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QuickView for Domperidone (compound)

Summary
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PubChem

PubChem Compound 3151

PubChem Compound 3151

Name:	Domperidone
PubChem Compound ID:	3151
Description:	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 formula:	C₂₂H₂₄ClN₅O₂
Molecular weight:	425.911 g/mol
Synonyms:	Prestwick1_000461; BRN 0903774; Domperidone [USAN:BAN:INN:JAN]; Domperidone; 57808-66-9; Prestwick0_000461; NCGC00015306-01; DivK1c_006921; EINECS 260-968-7; Domperidone (JAN/USAN). show more » Prestwick1_000461; BRN 0903774; Domperidone [USAN:BAN:INN:JAN]; Domperidone; 57808-66-9; Prestwick0_000461; NCGC00015306-01; DivK1c_006921; EINECS 260-968-7; Domperidone (JAN/USAN); R 33,812; nsc299589; KBio1_001865; Spectrum4_000087; Lopac-D-122; 2H-Benzimidazol-2-one, 5-chloro-1-(1-(3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl)-4-piperidinyl)-1,3-dihydro-; 2H-Benzimidazol-2-one, 5-chloro-1-[1-[3- (2, 3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl]-4-piperidinyl]-1, 3-dihydro-; 83898-65-1; SPBio_002501; R-33812; Prestwick_794; 2H-Benzimidazol-2-one, 1,3-dihydro-5-chloro-1-(1-(3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl)-4-piperidinyl)-; D01745; KBio2_000871; KBioGR_000354; 5-Chloro-1-[1-[3-(2-oxo-1-benzimidazolinyl)propyl]-4-piperidyl]-2- benzimidazolinone; KBioSS_000871; Nauzelin; Motilium (TN); NCIStruc2_001819; EU-0100427; 99497-03-7; KBio2_003439; SpecPlus_000825; 5-Chloro-1-(1-(3-(2-oxo-1-benzimidazolinyl)propyl)-4-piperidyl)-2-benzimidazolinone; KW 5338; NCGC00014670; NSC-299589; KBio2_006007; Motilium; Spectrum_000391; 5-chloro-1-(1-(3-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)propyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one; Domperidona [INN-Spanish]; 5-24-02-00402 (Beilstein Handbook Reference); NCI60_002512; Domperidonum [INN-Latin]; NCIStruc1_001686; KW-5338 show less «

DrugBank

Identification

Name:	Domperidone
Name (isomeric):	DB01184
Drug Type:	small molecule
Description:	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.
Brand:	Nauzelin, Lopac-D-122, Motilium
Category:	Antiemetics, Dopamine Antagonists
CAS number:	57808-66-9

Pharmacology

Indication:	For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.
Pharmacology:	Domperidone is 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.
Mechanism of Action:	Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lower... show more » Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting show less «
Absorption:	Fast
Protein binding:	91%-93%
Half Life:	7 hours
Toxicity:	Side effects include galactorrhea, gynecomastia, or menstrual irregularities.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take 15 to 30 minutes before meals.

Drug interaction:

Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
Zuclopenthixol	Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).

Targets

D(2) dopamine receptor

D(3) dopamine receptor

Enzymes

Cytochrome P450 3A5

Cytochrome P450 3A7

Cytochrome P450 3A4

Cytochrome P450 1A2

Cytochrome P450 2B6

Cytochrome P450 2C8

Cytochrome P450 2D6

Transporters

Multidrug resistance protein 1