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	246.41	16.51	164	14584	50485	50539891
Cardiac failure congestive	236.43	16.51	196	14552	84186	50506190
Hypervolaemia	235.73	16.51	125	14623	25374	50565002
Pulmonary arterial hypertension	229.48	16.51	114	14634	20205	50570171
Right ventricular failure	170.10	16.51	86	14662	15807	50574569
Dyspnoea	139.57	16.51	411	14337	547197	50043179
Drug ineffective	119.97	16.51	45	14703	819288	49771088
Pulmonary hypertension	106.92	16.51	84	14664	33333	50557043
Acute kidney injury	98.76	16.51	210	14538	227848	50362528
Oedema	92.43	16.51	108	14640	70073	50520303
Oedema peripheral	92.15	16.51	165	14583	157796	50432580
Calcium deficiency	70.20	16.51	21	14727	929	50589447
Electrolyte imbalance	70.17	16.51	50	14698	17119	50573257
Death	62.22	16.51	222	14526	325157	50265219
Gastrointestinal haemorrhage	60.94	16.51	90	14658	73231	50517145
Acute respiratory failure	58.78	16.51	56	14692	28726	50561650
Dyspnoea exertional	57.90	16.51	73	14675	51160	50539216
Cardiac failure acute	55.87	16.51	33	14715	8217	50582159
Off label use	55.54	16.51	35	14713	474391	50115985
Renal failure	54.10	16.51	105	14643	106528	50483848
Hospitalisation	53.04	16.51	81	14667	67856	50522520
Hypoxia	51.76	16.51	69	14679	51054	50539322
Cardiac failure	50.22	16.51	84	14664	75956	50514420
Pulmonary oedema	49.47	16.51	66	14682	48872	50541504
Atrial fibrillation	48.96	16.51	98	14650	101647	50488729
Hypokalaemia	48.78	16.51	90	14658	87902	50502474
Chronic kidney disease	43.87	16.51	56	14692	39715	50550661
Hypotension	43.51	16.51	159	14589	235310	50355066
Torsade de pointes	42.76	16.51	32	14716	11803	50578573
Transfusion	42.46	16.51	33	14715	12872	50577504
Rheumatoid arthritis	41.79	16.51	5	14743	202545	50387831
Gout	41.41	16.51	31	14717	11439	50578937
Hyperkalaemia	41.34	16.51	60	14688	48029	50542347
Dermatitis exfoliative	41.33	16.51	23	14725	5119	50585257
BRASH syndrome	40.89	16.51	10	14738	203	50590173
Respiratory failure	39.36	16.51	84	14664	91097	50499279
Blood potassium decreased	39.14	16.51	51	14697	36894	50553482
Ascites	38.77	16.51	50	14698	35811	50554565
Cor pulmonale	38.49	16.51	16	14732	1871	50588505
Cholecystitis	38.27	16.51	32	14716	13839	50576537
Arthralgia	38.24	16.51	43	14705	438659	50151717
Urine chloride decreased	38.15	16.51	8	14740	78	50590298
Joint swelling	36.44	16.51	13	14735	245273	50345103
Metabolic alkalosis	35.85	16.51	17	14731	2714	50587662
Urine sodium decreased	33.16	16.51	8	14740	153	50590223
Alopecia	33.12	16.51	15	14733	245032	50345344
Contraindicated product administered	32.45	16.51	3	14745	148955	50441421
Rash	30.90	16.51	50	14698	437421	50152955
Chest pain	29.77	16.51	116	14632	176766	50413610
Therapeutic product effect decreased	28.95	16.51	3	14745	136047	50454329
Oxygen consumption increased	28.92	16.51	16	14732	3520	50586856
Cardiac arrest	28.29	16.51	70	14678	83581	50506795
Blood creatinine increased	28.19	16.51	66	14682	76094	50514282
Pain in jaw	27.44	16.51	44	14704	38384	50551992
Weight increased	27.42	16.51	124	14624	201767	50388609
Cardiorenal syndrome	26.96	16.51	9	14739	570	50589806
Respiratory disorder	26.92	16.51	39	14709	31148	50559228
Synovitis	25.67	16.51	3	14745	123862	50466514
Hyperthyroidism	25.44	16.51	24	14724	12151	50578225
Pericardial haemorrhage	25.22	16.51	11	14737	1447	50588929
Pericardial effusion	25.06	16.51	34	14714	25555	50564821
Drug intolerance	24.43	16.51	17	14731	219087	50371289
Renal impairment	24.20	16.51	62	14686	75599	50514777
Blood urea increased	24.11	16.51	32	14716	23553	50566823
Dehydration	24.05	16.51	98	14650	152351	50438025
Bone density decreased	23.46	16.51	22	14726	11053	50579323
Paracentesis	22.93	16.51	9	14739	907	50589469
Arthropathy	22.38	16.51	9	14739	157897	50432479
Toxic epidermal necrolysis	22.26	16.51	29	14719	20963	50569413
Localised oedema	21.80	16.51	15	14733	4852	50585524
Atrial flutter	21.69	16.51	19	14729	8744	50581632
Neutropenia	21.69	16.51	8	14740	147957	50442419
Pulmonary arterial pressure increased	21.65	16.51	13	14735	3335	50587041
Discomfort	21.55	16.51	3	14745	108377	50481999
Multiple organ dysfunction syndrome	21.27	16.51	46	14702	50291	50540085
Abdominal distension	20.54	16.51	57	14691	72846	50517530
Musculoskeletal stiffness	20.49	16.51	6	14742	128475	50461901
Vascular parkinsonism	20.24	16.51	5	14743	106	50590270
Oxygen therapy	19.94	16.51	10	14738	1802	50588574
Orthopnoea	19.70	16.51	15	14733	5674	50584702
Cellulitis	19.60	16.51	55	14693	70743	50519633
Pulmonary arterial wedge pressure increased	19.46	16.51	6	14742	294	50590082
Chronic obstructive pulmonary disease	19.43	16.51	46	14702	53389	50536987
Oxygen saturation decreased	19.40	16.51	56	14692	73192	50517184
Device leakage	19.27	16.51	15	14733	5863	50584513
Blood aldosterone abnormal	18.81	16.51	4	14744	42	50590334
Elephantiasis	18.13	16.51	3	14745	6	50590370
Brain natriuretic peptide increased	18.07	16.51	13	14735	4514	50585862
Blood potassium increased	17.93	16.51	23	14725	16375	50574001
Hepatic enzyme increased	17.64	16.51	9	14739	137371	50453005
Renal disorder	17.63	16.51	30	14718	27475	50562901
Condition aggravated	17.53	16.51	147	14601	296911	50293465
Asthenia	17.32	16.51	155	14593	318887	50271489
Epistaxis	17.03	16.51	49	14699	63905	50526471
Restlessness	16.85	16.51	28	14720	25145	50565231
Pleural effusion	16.71	16.51	57	14691	81397	50508979
Haemodialysis	16.55	16.51	16	14732	8346	50582030

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	231.51	18.01	209	11160	76372	29486786
Acute kidney injury	166.65	18.01	334	11035	264933	29298225
Hypokalaemia	111.76	18.01	116	11253	50087	29513071
Fluid retention	107.95	18.01	82	11287	23478	29539680
Hypervolaemia	84.65	18.01	63	11306	17482	29545676
Pulmonary hypertension	83.54	18.01	64	11305	18544	29544614
Hypotension	81.51	18.01	209	11160	194145	29369013
Cardiac failure	73.91	18.01	119	11250	79168	29483990
Pulmonary arterial hypertension	60.59	18.01	37	11332	7412	29555746
Dyspnoea	58.57	18.01	264	11105	326468	29236690
Oedema peripheral	57.01	18.01	124	11245	103433	29459725
Oedema	53.99	18.01	72	11297	40411	29522747
Blood creatinine increased	52.75	18.01	107	11262	84995	29478163
Right ventricular failure	48.84	18.01	33	11336	7857	29555301
Chronic kidney disease	44.37	18.01	62	11307	36354	29526804
Blood potassium increased	44.10	18.01	40	11329	14611	29548547
Venous pressure jugular increased	41.05	18.01	14	11355	715	29562443
Weight increased	37.89	18.01	88	11281	76579	29486579
Hypovolaemia	36.81	18.01	28	11341	8017	29555141
Drug ineffective	36.60	18.01	52	11317	363118	29200040
Polyuria	34.52	18.01	26	11343	7336	29555822
Glomerular filtration rate decreased	34.38	18.01	31	11338	11235	29551923
Necrotising oesophagitis	33.25	18.01	11	11358	511	29562647
Renal failure	32.66	18.01	110	11259	118489	29444669
Generalised oedema	32.65	18.01	30	11339	11135	29552023
Off label use	32.37	18.01	41	11328	300759	29262399
Hyponatraemia	31.63	18.01	76	11293	67557	29495601
Blood pressure systolic decreased	31.02	18.01	19	11350	3825	29559333
Transfusion	30.34	18.01	24	11345	7274	29555884
Dehydration	30.34	18.01	105	11264	114643	29448515
Blood urea increased	30.05	18.01	45	11324	28067	29535091
Gastrointestinal haemorrhage	29.59	18.01	82	11287	79451	29483707
Venous pressure jugular decreased	28.85	18.01	6	11363	41	29563117
Syncope	28.42	18.01	82	11287	81289	29481869
Orthopnoea	25.69	18.01	18	11351	4542	29558616
Cellulitis	24.15	18.01	54	11315	45786	29517372
Blood potassium decreased	24.12	18.01	30	11339	15704	29547454
Peripheral swelling	22.02	18.01	64	11305	63675	29499483
Febrile neutropenia	21.72	18.01	8	11361	112232	29450926
Asthenia	21.58	18.01	149	11220	215101	29348057
Azotaemia	21.15	18.01	16	11353	4541	29558617
Dizziness	20.62	18.01	134	11235	189550	29373608
Blood loss anaemia	20.23	18.01	19	11350	7247	29555911
Chronic obstructive pulmonary disease	20.19	18.01	47	11322	40908	29522250
Atrial fibrillation	19.99	18.01	87	11282	105559	29457599
Brain natriuretic peptide increased	19.96	18.01	15	11354	4215	29558943
Burkholderia test positive	19.78	18.01	9	11360	990	29562168
Neutropenia	18.69	18.01	14	11355	131697	29431461
Acute respiratory failure	18.50	18.01	35	11334	26367	29536791

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	403.26	15.02	354	23359	130226	64344793
Fluid retention	314.81	15.02	222	23491	59384	64415635
Hypervolaemia	283.21	15.02	176	23537	38109	64436910
Pulmonary arterial hypertension	254.36	15.02	142	23571	25225	64449794
Acute kidney injury	233.86	15.02	511	23202	448729	64026290
Right ventricular failure	195.86	15.02	113	23600	21358	64453661
Pulmonary hypertension	165.98	15.02	133	23580	43006	64432013
Dyspnoea	161.23	15.02	603	23110	718071	63756948
Oedema	133.96	15.02	167	23546	91768	64383251
Hypokalaemia	126.81	15.02	188	23525	121715	64353304
Drug ineffective	124.70	15.02	78	23635	840169	63634850
Oedema peripheral	123.69	15.02	252	23461	210065	64264954
Cardiac failure	111.10	15.02	185	23528	132188	64342831
Hypotension	104.24	15.02	342	23371	380632	64094387
Off label use	97.56	15.02	56	23657	632750	63842269
Gastrointestinal haemorrhage	75.85	15.02	157	23556	132155	64342864
Chronic kidney disease	74.55	15.02	99	23614	57820	64417199
Blood creatinine increased	73.06	15.02	157	23556	135625	64339394
Renal failure	72.61	15.02	187	23526	181501	64293518
Transfusion	68.15	15.02	55	23658	17939	64457080
Death	67.88	15.02	353	23360	482352	63992667
Acute respiratory failure	66.82	15.02	87	23626	49847	64425172
Calcium deficiency	66.28	15.02	20	23693	718	64474301
Cardiac failure acute	61.99	15.02	50	23663	16294	64458725
Atrial fibrillation	59.20	15.02	167	23546	170922	64304097
Dyspnoea exertional	59.07	15.02	101	23612	73629	64401390
Blood potassium increased	56.22	15.02	58	23655	25922	64449097
Weight increased	55.03	15.02	188	23525	213160	64261859
Hypoxia	53.33	15.02	107	23606	88042	64386977
Pulmonary oedema	53.08	15.02	100	23613	78574	64396445
Blood urea increased	53.05	15.02	73	23640	44080	64430939
Blood potassium decreased	50.36	15.02	68	23645	40331	64434688
Dehydration	49.89	15.02	184	23529	216579	64258440
Neutropenia	48.46	15.02	14	23699	239610	64235409
Hospitalisation	47.55	15.02	93	23620	75114	64399905
Glomerular filtration rate decreased	46.57	15.02	46	23667	19526	64455493
Orthopnoea	45.79	15.02	33	23680	9101	64465918
Infusion related reaction	45.67	15.02	4	23709	164463	64310556
Rheumatoid arthritis	45.61	15.02	4	23709	164290	64310729
Generalised oedema	44.12	15.02	46	23667	20807	64454212
Hyperkalaemia	43.39	15.02	107	23606	101022	64373997
Polyuria	42.36	15.02	36	23677	12607	64462412
Metabolic alkalosis	42.12	15.02	23	23690	3905	64471114
Electrolyte imbalance	41.85	15.02	49	23664	25194	64449825
Hypovolaemia	39.85	15.02	38	23675	15448	64459571
Syncope	39.82	15.02	138	23575	157497	64317522
Pain in jaw	38.27	15.02	60	23653	40695	64434324
Cardiorenal syndrome	37.75	15.02	15	23698	1235	64473784
Arthralgia	37.29	15.02	66	23647	442194	64032825
Gout	36.22	15.02	42	23671	21371	64453648
Urine sodium decreased	36.01	15.02	10	23703	266	64474753
Urine chloride decreased	35.18	15.02	8	23705	91	64474928
Brain natriuretic peptide increased	34.70	15.02	26	23687	7607	64467412
Febrile neutropenia	34.36	15.02	13	23700	187644	64287375
Venous pressure jugular increased	34.16	15.02	14	23699	1249	64473770
Cor pulmonale	33.83	15.02	16	23697	2009	64473010
Hyponatraemia	33.32	15.02	125	23588	148214	64326805
Joint swelling	33.14	15.02	19	23694	215363	64259656
BRASH syndrome	32.93	15.02	10	23703	367	64474652
Cellulitis	32.92	15.02	92	23621	93565	64381454
Azotaemia	32.88	15.02	25	23688	7477	64467542
Treatment failure	32.00	15.02	3	23710	116813	64358206
Oxygen therapy	31.94	15.02	16	23697	2277	64472742
Respiratory failure	31.50	15.02	130	23583	161053	64313966
Necrotising oesophagitis	30.72	15.02	11	23702	679	64474340
Ascites	30.26	15.02	69	23644	61932	64413087
Asthenia	30.19	15.02	264	23449	427780	64047239
Chronic left ventricular failure	29.91	15.02	11	23702	733	64474286
Product use in unapproved indication	29.51	15.02	14	23699	176604	64298415
Torsade de pointes	29.27	15.02	34	23679	17329	64457690
Chronic obstructive pulmonary disease	29.23	15.02	74	23639	70974	64404045
Alopecia	27.89	15.02	13	23700	165677	64309342
Paracentesis	27.53	15.02	12	23701	1247	64473772
International normalised ratio increased	27.07	15.02	77	23636	79090	64395929
Oxygen consumption increased	26.33	15.02	18	23695	4563	64470456
Atrial flutter	26.27	15.02	34	23679	19346	64455673
Condition aggravated	25.88	15.02	229	23484	372197	64102822
Dermatitis exfoliative	25.87	15.02	25	23688	10327	64464692
Rash	25.53	15.02	85	23628	458464	64016555
Venous pressure jugular decreased	25.17	15.02	6	23707	85	64474934
Arthropathy	24.56	15.02	7	23706	120960	64354059
Blood sodium decreased	24.41	15.02	41	23672	29441	64445578
Cholecystitis	24.39	15.02	33	23680	19603	64455416
Pericardial effusion	24.14	15.02	48	23665	39206	64435813
Peripheral swelling	23.97	15.02	145	23568	209008	64266011
Chest pain	23.58	15.02	158	23555	235822	64239197
Pulmonary arterial pressure increased	23.25	15.02	16	23697	4100	64470919
White blood cell count decreased	22.78	15.02	15	23698	157822	64317197
Contraindicated product administered	22.34	15.02	6	23707	107823	64367196
Left ventricular failure	22.31	15.02	21	23692	8396	64466623
Musculoskeletal stiffness	21.78	15.02	9	23704	123197	64351822
Hypertension	21.53	15.02	39	23674	259222	64215797
Blood loss anaemia	21.43	15.02	26	23687	13866	64461153
Renal impairment	21.16	15.02	102	23611	134915	64340104
Pericardial haemorrhage	20.86	15.02	15	23698	4121	64470898
Respiratory disorder	20.83	15.02	43	23670	36068	64438951
Malignant neoplasm progression	20.35	15.02	8	23705	112863	64362156
Renal disorder	20.27	15.02	42	23671	35323	64439696
Completed suicide	20.25	15.02	32	23681	224382	64250637
Discomfort	19.87	15.02	3	23710	80875	64394144
Blood pressure systolic decreased	19.64	15.02	20	23693	8800	64466219
Bone density decreased	19.36	15.02	21	23692	9931	64465088
Vascular parkinsonism	19.22	15.02	5	23708	103	64474916
Localised oedema	19.18	15.02	18	23695	7173	64467846
Pulmonary arterial wedge pressure increased	19.17	15.02	7	23706	457	64474562
Oxygen saturation decreased	19.03	15.02	84	23629	107092	64367927
Systemic lupus erythematosus	18.79	15.02	3	23710	77609	64397410
Drug hypersensitivity	18.67	15.02	37	23676	237778	64237241
Abdominal distension	18.40	15.02	77	23636	95917	64379102
Blood pressure increased	18.18	15.02	22	23691	172530	64302489
Dizziness	17.98	15.02	239	23474	429924	64045095
Blood aldosterone abnormal	17.88	15.02	4	23709	42	64474977
Stomatitis	17.83	15.02	9	23704	109596	64365423
Gastrointestinal arteriovenous malformation	17.66	15.02	8	23705	911	64474108
Device leakage	17.06	15.02	18	23695	8248	64466771
Nasal congestion	16.61	15.02	54	23659	59604	64415415
Lower respiratory tract infection	16.58	15.02	7	23706	94607	64380412
Elephantiasis	16.57	15.02	3	23710	9	64475010
Catheter management	16.54	15.02	12	23701	3343	64471676
Urine output decreased	16.49	15.02	25	23688	16467	64458552
Overdose	16.12	15.02	21	23692	159545	64315474
Interstitial lung disease	15.93	15.02	8	23705	97724	64377295
Haemodialysis	15.83	15.02	25	23688	17052	64457967
Hypokalaemic syndrome	15.68	15.02	4	23709	76	64474943
Injection site pain	15.52	15.02	11	23702	111397	64363622
Paraesthesia	15.42	15.02	16	23697	134506	64340513
Pleural effusion	15.29	15.02	89	23624	126470	64348549
Dyspnoea at rest	15.28	15.02	15	23698	6314	64468705

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	0527-2216	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	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	0904-7138	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
Metolazone	HUMAN PRESCRIPTION DRUG LABEL	1	51407-432	TABLET	5 mg	ORAL	ANDA	12 sections
Metolazone	HUMAN PRESCRIPTION DRUG LABEL	1	51407-433	TABLET	10 mg	ORAL	ANDA	12 sections
Metolazone	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5056	TABLET	5 mg	ORAL	ANDA	23 sections
Metolazone	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5104	TABLET	2.50 mg	ORAL	ANDA	23 sections
Metolazone	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5119	TABLET	10 mg	ORAL	ANDA	23 sections