Identification

Name
Domperidone
Accession Number
DB01184
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.

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 425.911
Monoisotopic: 425.161852744
Chemical Formula
C22H24ClN5O2
Synonyms
  • 1-(3-(4-(5-chloro-2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)piperidin-1-yl)propyl)-1H-benzo[d]imidazol-2(3H)-one
  • 5-chloro-1-(1-(3-(2-oxo-1-benzimidazolinyl)propyl)-4-piperidyl)-2-benzimidazolinone
  • 5-chloro-1-(1-(3-(2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)propyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
  • 5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-propyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one
  • Domperidona
  • Domperidone
  • Domperidonum
External IDs
  • R 33,812
  • R-33812

Pharmacology

Indication

For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

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 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

TargetActionsOrganism
ADopamine D2 receptor
antagonist
Humans
ADopamine D3 receptor
antagonist
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

91%-93%

Metabolism

Hover over products below to view reaction partners

Route of elimination
Not Available
Half-life

7 hours

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Side effects include galactorrhea, gynecomastia, or menstrual irregularities.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Domperidone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Domperidone can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Domperidone can be increased when it is combined with Abiraterone.
AcalabrutinibThe metabolism of Domperidone can be decreased when combined with Acalabrutinib.
AcebutololThe risk or severity of QTc prolongation can be increased when Acebutolol is combined with Domperidone.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Domperidone.
AcetaminophenThe metabolism of Domperidone can be decreased when combined with Acetaminophen.
AclidiniumThe therapeutic efficacy of Domperidone can be decreased when used in combination with Aclidinium.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Domperidone.
AcyclovirThe metabolism of Domperidone can be decreased when combined with Acyclovir.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take before a meal. Take 15-30 minutes before meals.

Products

Product Ingredients
IngredientUNIICASInChI Key
Domperidone maleate899U5WF46A83898-65-1OAUUYDZHCOULIO-BTJKTKAUSA-N
International/Other Brands
Euciton (Roux-Ocefa) / Moperidona (Sidus) / Motilium (Janssen) / Nauzelin (Kyowa Hakko Kirin)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DomperidoneTabletOralSivem Pharmaceuticals Ulc1998-09-03Not applicableCanada flag
DomperidoneTabletOralSanis Health Inc2010-05-12Not applicableCanada flag
DomperidoneTabletOralRanbaxy Inc.Not applicableNot applicableCanada flag
Domperidone-10TabletOralPro Doc Limitee1998-07-13Not applicableCanada flag
MotilidoneTabletOralTechnilab Pharma Inc.1997-09-172005-08-05Canada flag
Motilium Tab 10mgTabletOralJanssen Pharmaceuticals1990-12-312002-01-07Canada flag
Prz-domperidoneTabletOralPharmaris Canada Inc2018-04-02Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-domperidone - Tab 10mgTabletOralApotex Corporation1997-09-17Not applicableCanada flag
Ava-domperidoneTabletOralAvanstra Inc2011-09-152014-08-21Canada flag
Bio-domperidoneTabletOralBiomed Pharma2016-04-26Not applicableCanada flag
Dom-domperidoneTabletOralDominion Pharmacal1998-09-17Not applicableCanada flag
Ftp-domperidone MaleateTabletOralGmd Distribution Inc.1998-10-092005-08-05Canada flag
Ipg-domperidoneTabletOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada flag
Jamp-domperidoneTabletOralJamp Pharma Corporation2011-10-07Not applicableCanada flag
Mar-domperidoneTabletOralMarcan Pharmaceuticals Inc2014-01-02Not applicableCanada flag
Mylan-domperidoneTabletOralMylan Pharmaceuticals2006-03-202017-01-09Canada flag
Nu-domperidone 10 Mg TabletsTabletOralNu Pharm Inc1998-03-182012-09-04Canada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
A03FA03 — Domperidone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzimidazoles
Sub Class
Not Available
Direct Parent
Benzimidazoles
Alternative Parents
Piperidines / N-substituted imidazoles / Benzenoids / Aryl chlorides / Heteroaromatic compounds / Ureas / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds
show 3 more
Substituents
Amine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Azole / Benzenoid / Benzimidazole / Heteroaromatic compound / Hydrocarbon derivative
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
benzimidazoles, heteroarylpiperidine (CHEBI:31515)

Chemical Identifiers

UNII
5587267Z69
CAS number
57808-66-9
InChI Key
FGXWKSZFVQUSTL-UHFFFAOYSA-N
InChI
InChI=1S/C22H24ClN5O2/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30)
IUPAC Name
5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)propyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
SMILES
ClC1=CC2=C(C=C1)N(C1CCN(CCCN3C(=O)NC4=CC=CC=C34)CC1)C(=O)N2

References

Synthesis Reference

Vanderberk, J., Kennis, L.E.J., Van der Aa, M.J.M.C. and Van Heertum, A.H.M.T.; U.S. Patents 4,066,772; January 3,1978; 4.1 10,333; August 29,1978; 4,126,687; November 21, 1978; 4,126,688; November 21,1978; 4,160,836; July 10,1979 and 4,175,129; November 20,1979; all assigned to Janssen Pharmaceutica NV (Belgium).

General References
  1. Silvers D, Kipnes M, Broadstone V, Patterson D, Quigley EM, McCallum R, Leidy NK, Farup C, Liu Y, Joslyn A: Domperidone in the management of symptoms of diabetic gastroparesis: efficacy, tolerability, and quality-of-life outcomes in a multicenter controlled trial. DOM-USA-5 Study Group. Clin Ther. 1998 May-Jun;20(3):438-53. [PubMed:9663360]
Human Metabolome Database
HMDB0015315
KEGG Drug
D01745
PubChem Compound
3151
PubChem Substance
46508314
ChemSpider
3039
BindingDB
50241107
RxNav
3626
ChEBI
31515
ChEMBL
CHEMBL219916
ZINC
ZINC000004175569
Therapeutic Targets Database
DAP001368
PharmGKB
PA134711056
Guide to Pharmacology
GtP Drug Page
Wikipedia
Domperidone
AHFS Codes
  • 56:32.00 — Prokinetic Agents
MSDS
Download (73.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedDiagnosticGastro-esophageal Reflux Disease (GERD)1
4CompletedTreatmentBreast Cancer1
4CompletedTreatmentDomperidone Overdose / Feeding Intolerance / Gastric Retention / Premature Births1
4CompletedTreatmentDyspepsia1
4CompletedTreatmentGastro-esophageal Reflux Disease (GERD)1
4CompletedTreatmentIdiopathic Parkinson's Disease1
4CompletedTreatmentInsufficient Lactation1
4RecruitingPreventionBowel preparation therapy1
4Unknown StatusScreeningCardiovascular Events / Gastro-esophageal Reflux Disease (GERD) / Safety Issues1
4Unknown StatusTreatmentDiabetic Gastroparesis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Professional Co.
Dosage Forms
FormRouteStrength
TabletOral
SyrupOral
CapsuleOral30 mg
Syrup5 mg/5mL
SuspensionOral5 mg/5mL
Tablet, film coatedOral10 MG
Tablet10 MG
SuspensionOral0.1 g
SuspensionOral100 mg
Tablet, coatedOral10 mg
Capsule30 mg
Capsule60 mg
CapsuleOral15 mg
Tablet, film coatedOral
TabletOral10 mg
Capsule, delayed release pelletsOral30 mg
Suspension
Granule10 MG
InjectionIntramuscular; Intravenous10 mg/2ml
Solution / drops20 ML
Solution / dropsOral10 mg/ml
Solution / dropsOral20 mg/ml
Suppository10 MG
Suppository30 MG
Suppository60 MG
SuspensionOral1 MG/ML
Syrup1 MG/ML
Tablet20 MG
Tablet, coated10 MG
Tablet, film coated10 mg
SuspensionOral
Tablet
CapsuleOral20 mg
Solution / drops; suspension / drops
Tablet, soluble
Prices
Unit descriptionCostUnit
Domperidone bp powder55.2USD g
Ratio-Domperidone Maleate 10 mg Tablet0.16USD tablet
Apo-Domperidone 10 mg Tablet0.16USD tablet
Mylan-Domperidone 10 mg Tablet0.16USD tablet
Novo-Domperidone 10 mg Tablet0.16USD tablet
Nu-Domperidone 10 mg Tablet0.16USD tablet
Pms-Domperidone 10 mg Tablet0.15USD tablet
Ran-Domperidone 10 mg Tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)242.5 °CVanderberk, J., Kennis, L.E.J., Van der Aa, M.J.M.C. and Van Heertum, A.H.M.T.; U.S. Patents 4,066,772; January 3,1978; 4.1 10,333; August 29,1978; 4,126,687; November 21, 1978; 4,126,688; November 21,1978; 4,160,836; July 10,1979 and 4,175,129; November 20,1979; all assigned to Janssen Pharmaceutica NV (Belgium).
water solubility0.986 mg/LNot Available
logP3.90EL TAYER,N ET AL. (1985)
pKa7.9EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.0925 mg/mLALOGPS
logP3.7ALOGPS
logP2.9ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)12.52ChemAxon
pKa (Strongest Basic)7.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area67.92 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity119.37 m3·mol-1ChemAxon
Polarizability45.61 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9967
Blood Brain Barrier+0.8686
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.7029
P-glycoprotein inhibitor IInhibitor0.7244
P-glycoprotein inhibitor IIInhibitor0.628
Renal organic cation transporterInhibitor0.6546
CYP450 2C9 substrateNon-substrate0.7974
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.6392
CYP450 1A2 substrateInhibitor0.8737
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.5577
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8695
Ames testNon AMES toxic0.6608
CarcinogenicityNon-carcinogens0.922
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9828 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7527
hERG inhibition (predictor II)Inhibitor0.917
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00xr-0700900000-fbaf0980af220c88125f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-0300900000-912de932579a7a2a6e2f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0900300000-877326ac38180c1229cd

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Cavallotti C, Nuti F, Bruzzone P, Mancone M: Age-related changes in dopamine D2 receptors in rat heart and coronary vessels. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):412-8. [PubMed:12010185]
  2. Osinski MA, Uchic ME, Seifert T, Shaughnessy TK, Miller LN, Nakane M, Cox BF, Brioni JD, Moreland RB: Dopamine D2, but not D4, receptor agonists are emetogenic in ferrets. Pharmacol Biochem Behav. 2005 May;81(1):211-9. [PubMed:15894081]
  3. de Mey C, Enterling D, Meineke I, Yeulet S: Interactions between domperidone and ropinirole, a novel dopamine D2-receptor agonist. Br J Clin Pharmacol. 1991 Oct;32(4):483-8. [PubMed:1683559]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  5. Ali I, Gupta VK, Singh P, Pant HV: Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31. doi: 10.1016/j.talanta.2005.06.027. Epub 2005 Jul 22. [PubMed:18970411]
Details
2. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Freedman SB, Patel S, Marwood R, Emms F, Seabrook GR, Knowles MR, McAllister G: Expression and pharmacological characterization of the human D3 dopamine receptor. J Pharmacol Exp Ther. 1994 Jan;268(1):417-26. [PubMed:8301582]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Chang SY, Fancher RM, Zhang H, Gan J: Mechanism-based inhibition of human cytochrome P4503A4 by domperidone. Xenobiotica. 2010 Feb;40(2):138-45. doi: 10.3109/00498250903406762. [PubMed:20082577]
  2. Simard C, Michaud V, Gibbs B, Masse R, Lessard E, Turgeon J: Identification of the cytochrome P450 enzymes involved in the metabolism of domperidone. Xenobiotica. 2004 Nov-Dec;34(11-12):1013-23. [PubMed:15801545]
  3. Michaud V, Simard C, Turgeon J: Characterization of CYP3A isozymes involved in the metabolism of domperidone: role of cytochrome b5 and inhibition by ketoconazole. Drug Metab Lett. 2010 Apr;4(2):95-103. [PubMed:21281268]
  4. Flockhart Table of Drug Interactions [Link]
  5. Health Canada Approved Drug Products: Domperidone Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Ward BA, Morocho A, Kandil A, Galinsky RE, Flockhart DA, Desta Z: Characterization of human cytochrome P450 enzymes catalyzing domperidone N-dealkylation and hydroxylation in vitro. Br J Clin Pharmacol. 2004 Sep;58(3):277-87. doi: 10.1111/j.1365-2125.2004.02156.x. [PubMed:15327587]
  2. Domperidone 10mg Tablets - Summary of Product Characteristics - eMC [Link]
  3. Domperidone FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Ward BA, Morocho A, Kandil A, Galinsky RE, Flockhart DA, Desta Z: Characterization of human cytochrome P450 enzymes catalyzing domperidone N-dealkylation and hydroxylation in vitro. Br J Clin Pharmacol. 2004 Sep;58(3):277-87. doi: 10.1111/j.1365-2125.2004.02156.x. [PubMed:15327587]
  2. Braun M, Cawello W, Boekens H, Horstmann R: Influence of domperidone on pharmacokinetics, safety and tolerability of the dopamine agonist rotigotine. Br J Clin Pharmacol. 2009 Feb;67(2):209-15. doi: 10.1111/j.1365-2125.2008.03334.x. Epub 2008 Dec 16. [PubMed:19094160]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Ward BA, Morocho A, Kandil A, Galinsky RE, Flockhart DA, Desta Z: Characterization of human cytochrome P450 enzymes catalyzing domperidone N-dealkylation and hydroxylation in vitro. Br J Clin Pharmacol. 2004 Sep;58(3):277-87. doi: 10.1111/j.1365-2125.2004.02156.x. [PubMed:15327587]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Ward BA, Morocho A, Kandil A, Galinsky RE, Flockhart DA, Desta Z: Characterization of human cytochrome P450 enzymes catalyzing domperidone N-dealkylation and hydroxylation in vitro. Br J Clin Pharmacol. 2004 Sep;58(3):277-87. doi: 10.1111/j.1365-2125.2004.02156.x. [PubMed:15327587]
  2. Braun M, Cawello W, Boekens H, Horstmann R: Influence of domperidone on pharmacokinetics, safety and tolerability of the dopamine agonist rotigotine. Br J Clin Pharmacol. 2009 Feb;67(2):209-15. doi: 10.1111/j.1365-2125.2008.03334.x. Epub 2008 Dec 16. [PubMed:19094160]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186]
  2. Schinkel AH, Wagenaar E, Mol CA, van Deemter L: P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest. 1996 Jun 1;97(11):2517-24. [PubMed:8647944]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2020 01:55

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