Generic
Cabergoline
8 brands available in the market
At a glance
Cabergoline is a dopamine agonist used in the treatment of hyperprolactinemia (high prolactin levels) and for stopping breast milk production after childbirth. It works by reducing the amount of prolactin released from the pituitary gland.
Description
Cabergoline belongs to a group of drugs called dopamine receptor agonists. It works by reducing the amount of prolactin (a hormone) released from the pituitary gland.
Cabergoline is a long-acting dopamine receptor agonist with high affinity for D2 receptors. In vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on prolactin secretion by rat pituitary lactotrophs. Receptor binding studies indicate that cabergoline has low affinity for dopamine D1, α1 and α2 adrenergic, and 5HT1, 5HT2 serotonin receptors.
Indications
- Hyperprolactinemia (high prolactin levels)
- Suppression of postpartum lactation
- Prolactinoma (microprolactinoma)
- Hyperprolactinemia-associated infertility and galactorrhea
Therapeutic class
Antiparkinson drugs
Pharmacological class
Dopamine Receptor Agonist
Pharmacology
Cabergoline is a dopamine receptor agonist. Prolactin secretion by the anterior pituitary is mainly under hypothalamic inhibitory control, exerted through dopamine release by tuberoinfundibular neurons. Cabergoline is a long-acting dopamine receptor agonist with high affinity for D2 receptors. It exerts a direct inhibitory effect on prolactin secretion by pituitary lactotrophs.
Mechanism of action
Cabergoline activates D2 dopamine receptors, inhibiting prolactin secretion through the hypothalamic-pituitary axis. This reduces blood prolactin levels and suppresses lactation.
Dosage
Prevention of postpartum lactation: 1 mg as a single dose on the first day after delivery.
Suppression of lactation (if breastfeeding already started): 0.25 mg every 12 hours for 2 days.
Hyperprolactinemia (initial): 0.25 mg twice weekly. Increase by 0.25 mg every 4 weeks up to 1 mg twice weekly (based on serum prolactin levels).
Hyperprolactinemia (usual dose): 0.5 mg once weekly (divided into two doses, e.g., half tablet on Monday and half on Thursday). Maximum: 4.5 mg/week.
Parkinson's disease (monotherapy): Initially 0.5 mg/day; increase by 0.5-1 mg every 7-14 days. Max: 3 mg/day.
Parkinson's disease (adjunctive to levodopa): Initially 1 mg/day; increase by 0.5-1 mg every 7-14 days. Max: 3 mg/day.
Hepatic impairment: Dose adjustments may be needed.
Elderly: Start with lower doses.
Note: After normal prolactin levels are maintained for 6 months, cabergoline may be discontinued with periodic monitoring.
Administration
Take with food (to reduce nausea). Swallow tablets whole; do not chew, crush, or break. Follow the dose and duration as advised by your physician.
Missed dose
If you miss a dose, skip it and continue with your normal schedule. Do not double the dose.
Side effects
Common side effects: Nausea, headache, dizziness, low blood pressure, fatigue, drowsiness, constipation, vomiting, indigestion, hot flashes, blurred vision, vertigo.
Uncommon: Allergic reactions, hallucinations, serotonin syndrome, fibrotic reactions (heart, lungs, retroperitoneal) - with long-term use.
Precautions & warnings
- To reduce the chance of feeling dizzy or passing out, rise slowly from sitting or lying positions.
- Be cautious while driving or doing anything requiring concentration (may cause dizziness and sleepiness).
- Take with or after food to avoid nausea or indigestion.
- Do not take if breastfeeding (suppresses lactation).
- Regular blood pressure monitoring may be advised during treatment.
- Caution/contraindicated in severe liver disease, uncontrolled hypertension, psychotic disorders.
- Long-term use may cause fibrotic reactions (heart valves, lungs, retroperitoneum); regular monitoring required.
Contraindications
- Hypersensitivity to cabergoline or other ergot alkaloids
- Severe liver disease
- Uncontrolled hypertension
- Pregnancy-induced hypertension (pre-eclampsia/eclampsia)
- History of serious mental illness/psychotic disorders
- History of puerperal psychosis
- Pregnancy and breastfeeding (suppresses lactation)
Drug interactions
- Antihypertensives (blood pressure lowering medicines): Increased risk of orthostatic hypotension.
- Antipsychotics (chlorpromazine, haloperidol): May antagonize cabergoline effects.
- Antiemetics (domperidone, metoclopramide): May reduce cabergoline effects.
- Migraine medicines (pergolide, bromocriptine, lisuride, ergotamine, dihydroergotamine, ergometrine, methysergide): Increased vasoconstrictive effects.
- SSRIs/TCAs: Increased risk of serotonin syndrome.
- Sibutramine: Risk of serotonin syndrome (potentially fatal).
Food interactions
Caution is advised when consuming alcohol with Cabergoline (may increase dizziness and drowsiness).
Use in pregnancy
Generally considered safe during pregnancy (Category B). Animal studies have shown low or no adverse effects; limited human studies. Cabergoline stops milk production during pregnancy. Ensure patient is not pregnant before starting treatment.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Probably unsafe during breastfeeding. Cabergoline suppresses lactation, so it is usually not used during breastfeeding. Limited human data suggests the drug may pass into breast milk and harm the baby.
Pediatric use
Safety and effectiveness in pediatric patients have not been established.
Geriatric use
Elderly patients should start with lower doses and titrate slowly.
Renal / hepatic impairment
Hepatic impairment: Use with caution; dose adjustment may be needed (cabergoline is extensively metabolized by the liver).
Overdose effects
Overdose symptoms: Nasal congestion, syncope, hallucinations. Measures to support blood pressure should be taken if necessary. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store in a cool and dry place, protected from light. Keep out of reach of children.
Chemical structure
Cabergoline (Dopamine Receptor Agonist)