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

Stem definition	Drug id	CAS RN
	1599	53179-11-6

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: loperamide loperamide hydrochloride imodium loperamide HCl

One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. Molecular weight: 477.05 Formula: C29H33ClN2O2 CLOGP: 4.66 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 43.78 ALOGS: -5.74 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1.40 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.48 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1976	FDA	MCNEIL CONS

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
Diarrhoea	1551.34	10.43	3088	77185	622458	52646335
Dehydration	289.80	10.43	723	79550	167687	53101106
Rheumatoid arthritis	205.05	10.43	109	80164	314422	52954371
Pneumonia viral	183.25	10.43	121	80152	6991	53261802
Maternal exposure during pregnancy	165.27	10.43	20	80253	155619	53113174
Drug ineffective	151.16	10.43	676	79597	816569	52452224
Vomiting	144.05	10.43	1255	79018	495884	52772909
Pneumonia aspiration	132.28	10.43	207	80066	34094	53234699
Drug abuse	131.56	10.43	299	79974	65227	53203566
Systemic lupus erythematosus	126.27	10.43	19	80254	125395	53143398
Torsade de pointes	122.74	10.43	123	80150	12882	53255911
Hypokalaemia	121.57	10.43	370	79903	96147	53172646
Soft tissue disorder	115.43	10.43	75	80198	4215	53264578
Ventricular tachycardia	113.71	10.43	137	80136	17625	53251168
Decreased appetite	112.69	10.43	628	79645	214346	53054447
Coma	102.61	10.43	262	80011	61521	53207272
Pain	98.88	10.43	503	79770	587895	52680898
Hypomagnesaemia	97.42	10.43	151	80122	24660	53244133
Electrocardiogram QT prolonged	96.60	10.43	242	80031	56161	53212632
Gastrooesophageal reflux disease	95.87	10.43	308	79965	82355	53186438
Colitis	95.20	10.43	200	80073	41352	53227441
Oral pain	91.27	10.43	153	80120	26684	53242109
Abdominal pain	89.48	10.43	675	79598	255228	53013565
Hypomania	88.48	10.43	67	80206	4815	53263978
Contraindicated product administered	85.32	10.43	49	80224	135580	53133213
Jaundice cholestatic	85.26	10.43	69	80204	5465	53263328
Nausea	85.00	10.43	1601	78672	754490	52514303
Glossodynia	84.74	10.43	23	80250	100268	53168525
Gastrointestinal stoma complication	79.14	10.43	42	80231	1614	53267179
Small intestinal obstruction	78.27	10.43	112	80161	17035	53251758
Pericarditis	69.01	10.43	8	80265	64398	53204395
Intestinal obstruction	68.95	10.43	141	80132	28600	53240193
Completed suicide	65.19	10.43	67	80206	138134	53130659
Drug hypersensitivity	63.98	10.43	196	80077	265046	53003747
Neuropathy peripheral	63.27	10.43	315	79958	102872	53165921
Exposure during pregnancy	63.00	10.43	57	80216	124803	53143990
Drug intolerance	61.69	10.43	136	80137	205357	53063436
Arthropathy	59.73	10.43	75	80198	141378	53127415
Blood magnesium increased	59.59	10.43	44	80229	3043	53265750
Schizophrenia	58.90	10.43	75	80198	10204	53258589
Presbyacusis	58.55	10.43	43	80230	2949	53265844
Infusion related reaction	58.54	10.43	90	80183	155867	53112926
Pleural thickening	55.93	10.43	40	80233	2632	53266161
Mucosal inflammation	54.74	10.43	165	80108	42619	53226174
Neutropenic sepsis	54.52	10.43	87	80186	14562	53254231
Colitis microscopic	54.28	10.43	60	80213	7034	53261759
Discomfort	53.87	10.43	39	80234	95433	53173360
Somnolence	52.77	10.43	432	79841	167302	53101491
Deafness neurosensory	52.24	10.43	49	80224	4729	53264064
Weight decreased	51.85	10.43	561	79712	234387	53034406
Intentional overdose	51.44	10.43	219	80054	66986	53201807
Pleural fibrosis	51.43	10.43	43	80230	3565	53265228
Blood magnesium decreased	49.34	10.43	74	80199	11740	53257053
Lethargy	49	10.43	185	80088	53575	53215218
Constipation	48.61	10.43	484	79789	197928	53070865
Therapeutic product effect decreased	47.64	10.43	72	80201	125583	53143210
Brain stem glioma	46.59	10.43	15	80258	152	53268641
Wound	45.93	10.43	42	80231	91515	53177278
Febrile neutropenia	44.92	10.43	291	79982	104645	53164148
Psoriatic arthropathy	44.76	10.43	9	80264	48181	53220612
Segmental diverticular colitis	43.74	10.43	14	80259	139	53268654
Respiration abnormal	42.79	10.43	47	80226	5471	53263322
Pedal pulse abnormal	42.79	10.43	14	80259	150	53268643
Swelling	42.72	10.43	146	80127	190959	53077834
Calcium ionised decreased	42.67	10.43	16	80257	263	53268530
Injection site pain	42	10.43	66	80207	113325	53155468
Injection site erythema	41.73	10.43	33	80240	77216	53191577
Malignant neoplasm progression	41.45	10.43	215	80058	71326	53197467
Psoriasis	41.30	10.43	42	80231	87047	53181746
Flatulence	40.74	10.43	122	80151	31395	53237398
Injection site pruritus	40.26	10.43	7	80266	41582	53227211
Electrocardiogram QRS complex prolonged	39.57	10.43	46	80227	5696	53263097
Nail dystrophy	39.53	10.43	20	80253	695	53268098
Helicobacter infection	39.11	10.43	6	80267	39063	53229730
Knee arthroplasty	39.05	10.43	3	80270	33566	53235227
Arthralgia	38.88	10.43	449	79824	439334	52829459
Headache	38.00	10.43	574	79699	536247	52732546
Clostridium difficile infection	37.99	10.43	110	80163	27783	53241010
Epigastric discomfort	36.89	10.43	46	80227	6127	53262666
Accidental overdose	36.59	10.43	92	80181	21387	53247406
Long QT syndrome	36.42	10.43	34	80239	3262	53265531
Device related infection	36.13	10.43	95	80178	22691	53246102
Treatment failure	36.07	10.43	88	80185	128315	53140478
Total lung capacity increased	35.48	10.43	20	80253	867	53267926
Herpes zoster	35.26	10.43	211	80062	73808	53194985
Pouchitis	34.65	10.43	16	80257	453	53268340
Blood potassium decreased	34.23	10.43	136	80137	40324	53228469
Sinusitis	34.22	10.43	134	80139	168430	53100363
Device expulsion	33.76	10.43	3	80270	29810	53238983
Appetite disorder	33.24	10.43	45	80228	6498	53262295
Pneumonia	33.14	10.43	824	79449	406345	52862448
Brugada syndrome	33.08	10.43	14	80259	320	53268473
Blood bilirubin increased	32.59	10.43	123	80150	35607	53233186
Gallbladder polyp	32.47	10.43	18	80255	755	53268038
Drug interaction	31.49	10.43	197	80076	219132	53049661
Red blood cell sedimentation rate increased	31.29	10.43	3	80270	28054	53240739
Cholelithiasis	30.96	10.43	133	80140	40831	53227962
Arteriovenous fistula occlusion	30.89	10.43	14	80259	379	53268414
Disease progression	30.69	10.43	260	80013	101660	53167133
Joint swelling	30.55	10.43	217	80056	234421	53034372
Frequent bowel movements	30.28	10.43	67	80206	14345	53254448
Injection site reaction	30.05	10.43	20	80253	51146	53217647
Blue toe syndrome	29.91	10.43	14	80259	409	53268384
Post procedural diarrhoea	29.78	10.43	11	80262	173	53268620
Stoma complication	29.76	10.43	13	80260	322	53268471
Hypersensitivity	29.33	10.43	191	80082	210474	53058319
Injection site bruising	29.32	10.43	10	80263	37636	53231157
Syncope	28.76	10.43	276	79997	111717	53157076
Hip arthroplasty	28.53	10.43	4	80269	27858	53240935
Wrong technique in product usage process	28.40	10.43	29	80244	60003	53208790
Dry skin	28.24	10.43	140	80133	45620	53223173
Intentional self-injury	28.19	10.43	93	80180	25191	53243602
Impaired healing	28.19	10.43	33	80240	64172	53204621
Ventricular arrhythmia	28.08	10.43	31	80242	3629	53265164
Conduction disorder	27.95	10.43	21	80252	1491	53267302
Drug use disorder	27.75	10.43	29	80244	3190	53265603
Rhinorrhoea	27.64	10.43	156	80117	53422	53215371
Liver function test abnormal	27.52	10.43	144	80129	47927	53220866
Therapeutic response decreased	27.39	10.43	19	80254	47550	53221243
Gastroenteritis radiation	27.27	10.43	14	80259	502	53268291
Heart sounds	26.79	10.43	14	80259	521	53268272
Feeding intolerance	26.64	10.43	14	80259	527	53268266
Brain injury	26.57	10.43	40	80233	6365	53262428
No adverse event	26.41	10.43	13	80260	39252	53229541
Weight increased	26.23	10.43	190	80083	204377	53064416
Premature delivery	26.15	10.43	4	80269	26100	53242693
Therapeutic reaction time decreased	25.55	10.43	19	80254	1328	53267465
Folliculitis	25.44	10.43	8	80265	31701	53237092
Bile acid malabsorption	25.14	10.43	10	80263	194	53268599
Urticaria	25.11	10.43	112	80161	135773	53133020
Clostridium difficile colitis	25.06	10.43	76	80197	19689	53249104
Anal abscess	24.65	10.43	30	80243	3898	53264895
Gastrointestinal stoma output increased	24.64	10.43	10	80263	205	53268588
Pulmonary embolism	24.61	10.43	272	80001	114170	53154623
Mydriasis	24.19	10.43	53	80220	11273	53257520
Thymus disorder	24.11	10.43	10	80263	217	53268576
Foetal exposure during pregnancy	24.11	10.43	11	80262	34704	53234089
Unresponsive to stimuli	24.09	10.43	107	80166	33319	53235474
Fatigue	24.01	10.43	1335	78938	729171	52539622
Product quality issue	23.80	10.43	13	80260	37010	53231783
Crohn's disease	23.63	10.43	39	80234	6711	53262082
Overdose	23.59	10.43	257	80016	107479	53161314
Skin fissures	23.50	10.43	45	80228	8700	53260093
Stomatitis	23.30	10.43	238	80035	97920	53170873
Injection site swelling	23.28	10.43	18	80255	42610	53226183
Ill-defined disorder	23.26	10.43	24	80249	49420	53219373
Multiple sclerosis relapse	23.18	10.43	20	80253	44833	53223960
Pneumonitis	23.12	10.43	100	80173	30788	53238005
Hypophagia	22.82	10.43	100	80173	30962	53237831
Anaemia	22.76	10.43	561	79712	276157	52992636
Off label use	22.51	10.43	540	79733	471672	52797121
Leukopenia	22.42	10.43	188	80085	73275	53195518
Pulmonary thrombosis	22.38	10.43	42	80231	7999	53260794
Pyrexia	22.12	10.43	777	79496	402416	52866377
Prolonged expiration	21.95	10.43	13	80260	619	53268174
Vascular device infection	21.84	10.43	30	80243	4391	53264402
Ear infection	21.75	10.43	6	80267	25894	53242899
Musculoskeletal stiffness	21.42	10.43	104	80169	123264	53145529
Abdominal discomfort	21.35	10.43	221	80052	220841	53047952
Sedation	21.24	10.43	9	80264	29666	53239127
Coronary artery disease	21.12	10.43	12	80261	33425	53235368
Blood creatinine increased	20.86	10.43	203	80070	82459	53186334
Loss of personal independence in daily activities	20.27	10.43	47	80226	69768	53199025
Palmar-plantar erythrodysaesthesia syndrome	20.22	10.43	75	80198	21531	53247262
Cardiotoxicity	20.16	10.43	38	80235	7261	53261532
Dermatitis acneiform	20.11	10.43	29	80244	4441	53264352
Short-bowel syndrome	20.07	10.43	11	80262	451	53268342
Femur fracture	20.03	10.43	18	80255	39567	53229226
Rash	19.97	10.43	515	79758	445676	52823117
Large intestine polyp	19.74	10.43	40	80233	8057	53260736
Enteritis	19.62	10.43	38	80235	7408	53261385
Therapeutic product effect incomplete	19.24	10.43	72	80201	91712	53177081
Hepatotoxicity	19.16	10.43	88	80185	27792	53241001
Type 2 diabetes mellitus	19.11	10.43	12	80261	31658	53237135
Paronychia	19.09	10.43	30	80243	4954	53263839
Food interaction	19.01	10.43	12	80261	641	53268152
Bone hypertrophy	18.99	10.43	10	80263	378	53268415
Product dose omission issue	18.73	10.43	191	80082	191429	53077364
Enterocolitis	18.59	10.43	36	80237	7016	53261777
Gastroenteritis	18.46	10.43	82	80191	25534	53243259
Dyspepsia	18.34	10.43	188	80085	77412	53191381
Tenderness	18.05	10.43	68	80205	19662	53249131
Dry eye	18.04	10.43	99	80174	33545	53235248
Drug resistance	17.98	10.43	4	80269	19958	53248835
Neutropenia	17.65	10.43	337	79936	158848	53109945
Pancreatitis chronic	17.64	10.43	20	80253	2410	53266383
Congenital knee deformity	17.54	10.43	5	80268	32	53268761
Pregnancy	17.52	10.43	13	80260	31428	53237365
Intestinal fibrosis	17.40	10.43	7	80266	140	53268653
Anal incontinence	17.34	10.43	50	80223	12597	53256196
Ileal stenosis	17.27	10.43	16	80257	1520	53267273
Reflux gastritis	17.25	10.43	13	80260	927	53267866
Accidental exposure to product	17.24	10.43	7	80266	23667	53245126
Alopecia	17.15	10.43	249	80024	234334	53034459
Autoimmune nephritis	17.15	10.43	9	80264	338	53268455
Hypovolaemia	17.14	10.43	44	80229	10358	53258435
Peripheral pulse decreased	17.04	10.43	5	80268	36	53268757
Proctitis	17.02	10.43	18	80255	2007	53266786
Ejection fraction decreased	17.01	10.43	67	80206	19781	53249012
Urinary tract infection	17.00	10.43	477	79796	239426	53029367
Sinus arrest	16.59	10.43	17	80256	1827	53266966
Long QT syndrome congenital	16.58	10.43	5	80268	40	53268753
Sepsis	16.57	10.43	311	79962	146118	53122675
Hypermagnesaemia	16.48	10.43	13	80260	992	53267801
Inflammatory bowel disease	16.28	10.43	24	80249	3749	53265044
Cor pulmonale acute	16.27	10.43	9	80264	376	53268417
Plantar erythema	16.19	10.43	8	80265	264	53268529
Hypocalcaemia	16.18	10.43	87	80186	29250	53239543
Bone cyst	16.10	10.43	18	80255	2136	53266657
Synovitis	15.94	10.43	96	80177	107797	53160996
Fracture pain	15.91	10.43	9	80264	393	53268400
Drug eruption	15.86	10.43	9	80264	25085	53243708
Stoma site ulcer	15.84	10.43	8	80265	277	53268516
Condition aggravated	15.77	10.43	334	79939	296800	52971993
Cyst	15.77	10.43	49	80224	12862	53255931
Gastrointestinal sounds abnormal	15.75	10.43	24	80249	3860	53264933
Abortion spontaneous	15.56	10.43	29	80244	46606	53222187
Enterocutaneous fistula	15.47	10.43	14	80259	1290	53267503
Asthenia	15.46	10.43	648	79625	342942	52925851
Rectal abscess	15.41	10.43	13	80260	1091	53267702
Dysgeusia	15.37	10.43	114	80159	42817	53225976
Influenza like illness	15.34	10.43	44	80229	60815	53207978
Intestinal anastomosis	15.33	10.43	8	80265	297	53268496
Failure to thrive	15.25	10.43	33	80240	6959	53261834
Paralysis recurrent laryngeal nerve	15.24	10.43	5	80268	54	53268739
Malnutrition	15.08	10.43	53	80220	14818	53253975
Food refusal	14.92	10.43	8	80265	314	53268479
Tachycardia	14.83	10.43	237	80036	107975	53160818
Ileostomy	14.82	10.43	13	80260	1150	53267643
Biliary sepsis	14.81	10.43	12	80261	952	53267841
Electrolyte imbalance	14.80	10.43	62	80211	18822	53249971
Peritoneal perforation	14.74	10.43	6	80267	124	53268669
Palmar erythema	14.66	10.43	15	80258	1609	53267184
Nail disorder	14.65	10.43	40	80233	9765	53259028
Intestinal perforation	14.65	10.43	44	80229	11336	53257457
Arthritis	14.64	10.43	198	80075	87100	53181693
Pruritus	14.53	10.43	334	79939	293498	52975295
Amoebic colitis	14.43	10.43	3	80270	3	53268790
Catheter site bruise	14.40	10.43	8	80265	337	53268456
Small intestine ulcer	14.21	10.43	8	80265	346	53268447
Hepatic lesion	14.19	10.43	24	80249	4213	53264580
Unmasking of previously unidentified disease	14.12	10.43	11	80262	824	53267969
Ileus	14.06	10.43	52	80221	14903	53253890
Onychalgia	13.83	10.43	11	80262	850	53267943
Blood potassium increased	13.53	10.43	58	80215	17783	53251010
Hepatic enzyme increased	13.50	10.43	123	80150	126072	53142721
Gluten sensitivity	13.40	10.43	9	80264	535	53268258
Amputation	13.32	10.43	6	80267	160	53268633
Peritoneal disorder	13.26	10.43	9	80264	544	53268249
Rectal haemorrhage	13.10	10.43	107	80166	41374	53227419
Product use in unapproved indication	13.10	10.43	107	80166	112182	53156611
Tumour inflammation	13.05	10.43	4	80269	34	53268759
Pleural effusion	12.89	10.43	196	80077	88383	53180410
Periventricular leukomalacia	12.87	10.43	5	80268	91	53268702
Acute kidney injury	12.85	10.43	485	79788	253383	53015410
Nail bed tenderness	12.84	10.43	7	80266	284	53268509
Ataxia	12.83	10.43	50	80223	14687	53254106
Ureteric obstruction	12.81	10.43	15	80258	1871	53266922
Hyperchlorhydria	12.73	10.43	14	80259	1632	53267161
Osteopenia	12.66	10.43	58	80215	18297	53250496
Eye irritation	12.57	10.43	6	80267	18443	53250350
Psychotic disorder	12.57	10.43	71	80202	24314	53244479
Road traffic accident	12.56	10.43	12	80261	25619	53243174
Cerebral haemorrhage	12.55	10.43	16	80257	29980	53238813
Accidental exposure to product by child	12.47	10.43	12	80261	1196	53267597
Adverse event	12.44	10.43	27	80246	41034	53227759
Autonomic neuropathy	12.31	10.43	11	80262	997	53267796
Megacolon	12.31	10.43	15	80258	1951	53266842
Foetal arrhythmia	12.29	10.43	6	80267	193	53268600
Anaemia of malignant disease	12.26	10.43	8	80265	453	53268340
Defaecation urgency	12.22	10.43	19	80254	3109	53265684
Device issue	12.01	10.43	9	80264	21649	53247144
Blood cholesterol increased	11.87	10.43	127	80146	52862	53215931
Cardiorenal syndrome	11.84	10.43	9	80264	650	53268143
Piloerection	11.79	10.43	7	80266	335	53268458
Autoimmune colitis	11.72	10.43	8	80265	488	53268305
Suicidal ideation	11.70	10.43	49	80224	60462	53208331
Pharyngo-oesophageal diverticulum	11.69	10.43	3	80270	12	53268781
Platelet count decreased	11.68	10.43	228	80045	107871	53160922
Ventricular fibrillation	11.67	10.43	42	80231	11883	53256910
Anxiety	11.66	10.43	217	80056	196487	53072306
Accidental poisoning	11.63	10.43	9	80264	668	53268125
Motion sickness	11.61	10.43	10	80263	863	53267930
Alveolar bone resorption	11.60	10.43	4	80269	51	53268742
Renal pain	11.53	10.43	27	80246	6000	53262793
Fibromyalgia	11.49	10.43	109	80164	43966	53224827
Abdominal mass	11.39	10.43	17	80256	2685	53266108
Joint effusion	11.39	10.43	3	80270	13349	53255444
Moraxella infection	11.33	10.43	7	80266	360	53268433
Hypophosphataemia	11.30	10.43	34	80239	8771	53260022
Large intestine perforation	11.29	10.43	32	80241	7982	53260811
Hip fracture	11.25	10.43	77	80196	28180	53240613
Gastroenteropancreatic neuroendocrine tumour disease	11.19	10.43	4	80269	57	53268736
Glaucoma	11.19	10.43	53	80220	16950	53251843
Neutrophil count decreased	11.15	10.43	118	80155	48980	53219813
Blood sodium decreased	11.07	10.43	66	80207	23050	53245743
Lip erosion	11.00	10.43	10	80263	927	53267866
Intentional product use issue	10.97	10.43	64	80209	72430	53196363
Osteosclerosis	10.92	10.43	20	80253	3738	53265055
Miosis	10.90	10.43	29	80244	6973	53261820
Soft tissue swelling	10.80	10.43	10	80263	949	53267844
Abdominal pain upper	10.77	10.43	327	79946	165964	53102829
Abdominal distension	10.64	10.43	174	80099	79616	53189177
Cardiac arrest	10.61	10.43	199	80074	93468	53175325
Obesity	10.49	10.43	6	80267	16656	53252137

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
Diarrhoea	1102.01	11.19	2026	49903	362776	32098821
Drug abuse	277.91	11.19	476	51453	79767	32381830
Torsade de pointes	222.75	11.19	142	51787	7273	32454324
Dehydration	198.32	11.19	551	51378	128407	32333190
Electrocardiogram QRS complex prolonged	187.61	11.19	107	51822	4467	32457130
Electrocardiogram QT prolonged	179.53	11.19	266	51663	39375	32422222
Intentional overdose	154.74	11.19	255	51674	41346	32420251
Colitis	130.15	11.19	211	51718	33740	32427857
Ventricular tachycardia	107.85	11.19	166	51763	25390	32436207
Abdominal pain	94.46	11.19	480	51449	149049	32312548
Drug ineffective	70.15	11.19	345	51584	383132	32078465
Small intestinal obstruction	65.27	11.19	96	51833	14100	32447497
Intestinal obstruction	63.60	11.19	117	51812	20681	32440916
Intentional self-injury	62.47	11.19	93	51836	13807	32447790
Brugada syndrome	62.36	11.19	28	51901	697	32460900
Vomiting	59.62	11.19	606	51323	234951	32226646
Blood mercury abnormal	58.31	11.19	19	51910	188	32461409
Conduction disorder	57.01	11.19	37	51892	1953	32459644
5-hydroxyindolacetic acid in urine increased	56.18	11.19	19	51910	213	32461384
Decreased appetite	53.48	11.19	439	51490	160374	32301223
Drug use disorder	51.08	11.19	44	51885	3577	32458020
Completed suicide	50.57	11.19	44	51885	92473	32369124
Overdose	48.36	11.19	270	51659	86807	32374790
Rheumatoid arthritis	47.95	11.19	7	51922	44537	32417060
Foetal exposure during pregnancy	43.30	11.19	7	51922	41294	32420303
Pouchitis	39.16	11.19	20	51909	667	32460930
Nausea	39.09	11.19	724	51205	320125	32141472
Electrolyte imbalance	37.96	11.19	70	51859	12392	32449205
Abscess intestinal	36.29	11.19	25	51904	1458	32460139
Respiratory depression	36.28	11.19	71	51858	13140	32448457
Alveolar lung disease	35.35	11.19	16	51913	406	32461191
Fatigue	34.00	11.19	765	51164	349936	32111661
Ileus	33.76	11.19	78	51851	16187	32445410
Product use in unapproved indication	30.53	11.19	58	51871	87146	32374451
Pulmonary interstitial emphysema syndrome	29.97	11.19	15	51914	479	32461118
Myocardial infarction	29.77	11.19	102	51827	125574	32336023
Abdominal distension	29.76	11.19	161	51768	51134	32410463
Hypomagnesaemia	29.42	11.19	81	51848	18724	32442873
Drug hypersensitivity	29.19	11.19	45	51884	73355	32388242
Weight decreased	29.12	11.19	396	51533	164422	32297175
Low density lipoprotein decreased	28.75	11.19	19	51910	1034	32460563
Psoriasis	27.62	11.19	20	51909	46103	32415494
Hepatic neoplasm	26.81	11.19	24	51905	2054	32459543
Gastrointestinal stoma complication	26.68	11.19	20	51909	1332	32460265
Cardiotoxicity	26.59	11.19	36	51893	4896	32456701
Cardiac arrest	26.33	11.19	253	51676	96523	32365074
Enteritis	26.28	11.19	44	51885	7217	32454380
Treatment failure	26.15	11.19	15	51914	39148	32422449
Ventricular arrhythmia	25.77	11.19	36	51893	5043	32456554
Crohn's disease	25.40	11.19	33	51896	4312	32457285
Asthma	25.24	11.19	20	51909	44045	32417552
Accidental overdose	25.17	11.19	78	51851	19261	32442336
Intentional product misuse	25.01	11.19	119	51810	35932	32425665
Clostridium difficile colitis	24.71	11.19	64	51865	14267	32447330
Enterocolitis	24.62	11.19	43	51886	7297	32454300
Colitis microscopic	24.30	11.19	22	51907	1910	32459687
Stomatitis	23.83	11.19	127	51802	40102	32421495
Blood potassium decreased	23.56	11.19	71	51858	17267	32444330
Enterocolonic fistula	23.09	11.19	8	51921	97	32461500
Expired product administered	22.25	11.19	26	51903	3049	32458548
Palmar-plantar erythrodysaesthesia syndrome	21.88	11.19	65	51864	15684	32445913
Colitis ulcerative	21.47	11.19	68	51861	16983	32444614
Wrong technique in product usage process	21.25	11.19	15	51914	35044	32426553
Gastrointestinal obstruction	21.12	11.19	14	51915	766	32460831
Frequent bowel movements	20.36	11.19	46	51883	9406	32452191
Mucosal inflammation	20.10	11.19	106	51823	33328	32428269
Abdominal abscess	20.06	11.19	29	51900	4192	32457405
Miosis	19.47	11.19	43	51886	8661	32452936
Proctalgia	19.39	11.19	30	51899	4604	32456993
Immune-mediated enterocolitis	18.99	11.19	18	51911	1657	32459940
Dysgeusia	18.97	11.19	86	51843	25445	32436152
Hepatic haematoma	18.80	11.19	11	51918	482	32461115
Anal fissure	18.44	11.19	23	51906	2886	32458711
Atrioventricular block first degree	18.18	11.19	33	51896	5770	32455827
Intestinal stenosis	18.12	11.19	19	51910	1976	32459621
Therapeutic product effect decreased	17.86	11.19	14	51915	31003	32430594
Brain herniation	17.53	11.19	26	51903	3845	32457752
Pneumonitis	17.07	11.19	94	51835	30040	32431557
Anal fistula infection	17.06	11.19	4	51925	9	32461588
Angioedema	16.69	11.19	20	51909	36269	32425328
Electrocardiogram PR prolongation	16.65	11.19	12	51917	752	32460845
Right ventricular dilatation	16.64	11.19	11	51918	599	32460998
Colorectal cancer metastatic	16.63	11.19	14	51915	1103	32460494
Interstitial lung disease	16.59	11.19	51	51878	64950	32396647
Lethargy	16.13	11.19	117	51812	41111	32420486
Autoimmune colitis	16.04	11.19	13	51916	971	32460626
Gastrointestinal sounds abnormal	15.99	11.19	18	51911	2027	32459570
Peripheral embolism	15.96	11.19	13	51916	978	32460619
Gastroenteritis	15.80	11.19	54	51875	14027	32447570
Coronary artery disease	15.74	11.19	35	51894	49671	32411926
Intestinal perforation	15.68	11.19	40	51889	8835	32452762
Product dose omission issue	15.51	11.19	98	51831	102477	32359120
Gastrointestinal inflammation	15.31	11.19	22	51907	3162	32458435
Wheezing	15.24	11.19	22	51907	36852	32424745
Basosquamous carcinoma	15.00	11.19	6	51923	111	32461486
Flatulence	14.99	11.19	66	51863	19289	32442308
Intestinal fistula	14.97	11.19	12	51917	882	32460715
Subileus	14.87	11.19	22	51907	3246	32458351
Bacterial diarrhoea	14.79	11.19	5	51924	56	32461541
Musculoskeletal stiffness	14.73	11.19	25	51904	39239	32422358
Nephroangiosclerosis	14.73	11.19	7	51922	199	32461398
Malignant neoplasm progression	14.40	11.19	190	51739	78306	32383291
Off label use	14.38	11.19	376	51553	305944	32155653
Vascular device infection	14.28	11.19	19	51910	2541	32459056
Post procedural diarrhoea	14.26	11.19	5	51924	63	32461534
Drug delivery device placement	14.13	11.19	6	51923	130	32461467
Sedation	14.02	11.19	6	51923	18520	32443077
Diffuse alveolar damage	13.83	11.19	17	51912	2102	32459495
Drug reaction with eosinophilia and systemic symptoms	13.81	11.19	19	51910	32466	32429131
Proctitis	13.81	11.19	18	51911	2360	32459237
Neoplasm	13.75	11.19	25	51904	4376	32457221
Drug resistance	13.69	11.19	10	51919	22955	32438642
Hypophosphataemia	13.65	11.19	38	51891	8837	32452760
Cardiac failure	13.65	11.19	88	51841	91585	32370012
Joint swelling	13.63	11.19	40	51889	51695	32409902
Immune-mediated hepatitis	13.45	11.19	14	51915	1443	32460154
Drug level above therapeutic	13.41	11.19	21	51908	3257	32458340
Dyschromatopsia	13.36	11.19	8	51921	366	32461231
Pyomyositis	13.34	11.19	6	51923	150	32461447
Blood magnesium decreased	13.31	11.19	29	51900	5788	32455809
Eye infection fungal	13.28	11.19	8	51921	370	32461227
Generalised oedema	13.25	11.19	47	51882	12436	32449161
Retinal ischaemia	13.22	11.19	8	51921	373	32461224
Medication error	13.19	11.19	10	51919	22525	32439072
Gastrointestinal stoma output increased	13.14	11.19	4	51925	31	32461566
Aggression	13.08	11.19	27	51902	39362	32422235
Device related infection	13.02	11.19	60	51869	17873	32443724
Short-bowel syndrome	13.01	11.19	7	51922	260	32461337
Gastrointestinal stenosis	12.94	11.19	5	51924	84	32461513
Gastroenteritis staphylococcal	12.89	11.19	7	51922	265	32461332
Cardiac failure congestive	12.86	11.19	81	51848	84771	32376826
Necrotising ulcerative gingivostomatitis	12.68	11.19	5	51924	89	32461508
CSF white blood cell count decreased	12.61	11.19	4	51925	36	32461561
Blood creatine phosphokinase increased	12.09	11.19	35	51894	45441	32416156
Splenic vein thrombosis	12.08	11.19	8	51921	437	32461160
Intracranial mass	12.04	11.19	12	51917	1175	32460422
Seizure	12.00	11.19	107	51822	103747	32357850
Biopsy intestine abnormal	11.94	11.19	3	51926	10	32461587
Feeling abnormal	11.76	11.19	53	51876	60370	32401227
Mixed dementia	11.73	11.19	7	51922	318	32461279
Hypokalaemia	11.67	11.19	137	51792	54957	32406640
No adverse event	11.61	11.19	9	51920	20044	32441553
Injection site pain	11.55	11.19	22	51907	33036	32428561
Sleep apnoea syndrome	11.47	11.19	8	51921	18806	32442791
Drug withdrawal syndrome	11.39	11.19	63	51866	20168	32441429
Product prescribing error	11.22	11.19	9	51920	19708	32441889
Faecaloma	11.21	11.19	24	51905	4732	32456865

Pharmacologic Action:

Source	Code	Description
ATC	A07DA03	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
ATC	A07DA53	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
FDA MoA	N0000000174	Opioid Agonists
MeSH PA	D000930	Antidiarrheals
MeSH PA	D005765	Gastrointestinal Agents
CHEBI has role	CHEBI:55322	mu opioid agonist
CHEBI has role	CHEBI:55323	antiperistaltics
CHEBI has role	CHEBI:149553	anti-coronaviral agents
FDA EPC	N0000175690	Opioid Agonist

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Traveler's diarrhea	indication	11840006
Diarrhea	indication	62315008
Diarrhea Secondary to Inflammatory Bowel Disease	indication
Chemotherapy-Induced Diarrhea	off-label use
Infectious diarrheal disease	contraindication	19213003	DOID:13250
Paralytic ileus	contraindication	55525008	DOID:8442
Hemorrhagic diarrhea	contraindication	95545007
Disease of liver	contraindication	235856003	DOID:409

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.78	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
2MG	LOPERAMIDE HYDROCHLORIDE	STRIDES PHARMA	A213070	Aug. 11, 2021	OTC	CAPSULE	ORAL	April 20, 2022	COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	Ki	8.82		WOMBAT-PK	CHEMBL
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN		IC50	6.62		CHEMBL
Glutamate receptor ionotropic, NMDA 2A	Ion channel	Q12879	NMDE1_HUMAN					WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.58		DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.93		DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.58		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.34		DRUG MATRIX
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		IC50	5.70		WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.52		DRUG MATRIX
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	5		WOMBAT-PK
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	Ion channel	O00555	CAC1A_HUMAN					WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5.70		DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	5.60		DRUG MATRIX
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	6.81		WOMBAT-PK
Calmodulin	Cytosolic other	P0DP23 P0DP24 P0DP25	CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN					WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		Ki	6.91		WOMBAT-PK
Somatostatin receptor type 5	GPCR	P35346	SSR5_HUMAN		Ki	5.35		WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2B	Ion channel	Q13224	NMDE2_HUMAN					WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2C	Ion channel	Q14957	NMDE3_HUMAN					WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2D	Ion channel	O15399	NMDE4_HUMAN					WOMBAT-PK
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.23		CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.63		CHEMBL
Cocaine esterase	Enzyme	O00748	EST2_HUMAN		IC50	5.39		CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	6.57		CHEMBL
Menin	Unclassified	O00255	MEN1_HUMAN		IC50	4.16		CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.69		DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	6.27		DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	6.07		DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.21		CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.80		CHEMBL
Delta-type opioid receptor	GPCR		OPRD_RAT		Ki	7.30		CHEMBL
Calmodulin	Cytosolic other		CALM_BOVIN		Kd	5.46		CHEMBL

External reference:

ID	Source
4019804	VUID
N0000147893	NUI
D00729	KEGG_DRUG
34552-83-5	SECONDARY_CAS_RN
4019178	VANDF
4019804	VANDF
C0023992	UMLSCUI
CHEBI:6532	CHEBI
CHEMBL841	ChEMBL_ID
CHEMBL1707	ChEMBL_ID
D008139	MESH_DESCRIPTOR_UI
DB00836	DRUGBANK_ID
7215	IUPHAR_LIGAND_ID
3098	INN_ID
6X9OC3H4II	UNII
3955	PUBCHEM_CID
151889	RXNORM
2069	MMSL
2336	MMSL
4992	MMSL
d01025	MMSL
001154	NDDF
004545	NDDF
116726003	SNOMEDCT_US
387040009	SNOMEDCT_US
57574005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Loperamide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0311	CAPSULE	2 mg	ORAL	ANDA	26 sections
good sense anti diarrheal anti gas	HUMAN OTC DRUG LABEL	2	0113-0087	TABLET	2 mg	ORAL	ANDA	16 sections
Good Sense anti diarrheal	HUMAN OTC DRUG LABEL	1	0113-0224	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
Good Sense Anti Diarrheal Anti Gas	HUMAN OTC DRUG LABEL	2	0113-1087	TABLET	2 mg	ORAL	ANDA	16 sections
Good Sense antidiarrheal	HUMAN OTC DRUG LABEL	1	0113-1645	SOLUTION	1 mg	ORAL	ANDA	16 sections
anti diarrheal	HUMAN OTC DRUG LABEL	1	0113-2224	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
basic care loperamide hydrochloride and simethicone	HUMAN OTC DRUG LABEL	2	0113-7119	TABLET	2 mg	ORAL	ANDA	16 sections
Basic Care loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	0113-7224	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-0375	TABLET	2 mg	ORAL	ANDA	16 sections
loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	0363-0645	SUSPENSION	1 mg	ORAL	ANDA	16 sections
anti diarrheal	HUMAN OTC DRUG LABEL	1	0363-1010	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-1176	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	16 sections
anti diarrheal and anti gas	HUMAN OTC DRUG LABEL	2	0363-1830	TABLET	2 mg	ORAL	ANDA	16 sections
Loperamide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2100	CAPSULE	2 mg	ORAL	ANDA	29 sections
Antidiarrheal Relief	HUMAN OTC DRUG LABEL	1	0498-1071	TABLET	2 mg	ORAL	ANDA	16 sections
Loperamide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-0362	CAPSULE	2 mg	ORAL	ANDA	25 sections
Loperamide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8087	CAPSULE	2 mg	ORAL	ANDA	29 sections
loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	0904-6836	SOLUTION	1 mg	ORAL	ANDA	16 sections
anti diarrheal	HUMAN OTC DRUG LABEL	1	0904-7725	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	11673-177	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	17 sections
Up and Up anti diarrheal	HUMAN OTC DRUG LABEL	1	11673-224	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
up and up anti diarrheal anti gas	HUMAN OTC DRUG LABEL	2	11673-646	TABLET	2 mg	ORAL	ANDA	16 sections
Up and Up anti diarrheal	HUMAN OTC DRUG LABEL	1	11673-900	SUSPENSION	1 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	11822-0375	TABLET	2 mg	ORAL	ANDA	16 sections
anti diarrheal anti gas	HUMAN OTC DRUG LABEL	2	11822-1003	TABLET	2 mg	ORAL	ANDA	16 sections
loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	11822-1645	SUSPENSION	1 mg	ORAL	ANDA	16 sections
loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	11822-5519	SOLUTION	1 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	11822-7834	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	17 sections
Loperamide Hydrochloride	HUMAN OTC DRUG LABEL	1	15127-338	TABLET	2 mg	ORAL	ANDA	16 sections
LOPERAMIDE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	16590-423	CAPSULE	2 mg	ORAL	ANDA	25 sections