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

Stem definition	Drug id	CAS RN
histamine-H2-receptor antagonists, cimetidine derivatives	1129	76824-35-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: famotidine agufam amfamox antodine apogastine bestidine brolin cepal digervin dispromil	A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. Computer-aided, structure-based, virtual screening of libraries of compounds against SARS-CoV-2 proteins suggested potential for famotidine to interact with viral proteases in-volved in coronavirus replication. HOWEVER, there is no clinical trial evidence supporting efficacy or safety for treatment of COVID-19. Molecular weight: 337.44 Formula: C8H15N7O2S3 CLOGP: -0.86 LIPINSKI: 1 HAC: 9 HDO: 6 TPSA: 170.83 ALOGS: -3.48 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

famotidine
agufam
amfamox
antodine
apogastine
bestidine
brolin
cepal
digervin
dispromil

A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. Computer-aided, structure-based, virtual screening of libraries of compounds against SARS-CoV-2 proteins suggested potential for famotidine to interact with viral proteases in-volved in coronavirus replication. HOWEVER, there is no clinical trial evidence supporting efficacy or safety for treatment of COVID-19.

Molecular weight: 337.44
Formula: C8H15N7O2S3
CLOGP: -0.86
LIPINSKI: 1
HAC: 9
HDO: 6
TPSA: 170.83
ALOGS: -3.48
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
40	mg	O
40	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	67 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.98 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	42 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	6.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.84 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.80 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Oct. 15, 1986	FDA	VALEANT PHARMS NORTH

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
Drug ineffective	368.70	9.42	764	114797	816481	52417024
Rheumatoid arthritis	314.76	9.42	144	115417	314387	52919118
Contraindicated product administered	237.52	9.42	14	115547	135615	53097890
Synovitis	209.71	9.42	5	115556	107888	53125617
Drug intolerance	200.86	9.42	97	115464	205396	53028109
Joint swelling	158.14	9.42	165	115396	234473	52999032
Hand deformity	147.78	9.42	9	115552	84840	53148665
Treatment failure	146.04	9.42	48	115513	128355	53105150
Systemic lupus erythematosus	138.95	9.42	49	115512	125365	53108140
Glossodynia	134.10	9.42	27	115534	100264	53133241
Therapeutic product effect decreased	127.84	9.42	56	115505	125599	53107906
Arthropathy	126.08	9.42	75	115486	141378	53092127
Hepatic function abnormal	122.06	9.42	256	115305	36643	53196862
Gastrooesophageal reflux disease	119.95	9.42	423	115138	82240	53151265
Pneumonia aspiration	114.65	9.42	239	115322	34062	53199443
Chronic kidney disease	104.92	9.42	266	115295	43104	53190401
Platelet count decreased	104.05	9.42	487	115074	107612	53125893
White blood cell count decreased	103.60	9.42	538	115023	123937	53109568
Maternal exposure during pregnancy	87.32	9.42	126	115435	155513	53077992
Lower respiratory tract infection	85.72	9.42	45	115516	90936	53142569
Wound	85.21	9.42	46	115515	91511	53141994
Pericarditis	84.72	9.42	18	115543	64388	53169117
Drug abuse	78.98	9.42	22	115539	65504	53168001
Toxicity to various agents	75.93	9.42	234	115327	219364	53014141
Alopecia	73.52	9.42	261	115300	234322	52999183
Disseminated intravascular coagulation	65.42	9.42	137	115424	19582	53213923
Hepatic enzyme increased	62.43	9.42	111	115450	126084	53107421
Off label use	61.72	9.42	690	114871	471522	52761983
General physical health deterioration	60.21	9.42	144	115417	146798	53086707
Helicobacter infection	60.21	9.42	7	115554	39062	53194443
Aspartate aminotransferase increased	59.03	9.42	347	115214	83682	53149823
Duodenal ulcer perforation	57.61	9.42	5	115556	35178	53198327
Neutrophil count decreased	56.95	9.42	234	115327	48864	53184641
Product use issue	55.45	9.42	139	115422	139445	53094060
Arthralgia	54.56	9.42	650	114911	439133	52794372
Cholecystitis chronic	53.72	9.42	88	115473	10430	53223075
Musculoskeletal stiffness	52.87	9.42	118	115443	123250	53110255
Flushing	50.52	9.42	293	115268	70307	53163198
Discomfort	49.02	9.42	82	115479	95390	53138115
Blood lactate dehydrogenase increased	48.97	9.42	130	115431	21651	53211854
Liver disorder	48.65	9.42	194	115367	39961	53193544
Swelling	48.35	9.42	231	115330	190874	53042631
Folliculitis	48.08	9.42	6	115555	31703	53201802
Dehydration	46.71	9.42	564	114997	167846	53065659
Butterfly rash	45.69	9.42	29	115532	1078	53232427
Drug hypersensitivity	45.52	9.42	362	115199	264880	52968625
Alanine aminotransferase increased	45.41	9.42	357	115204	94738	53138767
Angioedema	45.27	9.42	196	115365	41880	53191625
Therapeutic product effect incomplete	43.37	9.42	83	115478	91701	53141804
Hepatocellular injury	42.37	9.42	7	115554	29979	53203526
Interstitial lung disease	39.82	9.42	240	115321	58382	53175123
Pain	38.73	9.42	975	114586	587423	52646082
Ill-defined disorder	37.69	9.42	31	115530	49413	53184092
Anaphylactic reaction	36.00	9.42	233	115328	58093	53175412
Upper respiratory tract inflammation	35.17	9.42	37	115524	2837	53230668
Abdominal discomfort	35.06	9.42	308	115253	220754	53012751
Completed suicide	34.97	9.42	167	115394	138034	53095471
Enterocolitis	34.67	9.42	58	115503	6994	53226511
Mobility decreased	34.29	9.42	71	115490	76200	53157305
Torsade de pointes	33.80	9.42	82	115479	12923	53220582
Urticaria	32.96	9.42	444	115117	135441	53098064
Knee arthroplasty	32.51	9.42	16	115545	33553	53199952
Sopor	31.94	9.42	4	115557	21080	53212425
Chest discomfort	30.34	9.42	340	115221	99355	53134150
Cerebral infarction	30.33	9.42	119	115442	24325	53209180
Urinary tract infection	30.16	9.42	706	114855	239197	52994308
Diarrhoea	29.99	9.42	1648	113913	623898	52609607
Gallbladder disorder	29.88	9.42	97	115464	18068	53215437
Periorbital oedema	29.24	9.42	46	115515	5269	53228236
Lip swelling	28.71	9.42	126	115435	27075	53206430
Mental status changes	28.15	9.42	164	115397	39407	53194098
End stage renal disease	28.03	9.42	49	115512	6122	53227383
Exposure during pregnancy	26.52	9.42	160	115401	124700	53108805
Red blood cell sedimentation rate increased	26.23	9.42	14	115547	28043	53205462
Psoriatic arthropathy	26.04	9.42	40	115521	48150	53185355
Overdose	25.63	9.42	133	115428	107603	53125902
Drug resistance	23.50	9.42	7	115554	19955	53213550
Constipation	23.43	9.42	579	114982	197833	53035672
Haemorrhage subcutaneous	23.21	9.42	31	115530	3060	53230445
Impaired healing	23.17	9.42	67	115494	64138	53169367
Febrile neutropenia	23.06	9.42	337	115224	104599	53128906
Pneumonia	22.99	9.42	1090	114471	406079	52827426
Foetal exposure during pregnancy	22.68	9.42	25	115536	34690	53198815
Loss of personal independence in daily activities	22.28	9.42	77	115484	69738	53163767
Decreased appetite	22.11	9.42	616	114945	214358	53019147
Blood alkaline phosphatase increased	21.25	9.42	158	115403	41204	53192301
Renal injury	21.14	9.42	58	115503	9846	53223659
Basophil count decreased	20.64	9.42	8	115553	98	53233407
Acute respiratory failure	20.60	9.42	127	115434	31131	53202374
Hip arthroplasty	20.58	9.42	18	115543	27844	53205661
Lymphocyte stimulation test positive	20.14	9.42	14	115547	607	53232898
Nausea	20.10	9.42	1899	113662	754192	52479313
Dyspepsia	19.82	9.42	256	115305	77344	53156161
Hypoxia	19.80	9.42	196	115365	55484	53178021
Pyrexia	19.80	9.42	1065	114496	402128	52831377
Biliary dyskinesia	19.71	9.42	27	115534	2730	53230775
Infective pulmonary exacerbation of cystic fibrosis	19.65	9.42	61	115500	11095	53222410
Chest pain	19.56	9.42	545	115016	189640	53043865
Ventricular tachycardia	19.30	9.42	83	115478	17679	53215826
Coma	18.92	9.42	211	115350	61572	53171933
Dizziness	18.61	9.42	985	114576	371274	52862231
Acquired haemophilia	18.56	9.42	16	115545	956	53232549
Hospice care	18.51	9.42	41	115520	6089	53227416
Palmar erythema	18.28	9.42	20	115541	1604	53231901
Blood potassium decreased	18.27	9.42	150	115411	40310	53193195
Fibromyalgia	18.19	9.42	43	115518	44032	53189473
Neuropathy peripheral	18.03	9.42	319	115242	102868	53130637
Drug eruption	17.85	9.42	104	115457	24990	53208515
Cytokine release syndrome	17.75	9.42	48	115513	8081	53225424
Serotonin syndrome	17.27	9.42	19	115542	26387	53207118
Rebound acid hypersecretion	17.01	9.42	10	115551	323	53233182
Respiratory alkalosis	16.97	9.42	25	115536	2703	53230802
Premature baby	16.93	9.42	11	115550	19790	53213715
Throat irritation	16.83	9.42	122	115439	31559	53201946
Cholecystitis acute	16.81	9.42	46	115515	7797	53225708
Rheumatoid nodule	16.26	9.42	3	115558	11861	53221644
Hepatotoxicity	16.18	9.42	22	115539	27858	53205647
Full blood count decreased	16.07	9.42	98	115463	23931	53209574
Arthritis	15.95	9.42	117	115444	87181	53146324
Cystitis noninfective	15.92	9.42	14	115547	859	53232646
Erythema multiforme	15.90	9.42	54	115507	10295	53223210
Gastrointestinal disorder	15.79	9.42	122	115439	89882	53143623
Gallbladder injury	15.67	9.42	17	115544	1350	53232155
Gastritis	15.65	9.42	133	115428	36101	53197404
Swelling face	15.62	9.42	191	115370	56977	53176528
Abdominal distension	15.51	9.42	251	115310	79539	53153966
Lupus hepatitis	15.49	9.42	5	115556	34	53233471
Cholinergic syndrome	15.44	9.42	10	115551	385	53233120
Injection site reaction	15.29	9.42	58	115503	51108	53182397
Protein total decreased	15.19	9.42	37	115524	5846	53227659
Sepsis	15.15	9.42	420	115141	146009	53087496
Muscle spasticity	15.13	9.42	10	115551	17828	53215677
Throat tightness	15.11	9.42	91	115470	22125	53211380
Drug interaction	15.01	9.42	361	115200	218968	53014537
Injection site pain	15.00	9.42	165	115396	113226	53120279
Device expulsion	14.93	9.42	26	115535	29787	53203718
Anaphylactoid reaction	14.88	9.42	28	115533	3703	53229802
Hereditary angioedema	14.75	9.42	38	115523	6215	53227290
Hypokalaemia	14.65	9.42	292	115269	96225	53137280
Blister	14.65	9.42	105	115456	78648	53154857
Haematocrit decreased	14.56	9.42	134	115427	37197	53196308
Cholestasis	14.39	9.42	25	115536	28670	53204835
Somnolence	14.37	9.42	470	115091	167264	53066241
Blood pressure fluctuation	14.32	9.42	35	115526	35435	53198070
White blood cell count increased	14.19	9.42	158	115403	46087	53187418
Amino acid level decreased	14.17	9.42	5	115556	46	53233459
Red blood cell count decreased	14.06	9.42	129	115432	35774	53197731
Cholelithiasis	13.99	9.42	143	115418	40821	53192684
Burkholderia test positive	13.92	9.42	6	115555	98	53233407
Weight increased	13.91	9.42	337	115224	204230	53029275
Injection site bruising	13.79	9.42	39	115522	37607	53195898
Congenital neuropathy	13.77	9.42	4	115557	18	53233487
Disease progression	13.73	9.42	303	115258	101617	53131888
Intentional self-injury	13.64	9.42	21	115540	25263	53208242
Victim of chemical submission	13.54	9.42	8	115553	261	53233244
Hyperuricaemia	13.51	9.42	33	115528	5223	53228282
Small intestinal obstruction	13.47	9.42	73	115488	17074	53216431
Tubulointerstitial nephritis	13.47	9.42	71	115490	16433	53217072
Blood magnesium decreased	13.45	9.42	56	115505	11758	53221747
Lactic acidosis	13.35	9.42	39	115522	37214	53196291
Irritable bowel syndrome	13.33	9.42	49	115512	43583	53189922
Granulocytopenia	13.33	9.42	34	115527	5526	53227979
Dyspnoea	13.31	9.42	1457	114104	584775	52648730
Breast adenoma	13.22	9.42	5	115556	57	53233448
Medication error	13.08	9.42	38	115523	36327	53197178
Allergy test positive	13.03	9.42	9	115552	386	53233119
Pyuria	12.99	9.42	18	115543	1840	53231665
Cytomegalovirus enterocolitis	12.92	9.42	11	115550	646	53232859
Therapeutic response decreased	12.90	9.42	56	115505	47513	53185992
Brain natriuretic peptide increased	12.74	9.42	31	115530	4894	53228611
Putamen haemorrhage	12.72	9.42	7	115554	199	53233306
Ileus	12.67	9.42	65	115496	14890	53218615
Hypoparathyroidism	12.41	9.42	11	115550	682	53232823
Laboratory test abnormal	12.40	9.42	93	115468	24316	53209189
Asteatosis	12.36	9.42	5	115556	69	53233436
Swollen tongue	12.34	9.42	112	115449	30968	53202537
Blood bilirubin increased	12.33	9.42	125	115436	35605	53197900
Extrapyramidal disorder	11.87	9.42	6	115555	12396	53221109
Gastrointestinal haemorrhage	11.85	9.42	242	115319	80088	53153417
Xanthogranuloma	11.81	9.42	3	115558	7	53233498
Impaired work ability	11.81	9.42	8	115553	14082	53219423
Stress cardiomyopathy	11.71	9.42	43	115518	8519	53224986
Blood urea increased	11.71	9.42	97	115464	26134	53207371
Osteoarthritis	11.69	9.42	97	115464	70389	53163116
Neurological examination abnormal	11.64	9.42	7	115554	236	53233269
Infection	11.62	9.42	284	115277	171921	53061584
Atrioventricular block complete	11.60	9.42	41	115520	7974	53225531
Condition aggravated	11.53	9.42	526	115035	296608	52936897
Back pain	11.51	9.42	619	114942	233628	52999877
Therapy non-responder	11.47	9.42	61	115500	49059	53184446
Feeling hot	11.43	9.42	139	115422	41405	53192100
Plasma cell myeloma	11.41	9.42	156	115405	47718	53185787
Blood creatine phosphokinase MB increased	11.39	9.42	14	115547	1272	53232233
Liver injury	11.32	9.42	19	115542	22084	53211421
Haemoglobin decreased	11.31	9.42	383	115178	136924	53096581
Hypoalbuminaemia	11.04	9.42	50	115511	10886	53222619
Intraductal papillary breast neoplasm	11.03	9.42	3	115558	10	53233495
Contusion	11.02	9.42	171	115390	110561	53122944
Musculoskeletal pain	10.94	9.42	107	115454	75093	53158412
Chills	10.92	9.42	301	115260	104547	53128958
Anaemia	10.91	9.42	717	114844	276001	52957504
Coronary artery dissection	10.90	9.42	11	115550	803	53232702
Hyperlipidaemia	10.86	9.42	76	115485	19439	53214066
Ovarian cancer recurrent	10.85	9.42	13	115548	1150	53232355
Pulmonary hypertension	10.83	9.42	126	115435	37144	53196361
Restless arm syndrome	10.79	9.42	4	115557	43	53233462
Pityriasis lichenoides et varioliformis acuta	10.55	9.42	4	115557	46	53233459
Pupils unequal	10.46	9.42	14	115547	1385	53232120
Allergic transfusion reaction	10.39	9.42	4	115557	48	53233457
Deep vein thrombosis	10.39	9.42	244	115317	82669	53150836
Dermatitis acneiform	10.37	9.42	27	115534	4443	53229062
Vascular resistance systemic decreased	10.33	9.42	5	115556	108	53233397
Reticulocyte percentage increased	10.24	9.42	3	115558	14	53233491
Myocarditis infectious	10.24	9.42	3	115558	14	53233491
Inflammation	10.23	9.42	77	115484	57059	53176446
Blood albumin decreased	10.17	9.42	60	115501	14482	53219023
Tinea pedis	10.10	9.42	14	115547	1431	53232074
Lymphocyte count decreased	10.09	9.42	99	115462	27953	53205552
Ovarian cancer	10.09	9.42	33	115528	6169	53227336
Therapeutic hypothermia	10.07	9.42	3	115558	15	53233490
Mean arterial pressure increased	10.07	9.42	3	115558	15	53233490
Pyelonephritis acute	10.03	9.42	27	115534	4532	53228973
Seasonal allergy	10.01	9.42	62	115499	15223	53218282
Haemolytic anaemia	10.00	9.42	47	115514	10392	53223113
COVID-19	9.97	9.42	123	115438	36765	53196740
Hypoaesthesia	9.97	9.42	367	115194	132628	53100877
Neuroleptic malignant syndrome	9.86	9.42	7	115554	12026	53221479
Hypergeusia	9.76	9.42	3	115558	17	53233488
Histamine level increased	9.76	9.42	3	115558	17	53233488

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
Drug ineffective	148.93	9.96	478	80717	382999	32049332
Hepatic function abnormal	148.81	9.96	339	80856	44501	32387830
Drug abuse	119.45	9.96	27	81168	80216	32352115
Platelet count decreased	100.58	9.96	557	80638	114034	32318297
Alanine aminotransferase increased	97.96	9.96	422	80773	78057	32354274
Liver disorder	92.70	9.96	228	80967	31426	32400905
Aspartate aminotransferase increased	92.15	9.96	369	80826	66060	32366271
Toxicity to various agents	82.82	9.96	203	80992	177838	32254493
Disseminated intravascular coagulation	73.30	9.96	172	81023	23004	32409327
White blood cell count decreased	73.21	9.96	433	80762	90765	32341566
Off label use	71.58	9.96	460	80735	305860	32126471
Completed suicide	70.69	9.96	76	81119	92441	32339890
General physical health deterioration	66.60	9.96	116	81079	115143	32317188
Drug interaction	55.95	9.96	318	80877	217867	32214464
Neutrophil count decreased	55.37	9.96	249	80946	46890	32385441
Chronic kidney disease	46.82	9.96	211	80984	39764	32392567
Blood lactate dehydrogenase increased	45.76	9.96	139	81056	21666	32410665
Rheumatoid arthritis	43.29	9.96	29	81166	44515	32387816
Drug resistance	40.17	9.96	5	81190	22960	32409371
Interstitial lung disease	38.41	9.96	286	80909	64715	32367616
Treatment failure	37.39	9.96	26	81169	39137	32393194
Upper respiratory tract inflammation	34.92	9.96	33	81162	1924	32430407
Blood alkaline phosphatase increased	33.52	9.96	164	81031	31968	32400363
Cerebral infarction	33.26	9.96	147	81048	27467	32404864
Foetal exposure during pregnancy	31.44	9.96	34	81161	41267	32391064
Lymphocyte stimulation test positive	30.86	9.96	22	81173	859	32431472
Product use in unapproved indication	30.71	9.96	113	81082	87091	32345240
Overdose	29.90	9.96	114	81081	86963	32345368
Infusion related reaction	29.45	9.96	205	80990	45394	32386937
Pyrexia	27.39	9.96	1016	80179	318952	32113379
Pneumonitis	27.39	9.96	148	81047	29986	32402345
Contraindicated product administered	25.37	9.96	8	81187	19068	32413263
Psoriasis	25.20	9.96	48	81147	46075	32386256
Decreased appetite	25.01	9.96	551	80644	160262	32272069
Therapeutic product effect incomplete	24.40	9.96	41	81154	41300	32391031
End stage renal disease	23.63	9.96	58	81137	7979	32424352
Drug intolerance	23.51	9.96	57	81138	50178	32382153
Haematocrit decreased	22.64	9.96	146	81049	31516	32400815
Pneumonia	22.28	9.96	1092	80103	354160	32078171
Blood creatine phosphokinase MB increased	22.13	9.96	26	81169	1951	32430380
Blood bilirubin increased	21.97	9.96	169	81026	38615	32393716
Acute respiratory failure	21.49	9.96	134	81061	28594	32403737
Pneumonia bacterial	21.26	9.96	67	81128	10649	32421682
Rash	20.95	9.96	677	80518	208656	32223675
Blood urea increased	20.20	9.96	144	81051	32129	32400202
Blood albumin decreased	19.60	9.96	74	81121	12879	32419452
Enterocolitis	19.52	9.96	51	81144	7289	32425042
Erythema multiforme	19.50	9.96	58	81137	8934	32423397
Hypoxia	19.22	9.96	207	80988	51925	32380406
Lactic acidosis	19.11	9.96	34	81161	33502	32398829
Urticaria	18.96	9.96	230	80965	59384	32372947
Intentional product misuse	18.42	9.96	39	81156	36012	32396319
Cytokine release syndrome	17.80	9.96	74	81121	13461	32418870
Pneumonia aspiration	17.36	9.96	168	81027	40988	32391343
Constipation	17.16	9.96	425	80770	125948	32306383
Human ehrlichiosis	16.60	9.96	9	81186	214	32432117
Cholangitis acute	16.47	9.96	15	81180	834	32431497
Mast cell activation syndrome	16.33	9.96	8	81187	153	32432178
Wound secretion	16.22	9.96	26	81169	2621	32429710
Intentional product use issue	15.99	9.96	53	81142	42158	32390173
Hepatocellular injury	15.99	9.96	24	81171	25294	32407037
Ventricular tachycardia	15.97	9.96	114	81081	25442	32406889
Blood pressure ambulatory increased	15.91	9.96	6	81189	58	32432273
PO2 increased	15.85	9.96	13	81182	627	32431704
Rash maculo-papular	15.44	9.96	29	81166	27993	32404338
Psychotic disorder	15.35	9.96	21	81174	22999	32409332
Febrile neutropenia	15.32	9.96	399	80796	119167	32313164
Intentional overdose	15.23	9.96	53	81142	41548	32390783
Anaphylactic reaction	15.19	9.96	128	81067	30044	32402287
Joint swelling	15.12	9.96	72	81123	51663	32380668
Gastrointestinal mucosal necrosis	15.11	9.96	8	81187	181	32432150
Glossectomy	14.99	9.96	3	81192	0	32432331
Catheter site haemorrhage	14.84	9.96	23	81172	2252	32430079
Infective pulmonary exacerbation of cystic fibrosis	14.84	9.96	52	81143	8727	32423604
CADASIL	14.40	9.96	6	81189	77	32432254
Ultrasound skull abnormal	14.40	9.96	6	81189	77	32432254
Torsade de pointes	14.38	9.96	46	81149	7369	32424962
Cardiac autonomic neuropathy	14.20	9.96	6	81189	80	32432251
Magnetic resonance imaging spinal abnormal	14.13	9.96	6	81189	81	32432250
Lower respiratory tract infection	13.83	9.96	33	81162	29210	32403121
Visual evoked potentials abnormal	13.81	9.96	6	81189	86	32432245
Polyneuropathy	13.67	9.96	8	81187	13207	32419124
Aplastic anaemia	13.63	9.96	45	81150	7328	32425003
Sepsis	13.44	9.96	504	80691	158330	32274001
Convulsive threshold lowered	13.44	9.96	11	81184	529	32431802
Gastrooesophageal reflux disease	13.30	9.96	139	81056	34599	32397732
Blood pressure decreased	13.29	9.96	190	81005	50890	32381441
Drug dependence	13.21	9.96	24	81171	23460	32408871
Convulsions local	13.21	9.96	4	81191	18	32432313
Hypertensive crisis	13.04	9.96	3	81192	8814	32423517
Protein total decreased	12.99	9.96	35	81160	5095	32427236
Hiccups	12.93	9.96	54	81141	9841	32422490
Pneumonia staphylococcal	12.85	9.96	26	81169	3142	32429189
Burkholderia test positive	12.81	9.96	10	81185	449	32431882
Anal erosion	12.55	9.96	4	81191	22	32432309
Central nervous system inflammation	12.43	9.96	6	81189	111	32432220
Respiratory failure	12.40	9.96	353	80842	106829	32325502
Supine hypertension	12.39	9.96	9	81186	362	32431969
Renal impairment	12.39	9.96	309	80886	91663	32340668
Amino acid level decreased	12.38	9.96	5	81190	59	32432272
Cerebral microangiopathy	11.98	9.96	7	81188	193	32432138
Eczema asteatotic	11.98	9.96	7	81188	193	32432138
Ventricular flutter	11.87	9.96	5	81190	66	32432265
Double stranded DNA antibody positive	11.78	9.96	6	81189	125	32432206
Arthropathy	11.76	9.96	24	81171	22465	32409866
Sputum retention	11.76	9.96	10	81185	507	32431824
Cardiogenic shock	11.73	9.96	21	81174	20641	32411690
Nipple swelling	11.70	9.96	3	81192	6	32432325
Post procedural haematoma	11.58	9.96	17	81178	1587	32430744
Amino acid level increased	11.55	9.96	9	81186	403	32431928
Conduction disorder	11.45	9.96	19	81176	1971	32430360
Jaundice hepatocellular	11.42	9.96	5	81190	73	32432258
Aggression	11.40	9.96	55	81140	39334	32392997
Acute kidney injury	11.40	9.96	608	80587	292860	32139471
Saccadic eye movement	11.25	9.96	6	81189	138	32432193
White blood cell count increased	11.17	9.96	155	81040	41247	32391084
Ejaculation delayed	11.11	9.96	7	81188	222	32432109
Stomatitis	11.01	9.96	151	81044	40078	32392253
Progressive multifocal leukoencephalopathy	11.00	9.96	5	81190	9526	32422805
Death	10.96	9.96	815	80380	381702	32050629
Product use issue	10.90	9.96	82	81113	52695	32379636
Cholestasis	10.90	9.96	33	81162	27000	32405331
Granulocyte count decreased	10.88	9.96	11	81184	697	32431634
Viral rash	10.84	9.96	5	81190	83	32432248
Laboratory test abnormal	10.71	9.96	83	81112	19004	32413327
Musculoskeletal stiffness	10.70	9.96	56	81139	39208	32393123
Hypoalbuminaemia	10.69	9.96	58	81137	11764	32420567
Haemorrhagic diathesis	10.60	9.96	23	81172	2919	32429412
Inappropriate schedule of product administration	10.54	9.96	69	81126	45756	32386575
Granulocytopenia	10.51	9.96	38	81157	6477	32425854
Blood pH decreased	10.50	9.96	20	81175	2313	32430018
Sputum culture positive	10.44	9.96	18	81177	1926	32430405
Stevens-Johnson syndrome	10.30	9.96	81	81114	18628	32413703
Psoriatic arthropathy	10.27	9.96	18	81177	17842	32414489
Gastrointestinal tract mucosal pigmentation	10.27	9.96	8	81187	358	32431973
Depressed level of consciousness	10.25	9.96	151	81044	40696	32391635
Hepatitis fulminant	10.23	9.96	28	81167	4115	32428216
Oral pruritus	10.15	9.96	7	81188	259	32432072
Pancreatic enlargement	10.05	9.96	5	81190	99	32432232
Urine osmolarity decreased	9.99	9.96	4	81191	46	32432285
Accidental exposure to product	9.96	9.96	8	81187	11194	32421137
Aortic rupture	9.96	9.96	5	81190	101	32432230

Pharmacologic Action:

Source	Code	Description
ATC	A02BA03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) H2-receptor antagonists
ATC	A02BA53	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) H2-receptor antagonists
FDA MoA	N0000000151	Histamine H2 Receptor Antagonists
CHEBI has role	CHEBI:37961	H2-receptor blockers
CHEBI has role	CHEBI:49201	anti-ulcer agents
CHEBI has role	CHEBI:50183	cytochrome P450 inhibitor
MeSH PA	D000897	Anti-Ulcer Agents
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006635	Histamine H2 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
FDA EPC	N0000175784	Histamine-2 Receptor Antagonist

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Heartburn	indication	16331000
Erosive esophagitis	indication	40719004
Duodenal ulcer disease	indication	51868009	DOID:1724
Zollinger-Ellison syndrome	indication	53132006	DOID:0050782
Peptic reflux disease	indication	57643001
Indigestion	indication	162031009
Gastroesophageal reflux disease	indication	235595009	DOID:8534
Gastric ulcer	indication	397825006	DOID:10808
Dyspepsia Prevention	indication
Maintenance of Healing Duodenal Ulcer	indication
Heartburn Prevention	indication
Upper gastrointestinal hemorrhage	off-label use	37372002
Prevention of Stress Ulcer	off-label use
Constipation	contraindication	14760008	DOID:2089
Sarcoidosis	contraindication	31541009	DOID:11335
Dehydration	contraindication	34095006
Diarrhea	contraindication	62315008
Hypercalcemia	contraindication	66931009	DOID:12678
Hyperparathyroidism	contraindication	66999008	DOID:13543
Kidney disease	contraindication	90708001	DOID:557
Kidney stone	contraindication	95570007
Impaired renal function disorder	contraindication	197663003
Osteolysis	contraindication	203522001
Disease of liver	contraindication	235856003	DOID:409
Malignant tumor of stomach	contraindication	363349007	DOID:10534

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.84	acidic
pKa2	12.0	acidic
pKa3	6.97	Basic
pKa4	6.37	Basic
pKa5	2.56	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
26.6MG;800MG	DUEXIS	HORIZON	N022519	April 23, 2011	RX	TABLET	ORAL	8067451	July 18, 2026	RELIEF OF SIGNS AND SYMPTOMS OF RHEUMATOID ARTHRITIS AND OSTEOARTHRITIS AND TO DECREASE RISK OF DEVELOPING UPPER GASTROINTESTINAL ULCERS IN PATIENTS WHO ARE TAKING IBUPROFEN FOR THOSE INDICATIONS
26.6MG;800MG	DUEXIS	HORIZON	N022519	April 23, 2011	RX	TABLET	ORAL	8501228	July 18, 2026	RELIEF OF SIGNS AND SYMPTOMS OF RHEUMATOID ARTHRITIS AND OSTEOARTHRITIS AND TO DECREASE RISK OF DEVELOPING UPPER GASTROINTESTINAL ULCERS IN PATIENTS WHO ARE TAKING IBUPROFEN FOR THOSE INDICATIONS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN	ANTAGONIST	Kd	7.93	WOMBAT-PK	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	7.24	CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	6.04	CHEMBL
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN		Ki	6.03	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	6.90	CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	7.34	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	5.84	CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	5.27	CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	8.52	CHEMBL
Carbonic anhydrase 6	Enzyme	P23280	CAH6_HUMAN		Ki	7.01	CHEMBL
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		Ki	6.17	CHEMBL
Carbonic anhydrase 13	Enzyme	Q8N1Q1	CAH13_HUMAN		Ki	6.77	CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	4.44	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	6.12	CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	4.44	CHEMBL
Heat shock protein HSP 90-alpha	Cytosolic other	P07900	HS90A_HUMAN		IC50	5.30	WOMBAT-PK
Solute carrier family 22 member 3	Transporter	O75751	S22A3_HUMAN		IC50	4.97	CHEMBL
Histamine H2 receptor	GPCR		HRH2_CAVPO		Kd	7	CHEMBL

External reference:

ID	Source
4017970	VUID
N0000146320	NUI
D00318	KEGG_DRUG
4017970	VANDF
C0015620	UMLSCUI
CHEBI:4975	CHEBI
FO9	PDB_CHEM_ID
CHEMBL902	ChEMBL_ID
DB00927	DRUGBANK_ID
D015738	MESH_DESCRIPTOR_UI
5353622	PUBCHEM_CID
7074	IUPHAR_LIGAND_ID
5217	INN_ID
5QZO15J2Z8	UNII
4278	RXNORM
41331	MMSL
4713	MMSL
d00141	MMSL
003417	NDDF
387211002	SNOMEDCT_US
39128000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ibuprofen and famotidine	HUMAN PRESCRIPTION DRUG LABEL	2	0093-8107	TABLET, FILM COATED	26.60 mg	ORAL	ANDA	28 sections
Good Sense Dual Action Complete	HUMAN OTC DRUG LABEL	3	0113-0032	TABLET, CHEWABLE	10 mg	ORAL	ANDA	15 sections
good sense acid reducer	HUMAN OTC DRUG LABEL	1	0113-0141	TABLET, FILM COATED	10 mg	ORAL	ANDA	15 sections
Good Sense Acid Reducer	HUMAN OTC DRUG LABEL	1	0113-0194	TABLET, FILM COATED	20 mg	ORAL	ANDA	15 sections
basic care acid reducer	HUMAN OTC DRUG LABEL	1	0113-7141	TABLET, FILM COATED	10 mg	ORAL	ANDA	15 sections
Basic Care famotidine	HUMAN OTC DRUG LABEL	1	0113-7194	TABLET, FILM COATED	20 mg	ORAL	ANDA	14 sections
basic care dual action complete	HUMAN OTC DRUG LABEL	3	0113-7321	TABLET, CHEWABLE	10 mg	ORAL	ANDA	15 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0172-5728	TABLET, FILM COATED	20 mg	ORAL	ANDA	25 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0172-5729	TABLET, FILM COATED	40 mg	ORAL	ANDA	25 sections
Pepcid	HUMAN PRESCRIPTION DRUG LABEL	1	0187-4420	TABLET, FILM COATED	20 mg	ORAL	ANDA	25 sections
Pepcid	HUMAN PRESCRIPTION DRUG LABEL	1	0187-4440	TABLET, FILM COATED	40 mg	ORAL	ANDA	25 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0338-5197	INJECTION, SOLUTION	20 mg	INTRAVENOUS	ANDA	22 sections
Acid ControllerOriginal Strength	HUMAN OTC DRUG LABEL	1	0363-0141	TABLET, FILM COATED	10 mg	ORAL	ANDA	15 sections
Acid Reducer Complete	HUMAN OTC DRUG LABEL	3	0363-0511	TABLET, CHEWABLE	10 mg	ORAL	ANDA	15 sections
Acid Controller	HUMAN OTC DRUG LABEL	1	0363-0701	TABLET, FILM COATED	20 mg	ORAL	ANDA	15 sections
Acid Reducer Complete	HUMAN OTC DRUG LABEL	3	0363-0713	TABLET, CHEWABLE	10 mg	ORAL	ANDA	15 sections
Famotidine	Human OTC Drug Label	1	0363-1899	TABLET, FILM COATED	20 mg	ORAL	ANDA	16 sections
Famotidine	Human OTC Drug Label	1	0363-4400	TABLET, FILM COATED	10 mg	ORAL	ANDA	16 sections
Famotidine	Human OTC Drug Label	1	0363-5300	TABLET, FILM COATED	20 mg	ORAL	ANDA	16 sections
Rugby Famotidine	HUMAN OTC DRUG LABEL	1	0536-1298	TABLET, FILM COATED	20 mg	ORAL	ANDA	15 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-4582	TABLET, FILM COATED	20 mg	ORAL	ANDA	20 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8301	TABLET, FILM COATED	40 mg	ORAL	ANDA	20 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6021	INJECTION	10 mg	INTRAVENOUS	ANDA	22 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6022	INJECTION	10 mg	INTRAVENOUS	ANDA	22 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6023	INJECTION	10 mg	INTRAVENOUS	ANDA	22 sections
heartburn relieforiginal strength	HUMAN OTC DRUG LABEL	1	0904-5529	TABLET	10 mg	ORAL	ANDA	15 sections
Major Heartburn ReliefMaximum Strength	HUMAN OTC DRUG LABEL	1	0904-5780	TABLET, FILM COATED	20 mg	ORAL	ANDA	15 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7193	TABLET, FILM COATED	20 mg	ORAL	ANDA	24 sections
Famotidine	HUMAN PRESCRIPTION DRUG LABEL	1	10544-481	TABLET	20 mg	ORAL	ANDA	21 sections
up and up famotidine complete	HUMAN OTC DRUG LABEL	3	11673-007	TABLET, CHEWABLE	10 mg	ORAL	ANDA	15 sections