Generic
Bromocriptine
7 brands available in the market
At a glance
Bromocriptine is a dopamine agonist and prolactin inhibitor used in the treatment of hyperprolactinemia-associated infertility, abnormal milk production (galactorrhea), amenorrhea, acromegaly, and Parkinson's disease. It works by reducing prolactin secretion.
Description
Bromocriptine mesilate is a nonhormonal, nonestrogenic agent that inhibits the secretion of prolactin in humans, with little or no effect on other pituitary hormones, except in patients with acromegaly, where it lowers elevated blood levels of growth hormone.
Bromocriptine is a dopamine receptor agonist that activates post-synaptic dopamine receptors. The dopaminergic neurons in the tuberoinfundibular process modulate prolactin secretion from the anterior pituitary by secreting a prolactin inhibitory factor (thought to be dopamine).
Indications
- Hyperprolactinemia-associated dysfunctions (amenorrhea with or without galactorrhea, infertility, hypogonadism)
- Prolactin-secreting adenomas (to reduce tumor mass prior to surgery)
- Acromegaly
- Parkinson's disease (adjunctive treatment to levodopa)
Therapeutic class
Antiparkinson drugs, Motility stimulants/Dopamine antagonist
Pharmacological class
Dopamine Receptor Agonist (Ergot Alkaloid)
Pharmacology
Bromocriptine mesilate is a dopamine receptor agonist that activates post-synaptic dopamine receptors. The dopaminergic neurons in the tuberoinfundibular process modulate prolactin secretion from the anterior pituitary by secreting a prolactin inhibitory factor (thought to be dopamine). In the corpus striatum, dopaminergic neurons are involved in motor function control. Clinically, it significantly reduces plasma prolactin levels in patients with physiologically elevated prolactin and hyperprolactinemia.
Mechanism of action
Bromocriptine activates postsynaptic dopamine receptors in the tuberoinfundibular and nigrostriatal pathways. It inhibits prolactin secretion from the anterior pituitary and reduces growth hormone levels in acromegaly. In Parkinson's disease, it enhances levodopa efficacy.
Dosage
Hyperprolactinemia (Adults): Initial: 0.5-2.5 mg daily. Add 2.5 mg every 2-7 days until therapeutic response. Usual therapeutic dose: 5-7.5 mg/day (range: 2.5-15 mg/day). Up to 30 mg/day used in amenorrhea/galactorrhea.
Hyperprolactinemia (11-15 years): Initial: 1.25-2.5 mg daily; Maintenance: 2.5-10 mg/day.
Acromegaly: 1.25-2.5 mg at night (with food) for 3 days. Add 1.25-2.5 mg every 3-7 days. Maximum: 100 mg/day.
Parkinson's disease (adjunctive to levodopa): Week 1: 1-1.25 mg at night; Week 2: 2-2.5 mg at night; Week 3: 2.5 mg twice daily; Week 4: 2.5 mg 3 times daily; Maintenance: 10-40 mg/day.
Lactation suppression: 2.5 mg/day for 2-3 days, up to 2.5 mg twice daily for 14 days.
Prevention of puerperal lactation: 2.5 mg on delivery day, then 2.5 mg twice daily for 14 days.
Cyclical benign breast and menstrual disorders: 2.5 mg twice daily.
Hepatic impairment: Dose adjustment may be necessary; no guidelines available.
Administration
Take with food (after meals or with meals) to reduce nausea. Swallow tablet whole; do not chew, crush or break. During dose escalation, patients should be evaluated frequently to determine the lowest effective dose.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects (decreasing frequency):
Nausea, headache, dizziness, fatigue, lightheadedness, vomiting, abdominal cramps, nasal congestion, constipation, diarrhea, drowsiness.
A slight hypotensive effect may occur. Temporary dose reduction to 0.5 mg may lessen adverse reactions.
Laboratory abnormalities (elevated BUN, SGOT, SGPT, GGPT, CPK, alkaline phosphatase, uric acid) are usually transient and not clinically significant.
Precautions & warnings
- Taking with food helps avoid nausea or indigestion.
- To lower the chance of feeling dizzy or passing out, rise slowly from sitting or lying positions.
- May cause dizziness and sleepiness; use caution while driving or doing anything requiring concentration.
- Do not take if breastfeeding (suppresses lactation).
- Regular blood pressure monitoring may be advised during treatment.
- Caution in patients with renal or hepatic disease.
- Use with caution in patients with history of psychosis or cardiovascular disease.
Contraindications
- Uncontrolled hypertension
- Hypersensitivity to any ergot alkaloids
- Pregnancy (withdraw when pregnancy is diagnosed in hyperprolactinemia treatment)
- Postpartum period in women with history of coronary artery disease and other severe cardiovascular conditions
Drug interactions
- Dopamine antagonists (phenothiazines, haloperidol, metoclopramide, pimozide): Decrease bromocriptine efficacy.
- Other ergot alkaloids: Concomitant use is not recommended.
- Erythromycin: Bioavailability increased.
- Alcohol: Reduces tolerance to bromocriptine and vice versa.
- Antihypertensives: Effects may be potentiated.
- Psychotropics: Avoid concurrent use.
Food interactions
Alcohol consumption is unsafe (alcohol reduces tolerance to bromocriptine and vice versa).
Use in pregnancy
Generally considered safe during pregnancy (Category B). Animal studies have shown low or no adverse effects; limited human studies. In hyperprolactinemia, withdraw when pregnancy is diagnosed.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Probably unsafe during breastfeeding. Bromocriptine suppresses lactation, so it is usually not used during breastfeeding. Limited human data suggests the drug may pass into breast milk and harm the baby.
Pediatric use
No data available for children under 8 years. 11-15 years: Initial 1.25-2.5 mg/day; Maintenance 2.5-10 mg/day.
Geriatric use
No specific dose adjustment required for elderly, but caution advised (start with low dose).
Renal / hepatic impairment
Hepatic impairment: Limited information available; dose adjustment may be needed. Use with caution.
Overdose effects
Overdose symptoms: Nausea, vomiting, dizziness, hypotension, hallucinations, confusion. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.
Chemical structure
Bromocriptine Mesilate (Ergot Alkaloid Dopamine Agonist)