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Bromocriptine

Bromocriptine
Bromocriptine.svg
Bromocriptine ball-and-stick.png
Clinical data
Trade names Parlodel, Brotin
AHFS/Drugs.com Monograph,International Drug Names
MedlinePlus a682079
Pregnancy
category
  • AU: A
  • US: B (No risk in non-human studies)
Routes of
administration
oral, intravenous
ATC code G02CB01 (WHO) N04BC01 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability 28% of oral dose absorbed
Metabolism Extensively liver-mediated
Biological half-life 12-14 hours
Excretion 85% bile (faeces), 2.5-5.5% urine
Identifiers
Synonyms 2-Bromoergocriptine
CAS Number 25614-03-3 YesY
PubChem (CID) 31101
IUPHAR/BPS 35
DrugBank DB01200 YesY
ChemSpider 28858 YesY
UNII 3A64E3G5ZO YesY
KEGG D03165 YesY
ChEBI CHEBI:3181 YesY
ChEMBL CHEMBL493 YesY
ECHA InfoCard 100.042.829
Chemical and physical data
Formula C32H40BrN5O5
Molar mass 654.595 g/mol
3D model (Jmol) Interactive image
  

Bromocriptine (INN; trade names Parlodel, Cycloset, Brotin (Pakistan)), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.

Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated with this drug. Bromocriptine has completely treated gestational macromastia eliminating the need for reduction surgery, in a recent case. It has also been used in treating nonpuerperal mastitis. Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal. In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset (VeroScience). It is currently unknown how this drug improves glycemic control, but it has been shown to reduce HbA1c by ~0.5 percentage points.

Bromocriptine is a potent agonist at dopamine D2 receptors and various serotonin receptors. It also inhibits the release of glutamate, by reversing the glutamate GLT1 transporter.


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