Bromocriptine

Bromocriptine is a dopamine receptor agonist used to treat certain conditions caused by a hormone imbalance in which there is too much prolactin in the blood (hyperprolactinemia), and to treat these disorders when they are caused by brain tumors that can produce prolactin. Bromocriptine is sometimes used with surgery or radiation to treat acromegaly, and it is also used to treat symptoms of Parkinson's disease, such as stiffness, tremors, muscle spasms, and poor muscle control.

Bromocriptine is available under the following different brand names: Cycloset, and Parlodel.

Capsule

• 5mg

Tablet

• 0.8mg
• 2.5mg

Dosage Considerations – Should be Given as Follows:

Hyperprolactinemia (Parlodel)

• Adult and geriatric: Initial: 1.25-2.5 mg orally once/day
• May increase by 2.5 mg/day once every 2-7 days
• Usual therapeutic dosage 5-7.5 mg/day, ranges from 2.5-15 mg/day
• Up to 30 mg/day has been used in some patients with amenorrhea and/or galactorrhea
• Pediatric, Children 11-15 years: 1.25-2.5 mg orally once/day (initially)
• Maintenance: 2.5-10 mg/day
• Take with food

Parkinson Disease (Parlodel)

• Adult and geriatric: 1.25 mg orally every 12 hours
• May increase dose by 2.5 mg/day every 2-4 weeks
• Safety greater than 100 mg/day not established

Acromegaly (Parlodel)

• Adult and geriatric: 1.25-2.5 mg orally at bedtime for 3 days
• May increase by 1.25-2.5 mg/day at once every 3-7 days
• Not to exceed 100 mg/day

Diabetes (Cycloset)

• Quick release formulation (Cycloset) is the only bromocriptine product indicated for diabetes mellitus type 2 as adjunct to diet and exercise to improve glycemic control
• Adult and geriatric, initial dose: 1 tablet (0.8 mg) orally once/day increased weekly by 1 tablet until maximal tolerated daily dose of 1.6-4.8 mg is achieved
• Concomitant use of a moderate CYP3A4 inhibitor (e.g., erythromycin): Dose should not exceed 1.6 mg orally once/day
• Concomitant use of a strong CYP3A4 inhibitor (e.g., azole antimycotics, HIV protease inhibitors): Avoid use; ensure adequate washout of the strong CYP3A4 inhibitor drug before initiating CYCLOSET treatment
• Take within 2 hours after waking in the morning with food
• Note: Cycloset is not indicated for hyperprolactinemia, Parkinson’s disease, or acromegaly
• Limitations of use
  • Not for treatment of type 1 diabetes or diabetic ketoacidosis
  • Limited efficacy data in combination with thiazolidinediones
  • Efficacy not confirmed in combination with insulin
  • Neuroleptic Malignant Syndrome (Off-label)
  • Adult and geriatric: 2.5-5 mg orally 2-3 times/day; not to exceed 45 mg/day
  • Administration: take with food

Hepatic Impairment

• Dose adjustment may be necessary; there are no guidelines

Dosing Considerations

• Not for treatment of type 1 diabetes or diabetic ketoacidosis
• Limited efficacy data in combination with thiazolidinediones
• Efficacy has not been confirmed in combination with insulin

Common side effects of bromocriptine include:

• Nausea
• Low blood pressure (hypotension)
• Headache
• Dizziness
• Abdominal cramps
• Loss of appetite
• Constipation
• Indigestion
• Trouble swallowing
• Stomach/abdominal pain or discomfort
• Gastrointestinal bleeding
• Vomiting
• Drowsiness
• Fatigue
• Faintness
• Visual hallucinations
• Sleep problems (insomnia)
• Lightheadedness
• Nightmares
• Paranoia
• Psychosis
• Seizures
• Spinning sensation (vertigo)
• Irregular heartbeats (arrhythmias)
• Slow heart rate
• High blood pressure (hypertension)
• Heart attach (myocardial infarction)
• Mottled skin
• Dizziness on standing
• Vasospasm
• Palpitations
• Pericardial effusions
• Raynaud's syndrome exacerbation
• Fainting
• Eyelid twitching or closing
• BUN increased
• Burning discomfort of the eye
• Double vision
• Facial pallor
• Leg cramps
• Nasal congestion
• Rash
• Hives
• Depression
• Tired feeling
• Diarrhea
• Cold feeling or numbness in your fingers
• Dry mouth
• Stuffy nose

Serious side effects of bromocriptine include:

• Vision problems
• Constant runny nose
• Chest pain
• Pain when you breathe
• Fast heart rate
• Rapid breathing
• Shortness of breath
• Back pain
• Swelling in your ankles or feet
• Urinating less than usual or not at a
ll
• Confusion
• Hallucinations
• Feeling like you might pass out
• Low blood sugar (headache, hunger, weakness, sweating, tremors, irritability, trouble concentrating)
• Muscle movements you cannot control
• Loss of balance or coordination
• Bloody or tarry stools
• Coughing up blood or vomit that looks like coffee grounds
• Dangerously high blood pressure (severe headache, blurred vision, buzzing in your ears, anxiety, confusion, chest pain, shortness of breath, uneven heartbeats, seizures)

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe interactions of bromocriptine include:

• almotriptan
• eletriptan
• frovatriptan
• glyceryl trinitrate PR
• naratriptan
• nitroglycerin IV
• nitroglycerin sublingual
• nitroglycerin topical
• nitroglycerin transdermal
• nitroglycerin translingual
• nitroglycerin transmucosal
• sumatriptan
• sumatriptan intranasal
• sumatriptan transdermal
• zolmitriptan

Bromocriptine has serious interactions with at least 33 different drugs.

Bromocriptine has moderate interactions with at least 52 different drugs.

Mild interactions of bromocriptine include:

• ruxolitinib

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

Warnings

This medication contains bromocriptine. Do not take Cycloset or Parlodel if you are allergic to bromocriptine or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Sensitivity to ergot alkaloids
• Uncontrolled hypertension
• Nursing
• Cycloset: Diabetes mellitus type I, syncopal migraine, diabetes ketoacidosis

Effects of Drug Abuse

• No information available

Short-Term Effects

• May impair ability to drive/operate heavy machinery.
• Postmarketing reports suggest that patients treated with anti-Parkinson medications can experience intense urges to gamble, increased sexual urges, intense urges to spend money uncontrollably, and other intense urges.
• See "What Are Side Effects Associated with Using Bromocriptine?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Bromocriptine?"

Cautions

• Monitor blood pressure: risk of low blood pressure and dizziness upon standing (orthostatic hypotension).
• Concurrency with other hypotensive drugs concomitantly.
• Hepatic/renal impairment.
• In patients undergoing treatment for macroadenoma-related hyperprolactinemia or who have undergone trans-sphenoidal surgery, a persistent watery nasal discharge may be sign of cerebrospinal fluid runny nose (CSF rhinorrhea).
• Discontinuation of treatment in patients with macroadenomas associated with rapid regrowth of tumor and increased prolactin serum levels.
• May impair ability to drive/operate heavy machinery.
• History of heart attack (myocardial infarction [MI]) and a residual atrial, nodal or ventricular arrhythmia, especially with Parkinson's disease.
• Use for prevention of postpartum lactation no longer recommended.
• Postmarketing reports suggest that patients treated with anti-Parkinson medications can experience intense urges to gamble, increased sexual urges, intense urges to spend money uncontrollably, and other intense urges.
• Epidemiological studies have shown that patients with Parkinson's disease have a higher risk (2 to 6-fold higher) of developing melanoma than the general population (unsure if related to the disease or drug therapy).
• Avoid abrupt withdrawal (associated with neuroleptic malignant syndrome-like symptoms); discontinue gradually.
• Conclusive evidence of macrovascular risk reduction with bromocriptine or other antidiabetic agents not demonstrated.
• Fibrotic valve thickening (e.g., aortic, mitral, tricuspid), possibly due to excess serotonin activity, usually associated with long-term, chronic use of ergot alkaloids and derivatives reported.
• Visual or auditory hallucinations reported with administered alone or concomitantly.
• Cases of pleural and pericardial effusions, as well as pleural, pulmonary, and/or retroperitoneal fibrosis and constrictive pericarditis reported with prolonged high-dose daily use; discontinue therapy if fibrotic changes suspected.
• In the treatment of acromegaly, discontinuation recommended if tumor expansion occurs during therapy.
• Use with caution in patients with cardiovascular disease, dementia, hepatic impairment, and peptic ulcer disease.
• Parlodel: Avoid use in patients with galactose intolerance/malabsorption, severe lactase deficiency, or glucose/galactose malabsorption.
• In patients with severe psychotic disorders, treatment with a dopamine receptor agonist such as bromocriptine may exacerbate the disorder or may diminish the effectiveness of drugs used to treat the disorder; use in patients with severe psychotic disorders not recommended.
• Dopamine receptor antagonists, including neuroleptic agents that have dopamine D2 receptor antagonist properties (e.g., clozapine, olanzapine, ziprasidone), may reduce effectiveness of bromocriptine and bromocriptine may reduce effectiveness of these agents; bromocriptine has not been studied in patients taking neuroleptic drugs; concomitant use with dopamine receptor antagonists, including neuroleptic drugs, is not recommended.
• Effectiveness and safety are unknown in patients already taking dopamine receptor agonists for other indications; concomitant use not recommended.

Pregnancy and Lactation

• Bromocriptine may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• Bromocriptine should not be used during lactation.