Brand Name
Cycloset
Generic Name
Bromocriptine
View Brand Information FDA approval date: January 13, 1998
Classification: Ergot Derivative
Form: Tablet, Capsule
What is Cycloset (Bromocriptine)?
Hyperprolactinemia-Associated Dysfunctions Bromocriptine mesylate tablets and capsules are indicated for the treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism. Bromocriptine treatment is indicated in patients with prolactin-secreting adenomas, which may be the basic underlying endocrinopathy contributing to the above clinical presentations. Reduction in tumor size has been demonstrated in both male and female patients with macroadenomas. In cases where adenectomy is elected, a course of bromocriptine therapy may be used to reduce the tumor mass prior to surgery. Acromegaly Bromocriptine mesylate tablet and capsule therapy is indicated in the treatment of acromegaly. Bromocriptine therapy, alone or as adjunctive therapy with pituitary irradiation or surgery, reduces serum growth hormone by 50% or more in approximately ½ of patients treated, although not usually to normal levels. Since the effects of external pituitary radiation may not become maximal for several years, adjunctive therapy with bromocriptine offers potential benefit before the effects of irradiation are manifested. Parkinson’s Disease Bromocriptine mesylate tablets or capsules are indicated in the treatment of the signs and symptoms of idiopathic or postencephalitic Parkinson’s disease. As adjunctive treatment to levodopa , bromocriptine therapy may provide additional therapeutic benefits in those patients who are currently maintained on optimal dosages of levodopa, those who are beginning to deteriorate to levodopa therapy, and those who are experiencing “end of dose failure” on levodopa therapy. Bromocriptine therapy may permit a reduction of the maintenance dose of levodopa and, thus may ameliorate the occurrence and/or severity of adverse reactions associated with long-term levodopa therapy such as abnormal involuntary movements and the marked swings in motor function . Continued efficacy of bromocriptine therapy during treatment of more than 2 years has not been established. Data are insufficient to evaluate potential benefit from treating newly diagnosed Parkinson’s disease with bromocriptine. Studies have shown, however, significantly more adverse reactions in bromocriptine-treated patients than in levodopa/carbidopa-treated patients. Patients unresponsive to levodopa are poor candidates for bromocriptine therapy.
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Brand Information
CYCLOSET (bromocriptine mesylate)
1INDICATIONS AND USAGE
CYCLOSET is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
2DOSAGE FORMS AND STRENGTHS
0.8 mg tablets are white and round, imprinted with "C" on one side and "9" on the other.
3CONTRAINDICATIONS
CYCLOSET is contraindicated in:
- Patients with known hypersensitivity to bromocriptine, ergot-related drugs, or any of the excipients in CYCLOSET.
- Patients with syncopal migraine. Bromocriptine increases the likelihood of a hypotensive episode among patients with syncopal migraine. Loss of consciousness during a migraine may reflect dopamine receptor hypersensitivity. CYCLOSET is a dopamine receptor agonist and may, therefore, potentiate the risk for syncope in these patients.
- Postpartum patients. Serious and life-threatening adverse reactions have been reported with bromocriptine use in this population
- Lactating patients. CYCLOSET contains bromocriptine which inhibits lactation
4ADVERSE REACTIONS
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Hypotension
- Psychotic Disorders
- Somnolence
- Risks in Postpartum Women
4.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, the adverse reaction rates reported in one clinical trial may not be easily compared to those rates reported in another clinical trial and may not reflect the rates actually observed in clinical practice.
The CYCLOSET safety trial was a 52-week, placebo-controlled study. A total of 3,070 patients were randomized to CYCLOSET (titrated to 1.6 to 4.8 mg daily, as tolerated) or placebo. The study population had a mean baseline age of 60 years (range 27-80) and 33% were 65 years of age or older. Approximately 43% of the patients were female, 68% were Caucasian, 17% were Black, 13% were Hispanic, and 1% were Asian. The mean baseline body mass index was 32 kg/m
Table 1 summarizes the adverse reactions reported in ≥5% of patients treated with CYCLOSET in clinical trials regardless of investigator assessment of causality. The most commonly reported adverse reactions (nausea, fatigue, vomiting, headache, dizziness) lasted a median of 14 days and were more likely to occur during the initial titration of CYCLOSET. There were no differences in the pattern of common adverse reactions across race groups or age groups (<65 years old vs. >65 years old). In the 52-week CYCLOSET safety trial, 11.5% of CYCLOSET-treated women compared to 3.6% of placebo-treated women reported vomiting. In this same trial, 5.4% of CYCLOSET-treated men compared to 2.8% of placebo-treated men reported vomiting.
4.2Postmarketing Experience
The following adverse reactions have been identified during post approval use of other formulations of bromocriptine mesylate for indications for which CYCLOSET is not approved (e.g., hyperprolactinemia, acromegaly, and Parkinson's disease), generally at doses higher than those approved for the treatment of type 2 diabetes. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
5DRUG INTERACTIONS
- The active ingredient in CYCLOSET (bromocriptine mesylate) is highly bound to serum proteins. Therefore, CYCLOSET may increase the unbound fraction of other concomitantly used highly protein-bound therapies (e.g., salicylates, sulfonamides, chloramphenicol and probenecid), which may alter their effectiveness and risk for side effects.
- CYCLOSET is a dopamine receptor agonist. Concomitant use of dopamine receptor antagonists, such as neuroleptics (e.g., phenothiazines, butyrophenones, thioxanthenes), or metoclopramide may diminish the effectiveness of CYCLOSET, and CYCLOSET may diminish the effectiveness of these other therapies. The concurrent use of CYCLOSET with these agents has not been studied in clinical trials and is not recommended
- CYCLOSET in combination with ergot-related drugs may cause an increase in the occurrence of ergot-related side effects, such as nausea, vomiting, and fatigue, and may also reduce the effectiveness of these ergot therapies when used to treat migraine. The concurrent use of these ergot agents within 6 hours of CYCLOSET dosing is not recommended.
- CYCLOSET is extensively metabolized by the liver via CYP3A4. Therefore, potent inhibitors or inducers of CYP3A4 may increase or reduce the circulating levels of CYCLOSET, respectively. Use caution when co-administering drugs that are inhibitors or inducers of CYP3A4. CYCLOSET dose should not exceed 1.6 mg once daily during concomitant use of a moderate CYP3A4 inhibitor (e.g., erythromycin). Concomitant use of strong CYP3A4 inhibitors (e.g., azole antimycotics, HIV protease inhibitors) with CYCLOSET should be avoided. Ensure adequate washout of the strong CYP3A4 inhibitor drug before initiating CYCLOSET treatment
- There are postmarketing reports of hypertension and tachycardia when bromocriptine was co-administered with sympathomimetic drugs (e.g., phenylpropanolamine and isometheptene) in postpartum women. There are limited clinical trial data supporting the safety of co-administering sympathomimetic drugs and CYCLOSET for more than 10 days. Therefore, concomitant use of these agents with CYCLOSET for more than 10 days duration is not recommended. Also, there are limited clinical trial data supporting the safety of selective 5-hydroxytryptamine
6OVERDOSAGE
With another formulation of bromocriptine mesylate, the most commonly reported signs and symptoms associated with acute overdose were nausea, vomiting, constipation, diaphoresis, dizziness, pallor, severe hypotension, malaise, confusion, lethargy, drowsiness, delusions, hallucinations, and repetitive yawning. The lethal dose has not been established.
Treatment of overdose consists of removal of the drug by emesis (if conscious), gastric lavage, activated charcoal, or saline catharsis. Careful supervision and recording of fluid intake and output is essential. Hypotension should be treated by placing the patient in the Trendelenburg position and administering intravenous fluids. If satisfactory relief of hypotension cannot be achieved by using the above measures to their fullest extent, vasopressors should be considered.
7DESCRIPTION
CYCLOSET Tablets contain micronized bromocriptine mesylate, an ergot derivative. Bromocriptine mesylate is chemically designated [Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-, monomethanesulfonate (salt), (5'α)-]. CYCLOSET is a single enantiomer with absolute configuration 5
The structural formula of bromocriptine is shown below:
Bromocriptine mesylate in CYCLOSET is a white or slightly colored micronized crystalline powder with a molecular formula of C
8CLINICAL STUDIES
A total of 3,723 patients with type 2 diabetes were randomized across 4 double-blind, placebo-controlled clinical trials conducted to evaluate the safety and glycemic efficacy of CYCLOSET. In the pooled 24-week monotherapy trial and the two 24-week add-on to sulfonylurea trials (N = 653), the mean age of the CYCLOSET-treated patients (N = 324) was 55 years, 71% were male and 73% Caucasian. In the 52-week safety trial (N = 3,070), the mean age for the entire study population was 60 years and 43% of patients were female, 68% were Caucasian, 17% were Black, 13% were Hispanic, and 1% were Asian.
In all 4 clinical trials, patients assigned to treatment with CYCLOSET received an initial dose of 0.8 mg, which was increased by 0.8 mg each week for 6 weeks (4.8 mg/day final dose) if no intolerance occurred or until the maximum tolerated dose ≥1.6 mg/day was reached. In patients with type 2 diabetes, treatment with CYCLOSET produced clinically significant improvements in HbA1c and postprandial glucose (PPG).
8.1Monotherapy
A total of 159 adults with type 2 diabetes, overweight (body mass index ≥26.0 kg/m
8.2Changes in Lipids and Blood Pressure
CYCLOSET does not have an unfavorable effect on fasting plasma lipids.
CYCLOSET has not demonstrated an unfavorable hypertensive effect on blood pressure. Hypotension has been reported with use of CYCLOSET in clinical trials
9HOW SUPPLIED/STORAGE AND HANDLING
CYCLOSET 0.8 mg tablets are WHITE and round with "C" on one side and "9" on the other.
The tablets are supplied as follows:
10PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Information).
11PRINCIPAL DISPLAY PANEL - 0.8 mg Tablet Bottle Label
NDC 73515-123-30
CYCLOSET
0.8 mg
200 Tablets
