Cabergoline (Dostinex)
Long-acting ergot D2 dopamine agonist. EMA-approved (1992 Pharmacia, now Pfizer) for hyperprolactinemia. In AAS: 19-Nor/Tren prolactin-control golden-standard, 0.25-0.5 mg 2x/week bloodwork-titrated. Long t1/2 ~63 h.
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Related comparisons
Cabergoline vs Bromocriptine vs PramipexoleWHAT IS CABERGOLINE (DOSTINEX)?
Detailed overview
Cabergoline (Dostinex) is a long-acting ergot-structure selective D2 dopamine receptor agonist developed by Farmitalia Carlo Erba (later Pharmacia, now Pfizer) and approved by the EMA in 1992 (FDA 1996) for the treatment of hyperprolactinemia and prolactinoma. It exerts an agonist effect on D2 receptors of pituitary lactotrophs, suppressing prolactin secretion – the Webster 1994 head-to-head trial (PMID 8090165) demonstrated that cabergoline is more effective and better tolerated than the older bromocriptine (~95% prolactin normalization vs ~75%). In AAS context: 19-Nor steroids (trenbolone, nandrolone, MENT) elevate prolactin levels both directly and indirectly – trenbolone also agonizes the progesterone receptor, while nandrolone augments the cabergoline-sensitive prolactinergic pathway. Symptoms: Tren flu, lactation (galactorrhea), libido decline, gynecomastia formation (prolactin-mediated, NOT E2). Cabergoline is the classic 19-Nor/Tren cycle prolactin-control gold-standard: 0.25-0.5 mg 2x/week (Mon+Thu) bloodwork-titrated, targeting prolactin <15 ng/mL.
Mechanism
Long-acting ergot D2 DA agonist, pituitary lactotroph prolactin suppression
Dosing (AAS)
0.25-0.5 mg 2x/week (Mon+Thu) bloodwork-titrated
Half-life
~63-69 hours (very long)
Onset
Prolactin reduction measurable 3 h, plateau 48-72 h
Legal status
EMA + FDA Rx, HU + PL approved, WADA allowed (not listed)
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 7
- Nausea, vomiting and gastrointestinal upset, mainly with the first doses; reduced by taking it after food and titrating slowly.
- Orthostatic (postural) hypotension, dizziness and faintness, especially at the start of dosing or on standing up.
- Headache, fatigue and somnolence; rarely sudden sleep onset, so driving and operating machinery require caution.
- Impulse-control disorders (pathological gambling, hypersexuality, compulsive shopping or eating) – a dopamine-agonist class effect, rarer with cabergoline but documented.
- Cardiac valve damage (regurgitation, fibrotic change) – an ergot-derived, 5-HT2B-mediated class effect, mainly with prolonged high (Parkinson-level) doses; rare at AAS doses, but annual echocardiography is warranted with chronic use.
- Overdosing or too-aggressive titration can push prolactin below normal, causing low libido, low mood and persistent fatigue ('prolactin crash').
- Pulmonary, pleural and retroperitoneal fibrosis (connective-tissue scarring) – a rare, dose- and duration-dependent ergot-alkaloid effect with chronic use.
Contraindications · 7
- Pre-existing cardiac valve disease or previously documented valvular fibrosis/regurgitation – an ergot-derived agent is contraindicated here.
- Ergot-alkaloid hypersensitivity or allergy (e.g. cross-reactivity with bromocriptine, methysergide).
- Pregnancy and breastfeeding: cabergoline suppresses lactation and may restore ovulation; in planned pregnancy use only under supervision, and consider contraception.
- Uncontrolled severe hypertension or hypertensive disorders of pregnancy (preeclampsia/eclampsia) – increased blood-pressure and vasospasm risk.
- Concurrent D2-antagonist antipsychotic therapy (haloperidol, risperidone, olanzapine) – mechanistic conflict, the effects cancel each other.
- Severe hepatic impairment – reduced CYP3A4 metabolism leads to higher drug levels and increased side-effect risk.
- History of pulmonary, pleural or retroperitoneal fibrosis – ergot agents can worsen it.
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
Retrospective comparison of cabergoline and bromocriptine effects in hyperprolactinemia: a single center experience.
Arduc A, Gokay F, Isik S, Ozuguz U, Akbaba G, Tutuncu Y, Berker D, Guler S
Risks of Cardiac Valve Regurgitation and Heart Failure Associated with Ergot- and Non-Ergot-Derived Dopamine Agonist Use in Patients with Parkinson's Disease: A Systematic Review of Observational Studies.
Tran T, Brophy JM, Suissa S, Renoux C
Effects of acute prolactin manipulation on sexual drive and function in males.
Krüger TH, Haake P, Haverkamp J, Krämer M, Exton MS, Saller B, Mann K, Hartmann U, Schedlowski M
Impulse control disorders in Parkinson disease: a cross-sectional study of 3090 patients (DOMINION study)
Weintraub D, Koester J, Potenza MN, et al.
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