Dibor R

Dibor R

bromocriptine

Manufacturer:

Zifam Pinnacle

Distributor:

Pinnacle House
Full Prescribing Info
Contents
Bromocriptine mesilate.
Description
Each tablet contains bromocriptine (as mesilate) equivalent to bromocriptine 0.8 mg.
Action
Pharmacotherapeutic Group: Type 2 anti-diabetic drug.
Pharmacology: Pharmacodynamics: Mechanism of Action: Dibor R contains bromocriptine mesilate, an ergot derivative that is a dopamine receptor agonist. The mechanism by which bromocriptine improves glycemic control is unknown. Monitoring administration of bromocriptine improves glycemic control in patients with type 2 diabetes without increasing plasma insulin concentrations.
Once daily morning administration of bromocriptine to humans increases circulating levels of bromocriptine, a dopamine receptor agonist, for 4-5 hrs after administration.
Pharmacokinetics: Absorption: When administered orally, approximately 65-95% of the bromocriptine dose of bromocriptine mesilate is absorbed. Due to extensive hepatic extraction and first-pass metabolism, approximately 7% of the dose reaches the systemic circulation. Under fasting conditions the time to maximum plasma concentration is 53 min. In contrast, following a standard high-fat meal, the time to maximum plasma concentration is increased to approximately 90-120 min. Also, the relative bioavailability of bromocriptine is increased under fed as compared to fasting conditions by an average of approximately 55-65% (increase in AUCinf).
Distribution: Bromocriptine is 90-96% bound to plasma proteins. The volume of distribution is approximately 61 L.
Metabolism: Bromocriptine mesilate is extensively metabolized in the gastrointestinal tract and liver. Metabolism by CYP3A4 is the major metabolic pathway. Most of the absorbed dose (approximately 93%) undergoes the first-pass metabolism. The remaining 7% reaches the systemic circulation.
Elimination: The major route of bromocriptine is in the bile with the remaining approximately 2-6% of an oral dose excreted via the urine. The elimination half-life (t½) is approximately 6 hrs. Prior consumption of a standard high-fat meal has little to an effect on the elimination t½ of bromocriptine.
Indications/Uses
Improve glycemic control in adults with type 2 diabetes mellitus.
Dosage/Direction for Use
Recommended Dose: 1.6-4.8 mg administered once daily within 2 hrs after waking in the morning.
It should be initiated at 1 tablet (0.8 mg) and increased by 1 tab/week until a maximum daily dose of 6 tablets (4.8 mg) or until the maximal tolerated number of tablets between 2 and 6 per day is reached.
Administration: Dibor R should be taken with food to potentially reduce gastrointestinal adverse effects eg, nausea.
Overdosage
With another formulation of bromocriptine mesilate, the mostly 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 overdosage consists of removal of Dibor R 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 IV fluids. If satisfactory relief of hypotension cannot be achieved by using the above measures to their fullest extent, vasopressors should be considered.
Contraindications
Hypersensitivity to bromocriptine, ergot-related or to any of the excipients of Dibor R.
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. Bromocriptine Dibor R is a dopamine receptor agonist and may therefore, potentiate the risk for syncope in these patients.
Use in lactation: Dibor R is contraindicated in women who are nursing their children. It contains bromocriptine which inhibits lactation. The indication for use of bromocriptine for inhibition of postpartum lactation was withdrawn based on post-marketing reports of stroke in this setting.
Special Precautions
Hypotension: Can cause orthostatic hypotension and syncope, particularly upon initiation or dose escalation. Use caution in patients taking antihypertensive medications. Assess orthostatic vital signs prior to initiation of bromocriptine and periodically thereafter. Advise patients during early treatment to avoid situations that could lead to injury if syncope was to occur.
Psychosis: May exacerbate psychotic disorders or reduce the effectiveness of drugs that treat psychosis. Use in patients with severe psychotic disorders is not recommended.
Somnolence: May cause somnolence. Advise patients not to operate heavy machinery if symptoms of somnolence occur.
Interaction with Dopamine Antagonists: Concomitant use with dopamine antagonists eg, neuroleptic agents may diminish the effectiveness of both drugs. Concomitant use is not recommended.
Other Dopamine Receptor Agonists: Effectiveness and safety are unknown in patients already taking dopamine receptor agonists for other indications. Concomitant use in not recommended.
Macrovascular Outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with bromocriptine or any other antidiabetic drug. Bromocriptine does not increase the risk of macrovascular events.
Important Limitations of Use: Dibor R should not be used to treat type 1 diabetes or diabetic ketoacidosis; limited efficacy data in combination with thiazolidinediones; efficacy has not been confirmed in combination with insulin.
Effects on the Ability to Drive or Operate Machinery: May cause somnolence. Advise patients not to operate heavy machinery if symptoms of somnolence occur.
Use in pregnancy: Pregnancy Category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well controlled studies in pregnant women.
Use In Pregnancy & Lactation
Use in pregnancy: Pregnancy Category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well controlled studies in pregnant women.
Use in lactation: Dibor R is contraindicated in women who are nursing their children. It contains bromocriptine which inhibits lactation. The indication for use of bromocriptine for inhibition of postpartum lactation was withdrawn based on post-marketing reports of stroke in this setting.
Adverse Reactions
In controlled clinical trials, adverse reactions reported in ≥5% of patients treated with Dibor R and reported more commonly than in patients treated with placebo included nausea, fatigue, dizziness, vomiting and headache. Post-marketing reports with higher doses of bromocriptine used for other indications include psychotic disorders, hallucinations and fibrotic complications.
Drug Interactions
May increase the unbound fraction of highly protein-bound therapies, altering their effectiveness and safety profiles; may increase ergot-related adverse effects or reduce ergot effectiveness for migraines if co-administered within 6 hrs of ergot-related drugs; extensively metabolized by CYP3A4. Use caution when co-administering strong inhibitors, inducers or substrates for CYP3A4.
Storage
Store below 30°C. Protect from light and moisture.
MIMS Class
ATC Classification
G02CB01 - bromocriptine ; Belongs to the class of prolactine inhibitors. Used to suppress lactation.
Presentation/Packing
Tab 0.8 mg x 3 x 10's. 10 x 10's.
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