rapid correction of hyponatraemia 492.53 19.01 78 24627 155 110564439
Blood urea increased 419.39 19.01 217 24488 54740 110509854
Glomerular filtration rate decreased 392.71 19.01 170 24535 28786 110535808
Nocturia 383.78 19.01 144 24561 16846 110547748
Underdose 357.27 19.01 205 24500 63349 110501245
Blood sodium increased 349.76 19.01 102 24603 5421 110559173
Polydipsia 349.52 19.01 110 24595 7578 110557016
Blood creatinine increased 320.47 19.01 290 24415 182599 110381995
Incorrect product administration duration 276.77 19.01 120 24585 20378 110544216
Cardiac failure chronic 220.21 19.01 91 24614 13720 110550874
Alanine aminotransferase increased 215.07 19.01 234 24471 183539 110381055
Pollakiuria 207.56 19.01 127 24578 44068 110520526
Aspartate aminotransferase increased 201.85 19.01 212 24493 159724 110404870
Dehydration 193.09 19.01 273 24432 279238 110285356
Death 186.41 19.01 452 24253 698417 109866177
Inappropriate schedule of product administration 166.56 19.01 216 24489 203421 110361173
Hepatic encephalopathy 147.68 19.01 87 24618 28169 110536425
Blood sodium decreased 142.35 19.01 95 24610 38224 110526370
Blood pressure decreased 138.82 19.01 149 24556 114942 110449652
Pulmonary arterial hypertension 136.29 19.01 87 24618 32481 110532113
Hyperuricaemia 130.13 19.01 64 24641 14467 110550127
Renal transplant 121.26 19.01 40 24665 3198 110561396
Drug monitoring procedure incorrectly performed 119.40 19.01 29 24676 754 110563840
Brain natriuretic peptide increased 108.29 19.01 52 24653 11157 110553437
Urine output increased 106.68 19.01 35 24670 2751 110561843
Hyperkalaemia 106.22 19.01 141 24564 135655 110428939
Low cardiac output syndrome 104.71 19.01 28 24677 1078 110563516
Cerebral infarction 102.17 19.01 88 24617 51750 110512844
Renal cyst haemorrhage 99.95 19.01 25 24680 736 110563858
Concomitant disease aggravated 97.82 19.01 55 24650 16309 110548285
Pain 94.29 19.01 48 24657 954907 109609687
Altered state of consciousness 90.31 19.01 86 24619 57540 110507054
Liver disorder 89.39 19.01 133 24572 142110 110422484
Wrong technique in product usage process 86.35 19.01 102 24603 87246 110477348
Blood potassium increased 83.49 19.01 65 24640 33184 110531410
Drug titration error 80.85 19.01 25 24680 1622 110562972
Osmotic demyelination syndrome 79.33 19.01 26 24679 2037 110562557
Pulmonary congestion 78.76 19.01 61 24644 30905 110533689
Right ventricular failure 76.85 19.01 56 24649 25898 110538696
Toxicity to various agents 76.24 19.01 9 24696 480546 110084048
Nephrogenic anaemia 75.81 19.01 31 24674 4546 110560048
Drug ineffective 75.51 19.01 141 24564 1520399 109044195
Arthralgia 74.22 19.01 41 24664 779591 109785003
Marasmus 71.90 19.01 23 24682 1668 110562926
Platelet count decreased 70.89 19.01 158 24547 230285 110334309
Renal cyst ruptured 70.18 19.01 13 24692 84 110564510
Infusion related reaction 69.05 19.01 4 24701 381158 110183436
Renal cyst infection 67.37 19.01 15 24690 263 110564331
No adverse event 66.08 19.01 82 24623 73757 110490837
Urine output decreased 66.02 19.01 46 24659 19830 110544764
Pleural effusion 65.27 19.01 131 24574 177578 110387016
Therapy cessation 62.90 19.01 63 24642 44794 110519800
Hyponatraemia 62.25 19.01 145 24560 217508 110347086
Drug hypersensitivity 61.89 19.01 13 24692 454077 110110517
Joint swelling 61.77 19.01 12 24693 442833 110121761
Blood bilirubin increased 58.01 19.01 78 24627 75894 110488700
Swelling 57.11 19.01 6 24699 351035 110213559
Hepatic failure 56.23 19.01 73 24632 68666 110495928
Blood uric acid increased 56.04 19.01 43 24662 21486 110543108
Urine osmolarity decreased 54.34 19.01 11 24694 119 110564475
Off label use 53.60 19.01 540 24165 1499645 109064949
Ascites 52.94 19.01 83 24622 92725 110471869
Product dose omission issue 52.80 19.01 175 24530 321607 110242987
Gamma-glutamyltransferase increased 51.54 19.01 66 24639 61243 110503351
Rash 51.26 19.01 65 24640 820899 109743695
Pulmonary hypertension 50.49 19.01 62 24643 55158 110509436
Product use in unapproved indication 49.91 19.01 215 24490 447162 110117432
Cardiac failure acute 49.72 19.01 42 24663 24036 110540558
Rheumatoid arthritis 49.04 19.01 5 24700 299608 110264986
Gallbladder polyp 48.60 19.01 16 24689 1271 110563323
Hypersensitivity 48.45 19.01 15 24690 403983 110160611
Concomitant disease progression 48.27 19.01 21 24684 3589 110561005
Blood chloride increased 48.08 19.01 25 24680 6347 110558247
Cardiac failure congestive 48.06 19.01 105 24600 150895 110413699
Product use issue 48.04 19.01 166 24539 311529 110253065
Treatment failure 47.04 19.01 4 24701 277230 110287364
Renal pain 45.52 19.01 28 24677 9789 110554805
Polycystic liver disease 45.09 19.01 10 24695 172 110564422
Alopecia 42.92 19.01 14 24691 364739 110199855
Blood alkaline phosphatase increased 42.64 19.01 65 24640 70870 110493724
Paraesthesia 41.85 19.01 6 24699 276515 110288079
Mobility decreased 41.47 19.01 3 24702 237419 110327175
Wound 40.84 19.01 3 24702 234434 110330160
Drug intolerance 40.65 19.01 20 24685 406492 110158102
Dialysis 40.06 19.01 34 24671 19585 110545009
Carbon dioxide decreased 39.90 19.01 20 24685 4704 110559890
Defect conduction intraventricular 39.89 19.01 12 24693 709 110563885
Completed suicide 39.78 19.01 4 24701 242377 110322217
Anxiety 39.29 19.01 14 24691 345064 110219530
Pneumonia aspiration 38.71 19.01 67 24638 81166 110483428
Neutropenia 38.11 19.01 18 24687 374602 110189992
Disseminated intravascular coagulation 37.17 19.01 46 24659 41240 110523354
Transfusion 36.12 19.01 36 24669 25436 110539158
Sinusitis 35.59 19.01 11 24694 296677 110267917
Hepatocellular carcinoma 35.49 19.01 24 24681 9856 110554738
Fluid intake reduced 35.16 19.01 21 24684 6965 110557629
Liver transplant 34.61 19.01 18 24687 4571 110560023
Therapeutic product effect decreased 33.25 19.01 7 24698 244309 110320285
Pain in extremity 33.11 19.01 36 24669 487082 110077512
Hepatic cyst 33.07 19.01 21 24684 7762 110556832
Lower respiratory tract infection 33.01 19.01 7 24698 243099 110321495
Abdominal discomfort 32.89 19.01 24 24681 393834 110170760
Chronic kidney disease 32.60 19.01 60 24645 76231 110488363
Stomatitis 32.44 19.01 10 24695 270232 110294362
Congestive hepatopathy 32.43 19.01 18 24687 5202 110559392
Blood sodium abnormal 32.34 19.01 12 24693 1358 110563236
Hypoaesthesia 32.11 19.01 15 24690 314208 110250386
Peripheral swelling 31.98 19.01 26 24679 404008 110160586
End stage renal disease 31.66 19.01 31 24674 21442 110543152
Hepatotoxicity 31.14 19.01 53 24652 63347 110501247
Incorrect dose administered 30.64 19.01 70 24635 103571 110461023
Confusional state 30.36 19.01 36 24669 468644 110095950
Urine osmolarity increased 30.33 19.01 8 24697 292 110564302
Procedural failure 29.93 19.01 7 24698 154 110564440
Urticaria 29.93 19.01 17 24688 318840 110245754
Atrial tachycardia 29.92 19.01 21 24684 9157 110555437
Transaminases increased 29.83 19.01 52 24653 63338 110501256
N-terminal prohormone brain natriuretic peptide increased 29.77 19.01 18 24687 6103 110558491
Intentional dose omission 29.62 19.01 29 24676 20051 110544543
Prerenal failure 29.42 19.01 16 24689 4443 110560151
Ventricular tachycardia 28.89 19.01 45 24660 49964 110514630
Pericarditis 28.37 19.01 7 24698 219107 110345487
Oesophageal varices haemorrhage 27.88 19.01 16 24689 4929 110559665
Fatigue 27.74 19.01 159 24546 1215799 109348795
Discomfort 27.53 19.01 7 24698 214700 110349894
Folliculitis 26.90 19.01 3 24702 167650 110396944
Exposure during pregnancy 26.86 19.01 3 24702 167421 110397173
Febrile neutropenia 26.84 19.01 19 24686 316748 110247846
Injury 26.46 19.01 4 24701 177261 110387333
Type 2 diabetes mellitus 26.45 19.01 4 24701 177228 110387366
Blood potassium decreased 26.26 19.01 45 24660 54069 110510525
Asthma 25.49 19.01 12 24693 250279 110314315
Insurance issue 25.03 19.01 20 24685 10592 110554002
Infected cyst 24.84 19.01 10 24695 1408 110563186
Cardiac dysfunction 24.49 19.01 16 24689 6207 110558387
Chest pain 24.27 19.01 29 24676 376346 110188248
Upper respiratory tract inflammation 24.26 19.01 14 24691 4357 110560237
Aortic valve stenosis 24.19 19.01 16 24689 6334 110558260
Gastrointestinal disorder 24.03 19.01 12 24693 241940 110322654
Drug dose titration not performed 23.94 19.01 9 24696 1056 110563538
Haemorrhagic cyst 23.52 19.01 7 24698 399 110564195
Iron deficiency anaemia 23.47 19.01 32 24673 31527 110533067
Renal failure 23.03 19.01 106 24599 226468 110338126
Colon cancer 22.87 19.01 23 24682 16420 110548174
Decreased appetite 22.83 19.01 183 24522 475663 110088931
Oedema 22.66 19.01 100 24605 209876 110354718
Transplant 22.37 19.01 9 24696 1265 110563329
Renal cyst aspiration 22.22 19.01 3 24702 0 110564594
Haemoglobin decreased 22.14 19.01 112 24593 248615 110315979
Alanine aminotransferase decreased 22.08 19.01 10 24695 1878 110562716
Wheezing 22.02 19.01 15 24690 255215 110309379
Immobilisation syndrome 21.88 19.01 8 24697 868 110563726
Irritable bowel syndrome 21.74 19.01 5 24700 164210 110400384
Blood urea nitrogen/creatinine ratio decreased 21.68 19.01 6 24699 263 110564331
Renal disorder 21.24 19.01 39 24666 49440 110515154
Flank pain 21.19 19.01 26 24679 23104 110541490
Red blood cell count decreased 21.14 19.01 46 24659 65877 110498717
Hepatorenal syndrome 21.03 19.01 13 24692 4584 110560010
Hypoalbuminaemia 20.98 19.01 29 24676 28945 110535649
Hyperhidrosis 20.63 19.01 8 24697 187290 110377304
Pulmonary vein occlusion 20.55 19.01 5 24700 131 110564463
Hypokalaemia 20.54 19.01 88 24617 182360 110382234
Human chorionic gonadotropin positive 20.53 19.01 4 24701 35 110564559
Asthenia 20.39 19.01 82 24623 688917 109875677
Interstitial lung disease 20.39 19.01 73 24632 139261 110425333
Blood cholesterol increased 20.18 19.01 8 24697 184777 110379817
Urine albumin/creatinine ratio increased 20.02 19.01 8 24697 1105 110563489
Depression 19.88 19.01 25 24680 317310 110247284
Glomerular filtration rate abnormal 19.87 19.01 10 24695 2373 110562221
Inability to afford medication 19.86 19.01 12 24693 4064 110560530
Contraindicated product administered 19.60 19.01 16 24689 248251 110316343
Gait disturbance 19.51 19.01 20 24685 278188 110286406
Maternal exposure during pregnancy 19.42 19.01 17 24688 254866 110309728
Neuropathy peripheral 19.19 19.01 8 24697 179269 110385325

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03XA01 CARDIOVASCULAR SYSTEM
DIURETICS
OTHER DIURETICS
Vasopressin antagonists
MeSH PA D045283 Natriuretic Agents
MeSH PA D065092 Antidiuretic Hormone Receptor Antagonists
FDA MoA N0000193178 Vasopressin V2 Receptor Antagonists
FDA EPC N0000193181 Vasopressin V2 Receptor Antagonist
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:59680 vasopressin receptor antagonist
CHEBI has role CHEBI:62868 hepatoprotective agent
CHEBI has role CHEBI:194423 aquaretic
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

C03XA Vasopressin antagonists 1 drug
conivaptan

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

DiseaseRelationSNOMED_IDDOID
Polycystic kidney disease, adult type indication 28728008
Syndrome of inappropriate vasopressin secretion indication 55004003 DOID:3401
Hyponatremia indication 89627008
Fluid retention in heart failure indication
Nutritional disorder contraindication 2492009 DOID:374
Alcoholism contraindication 7200002
Hyperkalemia contraindication 14140009
Cirrhosis of liver contraindication 19943007 DOID:5082
Hypovolemia contraindication 28560003
Demyelination contraindication 32693004
Dehydration contraindication 34095006
Hepatic failure contraindication 59927004
Gastrointestinal hemorrhage contraindication 74474003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.1 acidic

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
Vasopressin V2 receptor GPCR ANTAGONIST Ki 9 WOMBAT-PK DRUG LABEL
5-hydroxytryptamine receptor 2C GPCR Ki 5.31 CHEMBL
Histamine H1 receptor GPCR Ki 5.17 CHEMBL
Vasopressin V1a receptor GPCR ANTAGONIST Ki 7.90 IUPHAR
Mu-type opioid receptor GPCR Ki 6.39 CHEMBL
Transmembrane protein 97 Enzyme Ki 5.99 CHEMBL
Vasopressin V1a receptor GPCR ANTAGONIST Ki 6.50 IUPHAR
Vasopressin V2 receptor GPCR ANTAGONIST Ki 8.90 IUPHAR

External reference:

IDSource
4028789 VUID
N0000178481 NUI
D01213 KEGG_DRUG
4028789 VANDF
C1176308 UMLSCUI
CHEBI:32246 CHEBI
CHEMBL344159 ChEMBL_ID
D000077602 MESH_DESCRIPTOR_UI
DB06212 DRUGBANK_ID
2226 IUPHAR_LIGAND_ID
7969 INN_ID
21G72T1950 UNII
216237 PUBCHEM_CID
358257 RXNORM
165174 MMSL
26477 MMSL
334368 MMSL
d07447 MMSL
013121 NDDF
442901006 SNOMEDCT_US
443058000 SNOMEDCT_US
21G72T1950 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 31722-868 TABLET 15 mg ORAL ANDA 27 sections
Tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 31722-869 TABLET 30 mg ORAL ANDA 27 sections
Tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 49884-768 TABLET 15 mg ORAL ANDA 27 sections
Tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 49884-770 TABLET 30 mg ORAL ANDA 27 sections
SAMSCA HUMAN PRESCRIPTION DRUG LABEL 1 59148-020 TABLET 15 mg ORAL NDA 33 sections
SAMSCA HUMAN PRESCRIPTION DRUG LABEL 1 59148-021 TABLET 30 mg ORAL NDA 33 sections
JYNARQUE HUMAN PRESCRIPTION DRUG LABEL 1 59148-082 TABLET 15 mg ORAL NDA 33 sections
JYNARQUE HUMAN PRESCRIPTION DRUG LABEL 1 59148-082 TABLET 15 mg ORAL NDA 33 sections
JYNARQUE HUMAN PRESCRIPTION DRUG LABEL 1 59148-083 TABLET 30 mg ORAL NDA 33 sections
JYNARQUE HUMAN PRESCRIPTION DRUG LABEL 1 59148-083 TABLET 30 mg ORAL NDA 33 sections
tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 60505-4317 TABLET 15 mg ORAL ANDA 29 sections
tolvaptan HUMAN PRESCRIPTION DRUG LABEL 1 60505-4318 TABLET 30 mg ORAL ANDA 29 sections
Tolvaptan Human Prescription Drug Label 1 67877-635 TABLET 15 mg ORAL ANDA 28 sections
Tolvaptan Human Prescription Drug Label 1 67877-636 TABLET 30 mg ORAL ANDA 28 sections
Tolvaptan Human Prescription Drug Label 1 67877-637 TABLET 60 mg ORAL ANDA 28 sections
TOLVAPTAN HUMAN PRESCRIPTION DRUG LABEL 1 70748-238 TABLET 15 mg ORAL ANDA 26 sections
TOLVAPTAN HUMAN PRESCRIPTION DRUG LABEL 1 70748-239 TABLET 30 mg ORAL ANDA 26 sections
TOLVAPTAN Human Prescription Drug Label 1 72205-130 TABLET 15 mg ORAL ANDA 27 sections
TOLVAPTAN Human Prescription Drug Label 1 72205-131 TABLET 30 mg ORAL ANDA 27 sections
TOLVAPTAN Human Prescription Drug Label 1 72603-932 TABLET 15 mg ORAL ANDA 27 sections
TOLVAPTAN Human Prescription Drug Label 1 72603-933 TABLET 30 mg ORAL ANDA 27 sections