CABERGOLINE 0.25mg ZPHC

Cabergoline is an ergot-derived dopamine receptor agonist that primarily acts on D2 dopamine receptors in the pituitary gland. By stimulating these receptors, cabergoline inhibits the secretion of prolactin, a hormone responsible for milk production and regulation of the menstrual cycle.

Uses:

• Hyperprolactinemia: Elevated prolactin levels causing menstrual irregularities, galactorrhea (abnormal milk secretion), and infertility.

• Prolactinomas: Benign pituitary tumors that overproduce prolactin.

• Occasionally used in Parkinson’s disease to supplement dopamine therapy.

Dosage & Administration:

• Typically administered orally, often 1–2 times per week, depending on the condition and patient response.

• Dose titration is common to minimize side effects.

Pharmacokinetics:

• Absorption: Well absorbed orally, but bioavailability may vary.

• Half-life: Long (~65 hours), allowing infrequent dosing.

• Metabolism: Primarily hepatic.

• Excretion: Mainly via urine and bile.

Side Effects:

• Common: Nausea, headache, dizziness, fatigue, low blood pressure (especially when standing).

• Rare/Serious: Cardiac valve disorders (with long-term high-dose use), psychiatric effects (e.g., hallucinations), and fibrotic reactions.

Precautions:

• Monitor heart function for long-term therapy.

• Use cautiously in patients with psychiatric disorders or hypotension.

• Pregnancy and lactation safety should be discussed with a healthcare provider.

Mechanism of Action:
Cabergoline mimics dopamine, binding to D2 receptors in the anterior pituitary. This suppresses prolactin secretion, restoring normal hormonal balance and alleviating symptoms caused by hyperprolactinemia.