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

Stem definition	Drug id	CAS RN
	1783	17560-51-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
5	mg	O

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.78 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Bocci G, Oprea TI, 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
S (Water solubility)	0.02 mg/mL	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Nov. 27, 1973	FDA	UCB INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	263.90	16.01	201	15149	92232	63381440
Fluid retention	259.58	16.01	168	15182	59518	63414154
Hypervolaemia	244.98	16.01	125	15225	28288	63445384
Pulmonary arterial hypertension	244.40	16.01	116	15234	22461	63451211
Right ventricular failure	191.18	16.01	90	15260	17098	63456574
Dyspnoea	145.79	16.01	418	14932	660895	62812777
Pulmonary hypertension	124.36	16.01	89	15261	37034	63436638
Drug ineffective	122.96	16.01	50	15300	1044715	62428957
Acute kidney injury	120.98	16.01	223	15127	263192	63210480
Oedema peripheral	95.28	16.01	167	15183	189344	63284328
Oedema	86.26	16.01	112	15238	97510	63376162
Death	83.32	16.01	238	15112	374143	63099529
Acute respiratory failure	76.93	16.01	65	15285	34420	63439252
Electrolyte imbalance	73.88	16.01	51	15299	20025	63453647
Calcium deficiency	70.77	16.01	21	15329	1093	63472579
Gastrointestinal haemorrhage	68.39	16.01	91	15259	81085	63392587
Off label use	65.95	16.01	41	15309	674421	62799251
Renal failure	64.74	16.01	108	15242	117544	63356128
Cardiac failure acute	62.59	16.01	35	15315	9488	63464184
Cardiac failure	61.78	16.01	91	15259	89051	63384621
Dyspnoea exertional	60.90	16.01	74	15276	60228	63413444
Hypokalaemia	60.77	16.01	98	15252	103706	63369966
Atrial fibrillation	57.52	16.01	102	15248	116534	63357138
Hypoxia	56.56	16.01	71	15279	59721	63413951
Hypotension	56.39	16.01	169	15181	272435	63201237
Hospitalisation	54.89	16.01	84	15266	84997	63388675
Pulmonary oedema	54.86	16.01	67	15283	54806	63418866
Torsade de pointes	54.08	16.01	36	15314	13315	63460357
Chronic kidney disease	52.97	16.01	60	15290	45338	63428334
Gout	51.88	16.01	35	15315	13236	63460436
Respiratory failure	45.05	16.01	85	15265	101773	63371899
Hyperkalaemia	44.46	16.01	60	15290	54143	63419529
Dermatitis exfoliative	44.07	16.01	23	15327	5436	63468236
Rheumatoid arthritis	43.93	16.01	5	15345	253814	63219858
Blood potassium decreased	43.12	16.01	52	15298	41974	63431698
Transfusion	43.10	16.01	33	15317	15184	63458488
Ascites	41.14	16.01	50	15300	40678	63432994
Contraindicated product administered	41.11	16.01	3	15347	217645	63256027
Joint swelling	41.10	16.01	14	15336	327652	63146020
Cholecystitis	40.63	16.01	32	15318	15345	63458327
Cor pulmonale	40.07	16.01	16	15334	2038	63471634
Alopecia	39.68	16.01	16	15334	337520	63136152
BRASH syndrome	39.44	16.01	11	15339	458	63473214
Arthralgia	39.41	16.01	48	15302	569662	62904010
Urine chloride decreased	38.85	16.01	8	15342	87	63473585
Metabolic alkalosis	37.03	16.01	17	15333	3044	63470628
Systemic lupus erythematosus	36.44	16.01	4	15346	208914	63264758
Therapeutic product effect decreased	35.53	16.01	3	15347	193184	63280488
Urine sodium decreased	34.17	16.01	8	15342	163	63473509
Synovitis	34.11	16.01	3	15347	186915	63286757
Rash	33.99	16.01	52	15298	560819	62912853
Drug intolerance	32.59	16.01	17	15333	308644	63165028
Cardiac arrest	32.29	16.01	70	15280	92475	63381197
Chest pain	31.39	16.01	119	15231	215840	63257832
Blood creatinine increased	31.28	16.01	67	15283	87777	63385895
Arthropathy	31.27	16.01	9	15341	234783	63238889
Chronic left ventricular failure	30.41	16.01	9	15341	464	63473208
Oxygen consumption increased	30.31	16.01	16	15334	3868	63469804
Dehydration	29.86	16.01	101	15249	173253	63300419
Discomfort	29.71	16.01	3	15347	167371	63306301
Pain in jaw	29.53	16.01	44	15306	43452	63430220
Renal impairment	28.76	16.01	65	15285	88290	63385382
Blood urea increased	27.64	16.01	33	15317	26346	63447326
Pericardial effusion	27.31	16.01	35	15315	30023	63443649
Atrial flutter	27.25	16.01	21	15329	9751	63463921
Musculoskeletal stiffness	26.64	16.01	6	15344	184612	63289060
Pericardial haemorrhage	26.09	16.01	11	15339	1608	63472064
Respiratory disorder	25.77	16.01	39	15311	39043	63434629
Hyperthyroidism	25.44	16.01	24	15326	14649	63459023
Cellulitis	25.24	16.01	59	15291	81899	63391773
Weight increased	25.11	16.01	127	15223	260665	63213007
Cardiorenal syndrome	24.97	16.01	9	15341	866	63472806
Hepatic enzyme increased	24.73	16.01	9	15341	202319	63271353
Multiple organ dysfunction syndrome	24.62	16.01	47	15303	56705	63416967
Paracentesis	24.06	16.01	9	15341	961	63472711
Abdominal distension	23.10	16.01	59	15291	86556	63387116
Pulmonary arterial pressure increased	23.04	16.01	13	15337	3582	63470090
Localised oedema	22.99	16.01	15	15335	5363	63468309
Toxic epidermal necrolysis	22.23	16.01	29	15321	25305	63448367
Bone density decreased	21.78	16.01	22	15328	14590	63459082
Chronic obstructive pulmonary disease	21.38	16.01	47	15303	62639	63411033
Neutropenia	21.03	16.01	8	15342	174997	63298675
Epistaxis	20.93	16.01	51	15299	72674	63400998
Orthopnoea	20.92	16.01	15	15335	6246	63467426
Vascular parkinsonism	20.30	16.01	5	15345	127	63473545
Haemodialysis	20.22	16.01	17	15333	8930	63464742
Oxygen therapy	19.97	16.01	10	15340	2168	63471504
Pulmonary arterial wedge pressure increased	19.95	16.01	6	15344	327	63473345
Asthenia	19.60	16.01	159	15191	383445	63090227
Pleural effusion	19.41	16.01	58	15292	93152	63380520
Haemoglobin decreased	19.35	16.01	78	15272	145407	63328265
Blood potassium increased	19.34	16.01	23	15327	18286	63455386
Oxygen saturation decreased	19.28	16.01	56	15294	88529	63385143
Device leakage	19.25	16.01	15	15335	7081	63466591
Blood aldosterone abnormal	19.22	16.01	4	15346	46	63473626
Renal disorder	19.09	16.01	31	15319	32943	63440729
Wound	18.74	16.01	8	15342	163255	63310417
Elephantiasis	18.69	16.01	3	15347	6	63473666
Brain natriuretic peptide increased	18.60	16.01	13	15337	5200	63468472
International normalised ratio increased	18.38	16.01	37	15313	46388	63427284
Syncope	18.13	16.01	66	15284	117319	63356353
Product use issue	18.10	16.01	16	15334	220504	63253168
Lower respiratory tract infection	17.73	16.01	5	15345	132302	63341370
Left ventricular failure	17.58	16.01	13	15337	5674	63467998
Restlessness	17.47	16.01	28	15322	29425	63444247
Respiratory distress	17.11	16.01	30	15320	33921	63439751
Generalised oedema	16.92	16.01	20	15330	15798	63457874
Delusion of replacement	16.61	16.01	3	15347	15	63473657
Dialysis	16.09	16.01	16	15334	10411	63463261

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	245.48	16.94	214	11873	83056	34861788
Acute kidney injury	166.98	16.94	341	11746	304647	34640197
Hypokalaemia	116.58	16.94	121	11966	58093	34886751
Fluid retention	112.64	16.94	85	12002	26802	34918042
Hypervolaemia	90.82	16.94	66	12021	19643	34925201
Pulmonary hypertension	89.51	16.94	67	12020	20857	34923987
Hypotension	87.37	16.94	218	11869	221431	34723413
Cardiac failure	80.39	16.94	126	11961	91122	34853722
Dyspnoea	61.61	16.94	275	11812	376507	34568337
Oedema peripheral	61.58	16.94	131	11956	119681	34825163
Pulmonary arterial hypertension	61.28	16.94	38	12049	8701	34936143
Oedema	56.14	16.94	74	12013	45667	34899177
Right ventricular failure	56.10	16.94	36	12051	8748	34936096
Blood creatinine increased	56.06	16.94	110	11977	94866	34849978
Blood potassium increased	45.63	16.94	41	12046	16454	34928390
Venous pressure jugular increased	45.17	16.94	15	12072	786	34944058
Chronic kidney disease	43.51	16.94	62	12025	41148	34903696
Drug ineffective	40.26	16.94	60	12027	456691	34488153
Renal failure	39.78	16.94	117	11970	130440	34814404
Gastrointestinal haemorrhage	38.94	16.94	91	11996	88386	34856458
Generalised oedema	38.65	16.94	33	12054	12375	34932469
Glomerular filtration rate decreased	37.40	16.94	33	12054	12928	34931916
Weight increased	36.99	16.94	92	11995	92941	34851903
Hypovolaemia	36.02	16.94	28	12059	9206	34935638
Polyuria	35.63	16.94	27	12060	8547	34936297
Dehydration	33.58	16.94	110	11977	129859	34814985
Necrotising oesophagitis	33.52	16.94	11	12076	555	34944289
Off label use	33.29	16.94	59	12028	419465	34525379
Blood pressure systolic decreased	32.63	16.94	20	12067	4483	34940361
Blood urea increased	31.04	16.94	45	12042	30319	34914525
Syncope	29.80	16.94	84	12003	91367	34853477
Venous pressure jugular decreased	29.49	16.94	6	12081	41	34944803
Transfusion	29.15	16.94	24	12063	8561	34936283
Hyponatraemia	28.97	16.94	78	12009	82613	34862231
Azotaemia	26.02	16.94	18	12069	4949	34939895
Orthopnoea	25.58	16.94	18	12069	5085	34939759
Cellulitis	23.86	16.94	55	12032	52896	34891948
Blood potassium decreased	23.54	16.94	30	12057	17885	34926959
Death	23.54	16.94	225	11862	397824	34547020
Asthenia	22.29	16.94	153	11934	245098	34699746
Atrial fibrillation	21.86	16.94	92	11995	122301	34822543
Cardiac failure acute	21.16	16.94	22	12065	10548	34934296
Blood sodium decreased	21.02	16.94	27	12060	16224	34928620
Peripheral swelling	20.84	16.94	66	12021	76475	34868369
Burkholderia test positive	20.49	16.94	9	12078	1014	34943830
Febrile neutropenia	20.32	16.94	11	12076	136838	34808006
Dizziness	20.24	16.94	137	11950	218384	34726460
Chronic obstructive pulmonary disease	20.08	16.94	49	12038	48869	34895975
Blood loss anaemia	20.00	16.94	19	12068	8175	34936669
Ventricular tachycardia	19.70	16.94	34	12053	26545	34918299
Acute respiratory failure	19.65	16.94	37	12050	30891	34913953
Brain natriuretic peptide increased	19.59	16.94	16	12071	5643	34939201
Urine output decreased	18.49	16.94	20	12067	10029	34934815
Product use in unapproved indication	18.10	16.94	9	12078	117490	34827354
Neutropenia	17.55	16.94	17	12070	156761	34788083
Sinus bradycardia	17.50	16.94	22	12065	12941	34931903
Pain in jaw	17.39	16.94	22	12065	13018	34931826

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	445.62	15.62	363	24544	142039	79577442
Fluid retention	332.19	15.62	229	24678	69580	79649901
Hypervolaemia	299.77	15.62	179	24728	42511	79676970
Pulmonary arterial hypertension	266.74	15.62	144	24763	28222	79691259
Acute kidney injury	262.43	15.62	530	24377	518874	79200607
Right ventricular failure	220.12	15.62	119	24788	23378	79696103
Pulmonary hypertension	190.12	15.62	141	24766	47939	79671542
Dyspnoea	170.97	15.62	620	24287	856405	78863076
Hypokalaemia	146.86	15.62	202	24705	143838	79575643
Oedema peripheral	131.05	15.62	261	24646	252027	79467454
Oedema	128.39	15.62	172	24735	119408	79600073
Cardiac failure	127.08	15.62	196	24711	154646	79564835
Drug ineffective	119.55	15.62	98	24809	1080815	78638666
Hypotension	119.18	15.62	354	24553	439963	79279518
Off label use	108.21	15.62	76	24831	907139	78812342
Death	94.50	15.62	388	24519	566126	79153355
Gastrointestinal haemorrhage	94.25	15.62	167	24740	147552	79571929
Renal failure	90.30	15.62	196	24711	200772	79518709
Acute respiratory failure	85.27	15.62	99	24808	59442	79660039
Chronic kidney disease	83.26	15.62	103	24804	66051	79653430
Blood creatinine increased	81.09	15.62	161	24746	154896	79564585
Cardiac failure acute	78.13	15.62	57	24850	18872	79700609
Atrial fibrillation	69.20	15.62	175	24732	197711	79521770
Transfusion	67.81	15.62	55	24852	21275	79698206
Calcium deficiency	65.61	15.62	20	24887	879	79718602
Dyspnoea exertional	64.16	15.62	105	24802	86968	79632513
Blood potassium increased	60.20	15.62	59	24848	29216	79690265
Blood urea increased	59.83	15.62	75	24832	48715	79670766
Dehydration	58.11	15.62	190	24717	247997	79471484
Pulmonary oedema	56.53	15.62	100	24807	88154	79631327
Infusion related reaction	56.45	15.62	4	24903	230233	79489248
Hypoxia	56.12	15.62	109	24798	103134	79616347
Blood potassium decreased	53.09	15.62	69	24838	46443	79673038
Generalised oedema	51.03	15.62	49	24858	23660	79695821
Glomerular filtration rate decreased	50.92	15.62	48	24859	22654	79696827
Rheumatoid arthritis	50.03	15.62	4	24903	208466	79511015
Weight increased	49.26	15.62	194	24713	277192	79442289
Hospitalisation	48.21	15.62	97	24810	94139	79625342
Orthopnoea	47.73	15.62	33	24874	10040	79709441
Hyperkalaemia	46.19	15.62	107	24800	114291	79605190
Metabolic alkalosis	45.58	15.62	24	24883	4465	79715016
Neutropenia	44.66	15.62	17	24890	287693	79431788
Syncope	44.35	15.62	140	24767	179309	79540172
Polyuria	44.14	15.62	37	24870	14977	79704504
Gout	43.80	15.62	46	24861	24703	79694778
Electrolyte imbalance	43.61	15.62	51	24856	30830	79688651
Chronic left ventricular failure	43.02	15.62	15	24892	1011	79718470
Arthralgia	42.34	15.62	71	24836	571732	79147749
Necrotising oesophagitis	41.82	15.62	15	24892	1098	79718383
Hypovolaemia	40.82	15.62	38	24869	17653	79701828
Pain in jaw	40.02	15.62	60	24847	46091	79673390
Venous pressure jugular increased	39.11	15.62	15	24892	1325	79718156
Treatment failure	38.94	15.62	4	24903	170482	79548999
Azotaemia	38.94	15.62	27	24880	8249	79711232
Joint swelling	38.65	15.62	21	24886	288625	79430856
Cellulitis	38.65	15.62	97	24810	108963	79610518
Respiratory failure	38.34	15.62	134	24773	180777	79538704
Torsade de pointes	37.99	15.62	38	24869	19274	79700207
Urine sodium decreased	37.20	15.62	10	24897	278	79719203
Brain natriuretic peptide increased	37.18	15.62	27	24880	8873	79710608
Hyponatraemia	37.05	15.62	131	24776	177717	79541764
Cardiorenal syndrome	36.63	15.62	15	24892	1574	79717907
Urine chloride decreased	35.71	15.62	8	24899	101	79719380
Alopecia	35.35	15.62	14	24893	231341	79488140
Cor pulmonale	34.59	15.62	16	24891	2252	79717229
Drug abuse	34.26	15.62	5	24902	162686	79556795
International normalised ratio increased	33.92	15.62	79	24828	84642	79634839
Arthropathy	33.90	15.62	7	24900	177104	79542377
Asthenia	32.71	15.62	272	24635	511417	79208064
Product use in unapproved indication	32.39	15.62	19	24888	250340	79469141
Oxygen therapy	31.44	15.62	16	24891	2774	79716707
Ascites	30.85	15.62	71	24836	75491	79643990
Febrile neutropenia	30.64	15.62	17	24890	230982	79488499
Contraindicated product administered	30.62	15.62	6	24901	157532	79561949
Chronic obstructive pulmonary disease	30.29	15.62	76	24831	85343	79634138
Rash	29.53	15.62	88	24819	578270	79141211
Musculoskeletal stiffness	29.47	15.62	9	24898	174999	79544482
Atrial flutter	29.35	15.62	35	24872	21590	79697891
Paracentesis	28.65	15.62	12	24895	1333	79718148
Discomfort	28.55	15.62	3	24904	125614	79593867
Dermatitis exfoliative	28.40	15.62	25	24882	10804	79708677
BRASH syndrome	28.31	15.62	11	24896	1006	79718475
Pericardial effusion	27.82	15.62	51	24856	46186	79673295
Oxygen consumption increased	27.64	15.62	18	24889	4961	79714520
Venous pressure jugular decreased	26.14	15.62	6	24901	85	79719396
Blood sodium decreased	25.70	15.62	41	24866	33214	79686267
Cholecystitis	25.42	15.62	33	24874	22179	79697302
Renal impairment	25.30	15.62	107	24800	157676	79561805
Left ventricular failure	24.89	15.62	22	24885	9559	79709922
Systemic lupus erythematosus	24.87	15.62	4	24903	121145	79598336
Chest pain	24.83	15.62	162	24745	282142	79437339
Blood loss anaemia	24.26	15.62	27	24880	15471	79704010
Pulmonary arterial pressure increased	24.15	15.62	16	24891	4539	79714942
Stomatitis	22.21	15.62	9	24898	146748	79572733
Glossodynia	22.17	15.62	3	24904	103334	79616147
Pericardial haemorrhage	21.94	15.62	15	24892	4480	79715001
Hypertension	21.87	15.62	44	24863	330948	79388533
Drug hypersensitivity	21.27	15.62	38	24869	298878	79420603
Renal disorder	21.11	15.62	43	24864	42062	79677419
Urine output decreased	20.97	15.62	27	24880	17995	79701486
Peripheral swelling	20.90	15.62	150	24757	269467	79450014
Haemodialysis	20.80	15.62	27	24880	18141	79701340
Blood pressure systolic decreased	20.34	15.62	21	24886	11055	79708426
Localised oedema	20.14	15.62	18	24889	7934	79711547
Haemoglobin decreased	19.84	15.62	128	24779	221991	79497490
White blood cell count decreased	19.53	15.62	18	24889	188270	79531211
Pulmonary arterial wedge pressure increased	19.44	15.62	7	24900	518	79718963
Lower respiratory tract infection	19.43	15.62	8	24899	129212	79590269
Respiratory disorder	19.25	15.62	43	24864	44813	79674668
Vascular parkinsonism	19.15	15.62	5	24902	124	79719357
Abdominal distension	19.07	15.62	81	24826	119569	79599912
Intentional product use issue	19.02	15.62	12	24895	152100	79567381
Epistaxis	18.95	15.62	77	24830	111438	79608043
Blood pressure increased	18.80	15.62	23	24884	211337	79508144
Oxygen saturation decreased	18.77	15.62	85	24822	128962	79590519
Respiratory distress	18.71	15.62	50	24857	58289	79661192
Myoclonus	18.55	15.62	32	24875	27628	79691853
Gastrointestinal arteriovenous malformation	18.51	15.62	8	24899	960	79718521
Pericarditis	18.20	15.62	5	24902	104231	79615250
Blood aldosterone abnormal	18.20	15.62	4	24903	46	79719435
Paraesthesia	18.12	15.62	17	24890	176306	79543175
Malignant neoplasm progression	18.03	15.62	10	24897	135980	79583501
Condition aggravated	17.98	15.62	237	24670	500887	79218594
C-reactive protein increased	17.83	15.62	9	24898	129018	79590463
Pleural effusion	17.75	15.62	91	24816	145171	79574310
Dizziness	17.67	15.62	246	24661	526195	79193286
Catheter management	17.35	15.62	12	24895	3651	79715830
Cardiac arrest	17.14	15.62	102	24805	171994	79547487
Bone density decreased	17.13	15.62	21	24886	13326	79706155
Elephantiasis	17.06	15.62	3	24904	9	79719472
Cardiomegaly	17.04	15.62	30	24877	26322	79693159
Shock	16.76	15.62	40	24867	43508	79675973

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.66	acidic
pKa2	1.3	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Solute carrier family 12 member 3	Transporter	P55017	S12A3_HUMAN	INHIBITOR			CHEMBL	CHEMBL
Solute carrier family 12 member 1	Transporter	Q13621	S12A1_HUMAN		Kd	8.45	WOMBAT-PK
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	8.68	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	10135-765	TABLET	2.50 mg	ORAL	ANDA	21 sections
METOLAZONE	HUMAN PRESCRIPTION DRUG LABEL	1	10135-766	TABLET	5 mg	ORAL	ANDA	21 sections
METOLAZONE	HUMAN PRESCRIPTION DRUG LABEL	1	10135-767	TABLET	10 mg	ORAL	ANDA	21 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	46708-532	TABLET	2.50 mg	ORAL	ANDA	22 sections
METOLAZONE	Human Prescription Drug Label	1	46708-533	TABLET	5 mg	ORAL	ANDA	22 sections