Evigrade

Bromocriptine

Dopamine D2 receptor agonist, ergot derivative

ATC code: N04BC01

Brand names: Parlodel, Cycloset

Updated · Methodology

Indications

A

Hyperprolactinemia

Second line

Bromocriptine is a second-line dopamine agonist for hyperprolactinemia and pituitary microadenomas. SEEN recommends cabergoline as first choice (better tolerability and twice-weekly dosing); bromocriptine remains an option in pregnancy and when cabergoline is unavailable. Effect over 1–3 months, dose titrated from 1.25 mg twice daily.

ICD-10: E22.1 · ICD-11: 5A60.1

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Activates postsynaptic dopamine D2 receptors in pituitary, striatum and other brain regions. In pituitary suppresses prolactin and growth hormone secretion. In nigrostriatal system compensates for dopamine deficit in Parkinson disease. Ergot structure retains vasoconstrictor activity and serotonin receptor binding, hence vasospasm and valvulopathy risk. Metabolised by CYP3A4.

Safety

Contraindications

  • Uncontrolled hypertension
  • Eclampsia, preeclampsia
  • Ischemic heart disease
  • Peripheral vascular disease
  • Prior psychosis
  • Combination with erythromycin, clarithromycin (CYP3A4)

Serious adverse effects

  • Stroke and MI (especially in lactation suppression)
  • Psychosis, hallucinations
  • Retroperitoneal and pleuropulmonary fibrosis on long-term use
  • Impulse control disorders

Common adverse effects

  • Nausea, vomiting
  • Orthostatic hypotension
  • Headache
  • Nasal congestion
  • Drowsiness

Pregnancy: can you take Bromocriptine?

Among dopamine agonists, bromocriptine has the most pregnancy data without increased birth defect rate. Used when pregnancy is planned in women with prolactinoma.

Breastfeeding: can you take Bromocriptine?

Suppresses lactation – not used in nursing mothers. Historically used for lactation suppression; FDA withdrew that indication in 1994 due to stroke cases.

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Drug–drug interactions

2 pairs found. Sorted from critical to minor.

CriticalClarithromycinMacrolide antibiotic

Mechanism

CYP3A4 inhibition – bromocriptine rises 4-5 fold.

Symptoms

MI, stroke.

Management

Combination contraindicated.

Pair details →Clarithromycin →

MajorErythromycinMacrolide antibiotic

Mechanism

Bromocriptine is broken down in the liver by CYP3A4, and erythromycin inhibits this enzyme. With erythromycin, bromocriptine area under the curve (AUC) rose 2.8- to 3.7-fold and peak concentration 4.6-fold.

Symptoms

Bromocriptine side effects get stronger: nausea, vomiting, headache, dizziness, a drop in blood pressure on standing (rarely with fainting), drowsiness, confusion and hallucinations.

Management

Avoid the combination. The intravenous erythromycin label advises against using it with dopaminergic ergot alkaloids, the group that includes bromocriptine. It allows erythromycin with bromocriptine only if bromocriptine effects and side effects can be closely monitored; otherwise bromocriptine is stopped for the erythromycin course (erythromycin label). The bromocriptine dose may need to be lowered during co-administration (erythromycin label). The bromocriptine label advises caution with macrolides because they raise bromocriptine levels (bromocriptine label). For the bromocriptine formulation used in type 2 diabetes in the US, the US Food and Drug Administration () caps the dose at 1.6 mg a day with erythromycin (bromocriptine FDA label).

Pair details →Erythromycin →

Label mentions8 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • MajorCYP3A4 inhibitorsclass named in the label
    «DRUG INTERACTIONS: Avoid concomitant use of bromocriptine mesylate with strong CYP3A4 inhibitors. Follow the recommended bromocriptine mesylate dosage modifications during concomitant use with…»

    FDA, section 7 · Open on DailyMed

From other drugs’ labels

  • «Levodopa: antagonismo recíproco de efectos entre levodopa y neurolépticos. Amisulprida puede oponerse al efecto de los agonistas dopaminérgicos p. ej., bromocriptina, ropinirol.»

    AEMPS, section 4.5 · Open on CIMA

  • «DRUG INTERACTIONS: Alfentanil Bromocriptine Cilostazol Methylprednisole Vinblastine Phenobarbital St. John’s Wort Use With Caution There have been spontaneous or published reports of CYP3A based…»

    FDA, section 7 · Open on DailyMed

  • ModerateErythromycin
    «La eritromicina es un inhibidor de la CYP3A4 y la proteína transportadora glucoproteína P. Es difícil predecir el alcance de la inhibición de los distintos sustratos del CYP3A4. Por lo tanto, no…»

    AEMPS, section 4.5 · Open on CIMA

  • «Los inhibidores del CYP3A4 pueden reducir el metabolismo de sirolimus y aumentar los niveles en sangre de sirolimus. Estos inhibidores incluyen ciertos antifúngicos (p.ej., clotrimazol, fluconazol…»

    AEMPS, section 4.5 · Open on CIMA

  • «Weak and Moderate Inducers or Inhibitors of CYP3A4 and P-gp: Drugs that could increase sirolimus blood concentrations: Bromocriptine, cimetidine, cisapride, clotrimazole, danazol, diltiazem…»

    FDA, section 7 · Open on DailyMed

  • «Recomendaciones relativas a la a dministración simultánea: In vitro , se ha demostrado que las siguientes sustancias son potenciales inhibidores del metabolismo de tacrólimus: bromocriptina…»

    AEMPS, section 4.5 · Open on CIMA

  • «Drug Interactions:: Concomitant bromocriptine therapy has been shown to elevate serum tamoxifen and N-desmethyl tamoxifen.»

    FDA, section 7 · Open on DailyMed

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Frequently asked

What is Bromocriptine used for?

Bromocriptine is evaluated for the following indications with varying evidence strength: Hyperprolactinemia (evidence tier A). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Bromocriptine?

Common side effects of Bromocriptine (≥ 1 in 100): Nausea, vomiting, Orthostatic hypotension, Headache, Nasal congestion, Drowsiness. See the Safety section for uncommon and serious reactions.

Is Bromocriptine safe during pregnancy?

Among dopamine agonists, bromocriptine has the most pregnancy data without increased birth defect rate. Used when pregnancy is planned in women with prolactinoma.

Is Bromocriptine compatible with breastfeeding?

Suppresses lactation – not used in nursing mothers. Historically used for lactation suppression; FDA withdrew that indication in 1994 due to stroke cases.

Who should not take Bromocriptine?

Bromocriptine is contraindicated in: Uncontrolled hypertension; Eclampsia, preeclampsia; Ischemic heart disease; Peripheral vascular disease; Prior psychosis. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Cabergoline, Levodopa + Carbidopa + Entacapone, Pramipexole, Rasagiline, Ropinirole, Selegiline