Cycloset Information
Cycloset () Dosage Forms And Strengths
0.8 mg tablets are white and round, imprinted with "C" on one side and "9" on the other.
Cycloset () Contraindications
Cycloset () is contraindicated in
Cycloset () Adverse Reactions
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.
In the pooled Cycloset () phase 3 clinical trials (Cycloset () N = 2298; placebo N = 1266), adverse events leading to discontinuation occurred in 539 (24%) Cycloset () -treated patients and 118 (9%) placebo-treated patients. This between-group difference was driven mostly by gastrointestinal adverse events, particularly nausea.
The Cycloset () safety trial was a 52-week, placebo-controlled study that included patients treated only with diet therapy or with other anti-diabetic medications. 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. The mean duration of diabetes at baseline was 8 years and the mean baseline HbA1c was 7.0% with a mean baseline fasting plasma glucose of 142 mg/dL. At baseline, 12% of patients were treated with diet only, 40% were treated with one oral anti-diabetic agent, 33% were treated with two oral anti-diabetic agents, and 16% were treated with insulin alone or insulin in combination with an oral anti-diabetic agent. At baseline, 76% of patients reported a history of hypercholesterolemia, 75% reported a history of hypertension, 11% reported a history of revascularization surgery, 10% reported a history of myocardial infarction, 10% reported a history of angina, and 5% reported a history of stroke. Forty-seven percent of the Cycloset () -treated patients and 32% of the placebo-treated patients prematurely discontinued treatment. Adverse events leading to discontinuation of study drug occurred among 24% of the Cycloset () -treated patients and 15% of the placebo-treated patients. This between-group difference was driven mostly by gastrointestinal adverse events, particularly nausea.
Table 1
Cycloset () Overdosage
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.
Cycloset () Description
Cycloset () Tablets contain bromocriptine mesylate, a dopamine receptor agonist. 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, 8, 2', 5', 11', 12'.
The structural formula of bromocriptine is shown below:
Bromocriptine mesylate is a white or slightly colored fine crystalline powder with a molecular formula of CHBrNO∙CHSO and a molecular weight of 750.72. Cycloset () tablets contain bromocriptine mesylate USP in an amount equivalent to 0.8 of bromocriptine. Each tablet contains the following inactive ingredients: lactose, corn starch, magnesium stearate, colloidal silicon dioxide, and citric acid.
Cycloset () Clinical Pharmacology
Cycloset () contains bromocriptine mesylate, an ergot derivative that is a dopamine receptor agonist. The mechanism by which Cycloset () improves glycemic control is unknown. Morning administration of Cycloset () improves glycemic control in patients with type 2 diabetes without increasing plasma insulin concentrations.
Once daily morning administration of Cycloset () to humans increases circulating levels of bromocriptine, a dopamine receptor agonist, for 4-5 hours after administration.
Cycloset () Clinical 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).
Cycloset () How 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:
Cycloset () Patient Counseling Information
[See FDA-Approved Patient Labeling ().]
Patients should be informed of the potential risks and benefits of Cycloset () and of alternative therapies. Patients should also be informed about the importance of adherence to dietary instructions, regular physical activity, periodic blood glucose monitoring and HbA1c testing, recognition and management of hypoglycemia and hyperglycemia, and assessment for diabetes complications. During periods of stress such as fever, trauma, infection, or surgery, medication requirements may change and patients should be advised to seek medical advice promptly.
Patients should be advised that they may develop postural (orthostatic) hypotension with or without symptoms such as dizziness, nausea, and diaphoresis. Hypotension and syncope may occur more frequently during initial therapy or with an increase in dose at any time. During early treatment with Cycloset () , patients should be advised to make slow postural changes and to avoid situations that could predispose to serious injury if syncope was to occur.
Patients should be advised that Cycloset () may cause somnolence. Advise patients not to operate heavy machinery if symptoms of somnolence occur
Women who are nursing their children should be advised to not take Cycloset () .
Physicians should instruct their patients to read the Patient Package Insert before starting Cycloset () therapy and to reread it each time the prescription is renewed. Patients should be instructed to inform their healthcare provider if they develop any unusual symptoms or if any known symptom persists or worsens.
Manufactured for:VeroScience, LLCTiverton, RI
Printed in USA
For information for health care professionals, call 1-877-757-0666
Cycloset () is a registered trademark of
VeroScience, LLC, Tiverton, RI 02878
This product is covered by one or more of the following: U.S. Patent Nos. 5,468,755; 5,679,685; 5,716,957; 5,756,513; 5,866,584
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