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

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	945	57808-66-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: domperidone betadex domperidone betacyclodextrin domperidone motilium peridon domperidone maleate	A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Molecular weight: 425.92 Formula: C22H24ClN5O2 CLOGP: 4.27 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 67.92 ALOGS: -3.66 ROTB: 5

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	P
0.12	g	R

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	15 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	3.40 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	9.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	7.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1982	YEAR INTRODUCED

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	82.08	11.61	227	32585	677611	45975639
Vomiting	79.67	11.61	567	32245	452227	46201023
Neutropenic sepsis	78.78	11.61	67	32745	12257	46640993
Completed suicide	71.79	11.61	9	32803	145911	46507339
Premature labour	71.35	11.61	61	32751	11238	46642012
Hyperprolactinaemia	69.06	11.61	36	32776	2896	46650354
Electrocardiogram QT prolonged	64.07	11.61	123	32689	51202	46602048
Product dose omission issue	61.26	11.61	21	32791	168499	46484751
Gastric pH decreased	54.24	11.61	17	32795	355	46652895
Cestode infection	54.18	11.61	16	32796	271	46652979
Torsade de pointes	43.42	11.61	48	32764	12106	46641144
Akathisia	41.43	11.61	38	32774	7676	46645574
Lip pruritus	41.20	11.61	15	32797	501	46652749
H1N1 influenza	40.12	11.61	20	32792	1464	46651786
Decreased appetite	39.44	11.61	252	32560	193584	46459666
Magnesium deficiency	39.32	11.61	14	32798	438	46652812
Arterial occlusive disease	38.92	11.61	30	32782	4774	46648476
Pituitary tumour benign	37.77	11.61	20	32792	1661	46651589
Premenstrual syndrome	37.33	11.61	15	32797	658	46652592
Hypokalaemia	37.12	11.61	141	32671	87883	46565367
Hyponatraemia	36.87	11.61	155	32657	101177	46552073
Subileus	36.46	11.61	24	32788	2979	46650271
Stoma site erythema	35.43	11.61	17	32795	1145	46652105
Gangrene	35.18	11.61	28	32784	4667	46648583
Derealisation	34.77	11.61	15	32797	788	46652462
On and off phenomenon	34.60	11.61	20	32792	1971	46651279
Pulmonary malformation	34.31	11.61	9	32803	96	46653154
Lichen sclerosus	32.55	11.61	15	32797	922	46652328
Stoma site discharge	32.42	11.61	19	32793	1921	46651329
Dyskinesia	32.08	11.61	66	32746	28859	46624391
Respiratory tract malformation	31.82	11.61	8	32804	71	46653179
Depersonalisation/derealisation disorder	31.47	11.61	15	32797	995	46652255
Cogwheel rigidity	31.43	11.61	17	32795	1473	46651777
Injection site erythema	31.26	11.61	7	32805	74420	46578830
Lung diffusion test decreased	31.03	11.61	13	32799	635	46652615
Drug abuse	30.95	11.61	4	32808	63404	46589846
Forced vital capacity decreased	29.89	11.61	14	32798	893	46652357
Polymenorrhoea	29.43	11.61	15	32797	1151	46652099
Dissociation	27.78	11.61	17	32795	1860	46651390
Menstruation delayed	27.43	11.61	16	32796	1604	46651646
General physical health deterioration	25.06	11.61	153	32659	115616	46537634
Hypomagnesaemia	25.01	11.61	51	32761	22159	46631091
Dystonia	24.97	11.61	35	32777	11222	46642028
Faecaloma	24.95	11.61	29	32783	7723	46645527
Pyrexia	24.86	11.61	363	32449	348439	46304811
Nightmare	24.78	11.61	43	32769	16555	46636695
Febrile neutropenia	24.38	11.61	131	32681	94496	46558754
Lung cyst	24.19	11.61	7	32805	110	46653140
Contraindicated product administered	24.19	11.61	13	32799	79934	46573316
Thyroid stimulating immunoglobulin increased	24.08	11.61	7	32805	112	46653138
Systemic lupus erythematosus	23.87	11.61	8	32804	65172	46588078
Drug hypersensitivity	23.51	11.61	90	32722	243735	46409515
Body temperature fluctuation	23.14	11.61	15	32797	1815	46651435
Oral candidiasis	23.08	11.61	43	32769	17489	46635761
Limbic encephalitis	23.04	11.61	8	32804	232	46653018
Rheumatoid arthritis	22.94	11.61	89	32723	240126	46413124
Duodenal stenosis	22.21	11.61	10	32802	582	46652668
Hypoaesthesia oral	22.20	11.61	32	32780	10527	46642723
Muscle rigidity	22.14	11.61	31	32781	9930	46643320
Vascular encephalopathy	21.93	11.61	9	32803	417	46652833
Maternal exposure during pregnancy	21.72	11.61	24	32788	102525	46550725
Gamma-glutamyltransferase increased	21.69	11.61	60	32752	31680	46621570
Glomerulonephritis chronic	21.57	11.61	7	32805	164	46653086
Nausea	21.22	11.61	632	32180	686822	45966428
Abdominal pain	21.21	11.61	251	32561	229780	46423470
Toxicity to various agents	21.17	11.61	77	32735	211689	46441561
Abdominal discomfort	20.96	11.61	47	32765	151118	46502132
Feeling of despair	20.89	11.61	14	32798	1791	46651459
Sensory loss	20.85	11.61	25	32787	6877	46646373
Respiratory depth decreased	20.46	11.61	5	32807	39	46653211
Constipation	20.23	11.61	199	32613	173898	46479352
Chronic sinusitis	19.95	11.61	21	32791	5012	46648238
Hyperchlorhydria	19.80	11.61	12	32800	1290	46651960
Injection site pain	19.64	11.61	28	32784	107124	46546126
Acute hepatic failure	19.25	11.61	36	32776	14685	46638565
Therapeutic product effect decreased	19	11.61	18	32794	82583	46570667
Hallucination, auditory	18.92	11.61	30	32782	10726	46642524
Arthropathy	18.86	11.61	19	32793	84681	46568569
Cardiac failure congestive	18.85	11.61	22	32790	91728	46561522
Restless legs syndrome	18.58	11.61	37	32775	15806	46637444
Abortion spontaneous	18.54	11.61	4	32808	43642	46609608
Freezing phenomenon	18.41	11.61	12	32800	1465	46651785
Treatment failure	18.41	11.61	23	32789	93064	46560186
Lower respiratory tract infection	18.28	11.61	82	32730	55007	46598243
Therapeutic product effect incomplete	18.01	11.61	17	32795	78136	46575114
Lung disorder	17.94	11.61	69	32743	43235	46610015
Adrenal suppression	17.72	11.61	10	32802	941	46652309
Mucosal inflammation	17.72	11.61	64	32748	38912	46614338
Drooling	17.61	11.61	16	32796	3193	46650057
Cholestasis	17.56	11.61	50	32762	26843	46626407
Maternal exposure during breast feeding	17.49	11.61	15	32797	2774	46650476
Oral cavity fistula	17.39	11.61	9	32803	713	46652537
Injection site reaction	17.30	11.61	6	32806	47843	46605407
Confusional state	17.25	11.61	180	32632	159712	46493538
Muscle disorder	17.19	11.61	18	32794	4268	46648982
Galactorrhoea	17.15	11.61	17	32795	3780	46649470
Bronchopulmonary aspergillosis allergic	17.11	11.61	9	32803	737	46652513
Psoriasis	17.08	11.61	18	32794	78586	46574664
Adverse drug reaction	17.04	11.61	5	32807	44357	46608893
Urinary retention	16.57	11.61	48	32764	26013	46627237
Rash maculo-papular	16.45	11.61	50	32762	27824	46625426
Weight decreased	16.41	11.61	223	32589	210626	46442624
Total lung capacity decreased	16.30	11.61	10	32802	1099	46652151
Infusion site vesicles	16.24	11.61	7	32805	367	46652883
Psoriatic arthropathy	16.15	11.61	3	32809	36376	46616874
Parosmia	16.00	11.61	17	32795	4099	46649151
Mental disorder	15.93	11.61	43	32769	22382	46630868
Rash	15.92	11.61	167	32645	356345	46296905
Menstrual disorder	15.83	11.61	17	32795	4151	46649099
Stoma complication	15.82	11.61	6	32806	225	46653025
Adrenal insufficiency	15.81	11.61	31	32781	13093	46640157
Feeling abnormal	15.66	11.61	41	32771	125019	46528231
Synovitis	15.65	11.61	12	32800	61063	46592187
Unresponsive to stimuli	15.63	11.61	54	32758	32120	46621130
Feeling of body temperature change	15.55	11.61	17	32795	4235	46649015
Hypersensitivity	15.45	11.61	54	32758	150267	46502983
Mydriasis	15.31	11.61	27	32785	10526	46642724
Paranoia	15.23	11.61	27	32785	10570	46642680
Sprue-like enteropathy	15.10	11.61	7	32805	436	46652814
Anti-thyroid antibody positive	15.07	11.61	7	32805	438	46652812
Cardio-respiratory arrest	15.04	11.61	12	32800	59857	46593393
Dysaesthesia pharynx	14.88	11.61	5	32807	131	46653119
Impaired gastric emptying	14.87	11.61	23	32789	8049	46645201
Wrong technique in product usage process	14.85	11.61	10	32802	54412	46598838
Hepatocellular injury	14.74	11.61	50	32762	29472	46623778
Injection site swelling	14.68	11.61	5	32807	40322	46612928
Dermatitis exfoliative generalised	14.56	11.61	14	32798	2999	46650251
Folate deficiency	14.51	11.61	11	32801	1707	46651543
Injection site pruritus	14.34	11.61	5	32807	39738	46613512
Microvillous inclusion disease	14.17	11.61	3	32809	11	46653239
Thyroxine free increased	14.17	11.61	8	32804	754	46652496
Bezoar	14.05	11.61	10	32802	1409	46651841
Stoma site pain	14.02	11.61	9	32803	1071	46652179
Neck pain	14.00	11.61	11	32801	55295	46597955
Overdose	13.89	11.61	32	32780	101947	46551303
Hallucinations, mixed	13.40	11.61	15	32797	3834	46649416
Cerebral calcification	13.33	11.61	5	32807	182	46653068
Repetitive strain injury	13.30	11.61	5	32807	183	46653067
Lung opacity	13.26	11.61	9	32803	1175	46652075
Intention tremor	13.19	11.61	6	32806	358	46652892
Functional residual capacity decreased	13.17	11.61	4	32808	75	46653175
Depressed level of consciousness	13.03	11.61	67	32745	47502	46605748
Stoma site inflammation	13.00	11.61	7	32805	601	46652649
Onychoclasis	12.94	11.61	17	32795	5127	46648123
Dehydration	12.93	11.61	170	32642	159370	46493880
Pseudocholinesterase deficiency	12.88	11.61	4	32808	81	46653169
Blood sodium decreased	12.85	11.61	39	32773	21687	46631563
Drug interaction	12.74	11.61	207	32605	202887	46450363
Infertility	12.64	11.61	7	32805	635	46652615
Gastritis fungal	12.61	11.61	4	32808	87	46653163
Plasma cell myeloma	12.37	11.61	8	32804	44470	46608780
Intestinal perforation	12.31	11.61	25	32787	10826	46642424
Gastric disorder	12.27	11.61	44	32768	26661	46626589
Rhinalgia	12.19	11.61	8	32804	988	46652262
Hospitalisation	12.18	11.61	16	32796	63369	46589881
Injury	12.13	11.61	8	32804	44019	46609231
Gingival pain	12.11	11.61	18	32794	6085	46647165
Serotonin syndrome	12.07	11.61	41	32771	24179	46629071
Altered state of consciousness	12.06	11.61	40	32772	23308	46629942
Delirium	12.04	11.61	55	32757	37173	46616077
Pneumonia aspiration	11.99	11.61	49	32763	31556	46621694
Myopathy	11.96	11.61	22	32790	8859	46644391
Chronic obstructive pulmonary disease	11.64	11.61	14	32798	57619	46595631
Internal haemorrhage	11.63	11.61	15	32797	4440	46648810

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
Vomiting	54.34	12.32	245	15606	219573	29717054
Drug ineffective	40.66	12.32	74	15777	340313	29596314
Aspiration	29.47	12.32	32	15819	10519	29926108
Impaired gastric emptying	28.61	12.32	19	15832	3187	29933440
Completed suicide	27.81	12.32	9	15842	99483	29837144
Neutropenic sepsis	27.43	12.32	32	15819	11377	29925250
Lower respiratory tract infection	27.34	12.32	50	15801	26664	29909963
Urine sodium decreased	27.03	12.32	8	15843	184	29936443
Toxicity to various agents	26.42	12.32	33	15818	177150	29759477
Dyskinesia	26.42	12.32	44	15807	21790	29914837
On and off phenomenon	25.47	12.32	17	15834	2874	29933753
Oesophagitis	24.66	12.32	30	15821	11141	29925486
General physical health deterioration	24.28	12.32	111	15740	99833	29836794
Oesophageal haemorrhage	24.02	12.32	12	15839	1176	29935451
Saliva altered	23.49	12.32	7	15844	165	29936462
Product dose omission issue	22.75	12.32	10	15841	91621	29845006
Nausea	22.56	12.32	248	15603	296709	29639918
Neutrophil count decreased	22.44	12.32	61	15790	42393	29894234
Impulse-control disorder	22.20	12.32	12	15839	1383	29935244
Gastroenteritis	22.08	12.32	31	15820	13235	29923392
Drug abuse	21.94	12.32	8	15843	82064	29854563
Hypomania	21.67	12.32	14	15837	2242	29934385
Hyperkinesia	20.10	12.32	13	15838	2085	29934542
Intentional medical device removal by patient	18.91	12.32	7	15844	328	29936299
Akinesia	18.03	12.32	13	15838	2487	29934140
Dysphagia	17.69	12.32	68	15783	56630	29879997
Pyroglutamic acidosis	17.55	12.32	5	15846	100	29936527
Device dislocation	17.19	12.32	17	15834	5014	29931613
Hepatocellular injury	17.01	12.32	40	15811	25431	29911196
Pneumonia aspiration	16.78	12.32	51	15800	37729	29898898
Gambling disorder	16.65	12.32	11	15840	1829	29934798
Decreased appetite	16.20	12.32	135	15716	149775	29786852
Stoma site discharge	16.13	12.32	10	15841	1491	29935136
Paralysis recurrent laryngeal nerve	15.80	12.32	4	15847	50	29936577
Colitis ischaemic	15.21	12.32	17	15834	5769	29930858
Inappropriate antidiuretic hormone secretion	15.15	12.32	24	15827	11398	29925229
Dyskinesia oesophageal	15.06	12.32	4	15847	61	29936566
Post inflammatory pigmentation change	13.87	12.32	5	15846	217	29936410
Deafness bilateral	13.67	12.32	8	15843	1074	29935553
Drug interaction	13.02	12.32	162	15689	199406	29737221
Shock symptom	13.01	12.32	4	15847	105	29936522
Lumbosacral plexus injury	12.95	12.32	3	15848	25	29936602
Hypocalcaemia	12.60	12.32	32	15819	21344	29915283
Platelet count increased	12.47	12.32	19	15832	8723	29927904
Skin erosion	12.38	12.32	9	15842	1744	29934883
Regurgitation	12.32	12.32	7	15844	889	29935738

Pharmacologic Action:

Source	Code	Description
ATC	A03FA03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS PROPULSIVES Propulsives
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018492	Dopamine Antagonists
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
CHEBI has role	CHEBI:48561	dopamine blocker
CHEBI has role	CHEBI:50919	antiemetico

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Nausea and vomiting	indication	16932000
Acute gastric ulcer with perforation	contraindication	19850005
Torsades de pointes	contraindication	31722008
Acute nephropathy	contraindication	58574008
Acute gastric ulcer with hemorrhage	contraindication	89748001
Prolonged QT interval	contraindication	111975006
Gastrointestinal obstruction	contraindication	126765001
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Congenital long QT syndrome	contraindication	442917000
Pituitary Prolactinoma	contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.45	acidic
pKa2	10.04	acidic
pKa3	7.79	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
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.40		IUPHAR	IUPHAR
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.77		DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.99		DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.79		DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.59		DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.96		DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.78		DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.16		DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.01		DRUG MATRIX
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.81		DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.83		DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.94		DRUG MATRIX
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	5.55		DRUG MATRIX
Calmodulin	Cytosolic other	P0DP23 P0DP24 P0DP25	CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN					WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	6.28		WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		Ki	5.10		WOMBAT-PK
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	5.52		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	6.65		WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.79		WOMBAT-PK
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.10		CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.46		CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	4.83		CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.64		CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN					WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.06		DRUG MATRIX
D(3) dopamine receptor	GPCR		DRD3_RAT		Ki	7.93		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	9.28		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	6.55		CHEMBL

External reference:

ID	Source
4025225	VUID
N0000171760	NUI
D01745	KEGG_DRUG
83898-65-1	SECONDARY_CAS_RN
4025225	VANDF
C0013015	UMLSCUI
CHEBI:31515	CHEBI
CHEMBL219916	ChEMBL_ID
DB01184	DRUGBANK_ID
D004294	MESH_DESCRIPTOR_UI
3151	PUBCHEM_CID
965	IUPHAR_LIGAND_ID
4110	INN_ID
5587267Z69	UNII
203007	RXNORM
003454	NDDF
005091	NDDF
32955006	SNOMEDCT_US
384972001	SNOMEDCT_US
387181004	SNOMEDCT_US

Pharmaceutical products:

None