Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
diuretics, chlorothiazide derivatives	305	73-48-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bendroflumethiazide bendrofluazide benzhydroflumethiazide benzidroflumetiazide benzydroflumethiazide benzylhydroflumethiazide benzylrodiuran	A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810) Molecular weight: 421.41 Formula: C15H14F3N3O4S2 CLOGP: 1.73 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 118.36 ALOGS: -3.29 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

bendroflumethiazide
bendrofluazide
benzhydroflumethiazide
benzidroflumetiazide
benzydroflumethiazide
benzylhydroflumethiazide
benzylrodiuran

A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)

Molecular weight: 421.41
Formula: C15H14F3N3O4S2
CLOGP: 1.73
LIPINSKI: 0
HAC: 7
HDO: 3
TPSA: 118.36
ALOGS: -3.29
ROTB: 4

Status: OFM

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

Drug dosage:

Dose	Unit	Route
2.50	mg	O
2.50	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.11 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	21 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.79 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	2.035		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	70.146		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	1.259	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	2.133	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	6.210	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	12.450	%	High	1
herg	hERG pIC50	4.300	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	1.858	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	6.592	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	4.930	%	High	1
kinase-safety-class	ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPKAPK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK	23
kinase-selectivity-class	AXL,GRK2,MAP2K6,PDK1,PDK4	5
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	6.383		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	17.298		High	1
mppb	Mouse plasma protein binding (% unbound)	4.470		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	10.593		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	1
pppb	Pig plasma protein binding (% unbound)	10.870	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	11.967	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	54.540	%	High	1
rppb	Rat plasma protein binding (% unbound)	6.040	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	105.196	uM	High	1

Approvals:

Date	Agency	Company	Orphan
Dec. 7, 1959	FDA

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
Cardiospasm	314.90	28.06	80	15179	3366	90609822
Palmoplantar keratoderma	313.51	28.06	80	15179	3427	90609761
Lip swelling	309.22	28.06	144	15115	38466	90574722
Tension headache	303.97	28.06	92	15167	7417	90605771
Pruritus genital	297.37	28.06	81	15178	4477	90608711
Sleep terror	294.36	28.06	80	15179	4384	90608804
Atrial tachycardia	279.88	28.06	82	15177	5908	90607280
Carotid artery occlusion	266.59	28.06	80	15179	6262	90606926
Immunisation	240.31	28.06	59	15200	2154	90611034
Anosmia	231.97	28.06	80	15179	9768	90603420
Hyponatraemia	228.25	28.06	185	15074	133353	90479835
Hallucination	213.82	28.06	135	15124	65824	90547364
Facial pain	212.80	28.06	81	15178	13101	90600087
Subarachnoid haemorrhage	205.42	28.06	86	15173	17818	90595370
Intentional product misuse	198.77	28.06	145	15114	89459	90523729
Pain of skin	197.18	28.06	81	15178	16001	90597187
Blindness	184.87	28.06	90	15169	26478	90586710
Diplopia	184.12	28.06	92	15167	28622	90584566
Vasculitis	179.62	28.06	84	15175	22609	90590579
Drug ineffective	175.77	28.06	16	15243	1384282	89228906
Ventricular tachycardia	172.81	28.06	84	15175	24624	90588564
Amyloid arthropathy	168.36	28.06	42	15217	1638	90611550
Pulmonary pain	166.31	28.06	53	15206	5061	90608127
Eye pruritus	165.73	28.06	86	15173	28941	90584247
Muscle twitching	162.44	28.06	80	15179	24122	90589066
Angioedema	152.99	28.06	109	15150	64767	90548421
Palpitations	141.68	28.06	143	15116	136585	90476603
Tinnitus	134.09	28.06	86	15173	43016	90570172
Transient ischaemic attack	129.02	28.06	84	15175	43092	90570096
Disturbance in attention	127.11	28.06	86	15173	47023	90566165
Cognitive disorder	111.81	28.06	93	15166	69314	90543874
Amnesia	106.03	28.06	110	15149	108395	90504793
Rash papular	98.40	28.06	54	15205	20301	90592887
Visual impairment	88.16	28.06	110	15149	132255	90480933
Disturbance in social behaviour	83.25	28.06	30	15229	4158	90609030
Hyperhidrosis	80.91	28.06	107	15152	136198	90476990
Myocardial infarction	80.24	28.06	94	15165	105878	90507310
Dry skin	80.16	28.06	86	15173	87987	90525201
Drug abuse	77.76	28.06	82	15177	82265	90530923
Tachycardia	76.02	28.06	112	15147	157561	90455627
Blood glucose increased	71.29	28.06	84	15175	95162	90518026
Malaise	67.36	28.06	234	15025	585752	90027436
Paranoia	67.27	28.06	36	15223	12872	90600316
Mouth swelling	64.25	28.06	27	15232	5635	90607553
Dehydration	58.70	28.06	112	15147	194335	90418853
Weight increased	58.05	28.06	3	15256	417924	90195264
Infusion related reaction	57.86	28.06	3	15256	416777	90196411
Feeling abnormal	57.63	28.06	102	15157	167133	90446055
Nasopharyngitis	56.30	28.06	3	15256	407101	90206087
Lethargy	56.29	28.06	61	15198	63078	90550110
Heart rate increased	55.55	28.06	81	15178	112821	90500367
Acute kidney injury	54.60	28.06	147	15112	320240	90292948
Vomiting	48.77	28.06	261	14998	788032	89825156
Swelling	45.27	28.06	8	15251	419050	90194138
Agitation	45.01	28.06	56	15203	67042	90546146
Muscular weakness	44.82	28.06	104	15155	206562	90406626
Abnormal behaviour	44.26	28.06	34	15225	22594	90590594
Hepatic enzyme increased	43.35	28.06	5	15254	360731	90252457
Superinfection	42.69	28.06	17	15242	3095	90610093
Ejection fraction decreased	41.87	28.06	35	15224	26218	90586970
Disorientation	41.75	28.06	44	15215	44070	90569118
Sinusitis	40.62	28.06	5	15254	343083	90270105
Nail dystrophy	40.14	28.06	13	15246	1305	90611883
Hypokalaemia	40.13	28.06	76	15183	131040	90482148
Death	39.16	28.06	14	15245	456537	90156651
Duodenal ulcer repair	38.68	28.06	7	15252	54	90613134
Dizziness	36.96	28.06	196	15063	589088	90024100
Condition aggravated	36.72	28.06	28	15231	595517	90017671
Orthostatic hypotension	36.56	28.06	40	15219	41787	90571401
Hypomagnesaemia	36.38	28.06	37	15222	35551	90577637
Drug hypersensitivity	35.27	28.06	17	15242	463592	90149596
Stomatitis	35.11	28.06	3	15256	274695	90338493
Hypersensitivity vasculitis	34.77	28.06	16	15243	4143	90609045
Confusional state	34.13	28.06	142	15117	386063	90227125
COVID-19	33.39	28.06	82	15177	168761	90444427
Duodenogastric reflux	33.34	28.06	7	15252	124	90613064
Femoral neck fracture	33.25	28.06	21	15238	10212	90602976
Cellulitis	33.11	28.06	57	15202	91280	90521908
Swelling face	32.46	28.06	53	15206	81299	90531889
Treatment failure	32.38	28.06	6	15253	303922	90309266
Memory impairment	32.05	28.06	89	15170	197155	90416033
Weight decreased	31.97	28.06	12	15247	379898	90233290
Emotional distress	31.93	28.06	35	15224	36627	90576561
Neutropenic sepsis	30.64	28.06	25	15234	18105	90595083
Back pain	29.90	28.06	119	15140	317056	90296132
Monoclonal B-cell lymphocytosis	29.86	28.06	7	15252	209	90612979
Glossodynia	29.09	28.06	9	15250	321770	90291418
Drug intolerance	28.93	28.06	20	15239	447571	90165617
Peripheral swelling	28.36	28.06	141	15118	412965	90200223
Wound	28.25	28.06	8	15251	302972	90310216
Migraine	28.10	28.06	83	15176	190309	90422879

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
Cardiospasm	317.14	35.64	77	10321	1830	42609107
Palmoplantar keratoderma	294.48	35.64	75	10323	2179	42608758
Lip swelling	285.24	35.64	123	10275	18930	42592007
Pruritus genital	282.75	35.64	75	10323	2564	42608373
Sleep terror	275.07	35.64	75	10323	2851	42608086
Tension headache	272.67	35.64	77	10321	3337	42607600
Atrial tachycardia	262.34	35.64	78	10320	4062	42606875
Carotid artery occlusion	252.69	35.64	76	10322	4118	42606819
Facial pain	247.23	35.64	75	10323	4185	42606752
Anosmia	236.94	35.64	76	10322	5100	42605837
Immunisation	210.20	35.64	51	10347	1207	42609730
Pain of skin	207.46	35.64	77	10321	8003	42602934
Muscle twitching	199.33	35.64	83	10315	11697	42599240
Subarachnoid haemorrhage	195.65	35.64	87	10311	14385	42596552
Eye pruritus	181.68	35.64	77	10321	11335	42599602
Pericarditis	169.56	35.64	77	10321	13367	42597570
Blindness	165.74	35.64	83	10315	17895	42593042
Rash papular	162.84	35.64	72	10326	11739	42599198
Vasculitis	152.34	35.64	79	10319	18315	42592622
Amnesia	150.50	35.64	91	10307	28346	42582591
Diplopia	139.43	35.64	77	10321	20239	42590698
Angioedema	132.92	35.64	98	10300	42379	42568558
Abdominal discomfort	129.84	35.64	123	10275	75132	42535805
Migraine	125.96	35.64	78	10320	25336	42585601
Hallucination	124.84	35.64	107	10291	57400	42553537
Disturbance in attention	124.06	35.64	82	10316	29784	42581153
Cognitive disorder	116.35	35.64	83	10315	34089	42576848
Transient ischaemic attack	115.00	35.64	82	10316	33657	42577280
Ventricular tachycardia	113.75	35.64	78	10320	30082	42580855
Tinnitus	109.51	35.64	75	10323	28863	42582074
Palpitations	107.15	35.64	93	10305	50704	42560233
Alopecia	106.37	35.64	74	10324	29202	42581735
Visual impairment	99.23	35.64	83	10315	43030	42567907
Intentional product misuse	98.84	35.64	97	10301	61803	42549134
Peripheral swelling	95.86	35.64	114	10284	90156	42520781
Drug ineffective	93.82	35.64	20	10378	630177	41980760
Radiation inflammation	89.85	35.64	25	10373	1023	42609914
Feeling abnormal	87.37	35.64	96	10302	69690	42541247
Abdominal pain upper	83.88	35.64	102	10296	82507	42528430
Memory impairment	82.58	35.64	80	10318	50142	42560795
Pulmonary pain	79.75	35.64	25	10373	1553	42609384
Dry skin	77.60	35.64	76	10322	48262	42562675
Malaise	72.90	35.64	160	10238	211996	42398941
Heart rate increased	69.66	35.64	75	10323	53180	42557757
Blood glucose increased	62.14	35.64	83	10315	73616	42537321
COVID-19	61.29	35.64	105	10293	115843	42495094
Muscular weakness	59.89	35.64	87	10311	83411	42527526
Death	58.68	35.64	21	10377	471164	42139773
Neutropenic sepsis	52.55	35.64	38	10360	15908	42595029
Tachycardia	51.38	35.64	90	10308	100997	42509940
Hyperhidrosis	50.50	35.64	84	10314	90428	42520509
Chest pain	45.31	35.64	103	10295	139427	42471510
Lower respiratory tract infection	45.25	35.64	53	10345	41153	42569784
Hyponatraemia	43.56	35.64	84	10314	101378	42509559
Dehydration	43.12	35.64	102	10296	141665	42469272
Toxicity to various agents	41.48	35.64	4	10394	229132	42381805
Genital pain	40.14	35.64	13	10385	897	42610040
Asthenia	39.43	35.64	10	10388	280783	42330154
Bradyarrhythmia	39.09	35.64	17	10381	2658	42608279
Anxiety	36.79	35.64	86	10312	118474	42492463
Genital ulceration	36.36	35.64	12	10386	879	42610058

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
Cardiospasm	579.25	27.33	149	25128	4818	110559204
Lip swelling	564.88	27.33	261	25016	50406	110513616
Palmoplantar keratoderma	557.66	27.33	147	25130	5240	110558782
Tension headache	537.29	27.33	162	25115	9456	110554566
Pruritus genital	534.41	27.33	148	25129	6374	110557648
Sleep terror	527.86	27.33	147	25130	6463	110557559
Atrial tachycardia	501.56	27.33	152	25125	9026	110554996
Carotid artery occlusion	478.43	27.33	148	25129	9417	110554605
Anosmia	439.82	27.33	148	25129	12324	110551698
Facial pain	413.60	27.33	149	25128	15190	110548832
Immunisation	408.08	27.33	103	25174	3080	110560942
Pain of skin	385.41	27.33	152	25125	19877	110544145
Subarachnoid haemorrhage	368.74	27.33	165	25112	29537	110534485
Blindness	336.89	27.33	165	25112	36194	110527828
Muscle twitching	335.93	27.33	155	25122	29780	110534242
Eye pruritus	322.52	27.33	155	25122	32620	110531402
Hallucination	317.20	27.33	228	25049	101204	110462818
Vasculitis	309.23	27.33	155	25122	35718	110528304
Diplopia	303.40	27.33	161	25116	41733	110522289
Hyponatraemia	282.84	27.33	296	24981	217357	110346665
Intentional product misuse	274.94	27.33	234	25043	132670	110431352
Ventricular tachycardia	258.34	27.33	154	25123	49855	110514167
Angioedema	255.60	27.33	198	25079	98302	110465720
Disturbance in attention	240.01	27.33	159	25118	61836	110502186
Rash papular	239.88	27.33	120	25157	27519	110536503
Pulmonary pain	235.02	27.33	78	25199	6215	110557807
Amnesia	233.25	27.33	193	25084	105215	110458807
Transient ischaemic attack	233.06	27.33	158	25119	63824	110500198
Drug ineffective	231.86	27.33	36	25241	1520504	109043518
Tinnitus	228.89	27.33	153	25124	60387	110503635
Palpitations	211.11	27.33	219	25058	158993	110405029
Cognitive disorder	209.96	27.33	168	25109	87343	110476679
Visual impairment	172.94	27.33	182	25095	134246	110429776
Amyloid arthropathy	155.60	27.33	42	25235	1638	110562384
Dry skin	153.37	27.33	154	25123	107499	110456523
Blood glucose increased	135.28	27.33	159	25118	132337	110431685
Feeling abnormal	129.61	27.33	182	25095	180529	110383493
Malaise	121.66	27.33	383	24894	671436	109892586
Hyperhidrosis	115.98	27.33	176	25101	187122	110376900
Tachycardia	113.04	27.33	193	25084	226452	110337570
Heart rate increased	110.83	27.33	150	25127	143684	110420338
Myocardial infarction	101.66	27.33	168	25109	191915	110372107
Abdominal discomfort	100.03	27.33	254	25023	393604	110170418
Dehydration	99.47	27.33	206	25071	279305	110284717
Migraine	94.71	27.33	153	25124	171499	110392523
Radiation inflammation	91.45	27.33	25	25252	1023	110562999
Muscular weakness	88.24	27.33	183	25094	248285	110315737
Peripheral swelling	86.86	27.33	245	25032	403789	110160233
Memory impairment	85.65	27.33	158	25119	196786	110367236
COVID-19	84.11	27.33	178	25099	244882	110319140
Weight increased	82.69	27.33	3	25274	419641	110144381
Neutropenic sepsis	82.27	27.33	63	25214	30683	110533339
Lethargy	80.42	27.33	103	25174	93473	110470549
Acute kidney injury	77.04	27.33	318	24959	635112	109928910
Death	76.61	27.33	32	25245	698837	109865185
Abdominal pain upper	72.37	27.33	209	25068	348902	110215120
Disturbance in social behaviour	68.86	27.33	30	25247	5028	110558994
Swelling face	64.67	27.33	92	25185	92229	110471793
Pericarditis	63.73	27.33	149	25128	218965	110345057
Rheumatoid arthritis	56.18	27.33	3	25274	299610	110264412
Dizziness	55.88	27.33	310	24967	697883	109866139
Chest pain	55.87	27.33	201	25076	376174	110187848
Infusion related reaction	55.59	27.33	10	25267	381152	110182870
Hepatic enzyme increased	55.01	27.33	5	25272	320887	110243135
Vomiting	54.46	27.33	375	24902	910300	109653722
Swelling	53.90	27.33	8	25269	351033	110212989
Toxicity to various agents	52.62	27.33	22	25255	480533	110083489
Sinusitis	52.57	27.33	4	25273	296684	110267338
Pruritus	52.51	27.33	267	25010	581293	109982729
General physical health deterioration	52.47	27.33	16	25261	425279	110138743
Mouth swelling	52.46	27.33	28	25249	7326	110556696
Confusional state	52.40	27.33	229	25048	468451	110095571
Weight decreased	51.94	27.33	21	25256	468036	110095986
Back pain	51.59	27.33	194	25083	370802	110193220
Orthostatic hypotension	50.85	27.33	69	25208	66180	110497842
Lower respiratory tract infection	50.77	27.33	146	25131	242960	110321062
Anxiety	45.95	27.33	178	25099	344900	110219122
Paranoia	43.35	27.33	38	25239	22336	110541686
Thrombocytopenia	43.25	27.33	13	25264	348872	110215150
Agitation	42.12	27.33	85	25192	112966	110451056
Drug abuse	39.42	27.33	109	25168	177302	110386720
Drug hypersensitivity	39.22	27.33	28	25249	454062	110109960
Alopecia	39.05	27.33	176	25101	364577	110199445
Condition aggravated	38.67	27.33	68	25209	734768	109829254
Anaemia	38.47	27.33	41	25236	547045	110016977
Nail dystrophy	37.15	27.33	13	25264	1215	110562807
Treatment failure	36.86	27.33	9	25268	277225	110286797
Knee arthroplasty	35.92	27.33	58	25219	64890	110499132
Bradyarrhythmia	35.79	27.33	19	25258	4915	110559107
Genital pain	35.48	27.33	13	25264	1387	110562635
Adverse drug reaction	35.38	27.33	76	25201	105483	110458539
Hypomagnesaemia	34.88	27.33	55	25222	60315	110503707
Pneumonia	34.70	27.33	95	25182	876619	109687403
Duodenal ulcer repair	34.31	27.33	7	25270	77	110563945
Psoriatic arthropathy	33.89	27.33	3	25274	196758	110367264
Dyspnoea	33.48	27.33	393	24884	1106479	109457543
Hypertension	32.85	27.33	41	25236	510043	110053979
Inappropriate schedule of product administration	32.76	27.33	4	25273	203633	110360389
Disorientation	32.33	27.33	58	25219	70613	110493409
Insomnia	32.09	27.33	165	25112	360425	110203597
Liver function test abnormal	32.07	27.33	57	25220	68893	110495129
Completed suicide	31.96	27.33	8	25269	242373	110321649
Hypokalaemia	31.91	27.33	103	25174	182345	110381677
Impaired healing	31.32	27.33	4	25273	196713	110367309
Mixed dementia	30.33	27.33	8	25269	285	110563737
Drug intolerance	30.23	27.33	29	25248	406483	110157539
Lid lag	29.56	27.33	7	25270	159	110563863
Wound	28.57	27.33	9	25268	234428	110329594
Duodenogastric reflux	27.86	27.33	7	25270	205	110563817
Genital ulceration	27.82	27.33	12	25265	1963	110562059
Superinfection	27.80	27.33	17	25260	5746	110558276
White blood cell count decreased	27.61	27.33	9	25268	229381	110334641
Abnormal loss of weight	27.39	27.33	21	25256	10236	110553786

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C03AA01	CARDIOVASCULAR SYSTEM DIURETICS LOW-CEILING DIURETICS, THIAZIDES Thiazides, plain
ATC	C03AB01	CARDIOVASCULAR SYSTEM DIURETICS LOW-CEILING DIURETICS, THIAZIDES Thiazides and potassium in combination
ATC	C03EA13	CARDIOVASCULAR SYSTEM DIURETICS DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION Low-ceiling diuretics and potassium-sparing agents
FDA CS	M0471776	Thiazides
FDA PE	N0000175359	Increased Diuresis
FDA EPC	N0000175419	Thiazide Diuretic
CHEBI has role	CHEBI:35498	diuretic
CHEBI has role	CHEBI:35554	cardiovascular drug
CHEBI has role	CHEBI:35674	antihypertensive agent
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004232	Diuretics
MeSH PA	D045283	Natriuretic Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D049993	Sodium Chloride Symporter Inhibitors

Related Drugs by ATC class:

C03AA Thiazides, plain 9 drugs

chlorothiazide cyclopenthiazide cyclothiazide hydrochlorothiazide hydroflumethiazide mebutizide methylclothiazide polythiazide trichlormethiazide

C03AB Thiazides and potassium in combination 8 drugs

chlorothiazide cyclopenthiazide cyclothiazide hydrochlorothiazide hydroflumethiazide methylclothiazide polythiazide trichlormethiazide

C03EA Low-ceiling diuretics and potassium-sparing agents 9 drugs

altizide butizide chlortalidone cyclopenthiazide epitizide hydrochlorothiazide mebutizide metolazone trichlormethiazide

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Anuria	contraindication	2472002	DOID:2983
Bronchospasm	contraindication	4386001
Hypercholesterolemia	contraindication	13644009
Complete atrioventricular block	contraindication	27885002
Depressive disorder	contraindication	35489007
Hyperuricemia	contraindication	35885006	DOID:1920
Anaphylaxis	contraindication	39579001
Hypokalemia	contraindication	43339004
Sinus bradycardia	contraindication	49710005
Systemic lupus erythematosus	contraindication	55464009	DOID:9074
Sympathectomy	contraindication	57071006
Acute nephropathy	contraindication	58574008
Hypercalcemia	contraindication	66931009	DOID:12678
Hyperparathyroidism	contraindication	66999008	DOID:13543
Hepatic coma	contraindication	72836002	DOID:12550
Diabetes mellitus	contraindication	73211009	DOID:9351
Oliguria	contraindication	83128009
Pulmonary emphysema	contraindication	87433001
Cardiogenic shock	contraindication	89138009
Hyponatremia	contraindication	89627008
Gout	contraindication	90560007	DOID:13189
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Hypomagnesemia	contraindication	190855004
Partial atrioventricular block	contraindication	195039008
Decompensated cardiac failure	contraindication	195111005
Acute pancreatitis	contraindication	197456007	DOID:2913
Disease of liver	contraindication	235856003	DOID:409
Raynaud's phenomenon	contraindication	266261006
Neonatal hyperbilirubinemia	contraindication	281610001
Pregnancy, function	contraindication	289908002
Severe chronic obstructive pulmonary disease	contraindication	313299006
Right ventricular failure	contraindication	367363000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.79	acidic
pKa2	10.52	acidic
pKa3	1.03	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	A2	8.30	WOMBAT-PK	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Kd	5.77	CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN				WOMBAT-PK
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN				WOMBAT-PK
Calcium-activated potassium channel subunit alpha-1	Ion channel	Q12791	KCMA1_HUMAN				WOMBAT-PK

External reference:

ID	Source
4017612	VUID
N0000145992	NUI
D00650	KEGG_DRUG
1369	RXNORM
C0004975	UMLSCUI
CHEBI:3013	CHEBI
CHEMBL1684	ChEMBL_ID
D001539	MESH_DESCRIPTOR_UI
DB00436	DRUGBANK_ID
2315	PUBCHEM_CID
7122	IUPHAR_LIGAND_ID
994	INN_ID
5Q52X6ICJI	UNII
3020	MMSL
4252	MMSL
d00641	MMSL
4017612	VANDF
002297	NDDF
387520007	SNOMEDCT_US
91135008	SNOMEDCT_US
5Q52X6ICJI	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nadolol and Bendroflumethiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0115-5311	TABLET	5 mg	ORAL	ANDA	25 sections
Nadolol and Bendroflumethiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0115-5322	TABLET	5 mg	ORAL	ANDA	25 sections

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

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: