Bromolac2.5 mg

Bromolac is a dopamine receptor agonist with the following evidence-based indications:

Established / FDA-approved uses

• Hyperprolactinemia-associated dysfunctions: amenorrhea (with or without galactorrhea), infertility, or hypogonadism caused by prolactin-secreting pituitary adenomas (micro- and macroadenomas) or idiopathic hyperprolactinemia. Bromolac can also be used to reduce tumor size before surgery in patients with prolactin-secreting adenomas.
• Acromegaly: used alone or as an adjunct to pituitary irradiation or surgery to reduce elevated growth hormone levels when other therapies are inadequate or not feasible.
• Parkinson's disease: used as adjunctive therapy with levodopa (with or without a decarboxylase inhibitor) to provide additional benefit in patients experiencing tolerance or "end-of-dose" failure.

Adjunct / specific-formulation use

• A quick-release formulation of Bromolac is approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus; this use requires a specific quick-release product and is not interchangeable with standard-release tablets/capsules.

Bromolac is not indicated for suppression of physiologic lactation.

Each tablet contains Bromocriptine Mesylate equivalent to 2.5 mg of bromocriptine base. Capsule formulations (2.5 mg and 5 mg, as Bromocriptine Mesylate) are also available in some markets. Excipients vary by manufacturer.

Bromolac is a semi-synthetic ergot alkaloid derivative that acts as a potent dopamine D2-receptor agonist. It was first developed for the treatment of hyperprolactinemia and has since found use in acromegaly, Parkinson's disease, and (as a specific quick-release formulation) as an adjunct for glycemic control in type 2 diabetes.

Bromolac is administered orally, typically taken with food to reduce gastrointestinal upset, and is dosed individually based on indication and patient tolerance.

Bromolac belongs to the therapeutic class of dopamine receptor agonists (ergot alkaloid derivatives), used as an anti-parkinsonian agent and prolactin-secretion inhibitor.

Bromocriptine Mesylate is a dopamine D2-receptor agonist derived from ergot. Its principal pharmacologic actions include:

• Inhibition of prolactin secretion: by directly stimulating dopamine D2 receptors on lactotroph cells of the anterior pituitary, Bromocriptine Mesylate suppresses prolactin release without affecting other pituitary hormones under normal conditions.
• Growth hormone reduction: in acromegaly, Bromocriptine Mesylate paradoxically lowers elevated growth hormone levels in a majority of patients, likely via stimulation of hypothalamic/pituitary dopamine receptors (the opposite effect seen in healthy individuals).
• Central dopaminergic activity: in Parkinson's disease, Bromocriptine Mesylate directly stimulates postsynaptic dopamine receptors in the corpus striatum, compensating for reduced endogenous dopamine synthesis.

Bromocriptine Mesylate is well absorbed after oral administration but undergoes extensive first-pass hepatic metabolism, resulting in low absolute bioavailability. It is highly protein-bound and eliminated mainly via biliary/fecal excretion, with a minor renal component.

Bromolac should be taken orally with food (a meal or snack) to reduce nausea and gastrointestinal upset. Tablets/capsules should be swallowed whole. The first dose is often taken at bedtime to reduce the impact of dizziness or hypotension. Do not stop or change the dose without consulting a physician, as abrupt changes can affect symptom control.

Bromolac has the following clinically significant drug interactions:

• Dopamine antagonists (phenothiazines, butyrophenones, metoclopramide, pimozide): may reduce the effectiveness of Bromolac by blocking dopamine receptors; concurrent use is generally avoided.
• Potent CYP3A4 inhibitors (e.g., azole antifungals, HIV protease inhibitors, certain macrolide antibiotics such as erythromycin): can significantly increase plasma concentrations of Bromolac (erythromycin has been shown to raise levels several-fold), increasing the risk of side effects; concurrent use requires caution and possible dose adjustment.
• Other ergot alkaloids: concurrent use with Bromolac is not recommended due to additive ergot-related toxicity.
• Octreotide and other somatostatin analogs: may increase systemic exposure to Bromolac.
• Alcohol: may potentiate side effects (nausea, dizziness) of Bromolac and should be limited.
• Antihypertensive agents: additive blood-pressure-lowering effect; monitor for symptomatic hypotension.

Side effects of Bromolac vary somewhat by indication and dose, but commonly include:

• Very common: nausea, headache, dizziness/lightheadedness, fatigue.
• Common: orthostatic (postural) hypotension, vomiting, abdominal cramps, constipation or diarrhea, nasal congestion, drowsiness.
• Less common but important: sudden onset of sleep, hallucinations and confusion (particularly in Parkinson's disease), impulse-control or compulsive behaviors (e.g., pathological gambling, hypersexuality), pleural or pericardial effusion, and retroperitoneal or cardiac valve fibrosis with prolonged high-dose use.

Starting at a low dose, titrating gradually, and taking Bromolac with food reduce the frequency of gastrointestinal and hypotensive side effects. Report any severe or persistent side effect to a physician promptly.

Pregnancy: Bromolac should be used during pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus; a physician should be consulted before use in pregnancy. For hyperprolactinemia, Bromolac is typically discontinued once pregnancy is confirmed unless there is a specific reason (e.g., a rapidly enlarging macroadenoma) to continue, in which case ongoing use requires close specialist supervision.

Lactation: Bromolac suppresses prolactin secretion and is not recommended for use during breastfeeding, as it can inhibit milk production; it should not be used to treat postpartum women who wish to breastfeed. Discuss any need for Bromolac during breastfeeding with a physician.

The following precautions apply to Bromolac therapy:

• Postpartum cardiovascular events: rare but serious events (stroke, myocardial infarction, seizures, severe hypertension) have been reported when Bromolac was used for lactation suppression; blood pressure should be monitored closely, especially during the first weeks of treatment, and postpartum women with a history of cardiovascular disease should generally avoid Bromolac.
• Symptomatic hypotension: may occur, especially at initiation; monitor blood pressure, particularly in the first days of treatment or after dose increases.
• Sudden sleep onset and somnolence: patients should be cautioned about driving or operating machinery until they know how Bromolac affects them.
• Peptic ulcer disease: use with caution, as Bromolac may rarely be associated with gastrointestinal bleeding.
• Psychiatric disorders: Bromolac can worsen psychosis and should be used cautiously, if at all, in patients with a history of severe psychiatric illness.
• Fibrotic complications: long-term, high-dose use has been associated with pleural, pericardial, and retroperitoneal fibrosis and cardiac valvulopathy; periodic clinical monitoring is advised for patients on prolonged high-dose therapy.

See Contraindications for absolute restrictions on use.

Overdose of Bromolac may cause nausea, vomiting, constipation, sweating, severe hypotension, confusion, hallucinations, and drowsiness.

If an overdose is suspected, seek immediate medical attention or contact a poison control center/emergency services right away. Treatment is supportive and may include measures to reduce further absorption and management of blood pressure under medical supervision; do not attempt specific home treatment.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Renal impairment: Bromolac has not been extensively studied in renal impairment; use with caution and monitor closely, as reduced clearance may increase side effects.

Hepatic impairment: since Bromolac undergoes extensive hepatic metabolism, patients with significant liver impairment may require lower doses and closer monitoring; caution is advised.

Elderly: may be more susceptible to orthostatic hypotension and confusion; start at the lowest effective dose and titrate slowly.

Pediatric use: see Pediatric Uses below.

Duration of treatment with Bromolac depends on indication. Hyperprolactinemia often requires long-term therapy with periodic reassessment of prolactin levels and tumor size (and a trial of dose reduction or discontinuation is sometimes considered after prolonged normal prolactin levels, under physician guidance). Parkinson's disease treatment is typically long-term/chronic as adjunctive therapy. Acromegaly treatment is generally long-term unless alternative definitive therapy (surgery/radiotherapy) achieves control. Treatment duration should always be determined and periodically reviewed by the prescribing physician.

Bromocriptine Mesylate is classified as an ergot-derived dopamine D2-receptor agonist.

Bromocriptine Mesylate directly stimulates dopamine D2 receptors. In the anterior pituitary, this action inhibits prolactin secretion from lactotroph cells. In the hypothalamic-pituitary axis of patients with acromegaly, it paradoxically reduces growth hormone secretion. In the central nervous system, particularly the corpus striatum, Bromocriptine Mesylate activates postsynaptic dopamine receptors, which helps compensate for dopamine deficiency in Parkinson's disease when used alongside levodopa.

B

For hyperprolactinemia, Bromolac may be used in children and adolescents aged 11–15 years at doses of 2.5–10 mg/day under close specialist supervision; safety and efficacy in children younger than 11 years have not been established.

For Parkinson's disease and acromegaly, safety and efficacy of Bromolac in pediatric patients have not been established, as these conditions are uncommon in children; use in this population should only occur under specialist guidance.