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QuickView for Bromocriptine (compound)

Name: Bromocriptine
PubChem Compound ID: 2443
Description: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.
Molecular formula: C32H40BrN5O5
Molecular weight: 654.595 g/mol
Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, (5'.alpha.)-; Bromocriptine
Name: Bromocriptine
Name (isomeric): DB01200
Drug Type: small molecule
Description: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.
Bromocryptine; Bromocriptinum [INN-Latin]; Bromoergocryptine; Bromergocryptine; Bromocryptine Mesylate; Bromoergocriptine; Bromocriptine Methanesulfonate; Bromocriptina [INN-Spanish]; Bromocriptine Mesylate; Bromocriptin
Brand: Bagren, Apo-Bromocriptine, Alti-Bromocriptine, Parlodel Snaptabs, Parlodel, Pravidel, Ergoset
Category: Antidyskinetics, Hormone Antagonists, Antiparkinson Agents, Dopamine Agonists
CAS number: 25614-03-3
Indication: For 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.
Bromocriptine 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 dopaminergi...
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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 sto...
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Absorption: Approximately 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.
Protein binding: 90-96% bound to serum albumin
Biotransformation: 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 elimination: Parent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.
Half Life: 2-8 hours
Toxicity: Symptoms 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
Food interaction:
Avoid alcohol.
Take with food to reduce irritation.
Drug interaction:
ZolmitriptanConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, bromocriptine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and bromocriptine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
PerphenazineThe phenothiazine decreases the effect of bromocriptine
MesoridazineThe phenothiazine decreases the effect of bromocriptine
PaliperidoneThe atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, bromocriptine. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
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