Bromocriptine

Bromocriptine mesylate is an ergot derivative indicated for the treatment of: Hyperprolactinemia-associated dysfunction including amenorrhea with or without galactorrhea, infertility, or hypogonadism in adults. Prolactin-secreting adenomas in adults and pediatric patients 11 years of age and older. Acromegaly in adults. Signs and symptoms of idiopathic Parkinson’s disease or postencephalitic parkinsonism in adults. Limitations of Use Avoid use of bromocriptine mesylate for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions

Bromocriptine mesylate contains bromocriptine, an ergot derivative and dopamine receptor agonist, which activates post-synaptic dopamine receptors. Dopaminergic neurons in the tuberoinfundibular process release dopamine that modulates the secretion of prolactin from the anterior pituitary, in the corpus striatum the dopaminergic neurons are involved in the control of motor function. Bromocriptine induces stereotyped behavior in rodents and turning behavior in rats (e.g., rats move in circles) that have unilateral lesions in the substantia nigra. These actions, characteristic of those produced by dopamine, are inhibited by dopamine antagonists and suggest a direct action of bromocriptine on striatal dopamine receptors.

Before initiating bromocriptine mesylate, evaluate for valvular heart disease, including with an echocardiogram. If valvular disease is detected, do not administer bromocriptine mesylate. Take bromocriptine mesylate orally with food. Recommended dosage for hyperprolactinemia-associated dysfunction is 1.25 mg (one-half of a tablet) to 2.5 mg once daily. Increase the dosage up to 2.5 mg once daily every two to seven days within a recommended dosage of 2.5 mg to 15 mg once daily. Recommended dosage for prolactin-secreting adenomas is 1.25 mg to 2.5 mg once daily. Increase the dosage within a recommended dosage of 2.5 mg to 10 mg once daily. Recommended dosage for acromegaly is 1.25 to 2.5 mg once at bedtime for 3 days. Increase the dosage 1.25 mg to 2.5 mg once daily every 3 to 7 days up to the maximum recommended dosage is 100 mg/daily.

Bromocriptine mesylate is contraindicated in patients with: History of cardiac valvular disorders or a history of pericardial fibrosis. History of pleural, pulmonary, or retroperitoneal fibrotic disorders. Uncontrolled hypertension. Hypersensitivity to bromocriptine or to any of the excipients of bromocriptine mesylate tablets or capsules or sensitivity to other ergot alkaloids.

Cardiac Valvulopathy and Pericardial Fibrosis: During bromocriptine mesylate treatment, monitor for the development of valvulopathy with a cardiac echocardiogram at intervals of 6 to 12 months or as clinically indicated and monitor for chest pain and signs and symptoms of heart failure (if heart failure occurs, exclude valvular fibrosis and pericarditis). Consider additional clinical and diagnostic monitoring at baseline and as necessary during bromocriptine mesylate treatment. Use bromocriptine mesylate in patients treated with other drugs associated with valvulopathy is not recommended. Discontinue bromocriptine mesylate if the patient has a new diagnosis of valvular regurgitation, valvular restriction, valve leaflet thickening, or pericarditis.

The following clinically significant adverse reactions are described elsewhere in the labeling: Cardiac Valvulopathy and Pericardial Fibrosis Pleural, Pulmonary, and Retroperitoneal Fibrosis Hypotension/Orthostatic Hypotension Risks with Use of Bromocriptine Mesylate for Postpartum Lactation Inhibition or Suppression Impulse Control Disorders and Compulsive Behaviors Falling Asleep During Activities of Daily Living Visual Impairment in Patients with Prolactin-secreting Adenomas Exacerbation of Psychosis in Patients with Severe Psychotic Disorders Risks in Patients with Hereditary Problems of Galactose Intolerance, Severe Lactase Deficiency, or Glucose-Galactose Malabsorption Additional Clinically Significant Adverse Reactions and Risks in Patients with Acromegaly Additional Clinically Significant Adverse Reactions and Risks in Patients with Idiopathic Parkinson’s Disease or Postencephalitic Parkinsonism Most common adverse reactions: Hyperprolactinemia-Associated Dysfunctions and Prolactin-secreting Adenomas: (incidence >5%) are nausea, headache, dizziness, fatigue, lightheadedness, and vomiting.

Alcohol Alcohol may potentiate bromocriptine mesylate-associated adverse reactions. Dopamine Antagonists The concomitant use of bromocriptine mesylate with dopamine antagonists resulted in a decreased efficacy of bromocriptine mesylate. Strong and Moderate CYP3A4 Inhibitors Avoid concomitant use of bromocriptine mesylate with strong CYP3A4 inhibitors. Follow the recommended bromocriptine mesylate dosage modifications during concomitant use with moderate CYP3A4 inhibitors. Bromocriptine is a substrate of CYP3A4. Concomitant use with strong and moderate CYP3A4 inhibitors increases bromocriptine exposure, which may increase the risk of bromocriptine mesylate-associated adverse reactions. Ergot Alkaloids Concomitant use of bromocriptine mesylate with other ergot alkaloids is not recommended.

Store and Dispense Store at 68°F to 77°F (20°C to 25°C), excursions permitted to 59°F to 86°F (15°C to 30°C). Protect from light.