Cabergoline 0.5mg Tablets
It is used to treat health problems where there are high prolactin levels.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Dopamine agonist, Prolactin inhibitor
Pharmacologic Class
Dopamine D2 receptor agonist
Pregnancy Category
Category B
FDA Approved
Dec 1996
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cabergoline is a medication used to lower high levels of a hormone called prolactin in your body. High prolactin levels can cause problems like irregular periods, infertility, or unwanted breast milk production. Cabergoline works by mimicking a natural brain chemical called dopamine, which helps reduce prolactin.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, as directed. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep it in its original container to maintain its potency. Ensure that all medications are stored in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, as directed. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep it in its original container to maintain its potency. Ensure that all medications are stored in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take cabergoline with food to help reduce stomach upset (nausea, vomiting).
- Do not stop taking this medication suddenly without talking to your doctor.
- Avoid alcohol or other medications that can cause drowsiness, as cabergoline can also cause dizziness or sleepiness.
- Be cautious when standing up quickly, especially from a sitting or lying position, to prevent dizziness or fainting (orthostatic hypotension).
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
0.25 mg twice weekly, increased gradually
Dose Range:
0.25 - 2 mg
Condition-Specific Dosing:
hyperprolactinemia:
Initial: 0.25 mg twice weekly. Increase by 0.25 mg twice weekly every 4 weeks as needed. Usual therapeutic dose: 0.5 mg to 1 mg twice weekly. Max: 1 mg twice weekly (2 mg total weekly).
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (safety and efficacy not established)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed
Moderate:
No specific adjustment needed
Severe:
No specific adjustment needed
Dialysis:
No specific adjustment needed; not significantly dialyzable.
Hepatic Impairment:
Mild:
No specific adjustment needed
Moderate:
Consider lower doses (e.g., 0.25 mg once weekly) and monitor for adverse effects due to potential for increased systemic exposure.
Severe:
Consider lower doses (e.g., 0.25 mg once weekly) and monitor for adverse effects due to potential for increased systemic exposure.
Pharmacology
Mechanism of Action
Cabergoline is a synthetic ergoline derivative and a potent, long-acting dopamine D2 receptor agonist. It directly inhibits prolactin secretion from the anterior pituitary gland by stimulating D2 receptors on lactotroph cells. It also has some affinity for D1, Îą2-adrenergic, 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C receptors, but its primary therapeutic effect is mediated via D2 agonism.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 60-90% (variable)
Tmax:
2-3 hours
FoodEffect:
Food does not appear to affect the absorption or pharmacokinetics of cabergoline.
Distribution:
Vd:
Approximately 43 L/kg
ProteinBinding:
40-42%
CnssPenetration:
Yes
Elimination:
HalfLife:
63-68 hours (in healthy volunteers); 79-115 hours (in hyperprolactinemic patients)
Clearance:
Approximately 4.3 L/min (total body clearance)
ExcretionRoute:
Mainly fecal (60%) and urinary (22%)
Unchanged:
Approximately 4% (urinary)
Pharmacodynamics
OnsetOfAction:
Within 3 hours (prolactin lowering)
PeakEffect:
4-8 hours (prolactin lowering)
DurationOfAction:
7-28 days (prolactin lowering, dose-dependent)
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Difficulty speaking or thinking
+ Changes in balance
+ Drooping on one side of the face
+ Blurred vision
Chest pain
Persistent cough
Severe dizziness or fainting
Changes in behavior
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
Back pain
Stomach pain
Seizures
Heart valve problems, which may be indicated by:
+ Fast or abnormal heartbeat
+ Shortness of breath
+ Swelling in the arms or legs
+ Sudden weight gain
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Constipation
Dizziness
Fatigue or weakness
Headache
* Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Difficulty speaking or thinking
+ Changes in balance
+ Drooping on one side of the face
+ Blurred vision
Chest pain
Persistent cough
Severe dizziness or fainting
Changes in behavior
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
Back pain
Stomach pain
Seizures
Heart valve problems, which may be indicated by:
+ Fast or abnormal heartbeat
+ Shortness of breath
+ Swelling in the arms or legs
+ Sudden weight gain
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Constipation
Dizziness
Fatigue or weakness
Headache
* Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent headache
- Vision changes
- Chest pain, shortness of breath, or persistent cough (signs of lung or heart problems)
- Swelling in your ankles, feet, or legs
- Unusual changes in behavior or mood, such as increased gambling, shopping, sexual urges, or aggression
- Severe dizziness or fainting
- Unusual bleeding or bruising
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have high blood pressure.
If you have a history of certain health conditions, such as:
+ Heart valve problems
+ Thickening (fibrosis) in areas like the lungs or heart
If you are taking any medications, including prescription and over-the-counter (OTC) drugs, natural products, or vitamins, that may interact with this medication. Specifically, inform your doctor about medications used to treat mental or mood problems, migraines, stomach or bowel problems, and other conditions. There are many medications that should not be taken with this drug.
If you are breastfeeding. Note that you should not breastfeed while taking this medication.
This is not an exhaustive list of all potential interactions or health problems that may affect your ability to take this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
Do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have high blood pressure.
If you have a history of certain health conditions, such as:
+ Heart valve problems
+ Thickening (fibrosis) in areas like the lungs or heart
If you are taking any medications, including prescription and over-the-counter (OTC) drugs, natural products, or vitamins, that may interact with this medication. Specifically, inform your doctor about medications used to treat mental or mood problems, migraines, stomach or bowel problems, and other conditions. There are many medications that should not be taken with this drug.
If you are breastfeeding. Note that you should not breastfeed while taking this medication.
This is not an exhaustive list of all potential interactions or health problems that may affect your ability to take this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
Do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. To minimize the risk of dizziness or fainting, stand up slowly when getting up from a sitting or lying down position, and exercise caution when climbing stairs.
Regular monitoring of your blood work and heart function is crucial, as directed by your doctor. Although rare, this medication has been associated with the development of thickening (fibrosis) in certain areas, such as the lungs or heart. If you have any concerns or questions, discuss them with your doctor.
If you are pregnant or planning to become pregnant, it is vital to consult with your doctor to weigh the benefits and risks of using this medication during pregnancy.
Regular monitoring of your blood work and heart function is crucial, as directed by your doctor. Although rare, this medication has been associated with the development of thickening (fibrosis) in certain areas, such as the lungs or heart. If you have any concerns or questions, discuss them with your doctor.
If you are pregnant or planning to become pregnant, it is vital to consult with your doctor to weigh the benefits and risks of using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Nasal congestion
- Fainting
- Hallucinations
- Psychosis
- Hypotension (low blood pressure)
- Nausea
- Vomiting
What to Do:
Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is generally supportive, including maintaining blood pressure and, if appropriate, administering dopamine antagonists.
Drug Interactions
Contraindicated Interactions
- Drugs known to cause fibrotic disorders (e.g., ergot derivatives, unless for specific indications)
- Patients with a history of cardiac valvulopathy or pulmonary/retroperitoneal fibrosis
Major Interactions
- Dopamine antagonists (e.g., phenothiazines, butyrophenones, thioxanthenes, metoclopramide, domperidone): May reduce the prolactin-lowering effect of cabergoline.
- Antihypertensives: May cause additive hypotensive effects.
Moderate Interactions
- Macrolide antibiotics (e.g., erythromycin, clarithromycin): Theoretical potential for increased cabergoline levels due to minor CYP3A4 inhibition, though not clinically significant for cabergoline's primary metabolism.
- Other ergot alkaloids (e.g., bromocriptine, pergolide): Additive effects or antagonism.
Minor Interactions
- Alcohol: May increase risk of CNS depression or orthostatic hypotension.
Monitoring
Baseline Monitoring
Serum Prolactin Levels
Rationale: To confirm diagnosis of hyperprolactinemia and establish baseline for treatment efficacy.
Timing: Prior to initiation of therapy
Blood Pressure (sitting and standing)
Rationale: To assess for baseline hypotension and monitor for orthostatic hypotension, a common side effect.
Timing: Prior to initiation of therapy
Echocardiogram
Rationale: Recommended for patients on long-term, high-dose therapy (e.g., >2 mg/week) or those with a history of cardiac valvulopathy, due to risk of fibrotic reactions.
Timing: Prior to initiation of therapy (if indicated)
Renal and Hepatic Function Tests
Rationale: To assess baseline organ function, especially in patients with pre-existing impairment.
Timing: Prior to initiation of therapy
Routine Monitoring
Serum Prolactin Levels
Frequency: Every 4 weeks during dose titration, then every 3-6 months once stable
Target: Normalization of prolactin levels
Action Threshold: If prolactin levels remain elevated, consider dose increase; if normalized, continue monitoring.
Blood Pressure (sitting and standing)
Frequency: Regularly, especially during dose titration and if symptoms of hypotension occur
Target: Within patient's normal range, without significant orthostatic drop
Action Threshold: Significant hypotension or orthostatic changes may require dose reduction or discontinuation.
Symptoms of Fibrotic Reactions (e.g., dyspnea, persistent cough, chest pain, abdominal pain, peripheral edema)
Frequency: Regularly, at each visit
Target: Absence of symptoms
Action Threshold: If symptoms develop, discontinue cabergoline and perform appropriate diagnostic work-up (e.g., echocardiogram, chest X-ray, ESR).
Echocardiogram
Frequency: Every 6-12 months for patients on long-term, high-dose therapy (>2 mg/week) or if symptoms of valvulopathy develop.
Target: Normal cardiac valve function
Action Threshold: Evidence of valvular thickening or restriction may require discontinuation.
Symptom Monitoring
- Nausea
- Headache
- Dizziness
- Fatigue
- Orthostatic hypotension
- Constipation
- Abdominal pain
- Dyspepsia
- Vomiting
- Breast pain
- Hot flashes
- Depression
- Nervousness
- Sleep disturbances (insomnia, somnolence)
- Psychiatric changes (e.g., impulse control disorders, psychosis, aggression)
- Symptoms of fibrotic reactions (e.g., shortness of breath, persistent cough, chest pain, flank pain, leg swelling)
Special Patient Groups
Pregnancy
Cabergoline is Pregnancy Category B. Studies in animals have shown no evidence of teratogenicity. Limited human data suggest no increased risk of major congenital malformations. Treatment may be continued during pregnancy if the benefits outweigh the potential risks, especially for large or invasive prolactinomas.
Trimester-Specific Risks:
First Trimester:
No increased risk of major congenital malformations observed in limited human data.
Second Trimester:
Generally considered safe if continued.
Third Trimester:
Generally considered safe if continued.
Lactation
Not recommended during lactation. Cabergoline inhibits prolactin secretion, which will prevent or suppress lactation. It is unknown if cabergoline is excreted in human milk, but due to its mechanism of action, it would likely suppress milk production.
Infant Risk:
Risk of insufficient milk supply; potential unknown effects if excreted into milk.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Use is generally not recommended.
Geriatric Use
No specific dose adjustments are generally required for elderly patients. However, elderly patients may be more sensitive to the hypotensive and CNS effects of cabergoline, so careful monitoring is advised.
Clinical Information
Clinical Pearls
- Cabergoline has a very long half-life, allowing for twice-weekly dosing, which improves patient adherence compared to daily bromocriptine.
- It is generally better tolerated than bromocriptine, with fewer gastrointestinal side effects.
- Fibrotic reactions (cardiac valvulopathy, pleuropulmonary fibrosis, retroperitoneal fibrosis) are rare but serious side effects, primarily associated with long-term, high-dose use (e.g., for Parkinson's disease, not typically for hyperprolactinemia at standard doses). Regular cardiac monitoring (echocardiogram) is recommended for patients on high doses or long-term therapy.
- Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping) can occur with dopamine agonists; patients and caregivers should be counselled on these potential side effects.
- Dosing should be initiated at a low dose and gradually titrated up to minimize side effects, especially orthostatic hypotension.
Alternative Therapies
- Bromocriptine (another dopamine D2 agonist)
- Transsphenoidal surgery (for prolactinomas resistant to medical therapy or with mass effect)
- Radiation therapy (for resistant or recurrent prolactinomas)
Cost & Coverage
Average Cost:
$50 - $200 per 8 tablets (0.5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.