Bromocriptine

Class
Antiparkinsonian agents
Subclass
Dopamine agonists
Substance name
Bromocriptine mesylate
Brand names
Parlodel®, Cycloset®
Common formulations
Gelatin-coated capsule, Tablet
Dosage and administration
Adults patients
Symptomatic relief
Mastalgia with premenstrual syndrome • Off-label
•
2.5 mg PO BID
Treatment
Acromegaly
•
Start at: 1.25-2.5 mg PO daily for 3 days
•
Maintenance: 20-30 mg PO daily
•
Maximum: 100 mg per day
Titrate in 1.25-2.5 mg every 3-7 days to achieve optimal response. Reevaluate monthly and adjust dosage based on GH reduction and clinical response. Withdraw bromocriptine every year for 4-8 weeks in patients treated with irradiation.
Diabetes mellitus type 2
•
Start at: 0.8 mg PO qAM
•
Maintenance: 1.6-4.8 mg PO qAM, within 2 hours after waking
•
Maximum: 4.8 mg per day
Titrate in 0.8 mg increments weekly to the maximal tolerated dose.
Hyperprolactinemia
•
Start at: 1.25-2.5 mg PO daily
•
Maintenance: 2.5-15 mg PO daily
Titrate in 2.5 mg increments every 2-7 days to achieve optimal response.
Other off-label uses
•
Facilitation of lactation suppression in females
•
Adjunctive treatment for neuroleptic malignant syndrome (moderate-to-severe)
Indications for use
Labeled indications
Adults
•
Treatment of acromegaly
•
Treatment of diabetes mellitus type 2
•
Treatment of hyperprolactinemia
•
Adjunctive treatment for Parkinson's disease
Off-label indications
Adults
•
Symptomatic relief of mastalgia with premenstrual syndrome
•
Facilitation of lactation suppression in females
•
Adjunctive treatment for neuroleptic malignant syndrome (moderate-to-severe)
Safety risks
Contraindications
Hypersensitivity to bromocriptine or its components or to other ergot alkaloids
Galactose intolerance, severe lactase deficiency, or glucose-galactose malabsorption
Postpartum patients
•
Do not use bromocriptine in postpartum patients due to the increased risk of hypertension, myocardial infarction, stroke, and seizures.
Severe psychotic disorders
•
Use caution in patients with a history of psychotic disorders.
Syncopal migraine
T1DM or diabetic ketoacidosis
Uncontrolled hypertension
Concomitant use of dopamine receptor antagonists
•
Do not use bromocriptine with dopamine receptor antagonists, including neuroleptic agents having dopamine D2 receptor antagonist properties, such as clozapine, olanzapine, and ziprasidone.
Concomitant use of ergot alkaloids
Concomitant use of other dopamine receptor agonists
Concomitant use of strong CYP3A4 inhibitors
•
Do not use bromocriptine with strong CYP3A4 inhibitors (such as azole antimycotics, human imunodeficiency virus protease inhibitors), and ensure adequate washout of the strong CYP3A4 inhibitor before initiating bromocriptine. Do not exceed bromocriptine dose of 1.6 mg once daily when used with a moderate CYP3A4 inhibitor (such as erythromycin).
Warnings and precautions
Confusion
•
Use caution in patients with Parkinson's disease, especially when receiving high doses of bromocriptine, as patients with Parkinson's disease may present with mild degrees of dementia.
Digital vasospasm
•
Maintain a high level of suspicion, as bromocriptine has been reported to cause cold-sensitive digital vasospasm in patients with acromegaly.
Exacerbation of cardiac arrhythmias
•
Use caution in patients with a history of myocardial infarction with residual atrial, nodal, or ventricular arrhythmia.
Exacerbation of CVD
•
Use caution in patients with CVDs.
Fibrotic complications
•
Maintain a high level of suspicion, as bromocriptine has been associated with an increased risk of pleural and pericardial effusions, pleural and pulmonary fibrosis, constrictive pericarditis, and retroperitoneal fibrosis, particularly with long-term or high-dose treatment.
Gastrointestinal bleeding
•
Use caution in patients with a history of peptic ulcer disease or gastrointestinal bleeding, especially with acromegaly.
Hallucinations
•
Maintain a high level of suspicion, as bromocriptine has been associated with an increased risk of visual and auditory hallucinations in patients with Parkinson's disease. Assess orthostatic vital signs before initiation and during treatment.
Hypotension
•
Use caution in patients taking antihypertensive agents.
•
Maintain a high level of suspicion, as bromocriptine may cause symptomatic hypotension, particularly upon initiation and dose escalation. Assess orthostatic vital signs before initiation and during treatment.
Impulsivity, compulsive behavior
•
Maintain a high level of suspicion, as bromocriptine has been associated with an increased risk of impulsive behaviors, including intense urges for gambling, spending money, sexual activity, and other impulses.
Neuroleptic malignant syndrome, dopamine agonist withdrawal syndrome
•
Do not discontinue abruptly in patients taking the drug for a prolonged period.
Somnolence
•
Use extreme caution in patients performing activities requiring mental alertness, such as driving or operating machinery.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Use caution in patients receiving bromocriptine for diabetes.
Renal replacement therapy
Any modality
•
Use acceptable. No dose adjustment required. Use caution in patients receiving bromocriptine for diabetes.
Hepatic impairment
Any severity
•
Use with caution.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B2, A
•
Use only if benefits outweigh potential risks. Obtain pregnancy testing at least every 4 weeks during the amenorrheic period, and, once menstruation is reinitiated, every time a patient misses a menstrual period, as pregnancy may occur before reinitiation of menstruation. Advise patients to use contraceptive measures, other than oral contraceptives, during treatment with bromocriptine if they do not seek pregnancy or have large adenomas.
•
Withdraw therapy when bromocriptine is used for hyperprolactinemia in patients who subsequently become pregnant. Decide whether to continue therapy if medically necessary or to withdraw therapy when bromocriptine is used for acromegaly, prolactinoma, or Parkinson's disease in patients who subsequently become pregnant.
•
Weigh the benefits against the potential risks of using bromocriptine in hypertensive disorders of pregnancy when it is reinstituted to control a rapidly expanding macroadenoma.
•
Do not use bromocriptine during the postpartum period in patients with a history of coronary artery disease or other severe cardiovascular conditions unless withdrawal is considered medically contraindicated. Observe the patients with caution if bromocriptine is used in the postpartum period.
Breastfeeding
Do not use during breastfeeding.
Unknown drug levels in breastfed infants.
Unlikely to cause adverse effects in breastfed infants.
Significant adverse effects on lactation reported.
Adverse reactions
Very common > 10%
•
Asthenia, constipation, dizziness, fatigue, headache, nasal congestion, nausea
Common 1-10%
•
Amblyopia, ↓ blood glucose, gastrointestinal bleeding, raynaud's phenomenon, orthostatic hypotension, abdominal cramps, dry mouth, confusion, abdominal discomfort, ataxia, depression, hypotension, diarrhea, dyspepsia, hypoesthesia, lightheadedness, loss of appetite, somnolence, digital vasospasm, syncope, vomiting, sinusitis
Uncommon < 1%
•
Alcohol potentiation, anxiety, blepharospasm, dysphagia, peripheral edema, erythromelalgia, seizure, lethargy, skin mottling, nervousness, nightmares, skin rash, urinary frequency, urinary incontinence, urinary retention, hair loss, cardiac arrhythmias, VT, visual hallucinations, dyspnea, bradycardia, vertigo, paresthesia, delusions, insomnia, paranoid ideation, cold intolerance, tinnitus, muscle cramps, pallor
Rare < 0.1%
•
Ergotism, pulmonary fibrosis
Unknown frequency
•
↑ serum transaminases, ↑ serum gamma-glutamyltransferase, ↑ serum CK, ↑ serum ALP, ↑ serum uric acid, agitation, ↑ libido, impulsivity, compulsive behavior, dyskinesia, blurred vision, visual disturbances, leg cramps, pericardial effusion, pleural effusion, constrictive pericarditis, retroperitoneal fibrosis, cardiac valve fibrosis, pleurisy, pleural fibrosis, peptic ulcer disease, neuroleptic malignant syndrome, dopamine agonist withdrawal syndrome, myocardial infarction
Interactions
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