Bromocriptine (Parlodel)
First-generation ergot D2 dopamine agonist, Sandoz 1972 (Parlodel). Cabergoline's predecessor; shorter half-life (~3-12 h), more vegetative side effects (nausea, hypotension). Also marketed as Cycloset (2009 FDA) for T2DM.
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WHAT IS BROMOCRIPTINE (PARLODEL)?
Detailed overview
Bromocriptine (Parlodel) is a first-generation ergot-structure dopamine D2 receptor agonist synthesized by Sandoz (now Novartis) in 1972 and FDA-approved in 1978 for hyperprolactinemia (Parlodel 2.5/5 mg). It has a longer clinical history than cabergoline, and although largely superseded by the cleaner D2-selective cabergoline, it has remained in the AAS-PCT arsenal for three reasons: (1) Price – generic ~€3/box (vs cabergoline ~€25-40), particularly attractive on emerging-markets pharmaceutical markets; (2) Cabergoline intolerance fallback (when impulse-control disorder or persisting nausea occurs on cabergoline); (3) Metabolic-benefit secondary application – Cycloset (S2 Therapeutics, FDA 2009) is a special quick-release formulation of bromocriptine mesylate for improving insulin sensitivity in type 2 diabetes (Cincotta 1991/1996 PMIDs basis), which can be incidentally useful in the obese AAS cycler. Mechanistic profile: D1+D2 mixed agonist (vs cabergoline D2-selective), thus more vegetative side effects (nausea, orthostatic hypotension, dyskinesia), shorter half-life (~3-12 h, requiring 2-3× daily dosing).
Mechanism
First-gen ergot D1+D2 mixed DA agonist, prolactin suppression + secondary T2DM insulin sensitivity boost
Dosing (AAS prolactin)
1.25-5 mg/day divided 2-3× (start 1.25 mg with food, slow titration)
Half-life
~3-12 hours
Onset
Prolactin reduction 1-2 h, plateau 8-24 h
Legal status
FDA + EMA Rx, HU + PL approved, WADA allowed
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 8
- Nausea and vomiting (the most common effect, in a majority of patients), especially at the start of titration; mitigated by taking with food and slow dose escalation.
- Orthostatic (postural) hypotension, dizziness, fainting, especially after the first doses; rise slowly from sitting or lying.
- Headache, fatigue, nasal congestion and abdominal discomfort, vegetative accompaniments of the ergot-dopaminergic effect.
- Impulse-control disorders (compulsive gambling, shopping, hypersexuality, binge eating) plus daytime somnolence or sudden sleep onset, a class effect of dopamine agonists.
- Psychiatric symptoms at higher doses: confusion, hallucinations, dyskinesia (involuntary movements), agitation; usually dose-dependent and reversible on stopping.
- Raynaud-like peripheral vasospasm, coldness and digital discoloration; rarely severe, an ergot-class vasoconstrictive effect.
- With chronic high-dose use (Parkinson-protocol level) fibrotic complications: cardiac valve fibrosis, retroperitoneal and pleuropulmonary fibrosis; low at PCT doses, but annual echocardiography is warranted with prolonged use.
- Cycloset (quick-release 0.8 mg morning) form: milder vegetative profile, but nausea, fatigue and hypotension can still occur, especially combined with antihypertensives.
Contraindications · 7
- Uncontrolled hypertension, hypertensive disorders of pregnancy, eclampsia or preeclampsia history, and severe ischemic heart disease, because ergot vasospasm is dangerous (the postpartum indication was withdrawn for this reason).
- Ergot-alkaloid hypersensitivity (e.g. ergotamine, methylergometrine, other ergot derivatives) due to cross-allergy.
- Co-administration with antipsychotics (D2 antagonists) and other dopamine blockers (e.g. metoclopramide): mutually antagonistic effect, so antiemesis must NOT use metoclopramide.
- Impulse-control disorder, uncontrolled psychosis or significant psychiatric history, because the dopamine agonist can worsen them (also caution if ICD occurred on Cabergoline).
- Severe hepatic or renal impairment, because CYP3A4 metabolism and clearance are disturbed and drug levels can rise.
- Together with strong CYP3A4 inhibitors (macrolide antibiotics, azole antifungals, protease inhibitors): bromocriptine levels and toxicity rise, requiring dose reduction or avoidance.
- Pregnancy and breastfeeding: prolactin suppression inhibits lactation, and in pregnancy use only on strict indication; it can restore fertility, so unintended conception may occur.
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
Impact of menopause on outcomes in prolactinomas after dopamine agonist treatment withdrawal.
Santharam S, Fountas A, Tampourlou M
Evidence-based practice use of quick-release bromocriptine across the natural history of type 2 diabetes mellitus.
Schwartz SS, Zangeneh F
Bromocriptine in type 2 diabetes: a promising alternative, a systematic review and meta-analysis.
Dara T, Zabihi M, Hoseinzade F
Bromocriptine for diabetes – randomized controlled trial
Pijl H, Ohashi S, Matsuda M, et al.
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