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Cabergoline

Ergot-derived dopamine D2-receptor agonist · Antiprolactinemic, Ergoline derivative

Also known as Dostinex, Caberlin, Caba

START
Hyperprolactinaemia 0.25 mg twice weekly, titrate q4 weeks to prolactin
TYPICAL MAX
4.5 mg/week
STOP IF
New cardiac murmur/valvulopathy, fibrotic disease, impulse-control disorder
WATCH
Echocardiography (baseline + periodic on chronic therapy), prolactin, BP, impulse-control behaviours
CDSCO approvedSchedule H (Prescription drug in India)ATC G02CB03
Dose laddermg/d
0.25start1titrate4.5max weekly total
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR≥90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
30minONSET2hPEAK2.7dt½1wDURATION
ONSET
30min · absorption onset
PEAK
2h · Cmax
t½
2.7d · plasma t½
DURATION
1w · weekly dosing interval
EXCRETION
Hepatic hydrolysis; mainly faecal, minor renal
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Discontinue once pregnancy confirmed (restore fertility intentionally; limited late-pregnancy data) — use only if clearly needed
FDA category + note
Top interactionssee all 12 →
  • Serotonin 5ht2b ReceptorSevereTextbookG&G 14e · p929
  • AlmotriptanSevereDatabaseDDInter
  • AmisulprideSevereDatabaseDDInter
  • ClarithromycinSevereDatabaseDDInter
Available in India

44 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Long-acting selective D2-receptor agonist; inhibits pituitary prolactin secretion and (higher doses) reduces growth hormone; also dopaminergic CNS effects relevant in Parkinson disease (less used now due to fibrosis).

Indications

Hyperprolactinaemia (idiopathic, prolactinoma)Suppression/inhibition of physiological lactation (short course)Parkinson disease (adjunct — limited use due to valvulopathy risk)

Dosing

Adult
Hyperprolactinaemia: 0.25 mg twice weekly, titrate by 0.25 mg every ~4 weeks to prolactin response (usual 0.5–1 mg/week; max 4.5 mg/week). Lactation inhibition: 1 mg single dose day 1 postpartum (or 0.25 mg q12h ×2 for established).
Pediatric
Not established.
Renal adjustment
No adjustment.
Hepatic adjustment
Severe hepatic impairment: reduce dose.
Geriatric
Caution; monitor BP/fibrosis.
Max dose
4.5 mg/week (hyperprolactinaemia); higher Parkinson doses largely abandoned

Pharmacokinetics

Onset
Prolactin fall within hours; sustained
Peak effect
0.5–4 h (Cmax)
Duration
Days–week (very long action)
Half-life
~63–69 h
Bioavailability
Not fully defined; extensive tissue distribution
Protein binding
~40–42%
Metabolism
Hepatic hydrolysis (non-CYP predominant)
Excretion
Faecal (major) and renal (minor)

Contraindications

  • Uncontrolled hypertension / pre-eclampsia / eclampsia (lactation suppression)
  • History of cardiac valvulopathy or fibrotic disorders
  • Hypersensitivity to ergot derivatives

Side effects

Common
NauseaHeadacheDizziness/postural hypotensionFatigueConstipation
Serious
  • Cardiac valvular fibrosis/regurgitation (dose/duration-related)
  • Pleural/retroperitoneal/pericardial fibrosis
  • Impulse-control disorders (gambling, hypersexuality)
  • Severe hypotension; psychosis

Pregnancy & lactation

Pregnancy

Discontinue once pregnancy confirmed (restore fertility intentionally; limited late-pregnancy data) — use only if clearly needed

Lactation

Inhibits lactation — do not use when breastfeeding is desired

Drug interactions

Serotonin 5ht2b Receptor
Severe
Textbook

Valvular heart disease.

This effect is seen primarily at the high doses used in patients being treated for Parkinson disease and is not seen in the conventionally used doses (≤2 mg/week) for patients with prolactinomas.

Source: G&G 14e · p929

Almotriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Clarithromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Dextropropoxyphene
Severe
Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Dopamine Antagonists
Severe
Database

Antagonise cabergoline → loss of prolactin control

Avoid combination; use non-antagonist antiemetic

Source: Kimi deep-research + Cla

Eletriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Erythromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Frovatriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Lorcaserin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Naratriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Rizatriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Coeliac disease
OTHER · Gastroenterology · 2016
Inflammatory bowel disease
OTHER · Gastroenterology · 2015
Chronic kidney disease — assessment and management
KDIGO · Nephrology · 2024
Glomerular diseases
KDIGO · Nephrology · 2021
Chronic kidney disease — assessment and management
NICE · Nephrology · 2021

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19