Cabergoline is a potent dopamine receptor agonist that serves as a first-line treatment for hyperprolactinemia, a condition marked by abnormally high prolactin levels. By targeting the root cause of excessive prolactin secretion, this medication effectively restores hormonal balance, alleviating symptoms like irregular menstruation, infertility, and lactation abnormalities.

With superior efficacy compared to alternatives and a favorable safety profile, Cabergoline has become a cornerstone therapy for managing prolactin-related disorders.

What is Cabergoline Tablet?

Cabergoline is a synthetic ergot-derived dopamine agonist that selectively activates D2 dopamine receptors in the pituitary gland. This action suppresses prolactin release, addressing the hormonal imbalance driving conditions like hyperprolactinemia.

Available as Cabergoline 0.5 mg tablets, this medication is marketed under brand names such as Dostinex. Each Cabergoline tablet delivers long-lasting effects, often requiring only twice-weekly dosing.

What are the Uses of Cabergoline tablets?

Cabergoline tablet uses include treating hyperprolactinemia, prolactinomas, and restoring fertility. Specifically, Cabergoline 0.5 mg tablet uses have been well-documented in clinical guidelines for managing elevated prolactin levels.

Conditions Cabergoline Treats

Primary Uses:

  • Hyperprolactinemia treatment: Effectively manages elevated prolactin levels that cause menstrual irregularities, fertility problems, and unwanted breast milk production
  • Prolactinomas: Treat pituitary tumours that secrete excess prolactin hormone
  • Fertility restoration: Helps both men and women overcome fertility issues related to high prolactin levels
  • Menstrual disorders: Normalises irregular periods and restores normal ovulatory cycles

Symptoms Addressed:

  • Unwanted breast milk production (galactorrhea)
  • Missed or irregular menstrual periods
  • Male breast enlargement (gynecomastia)
  • Reduced sexual desire and erectile dysfunction
  • Bone loss due to prolonged high prolactin levels

Secondary Uses of Cabergoline

Beyond its primary indication for hyperprolactinemia, cabergoline is sometimes prescribed off-label for Parkinson's disease management. The medication can help with movement difficulties, muscle control issues, and balance problems associated with this neurological condition.

How Does Cabergoline Work?

Cabergoline functions as a potent dopamine D2 receptor agonist with a unique mechanism of action. The medication works by directly stimulating dopamine receptors on lactotroph cells in the pituitary gland, which are responsible for prolactin production. This stimulation effectively inhibits the secretion of the prolactin hormone from the pituitary gland.

The drug's long-acting properties make it particularly effective, with prolactin-lowering effects lasting up to 21 days after a single dose in some patients. Unlike other treatments, cabergoline's selective action on D2 receptors provides targeted therapy with minimal interference with other hormone systems.

Cabergoline Dosage

Proper dosing of the cabergoline tablet is crucial for achieving optimal therapeutic outcomes while minimising side effects. The medication'should always be taken exactly as prescribed by your healthcare provider.

Typical Dosage Instructions:

Age Group Recommended Dosage
Adults Start with 0.25 mg twice a week. The dose may be increased every 4 weeks based on prolactin levels, up to a maximum of 1 mg twice a week.
Children Dosage and use must be determined by a healthcare professional.

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How to Use

  • Dosage:Take orally, with or without food, typically twice a week as prescribed by your doctor.
  • Adjustments:Dose depends on your medical condition and treatment response.
  • Regular intake:Take the medication consistently, and mark your calendar to help remember the doses.

What Should I Do If I Miss a Dose?

If you miss a dose of cabergoline, take it as soon as you remember. However, if it's almost time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Never take a double dose to make up for a missed one, as this can increase the risk of side effects.

What Happens if an Overdose?

Symptoms of Overdose:

  • Extreme dizziness and fainting
  • Severe nausea and vomiting
  • Mental changes, including hallucinations
  • Severe low blood pressure
  • Racing heartbeat

What to Avoid: If overdose is suspected, contact poison control immediately or seek emergency medical attention. Do not attempt to treat overdose symptoms at home, and avoid driving or operating machinery if experiencing severe dizziness.

Note

  • Do not share:This medication is prescribed specifically for you.
  • Regular monitoring:Laboratory tests (e.g., prolactin levels, EKG) may be conducted to monitor your progress and check for side effects.

What is the difference between Cabergoline 0.25 mg and 0.5 mg tablets?

Feature Cabergoline 0.25 mg Cabergoline 0.5 mg
Strength 0.25 mg 0.5 mg
Common Use Starting dose, dose titration Maintenance, higher dose needs
Dose Flexibility High (easy to adjust doses) Lower (fixed double dose)
Pill Burden (for higher doses) More tablets per week Fewer tablets per week

What are the Side Effects of Cabergoline?

While cabergoline tab is generally well-tolerated, understanding potential side effects helps ensure safe usage. Most side effects are mild and tend to improve as your body adjusts to the medication.

Common Side Effects

  • Nausea (affects up to 27% of patients)
  • Headache (26% of patients)
  • Dizziness (15% of patients)
  • Constipation
  • Fatigue and weakness
  • Abdominal discomfort
  • Breast pain during initial treatment

Serious but Rare Side Effects

  • Heart valve problems with symptoms like chest pain and breathing difficulties
  • Tissue scarring (fibrosis) in organs, including the heart, lungs, or kidneys
  • Severe allergic reactions
  • Unusual compulsive behaviours (gambling, shopping, increased sexual urges)
  • Severe low blood pressure when standing

Important: Contact your doctor immediately if you experience a persistent cough, chest pain, swelling in your extremities, or any signs of heart problems. Regular monitoring through echocardiograms may be recommended for individuals who use the device on a long-term basis.

Precautions and Warnings

Understanding who should avoid cabergoline and taking necessary precautions ensures safe treatment outcomes. Certain medical conditions require special consideration before starting this medication.

Who Should Avoid This Medicine

  • Patients with uncontrolled high blood pressure
  • Individuals with known allergies to cabergoline or other ergot medications
  • People with severe heart valve disease
  • Patients with active fibrotic disorders

Conditions Where Caution is Needed

  • Liver disease: Dosage adjustments may be necessary
  • Kidney problems: Regular monitoring required
  • History of heart valve problems: Baseline and periodic cardiac evaluations needed
  • Mental health conditions: Particularly bipolar disorder or a history of compulsive behaviours
  • Pregnancy and breastfeeding: Requires careful medical supervision

Are There Any Age Restrictions for Using Cabergoline?

Cabergoline safety and effectiveness in pediatric patients have not been established. The medication is primarily prescribed for adults, and elderly patients may require closer monitoring due to increased sensitivity to side effects, particularly dizziness and blood pressure changes.

Alcohol and Food Interactions

  • Alcohol can increase dizziness and drowsiness
  • Food does not significantly affect absorption, so cabergoline can be taken with or without meals
  • Avoid activities requiring alertness until you know how the medication affects you.

Possible Interactions with Other Medications

Cabergoline can interact with numerous medications, making it essential to inform your healthcare provider about all drugs and supplements you're taking. There are 156 known drug interactions with cabergoline.

Major Drug Interactions

  • Antipsychotic medications: Can counteract cabergoline's effects (haloperidol, chlorpromazine)
  • Anti-nausea drugs: Metoclopramide and promethazine can reduce effectiveness
  • Blood pressure medications: May enhance hypotensive effects
  • Sedating medications: Can increase drowsiness and dizziness

Supplement and Herbal Interactions: Cabergoline may interact with various herbal products and supplements. St. John's Wort, for example, can affect how the medication is metabolised. Always discuss all supplements, vitamins, and herbal products with your healthcare provider before starting treatment.

How Should Cabergoline Be Stored?

Proper storage of cabergoline is essential for maintaining the medication's effectiveness and safety. Following storage guidelines helps ensure the drug remains potent throughout its shelf life.

Recommended Storage Temperature for Cabergoline

Store cabergoline tablets at room temperature between 68°F and 77°F (20°C and 25°C). The medication can tolerate brief temperature excursions between 59°F and 86°F (15°C and 30°C) during transport, but should be returned to proper storage conditions promptly.

Storage Requirements

  • Keep in the original container with a tight closure
  • Protect from light, heat, and moisture
  • Do not store in bathrooms or other humid areas
  • Keep desiccant packets in bottle caps (do not remove)
  • Store away from direct sunlight

What Happens If Cabergoline Is Not Stored Properly?

Improper storage can lead to medication degradation, reducing effectiveness and potentially creating harmful breakdown products. Exposure to excessive heat, moisture, or light can compromise the stability of the drug's chemical properties. Always check expiration dates and discard any medication that has been stored improperly or appears discoloured or damaged.

Safety Measures

  • Keep away from children and pets - use child-resistant containers
  • Never share medication with others
  • Dispose of expired or unused medication through proper pharmaceutical disposal programs
  • Contact your pharmacist for guidance on safe disposal methods.

Cabergoline vs Bromocriptine

Cabergoline Bromocriptine
Formula: C26H37N5O2
Molecular Weight: 451.6 g/mol
Formula: C32H40BrN5O5
Molecular Weight: 654.6 g/mol
Elimination half-life: 63-69 hours (estimated) Elimination half-life: 12-14 hours
Cabergoline is an ergot derivative used to treat medical conditions associated with high levels of prolactin, such as prolactinomas or menstrual disorders. Bromocriptine is an ergoline derivative used in treating hyperprolactinemia, Parkinson's disease, pituitary tumors, neuroleptic malignant syndrome, and as an adjunct in type 2 diabetes.
Common side effects:
  • Nausea/Vomiting
  • Headache/Migraine
  • Dizziness/Vertigo
  • Drop in blood pressure (often asymptomatic)
Common side effects:
  • Nausea
  • Headache
  • Dizziness
  • Fatigue
  • Constipation

References

Cabergoline | Drugs | Springer
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Frequently Asked Questions

Cabergoline is used to treat hyperprolactinemia, a condition with high prolactin levels causing symptoms like infertility, sexual issues, and bone loss in non-breastfeeding women and men. It also treats prolactinomas and may be used for Parkinson’s disease.

Cabergoline starts lowering prolactin levels within 3 hours, with effects lasting 7–28 days in healthy volunteers and hyperprolactinemic patients, or 14–21 days in puerperal women.

Cabergoline reaches peak plasma levels within 2–3 hours after a single oral dose of 0.5–1.5 mg, but clinical effects may take longer to manifest.

Stopping Cabergoline suddenly can cause prolactin levels to remain high, potentially disrupting ovulation, menstrual cycles, and breast milk production in women, and causing sexual or reproductive issues in men.

Cabergoline is not primarily an antidepressant but has antidepressant-like properties by acting as a dopamine receptor agonist and enhancing brain-derived neurotrophic factor signaling.

Cabergoline is a dopamine receptor agonist used to treat hyperprolactinemia by reducing excess prolactin hormone levels in the blood, not a hormone drug itself.

Some research indicates that cabergoline administration can normalize androgen levels and boost menstrual irregularity in PCOS women. They conclude that cabergoline may play a useful role in treating menstrual abnormalities in PCOS patients by reducing prolactin secretion (30-31).

Cabergoline 0.5 mg tablet is used to treat hyperprolactinemia, a condition where excess prolactin causes hormonal imbalance. It is also effective in managing prolactinomas and restoring fertility.

Cabergoline 0.25 mg is typically used to initiate therapy, especially in sensitive individuals. The 0.5 mg dose is used for maintenance once tolerance and response are established.

When taken under medical supervision with periodic monitoring, cabergoline tablets can be safely used long-term, especially in treating chronic conditions like prolactinomas.


Disclaimer: The information provided is accurate and up-to-date to the best of our knowledge. However, it should not be considered a substitute for medical advice or consultation. We do not guarantee its completeness or accuracy. The absence of specific warnings does not mean a medicine is safe for all users. We are not responsible for any outcomes based on this information and strongly recommend consulting a doctor for any medical concerns or questions.

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