Bromocriptine is a medication primarily used in the treatment of Parkinson's disease and certain hormone-related disorders like hyperprolactinemia (excessive prolactin production). It belongs to a class of medications called dopamine agonists, which means it works by activating dopamine receptors in the brain.

In Parkinson's disease, a lack of dopamine in certain parts of the brain leads to movement difficulties. Bromocriptine helps alleviate these symptoms by mimicking the action of dopamine. It can improve motor function and reduce tremors, stiffness, and slowness of movement.

In the case of hyperprolactinemia, bromocriptine works by reducing the secretion of prolactin from the pituitary gland. This can be beneficial in treating conditions such as infertility, menstrual disorders, and certain types of tumors that cause excessive prolactin production.

Bromocriptine is an ergot derivative that activates post-synaptic dopamine receptors in the brain. It is used in the treatment of the following conditions:

• Therapy for acromegaly.
• For glycemic control in addition to diet and exercise in individuals with type 2 diabetes.
• Prolactin-secreting pituitary adenoma treatment
• Treatment of hyperprolactinemia-related amenorrhea, galactorrhea, hypogonadism, or infertility.
• As a supplement to levodopa or levodopa/carbidopa for the symptomatic treatment of post-encephalitic or idiopathic Parkinson's disease.
• As an off-label use for the treatment of the neuroleptic malignant syndrome.

Bromocriptine Dose in Adults

Bromocriptine Use in the treatment of Acromegaly:

• When using bromocriptine for acromegaly, the typical starting dose is between 1.25 to 2.5 milligrams taken by mouth once a day.
• If needed, the dose can be increased gradually every 3 to 7 days by another 1.25 to 2.5 milligrams per day.
• The usual total daily dose ranges from 20 to 30 milligrams, but in some cases, it can go up to a maximum of 100 milligrams per day.

Remember, it's essential to follow your doctor's instructions carefully and not to adjust your dose without consulting them first. They'll monitor your progress and adjust your dosage as needed to get the best results while minimizing side effects.

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Bromocriptine Use in the treatment of Type 2 Diabetes mellitus (Cycloset only):

Bromocriptine, specifically in its Cycloset form, is used to treat type 2 diabetes mellitus, a condition where the body struggles to regulate blood sugar levels. However, it's important to note that other medications are usually recommended as the first choice for treating type 2 diabetes.

• For Cycloset, the initial dose is typically 0.8 milligrams taken orally once daily in the morning.
• This dose can be increased weekly by 0.8 milligrams if tolerated.
• The usual dose falls between 1.6 to 4.8 milligrams taken once daily, with a maximum dose of 4.8 milligrams per day.

Cycloset dose adjustment in patients on concomitant moderate CYP3A4 inhibitor therapy like erythromycin:

• If you're taking other medications that may interact with Cycloset, such as moderate CYP3A4 inhibitors like erythromycin, the maximum dose should not exceed 1.6 milligrams per day.

Patients on Strong CYP3A4 inhibitors like azole antimycotics and HIV protease inhibitors:

• For strong CYP3A4 inhibitors (like certain antifungal or HIV medications), it's advised to avoid using them together with Cycloset.
• If you're switching from a strong CYP3A4 inhibitor to Cycloset, make sure there's enough time for the inhibitor to clear out of your system before starting bromocriptine.

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Bromocriptine Use in the treatment of Hyperprolactinemia:

• For hyperprolactinemia, the typical starting dose of bromocriptine is between 1.25 to 2.5 milligrams taken orally once a day.
• Depending on how well it's tolerated and how your body responds, your doctor may increase the dose by another 2.5 milligrams daily every 2 to 7 days.
• The goal is to find the lowest effective dose that brings your prolactin levels back to normal.
• The dosage range for treating hyperprolactinemia with bromocriptine typically falls between 2.5 to 15 milligrams per day.
• Your doctor will monitor your prolactin levels and adjust your dose accordingly to achieve the best results while minimizing side effects.

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Bromocriptine Use in the treatment of Parkinsonism:

• When using bromocriptine for Parkinsonism, the typical starting dose is 1.25 milligrams taken orally twice daily.
• Your doctor may increase the dose by 2.5 milligrams daily every 2 to 4 weeks as necessary, depending on how well it's working for you and how your body tolerates it.
• The maximum daily dose of bromocriptine for Parkinsonism is 100 milligrams.
• However, it's essential to reach this dosage gradually under the supervision of your doctor to minimize side effects and ensure the best results.

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Bromocriptine off-label use in the treatment of Neuroleptic malignant syndrome:

• When using bromocriptine for NMS, the typical starting dose is 2.5 milligrams taken orally or through a gastric tube every 8 to 12 hours.
• Depending on the severity of the symptoms and how well the medication works for you, your doctor may increase the dose gradually.
• The maximum daily dose of bromocriptine for treating NMS is 45 milligrams.
• Treatment with bromocriptine continues until the symptoms of NMS are under control.
• Once the condition is stabilized, your doctor will slowly taper off the medication to prevent any recurrence of symptoms.

Bromocriptine Dose in Children

Bromocriptine Use in the treatment of Hyperprolactinemia secondary to pituitary adenoma:

For children and adolescents under 16 years old with hyperprolactinemia caused by a pituitary adenoma, the use of bromocriptine is based on limited data:

• Initial dose: 1.25 to 2.5 milligrams taken orally once a day.
• The dosage can be increased gradually as tolerated to achieve a therapeutic response.
• The typical effective range is between 5 to 7.5 milligrams per day, divided into multiple doses.
• The maximum daily dose should not exceed 10 milligrams per day.

For adolescents aged 16 years and older with the same condition:

• Initial dose: 1.25 to 2.5 milligrams taken orally once a day.
• The dose may be increased by 2.5 milligrams daily every 2 to 7 days as tolerated until the optimal response is achieved.
• The usual effective range is between 5 to 7.5 milligrams per day, divided into multiple doses.
• The maximum daily dose should not exceed 15 milligrams per day.

Pregnancy Risk Factor B

• Bromocriptine is considered relatively safe during pregnancy, with a low risk factor (Pregnancy Risk Factor B).
• While it can cross the placenta, studies haven't shown an increased risk of birth defects when used during pregnancy, especially if discontinued within the first 8 weeks of pregnancy.
• However, it's crucial for women with hyperprolactinemia, who might have fertility issues, to use mechanical contraception while on bromocriptine until normal ovulatory cycles resume.
• If pregnancy is desired, contraception can be stopped once normal cycles return.
• If bromocriptine is needed during pregnancy, close monitoring is necessary for signs of a prolactin-secreting tumor enlargement or hypertensive disorders.
• Regular pregnancy tests are recommended during amenorrhea, as fertility may return before menstruation resumes.
• Women not planning pregnancy should use contraception.
• For conditions like acromegaly or Parkinson's, consider stopping bromocriptine during pregnancy, but in cases of rapidly growing pituitary tumors, continued treatment may be necessary.

Bromocriptine uses during breastfeeding:

• Bromocriptine should not be used by nursing women for treating type 2 diabetes or by postpartum women with a history of severe cardiovascular conditions like coronary artery disease, unless withdrawing the medication is medically unfeasible.
• It's known to inhibit lactation, and its previous use for preventing postpartum lactation was discontinued by the manufacturer due to serious adverse reactions reported, such as stroke, heart attack, seizures, and severe hypertension.

Bromocriptine Dose in Renal Disease:

• The manufacturer's labeling for bromocriptine does not include specific dosage adjustments for individuals with renal impairment because it hasn't been studied in this population.

Bromocriptine Dose in Liver Disease:

• The manufacturer's labeling for bromocriptine doesn't include specific dosage adjustments.
• However, caution is advised when using it because it undergoes extensive metabolism in the liver.

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Note: The frequency of adverse effects may vary by dose and/or indication.

Common side effects of bromocriptine include:

• Central Nervous System:
  • Fatigue
  • Dizziness
  • Headache
• Neuromuscular & Skeletal:
  • Weakness
• Gastrointestinal:
  • Constipation
  • Nausea
• Respiratory:
  • Rhinitis

Less Common Side Effects of Bromocriptine Include:

• Central Nervous System:
  • Drowsiness
  • Lightheadedness
• Endocrine & Metabolic:
  • Hypoglycemia
• Cardiovascular:
  • Hypotension
  • Raynaud's Phenomenon
  • Syncope
  • Vasospasm
• Gastrointestinal:
  • Abdominal Cramps
  • Anorexia
  • Diarrhea
  • Dyspepsia
  • Gastrointestinal Hemorrhage
  • Vomiting
  • Xerostomia
• Infection:
  • Increased Susceptibility To Infection
• Ophthalmic:
  • Amblyopia
• Respiratory:
  • Flu-Like Symptoms
  • Nasal Congestion
  • Sinusitis

Contraindications to Bromocriptine include:

• Individuals with a known hypersensitivity to bromocriptine, ergot alkaloids, or any component of the formulation should not use bromocriptine.
• Additionally, specific product formulations like Cycloset should be avoided in individuals with syncopal migraine or during breastfeeding.
• For Parlodel, contraindications include uncontrolled hypertension, pregnancy (although a risk-to-benefit evaluation is needed in certain cases), and postpartum women with a history of severe cardiovascular conditions (unless discontinuing the medication is not medically feasible).

Warnings and Precautions

Cardiac valvular fibrosis:

• Long-term, chronic use of ergot alkaloids and derivatives, including bromocriptine, has been linked to a condition called cardiac valvular fibrosis.
• This condition involves the thickening of heart valves, such as the aortic, mitral, and tricuspid valves.

Cardiovascular effects

• Bromocriptine can affect the cardiovascular system, potentially leading to hypotension (including orthostatic hypotension), syncope (fainting), hypertension, seizures, heart attacks (MI), and strokes.
• Symptoms such as severe headache or visual changes may precede these events.
• These reactions can occur immediately or with a delay, often in the second week of therapy.
• If patients experience severe, progressive, or unremitting headache (with or without visual disturbance), hypertension, or signs of CNS toxicity, discontinuation of therapy is recommended, followed by prompt evaluation.
• According to a scientific statement from the American Heart Association, bromocriptine has been classified as an agent that may cause direct toxicity to the heart muscle, with a major magnitude.

CNS depression:

• Bromocriptine can lead to central nervous system (CNS) depression, potentially impairing both physical and mental abilities.
• This effect may be more pronounced in patients with Parkinson's disease and could result in sudden episodes of sleep onset.
• Patients should be advised to exercise caution when engaging in tasks that require mental alertness, such as operating machinery or driving.
• If symptoms of CNS depression occur, dosage reduction or discontinuation of therapy should be considered.

Hallucinations

• Bromocriptine, either taken alone or together with levodopa, may lead to visual or auditory hallucinations.
• If these symptoms occur, dosage reductions or discontinuation of the medication may be necessary.
• It's important to note that hallucinations may persist for several weeks even after stopping the medication.
• Patients and caregivers should be vigilant for any signs of hallucinations and inform their healthcare provider promptly if they occur.

Impulse control disorders:

• Dopamine agonists like bromocriptine, when used to treat Parkinson's disease or restless legs syndrome, have been linked to impulse control disorders.
• These can include new or intensified urges for activities like gambling, sexual behavior, or spending money excessively.
• In some cases, reducing the dose or stopping the medication can reverse these behaviors, but not always.
• It's crucial for patients and caregivers to be aware of these potential side effects and to promptly report any unusual or concerning behaviors.

Melanoma

• Patients with Parkinson's disease have an increased risk of developing melanoma.
• While it's not clear whether medications like bromocriptine directly cause melanoma or contribute to the risk, it's important to closely monitor all patients for signs of melanoma and perform regular skin examinations.

Retroperitoneal and pleural fibrosis

• Prolonged and high-dose daily use of bromocriptine has been associated with cases of pleural and pericardial effusions, as well as fibrosis in the pleura, lungs, and retroperitoneum, along with constrictive pericarditis.
• If fibrotic changes are suspected, discontinuation of therapy is recommended.

Acromegaly:

• In the treatment of acromegaly, if there is evidence of tumor expansion during therapy with bromocriptine, discontinuation of the medication is recommended.
• For patients who have undergone pituitary irradiation, therapy with bromocriptine should be withheld for 4 to 8 weeks annually to assess both the clinical effects of radiation on the disease process and the effects of bromocriptine.
• Some patients with acromegaly may experience digital vasospasm, which is sensitive to cold and may necessitate a dosage reduction of bromocriptine.

Cardiovascular disease

• Bromocriptine should be used with caution in patients with cardiovascular disease, including those with a history of myocardial infarction (heart attack) or residual atrial, nodal, or ventricular arrhythmias (irregular heart rhythms).
• These conditions can increase the risk of cardiovascular complications associated with bromocriptine use.

Dementia

• Bromocriptine should be used cautiously in patients with dementia.
• High doses of bromocriptine may potentially exacerbate confusion and mental disturbances in these patients.

Galactose intolerance (Parlodel),

• Patients with rare hereditary conditions such as galactose intolerance, severe lactase deficiency, or glucose-galactose malabsorption should avoid using Parlodel, a specific formulation of bromocriptine.
• This medication contains certain ingredients that could worsen these conditions or cause adverse effects.

Hepatic impairment

• Patients with hepatic impairment should use bromocriptine with caution.
• Since bromocriptine undergoes extensive metabolism in the liver, dosage adjustments may be necessary in these patients.

Macroadenomas:

• Discontinuing bromocriptine therapy in patients with macroadenomas, which are large pituitary tumors, has been linked to rapid regrowth of the tumor and increased levels of prolactin in the blood.

Peptic ulcer disease:

• Bromocriptine should be used cautiously in patients with peptic ulcer disease.
• There have been reports of severe gastrointestinal bleeding, including some fatal cases, associated with its use in this population.

Adenomas that secrete prolactin:

• In patients with prolactin-secreting adenomas, there have been observations of cerebrospinal fluid rhinorrhea, which is the leakage of cerebrospinal fluid from the nose.
• This condition may occur due to the effects of the adenoma on the surrounding structures, particularly the skull base and adjacent tissues.

Psychosis:

• Bromocriptine should be used cautiously in patients with psychosis.
• Dopamine agonists like bromocriptine can potentially worsen psychotic symptoms or reduce the effectiveness of medications used to treat psychosis.
• Therefore, it's important for healthcare providers to carefully assess the risks and benefits of bromocriptine therapy in patients with psychosis.
• Additionally, the use of bromocriptine in patients with severe psychotic disorders is not recommended due to the risk of exacerbating symptoms and worsening the underlying condition.

Bromocriptine: Drug Interaction

Risk Factor C (Monitor therapy)
Alcohol (Ethyl)	May enhance the adverse/toxic effect of Bromocriptine. Bromocriptine may enhance the adverse/toxic effect of Alcohol (Ethyl).
Alfuzosin	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Alpha-Lipoic Acid	May enhance the hypoglycemic effect of Antidiabetic Agents.
Androgens	May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Exceptions: Danazol.
Antiemetics (5HT3 Antagonists)	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Barbiturates	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Blood Pressure Lowering Agents	May enhance the hypotensive effect of HypotensionAssociated Agents.
Brimonidine (Topical)	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Bromopride	May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist).
BuPROPion	Dopamine agonists (anti-Parkinson agents) may intensify the negative/toxic effects of bupropion.
Chloroprocaine	Ergot derivatives' ability to cause hypertension may be increased.
Clofazimine	may lead to a rise in CYP3A4 substrate serum concentration (high risk with inhibitors).
Diazoxide	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Diethylstilbestrol	Bromocriptine's toxic or harmful effects might be exacerbated. Specifically, the risk for amenorrhea may be increased with the combination.
Direct Acting Antiviral Agents (HCV)	could make anti-diabetic medications more effective at lowering blood sugar.
DULoxetine	DULoxetine's hypotensive effect may be strengthened by blood pressure-lowering medications.
Fosaprepitant	may lead to a rise in CYP3A4 substrate serum concentration (high risk with inhibitors).
Guanethidine	could make anti-diabetic medications more effective at lowering blood sugar.
Herbs (Hypotensive Properties)	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Hyperglycemia-Associated Agents	could lessen the therapeutic effect of diabetes treatment drugs.
Hypoglycemia-Associated Agents	Anti-diabetic medications can make hypoglycemia-associated medications work more effectively.
Hypotension-Associated Agents	Hypotension-Associated Agents may have a stronger hypotensive effect when combined with blood pressure-lowering medications.
Larotrectinib	CYP3A4 substrates' serum concentration may rise (high risk with inhibitors).
Levodopa-Containing Products	Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products.
Lormetazepam	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Maitake	May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Metaxalone	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Methylphenidate	May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist).
Methylphenidate	May enhance the adverse/toxic effect of Serotonin Modulators. Specifically, the risk of serotonin syndrome or serotonin toxicity may be increased.
Metoclopramide	May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist).
Metoclopramide	Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome.
Molsidomine	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Monoamine Oxidase Inhibitors	May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Naftopidil	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Nicergoline	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Nicorandil	May enhance the hypotensive effect of Blood Pressure Lowering Agents.
Nitroprusside	Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside.
Opioid Agonists	could make serotonin modulators' serotonergic effects stronger. This could result in serotonin syndrome.
Palbociclib	may lead to a rise in CYP3A4 substrate serum concentration (high risk with inhibitors).
Pegvisomant	Can make blood glucose lowering medications more effective at lowering blood sugar.
Pentoxifylline	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Pholcodine	The hypotensive effects of pholcodine may be strengthened by blood pressure lowering medications.
Phosphodiesterase 5 Inhibitors	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Prostacyclin Analogues	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Prothionamide	Can make blood glucose lowering medications more effective at lowering blood sugar.
Quinagolide	The hypotensive effects of blood pressure-lowering medications may be strengthened.
Quinolones	Can make blood glucose lowering medications more effective at lowering blood sugar. Quinolones may lessen the therapeutic impact of glucose lowering medications. More specifically, quinolone use may result in a loss of blood sugar control if a medication is being used to treat diabetes.
Reboxetine	could make ergot derivatives' hypertensive effects more potent.
Ritodrine	may lessen the therapeutic effect of diabetes medications.
Salicylates	Can make blood glucose lowering medications more effective at lowering blood sugar.
Selective Serotonin Reuptake Inhibitors	May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Serotonin Modulators	May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid.
Simeprevir	may lead to a rise in CYP3A4 substrate serum concentration (high risk with inhibitors).
Solriamfetol	Solriamfetol's ability to increase blood pressure may be enhanced by anti-Parkinson drugs (dopamine agonist).
Somatostatin Analogs	Potentially raising bromocriptine's serum concentration. Somatostatin Analogs may also delay bromocriptine absorption and time to maximum plasma concentrations.
Tedizolid	Serotonin Modulators may have a stronger serotonergic effect. This could result in serotonin syndrome.
Thiazide and Thiazide-Like Diuretics	could lessen the therapeutic effect of diabetes treatment drugs.
TraMADol	Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Risk Factor D (Consider therapy modification)
Amifostine	Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered.
Anti-Parkinson Agents (Monoamine Oxidase Inhibitor)	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline, rasagiline, or safinamide is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated.
Antipsychotic Agents (First Generation [Typical])	reduce the therapeutic benefit of dopamine antagonists (anti-Parkinson agents). The therapeutic benefit of First Generation [Typical] Antipsychotic Agents may be reduced by Anti-Parkinson Agents (Dopamine Agonist). Management: If concurrent therapy cannot be avoided, monitor for diminished effects of both medications and avoid it as much as you can. Atypical antipsychotics like quetiapine and clozapine may have a lower likelihood of reducing the effects of anti-Parkinson medications.
Antipsychotic Agents (Second Generation [Atypical])	reduce the therapeutic benefit of dopamine antagonists (anti-Parkinson agents). When possible, alternative antipsychotic medications should be used with Parkinson disease patients. If an atypical antipsychotic is required, take into account quetiapine or clozapine as they may carry the lowest risk of interactions.
Beta-Blockers	Could make ergot derivatives' vasoconstricting effects stronger.
CYP3A4 Inhibitors (Moderate)	May increase the serum concentration of Bromocriptine. Management: The bromocriptine dose should not exceed 1.6 mg daily with use of a moderate CYP3A4 inhibitor. The Cycloset brand specifically recommends this dose limitation, but other bromocriptine products do not make such specific recommendations.
Linezolid	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely.
Obinutuzumab	May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion.
Stiripentol	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.
Risk Factor X (Avoid combination)
Alizapride	may reduce the therapeutic benefit of dopamine agonists (anti-Parkinson agents).
Alpha-/Beta-Agonists	Alpha-/BetaAgonists' ability to increase blood pressure may be enhanced by ergot derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists.
Alpha1-Agonists	Alpha1-Agonists' ability to cause hypertension may be increased by ergot derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists.
Amisulpride	may lessen the therapeutic benefit of dopamine agonists, which are anti-Parkinson's drugs. Amisulpride's therapeutic effect may be reduced by anti-Parkinson drugs (dopamine agonist).
Bromperidol	Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents.
Conivaptan	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Inhibitors (Strong)	May increase the serum concentration of Bromocriptine.
Dapoxetine	Serotonin modulators' toxic or harmful effects could be increased.
Fusidic Acid (Systemic)	may raise serum levels of CYP3A4 substrates (high risk with inhibitors).
Idelalisib	may raise serum levels of CYP3A4 substrates (high risk with inhibitors).
Lorcaserin	may enhance the adverse/toxic effects of ergot derivatives. Specifically, the use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome.
Methylene Blue	May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Nitroglycerin	Ergot derivatives may diminish the vasodilatory effect of nitroglycerin. For patients receiving angina treatment, this is especially concerning. The serum level of ergot derivatives may rise when using nitroglycerin.
Protease Inhibitors	could make ergot derivatives more concentrated in the blood.
Roxithromycin	could make ergot derivatives more concentrated in the blood.
Serotonin 5-HT1D Receptor Agonists	Serotonin 5-HT1D Receptor Agonists' ability to constrict blood vessels may be enhanced by ergot derivatives. The vasoconstrictive effects of ergot derivatives may be enhanced by serotonin 5-HT1D receptor antagonists.
Sulpiride	may reduce the therapeutic benefit of dopamine agonists (anti-Parkinson agents).

Monitor:

Monitoring for Bromocriptine Therapy

• Blood Pressure and Heart Rate:
  • Check orthostatic vital signs initially and periodically thereafter.
• Organ Function:
  • Assess hepatic, renal, hematopoietic, and cardiovascular function periodically.
• Visual Fields:
  • Perform periodic assessments, especially in patients with prolactinoma.
• Pregnancy Test:
  • Conduct during the amenorrheic period.
• Hormone Levels:
  • Monitor growth hormone levels periodically in acromegaly patients.
  • Check prolactin levels regularly.
• Gastrointestinal Bleeding:
  • Monitor closely in patients with a history of peptic ulcer.
• Melanoma Skin Examinations:
  • Conduct regular assessments for signs of melanoma.

Monitoring for Diabetes Mellitus, Type 2

• Serum Glucose and HbA1c:
  • Test at least twice yearly for patients with stable glycemic control and meeting treatment goals.
  • Conduct quarterly in patients not meeting treatment goals or with therapy changes according to ADA 2019 guidelines.

How to take bromocriptine?

• With Food:
  • Administer bromocriptine with food to reduce gastrointestinal distress.

Specific Instructions for Cycloset

• Timing:
  • Take Cycloset within 2 hours of waking up in the morning.
• Missed Dose:
  • If the morning dose is missed, wait until the next morning to resume with the usual dose.

Mechanism of action of Bromocriptine:

• Bromocriptine is a medication derived from ergot alkaloids and acts as a dopamine D receptor agonist.
• In the brain, it activates dopamine receptors in two key pathways: the tuberoinfundibular pathway, which inhibits the release of prolactin from the pituitary gland, and the nigrostriatal pathway, which helps regulate motor control.
• In the treatment of type 2 diabetes mellitus, bromocriptine's exact mechanism of action is not fully understood.
• However, it's thought to influence circadian rhythms, which are partly controlled by dopamine activity and are implicated in obesity and insulin resistance.
• By administering bromocriptine in the morning and causing a rapid release into the bloodstream, it may help reset hypothalamic circadian activities disrupted by obesity.
• This resetting could lead to improved insulin sensitivity and reduced glucose production without increasing insulin levels in the blood.

Distribution:

• Volume of Distribution (V): Approximately 61 liters.

Protein Binding:

• Bromocriptine is highly bound to proteins, primarily albumin, with binding ranging from 90% to 96%.

Metabolism:

• Metabolized mainly in the liver via the CYP3A enzyme system, undergoing extensive first-pass biotransformation.
• Cycloset undergoes approximately 93% metabolism.

Bioavailability:

• Cycloset has a bioavailability ranging from 65% to 95%.

Half-life Elimination:

• Cycloset: Approximately 6 hours.
• Parlodel: Approximately 4.85 hours.

Time to Peak Serum Concentration:

• Cycloset: Around 53 minutes.
• Parlodel: Approximately 2.5 ± 2 hours.

Excretion:

• Bromocriptine is primarily excreted in the feces (approximately 82%).
• A smaller proportion is excreted in the urine (ranging from 2% to 6%).

International brands of Bromocriptine:

• Bromocriptine
• DOM-Bromocriptine
• NU-Bromocriptine
• PMS-Bromocriptine
• Antiprotin
• Apo-Bromocriptine
• Aspen Bromocriptine
• Barlolin
• Brameston
• Brom
• Bromergon
• Bromo-Kin
• Bromocriptin-Richter
• Bromocriptina
• Bromolac
• Butin
• Cripsa
• Criptine
• Criten
• Demil
• Deprolac
• Dopagon
• Kripton
• Lactodel
• Medocriptine
• Parlodel
• Pravidel
• Protinal
• Ronalin
• Serocryptin
• Suplac
• Umprel

Bromocriptine brand names in Pakistan:

Bromocriptine (Mesylate) [Tabs 10 mg]
Brolib	Libra Pharmaceuticals (Pvt) Ltd

 

Bromocriptine (Mesylate) [Tabs 2.5 mg]
Bromicon	Helicon Pharmaceutek Pakistan (Pvt) Ltd.
Bromotin	Caraway Pharmaceuticals
Brotin	Shaigan Pharmaceuticals (Pvt) Ltd
Cripton	Evron (Pvt) Ltd.
Cripton	Evron (Pvt) Ltd.
Parlodel	Novartis Pharma (Pak) Ltd