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)	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:

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
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 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	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 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	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:

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	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