Identification

Name
Pergolide
Accession Number
DB01186  (APRD00663)
Type
Small Molecule
Groups
Approved, Investigational, Vet Approved, Withdrawn
Description

Pergolide is a long-acting dopamine agonist approved in 1982 for the treatment of Parkinson’s Disease. It is an ergot derivative that acts on the dopamine D2 and D3, alpha2- and alpha1-adrenergic, and 5-hydroxytryptamine (5-HT) receptors. It was indicated as adjunct therapy with levodopa/carbidopa in the symptomatic treatment of parkinsonian syndrome. It was later found that pergolide increased the risk of cardiac valvulopathy. The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.

Structure
Thumb
Synonyms
  • Pergolida
  • Pergolidum
Product Ingredients
IngredientUNIICASInChI Key
Pergolide mesylate55B9HQY61666104-23-2UWCVGPLTGZWHGS-ZORIOUSZSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Permax Tab 0.05mgTablet0.05 mgOralEli Lilly & Co. Ltd.1991-01-012000-08-03Canada
Permax Tab 0.25mgTablet0.25 mgOralEli Lilly & Co. Ltd.1991-01-012000-08-03Canada
Permax Tab 1mgTablet1 mgOralEli Lilly & Co. Ltd.1991-01-012000-08-03Canada
International/Other Brands
Permax (Eli Lilly)
Categories
UNII
24MJ822NZ9
CAS number
66104-22-1
Weight
Average: 314.488
Monoisotopic: 314.181669532
Chemical Formula
C19H26N2S
InChI Key
YEHCICAEULNIGD-MZMPZRCHSA-N
InChI
InChI=1S/C19H26N2S/c1-3-7-21-11-13(12-22-2)8-16-15-5-4-6-17-19(15)14(10-20-17)9-18(16)21/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3/t13-,16-,18-/m1/s1
IUPAC Name
(2R,4R,7R)-4-[(methylsulfanyl)methyl]-6-propyl-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),9,12,14-tetraene
SMILES
[H][[email protected]@]12CC3=CNC4=CC=CC(=C34)[[email protected]@]1([H])C[[email protected]@H](CSC)CN2CCC

Pharmacology

Indication

Indicated as adjunctive treatment to levodopa/carbidopa in the management of the signs and symptoms of Parkinson's disease. It was withdrawn from the US and Canadian markets in 2007 due to an increased risk of cardiac valvulopathy.

Structured Indications
Not Available
Pharmacodynamics

Pergolide 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 and are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors and has been 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- and D3-receptors. It also exhibits agonist activity on dopamine D4, D1, and D5, 5-hydroxytryptamine (5-HT)1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, α2A-, α2B-, α2C-, α1A-, α1B-, and α1D-adrenergic 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. Pergolide also causes transient increases in somatotropin (growth hormone) secretion and decreases in luteinizing hormone (LH) concentrations.

Mechanism of action

The 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.

TargetActionsOrganism
AD(2) dopamine receptor
agonist
Human
AD(3) dopamine receptor
agonist
Human
UD(4) dopamine receptor
agonist
Human
U5-hydroxytryptamine receptor 1A
agonist
Human
U5-hydroxytryptamine receptor 2B
agonist
Human
U5-hydroxytryptamine receptor 2A
agonist
Human
U5-hydroxytryptamine receptor 1D
agonist
Human
UAlpha-2B adrenergic receptor
agonist
Human
UAlpha-2A adrenergic receptor
agonist
Human
UAlpha-2C adrenergic receptor
agonist
Human
UD(1B) dopamine receptor
agonist
Human
UD(1A) dopamine receptor
agonist
Human
U5-hydroxytryptamine receptor 1B
agonist
Human
U5-hydroxytryptamine receptor 2C
agonist
Human
UAlpha-1A adrenergic receptor
agonist
Human
UAlpha-1B adrenergic receptor
agonist
Human
UAlpha-1D adrenergic receptor
agonist
Human
Absorption

Significant amount may be absorbed (evidence on bioavailability still lacking).

Volume of distribution
Not Available
Protein binding

90%

Metabolism

Extensively hepatic.

Route of elimination

The major route of excretion is the kidney.

Half life

27 hours

Clearance
Not Available
Toxicity

Oral, rat LD50: 15 mg/kg. Symptoms of overdose include nausea, vomiting, convulsions, decreased blood pressure, and CNS stimulation.

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

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe metabolism of Pergolide can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.Experimental
AcebutololPergolide may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AcetaminophenThe risk or severity of adverse effects can be increased when Pergolide is combined with Acetaminophen.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Acetazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Pergolide is combined with Aldesleukin.Approved
AlprazolamThe risk or severity of adverse effects can be increased when Pergolide is combined with Alprazolam.Approved, Illicit, Investigational
AlprenololPergolide may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmbroxolThe risk or severity of adverse effects can be increased when Pergolide is combined with Ambroxol.Approved, Investigational
AmineptineAmineptine may decrease the antihypertensive activities of Pergolide.Illicit, Withdrawn
AmiodaroneThe metabolism of Pergolide can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Pergolide.Approved
AmlodipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Amlodipine.Approved
AmprenavirThe risk or severity of adverse effects can be increased when Pergolide is combined with Amprenavir.Approved
AnastrozoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Anastrozole.Approved, Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Pergolide is combined with Antipyrine.Approved
AprepitantThe serum concentration of Pergolide can be increased when it is combined with Aprepitant.Approved, Investigational
ArotinololPergolide may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved, Investigational
Arsenic trioxideThe risk or severity of adverse effects can be increased when Pergolide is combined with Arsenic trioxide.Approved, Investigational
AstemizoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Pergolide can be decreased when combined with Atazanavir.Approved, Investigational
AtenololPergolide may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
AtomoxetineThe metabolism of Pergolide can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Pergolide is combined with Atorvastatin.Approved
AzelastineThe risk or severity of adverse effects can be increased when Pergolide is combined with Azelastine.Approved
AzithromycinThe risk or severity of adverse effects can be increased when Pergolide is combined with Azithromycin.Approved
BefunololPergolide may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BenmoxinThe metabolism of Pergolide can be decreased when combined with Benmoxin.Withdrawn
BetamethasoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Betamethasone.Approved, Vet Approved
BetaxololPergolide may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BevantololPergolide may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BicalutamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Bicalutamide.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Bifonazole.Approved, Investigational
BisoprololPergolide may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BoceprevirThe metabolism of Pergolide can be decreased when combined with Boceprevir.Approved, Withdrawn
BopindololPergolide may increase the atrioventricular blocking (AV block) activities of Bopindolol.Approved
BortezomibThe metabolism of Pergolide can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Pergolide can be decreased when it is combined with Bosentan.Approved, Investigational
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Pergolide is combined with Brentuximab vedotin.Approved
BrofaromineThe metabolism of Pergolide can be decreased when combined with Brofaromine.Experimental
BromocriptineBromocriptine may increase the vasoconstricting activities of Pergolide.Approved, Investigational
BucindololPergolide may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolPergolide may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BupranololPergolide may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Pergolide is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
CabergolineCabergoline may increase the vasoconstricting activities of Pergolide.Approved
CaffeineThe risk or severity of adverse effects can be increased when Pergolide is combined with Caffeine.Approved
CapsaicinThe risk or severity of adverse effects can be increased when Pergolide is combined with Capsaicin.Approved
CarbamazepineThe metabolism of Pergolide can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneThe metabolism of Pergolide can be decreased when combined with Caroxazone.Withdrawn
CarteololPergolide may increase the atrioventricular blocking (AV block) activities of Carteolol.Approved
CarvedilolPergolide may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CaspofunginThe risk or severity of adverse effects can be increased when Pergolide is combined with Caspofungin.Approved
CeliprololPergolide may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Pergolide can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Pergolide.Withdrawn
ChloramphenicolThe risk or severity of adverse effects can be increased when Pergolide is combined with Chloramphenicol.Approved, Vet Approved
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Chlorzoxazone.Approved
CilostazolThe risk or severity of adverse effects can be increased when Pergolide is combined with Cilostazol.Approved
CiprofloxacinThe risk or severity of adverse effects can be increased when Pergolide is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe risk or severity of adverse effects can be increased when Pergolide is combined with Cisapride.Approved, Investigational, Withdrawn
ClarithromycinThe metabolism of Pergolide can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Pergolide can be decreased when combined with Clemastine.Approved
ClindamycinThe risk or severity of adverse effects can be increased when Pergolide is combined with Clindamycin.Approved, Vet Approved
ClofazimineThe risk or severity of adverse effects can be increased when Pergolide is combined with Clofazimine.Approved, Investigational
ClomifeneThe risk or severity of adverse effects can be increased when Pergolide is combined with Clomifene.Approved, Investigational
ClomipramineClomipramine may decrease the antihypertensive activities of Pergolide.Approved, Vet Approved
CloranololPergolide may increase the atrioventricular blocking (AV block) activities of Cloranolol.Experimental
ClotiazepamThe risk or severity of adverse effects can be increased when Pergolide is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe metabolism of Pergolide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Pergolide is combined with Clozapine.Approved
CobicistatThe metabolism of Pergolide can be decreased when combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Pergolide is combined with Cocaine.Approved, Illicit
ColchicineThe risk or severity of adverse effects can be increased when Pergolide is combined with Colchicine.Approved
ConivaptanThe serum concentration of Pergolide can be increased when it is combined with Conivaptan.Approved, Investigational
Cortisone acetateThe risk or severity of adverse effects can be increased when Pergolide is combined with Cortisone acetate.Approved
CrizotinibThe metabolism of Pergolide can be decreased when combined with Crizotinib.Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Pergolide.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Pergolide can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Pergolide can be decreased when it is combined with Dabrafenib.Approved
DalfopristinThe risk or severity of adverse effects can be increased when Pergolide is combined with Dalfopristin.Approved
DanazolThe risk or severity of adverse effects can be increased when Pergolide is combined with Danazol.Approved
DarunavirThe metabolism of Pergolide can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Pergolide can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe risk or severity of adverse effects can be increased when Pergolide is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Pergolide can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Pergolide can be decreased when combined with Delavirdine.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Pergolide.Approved
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Pergolide.Approved
DextropropoxypheneThe risk or severity of adverse effects can be increased when Pergolide is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DiazepamThe risk or severity of adverse effects can be increased when Pergolide is combined with Diazepam.Approved, Illicit, Vet Approved
DibenzepinDibenzepin may decrease the antihypertensive activities of Pergolide.Experimental
DiethylstilbestrolThe risk or severity of adverse effects can be increased when Pergolide is combined with Diethylstilbestrol.Approved, Investigational
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Pergolide.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Pergolide.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Pergolide.Experimental
DihydroergotamineThe metabolism of Pergolide can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Pergolide can be decreased when combined with Diltiazem.Approved
Dimethyl sulfoxideThe risk or severity of adverse effects can be increased when Pergolide is combined with Dimethyl sulfoxide.Approved, Vet Approved
DocetaxelThe risk or severity of adverse effects can be increased when Pergolide is combined with Docetaxel.Approved, Investigational
DosulepinDosulepin may decrease the antihypertensive activities of Pergolide.Approved
DoxepinDoxepin may decrease the antihypertensive activities of Pergolide.Approved
DoxorubicinThe risk or severity of adverse effects can be increased when Pergolide is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Pergolide can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Pergolide can be decreased when combined with Dronedarone.Approved
DroxidopaPergolide may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineDuloxetine may decrease the antihypertensive activities of Pergolide.Approved
EconazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Econazole.Approved
ElbasvirThe risk or severity of adverse effects can be increased when Pergolide is combined with Elbasvir.Approved
EnasidenibThe risk or severity of adverse effects can be increased when Pergolide is combined with Enasidenib.Approved
EnzalutamideThe serum concentration of Pergolide can be decreased when it is combined with Enzalutamide.Approved
EpanololPergolide may increase the atrioventricular blocking (AV block) activities of Epanolol.Experimental
EpinephrineThe risk or severity of adverse effects can be increased when Pergolide is combined with Epinephrine.Approved, Vet Approved
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Pergolide.Approved
ErgonovineErgonovine may increase the vasoconstricting activities of Pergolide.Approved
ErgotamineErgotamine may increase the vasoconstricting activities of Pergolide.Approved
ErythromycinThe metabolism of Pergolide can be decreased when combined with Erythromycin.Approved, Vet Approved
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Pergolide.Investigational
EsmololPergolide may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
EthanolThe risk or severity of adverse effects can be increased when Pergolide is combined with Ethanol.Approved
EtoposideThe risk or severity of adverse effects can be increased when Pergolide is combined with Etoposide.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Pergolide is combined with Etoricoxib.Approved, Investigational
EzetimibeThe risk or severity of adverse effects can be increased when Pergolide is combined with Ezetimibe.Approved
FelodipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Felodipine.Approved, Investigational
FentanylThe risk or severity of adverse effects can be increased when Pergolide is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pergolide.Approved
FluconazoleThe metabolism of Pergolide can be decreased when combined with Fluconazole.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Pergolide is combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Pergolide is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Pergolide.Approved
FluvoxamineThe metabolism of Pergolide can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Pergolide can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Pergolide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Pergolide can be increased when combined with Fosphenytoin.Approved
FurazolidoneThe metabolism of Pergolide can be decreased when combined with Furazolidone.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Pergolide can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe risk or severity of adverse effects can be increased when Pergolide is combined with Gemfibrozil.Approved
GlyburideThe risk or severity of adverse effects can be increased when Pergolide is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe risk or severity of adverse effects can be increased when Pergolide is combined with Glycerol Phenylbutyrate.Approved
HaloperidolThe risk or severity of adverse effects can be increased when Pergolide is combined with Haloperidol.Approved
HarmalineThe metabolism of Pergolide can be decreased when combined with Harmaline.Experimental
HistamineThe risk or severity of adverse effects can be increased when Pergolide is combined with Histamine.Approved, Investigational
HydracarbazineThe metabolism of Pergolide can be decreased when combined with Hydracarbazine.Experimental
HydralazineThe risk or severity of adverse effects can be increased when Pergolide is combined with Hydralazine.Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Pergolide can be increased when it is combined with Idelalisib.Approved
IfosfamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Ifosfamide.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Iloperidone.Approved
ImatinibThe metabolism of Pergolide can be decreased when combined with Imatinib.Approved
ImipramineImipramine may decrease the antihypertensive activities of Pergolide.Approved
IndenololPergolide may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndinavirThe metabolism of Pergolide can be decreased when combined with Indinavir.Approved
indisulamThe risk or severity of adverse effects can be increased when Pergolide is combined with indisulam.Investigational
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Pergolide.Approved, Investigational
IprindoleIprindole may decrease the antihypertensive activities of Pergolide.Experimental
IproclozideThe metabolism of Pergolide can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Pergolide can be decreased when combined with Iproniazid.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Pergolide is combined with Irbesartan.Approved, Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Pergolide is combined with Irinotecan.Approved, Investigational
IsavuconazoniumThe metabolism of Pergolide can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe metabolism of Pergolide can be decreased when combined with Isocarboxazid.Approved
IsoniazidThe risk or severity of adverse effects can be increased when Pergolide is combined with Isoniazid.Approved
IsradipineThe metabolism of Pergolide can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Pergolide can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Pergolide can be increased when it is combined with Ivacaftor.Approved
JosamycinThe risk or severity of adverse effects can be increased when Pergolide is combined with Josamycin.Approved, Investigational
KetazolamThe risk or severity of adverse effects can be increased when Pergolide is combined with Ketazolam.Approved
KetoconazoleThe metabolism of Pergolide can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolPergolide may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LandiololPergolide may increase the atrioventricular blocking (AV block) activities of Landiolol.Investigational
LansoprazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Lansoprazole.Approved, Investigational
LapatinibThe risk or severity of adverse effects can be increased when Pergolide is combined with Lapatinib.Approved, Investigational
LercanidipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Lercanidipine.Approved, Investigational
LevofloxacinThe risk or severity of adverse effects can be increased when Pergolide is combined with Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Pergolide.Approved
LevosalbutamolThe risk or severity of adverse effects can be increased when Pergolide is combined with Levosalbutamol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Pergolide is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe risk or severity of adverse effects can be increased when Pergolide is combined with Linagliptin.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Pergolide.Approved, Investigational
LofepramineLofepramine may decrease the antihypertensive activities of Pergolide.Experimental
LomitapideThe risk or severity of adverse effects can be increased when Pergolide is combined with Lomitapide.Approved
LomustineThe risk or severity of adverse effects can be increased when Pergolide is combined with Lomustine.Approved
LopinavirThe metabolism of Pergolide can be decreased when combined with Lopinavir.Approved
LoratadineThe risk or severity of adverse effects can be increased when Pergolide is combined with Loratadine.Approved
LosartanThe risk or severity of adverse effects can be increased when Pergolide is combined with Losartan.Approved
LovastatinThe metabolism of Pergolide can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Pergolide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Pergolide can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Pergolide.Illicit, Investigational, Withdrawn
ManidipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Manidipine.Approved, Investigational
MebanazineThe metabolism of Pergolide can be decreased when combined with Mebanazine.Withdrawn
MefloquineThe risk or severity of adverse effects can be increased when Pergolide is combined with Mefloquine.Approved
MepindololPergolide may increase the atrioventricular blocking (AV block) activities of Mepindolol.Experimental
MequitazineThe risk or severity of adverse effects can be increased when Pergolide is combined with Mequitazine.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Pergolide.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Methadone.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Methazolamide.Approved
MethimazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Methimazole.Approved
Methylene blueThe metabolism of Pergolide can be decreased when combined with Methylene blue.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Pergolide.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Pergolide is combined with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Pergolide.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Pergolide.Approved, Investigational
MetronidazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Metronidazole.Approved
MetyraponeThe risk or severity of adverse effects can be increased when Pergolide is combined with Metyrapone.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Pergolide.Experimental
MianserinThe therapeutic efficacy of Pergolide can be decreased when used in combination with Mianserin.Approved, Investigational
MibefradilThe risk or severity of adverse effects can be increased when Pergolide is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe risk or severity of adverse effects can be increased when Pergolide is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Pergolide can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may decrease the antihypertensive activities of Pergolide.Approved
MinaprineThe metabolism of Pergolide can be decreased when combined with Minaprine.Approved
MirtazapineMirtazapine may decrease the antihypertensive activities of Pergolide.Approved
MitotaneThe serum concentration of Pergolide can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe risk or severity of adverse effects can be increased when Pergolide is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Pergolide can be decreased when combined with Moclobemide.Approved
NadololPergolide may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NefazodoneThe metabolism of Pergolide can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Pergolide can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Pergolide can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Pergolide can be increased when combined with Nevirapine.Approved
NialamideThe metabolism of Pergolide can be decreased when combined with Nialamide.Withdrawn
NicardipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Nicardipine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Pergolide.Approved, Investigational
NicotinamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Nicotinamide.Approved
NifedipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Nifedipine.Approved
NilotinibThe metabolism of Pergolide can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Nilvadipine.Approved, Investigational
NisoldipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Nisoldipine.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Pergolide is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe risk or severity of adverse effects can be increased when Pergolide is combined with Nitric Oxide.Approved
NorfloxacinThe risk or severity of adverse effects can be increased when Pergolide is combined with Norfloxacin.Approved
NortriptylineNortriptyline may decrease the antihypertensive activities of Pergolide.Approved
NoscapineThe risk or severity of adverse effects can be increased when Pergolide is combined with Noscapine.Investigational
OctamoxinThe metabolism of Pergolide can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Pergolide is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Pergolide can be decreased when combined with Olaparib.Approved
OmeprazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Omeprazole.Approved, Investigational, Vet Approved
OpipramolOpipramol may decrease the antihypertensive activities of Pergolide.Investigational
OsimertinibThe serum concentration of Pergolide can be increased when it is combined with Osimertinib.Approved
OxprenololPergolide may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Pergolide is combined with Oxybutynin.Approved, Investigational
OxymetholoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Oxymetholone.Approved, Illicit
PaclitaxelThe risk or severity of adverse effects can be increased when Pergolide is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Pergolide can be increased when it is combined with Palbociclib.Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Paramethasone.Approved
PargylineThe metabolism of Pergolide can be decreased when combined with Pargyline.Approved
PazopanibThe risk or severity of adverse effects can be increased when Pergolide is combined with Pazopanib.Approved
PenbutololPergolide may increase the atrioventricular blocking (AV block) activities of Penbutolol.Approved, Investigational
PentobarbitalThe metabolism of Pergolide can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenelzineThe metabolism of Pergolide can be decreased when combined with Phenelzine.Approved
PheniprazineThe metabolism of Pergolide can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Pergolide can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Pergolide can be decreased when combined with Phenoxypropazine.Withdrawn
PhenytoinThe metabolism of Pergolide can be increased when combined with Phenytoin.Approved, Vet Approved
PilocarpineThe risk or severity of adverse effects can be increased when Pergolide is combined with Pilocarpine.Approved
PimozideThe risk or severity of adverse effects can be increased when Pergolide is combined with Pimozide.Approved
PindololPergolide may increase the atrioventricular blocking (AV block) activities of Pindolol.Approved
PirlindoleThe metabolism of Pergolide can be decreased when combined with Pirlindole.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Pergolide.Approved
PivhydrazineThe metabolism of Pergolide can be decreased when combined with Pivhydrazine.Withdrawn
PosaconazoleThe metabolism of Pergolide can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PractololPergolide may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Pergolide.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Pergolide is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Prednisone.Approved, Vet Approved
PrimaquineThe risk or severity of adverse effects can be increased when Pergolide is combined with Primaquine.Approved
PrimidoneThe metabolism of Pergolide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe risk or severity of adverse effects can be increased when Pergolide is combined with Progesterone.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Pergolide is combined with Propofol.Approved, Investigational, Vet Approved
PropranololPergolide may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProtriptylineProtriptyline may decrease the antihypertensive activities of Pergolide.Approved
QuinidineThe risk or severity of adverse effects can be increased when Pergolide is combined with Quinidine.Approved
QuinineThe risk or severity of adverse effects can be increased when Pergolide is combined with Quinine.Approved
QuinupristinThe risk or severity of adverse effects can be increased when Pergolide is combined with Quinupristin.Approved
RabeprazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Rabeprazole.Approved, Investigational
RaloxifeneThe risk or severity of adverse effects can be increased when Pergolide is combined with Raloxifene.Approved, Investigational
RanitidineThe risk or severity of adverse effects can be increased when Pergolide is combined with Ranitidine.Approved
RanolazineThe metabolism of Pergolide can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe metabolism of Pergolide can be decreased when combined with Rasagiline.Approved
RegorafenibThe risk or severity of adverse effects can be increased when Pergolide is combined with Regorafenib.Approved
RepaglinideThe risk or severity of adverse effects can be increased when Pergolide is combined with Repaglinide.Approved, Investigational
ResveratrolThe risk or severity of adverse effects can be increased when Pergolide is combined with Resveratrol.Approved, Experimental, Investigational
RifabutinThe metabolism of Pergolide can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Pergolide can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Pergolide can be increased when combined with Rifapentine.Approved
RilpivirineThe risk or severity of adverse effects can be increased when Pergolide is combined with Rilpivirine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Risperidone.Approved, Investigational
RitonavirThe metabolism of Pergolide can be decreased when combined with Ritonavir.Approved, Investigational
RivastigmineThe risk or severity of adverse effects can be increased when Pergolide is combined with Rivastigmine.Approved, Investigational
RolitetracyclineThe risk or severity of adverse effects can be increased when Pergolide is combined with Rolitetracycline.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Pergolide.Approved
RoxithromycinThe risk or severity of adverse effects can be increased when Pergolide is combined with Roxithromycin.Approved, Investigational, Withdrawn
RutinThe risk or severity of adverse effects can be increased when Pergolide is combined with Rutin.Experimental, Investigational
SafrazineThe metabolism of Pergolide can be decreased when combined with Safrazine.Withdrawn
SalbutamolThe risk or severity of adverse effects can be increased when Pergolide is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe metabolism of Pergolide can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe risk or severity of adverse effects can be increased when Pergolide is combined with Sarilumab.Approved
SelegilineThe metabolism of Pergolide can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe risk or severity of adverse effects can be increased when Pergolide is combined with Sertraline.Approved
SildenafilThe metabolism of Pergolide can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Pergolide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Pergolide can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Pergolide.Approved
SirolimusThe risk or severity of adverse effects can be increased when Pergolide is combined with Sirolimus.Approved, Investigational
SitaxentanThe risk or severity of adverse effects can be increased when Pergolide is combined with Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe risk or severity of adverse effects can be increased when Pergolide is combined with Sorafenib.Approved, Investigational
SotalolPergolide may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
St. John's WortThe serum concentration of Pergolide can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Pergolide can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Sulfamethoxazole.Approved
SulfanilamideThe risk or severity of adverse effects can be increased when Pergolide is combined with Sulfanilamide.Approved
SulfinpyrazoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Pergolide can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe risk or severity of adverse effects can be increased when Pergolide is combined with Tacrolimus.Approved, Investigational
TadalafilThe risk or severity of adverse effects can be increased when Pergolide is combined with Tadalafil.Approved, Investigational
TalinololPergolide may increase the atrioventricular blocking (AV block) activities of Talinolol.Investigational
TamoxifenThe risk or severity of adverse effects can be increased when Pergolide is combined with Tamoxifen.Approved
TelaprevirThe metabolism of Pergolide can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Pergolide can be decreased when combined with Telithromycin.Approved
TemsirolimusThe risk or severity of adverse effects can be increased when Pergolide is combined with Temsirolimus.Approved
TeniposideThe risk or severity of adverse effects can be increased when Pergolide is combined with Teniposide.Approved
TerfenadineThe risk or severity of adverse effects can be increased when Pergolide is combined with Terfenadine.Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Pergolide.Experimental
TertatololPergolide may increase the atrioventricular blocking (AV block) activities of Tertatolol.Experimental
TesmilifeneThe risk or severity of adverse effects can be increased when Pergolide is combined with Tesmilifene.Investigational
TestosteroneThe risk or severity of adverse effects can be increased when Pergolide is combined with Testosterone.Approved, Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Pergolide is combined with Tetracycline.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Pergolide is combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Pergolide.Approved, Withdrawn
TianeptineTianeptine may decrease the antihypertensive activities of Pergolide.Approved, Investigational
TicagrelorThe risk or severity of adverse effects can be increased when Pergolide is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Pergolide can be decreased when combined with Ticlopidine.Approved
TimololPergolide may increase the atrioventricular blocking (AV block) activities of Timolol.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Pergolide is combined with Tioconazole.Approved
TipranavirThe risk or severity of adverse effects can be increased when Pergolide is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Pergolide can be decreased when it is combined with Tocilizumab.Approved
TofisopamThe risk or severity of adverse effects can be increased when Pergolide is combined with Tofisopam.Approved
ToloxatoneThe metabolism of Pergolide can be decreased when combined with Toloxatone.Approved
TopiroxostatThe risk or severity of adverse effects can be increased when Pergolide is combined with Topiroxostat.Approved, Investigational
TopotecanThe risk or severity of adverse effects can be increased when Pergolide is combined with Topotecan.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Pergolide is combined with Tramadol.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe metabolism of Pergolide can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe metabolism of Pergolide can be decreased when combined with Tranylcypromine.Approved
TrimipramineTrimipramine may decrease the antihypertensive activities of Pergolide.Approved
TroglitazoneThe risk or severity of adverse effects can be increased when Pergolide is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe risk or severity of adverse effects can be increased when Pergolide is combined with Troleandomycin.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Pergolide.Approved, Experimental
Valproic AcidThe risk or severity of adverse effects can be increased when Pergolide is combined with Valproic Acid.Approved, Investigational
VenlafaxineThe metabolism of Pergolide can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Pergolide can be decreased when combined with Verapamil.Approved
VinblastineThe risk or severity of adverse effects can be increased when Pergolide is combined with Vinblastine.Approved
VincristineThe risk or severity of adverse effects can be increased when Pergolide is combined with Vincristine.Approved, Investigational
VinorelbineThe risk or severity of adverse effects can be increased when Pergolide is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Pergolide can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe risk or severity of adverse effects can be increased when Pergolide is combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Pergolide can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe risk or severity of adverse effects can be increased when Pergolide is combined with Zucapsaicin.Approved
Food Interactions
  • Take with food to reduce gastric irritation and nausea

References

Synthesis Reference
US5034394
General References
  1. Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E: Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med. 2007 Jan 4;356(1):29-38. [PubMed:17202453]
  2. Breitenstein C, Korsukewitz C, Floel A, Kretzschmar T, Diederich K, Knecht S: Tonic dopaminergic stimulation impairs associative learning in healthy subjects. Neuropsychopharmacology. 2006 Nov;31(11):2552-64. Epub 2006 Jul 26. [PubMed:16880771]
External Links
Human Metabolome Database
HMDB15317
KEGG Compound
C07425
PubChem Compound
47811
PubChem Substance
46507604
ChemSpider
43503
BindingDB
50017543
ChEBI
63617
ChEMBL
CHEMBL531
Therapeutic Targets Database
DAP000069
PharmGKB
PA450873
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pergolide
ATC Codes
N04BC02 — Pergolide
FDA label
Download (204 KB)
MSDS
Download (76 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentCocaine-Related Disorders1
2CompletedTreatmentCocaine-Related Disorders / Substance-Related Disorders1
2SuspendedNot AvailableCognitive Impairments / Negative Symptoms / Schizophrenic Disorders1
3CompletedTreatmentCocaine-Related Disorders1
3CompletedTreatmentIdiopathic Parkinson's Disease1
Not AvailableCompletedBasic ScienceSchizophrenic Disorders1
Not AvailableCompletedTreatmentGilles de la Tourette's Syndrome1
Not AvailableNo Longer AvailableNot AvailableParkinson's Disease (PD)1
Not AvailableUnknown StatusDiagnosticOther Personality Disorders / Schizotypal Personality Disorder1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral0.05 mg
TabletOral0.25 mg
TabletOral1 mg
Prices
Unit descriptionCostUnit
Pergolide mesylate 100% powder1009.8USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5114948No1992-10-192009-10-19Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)207.5 °CPhysProp
logP4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000584 mg/mLALOGPS
logP4.17ALOGPS
logP4.23ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)17.35ChemAxon
pKa (Strongest Basic)9.49ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area19.03 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity97.02 m3·mol-1ChemAxon
Polarizability38.4 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9871
Caco-2 permeable+0.5668
P-glycoprotein substrateSubstrate0.7201
P-glycoprotein inhibitor IInhibitor0.5589
P-glycoprotein inhibitor IIInhibitor0.5145
Renal organic cation transporterInhibitor0.7757
CYP450 2C9 substrateNon-substrate0.8671
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5
CYP450 1A2 substrateInhibitor0.8932
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.5623
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6145
Ames testAMES toxic0.751
CarcinogenicityNon-carcinogens0.9694
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8857 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.66
hERG inhibition (predictor II)Inhibitor0.791
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/MSsplash10-014i-0009000000-2ad79ab70c752608fcb3
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-066r-0679000000-884687417c70aa3885ba
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0gbc-0910000000-9ab47ed0d8af7d82612b
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0329000000-1f96cb9d349909c64088

Taxonomy

Description
This compound belongs to the class of organic compounds known as indoloquinolines. These are polycyclic aromatic compounds containing an indole fused to a quinoline.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Indoloquinolines
Direct Parent
Indoloquinolines
Alternative Parents
Ergoline and derivatives / Benzoquinolines / Pyrroloquinolines / 3-alkylindoles / Isoindoles and derivatives / Aralkylamines / Benzenoids / Piperidines / Pyrroles / Heteroaromatic compounds
show 6 more
Substituents
Ergoline skeleton / Indoloquinoline / Benzoquinoline / Pyrroloquinoline / 3-alkylindole / Indole / Indole or derivatives / Alkaloid or derivatives / Isoindole or derivatives / Aralkylamine
show 17 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organic heterotetracyclic compound, methyl sulfide, diamine (CHEBI:63617)

Targets

Details
1. D(2) dopamine receptor
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
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Fuller RW, Hemrick-Luecke SK, Perry KW, Toomey RE: Pergolide elevation of MHPG sulphate concentration in rat hypothalamus blocked by spiperone and mimicked by other dopamine agonists. J Pharm Pharmacol. 1985 Apr;37(4):268-70. [PubMed:2860228]
  3. Huettl P, Gerhardt GA, Browning MD, Masserano JM: Effects of dopamine receptor agonists and antagonists on catecholamine release in bovine chromaffin cells. J Pharmacol Exp Ther. 1991 May;257(2):567-74. [PubMed:1674528]
  4. 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]
  5. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
  6. Linazasoro G, Obeso JA, Gomez JC, Martinez M, Antonini A, Leenders KL: Modification of dopamine D2 receptor activity by pergolide in Parkinson's disease: an in vivo study by PET. Clin Neuropharmacol. 1999 Sep-Oct;22(5):277-80. [PubMed:10516878]
  7. Mehta MA, Riedel WJ: Dopaminergic enhancement of cognitive function. Curr Pharm Des. 2006;12(20):2487-500. [PubMed:16842172]
  8. Paturle L, Fage D, Fourrier O, Vernier P, Feuerstein C, Demenge P, Scatton B: Cortical ablation fails to influence striatal dopamine target cell supersensitivity induced by nigrostriatal denervation in the rat. Brain Res. 1987 Feb 3;402(2):383-6. [PubMed:3828803]
Details
2. D(3) dopamine receptor
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
Uniprot Name
D(3) dopamine receptor
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]
  3. Wachtel H: Antiparkinsonian dopamine agonists: a review of the pharmacokinetics and neuropharmacology in animals and humans. J Neural Transm Park Dis Dement Sect. 1991;3(3):151-201. [PubMed:1683537]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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 ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
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
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
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
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...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
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
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-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
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 subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
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
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 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
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 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
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
Uniprot Name
D(1B) dopamine receptor
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]
Details
12. D(1A) dopamine receptor
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
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  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 subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
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-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
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
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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
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
Uniprot Name
Alpha-1D adrenergic receptor
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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. 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. 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
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. 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. 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]

Drug created on June 13, 2005 07:24 / Updated on November 09, 2017 02:57