Cabergoline

Products

Cabergoline is commercially available in tablet form (Cabaser, Dostinex). It has been approved in many countries since 1995.

Structure and properties

Cabergoline (C26H37N5O2, Mr = 451.6 g/mol) is a dopaminergic ergoline derivative. It exists as a white crystalline powder that is practically insoluble in water.

Effects

Cabergoline (ATC N04BC06) has dopaminergic properties and reduces prolactin secretion. The effects are due to binding to the dopamine D2 receptor. Cabergoline has a long half-life of up to 68 hours.

Indications

  • For the treatment of Parkinson’s disease (2nd-line agent).
  • For weaning
  • Hyperprolactinemic disorders, prolactinoma.

Dosage

According to the professional information (depending on the indication). It should be taken with a meal.

Contraindications

For complete precautions, see the drug label.

Interactions

Cabergoline is a substrate of CYP3A4. Combination with CYP3A4 inhibitors is contraindicated. Other drug-drug interactions are possible with other ergot alkaloids and with dopamine antagonists.

Adverse effects

The most common possible adverse effects include headache, dizziness, and nausea. In addition, numerous other side effects are possible.