Cycloset (bromocriptine mesylate)

Dosage of bromocriptine mesylate is expressed in terms of bromocriptine. Dosage of bromocriptine should be individualized and carefully adjusted, using frequent evaluation during dosage adjustment and employing the lowest possible effective dosage. A temporary reduction in dosage or discontinuance of the drug may occasionally be necessary in patients who develop intolerable adverse effects.

When bromocriptine therapy is discontinued (e.g., during pregnancy) in patients receiving the drug for hyperprolactinemic disorders, the patient should be carefully monitored for signs and symptoms of tumor development or progression. (See Cautions: Carcinogenicity.) Patients receiving bromocriptine for the treatment of macroadenomas should be warned to not discontinue the drug unless otherwise directed by their physician, since such discontinuance could result in rapid regrowth of the tumor and recurrence of symptoms.

Bromocriptine is administered orally with food.

No dosing information is available for this tab.

No dosing information is available for this tab.

Bromocriptine is metabolized by cytochrome P-450 (CYP) 3A4; concomitant use of drugs that inhibit or induce CYP3A4 may increase or decrease plasma bromocriptine concentrations, respectively.

Concomitant use of a known moderate CYP3A4 inhibitor (erythromycin) and bromocriptine increased peak plasma concentrations and systemic exposure of bromocriptine by 4.6- and 3.7-fold, respectively. The manufacturer of the rapid-release formulation of bromocriptine (Cycloset(R)) states that dosage should not exceed 1.6 mg once daily during concomitant use of a moderate CYP3A4 inhibitor (e.g., erythromycin). Some manufacturers state that concomitant use of bromocriptine and potent CYP3A4 inhibitors (e.g., azole antifungals, HIV protease inhibitors) should be avoided.

Concomitant use of bromocriptine and octreotide in patients with acromegaly increased systemic exposure to bromocriptine by about 38%.

Effectiveness of bromocriptine may be reduced by dopamine receptor antagonists such as butyrophenones, haloperidol, metoclopramide, pimozide, and phenothiazines; some manufacturers state that concomitant use of these drugs is not recommended.

Administration of bromocriptine, especially in high dosages, may result in decreased alcohol tolerance and patients should be cautioned to limit alcohol intake while receiving bromocriptine.

Because bromocriptine is extensively bound to plasma proteins, the drug may increase the unbound fraction of other highly protein-bound drugs (e.g., salicylates, sulfonamides, chloramphenicol, probenecid), which can result in altered efficacy or safety of the concomitantly administered drug.

Additive hypotensive effects may occur in patients receiving bromocriptine and antihypertensive agents. Careful adjustment of the antihypertensive dosage may be necessary when these drugs are used concomitantly.

Although there currently is no conclusive evidence of an interaction between bromocriptine and other ergot alkaloids, concomitant use of the drugs is not recommended since potentially severe adverse effects (e.g., hypertension, myocardial infarction) have occurred when the drugs were used together. (See Cautions: Cardiovascular Effects.)

Hypertension and tachycardia have been reported in postpartum women receiving bromocriptine and sympathomimetic drugs (e.g., phenylpropanolamine) concomitantly. The safety of concomitant use of these drugs for more than 10 days is not known; therefore, such concomitant use for more than a 10-day period is not recommended.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

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There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

There is no enhanced messaging for this drug.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

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No enhanced messaging available.

Cumulative data in women who have taken bromocriptine during pregnancy indicate that the incidence of spontaneous abortions and congenital malformations appears to be similar to that reported in the general population. Most of these women received the drug during the first 2-3 weeks of pregnancy, although some received the drug throughout pregnancy. Use of bromocriptine to reduce serum prolactin concentrations and prevent possible pituitary tumor expansion has been reported in some women during the last week of pregnancy. However, dopamine agonists generally should not be used during pregnancy and should be discontinued immediately if pregnancy occurs. In pregnant women with underlying prolactin-secreting pituitary tumors, sudden enlargement of the tumors as a result of an increase in pituitary size which normally occurs during pregnancy may cause optic nerve compression, visual impairment, and even blindness, which usually disappear after delivery.

In pregnant women receiving bromocriptine, fetal prolactin (but not growth hormone) concentrations are suppressed; concentrations of prolactin in amniotic fluid are not affected. Prolactin concentrations return to normal in these infants after birth.

Since bromocriptine interferes with lactation, the drug should not be used in nursing women (some manufacturers state that the drug is contraindicated in this population).

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