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Identification
NameBromocriptine
Accession NumberDB01200  (APRD00622)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity. It is indicated for the management of signs and symptoms of Parkinsonian Syndrome. Bromocriptine also inhibits prolactin secretion and may be used to treat dysfunctions associated with hyperprolactinemia. It also causes sustained suppression of somatotropin (growth hormone) secretion in some patients with acromegaly. Bromocriptine has been associated with pulmonary fibrosis.

Structure
Thumb
Synonyms
(5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-3',6',18-trioxoergotaman
(5'alpha)-2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione
(5'alpha)-2-bromo-12'-hydroxy-5'-isobutyl-2'-isopropyl-3',6',18-trioxoergotaman
2-Bromo-alpha-ergocryptine
2-Bromo-alpha-ergokryptin
2-Bromo-alpha-ergokryptine
2-bromo-α-ergocryptine
2-bromo-α-ergokryptin
2-bromo-α-ergokryptine
Bromocriptina
Bromocriptinum
Bromocryptine
Bromoergocriptine
Bromoergocryptine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bromocriptinecapsule5 mgoralAa Pharma Inc1997-01-08Not applicableCanada
Bromocriptinetablet2.5 mgoralAa Pharma Inc1994-12-31Not applicableCanada
Bromocriptinecapsule5 mgoralPharmel Inc1998-09-03Not applicableCanada
Bromocriptinetablet2.5 mgoralPharmel Inc1998-09-03Not applicableCanada
Bromocriptine-2.5 - Tab 2.5mgtablet2.5 mgoralPro Doc Limitee1996-12-312010-07-13Canada
Bromocriptine-5capsule5 mgoralPro Doc Limitee1998-08-112010-07-13Canada
Co Bromocriptine Capsules 5mgcapsule5 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Co Bromocriptine Tablets 2.5mgtablet2.5 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Cyclosettablet.8 mg/1oralSantarus, Inc.2010-11-15Not applicableUs
Dom-bromocriptinecapsule5 mgoralDominion Pharmacal1998-10-22Not applicableCanada
Dom-bromocriptinetablet2.5 mgoralDominion Pharmacal1998-10-22Not applicableCanada
Nu-bromocriptinecapsule5.0 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-bromocriptinetablet2.5 mgoralNu Pharm IncNot applicableNot applicableCanada
Parlodelcapsule, gelatin coated5 mg/1oralValidus Pharmaceuticals LLC2014-04-28Not applicableUs
Parlodeltablet2.5 mg/1oralValidus Pharmaceuticals LLC2014-06-20Not applicableUs
Parlodel Cap 5mgcapsule5 mgoralNovartis Pharmaceuticals Canada Inc1983-12-312005-09-09Canada
Parlodel Tab 2.5mgtablet2.5 mgoralNovartis Pharmaceuticals Canada Inc1976-12-312007-07-18Canada
PMS-bromocriptinecapsule5 mgoralPharmascience Inc1998-03-05Not applicableCanada
PMS-bromocriptinetablet2.5 mgoralPharmascience Inc1998-03-09Not applicableCanada
Syn-bromocriptine Cap 5mgcapsule5 mgoralSyncare Pharmaceutical Inc.1994-12-311997-08-11Canada
Syn-bromocriptine Tab 2.5mgtablet2.5 mgoralSyncare Pharmaceutical Inc.1994-12-311997-08-11Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bromocriptine Mesylatetablet2.5 mg/1oralKAISER FOUNDATION HOSPITALS2014-10-10Not applicableUs
Bromocriptine Mesylatecapsule5 mg/1oralCadila Healthcare Limited2009-01-23Not applicableUs
Bromocriptine Mesylatetablet2.5 mg/1oralPhysicians Total Care, Inc.2006-09-08Not applicableUs
Bromocriptine Mesylatetablet2.5 mg/1oralSandoz Inc1998-01-13Not applicableUs
Bromocriptine Mesylatetablet2.5 mg/1oralPaddock Laboratories, LLC2008-10-01Not applicableUs
Bromocriptine Mesylatecapsule5 mg/1oralAmerican Health Packaging2010-01-132015-12-29Us
Bromocriptine Mesylatecapsule5 mg/1oralMylan Pharmaceuticals Inc.2013-06-17Not applicableUs
Bromocriptine Mesylatecapsule5 mg/1oralZydus Pharmaceuticals (USA) Inc.2009-01-23Not applicableUs
Bromocriptine Mesylatetablet2.5 mg/1oralMylan Pharmaceuticals Inc.2013-06-06Not applicableUs
Bromocriptine Mesylatetablet2.5 mg/1oralCarilion Materials Management2008-10-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Apo-BromocriptineApotex
BagrenSerono (Brazil)
ErgosetNot Available
Parlodel SnaptabsNovartis
PravidelMeda (Germany, Sweden), Novartis (Canada, discontinued)
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Bromocriptine mesylate
ThumbNot applicableDBSALT001209
Categories
UNII3A64E3G5ZO
CAS number25614-03-3
WeightAverage: 654.595
Monoisotopic: 653.221282062
Chemical FormulaC32H40BrN5O5
InChI KeyInChIKey=OZVBMTJYIDMWIL-AYFBDAFISA-N
InChI
InChI=1S/C32H40BrN5O5/c1-16(2)12-24-29(40)37-11-7-10-25(37)32(42)38(24)30(41)31(43-32,17(3)4)35-28(39)18-13-20-19-8-6-9-22-26(19)21(27(33)34-22)14-23(20)36(5)15-18/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39)/t18-,23-,24+,25+,31-,32+/m1/s1
IUPAC Name
(4R,7R)-10-bromo-N-[(1S,2S,4R,7S)-2-hydroxy-7-(2-methylpropyl)-5,8-dioxo-4-(propan-2-yl)-3-oxa-6,9-diazatricyclo[7.3.0.0²,⁶]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide
SMILES
[H][C@@]12CCCN1C(=O)[[email protected]](CC(C)C)N1C(=O)[C@](NC(=O)[[email protected]]3CN(C)[C@]4([H])CC5=C(Br)NC6=CC=CC(=C56)C4=C3)(O[C@@]21O)C(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as ergopeptines. These are ergoline derivatives that contain a tripeptide structure attached to the basic ergoline ring in the same location as the amide group of the lysergic acid derivatives.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassErgoline and derivatives
Sub ClassLysergic acids and derivatives
Direct ParentErgopeptines
Alternative Parents
Substituents
  • Hybrid peptide
  • Ergopeptine
  • Lysergic acid amide
  • Indoloquinoline
  • Benzoquinoline
  • Quinoline-3-carboxamide
  • Pyrroloquinoline
  • N-acyl-alpha amino acid or derivatives
  • Quinoline
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • N-alkylpiperazine
  • Tetrahydropyridine
  • Benzenoid
  • Substituted pyrrole
  • Piperazine
  • Oxazolidinone
  • 1,4-diazinane
  • Aryl halide
  • Aryl bromide
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Pyrrole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Orthocarboxylic acid derivative
  • Lactam
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Alkanolamine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organobromide
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of galactorrhea due to hyperprolactinemia, prolactin-dependent menstrual disorders and infertility, prolactin-secreting adenomas, prolactin-dependent male hypogonadism, as adjunct therapy to surgery or radiotherapy for acromegaly or as monotherapy is special cases, as monotherapy in early Parksinsonian Syndrome or as an adjunct with levodopa in advanced cases with motor complications. Bromocriptine has also been used off-label to treat restless legs syndrome and neuroleptic malignant syndrome.
PharmacodynamicsBromocriptine stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors, which are associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D2 and D3 receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D2 stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D2 stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D2-receptors. It also exhibits agonist activity (in order of decreasing binding affinity) on 5-hydroxytryptamine (5-HT)1D, dopamine D3, 5-HT1A, 5-HT2A, 5-HT1B, and 5-HT2C receptors, antagonist activity on α2A-adrenergic, α2C, α2B, and dopamine D1 receptors, partial agonist activity at receptor 5-HT2B, and inactivates dopamine D4 and 5-HT7 receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT2A agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion making bromocriptine an effective agent for treating disorders associated with hypersecretion of prolactin. Pulmonary fibrosis may be associated bromocriptine’s agonist activity at 5-HT1B and 5-HT2B receptors.
Mechanism of actionThe dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
Related Articles
AbsorptionApproximately 28% of the oral dose is absorbed; however due to a substantial first pass effect, only 6% of the oral dose reaches the systemic circulation unchanged. Bromocriptine and its metabolites appear in the blood as early as 10 minutes following oral administration and peak plasma concentration are reached within 1-1.5 hours. Serum prolactin may be decreased within 2 hours or oral administration with a maximal effect achieved after 8 hours. Growth hormone concentrations in patients with acromegaly is reduced within 1-2 hours with a single oral dose of 2.5 mg and decreased growth hormone concentrations persist for at least 4-5 hours.
Volume of distributionNot Available
Protein binding90-96% bound to serum albumin
Metabolism

Completely metabolized by the liver, primarily by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment, both inactive and non-toxic. Bromocriptine is metabolized by cytochrome P450 3A4 and excreted primarily in the feces via biliary secretion.

Route of eliminationParent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.
Half life2-8 hours
ClearanceNot Available
ToxicitySymptoms of overdosage include nausea, vomiting, and severe hypotension. The most common adverse effects include nausea, headache, vertigo, constipation, light-headedness, abdominal cramps, nasal congestion, diarrhea, and hypotension.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.915
Blood Brain Barrier-0.9845
Caco-2 permeable-0.6618
P-glycoprotein substrateSubstrate0.8881
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.837
CYP450 2C9 substrateNon-substrate0.8345
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7454
CYP450 1A2 substrateNon-inhibitor0.9031
CYP450 2C9 inhibitorInhibitor0.8326
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5149
Ames testNon AMES toxic0.7879
CarcinogenicityNon-carcinogens0.9353
BiodegradationNot ready biodegradable0.9973
Rat acute toxicity2.7499 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9313
hERG inhibition (predictor II)Inhibitor0.5
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral5 mg
Tabletoral2.5 mg
Capsuleoral5 mg/1
Tabletoral2.5 mg/1
Tabletoral.8 mg/1
Capsuleoral5.0 mg
Capsule, gelatin coatedoral5 mg/1
Prices
Unit descriptionCostUnit
Bromocriptine mesylate powd384.03USD g
Parlodel 5 mg capsule9.25USD capsule
Parlodel 2.5 mg tablet5.64USD tablet
Bromocriptine Mesylate 5 mg capsule5.21USD capsule
Bromocriptine Mesylate 2.5 mg tablet2.28USD tablet
Bromocriptine 2.5 mg tablet2.18USD tablet
Apo-Bromocriptine 5 mg Capsule1.02USD capsule
Pms-Bromocriptine 5 mg Capsule1.02USD capsule
Apo-Bromocriptine 2.5 mg Tablet0.57USD tablet
Pms-Bromocriptine 2.5 mg Tablet0.57USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5468755 No1992-11-212012-11-21Us
US5716957 No1995-02-102015-02-10Us
US7888310 No2003-07-252023-07-25Us
US8137992 No2003-07-252023-07-25Us
US8137993 No2003-07-252023-07-25Us
US8137994 No2003-07-252023-07-25Us
US8431155 No2012-04-302032-04-30Us
US8613947 No2012-04-302032-04-30Us
US8877708 No2010-06-072030-06-07Us
US9192576 No2012-04-302032-04-30Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point215-218Fluckiger, E.,Troxler, F. and Hofmann, A,; US. Patent 3,752,814; August 14, 1973; assigned to Sandoz Ltd., Switzerland. Fluckiger, E., Troxler, F. and Hofmann, A.; U.S. Patent 3,752,888; August 14, 1973; assigned to Sandoz Ltd., Switzerland.
logP3.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0858 mg/mLALOGPS
logP3.2ALOGPS
logP3.89ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)9.68ChemAxon
pKa (Strongest Basic)6.71ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area118.21 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity165.51 m3·mol-1ChemAxon
Polarizability66.44 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Luigi Moro, Achille Fiori, Alberto Natali, “Processes for the preparation of pharmaceutical compositions containing bromocriptine having high stability and related products.” U.S. Patent US5066495, issued May, 1988.

US5066495
General References
  1. Banihashemi B, Albert PR: Dopamine-D2S receptor inhibition of calcium influx, adenylyl cyclase, and mitogen-activated protein kinase in pituitary cells: distinct Galpha and Gbetagamma requirements. Mol Endocrinol. 2002 Oct;16(10):2393-404. [PubMed:12351703 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  4. Malgaroli A, Vallar L, Elahi FR, Pozzan T, Spada A, Meldolesi J: Dopamine inhibits cytosolic Ca2+ increases in rat lactotroph cells. Evidence of a dual mechanism of action. J Biol Chem. 1987 Oct 15;262(29):13920-7. [PubMed:2443499 ]
  5. Nishina Y, Takano K, Yasufuku-Takano J, Teramoto A, Fujita T: Mechanism of D(2) agonist-induced inhibition of GH secretion from human GH-secreting adenoma cells. Endocr J. 2005 Dec;52(6):775-9. [PubMed:16410672 ]
  6. Vallar L, Meldolesi J: Mechanisms of signal transduction at the dopamine D2 receptor. Trends Pharmacol Sci. 1989 Feb;10(2):74-7. [PubMed:2655242 ]
  7. Vallar L, Vicentini LM, Meldolesi J: Inhibition of inositol phosphate production is a late, Ca2+-dependent effect of D2 dopaminergic receptor activation in rat lactotroph cells. J Biol Chem. 1988 Jul 25;263(21):10127-34. [PubMed:2839476 ]
External Links
ATC CodesG02CB01N04BC01
AHFS Codes
  • 28:36.20.04
PDB EntriesNot Available
FDA labelDownload (105 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Bromocriptine.
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Bromocriptine.
AprepitantThe serum concentration of Bromocriptine can be increased when it is combined with Aprepitant.
AripiprazoleThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Aripiprazole.
AsenapineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Asenapine.
BatimastatThe serum concentration of Bromocriptine can be increased when it is combined with Batimastat.
BrexpiprazoleThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Brexpiprazole.
BupropionThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Bupropion.
ChlorpromazineThe therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Bromocriptine.
ClarithromycinThe serum concentration of Bromocriptine can be increased when it is combined with Clarithromycin.
ClozapineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Clozapine.
ConivaptanThe serum concentration of Bromocriptine can be increased when it is combined with Conivaptan.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Bromocriptine.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Bromocriptine.
DasatinibThe serum concentration of Bromocriptine can be increased when it is combined with Dasatinib.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Bromocriptine.
DipivefrinBromocriptine may increase the hypertensive activities of Dipivefrin.
DroperidolThe therapeutic efficacy of Droperidol can be decreased when used in combination with Bromocriptine.
EletriptanBromocriptine may increase the vasoconstricting activities of Eletriptan.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Bromocriptine.
FluconazoleThe metabolism of Bromocriptine can be decreased when combined with Fluconazole.
FlupentixolThe therapeutic efficacy of Flupentixol can be decreased when used in combination with Bromocriptine.
FluphenazineThe therapeutic efficacy of Fluphenazine can be decreased when used in combination with Bromocriptine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Bromocriptine.
FosaprepitantThe serum concentration of Bromocriptine can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Bromocriptine can be increased when it is combined with Fusidic Acid.
GranisetronGranisetron may increase the serotonergic activities of Bromocriptine.
HaloperidolThe therapeutic efficacy of Haloperidol can be decreased when used in combination with Bromocriptine.
IdelalisibThe serum concentration of Bromocriptine can be increased when it is combined with Idelalisib.
IloperidoneThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Iloperidone.
Insulin HumanBromocriptine may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproBromocriptine may increase the hypoglycemic activities of Insulin Lispro.
IsoflurophateThe serum concentration of Bromocriptine can be increased when it is combined with Isoflurophate.
IvacaftorThe serum concentration of Bromocriptine can be increased when it is combined with Ivacaftor.
LanreotideThe serum concentration of Bromocriptine can be increased when it is combined with Lanreotide.
LeuprolideThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Leuprolide.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Bromocriptine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Bromocriptine.
LoxapineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Bromocriptine.
LuliconazoleThe serum concentration of Bromocriptine can be increased when it is combined with Luliconazole.
LurasidoneThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Lurasidone.
MethotrimeprazineThe therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Bromocriptine.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Bromocriptine.
MetoclopramideThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Metoclopramide.
MidodrineBromocriptine may increase the hypertensive activities of Midodrine.
MifepristoneThe serum concentration of Bromocriptine can be increased when it is combined with Mifepristone.
NadololNadolol may increase the vasoconstricting activities of Bromocriptine.
NelfinavirThe metabolism of Bromocriptine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Bromocriptine can be increased when it is combined with Netupitant.
NitroglycerinBromocriptine may decrease the vasodilatory activities of Nitroglycerin.
OctreotideThe serum concentration of Bromocriptine can be increased when it is combined with Octreotide.
OlanzapineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Olanzapine.
OxandroloneOxandrolone may increase the hypoglycemic activities of Bromocriptine.
PalbociclibThe serum concentration of Bromocriptine can be increased when it is combined with Palbociclib.
PaliperidoneThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Paliperidone.
PasireotideThe serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Bromocriptine.
PerphenazineThe therapeutic efficacy of Perphenazine can be decreased when used in combination with Bromocriptine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Bromocriptine.
PimozideThe therapeutic efficacy of Pimozide can be decreased when used in combination with Bromocriptine.
ProchlorperazineThe therapeutic efficacy of Prochlorperazine can be decreased when used in combination with Bromocriptine.
PromazineThe therapeutic efficacy of Promazine can be decreased when used in combination with Bromocriptine.
QuetiapineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Quetiapine.
RisperidoneThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Risperidone.
SimeprevirThe serum concentration of Bromocriptine can be increased when it is combined with Simeprevir.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Bromocriptine.
StiripentolThe serum concentration of Bromocriptine can be increased when it is combined with Stiripentol.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Bromocriptine.
TestosteroneTestosterone may increase the hypoglycemic activities of Bromocriptine.
ThioridazineThe therapeutic efficacy of Thioridazine can be decreased when used in combination with Bromocriptine.
ThiothixeneThe therapeutic efficacy of Thiothixene can be decreased when used in combination with Bromocriptine.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Bromocriptine.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Bromocriptine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Bromocriptine.
TrichlormethiazideThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Trichlormethiazide.
TrifluoperazineThe therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Bromocriptine.
ZiprasidoneThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Ziprasidone.
ZuclopenthixolThe therapeutic efficacy of Zuclopenthixol can be decreased when used in combination with Bromocriptine.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  4. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  5. Lahlou S: Cardiovascular responses to intrathecal dopamine receptor agonists in conscious DOCA-salt hypertensive rats. Fundam Clin Pharmacol. 1999;13(6):624-34. [PubMed:10626749 ]
  6. Lahlou S, Araujo Lima PF, Interaminense LF, Duarte GP: Blunted central bromocriptine-induced tachycardia in conscious, malnourished rats. Pharmacol Toxicol. 2003 Apr;92(4):189-94. [PubMed:12753422 ]
  7. Lahlou S, Lima GC, Leao-Filho CS, Duarte GP: Effects of long-term pretreatment with isoproterenol on bromocriptine-induced tachycardia in conscious rats. Can J Physiol Pharmacol. 2000 Mar;78(3):260-5. [PubMed:10721819 ]
  8. Stefaneanu L, Kovacs K, Horvath E, Buchfelder M, Fahlbusch R, Lancranjan L: Dopamine D2 receptor gene expression in human adenohypophysial adenomas. Endocrine. 2001 Apr;14(3):329-36. [PubMed:11444429 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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
Molecular Weight:
44224.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. de Leeuw van Weenen JE, Parlevliet ET, Maechler P, Havekes LM, Romijn JA, Ouwens DM, Pijl H, Guigas B: The dopamine receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic receptors in beta cells. Biochem Pharmacol. 2010 Jun 15;79(12):1827-36. doi: 10.1016/j.bcp.2010.01.029. Epub 2010 Feb 4. [PubMed:20138024 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. de Leeuw van Weenen JE, Parlevliet ET, Maechler P, Havekes LM, Romijn JA, Ouwens DM, Pijl H, Guigas B: The dopamine receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic receptors in beta cells. Biochem Pharmacol. 2010 Jun 15;79(12):1827-36. doi: 10.1016/j.bcp.2010.01.029. Epub 2010 Feb 4. [PubMed:20138024 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. de Leeuw van Weenen JE, Parlevliet ET, Maechler P, Havekes LM, Romijn JA, Ouwens DM, Pijl H, Guigas B: The dopamine receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic receptors in beta cells. Biochem Pharmacol. 2010 Jun 15;79(12):1827-36. doi: 10.1016/j.bcp.2010.01.029. Epub 2010 Feb 4. [PubMed:20138024 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. Cussac D, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Martel JC, Danty N, Rauly-Lestienne I: Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol. 2008 Oct 10;594(1-3):32-8. doi: 10.1016/j.ejphar.2008.07.040. Epub 2008 Jul 30. [PubMed:18703043 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Cussac D, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Martel JC, Danty N, Rauly-Lestienne I: Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol. 2008 Oct 10;594(1-3):32-8. doi: 10.1016/j.ejphar.2008.07.040. Epub 2008 Jul 30. [PubMed:18703043 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Cussac D, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Martel JC, Danty N, Rauly-Lestienne I: Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol. 2008 Oct 10;594(1-3):32-8. doi: 10.1016/j.ejphar.2008.07.040. Epub 2008 Jul 30. [PubMed:18703043 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD5
Uniprot ID:
P21918
Molecular Weight:
52950.5 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Knight JA, Smith C, Toohey N, Klein MT, Teitler M: Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists. Mol Pharmacol. 2009 Feb;75(2):374-80. doi: 10.1124/mol.108.052084. Epub 2008 Nov 7. [PubMed:18996971 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Fernando H, Halpert JR, Davydov DR: Resolution of multiple substrate binding sites in cytochrome P450 3A4: the stoichiometry of the enzyme-substrate complexes probed by FRET and Job's titration. Biochemistry. 2006 Apr 4;45(13):4199-209. [PubMed:16566594 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  3. Nath A, Grinkova YV, Sligar SG, Atkins WM: Ligand binding to cytochrome P450 3A4 in phospholipid bilayer nanodiscs: the effect of model membranes. J Biol Chem. 2007 Sep 28;282(39):28309-20. Epub 2007 Jun 15. [PubMed:17573349 ]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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
Molecular Weight:
141477.255 Da
References
  1. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113 ]
  2. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267 ]
  3. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
  4. Renaud JP, Davydov DR, Heirwegh KP, Mansuy D, Hui Bon Hoa GH: Thermodynamic studies of substrate binding and spin transitions in human cytochrome P-450 3A4 expressed in yeast microsomes. Biochem J. 1996 Nov 1;319 ( Pt 3):675-81. [PubMed:8920966 ]
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 02:00