Cabergoline

Antiparkinsonian Drug

Drug class: Dopaminergic Antiparkinsonian Agent; Prolactin Inhibitor

Cabergoline (DOSTINEX)（中文：卡麥角林）

Common Strengths

• 0.5 mg

Drug Trade Names

• Dostinex

Drug Usage

Cabergoline is utilized for:

• Treating hyperprolactinemia (high prolactin levels).
• Managing prolactinomas (tumors that produce prolactin).
• Adjunct therapy in Parkinson's disease.

Mechanism of Action

Cabergoline works by stimulating dopamine D2 receptors, which inhibits the secretion of prolactin from the pituitary gland. This action helps normalize prolactin levels and can improve symptoms related to hyperprolactinemia and certain cases of Parkinson's disease.

Route of Administration

Cabergoline is administered orally in tablet form.

Dosages

• Initial dose: 0.25 mg twice weekly
• Maximum dose: 1 mg twice weekly

Side Effects

Frequency	Adverse reactions
Common Side Effects	Nausea, vomiting, dizziness, fatigue, and abdominal pain.
Serious Side Effects	Cardiac valvopathy, pulmonary fibrosis, severe hypotension, and compulsive behaviors (e.g. gambling)

Pharmacokinetics

• Onset of Action: Typically, within a few hours after administration.
• Duration of Action: Long-lasting effects, allowing for dosing twice weekly.
• Half-life: Approximately 63 to 109 hours after oral administration.

Drug Precautions

Pregnancy

The safety of cabergoline during pregnancy is not well established.

Breastfeeding

Cabergoline is not recommended during breastfeeding due to its potential effects on milk production.

Children and Elderly

Use in children requires careful consideration and monitoring. In elderly patients, increased sensitivity to side effects may occur; dosage adjustments may be necessary.

Drug Monitoring Items

Regular monitoring of:

• Prolactin levels
• Cardiac function (echocardiograms) to assess for valvular disease. Discontinuation is advised if new valvular regurgitation or thickening is detected.
• Blood pressure due to risk of orthostatic hypotension.
• Impulse Control Issues: Some patients may experience increased sexual urges or compulsive behaviors. Monitoring and possible dose adjustment are recommended if these symptoms occur.

Drug Interactions

• Dopamine Antagonists: Drugs like metoclopramide, phenothiazines, and butyrophenones may reduce the prolactin-lowering effect of cabergoline and should not be used concurrently.
• Anti-depressants such as
  • Cymbalta (duloxetine)
  • Lexapro (escitalopram)
  • Prozac (fluoxetine)
  • Zoloft (sertraline)
• Macrolide Antibiotics: Co-administration with macrolides (e.g. erythromycin) can increase the systemic bioavailability of cabergoline, thus increasing the risk of side effects.

FAQ

How Should I Take the Tablet?

Take cabergoline by mouth with or without food as directed by your healthcare provider.

What Should I Avoid While Taking?

Avoid activities requiring mental alertness until you know how cabergoline affects you; also limit alcohol consumption due to potential interactions.

What Happens if I Miss a Dose?

If you miss a dose, take it as soon as you remember unless it s almost time for your next dose; do not double up on doses.