metolazone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1783 17560-51-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • SR72022
  • zaroxolyn
  • metolazone
  • metozalone
Metolazone is a quinazoline diuretic, with properties generally similar to the thiazide diuretics. The actions of metolazone result from interference with the renal tubular mechanism of electrolyte reabsorption. Metolazone acts primarily to inhibit sodium reabsorption at the cortical diluting site and to a lesser extent in the proximal convoluted tubule. Sodium and chloride ions are excreted in approximately equivalent amounts. The increased delivery of sodium to the distal tubular exchange site results in increased potassium excretion. Metolazone does not inhibit carbonic anhydrase. A proximal action of metolazone has been shown in humans by increased excretion of phosphate and magnesium ions and by a markedly increased fractional excretion of sodium in patients with severely compromised glomerular filtration. This action has been demonstrated in animals by micropuncture studies.
  • Molecular weight: 365.83
  • Formula: C16H16ClN3O3S
  • CLOGP: 2.06
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 92.50
  • ALOGS: -3.95
  • ROTB: 2

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
5 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.78 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 65 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 27, 1973 FDA UCB INC

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
Fluid retention 259.53 17.30 168 14860 53910 56223129
Cardiac failure congestive 255.58 17.30 201 14827 87519 56189520
Hypervolaemia 241.70 17.30 125 14903 26333 56250706
Pulmonary arterial hypertension 215.92 17.30 116 14912 26387 56250652
Right ventricular failure 180.78 17.30 88 14940 16291 56260748
Dyspnoea 145.67 17.30 415 14613 592162 55684877
Drug ineffective 122.00 17.30 47 14981 918942 55358097
Pulmonary hypertension 116.81 17.30 88 14940 35856 56241183
Acute kidney injury 110.86 17.30 216 14812 240547 56036492
Oedema peripheral 95.56 17.30 167 14861 171087 56105952
Oedema 93.08 17.30 112 14916 81808 56195231
Rheumatoid arthritis 82.37 17.30 5 15023 382599 55894440
Acute respiratory failure 75.30 17.30 64 14964 30930 56246109
Death 73.75 17.30 229 14799 341197 55935842
Electrolyte imbalance 71.91 17.30 50 14978 17983 56259056
Cardiac failure 70.89 17.30 98 14930 81995 56195044
Calcium deficiency 70.60 17.30 21 15007 996 56276043
Gastrointestinal haemorrhage 66.07 17.30 91 14937 75860 56201179
Cardiac failure acute 61.66 17.30 35 14993 8838 56268201
Dyspnoea exertional 60.82 17.30 74 14954 54615 56222424
Renal failure 60.57 17.30 107 14921 110393 56166646
Off label use 57.74 17.30 39 14989 556141 55720898
Hypoxia 56.83 17.30 71 14957 53826 56223213
Hospitalisation 55.18 17.30 83 14945 74917 56202122
Pulmonary oedema 53.33 17.30 67 14961 51076 56225963
Atrial fibrillation 51.55 17.30 99 14929 108798 56168241
Torsade de pointes 50.78 17.30 35 14993 12405 56264634
Hypokalaemia 49.88 17.30 90 14938 94347 56182692
Chronic kidney disease 48.54 17.30 58 14970 41998 56235041
Hypotension 48.51 17.30 162 14866 250346 56026693
Gout 44.35 17.30 32 14996 12189 56264850
Transfusion 43.67 17.30 33 14995 13487 56263552
BRASH syndrome 43.34 17.30 11 15017 286 56276753
Hyperkalaemia 42.80 17.30 60 14968 50805 56226234
Dermatitis exfoliative 42.57 17.30 23 15005 5276 56271763
Respiratory failure 42.04 17.30 84 14944 94978 56182061
Blood potassium decreased 40.84 17.30 51 14977 38621 56238418
Ascites 40.43 17.30 50 14978 37494 56239545
Cholecystitis 39.62 17.30 32 14996 14403 56262636
Joint swelling 39.57 17.30 14 15014 289786 55987253
Cor pulmonale 39.09 17.30 16 15012 1965 56275074
Arthralgia 39.03 17.30 46 14982 501623 55775416
Alopecia 38.68 17.30 15 15013 293443 55983596
Contraindicated product administered 38.38 17.30 3 15025 186283 56090756
Urine chloride decreased 38.14 17.30 8 15020 86 56276953
Systemic lupus erythematosus 36.82 17.30 3 15025 180075 56096964
Metabolic alkalosis 36.58 17.30 17 15011 2834 56274205
Therapeutic product effect decreased 34.16 17.30 3 15025 169449 56107590
Urine sodium decreased 33.47 17.30 8 15020 161 56276878
Chest pain 32.57 17.30 118 14910 189679 56087360
Rash 32.49 17.30 51 14977 492996 55784043
Synovitis 32.12 17.30 3 15025 161302 56115737
Blood creatinine increased 30.92 17.30 67 14961 80124 56196915
Cardiac arrest 30.90 17.30 70 14958 86244 56190795
Oxygen consumption increased 29.84 17.30 16 15012 3615 56273424
Drug intolerance 29.57 17.30 17 15011 264801 56012238
Dehydration 29.18 17.30 101 14927 158724 56118315
Pain in jaw 28.99 17.30 44 14984 39992 56237047
Arthropathy 28.50 17.30 9 15019 200266 56076773
Renal impairment 28.38 17.30 65 14963 80648 56196391
Weight increased 27.66 17.30 128 14900 229575 56047464
Discomfort 27.28 17.30 3 15025 141758 56135281
Blood urea increased 27.00 17.30 33 14995 24440 56252599
Respiratory disorder 27 17.30 39 14989 33918 56243121
Pericardial effusion 25.80 17.30 34 14994 27141 56249898
Pericardial haemorrhage 25.71 17.30 11 15017 1509 56275530
Generalised oedema 25.52 17.30 25 15003 14476 56262563
Hyperthyroidism 25.35 17.30 24 15004 13328 56263711
Cardiorenal syndrome 24.67 17.30 9 15019 811 56276228
Atrial flutter 24.47 17.30 20 15008 9149 56267890
Musculoskeletal stiffness 24.07 17.30 6 15022 156001 56121038
Multiple organ dysfunction syndrome 23.75 17.30 47 14981 52723 56224316
Paracentesis 23.54 17.30 9 15019 924 56276115
Toxic epidermal necrolysis 23.16 17.30 29 14999 22013 56255026
Localised oedema 22.61 17.30 15 15013 4994 56272045
Pulmonary arterial pressure increased 22.50 17.30 13 15015 3392 56273647
Bone density decreased 22.46 17.30 22 15006 12738 56264301
Hepatic enzyme increased 22.16 17.30 9 15019 171375 56105664
Cellulitis 21.69 17.30 56 14972 74893 56202146
Abdominal distension 21.44 17.30 57 14971 77569 56199470
Chronic obstructive pulmonary disease 21.02 17.30 47 14981 57368 56219671
Neutropenia 20.96 17.30 8 15020 158159 56118880
Vascular parkinsonism 20.63 17.30 5 15023 107 56276932
Orthopnoea 20.58 17.30 15 15013 5801 56271238
Oxygen therapy 20.21 17.30 10 15018 1913 56275126
Pulmonary arterial wedge pressure increased 19.86 17.30 6 15022 300 56276739
Oxygen saturation decreased 19.79 17.30 56 14972 79011 56198028
Haemodialysis 19.35 17.30 17 15011 8574 56268465
Device leakage 19.35 17.30 15 15013 6360 56270679
Epistaxis 19.31 17.30 50 14978 66973 56210066
Pleural effusion 18.96 17.30 58 14970 85422 56191617
Blood aldosterone abnormal 18.83 17.30 4 15024 46 56276993
Asthenia 18.82 17.30 156 14872 342817 55934222
Chronic left ventricular failure 18.71 17.30 6 15022 366 56276673
Blood potassium increased 18.60 17.30 23 15005 17238 56259801
Brain natriuretic peptide increased 18.59 17.30 13 15015 4713 56272326
Elephantiasis 18.39 17.30 3 15025 6 56277033
Renal disorder 17.94 17.30 30 14998 29575 56247464
Haemoglobin decreased 17.82 17.30 77 14951 134060 56142979
Restlessness 17.54 17.30 28 15000 26558 56250481
Syncope 17.47 17.30 66 14962 108133 56168906

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 congestive 254.62 17.46 220 11465 79167 31606492
Acute kidney injury 168.79 17.46 338 11347 279376 31406283
Fluid retention 120.67 17.46 88 11597 24714 31660945
Hypokalaemia 113.10 17.46 118 11567 53456 31632203
Hypervolaemia 89.30 17.46 65 11620 18186 31667473
Pulmonary hypertension 86.06 17.46 66 11619 19975 31665684
Hypotension 83.31 17.46 212 11473 204406 31481253
Cardiac failure 82.79 17.46 128 11557 85825 31599834
Oedema peripheral 62.47 17.46 130 11555 109709 31575950
Dyspnoea 58.92 17.46 266 11419 343213 31342446
Oedema 58.18 17.46 75 11610 42486 31643173
Blood creatinine increased 54.86 17.46 109 11576 88969 31596690
Right ventricular failure 53.47 17.46 35 11650 8247 31677412
Pulmonary arterial hypertension 52.67 17.46 37 11648 9784 31675875
Blood potassium increased 45.92 17.46 41 11644 15304 31670355
Venous pressure jugular increased 44.71 17.46 15 11670 760 31684899
Chronic kidney disease 44.36 17.46 62 11623 37913 31647746
Polyuria 38.69 17.46 28 11657 7755 31677904
Drug ineffective 38.55 17.46 54 11631 395519 31290140
Glomerular filtration rate decreased 38.10 17.46 33 11652 11832 31673827
Weight increased 37.89 17.46 90 11595 82857 31602802
Hypovolaemia 36.86 17.46 28 11657 8344 31677315
Gastrointestinal haemorrhage 34.96 17.46 87 11598 82462 31603197
Renal failure 33.73 17.46 111 11574 123219 31562440
Necrotising oesophagitis 33.58 17.46 11 11674 517 31685142
Blood pressure systolic decreased 33.09 17.46 20 11665 4099 31681560
Generalised oedema 32.97 17.46 30 11655 11471 31674188
Dehydration 31.49 17.46 106 11579 119005 31566654
Hyponatraemia 30.42 17.46 77 11608 73722 31611937
Blood urea increased 30.41 17.46 45 11640 28967 31656692
Off label use 30.34 17.46 51 11634 347223 31338436
Transfusion 30.26 17.46 24 11661 7616 31678043
Venous pressure jugular decreased 29.10 17.46 6 11679 41 31685618
Syncope 28.22 17.46 82 11603 85100 31600559
Orthopnoea 25.60 17.46 18 11667 4763 31680896
Blood potassium decreased 24.09 17.46 30 11655 16396 31669263
Cellulitis 23.99 17.46 54 11631 47964 31637695
Azotaemia 23.59 17.46 17 11668 4675 31680984
Peripheral swelling 23.11 17.46 66 11619 67799 31617860
Asthenia 22.08 17.46 150 11535 224605 31461054
Dizziness 21.43 17.46 136 11549 199011 31486648
Brain natriuretic peptide increased 20.79 17.46 16 11669 4860 31680799
Febrile neutropenia 19.95 17.46 10 11675 121839 31563820
Burkholderia test positive 19.94 17.46 9 11676 1013 31684646
Blood loss anaemia 19.93 17.46 19 11666 7700 31677959
Death 19.69 17.46 211 11474 360358 31325301
Neutropenia 19.50 17.46 14 11671 140350 31545309
Acute respiratory failure 19.27 17.46 36 11649 28019 31657640
Atrial fibrillation 19.24 17.46 88 11597 113695 31571964
Chronic obstructive pulmonary disease 18.46 17.46 47 11638 45119 31640540
Urine output decreased 18.39 17.46 20 11665 9466 31676193
Product use in unapproved indication 18.03 17.46 7 11678 99164 31586495
Blood sodium decreased 17.86 17.46 25 11660 15290 31670369
Sinus bradycardia 17.60 17.46 22 11663 12065 31673594

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 congestive 447.10 14.71 370 23901 135087 70769086
Fluid retention 340.42 14.71 232 24039 63153 70841020
Hypervolaemia 294.08 14.71 178 24093 39528 70864645
Acute kidney injury 250.20 14.71 520 23751 474104 70430069
Pulmonary arterial hypertension 232.27 14.71 143 24128 32712 70871461
Right ventricular failure 207.68 14.71 116 24155 22158 70882015
Pulmonary hypertension 178.40 14.71 139 24132 46397 70857776
Dyspnoea 166.34 14.71 608 23663 769452 70134721
Cardiac failure 143.30 14.71 209 24062 143332 70760841
Oedema 137.10 14.71 173 24098 103408 70800765
Hypokalaemia 130.91 14.71 191 24080 130997 70773176
Oedema peripheral 130.39 14.71 259 24012 227832 70676341
Drug ineffective 130.10 14.71 81 24190 939671 69964502
Hypotension 110.37 14.71 346 23925 404035 70500138
Off label use 95.99 14.71 69 24202 742991 70161182
Gastrointestinal haemorrhage 86.94 14.71 163 24108 137245 70766928
Rheumatoid arthritis 83.17 14.71 4 24267 291801 70612372
Acute respiratory failure 82.93 14.71 97 24174 53568 70850605
Death 81.07 14.71 367 23904 509694 70394479
Renal failure 79.71 14.71 190 24081 188880 70715293
Chronic kidney disease 79.17 14.71 101 24170 60956 70843217
Blood creatinine increased 78.74 14.71 160 24111 142841 70761332
Transfusion 69.41 14.71 55 24216 18781 70885392
Calcium deficiency 66.71 14.71 20 24251 756 70903417
Cardiac failure acute 66.46 14.71 52 24219 17435 70886738
Dyspnoea exertional 63.84 14.71 104 24167 78326 70825847
Atrial fibrillation 59.87 14.71 168 24103 184180 70719993
Blood potassium increased 59.09 14.71 59 24212 27267 70876906
Blood urea increased 58.02 14.71 75 24196 45834 70858339
Hypoxia 56.86 14.71 109 24162 93235 70810938
Dehydration 55.63 14.71 187 24084 225955 70678218
Pulmonary oedema 55.01 14.71 100 24171 82178 70821995
Generalised oedema 54.72 14.71 51 24220 21657 70882516
Weight increased 53.22 14.71 193 24078 242138 70662035
Infusion related reaction 52.37 14.71 4 24267 197530 70706643
Blood potassium decreased 51.58 14.71 68 24203 42353 70861820
Glomerular filtration rate decreased 50.85 14.71 48 24223 20708 70883465
Hospitalisation 48.55 14.71 95 24176 82473 70821700
Neutropenia 48.37 14.71 14 24257 257142 70647031
Orthopnoea 47.04 14.71 33 24238 9375 70894798
Polyuria 46.95 14.71 38 24233 13368 70890805
Metabolic alkalosis 45.47 14.71 24 24247 4092 70900081
Hyperkalaemia 44.73 14.71 107 24164 106484 70797689
Electrolyte imbalance 42.23 14.71 49 24222 26812 70877361
Syncope 41.58 14.71 138 24133 165571 70738602
Arthralgia 41.28 14.71 68 24203 503322 70400851
Hypovolaemia 41.13 14.71 38 24233 15955 70888218
Pain in jaw 39.44 14.71 60 24211 42609 70861564
Venous pressure jugular increased 38.09 14.71 15 24256 1297 70902876
Gout 37.91 14.71 43 24228 22963 70881210
Hyponatraemia 37.24 14.71 130 24141 159957 70744216
Brain natriuretic peptide increased 37.03 14.71 27 24244 8144 70896029
Urine sodium decreased 36.37 14.71 10 24261 276 70903897
Cardiorenal syndrome 36.10 14.71 15 24256 1489 70902684
Azotaemia 36.01 14.71 26 24245 7727 70896446
Joint swelling 35.97 14.71 21 24250 253190 70650983
Torsade de pointes 35.32 14.71 37 24234 18079 70886094
Treatment failure 35.32 14.71 4 24267 144138 70760035
Urine chloride decreased 35.06 14.71 8 24263 100 70904073
Respiratory failure 35.00 14.71 132 24139 168603 70735570
Cellulitis 34.91 14.71 93 24178 98835 70805338
Cor pulmonale 34.35 14.71 16 24255 2087 70902086
Alopecia 33.49 14.71 13 24258 198477 70705696
Chronic left ventricular failure 33.42 14.71 12 24259 803 70903370
Product use in unapproved indication 32.74 14.71 15 24256 207463 70696710
BRASH syndrome 32.35 14.71 11 24260 626 70903547
Oxygen therapy 31.95 14.71 16 24255 2446 70901727
Asthenia 31.77 14.71 266 24005 457400 70446773
Necrotising oesophagitis 31.14 14.71 11 24260 702 70903471
Ascites 30.72 14.71 70 24201 67477 70836696
International normalised ratio increased 30.64 14.71 78 24193 80648 70823525
Arthropathy 30.44 14.71 7 24264 150050 70754123
Febrile neutropenia 30.38 14.71 16 24255 204302 70699871
Chronic obstructive pulmonary disease 28.42 14.71 74 24197 77567 70826606
Paracentesis 28.18 14.71 12 24259 1266 70902907
Rash 27.92 14.71 86 24185 510476 70393697
Contraindicated product administered 27.87 14.71 6 24265 134606 70769567
Oxygen consumption increased 27.16 14.71 18 24253 4662 70899511
Dermatitis exfoliative 27.00 14.71 25 24246 10526 70893647
Atrial flutter 26.92 14.71 34 24237 20293 70883880
Chest pain 26.09 14.71 161 24110 251099 70653074
Musculoskeletal stiffness 26.06 14.71 9 24262 147751 70756422
Pericardial effusion 25.68 14.71 49 24222 41727 70862446
Discomfort 25.64 14.71 3 24268 105433 70798740
Venous pressure jugular decreased 25.60 14.71 6 24265 85 70904088
Blood sodium decreased 25.06 14.71 41 24230 30957 70873216
Cholecystitis 24.88 14.71 33 24238 20668 70883505
Renal impairment 24.56 14.71 106 24165 143831 70760342
Blood loss anaemia 23.80 14.71 27 24244 14414 70889759
Pulmonary arterial pressure increased 23.63 14.71 16 24255 4293 70899880
Peripheral swelling 22.95 14.71 149 24122 236414 70667759
Left ventricular failure 22.95 14.71 21 24250 8707 70895466
Hypertension 22.40 14.71 42 24229 295991 70608182
Systemic lupus erythematosus 22.23 14.71 4 24267 101898 70802275
White blood cell count decreased 21.59 14.71 16 24255 170125 70734048
Pericardial haemorrhage 21.40 14.71 15 24256 4253 70899920
Condition aggravated 21.40 14.71 232 24039 427403 70476770
Blood pressure systolic decreased 21.12 14.71 21 24250 9650 70894523
Stomatitis 20.72 14.71 9 24262 128502 70775671
Respiratory disorder 20.58 14.71 43 24228 39080 70865093
Malignant neoplasm progression 20.48 14.71 8 24263 121731 70782442
Renal disorder 20.26 14.71 42 24229 37967 70866206
Drug hypersensitivity 20.06 14.71 37 24234 262422 70641751
Haemodialysis 19.82 14.71 27 24244 17339 70886834
Localised oedema 19.80 14.71 18 24253 7403 70896770
Pulmonary arterial wedge pressure increased 19.53 14.71 7 24264 466 70903707
Vascular parkinsonism 19.53 14.71 5 24266 104 70904069
Lower respiratory tract infection 19.42 14.71 7 24264 111906 70792267
Dizziness 19.31 14.71 243 24028 463898 70440275
Oxygen saturation decreased 19.29 14.71 85 24186 116344 70787829
Blood pressure increased 18.88 14.71 22 24249 188495 70715678
Urine output decreased 18.79 14.71 26 24245 16944 70887229
Abdominal distension 18.56 14.71 78 24193 104591 70799582
Bone density decreased 18.15 14.71 21 24250 11453 70892720
Gastrointestinal arteriovenous malformation 18.04 14.71 8 24263 931 70903242
Blood aldosterone abnormal 17.84 14.71 4 24267 46 70904127
Haemoglobin decreased 17.38 14.71 125 24146 205034 70699139
Completed suicide 17.37 14.71 32 24239 227103 70677070
Catheter management 16.98 14.71 12 24259 3447 70900726
Elephantiasis 16.79 14.71 3 24268 9 70904164
Cardiomegaly 16.60 14.71 30 24241 24515 70879658
Device leakage 16.36 14.71 18 24253 9290 70894883
Pleural effusion 16.29 14.71 89 24182 132775 70771398
Respiratory distress 15.97 14.71 48 24223 54602 70849571
C-reactive protein increased 15.92 14.71 9 24262 110508 70793665
Nasal congestion 15.84 14.71 54 24217 65618 70838555
Hypokalaemic syndrome 15.82 14.71 4 24267 79 70904094
Overdose 15.75 14.71 21 24250 169724 70734449
Cardiac arrest 15.69 14.71 101 24170 159733 70744440
Paraesthesia 15.66 14.71 16 24255 145521 70758652
Epistaxis 15.57 14.71 73 24198 102554 70801619
Dyspnoea at rest 15.25 14.71 15 24256 6804 70897369
Pericarditis 15.21 14.71 5 24266 84700 70819473
Multiple organ dysfunction syndrome 14.89 14.71 75 24196 108440 70795733

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03BA08 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, EXCL. THIAZIDES
Sulfonamides, plain
ATC C03EA12 CARDIOVASCULAR SYSTEM
DIURETICS
DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION
Low-ceiling diuretics and potassium-sparing agents
FDA PE N0000175359 Increased Diuresis
FDA EPC N0000175420 Thiazide-like Diuretic
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004232 Diuretics
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D045283 Natriuretic Agents
MeSH PA D049993 Sodium Chloride Symporter Inhibitors
CHEBI has role CHEBI:35498 diuretics
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:50184 ion-transport inhibitor

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Renal Disease with Edema indication
Peripheral Edema due to Chronic Heart Failure indication
Pulmonary Edema due to Chronic Heart Failure indication
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hepatic encephalopathy contraindication 13920009 DOID:13413
Orthostatic hypotension contraindication 28651003
Hypokalemia contraindication 43339004
Pregnancy-induced hypertension contraindication 48194001
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hypercalcemia contraindication 66931009 DOID:12678
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Oliguria contraindication 83128009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Hypomagnesemia contraindication 190855004
Persistent vomiting contraindication 196746003
Acute pancreatitis contraindication 197456007 DOID:2913
Severe diarrhea contraindication 409587002
Azotemia contraindication 445009001




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.66 acidic
pKa2 1.3 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
Solute carrier family 12 member 3 Transporter INHIBITOR CHEMBL CHEMBL
Solute carrier family 12 member 1 Transporter Kd 8.45 WOMBAT-PK
Carbonic anhydrase 7 Enzyme Ki 8.68 CHEMBL

External reference:

IDSource
D00431 KEGG_DRUG
4018161 VANDF
C0025854 UMLSCUI
CHEBI:64354 CHEBI
CHEMBL878 ChEMBL_ID
DB00524 DRUGBANK_ID
D008788 MESH_DESCRIPTOR_UI
4170 PUBCHEM_CID
4838 IUPHAR_LIGAND_ID
2627 INN_ID
TZ7V40X7VX UNII
203794 RXNORM
1440 MMSL
47402 MMSL
5101 MMSL
d00299 MMSL
002310 NDDF
22198003 SNOMEDCT_US
387123003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-0055 TABLET 5 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-0055 TABLET 5 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5050 TABLET 2.50 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5050 TABLET 2.50 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5600 TABLET 10 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5600 TABLET 10 mg ORAL ANDA 23 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0378-6172 TABLET 2.50 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0378-6173 TABLET 5 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0378-6174 TABLET 10 mg ORAL ANDA 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2215 TABLET 2.50 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2215 TABLET 2.50 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2216 TABLET 5 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2216 TABLET 5 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2217 TABLET 10 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0527-2217 TABLET 10 mg ORAL NDA AUTHORIZED GENERIC 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6915 TABLET 5 mg ORAL NDA authorized generic 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6915 TABLET 5 mg ORAL NDA authorized generic 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6916 TABLET 2.50 mg ORAL NDA authorized generic 24 sections
metolazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6916 TABLET 2.50 mg ORAL NDA authorized generic 24 sections
METOLAZONE HUMAN PRESCRIPTION DRUG LABEL 1 0904-7138 TABLET 2.50 mg ORAL ANDA 22 sections
METOLAZONE HUMAN PRESCRIPTION DRUG LABEL 1 0904-7139 TABLET 5 mg ORAL ANDA 22 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 43353-890 TABLET 2.50 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 43353-931 TABLET 5 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 43353-999 TABLET 2.50 mg ORAL NDA AUTHORIZED GENERIC 24 sections
METOLAZONE Human Prescription Drug Label 1 46708-532 TABLET 2.50 mg ORAL ANDA 22 sections
METOLAZONE Human Prescription Drug Label 1 46708-533 TABLET 5 mg ORAL ANDA 22 sections
METOLAZONE Human Prescription Drug Label 1 46708-534 TABLET 10 mg ORAL ANDA 22 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 51079-023 TABLET 2.50 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 51079-024 TABLET 5 mg ORAL ANDA 24 sections
Metolazone HUMAN PRESCRIPTION DRUG LABEL 1 51407-431 TABLET 2.50 mg ORAL ANDA 12 sections