Bromotine

• Parkinson’s Disease:
• Treatment of idiopathic Parkinson’s disease, either as monotherapy in early stages or adjunct to levodopa in advanced stages.
• Hyperprolactinemia:
• Management of elevated prolactin levels due to pituitary adenomas (prolactinomas), amenorrhea, galactorrhea, infertility, and hypogonadism.
• Acromegaly:
• Adjunct treatment to reduce growth hormone levels in acromegaly patients.
• Type 2 Diabetes Mellitus:
• Adjunctive treatment to improve glycemic control in adult patients with type 2 diabetes mellitus, especially those with obesity.
• Other Uses:
• Prevention and treatment of postpartum lactation suppression (off-label).

• Parkinson’s Disease:
• Initial dose: 1.25 mg once daily, increased gradually every 3-7 days by 1.25 mg to 2.5 mg increments.
• Usual maintenance: 15 to 30 mg daily divided into 2-3 doses.
• Hyperprolactinemia:
• Initial dose: 1.25 mg once daily or every other day.
• Maintenance dose: 2.5 to 15 mg daily in divided doses; dose adjusted based on serum prolactin levels.
• Acromegaly:
• Typically 1.25 mg daily, titrated up to 7.5 mg or more as tolerated.
• Type 2 Diabetes Mellitus:
• Starting dose: 0.8 mg once daily in the morning with food.
• Titrate weekly in 0.8 mg increments up to 4.8 mg daily.
• Pediatrics:
• Safety and efficacy not established.
• Elderly:
• Start with lower doses and titrate cautiously due to increased sensitivity.
• Renal or Hepatic Impairment:
• Use with caution; no formal dose adjustment guidelines but monitor for toxicity.
• Administration:
• Oral tablets taken with water, preferably with food to reduce gastrointestinal side effects.

Bromocriptine is a dopamine D2 receptor agonist that acts primarily by stimulating dopamine receptors in the central nervous system, notably in the hypothalamus and pituitary gland. In Parkinson’s disease, it compensates for diminished dopaminergic activity by activating dopamine receptors, improving motor control. In hyperprolactinemia, bromocriptine inhibits prolactin secretion from pituitary lactotroph cells via dopaminergic inhibition. Additionally, bromocriptine modulates metabolic pathways in the hypothalamus to improve insulin sensitivity, which underlies its glucose-lowering effects in type 2 diabetes.

• Absorption:
• Rapid and extensive absorption after oral administration; bioavailability ~28% due to significant first-pass metabolism.
• Distribution:
• Widely distributed; crosses blood-brain barrier; highly protein bound (~90%).
• Metabolism:
• Metabolized extensively in the liver by CYP3A4 enzyme and other pathways.
• Elimination:
• Primarily excreted in feces as metabolites; less than 2% excreted unchanged in urine.
• Half-life:
• Plasma half-life approximately 12–14 hours.

• Pregnancy:
• FDA Category B: Animal studies show no risk but adequate human studies are lacking. Bromocriptine is used to suppress lactation and thus generally avoided in pregnancy unless necessary.
• Lactation:
• Inhibits lactation; not recommended during breastfeeding as it suppresses milk production and can affect the infant.

• Primary Class: Dopamine Agonist
• Subclass: Ergot Derivative

• Known hypersensitivity to bromocriptine or ergot derivatives
• Uncontrolled hypertension, especially with pregnancy-induced hypertension or preeclampsia
• History of myocardial infarction or ischemic heart disease (relative contraindication)
• Use with potent CYP3A4 inhibitors may increase bromocriptine toxicity

• Risk of orthostatic hypotension and syncope; advise patients to rise slowly from sitting or lying positions.
• Potential for psychiatric effects: hallucinations, psychosis, confusion.
• Monitor for pulmonary fibrosis or pleural effusion with long-term use (rare).
• Caution in patients with cardiovascular disease due to possible vasospastic events.
• Use caution in patients with renal or hepatic impairment.
• Sudden discontinuation may cause symptom exacerbation; taper dose gradually.
• Monitor blood glucose closely when used in diabetes patients.

• Common:
• Nausea, vomiting
• Headache, dizziness
• Fatigue, nasal congestion
• Orthostatic hypotension, syncope
• Less Common:
• Abdominal cramps, constipation
• Psychosis, hallucinations
• Raynaud’s phenomenon
• Pulmonary infiltrates or fibrosis (rare)
• Rare:
• Cardiac valve fibrosis (very rare)
• Cerebral ischemia

• CYP3A4 Inhibitors (e.g., ketoconazole, erythromycin): Increase bromocriptine plasma levels and toxicity risk.
• Dopamine antagonists (e.g., antipsychotics): May reduce efficacy of bromocriptine.
• Antihypertensives: Additive hypotensive effects; monitor blood pressure.
• Ergot alkaloids: Avoid concomitant use due to risk of additive vasospasm.
• Alcohol and CNS depressants: Increased risk of sedation and hypotension.

• Bromocriptine remains a recommended dopamine agonist in Parkinson’s treatment, with updated caution on cardiovascular risks.
• FDA-approved for adjunctive treatment of type 2 diabetes mellitus emphasizing morning dosing with meals for optimal efficacy.
• Increased monitoring advised for psychiatric side effects and rare fibrotic complications.
• No major changes to dosing regimens recently.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep container tightly closed and out of reach of children.
• Do not freeze.