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	1283.11	10.37	2732	70059	556870	46056401
Dehydration	263.04	10.37	689	72102	158851	46454420
Pneumonia viral	182.28	10.37	119	72672	6505	46606766
Rheumatoid arthritis	137.78	10.37	104	72687	240111	46373160
Vomiting	129.04	10.37	1171	71620	451623	46161648
Torsade de pointes	115.00	10.37	117	72674	12037	46601234
Drug ineffective	112.44	10.37	611	72180	677227	45936044
Drug abuse	110.58	10.37	280	72511	63128	46550143
Soft tissue disorder	109.82	10.37	73	72718	4113	46609158
Pneumonia aspiration	107.82	10.37	184	72607	31421	46581850
Ventricular tachycardia	98.76	10.37	127	72664	16840	46596431
Maternal exposure during pregnancy	98.45	10.37	20	72771	102529	46510742
Decreased appetite	96.94	10.37	574	72217	193262	46420009
Hypomagnesaemia	88.88	10.37	139	72652	22071	46591200
Hypokalaemia	87.53	10.37	319	72472	87705	46525566
Electrocardiogram QT prolonged	86.73	10.37	224	72567	51101	46562170
Coma	85.89	10.37	242	72549	58107	46555164
Oral pain	85.41	10.37	145	72646	24652	46588619
Completed suicide	83.80	10.37	63	72728	145857	46467414
Colitis	82.61	10.37	181	72610	37166	46576105
Gastrointestinal stoma complication	80.07	10.37	42	72749	1519	46611752
Gastrooesophageal reflux disease	74.38	10.37	270	72521	74074	46539197
Hypomania	72.83	10.37	58	72733	4330	46608941
Abdominal pain	72.53	10.37	609	72182	229422	46383849
Jaundice cholestatic	69.96	10.37	60	72731	4969	46608302
Small intestinal obstruction	67.21	10.37	103	72688	16069	46597202
Drug hypersensitivity	65.12	10.37	181	72610	243644	46369627
Nausea	61.93	10.37	1453	71338	686001	45927270
Pain	59.91	10.37	467	72324	476481	46136790
Presbyacusis	57.17	10.37	42	72749	2780	46610491
Blood magnesium increased	56.74	10.37	43	72748	2984	46610287
Exposure during pregnancy	55.61	10.37	52	72739	108160	46505111
Intestinal obstruction	54.98	10.37	124	72667	25951	46587320
Systemic lupus erythematosus	54.28	10.37	17	72774	65163	46548108
Pleural thickening	53.42	10.37	39	72752	2556	46610715
Neutropenic sepsis	53.35	10.37	80	72711	12244	46601027
Deafness neurosensory	51.39	10.37	48	72743	4446	46608825
Schizophrenia	49.65	10.37	64	72727	8504	46604767
Pleural fibrosis	48.47	10.37	42	72749	3527	46609744
Stomatitis	47.67	10.37	222	72569	68075	46545196
Blood magnesium decreased	47.08	10.37	71	72720	10921	46602350
Injection site erythema	46.88	10.37	29	72762	74398	46538873
Colitis microscopic	46.12	10.37	54	72737	6502	46606769
Lethargy	44.69	10.37	178	72613	50993	46562278
Injection site pain	44.69	10.37	61	72730	107091	46506180
Injection site pruritus	44.40	10.37	5	72786	39738	46573533
Intentional overdose	43.79	10.37	209	72582	64735	46548536
Psoriasis	42.51	10.37	36	72755	78568	46534703
Mucosal inflammation	41.05	10.37	144	72647	38832	46574439
Segmental diverticular colitis	40.08	10.37	13	72778	130	46613141
Calcium ionised decreased	39.97	10.37	15	72776	238	46613033
Somnolence	39.90	10.37	396	72395	156125	46457146
Pedal pulse abnormal	39.13	10.37	13	72778	141	46613130
Therapeutic response decreased	38.23	10.37	10	72781	43135	46570136
Total lung capacity increased	37.37	10.37	20	72771	754	46612517
Long QT syndrome	37.36	10.37	34	72757	3046	46610225
Brugada syndrome	37.08	10.37	14	72777	226	46613045
Epigastric discomfort	36.99	10.37	45	72746	5639	46607632
Electrocardiogram QRS complex prolonged	36.87	10.37	44	72747	5405	46607866
Headache	36.84	10.37	525	72266	477827	46135444
Malignant neoplasm progression	36.13	10.37	198	72593	64728	46548543
Weight decreased	36.12	10.37	494	72297	210355	46402916
Pouchitis	34.84	10.37	16	72775	431	46612840
Accidental overdose	34.32	10.37	88	72703	19978	46593293
Nail dystrophy	34.23	10.37	16	72775	449	46612822
Flatulence	34.21	10.37	111	72680	28767	46584504
Constipation	33.62	10.37	417	72374	173680	46439591
Drug interaction	33.44	10.37	183	72608	202911	46410360
Herpes zoster	33.19	10.37	200	72591	67672	46545599
Psoriatic arthropathy	33.07	10.37	8	72783	36371	46576900
Frequent bowel movements	32.32	10.37	65	72726	12567	46600704
Neuropathy peripheral	32.02	10.37	247	72544	90646	46522625
Device expulsion	31.97	10.37	3	72788	27539	46585732
Gallbladder polyp	31.96	10.37	18	72773	751	46612520
Contraindicated product administered	31.85	10.37	47	72744	79900	46533371
Off label use	31.69	10.37	410	72381	379431	46233840
Injection site reaction	31.03	10.37	18	72773	47831	46565440
Blood potassium decreased	29.77	10.37	128	72663	37935	46575336
Respiration abnormal	29.76	10.37	36	72755	4485	46608786
Gastroenteritis radiation	29.63	10.37	15	72776	503	46612768
Drug use disorder	28.96	10.37	28	72763	2707	46610564
Conduction disorder	28.75	10.37	21	72770	1377	46611894
Fatigue	28.69	10.37	1190	71601	607507	46005764
Drug intolerance	28.52	10.37	125	72666	146924	46466347
Gastrointestinal stoma output increased	28.45	10.37	11	72780	190	46613081
Pneumonia	27.93	10.37	776	72015	375544	46237727
Febrile neutropenia	27.89	10.37	247	72544	94380	46518891
Clostridium difficile infection	27.52	10.37	94	72697	25009	46588262
Stoma complication	26.97	10.37	11	72780	220	46613051
Wrong technique in product usage process	26.96	10.37	27	72764	54395	46558876
Injection site bruising	26.76	10.37	11	72780	35625	46577646
Knee arthroplasty	26.38	10.37	3	72788	23662	46589609
Arteriovenous fistula occlusion	26.34	10.37	12	72779	317	46612954
Intentional self-injury	26.06	10.37	90	72701	24076	46589195
Liver function test abnormal	26.01	10.37	142	72649	46345	46566926
Multiple sclerosis relapse	25.72	10.37	17	72774	42108	46571163
Infusion related reaction	25.60	10.37	77	72714	101131	46512140
Blue toe syndrome	25.47	10.37	12	72779	343	46612928
Ventricular arrhythmia	25.44	10.37	29	72762	3392	46609879
Red blood cell sedimentation rate increased	25.27	10.37	3	72788	22886	46590385
Injection site swelling	24.99	10.37	16	72775	40311	46572960
Arthralgia	24.66	10.37	410	72381	364193	46249078
Mydriasis	24.30	10.37	52	72739	10501	46602770
Feeding intolerance	24.12	10.37	13	72778	497	46612774
Post procedural diarrhoea	24.07	10.37	10	72781	210	46613061
Pulmonary thrombosis	23.80	10.37	42	72749	7360	46605911
Blood bilirubin increased	23.75	10.37	111	72680	34073	46579198
Product quality issue	23.71	10.37	13	72778	35635	46577636
Leukopenia	23.66	10.37	185	72606	68158	46545113
Urticaria	23.60	10.37	99	72692	117793	46495478
Dry skin	23.43	10.37	126	72665	40890	46572381
Glossodynia	23.16	10.37	21	72770	44352	46568919
Coronary artery disease	22.90	10.37	12	72779	33740	46579531
Syncope	22.85	10.37	257	72534	104546	46508725
Anal abscess	22.79	10.37	28	72763	3544	46609727
Crohn's disease	22.53	10.37	39	72752	6732	46606539
No adverse event	22.02	10.37	13	72778	34218	46579053
Therapeutic reaction time decreased	21.87	10.37	16	72775	1052	46612219
Premature delivery	21.81	10.37	4	72787	22065	46591206
Thymus disorder	21.32	10.37	9	72782	197	46613074
Ear infection	21.03	10.37	5	72786	23008	46590263
Foetal exposure during pregnancy	20.76	10.37	11	72780	30736	46582535
Product dose omission issue	20.59	10.37	166	72625	168354	46444917
Brain stem glioma	20.59	10.37	7	72784	82	46613189
Pyrexia	20.45	10.37	699	72092	348103	46265168
Skin fissures	20.22	10.37	40	72751	7640	46605631
Cholelithiasis	20.21	10.37	116	72675	38565	46574706
Food interaction	19.89	10.37	12	72779	570	46612701
Pneumonitis	19.54	10.37	92	72699	28328	46584943
Paronychia	18.85	10.37	29	72762	4537	46608734
Loss of personal independence in daily activities	18.77	10.37	38	72753	57145	46556126
Femur fracture	18.73	10.37	18	72773	36979	46576292
Bone hypertrophy	18.68	10.37	10	72781	377	46612894
Sinusitis	18.66	10.37	122	72669	129646	46483625
Hip arthroplasty	18.52	10.37	3	72788	18109	46595162
Dermatitis acneiform	18.45	10.37	27	72764	4043	46609228
Blood cholesterol increased	18.35	10.37	116	72675	39897	46573374
Congenital knee deformity	18.24	10.37	5	72786	26	46613245
Device related infection	18.21	10.37	73	72718	20968	46592303
Therapeutic product effect decreased	18.03	10.37	67	72724	82534	46530737
Short-bowel syndrome	17.92	10.37	10	72781	410	46612861
Blood creatinine increased	17.86	10.37	190	72601	76213	46537058
Gastroenteritis	17.83	10.37	80	72711	24139	46589132
Unresponsive to stimuli	17.81	10.37	98	72693	32076	46581195
Palmar-plantar erythrodysaesthesia syndrome	17.73	10.37	71	72720	20380	46592891
Proctitis	17.63	10.37	17	72774	1638	46611633
Hypovolaemia	17.57	10.37	44	72747	9844	46603427
Fibromyalgia	17.53	10.37	107	72684	36356	46576915
Anal incontinence	17.46	10.37	49	72742	11729	46601542
Tenderness	17.45	10.37	62	72729	16819	46596452
Suicidal ideation	17.23	10.37	39	72752	56343	46556928
Ileal stenosis	17.21	10.37	16	72775	1473	46611798
Hypermagnesaemia	17.07	10.37	13	72778	909	46612362
Overdose	17.04	10.37	238	72553	101741	46511530
Intestinal fibrosis	17.03	10.37	7	72784	143	46613128
Pericarditis	16.99	10.37	8	72783	23919	46589352
Sinus arrest	16.99	10.37	17	72774	1714	46611557
Peripheral pulse decreased	16.86	10.37	5	72786	36	46613235
Dyspepsia	16.82	10.37	172	72619	68300	46544971
Ileostomy	16.65	10.37	14	72777	1128	46612143
Influenza like illness	16.65	10.37	41	72750	57529	46555742
Clostridium difficile colitis	16.56	10.37	65	72726	18488	46594783
Cardiotoxicity	16.50	10.37	34	72757	6688	46606583
Pulmonary embolism	16.40	10.37	249	72542	108336	46504935
Brain injury	16.16	10.37	32	72759	6118	46607153
Plantar erythema	16.15	10.37	8	72783	256	46613015
Arthritis	16.13	10.37	188	72603	77128	46536143
Abortion spontaneous	16.10	10.37	27	72764	43619	46569652
Cor pulmonale acute	16.08	10.37	9	72782	371	46612900
Hypophagia	16.04	10.37	89	72702	29217	46584054
Onychalgia	15.96	10.37	11	72780	658	46612613
Rhinorrhoea	15.93	10.37	128	72663	47537	46565734
Anaemia	15.84	10.37	516	72275	255263	46358008
Fracture pain	15.82	10.37	9	72782	383	46612888
Arthropathy	15.81	10.37	73	72718	84627	46528644
Treatment failure	15.78	10.37	83	72708	93004	46520267
Failure to thrive	15.53	10.37	33	72758	6631	46606640
Drug resistance	15.43	10.37	4	72787	17364	46595907
Food refusal	15.41	10.37	8	72783	283	46612988
Dysgeusia	15.36	10.37	112	72679	40379	46572892
Gastrointestinal disorder	15.28	10.37	151	72640	59425	46553846
Anxiety	15.27	10.37	196	72595	181761	46431510
Intestinal anastomosis	15.23	10.37	8	72783	290	46612981
Enteritis	15.22	10.37	33	72758	6722	46606549
Paralysis recurrent laryngeal nerve	15.15	10.37	5	72786	53	46613218
Hepatotoxicity	15.08	10.37	78	72713	24931	46588340
Tumour inflammation	15.07	10.37	4	72787	18	46613253
Large intestine polyp	15.05	10.37	36	72755	7825	46605446
Accidental exposure to product	15.05	10.37	7	72784	21074	46592197
Catheter site bruise	14.82	10.37	8	72783	307	46612964
Cyst	14.77	10.37	47	72744	12053	46601218
Bone cyst	14.60	10.37	17	72774	2034	46611237
Autoimmune nephritis	14.56	10.37	8	72783	318	46612953
Peritoneal perforation	14.53	10.37	6	72785	124	46613147
Condition aggravated	14.50	10.37	282	72509	244770	46368501
Tachycardia	14.49	10.37	227	72564	99395	46513876
Hypocalcaemia	14.43	10.37	81	72710	26704	46586567
Amoebic colitis	14.32	10.37	3	72788	3	46613268
Sedation	14.32	10.37	9	72782	22901	46590370
Electrolyte imbalance	14.30	10.37	59	72732	17167	46596104
Therapeutic product effect incomplete	14.21	10.37	68	72723	78085	46535186
Perforation	14.19	10.37	12	72779	975	46612296
Musculoskeletal stiffness	14.15	10.37	92	72699	97901	46515370
Gastrointestinal sounds abnormal	14.10	10.37	22	72769	3484	46609787
Neutropenia	14.08	10.37	307	72484	142897	46470374
Asthenia	14.07	10.37	606	72185	310469	46302802
Palmar erythema	14.04	10.37	14	72777	1406	46611865
Ileus	13.98	10.37	51	72740	14013	46599258
Enterocutaneous fistula	13.98	10.37	13	72778	1197	46612074
Pregnancy	13.98	10.37	13	72778	27124	46586147
Dry eye	13.96	10.37	88	72703	30234	46583037
Drug eruption	13.86	10.37	8	72783	21321	46591950
Weight increased	13.86	10.37	177	72614	164296	46448975
Urinary tract infection	13.80	10.37	445	72346	219821	46393450
Gluten sensitivity	13.76	10.37	9	72782	493	46612778
Appetite disorder	13.40	10.37	27	72764	5227	46608044
Peritoneal disorder	13.23	10.37	9	72782	527	46612744
Amputation	13.22	10.37	6	72785	157	46613114
Blood potassium increased	13.22	10.37	57	72734	16910	46596361
Piloerection	13.12	10.37	7	72784	262	46613009
Foetal arrhythmia	13.12	10.37	6	72785	160	46613111
Intestinal perforation	13.11	10.37	42	72749	10809	46602462
Soft tissue swelling	13.08	10.37	11	72780	887	46612384
Cerebral haemorrhage	13.02	10.37	15	72776	28356	46584915
Anaemia of malignant disease	12.96	10.37	8	72783	396	46612875
Product use in unapproved indication	12.90	10.37	85	72706	90188	46523083
Myocardial infarction	12.87	10.37	94	72697	97434	46515837
Accidental exposure to product by child	12.85	10.37	12	72779	1111	46612160
Ureteric obstruction	12.72	10.37	15	72776	1819	46611452
Periventricular leukomalacia	12.69	10.37	5	72786	91	46613180
Enterocolitis	12.63	10.37	29	72762	6139	46607132
Abdominal pain upper	12.58	10.37	306	72485	144999	46468272
Ventricular fibrillation	12.56	10.37	43	72748	11453	46601818
Defaecation urgency	12.53	10.37	18	72773	2649	46610622
Malnutrition	12.45	10.37	49	72742	13954	46599317
Hepatic lesion	12.39	10.37	22	72769	3875	46609396
Surgery	12.38	10.37	16	72775	28769	46584502
Ejection fraction decreased	12.28	10.37	58	72733	17879	46595392
Bile acid malabsorption	12.26	10.37	5	72786	100	46613171
Frustration tolerance decreased	12.21	10.37	26	72765	5231	46608040
Cardiorenal syndrome	12.05	10.37	9	72782	611	46612660
Autoimmune colitis	12.04	10.37	8	72783	450	46612821
Megacolon	12.01	10.37	14	72777	1677	46611594
Muscle twitching	11.90	10.37	4	72787	14668	46598603
Motion sickness	11.80	10.37	10	72781	815	46612456
Injection site rash	11.68	10.37	5	72786	15808	46597463
Sepsis	11.64	10.37	286	72505	135728	46477543
Alveolar bone resorption	11.46	10.37	4	72787	51	46613220
Road traffic accident	11.45	10.37	12	72779	23679	46589592
Peripheral swelling	11.41	10.37	325	72466	157746	46455525
Inflammatory bowel disease	11.37	10.37	19	72772	3186	46610085
Miosis	11.18	10.37	29	72762	6628	46606643
Moraxella infection	11.17	10.37	7	72784	356	46612915
Eye irritation	11.13	10.37	6	72785	16608	46596663
Gastroenteropancreatic neuroendocrine tumour disease	11.05	10.37	4	72787	57	46613214
Pharyngo-oesophageal diverticulum	11.04	10.37	3	72788	15	46613256
Bone disorder	11.04	10.37	9	72782	20024	46593247
Device issue	10.98	10.37	9	72782	19971	46593300
Portal tract inflammation	10.88	10.37	3	72788	16	46613255
Obstruction	10.81	10.37	13	72778	1609	46611662
Joint space narrowing	10.81	10.37	5	72786	137	46613134
Abdominal mass	10.78	10.37	16	72775	2426	46610845
Injury	10.77	10.37	34	72757	43993	46569278
Heart sounds	10.73	10.37	6	72785	247	46613024
Stoma site extravasation	10.65	10.37	7	72784	387	46612884
Immobilisation syndrome	10.61	10.37	5	72786	143	46613128
Pleural effusion	10.58	10.37	185	72606	82767	46530504
Injection site haemorrhage	10.57	10.37	10	72781	20699	46592572
Gait disturbance	10.57	10.37	161	72630	145102	46468169
Cardiac failure congestive	10.46	10.37	92	72699	91658	46521613
Forced expiratory volume decreased	10.45	10.37	24	72767	5080	46608191
Renal pain	10.44	10.37	25	72766	5436	46607835
Vulvovaginal inflammation	10.44	10.37	8	72783	564	46612707
Emotional distress	10.42	10.37	20	72771	30687	46582584

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	1019.21	10.88	1870	46266	332233	29572109
Drug abuse	252.70	10.88	464	47672	81608	29822734
Torsade de pointes	206.11	10.88	134	48002	7056	29897286
Dehydration	194.06	10.88	534	47602	123005	29781337
Electrocardiogram QRS complex prolonged	190.97	10.88	106	48030	4171	29900171
Electrocardiogram QT prolonged	170.61	10.88	247	47889	35588	29868754
Intentional overdose	151.46	10.88	253	47883	41228	29863114
Colitis	128.91	10.88	200	47936	30620	29873722
Ventricular tachycardia	102.79	10.88	157	47979	23705	29880637
Abdominal pain	94.69	10.88	450	47686	135204	29769138
Small intestinal obstruction	67.66	10.88	96	48040	13563	29890779
Intentional self-injury	63.94	10.88	93	48043	13439	29890903
Completed suicide	61.89	10.88	42	48094	99450	29804892
Drug ineffective	60.99	10.88	311	47825	340076	29564266
Conduction disorder	57.47	10.88	37	48099	1914	29902428
Vomiting	57.43	10.88	572	47564	219246	29685096
Intestinal obstruction	56.92	10.88	107	48029	19105	29885237
Drug use disorder	55.03	10.88	44	48092	3204	29901138
Brugada syndrome	53.81	10.88	24	48112	584	29903758
Blood mercury abnormal	52.09	10.88	17	48119	168	29904174
5-hydroxyindolacetic acid in urine increased	49.97	10.88	17	48119	193	29904149
Decreased appetite	46.05	10.88	404	47732	149506	29754836
Overdose	45.07	10.88	260	47876	84077	29820265
Rheumatoid arthritis	43.52	10.88	7	48129	41190	29863152
Respiratory depression	43.06	10.88	71	48065	11432	29892910
Electrolyte imbalance	39.09	10.88	68	48068	11432	29892910
Foetal exposure during pregnancy	37.33	10.88	7	48129	36864	29867478
Abscess intestinal	37.05	10.88	25	48111	1400	29902942
Nausea	36.67	10.88	675	47461	296282	29608060
Abdominal distension	34.27	10.88	155	47981	45554	29858788
Pouchitis	34.11	10.88	18	48118	639	29903703
Myocardial infarction	33.90	10.88	97	48039	125528	29778814
Alveolar lung disease	33.11	10.88	15	48121	379	29903963
Treatment failure	32.23	10.88	8	48128	34671	29869671
Ventricular arrhythmia	30.42	10.88	36	48100	4252	29900090
Pulmonary interstitial emphysema syndrome	29.61	10.88	14	48122	391	29903951
Hypomagnesaemia	29.23	10.88	75	48061	16523	29887819
Ileus	29.19	10.88	72	48064	15483	29888859
Fatigue	28.54	10.88	695	47441	319978	29584364
Product use in unapproved indication	28.05	10.88	47	48089	73646	29830696
Crohn's disease	25.20	10.88	33	48103	4319	29900023
Low density lipoprotein decreased	25.01	10.88	17	48119	964	29903378
Hepatic neoplasm	24.92	10.88	22	48114	1837	29902505
Drug hypersensitivity	24.89	10.88	45	48091	68474	29835868
Enteritis	24.85	10.88	41	48095	6604	29897738
Cardiotoxicity	24.83	10.88	33	48103	4381	29899961
Accidental overdose	24.71	10.88	75	48061	18200	29886142
Enterocolonic fistula	24.52	10.88	8	48128	79	29904263
Weight decreased	24.07	10.88	358	47778	150563	29753779
Blood potassium decreased	24.06	10.88	70	48066	16592	29887750
Gastrointestinal stoma complication	22.96	10.88	18	48118	1274	29903068
Intentional product misuse	22.66	10.88	113	48023	34554	29869788
Miosis	22.64	10.88	43	48093	7733	29896609
Psoriasis	22.56	10.88	21	48115	42485	29861857
Gastrointestinal obstruction	21.80	10.88	14	48122	721	29903621
Clostridium difficile colitis	21.77	10.88	57	48079	12711	29891631
Inferior vena cava dilatation	21.40	10.88	9	48127	189	29904153
Abdominal abscess	21.10	10.88	29	48107	3975	29900367
Wrong technique in product usage process	20.94	10.88	12	48124	31143	29873199
Proctalgia	20.58	10.88	30	48106	4342	29900000
Colitis microscopic	20.56	10.88	19	48117	1684	29902658
Expired product administered	20.21	10.88	24	48112	2845	29901497
Palmar-plantar erythrodysaesthesia syndrome	20.08	10.88	61	48075	14809	29889533
Basosquamous carcinoma	19.29	10.88	8	48128	162	29904180
Cardiac arrest	19.24	10.88	231	47905	92619	29811723
Hepatic haematoma	18.84	10.88	11	48125	477	29903865
Intestinal stenosis	18.75	10.88	19	48117	1886	29902456
Coronary artery disease	18.64	10.88	32	48104	49680	29854662
Dysgeusia	18.50	10.88	84	48052	24717	29879625
Right ventricular dilatation	18.41	10.88	11	48125	498	29903844
Colitis ulcerative	18.36	10.88	58	48078	14376	29889966
Enterocolitis	18.28	10.88	36	48100	6651	29897691
Mucosal inflammation	18.26	10.88	97	48039	30397	29873945
Interstitial lung disease	18.11	10.88	44	48092	60153	29844189
Brain herniation	18.09	10.88	26	48110	3714	29900628
Stomatitis	18.01	10.88	112	48024	37167	29867175
Colorectal cancer metastatic	17.89	10.88	14	48122	988	29903354
Peripheral embolism	17.32	10.88	13	48123	862	29903480
Atrioventricular block first degree	17.24	10.88	32	48104	5656	29898686
Joint swelling	16.89	10.88	31	48105	46915	29857427
Lethargy	16.82	10.88	115	48021	39404	29864938
Asthma	16.81	10.88	20	48116	36154	29868188
Angioedema	15.99	10.88	19	48117	34365	29869977
Subileus	15.73	10.88	22	48114	3065	29901277
Intestinal perforation	15.52	10.88	39	48097	8480	29895862
Anal fissure	15.21	10.88	19	48117	2372	29901970
Gastrointestinal inflammation	15.17	10.88	21	48115	2898	29901444
Cardiac failure congestive	15.08	10.88	77	48059	84330	29820012
Dyschromatopsia	15.03	10.88	8	48128	289	29904053
Frequent bowel movements	14.82	10.88	38	48098	8367	29895975
Gastroenteritis	14.81	10.88	51	48085	13215	29891127
Flatulence	14.73	10.88	63	48073	18066	29886276
Therapeutic product effect decreased	14.69	10.88	15	48121	29061	29875281
Nephroangiosclerosis	14.69	10.88	7	48129	199	29904143
Gastrointestinal sounds abnormal	14.55	10.88	17	48119	1981	29902361
Electrocardiogram PR prolongation	14.52	10.88	11	48125	740	29903602
Mixed dementia	14.41	10.88	7	48129	208	29904134
Post procedural diarrhoea	14.30	10.88	5	48131	62	29904280
Eye infection fungal	14.24	10.88	8	48128	322	29904020
Anal fistula infection	14.23	10.88	3	48133	3	29904339
Drug delivery device placement	14.05	10.88	6	48130	131	29904211
Intestinal fistula	13.91	10.88	11	48125	788	29903554
Ascites	13.81	10.88	102	48034	35819	29868523
Autoimmune colitis	13.77	10.88	11	48125	800	29903542
Pneumonitis	13.59	10.88	83	48053	27371	29876971
Pyomyositis	13.53	10.88	6	48130	144	29904198
Retinal ischaemia	13.35	10.88	8	48128	364	29903978
Malignant neoplasm progression	13.32	10.88	176	47960	72111	29832231
Hypophosphataemia	13.24	10.88	36	48100	8209	29896133
Gastrointestinal stenosis	13.20	10.88	5	48131	79	29904263
Drug resistance	13.18	10.88	8	48128	20125	29884217
Diffuse alveolar damage	13.18	10.88	16	48120	1940	29902402
Electrocardiogram abnormal	12.93	10.88	29	48107	5863	29898479
Hypokalaemia	12.73	10.88	130	48006	50062	29854280
Necrotising ulcerative gingivostomatitis	12.65	10.88	5	48131	89	29904253
Immune-mediated hepatitis	12.60	10.88	12	48124	1104	29903238
Product dose omission issue	12.49	10.88	91	48045	91540	29812802
Faecaloma	12.38	10.88	24	48112	4381	29899961
Neoplasm	12.36	10.88	23	48113	4073	29900269
Proctitis	12.07	10.88	16	48120	2118	29902224
Blood magnesium decreased	12.05	10.88	27	48109	5456	29898886
Intracranial mass	12.03	10.88	12	48124	1169	29903173
Sepsis	11.97	10.88	314	47822	146081	29758261
Seizure	11.93	10.88	101	48035	98374	29805968
Biopsy intestine abnormal	11.92	10.88	3	48133	10	29904332
Megacolon	11.90	10.88	14	48122	1643	29902699
Feeling abnormal	11.78	10.88	49	48087	56707	29847635
Musculoskeletal stiffness	11.78	10.88	25	48111	35856	29868486
Blood creatine phosphokinase increased	11.70	10.88	34	48102	43814	29860528
Medication error	11.56	10.88	10	48126	20962	29883380
Splenic vein thrombosis	11.55	10.88	7	48129	325	29904017
Device related infection	11.50	10.88	56	48080	16959	29887383
Sedation	11.45	10.88	6	48130	16367	29887975
Dermatitis acneiform	11.38	10.88	27	48109	5662	29898680
Anal abscess	11.18	10.88	25	48111	5044	29899298
Aggression	11.08	10.88	27	48109	36880	29867462
Angina pectoris	11.06	10.88	19	48117	29499	29874843
Generalised oedema	11.00	10.88	43	48093	11842	29892500
Drug reaction with eosinophilia and systemic symptoms	10.99	10.88	18	48118	28470	29875872
Transcription medication error	10.98	10.88	5	48131	128	29904214
Enzyme inhibition	10.95	10.88	3	48133	15	29904327
Creatinine renal clearance abnormal	10.95	10.88	6	48130	230	29904112
Injection site pain	10.92	10.88	20	48116	30290	29874052

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
FDA EPC	N0000175690	Opioid Agonist
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

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)

None

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
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 H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.52		DRUG MATRIX
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
Glutamate receptor ionotropic, NMDA 2D	Ion channel	O15399	NMDE4_HUMAN					WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2C	Ion channel	Q14957	NMDE3_HUMAN					WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2B	Ion channel	Q13224	NMDE2_HUMAN					WOMBAT-PK
Somatostatin receptor type 5	GPCR	P35346	SSR5_HUMAN		Ki	5.34		WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		Ki	6.91		WOMBAT-PK
Calmodulin	Cytosolic other	P0DP23 P0DP24 P0DP25	CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN					WOMBAT-PK
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	6.81		WOMBAT-PK
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	Ion channel	O00555	CAC1A_HUMAN					WOMBAT-PK
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	5		WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		IC50	5.70		WOMBAT-PK
Glutamate receptor ionotropic, NMDA 2A	Ion channel	Q12879	NMDE1_HUMAN					WOMBAT-PK
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.63		CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.23		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
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.68		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
Delta-type opioid receptor	GPCR		OPRD_RAT		Ki	7.30		CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.80		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.21		CHEMBL

External reference:

ID	Source
4019804	VUID
N0000147893	NUI
D00729	KEGG_DRUG
34552-83-5	SECONDARY_CAS_RN
4019178	VANDF
4019804	VANDF
C0591635	UMLSCUI
CHEBI:6533	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	0363-1176	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	16 sections
loperamide hydrochloride	HUMAN OTC DRUG LABEL	1	0363-1645	SOLUTION	1 mg	ORAL	ANDA	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	0615-8012	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
Loperamide HCl	HUMAN OTC DRUG LABEL	1	11673-520	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	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