irbesartan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	1481	138402-11-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: irbesartan aprovel irbesartan hydrochloride karvea ifirmasta irbesartan HCl	A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease. Molecular weight: 428.54 Formula: C25H28N6O CLOGP: 6.04 LIPINSKI: 1 HAC: 7 HDO: 1 TPSA: 87.13 ALOGS: -4.70 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
0.15	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.08 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	10 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	70 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.94 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.10 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	14 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 30, 1997	FDA	SANOFI AVENTIS US

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
Acute kidney injury	534.85	10.19	954	54932	252914	53040266
Hyponatraemia	456.09	10.19	565	55321	108042	53185138
Neurologic neglect syndrome	238.63	10.19	76	55810	1099	53292081
Carotid artery thrombosis	235.09	10.19	76	55810	1156	53292024
Personality disorder	199.76	10.19	94	55792	4037	53289143
Adjustment disorder	198.35	10.19	75	55811	1848	53291332
Hemiplegia	171.36	10.19	105	55781	7695	53285485
Hyperkalaemia	161.41	10.19	239	55647	54017	53239163
Lactic acidosis	148.38	10.19	189	55697	37064	53256116
Affect lability	132.75	10.19	96	55790	9279	53283901
Rheumatoid arthritis	125.83	10.19	88	55798	314443	52978737
Fall	118.16	10.19	709	55177	357731	52935449
Sensory loss	116.64	10.19	83	55803	7822	53285358
Drug ineffective	116.24	10.19	453	55433	816792	52476388
Motor dysfunction	106.13	10.19	80	55806	8238	53284942
Pain	100.53	10.19	301	55585	588097	52705083
Aphasia	99.39	10.19	141	55745	30637	53262543
Maternal exposure during pregnancy	89.48	10.19	26	55860	155613	53137567
Eating disorder	89.14	10.19	97	55789	16100	53277080
Treatment failure	88.96	10.19	14	55872	128389	53164791
Renal failure	88.32	10.19	299	55587	118153	53175027
Coordination abnormal	86.56	10.19	83	55803	11868	53281312
Drug interaction	85.42	10.19	454	55432	218875	53074305
Hypoglycaemia	81.95	10.19	187	55699	58826	53234354
Hypotension	81.28	10.19	499	55387	253577	53039603
Hemiparesis	80.87	10.19	106	55780	21369	53271811
Muscle spasticity	79.85	10.19	96	55790	17742	53275438
Therapeutic product effect decreased	75.97	10.19	19	55867	125636	53167544
Contraindicated product administered	75.52	10.19	24	55862	135605	53157575
Sinus bradycardia	74.41	10.19	84	55802	14517	53278663
Glossodynia	74.03	10.19	9	55877	100282	53192898
Systemic lupus erythematosus	73.84	10.19	20	55866	125394	53167786
Drug hypersensitivity	70.94	10.19	105	55781	265137	53028043
Blood pressure increased	70.62	10.19	313	55573	140166	53153014
Hand deformity	69.56	10.19	5	55881	84844	53208336
Hypertension	64.19	10.19	430	55456	225001	53068179
Synovitis	63.90	10.19	17	55869	107876	53185304
Cerebrovascular accident	61.14	10.19	245	55641	104929	53188251
Bradycardia	60.74	10.19	188	55698	70868	53222312
Hypertensive crisis	58.37	10.19	74	55812	14432	53278748
Blood pressure systolic increased	57.41	10.19	119	55767	35058	53258122
Off label use	55.74	10.19	280	55606	471932	52821248
Hepatocellular injury	55.61	10.19	107	55779	29879	53263301
Ischaemic stroke	54.53	10.19	80	55806	17913	53275267
Atrial fibrillation	54.01	10.19	246	55640	111406	53181774
Dysarthria	53.50	10.19	126	55760	40442	53252738
Pemphigoid	52.92	10.19	48	55838	6396	53286784
Confusional state	52.60	10.19	366	55520	193855	53099325
Death	48.56	10.19	201	55685	357031	52936149
Syncope	48.52	10.19	239	55647	111754	53181426
Arthropathy	47.30	10.19	47	55839	141406	53151774
Rhabdomyolysis	47	10.19	126	55760	43797	53249383
Hypokalaemia	46.93	10.19	213	55673	96304	53196876
Inappropriate antidiuretic hormone secretion	46.07	10.19	67	55819	14884	53278296
Swelling	46.03	10.19	81	55805	191024	53102156
Vertigo	45.73	10.19	146	55740	55935	53237245
Alopecia	44.33	10.19	114	55772	234469	53058711
Exposure during pregnancy	43.48	10.19	40	55846	124820	53168360
Asthenia	43.46	10.19	550	55336	343040	52950140
Cholestasis	43.27	10.19	94	55792	28601	53264579
Dehydration	42.47	10.19	312	55574	168098	53125082
Joint swelling	39.90	10.19	120	55766	234518	53058662
Atrioventricular block first degree	39.24	10.19	41	55845	6494	53286686
Shock haemorrhagic	38.79	10.19	48	55838	9135	53284045
Product dose omission issue	37.06	10.19	92	55794	191528	53101652
Pericarditis	36.55	10.19	11	55875	64395	53228785
Infection	36.26	10.19	79	55807	172126	53121054
Oedema peripheral	36.22	10.19	304	55582	170483	53122697
Abdominal discomfort	36.20	10.19	115	55771	220947	53072233
Therapeutic product effect incomplete	36.19	10.19	26	55860	91758	53201422
Fear of eating	35.79	10.19	14	55872	379	53292801
Arteriovenous fistula occlusion	35.79	10.19	14	55872	379	53292801
Atrioventricular block complete	35.64	10.19	43	55843	7972	53285208
Blue toe syndrome	34.79	10.19	14	55872	409	53292771
Completed suicide	34.71	10.19	57	55829	138144	53155036
Drug intolerance	34.28	10.19	106	55780	205387	53087793
Product use issue	32.84	10.19	60	55826	139524	53153656
Angioedema	31.13	10.19	106	55780	41970	53251210
Muscular weakness	30.72	10.19	196	55690	100796	53192384
Hepatic cytolysis	29.80	10.19	39	55847	7846	53285334
Rash	29.52	10.19	312	55574	445879	52847301
Tubulointerstitial nephritis	29.51	10.19	58	55828	16446	53276734
Malaise	29.08	10.19	531	55355	357086	52936094
Renal impairment	28.05	10.19	166	55720	83152	53210028
Dysphagia	27.68	10.19	167	55719	84230	53208950
Prothrombin time ratio decreased	27.01	10.19	12	55874	450	53292730
Neurofibrosarcoma	26.91	10.19	9	55877	153	53293027
Blood potassium increased	26.39	10.19	58	55828	17783	53275397
Anuria	26.33	10.19	47	55839	12393	53280787
Hypersensitivity	25.87	10.19	123	55763	210542	53082638
Vascular purpura	25.68	10.19	17	55869	1424	53291756
Blood pressure fluctuation	25.05	10.19	88	55798	35382	53257798
Haematoma	24.80	10.19	85	55801	33759	53259421
International normalised ratio increased	24.40	10.19	107	55779	47654	53245526
Psoriatic arthropathy	24.31	10.19	10	55876	48180	53245000
Sinus arrest	24.11	10.19	18	55868	1826	53291354
Acidosis	24.06	10.19	43	55843	11349	53281831
Febrile neutropenia	23.89	10.19	46	55840	104890	53188290
Blood creatinine increased	23.66	10.19	158	55728	82504	53210676
Meningorrhagia	23.60	10.19	8	55878	142	53293038
Intestinal angioedema	23.31	10.19	12	55874	627	53292553
Hypergammaglobulinaemia	23.16	10.19	11	55875	482	53292698
Haemangioma congenital	22.97	10.19	11	55875	491	53292689
Blood pressure inadequately controlled	22.91	10.19	27	55859	4884	53288296
Anal polyp	22.62	10.19	6	55880	43	53293137
Blood sodium decreased	22.43	10.19	64	55822	23052	53270128
Injection site reaction	22.20	10.19	13	55873	51153	53242027
Heart rate decreased	22.19	10.19	87	55799	36860	53256320
Injection site erythema	22.19	10.19	29	55857	77220	53215960
Sinusitis	22.13	10.19	96	55790	168468	53124712
Toxicity to various agents	22.12	10.19	137	55749	219461	53073719
Prevertebral soft tissue swelling of cervical space	22.04	10.19	6	55880	48	53293132
Interstitial lung disease	21.83	10.19	120	55766	58502	53234678
Discomfort	21.60	10.19	42	55844	95430	53197750
Diabetic metabolic decompensation	21.53	10.19	16	55870	1612	53291568
Cutaneous vasculitis	21.42	10.19	25	55861	4476	53288704
Torsade de pointes	21.22	10.19	44	55842	12961	53280219
Renin decreased	21.21	10.19	7	55879	114	53293066
Hypochloraemia	21.10	10.19	17	55869	1929	53291251
Eosinophilia	20.64	10.19	59	55827	21276	53271904
Primary hyperaldosteronism	20.33	10.19	6	55880	66	53293114
Botryomycosis	20.22	10.19	5	55881	26	53293154
Dermatitis bullous	20.12	10.19	33	55853	8130	53285050
Coronary artery disease	19.49	10.19	78	55808	33359	53259821
Loss of consciousness	19.46	10.19	194	55692	114018	53179162
Injection site pain	19.24	10.19	58	55828	113333	53179847
Haemodialysis	19.23	10.19	35	55851	9369	53283811
Milk-alkali syndrome	19.12	10.19	11	55875	717	53292463
Fatigue	19.04	10.19	602	55284	729904	52563276
Vulvar basal cell carcinoma	18.95	10.19	5	55881	35	53293145
Blood aldosterone increased	18.27	10.19	7	55879	179	53293001
Duodenal ulcer perforation	18.24	10.19	7	55879	35176	53258004
Dizziness	18.05	10.19	514	55372	371745	52921435
Electrolyte imbalance	18.05	10.19	52	55834	18832	53274348
Hyperlactacidaemia	18.00	10.19	18	55868	2707	53290473
Upper respiratory tract infection	17.81	10.19	28	55858	69069	53224111
Histoplasmosis	17.72	10.19	15	55871	1823	53291357
Irritable bowel syndrome	17.67	10.19	12	55874	43620	53249560
Wound	17.65	10.19	44	55842	91513	53201667
Abortion spontaneous	17.37	10.19	14	55872	46621	53246559
Hepatitis	17.36	10.19	76	55810	33818	53259362
Congenital musculoskeletal anomaly	17.27	10.19	9	55877	482	53292698
Product use in unapproved indication	17.27	10.19	60	55826	112229	53180951
Sebaceous gland infection	17.22	10.19	6	55880	116	53293064
Cardiac failure	17.22	10.19	151	55735	85693	53207487
Renal pain	17.12	10.19	26	55860	6001	53287179
Reversible cerebral vasoconstriction syndrome	17.03	10.19	16	55870	2229	53290951
Left atrial dilatation	16.98	10.19	15	55871	1930	53291250
Blood pressure diastolic decreased	16.77	10.19	47	55839	16756	53276424
Brucellosis	16.63	10.19	5	55881	59	53293121
Myocardial infarction	16.56	10.19	168	55718	99186	53193994
Sepsis	16.53	10.19	88	55798	146341	53146839
Product substitution issue	16.45	10.19	45	55841	15821	53277359
Arthralgia	16.34	10.19	344	55542	439439	52853741
Incision site haemorrhage	16.27	10.19	9	55877	544	53292636
Orthostatic hypotension	16.23	10.19	68	55818	29685	53263495
Cardiac ventricular thrombosis	16.18	10.19	9	55877	550	53292630
Impaired healing	15.63	10.19	27	55859	64178	53229002
Adverse drug reaction	15.53	10.19	20	55866	53605	53239575
Hospitalisation	15.41	10.19	32	55854	70980	53222200
Emphysematous cystitis	15.39	10.19	6	55880	161	53293019
Body temperature decreased	15.14	10.19	45	55841	16582	53276598
Depression	15.09	10.19	121	55765	182931	53110249
Electrocardiogram QT prolonged	15.06	10.19	106	55780	56297	53236883
Intentional self-injury	14.93	10.19	4	55882	25280	53267900
Pulmonary artery atresia	14.92	10.19	4	55882	30	53293150
Jaundice	14.79	10.19	67	55819	30246	53262934
Oliguria	14.77	10.19	31	55855	9207	53283973
Enterococcal sepsis	14.74	10.19	12	55874	1382	53291798
Intra-abdominal haematoma	14.72	10.19	13	55873	1672	53291508
Device related infection	14.65	10.19	3	55883	22783	53270397
Shock	14.31	10.19	55	55831	23084	53270096
Sinus node dysfunction	14.10	10.19	20	55866	4341	53288839
Electrocardiogram PR prolongation	14.08	10.19	9	55877	710	53292470
Disease progression	14.02	10.19	57	55829	101863	53191317
Wrong patient received product	13.95	10.19	14	55872	2114	53291066
Retching	13.93	10.19	39	55847	13894	53279286
Premature delivery	13.85	10.19	5	55881	26099	53267081
Injection site pruritus	13.68	10.19	14	55872	41575	53251605
Necrotising myositis	13.68	10.19	7	55879	361	53292819
Disorientation	13.61	10.19	79	55807	39280	53253900
Hypochromic anaemia	13.45	10.19	13	55873	1876	53291304
Device dislocation	13.44	10.19	4	55882	23593	53269587
Respiratory acidosis	13.35	10.19	24	55862	6364	53286816
Malignant neoplasm progression	13.31	10.19	35	55851	71506	53221674
Injection site swelling	13.30	10.19	15	55871	42613	53250567
Pulmonary pain	13.09	10.19	14	55872	2278	53290902
Skin sensitisation	13.04	10.19	9	55877	807	53292373
Pneumonia	13.00	10.19	326	55560	406843	52886337
Parotid gland enlargement	12.95	10.19	9	55877	816	53292364
Musculoskeletal stiffness	12.91	10.19	76	55810	123292	53169888
Drug ineffective for unapproved indication	12.77	10.19	3	55883	20717	53272463
Pure white cell aplasia	12.74	10.19	4	55882	55	53293125
Tendon injury	12.72	10.19	12	55874	1680	53291500
Multiple sclerosis relapse	12.71	10.19	17	55869	44836	53248344
Fundoscopy abnormal	12.58	10.19	3	55883	13	53293167
Transient ischaemic attack	12.55	10.19	72	55814	35653	53257527
Anaphylactic reaction	12.43	10.19	104	55782	58222	53234958
Ascites	12.38	10.19	14	55872	39721	53253459
Migraine	12.34	10.19	43	55843	80374	53212806
Oropharyngeal swelling	12.28	10.19	9	55877	887	53292293
Acute coronary syndrome	12.27	10.19	31	55855	10393	53282787
Cerebral haemorrhage	12.26	10.19	63	55823	29933	53263247
Subacute kidney injury	12.23	10.19	3	55883	15	53293165
Rash morbilliform	12.12	10.19	16	55870	3247	53289933
Drug resistance	12.09	10.19	3	55883	19959	53273221
Anaemia	12.02	10.19	377	55509	276341	53016839
Injection site bruising	12.02	10.19	13	55873	37633	53255547
Haematoma muscle	11.96	10.19	8	55878	682	53292498
Impaired work ability	11.77	10.19	37	55849	14053	53279127
Peripheral swelling	11.68	10.19	149	55737	205959	53087221
Blood immunoglobulin E increased	11.53	10.19	13	55873	2242	53290938
Bronchopulmonary aspergillosis allergic	11.49	10.19	10	55876	1262	53291918
Renal tubular necrosis	11.45	10.19	32	55854	11387	53281793
Fibrous histiocytoma	11.44	10.19	7	55879	511	53292669
Condition aggravated	11.43	10.19	231	55655	296903	52996277
Physical assault	11.42	10.19	9	55877	989	53292191
Optic nerve infarction	11.37	10.19	3	55883	21	53293159
Localised oedema	11.16	10.19	20	55866	5289	53287891
Respiratory tract infection	11.14	10.19	11	55875	33213	53259967
Stomatitis	11.07	10.19	59	55827	98099	53195081
Oral lichen planus	11.06	10.19	7	55879	543	53292637
Subacute cutaneous lupus erythematosus	11.02	10.19	13	55873	2355	53290825
Blood pressure decreased	10.97	10.19	106	55780	61763	53231417
Ear pain	10.93	10.19	9	55877	29664	53263516
Helicobacter infection	10.88	10.19	15	55871	39054	53254126
Contraindicated product prescribed	10.85	10.19	8	55878	796	53292384
Hepatorenal syndrome	10.82	10.19	12	55874	2033	53291147
Drug abuse	10.77	10.19	34	55852	65492	53227688
C-reactive protein abnormal	10.63	10.19	7	55879	25863	53267317
Toxic skin eruption	10.51	10.19	34	55852	13105	53280075
White blood cell analysis abnormal	10.43	10.19	3	55883	30	53293150
Insulinoma	10.38	10.19	4	55882	104	53293076

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
Acute kidney injury	295.96	10.83	916	39499	292552	32180559
Lactic acidosis	120.85	10.83	177	40238	33359	32439752
Death	114.07	10.83	188	40227	382329	32090782
Hyponatraemia	97.22	10.83	256	40159	74257	32398854
Hyperkalaemia	96.52	10.83	245	40170	69505	32403606
Oesophageal pain	59.73	10.83	26	40389	778	32472333
Anorectal discomfort	59.39	10.83	34	40381	1846	32471265
Hypoglycaemia	59.20	10.83	175	40240	54207	32418904
Hypotension	58.16	10.83	463	39952	215647	32257464
Drug abuse	56.41	10.83	15	40400	80228	32392883
Off label use	55.70	10.83	195	40220	306125	32166986
Bradycardia	52.78	10.83	202	40213	71360	32401751
Completed suicide	48.97	10.83	27	40388	92490	32380621
Eosinophilia	48.13	10.83	100	40315	24858	32448253
Seronegative arthritis	45.43	10.83	23	40392	974	32472137
Blood pressure increased	45.22	10.83	207	40208	79147	32393964
Fractured coccyx	45.17	10.83	14	40401	153	32472958
Syncope	44.09	10.83	225	40190	89899	32383212
Presyncope	41.49	10.83	76	40339	17225	32455886
Febrile neutropenia	41.09	10.83	53	40362	119513	32353598
Blood pressure systolic increased	39.94	10.83	75	40340	17321	32455790
Foetal exposure during pregnancy	39.85	10.83	3	40412	41298	32431813
Drug ineffective	39.57	10.83	297	40118	383180	32089931
N-terminal prohormone brain natriuretic peptide abnormal	37.83	10.83	13	40402	201	32472910
Failure to suspend medication	35.88	10.83	14	40401	315	32472796
Blood thyroid stimulating hormone abnormal	35.40	10.83	13	40402	246	32472865
Pneumonia	34.81	10.83	279	40136	354973	32118138
Treatment failure	34.71	10.83	4	40411	39159	32433952
Pulmonary arterial pressure abnormal	34.26	10.83	12	40403	197	32472914
Lipoma	33.79	10.83	22	40393	1506	32471605
Electrocardiogram QRS complex abnormal	32.50	10.83	13	40402	313	32472798
Eczema	32.43	10.83	63	40352	14917	32458194
Brain natriuretic peptide abnormal	31.28	10.83	13	40402	346	32472765
Oxygen saturation increased	31.22	10.83	12	40403	259	32472852
Agranulocytosis	30.91	10.83	81	40334	23396	32449715
Rhabdomyolysis	30.85	10.83	165	40250	67100	32406011
Disease progression	30.35	10.83	38	40377	86824	32386287
Blood creatinine increased	30.31	10.83	214	40201	95918	32377193
Fall	29.58	10.83	373	40042	195828	32277283
Lung diffusion test decreased	28.95	10.83	15	40400	667	32472444
Congenital diaphragmatic anomaly	28.61	10.83	7	40408	28	32473083
Tongue abscess	28.46	10.83	5	40410	0	32473111
Renal failure	28.21	10.83	273	40142	134205	32338906
Arrhythmia	27.96	10.83	102	40313	35201	32437910
Dysgeusia	27.61	10.83	82	40333	25449	32447662
Carotid arteriosclerosis	27.61	10.83	17	40398	1056	32472055
Plasma cell myeloma	27.44	10.83	19	40396	57595	32415516
Gastrointestinal motility disorder	27.41	10.83	23	40392	2324	32470787
Hypoparathyroidism	27.38	10.83	13	40402	478	32472633
Mycobacterium test positive	27.35	10.83	12	40403	366	32472745
Drug interaction	26.85	10.83	400	40015	217785	32255326
Pemphigoid	26.78	10.83	42	40373	8394	32464717
Hypovolaemia	26.54	10.83	43	40372	8834	32464277
Vomiting projectile	25.64	10.83	14	40401	693	32472418
Left ventricular dilatation	25.56	10.83	14	40401	697	32472414
Cerebrovascular accident	24.82	10.83	188	40227	86132	32386979
Vestibular neuronitis	24.43	10.83	9	40406	172	32472939
Product dose omission issue	23.88	10.83	58	40357	102517	32370594
Pancreatitis acute	23.37	10.83	81	40334	27254	32445857
Antiphospholipid antibodies positive	22.89	10.83	10	40405	302	32472809
Wrong patient received product	22.51	10.83	21	40394	2441	32470670
Sepsis	22.03	10.83	112	40303	158722	32314389
Shock	21.98	10.83	73	40342	24041	32449070
Tachyarrhythmia	21.92	10.83	24	40391	3375	32469736
Anuria	21.56	10.83	44	40371	10793	32462318
Left atrial dilatation	21.16	10.83	18	40397	1854	32471257
Ear discomfort	21.01	10.83	20	40395	2384	32470727
Rash maculo-papular	20.55	10.83	79	40336	27943	32445168
Cholestasis	20.47	10.83	77	40338	26956	32446155
Blood creatine phosphokinase increased	20.47	10.83	111	40304	45365	32427746
Toxicity to various agents	20.17	10.83	134	40281	177907	32295204
Preternatural anus	20.09	10.83	7	40408	113	32472998
Acute pulmonary oedema	19.83	10.83	35	40380	7706	32465405
Mucosal dryness	19.63	10.83	14	40401	1113	32471998
Hypertension	19.61	10.83	250	40165	131500	32341611
Malignant neoplasm progression	19.38	10.83	43	40372	78453	32394658
Neutrophil count decreased	19.37	10.83	18	40397	47121	32425990
White blood cell count decreased	19.36	10.83	54	40361	91144	32381967
Procedural failure	19.24	10.83	6	40409	67	32473044
Mental status changes	19.12	10.83	12	40403	38325	32434786
Myopathy	19.06	10.83	43	40372	11298	32461813
Renal haemorrhage	19.01	10.83	15	40400	1390	32471721
Product use in unapproved indication	18.99	10.83	51	40364	87153	32385958
Supraventricular extrasystoles	18.92	10.83	22	40393	3303	32469808
SARS-CoV-2 sepsis	18.89	10.83	7	40408	136	32472975
Dyslipidaemia	18.78	10.83	32	40383	6851	32466260
Platelet count decreased	18.75	10.83	76	40339	114515	32358596
Morganella infection	18.69	10.83	10	40405	475	32472636
Diabetes mellitus inadequate control	18.63	10.83	48	40367	13720	32459391
Hyperlactacidaemia	18.61	10.83	21	40394	3053	32470058
Cerebral haematoma	18.20	10.83	26	40389	4785	32468326
Tenoplasty	18.06	10.83	4	40411	9	32473102
Melaena	17.95	10.83	88	40327	34577	32438534
Muscle strain	17.92	10.83	23	40392	3822	32469289
Lividity	17.92	10.83	7	40408	158	32472953
Pseudoporphyria	17.62	10.83	8	40407	265	32472846
Carcinoma in situ of skin	17.57	10.83	6	40409	91	32473020
Hospitalisation	17.54	10.83	21	40394	48950	32424161
Pruritus	17.40	10.83	240	40175	128462	32344649
Toxic skin eruption	17.30	10.83	42	40373	11572	32461539
Goitre	17.27	10.83	15	40400	1589	32471522
Nephrectomy	17.18	10.83	11	40404	732	32472379
Metabolic acidosis	16.76	10.83	97	40318	40602	32432509
Therapeutic product effect incomplete	16.73	10.83	16	40399	41325	32431786
Renal impairment	16.54	10.83	181	40234	91791	32381320
Dizziness	16.42	10.83	358	40057	209260	32263851
Atrial thrombosis	16.37	10.83	16	40399	1971	32471140
Precancerous skin lesion	16.36	10.83	10	40405	613	32472498
Conduction disorder	16.35	10.83	16	40399	1974	32471137
Lung disorder	16.29	10.83	84	40331	33670	32439441
Superficial spreading melanoma stage I	16.15	10.83	4	40411	17	32473094
Neoplasm prostate	16.10	10.83	7	40408	209	32472902
Myalgia	16.08	10.83	163	40252	81067	32392044
Haematocrit increased	16.05	10.83	15	40400	1748	32471363
Echinococciasis	15.97	10.83	4	40411	18	32473093
Rectal haemorrhage	15.94	10.83	90	40325	37333	32435778
Cardiac ablation	15.91	10.83	10	40405	644	32472467
Enterocutaneous fistula	15.90	10.83	11	40404	833	32472278
Sneezing	15.64	10.83	24	40391	4707	32468404
Enterochromaffin cell hyperplasia	15.46	10.83	4	40411	21	32473090
Haemochromatosis	15.42	10.83	12	40403	1089	32472022
Drug dependence	15.38	10.83	5	40410	23479	32449632
Periorbital haematoma	15.25	10.83	8	40407	365	32472746
Dermatitis exfoliative	15.17	10.83	31	40384	7613	32465498
Musculoskeletal discomfort	15.09	10.83	29	40386	6811	32466300
Bronchial haemorrhage	14.99	10.83	10	40405	713	32472398
Vascular purpura	14.86	10.83	14	40401	1648	32471463
Drug resistance	14.84	10.83	5	40410	22960	32450151
Eosinophilic pleural effusion	14.83	10.83	7	40408	254	32472857
Blood lactic acid	14.76	10.83	8	40407	390	32472721
Product substitution issue	14.76	10.83	37	40378	10399	32462712
Oedema peripheral	14.71	10.83	211	40204	113880	32359231
Bundle branch block left	14.63	10.83	26	40389	5753	32467358
Drug hypersensitivity	14.46	10.83	45	40370	73355	32399756
Hepatocellular injury	14.37	10.83	66	40349	25252	32447859
Shock haemorrhagic	14.29	10.83	37	40378	10608	32462503
Asthenia	14.27	10.83	389	40026	235555	32237556
Respiratory failure	14.05	10.83	77	40338	107105	32366006
Rheumatoid arthritis	14.02	10.83	21	40394	44523	32428588
Inflammation	14.01	10.83	64	40351	24429	32448682
Sedation	13.92	10.83	3	40412	18523	32454588
Inflammatory marker increased	13.88	10.83	20	40395	3709	32469402
Blood pressure inadequately controlled	13.83	10.83	17	40398	2705	32470406
Blood creatine increased	13.78	10.83	23	40392	4842	32468269
Granuloma	13.76	10.83	17	40398	2718	32470393
Appetite disorder	13.75	10.83	15	40400	2100	32471011
Blood osmolarity decreased	13.64	10.83	9	40406	630	32472481
Interstitial lung disease	13.62	10.83	132	40283	64869	32408242
Hepatitis	13.62	10.83	62	40353	23631	32449480
Atrial fibrillation	13.55	10.83	212	40203	116492	32356619
Renal cyst	13.49	10.83	32	40383	8687	32464424
Acute coronary syndrome	13.42	10.83	43	40372	13898	32459213
Myocardial infarction	13.37	10.83	225	40190	125451	32347660
Actinic keratosis	13.16	10.83	20	40395	3890	32469221
Injection site pain	13.14	10.83	13	40402	33045	32440066
Extrasystoles	13.05	10.83	20	40395	3917	32469194
Malignant melanoma stage I	13.05	10.83	5	40410	107	32473004
Dyspnoea exertional	13.01	10.83	88	40327	38873	32434238
Atrial flutter	12.98	10.83	45	40370	15138	32457973
Thyroiditis	12.80	10.83	14	40401	1966	32471145
Angioedema	12.74	10.83	83	40332	36206	32436905
Hypergastrinaemia	12.64	10.83	4	40411	47	32473064
Gastrointestinal tract mucosal pigmentation	12.59	10.83	7	40408	359	32472752
Hypoxia	12.50	10.83	29	40386	52103	32421008
Orthostatic hypotension	12.49	10.83	64	40351	25586	32447525
Ventricular hypokinesia	12.35	10.83	22	40393	4878	32468233
Hypertensive crisis	12.20	10.83	31	40384	8786	32464325
Haemoglobin increased	12.17	10.83	17	40398	3065	32470046
Product use issue	12.15	10.83	30	40385	52747	32420364
Chronic kidney disease	12.00	10.83	88	40327	39887	32433224
Spinal epidural haemorrhage	11.88	10.83	4	40411	58	32473053
Obstruction	11.85	10.83	13	40402	1832	32471279
Blood bicarbonate decreased	11.80	10.83	15	40400	2469	32470642
Psychotic disorder	11.76	10.83	7	40408	23013	32450098
Accidental death	11.72	10.83	14	40401	2163	32470948
Medication error	11.52	10.83	57	40358	22478	32450633
Coronary artery disease	11.45	10.83	103	40312	49603	32423508
Inappropriate antidiuretic hormone secretion	11.42	10.83	37	40378	12026	32461085
Concomitant disease progression	11.36	10.83	15	40400	2563	32470548
Cytomegalovirus infection	11.34	10.83	9	40406	25455	32447656
Foreign body in respiratory tract	11.29	10.83	5	40410	156	32472955
Pancreatic carcinoma metastatic	11.16	10.83	17	40398	3312	32469799
Post thrombotic syndrome	11.15	10.83	5	40410	161	32472950
Skin cancer	11.10	10.83	30	40385	8820	32464291
Tubulointerstitial nephritis	11.08	10.83	51	40364	19526	32453585
Leukopenia	11.05	10.83	38	40377	60084	32413027
Transient ischaemic attack	10.96	10.83	62	40353	25732	32447379
Scan myocardial perfusion abnormal	10.88	10.83	4	40411	76	32473035

Pharmacologic Action:

Source	Code	Description
ATC	C09CA04	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA04	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
ATC	C09DB05	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and calcium channel blockers
ATC	C09DX07	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs), other combinations
FDA MoA	N0000000070	Angiotensin 2 Receptor Antagonists
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
MeSH PA	D047228	Angiotensin II Type 1 Receptor Blockers
MeSH PA	D057911	Angiotensin Receptor Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
CHEBI has role	CHEBI:35674	antihypertensive
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:61016	angiotensin receptor antagonists
CHEBI has role	CHEBI:78298	environmental contaminants

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Diabetic renal disease	indication	127013003
Chronic heart failure	off-label use	48447003
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Anuria	contraindication	2472002	DOID:2983
Hypercholesterolemia	contraindication	13644009
Hyperkalemia	contraindication	14140009
Secondary angle-closure glaucoma	contraindication	21571006
Hypovolemia	contraindication	28560003
Dehydration	contraindication	34095006
Hyperuricemia	contraindication	35885006	DOID:1920
Angioedema	contraindication	41291007	DOID:1558
Hypokalemia	contraindication	43339004
Low blood pressure	contraindication	45007003
Systemic lupus erythematosus	contraindication	55464009	DOID:9074
Sympathectomy	contraindication	57071006
Hypercalcemia	contraindication	66931009	DOID:12678
Hyperparathyroidism	contraindication	66999008	DOID:13543
Hypochloremic alkalosis	contraindication	70134007
Hepatic coma	contraindication	72836002	DOID:12550
Diabetes mellitus	contraindication	73211009	DOID:9351
Hyponatremia	contraindication	89627008
Gout	contraindication	90560007	DOID:13189
Disorder of muscle	contraindication	129565002	DOID:423
Hypomagnesemia	contraindication	190855004
Acute pancreatitis	contraindication	197456007	DOID:2913
Rhabdomyolysis	contraindication	240131006
Neonatal hyperbilirubinemia	contraindication	281610001
Pregnancy, function	contraindication	289908002
Renal artery stenosis	contraindication	302233006
Azotemia	contraindication	445009001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.37	acidic
pKa2	3.63	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])	Mechanism action	Bioact source	MoA source
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	Ki	9.10		CHEMBL	CHEMBL
Endothelin-1 receptor	GPCR	P25101	EDNRA_HUMAN		Ki	5		CHEMBL
Sodium/bile acid cotransporter	Transporter	Q14973	NTCP_HUMAN	INHIBITOR	Ki	4.92		IUPHAR
Type-1B angiotensin II receptor	GPCR		AGTRB_RAT		Ki	9.10		CHEMBL
Angiotensin II receptor (AT-1) type-1	GPCR		AGTRA_RAT AGTRB_RAT		IC50	8.89		CHEMBL
Angiotensin II receptor	GPCR		AGTRA_RAT AGTRB_RAT AGTR2_RAT		IC50	8.89		CHEMBL

External reference:

ID	Source
4021071	VUID
N0000148533	NUI
D00523	KEGG_DRUG
329055-23-4	SECONDARY_CAS_RN
4021071	VANDF
C0288171	UMLSCUI
CHEBI:5959	CHEBI
CHEMBL1513	ChEMBL_ID
D000077405	MESH_DESCRIPTOR_UI
DB01029	DRUGBANK_ID
3749	PUBCHEM_CID
589	IUPHAR_LIGAND_ID
7229	INN_ID
J0E2756Z7N	UNII
83818	RXNORM
4917	MMSL
52343	MMSL
d04222	MMSL
006921	NDDF
108585000	SNOMEDCT_US
386877005	SNOMEDCT_US
734504000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Avapro	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5850	TABLET, FILM COATED	75 mg	ORAL	NDA	29 sections
Avapro	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5851	TABLET, FILM COATED	150 mg	ORAL	NDA	29 sections
Avapro	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5852	TABLET, FILM COATED	300 mg	ORAL	NDA	29 sections
Avalide	HUMAN PRESCRIPTION DRUG LABEL	2	0024-5855	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
Avalide	HUMAN PRESCRIPTION DRUG LABEL	2	0024-5856	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0054-0254	TABLET	150 mg	ORAL	ANDA	28 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0054-0255	TABLET	300 mg	ORAL	ANDA	28 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0093-8232	TABLET, FILM COATED	300 mg	ORAL	ANDA	28 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0093-8238	TABLET, FILM COATED	150 mg	ORAL	ANDA	28 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	0955-1040	TABLET, FILM COATED	75 mg	ORAL	NDA AUTHORIZED GENERIC	27 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	0955-1041	TABLET, FILM COATED	150 mg	ORAL	NDA AUTHORIZED GENERIC	27 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	0955-1042	TABLET, FILM COATED	300 mg	ORAL	NDA AUTHORIZED GENERIC	27 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0955-1045	TABLET, FILM COATED	150 mg	ORAL	NDA AUTHORIZED GENERIC	29 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	0955-1046	TABLET, FILM COATED	300 mg	ORAL	NDA AUTHORIZED GENERIC	29 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	29300-212	TABLET	75 mg	ORAL	ANDA	23 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	29300-213	TABLET	150 mg	ORAL	ANDA	23 sections
Irbesartan	HUMAN PRESCRIPTION DRUG LABEL	1	29300-214	TABLET	300 mg	ORAL	ANDA	23 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	29300-215	TABLET, FILM COATED	150 mg	ORAL	ANDA	26 sections
Irbesartan and Hydrochlorothiazide	HUMAN PRESCRIPTION DRUG LABEL	2	29300-216	TABLET, FILM COATED	300 mg	ORAL	ANDA	26 sections
Irbesartan	Human Prescription Drug Label	1	31722-160	TABLET	75 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	31722-161	TABLET	150 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	31722-162	TABLET	300 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	31722-729	TABLET	75 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	31722-730	TABLET	150 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	31722-731	TABLET	300 mg	ORAL	ANDA	27 sections
Irbesartan	Human Prescription Drug Label	1	33342-047	TABLET	75 mg	ORAL	ANDA	26 sections
Irbesartan	Human Prescription Drug Label	1	33342-048	TABLET	150 mg	ORAL	ANDA	26 sections
Irbesartan	Human Prescription Drug Label	1	33342-049	TABLET	300 mg	ORAL	ANDA	26 sections
Irbesartan and Hydrochlorothiazide	Human Prescription Drug Label	2	33342-057	TABLET, FILM COATED	150 mg	ORAL	ANDA	23 sections
Irbesartan and Hydrochlorothiazide	Human Prescription Drug Label	2	33342-058	TABLET, FILM COATED	300 mg	ORAL	ANDA	23 sections