Overview:
Bromocriptine mesylate is a routinely advised medication with multiple indications. The United States drug regulatory authority, the Food and Drug Administration (FDA), authorized the use of Bromocriptine mesylate for type 2 diabetes mellitus where there is an abnormal inflation in the patient’s blood sugar level. Bromocriptine mesylate gained FDA authorization on May 5, 2009, after which it has been extensively employed to tackle enhanced sugar levels.
In addition to type 2 diabetes mellitus, Bromocriptine is also advised for various ailments like acromegaly (abnormal growth elicited by exaggerated growth hormone), hyperprolactinemia (magnified prolactin level), and Parkinson's disease (a neuronal condition with deteriorating motor skills). Currently, it is being advised as monotherapy or combination therapy to curb the enhanced blood sugar level by eliciting a peculiar working mechanism.
Drug Group:
Bromocriptine mesylate belongs to the dopamine receptor agonist drug class. It promotes therapeutic effects by mimicking dopamine, a potent neurotransmitter that facilitates signal conveyance across the body.
Available Doses and Dosage Forms:
1. Dosage Forms: Bromocriptine mesylate is marketed in tablet form and is being advised for type 2 diabetes patients.
2. Available Doses: 0.8 milligrams (mg) is the available dosage of Bromocriptine mesylate. However, the concerned doctors will determine the individual dosage for the patients, and accordingly, the number of tablets will be adjusted to achieve that particular dose.
For Patients:
What Is Type 2 Diabetes Mellitus?
Type 2 diabetes mellitus is a specific form of diabetes where there is a collapsed response toward a particular hormone called insulin. Insulin is concerned with blood sugar regulation, and its action brings about a remarkable depreciation in blood sugar. Following food intake, there is an appreciable surge in the blood sugar level, which triggers insulin. It could bring the blood sugar level within the normal parameters.
In type 2 diabetes mellitus, insulin fails to elicit its action effectively. Consequently, the blood sugar level remains dramatically inflated. It is the most frequently reported form of diabetes, with a higher incident rate. Initially, the dip in insulin effectivity is counterbalanced by enhanced insulin production. Later, over time, insulin production may fail to catch up with the collapsed effectivity precipitating type 2 diabetes.
Exaggerated urinary frequency, urgency, thirst, hunger, and tiredness are the frequently encountered manifestations of type 2 diabetes mellitus. Unexplainable dip in body weight, diminishing vision, frequent infections, and numb feet are other associated manifestations of type 2 diabetes mellitus.
How Does Bromocriptine Mesylate Work?
Bromocriptine mesylate elicits a unique working principle, unlike other antidiabetic medicines. It works by influencing the brain, particularly the hypothalamus. It also aids in regulating the body’s circadian rhythm, thereby enhancing the effectiveness of the insulin hormone. In addition, the depreciation in blood glucose is potentiated by Bromocriptine’s ability to hinder glucose production within the liver.
What Is the Dosage of Bromocriptine Mesylate?
The dosage of Bromocriptine mesylate is determined by considering the patient’s response. However, the daily dosage ranges between 1.6 to 4.8 milligrams. The inceptive dose should be made as low as 0.8 milligrams, and later on, the dosage can be gradually titrated every week. The titration is continued until the daily dose hits 4.8 milligrams.
How Effective Is Bromocriptine Mesylate?
Bromocriptine mesylate is proven to be efficacious for tackling type 2 diabetes mellitus. It precipitates a notable depreciation in blood glucose levels and brings down the body’s resistance toward insulin’s actions. It potentiates the effectiveness of the insulin hormone and curbs the blood sugar level. In addition to the blood sugar level, it also narrows down the lipid profile, including free fatty acids and triglycerides. Thus, it diminishes the possibility of associated cardiovascular complications.
What Are the Things to Inform the Doctor Before Taking the Drug?
Before the inception of any therapy, there should be proper communication between the doctor and the patient to ensure the success and safety of the therapy.
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The doctor should be provided with the patient’s detailed medical history, encompassing all the medical conditions from which the patient suffered or is suffering. Enhanced blood pressure, headaches, heart problems, intestinal issues, and compromised kidney functions need to be informed without fail, as they can pose health complications upon initiation of therapy using Bromocriptine mesylate.
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Prior hypersensitivity encounters with Bromocriptine mesylate, other medicines of the same drug class, or any of the components listed under the Bromocriptine mesylate tablet’s ingredient list must be informed beforehand. Subsequent exposure to an allergic medicine can bring out adverse reactions in the body.
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It is imperative to share the patient’s drug history with the concerned doctor before therapy initiation. The drug history should be comprehensive and inclusive of all medicines, whether herbal, over-the-counter, dietary supplements or alternative medicines. Antifungal, antivirals, antihistamine, and anti-asthmatic medicines may tend to interfere with and influence the working mechanism of Bromocriptine. Keeping the doctors aware of the patient’s drug history aids in better drug choices, minimizing the possibility of drug-to-drug associations and their related consequences.
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The doctors should be aware of the patient’s pregnancy and lactation status. Bromocriptine mesylate therapy is not advisable during pregnancy as it can potentially impact the baby in the womb. Doctors may advise effective contraceptive measures to check unplanned pregnancy while on Bromocriptine therapy. Similarly, lactating women are not supposed to undergo Bromocriptine therapy, and hence lactating status should be drawn into the doctor’s attention.
How Is Bromocriptine Mesylate Administered?
Bromocriptine mesylate is marketed and circulated in pill form, which is intended to be taken by mouth. There is a specific time for the pill intake to procure the maximum therapeutic benefit. After rousing from bed in the morning, the medicine should be consumed within the first two hours, preferably with food, to reduce stomach issues.
What Are the Side Effects of Bromocriptine Mesylate?
Bromocriptine mesylate can precipitate certain adverse reactions following administration. Some of the routinely encountered side effects include the following:
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Stomach issues like constipation, vomiting, diarrhea, nausea, stomach pain, loss of hunger, and acid reflux (heartburn).
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Dizziness, tiredness, a dip in blood pressure, and headaches are also reported.
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Black stool, blood-tinged vomit, nasal discharge, chest pain, short breath, blurry vision, slurred speech, psychosis (hallucination), seizure (abnormal brain activity), and collapse are potentially serious adverse effects that mandate medical attention.
Dietary Considerations:
There are no specific dietary instructions that need to be adhered to while undergoing therapy using Bromocriptine mesylate. The medicine is advised to be consumed along with a meal to reduce the gastric irritation induced by Bromocriptine mesylate.
Missed Dose:
Bromocriptine mesylate is to be taken only once daily, that is, in the morning. If, by chance, the patient forgets about the morning dose, it is advised to disregard the forgotten dose and to move ahead with the subsequent dose (the next morning). No attempt should be made to counterbalance the forgotten one by altering the next day’s drug dosage.
Overdose:
Intake of more than the stipulated dosage of Bromocriptine mesylate can cause overdose issues. Vomiting, dizziness, constipation, exaggerated sweating, pale skin, collapsed blood pressure, extreme confusion, and loss of consciousness are reported upon exposure to Bromocriptine overdose. Gastric lavage (stomach wash) and induced vomiting (emesis) are measures to drive out the excess quantity of ingested medicine. The patient should be kept under close surveillance to keep track of their vital signs. Appropriate measures should be taken to tackle the collapsed blood pressure. The functional status of the kidneys should also be gauged.
Storage:
25 degrees Celsius (77 degrees Fahrenheit) is the preferred storage temperature for Bromocriptine mesylate. It is marketed in blister packaging and is also available in medicine bottles. The pills should be kept within the packaging until the time for ingestion. Before consumption, ensure that the pills are within the usage period.
For Doctors:
Indication:
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Type 2 Diabetes mellitus.
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Hyperprolactinemia.
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Hypogonadism.
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Acromegaly.
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Parkinson’s disease.
Dose:
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Recommended Dosage: 1.6 to 4.8 mg is the recommended dosage for type 2 diabetes mellitus patients.
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Initial Dose: The recommended inceptive dose for Bromocriptine mesylate therapy is 0.8 mg, which is the drug dose of a single pill.
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Dose Titration: Every week, the drug dose is titrated by 0.8 mg until it attains the safe tolerable dose of 4.8 mg. Doses exceeding six pills daily are not advised as they potentiate adverse reactions in the body.
Dosing Considerations:
Certain considerations in Bromocriptine dosage need to be employed when it is advised alongside moderate cytochrome 3A4 inhibitor drugs. In such cases, the maximum dosage must be restricted to 1.6 milligrams (two pills) rather than 4.8 milligrams (six pills).
What Are the Pharmacological Aspects of Bromocriptine Mesylate?
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Mechanism of Action: The mechanism with which Bromocriptine mesylate works to tackle boosted blood sugar levels is quite different from its normal mechanism. It targets the dopamine receptors in the hypothalamus and interacts with them to get the receptors activated. Upon activation, these receptors can influence the nerve signals. Bromocriptine works to overcome the insulin resistance precipitated by circadian rhythm disruptions. Bromocriptine refixes the circadian rhythm and curbs insulin resistance, contributing to better glucose metabolism. By potentiating the peripheral cell’s insulin sensitivity, the uptake and breakdown of glucose will be triggered. All these processes contribute significantly to curbing the blood sugar level.
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Pharmacodynamics: In addition to its impact on insulin sensitivity and resistance, Bromocriptine mesylate dramatically reduces glucose production, particularly in the liver. It offers sufficient collapse in the post-prandial sugar level. Furthermore, it aids in bringing the glycated hemoglobin (HbA1c) concentration within the normal range by augmenting the insulin-mediated breakdown of the glucose molecules.
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Pharmacokinetics: Upon oral ingestion, Bromocriptine mesylate is promptly uptaken from the intestine, which is then exposed to first-pass metabolism. The utmost plasma concentration is attained in about 53 minutes, provided the Bromocriptine ingestion occurs under fasting conditions. It takes around 90 to 120 minutes to attain the utmost plasma concentration in the presence of food. The distribution of Bromocriptine is primarily through plasma proteins, which form complexes with them.
The metabolic process of Bromocriptine happens in the gastrointestinal tract as well as in the liver. Liver enzymes, particularly cytochrome 3A4, are reported to be the predominant pathway for Bromocriptine’s metabolism. Only seven percent of the administered Bromocriptine is available for action in the bloodstream and the remaining 93 percent gets driven out by first-pass metabolism. Bromocriptine removal is through the biliary and urinary routes, in which the former accounts for eliminating a major proportion compared to the latter.
Toxicity:
Bromocriptine mesylate does not exhibit mutagenic or carcinogenic potentials following oral intake. In vitro studies also failed to reveal any carcinogenic properties. However, there needs to be more information concerning the long-term impacts of Bromocriptine therapy. The toxicology profile of Bromocriptine mesylate needs to be explored more to arrive at conclusive results. More studies and discussions are needed to comment on Bromocriptine’s impact on one's fertility.
Clinical Studies:
Numerous clinical studies and trials have been conducted to expose Bromocriptine's efficacy and safety aspects. Monotherapy and combination (in conjunction with other antidiabetic medicines) studies successfully demonstrated the potency of Bromocriptine as an antidiabetic medicine. All the studies demonstrated an appreciable modulation of the glycated hemoglobin concentration and an appreciable hike in glucose uptake. Bromocriptine therapy was found to be more fruitful when it is coupled with exercise and dietary alterations to bring down the blood sugar level.
What Are the Contraindications of Bromocriptine Mesylate?
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Patients who have had hyperreactivity encounters with Bromocriptine mesylate or medicines falling under the same drug class are not supposed to undergo therapy using Bromocriptine mesylate.
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Lactating women should refrain from Bromocriptine therapy, as it can curb milk production. Certain study reports pointed to incidences of stroke in lactating women following Bromocriptine therapy.
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Patients diagnosed with syncopal migraine are contraindicated for Bromocriptine therapy. Bromocriptine mesylate potentiates and worsens syncopal migraine by triggering hypotensive episodes.
Warnings and Precautions:
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Mental Disorder: Being a dopamine receptor agonist, Bromocriptine mesylate can potentially aggravate the manifestations associated with psychotic disorders. In addition, it can impair the potency of certain antipsychotic medications, further contributing to symptomatic worsening.
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Sleepiness: Bromocriptine mesylate therapy induces dizziness and somnolence, which may compromise the patient's ability to pay attention and exercise fine motor skills. Therefore, the patient should be warned about this before commencing Bromocriptine therapy so that they can abstain from such activities that would otherwise bring the patient’s life into danger.
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Hypotension: Bromocriptine mesylate therapy can precipitate an abrupt collapse in blood pressure, particularly upon postural change. The effects are more pronounced in patients who are undergoing simultaneous therapy using antihypertensives. Patients need to be warned not to indulge in abrupt postural changes while undergoing Bromocriptine therapy.
What Are the Drug Interactions of Bromocriptine Mesylate?
When two or more medicines are ingested simultaneously, there are possibilities for the medicines to exhibit interactions with each other. These interactions can modify or alter how these medicines are designed to work in the body.
Some of the potent drug interactions associated with Bromocriptine mesylate include the following:
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Bromocriptine mesylate, when concomitantly ingested with dopamine receptor antagonists, brings about an evident depreciation in the potency of both medicines. Both dopamine receptor agonists and antagonists act against each other’s mechanisms, hindering their efficacy.
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Simultaneous usage of Bromocriptine mesylate and ergot-related drugs enhances the side effects of the ergot-related medicines and, at the same time, depletes their potency.
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When Bromocriptine mesylate is administered concurrently with any cytochrome 3A4 inducer or inhibitor, it remarkably impacts Bromocriptine’s breakdown processes. Potent cytochrome 3A4 inhibitor therapy can check Bromocriptine's metabolism and hence is not advised. However, applying moderate cytochrome 3A4 inhibitors necessitates a dose reduction of Bromocriptine mesylate.
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Post-marketing surveillance reports demonstrated incidences of tachycardia and hypertension upon simultaneous administration of sympathomimetic drugs with Bromocriptine. Since only a restricted amount of information is available concerning the safety aspects of simultaneous administration, it is generally not advisable.
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Bromocriptine, when given along with therapies involving Probenecid, sulfonamides, salicylates, or Chloramphenicol, can result in deteriorated drug efficacy and a drastic rise in the incidence of adverse reactions.
Specific Considerations:
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Bromocriptine Mesylate During Pregnancy: Bromocriptine mesylate is generally not advisable for expecting women as its safety aspects are not proven in the pregnant population. There are incidences of miscarriage following Bromocriptine therapy. Therefore, expectant women are supposed to undergo Bromocriptine therapy only upon the doctor’s advice. Doctors analyze the case and determine the necessity for Bromocriptine therapy.
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Bromocriptine Mesylate During Lactation: Lactating women should ideally refrain from Bromocriptine therapy, as it can dramatically deplete breast milk production. Certain studies report incidences of stroke following Bromocriptine therapy post-childbirth.
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Bromocriptine in Pediatric Patients: Bromocriptine mesylate is not extended to the pediatric population because of the need for more reliable information concerning potency and safety.
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Bromocriptine in Geriatric Patients: Bromocriptine therapy in geriatric patients necessitates close monitoring as it poses enhanced sensitivity issues. However, Bromocritpine’s safety and effectiveness in the geriatric population are demonstrated to be on par with those of the adult population.
