Usual Adult Dose for Hyperprolactinemia

Initial dose: 1.25 to 2.5 mg orally once a day

• Increase in increments of 2.5 mg every 2 to 7 days as tolerated until optimal response is achieved

Maintenance dose: 2.5 to 15 mg orally once a day

Comments:

• Prior to restoring normal ovulatory menstrual cycles, unexpected pregnancy may occur; to avoid excess exposure to this drug during pregnancy, mechanical methods of contraception are recommended until normal ovulatory menstrual cycles have been restored. Once restored, contraception may be discontinued in patients wanting to get pregnant.
• If menstruation does not occur within 3 days of expected date, this drug should be held and a pregnancy test performed.
• For patients electing adenectomy, this drug may be used to reduce the tumor mass prior to surgery.

Uses:

• For the treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism.
• For patients with prolactin-secreting adenomas.
• For reduction in tumor size in both male and female patients with macroadenomas.

Usual Adult Dose for Acromegaly

Initial dose: 1.25 to 2.5 mg orally once a day at bedtime for 3 days

• Increase in increments of 1.25 to 2.5 mg as tolerated every 3 to 7 days until optimal response is achieved

Maintenance dose: 20 to 30 mg/day
Maximum dose: 100 mg/day

Comments:

• Since patients who have beneficial results generally show reductions in circulating levels of growth hormone, periodic assessment of growth hormone levels will serve as a guide in assessing efficacy.
• Patients who have undergone pituitary irradiation should stop this drug for 4 to 8 weeks once a year to assess the clinical effects of radiation and effects of the drug; recurrence of the signs and symptoms or increases in growth hormone suggest drug therapy should continue.

Use: For the treatment of acromegaly.

Usual Adult Dose for Parkinson's Disease

Initial dose: 1.25 mg orally twice a day

• Increase in increments of 2.5 mg/day every 14 to 28 days to the lowest dose producing optimal response

Maximum dosage: 100 mg/day

Comments:

• The dose of levodopa should be maintained during therapy initiation; then, if needed, it can be reduced because of adverse reactions.
• This drug may provide additional therapeutic benefits to patients maintained on optimal doses of levodopa, those beginning to develop tolerance to levodopa, and those who are experience end of dose failure with levodopa.
• Continued efficacy beyond 2 years has not been established.

Use: As adjunctive treatment to levodopa (alone or with a peripheral decarboxylase inhibitor).

Usual Adult Dose for Diabetes Type 2

Cycloset(R) only:

Initial: 0.8 mg orally once a day

• Increase in increments of 0.8 mg weekly as tolerated

Maintenance: 1.6 to 4.8 mg orally once a day
Maximum Dose: 4.8 mg/day

Dose should be taken within 2 hours of waking in the morning with food

Concomitant Administration with CYP450 3A4 inhibitors:

• Moderate CYP450 3A4 inhibitors (e.g., erythromycin): Do not exceed 1.6 mg/day
• Strong CYP450 3A4 inhibitors (e,g., azole antimycotics, HIV protease inhibitors): Avoid concomitant use and ensure adequate washout of strong CYP450 3A4 inhibitors before initiating therapy

Comments:

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

Use: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Usual Pediatric Dose for Hyperprolactinemia

Prolactin-secreting Pituitary Adenomas:

11 to less than 16 years:
Initial: 1.25 to 2.5 mg orally once a day

• Increase dose as tolerated until an optimal response is achieved

Maintenance: 2.5 to 10 mg orally once a day

16 years or older:
Initial dose: 1.25 to 2.5 mg orally once a day

• Increase in increments of 2.5 mg every 2 to 7 days as tolerated until optimal response is achieved

Maintenance dose: 2.5 to 15 mg orally once a day

Renal Dose Adjustments

No dose adjustment recommended

Liver Dose Adjustments

Use with caution as bromocriptine levels may increase

Dose Adjustments

Elderly: Dose selection should be cautious, starting at the lower end of the dose range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy in this population

Concomitant Administration of Cycloset(R) and CYP450 3A4 inhibitors:

• Moderate CYP450 3A4 inhibitors (e.g., erythromycin): Do not exceed 1.6 mg/day
• Strong CYP450 3A4 inhibitors (e,g., azole antimycotics, HIV protease inhibitors): Avoid concomitant use and ensure adequate washout of strong CYP450 3A4 inhibitors before initiating therapy

Precautions

CONTRAINDICATIONS:

• Hypersensitivity to this drug or any of the product excipients
• Uncontrolled hypertension or sensitivity to any ergot alkaloid
• Syncopal migraines
• Breastfeeding
• Postpartum use in women with a history of coronary artery disease or other severe cardiovascular conditions unless withdrawal is medically contraindicated

Safety and efficacy have not been established in patients younger than 11 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:

• Take orally with food to reduce gastrointestinal upset

For treatment of Type 2 diabetes mellitus: Take within 2 hours after waking in the morning with food

Storage requirements:

• Protect from light and moisture

General:

• Patients should be evaluated frequently during dose escalation to determine the lowest dose that produces a therapeutic response.
• Since hyperprolactinemia with amenorrhea/galactorrhea and infertility has been found in patients with pituitary tumors, a complete evaluation of the pituitary is indicated before treatment begins.

Monitoring:

• Monitor blood pressure
• Monitor for melanomas
• Hyperprolactinemic states: Monitor visual fields in patients with macroprolactinomas
• Parkinson's disease: Periodic evaluation of hepatic, hematopoietic, cardiovascular, and renal function
• Type 2 diabetes mellitus: Periodic blood glucose monitoring
• Type 2 diabetes mellitus: Assess orthostatic vital signs prior to initiation and periodically during therapy

Patient advice:

• For patients treating type 2 diabetes mellitus, information should be provided about the importance of diet, regular exercise, blood glucose monitoring, and recognition and treatment of hypoglycemia and hyperglycemia; patients should be instructed on diabetes management during periods of stress such as fever, trauma, infection, or surgery.
• Patients should be advised that orthostatic hypotension, drowsiness, faintness, fainting, and syncope may occur especially early in treatment and with dose increases; patients should be instructed to make slow postural changes and advised to avoid situations that could predispose them to serious injury if syncope occurs.
• Patients should be advised that this drug may cause somnolence and episodes of sudden onset of sleep; patients should not drive or operate hazardous machinery if they experience somnolence and/or an episode of sudden onset of sleep.
• Women should not breastfeed while taking this drug; women should talk with their healthcare provider if they are pregnant or planning to become pregnant.
• Patients and caregivers should be alerted to the possibility that this drug may cause intense urges to spend money, gamble, and other intense urges and the inability to control these urges; these urges should be reported to their health care provider.
• Patients should be instructed to report changes in the size, shape, or color of moles on their skin and should have their skin checked on a regular basis for melanomas.