Dostinex (Cabergoline)
Dopamine Agonist for Hyperprolactinaemia and Lactation Inhibition
Quick Facts About Dostinex
Key Takeaways About Dostinex
- Highly effective prolactin suppression: Cabergoline is the most potent dopamine agonist for reducing prolactin levels, with normalisation achieved in up to 90% of patients with prolactinomas
- Convenient weekly dosing: Its long half-life (63–69 hours) allows once- or twice-weekly dosing, improving adherence compared to daily alternatives
- Cardiac monitoring required: Long-term use necessitates echocardiographic surveillance due to the risk of fibrotic cardiac valve disease
- Take with food: Dostinex should be taken with meals to reduce gastrointestinal side effects such as nausea, vomiting, and abdominal pain
- Impulse control warning: Some patients may experience compulsive behaviours including pathological gambling, hypersexuality, or binge eating – report these to your doctor immediately
What Is Dostinex and What Is It Used For?
Dostinex (cabergoline) is a dopamine agonist that reduces blood levels of the hormone prolactin. It is primarily used to treat hyperprolactinaemia (excess prolactin) and to inhibit or suppress breast milk production when this is medically necessary. By stimulating dopamine D2 receptors in the pituitary gland, Dostinex directly suppresses prolactin secretion.
Prolactin is a hormone produced by the anterior pituitary gland, a small structure at the base of the brain. Under normal circumstances, prolactin plays a central role in stimulating breast milk production after childbirth. However, when prolactin levels become abnormally elevated outside of pregnancy and breastfeeding – a condition known as hyperprolactinaemia – it can cause a wide range of symptoms and health problems.
In women, hyperprolactinaemia may lead to irregular or absent menstrual periods (amenorrhoea), unwanted breast milk production (galactorrhoea), reduced fertility, and decreased bone density over time. In men, elevated prolactin can cause decreased libido, erectile dysfunction, gynaecomastia (breast tissue enlargement), and in some cases, infertility. Both sexes may experience headaches and visual disturbances if the underlying cause is a prolactin-secreting pituitary tumour (prolactinoma).
Cabergoline, the active ingredient in Dostinex, is an ergot-derived compound that acts as a potent and selective agonist at dopamine D2 receptors. Because dopamine is the primary physiological inhibitor of prolactin secretion, stimulating these receptors directly suppresses the release of prolactin from the pituitary lactotroph cells. This makes cabergoline one of the most effective medications available for reducing prolactin levels, with studies demonstrating normalisation of prolactin in approximately 85–90% of patients with microprolactinomas and 70–80% of patients with macroprolactinomas.
Dostinex is also used for lactation inhibition – stopping breast milk production shortly after delivery when breastfeeding is contraindicated or not desired for medical reasons. A single dose can effectively prevent the onset of lactation. Additionally, Dostinex can be used to suppress established lactation when breastfeeding has already begun but needs to be stopped due to medical circumstances such as maternal illness, medication use that is incompatible with breastfeeding, or other clinical indications.
Cabergoline was first approved for clinical use in the 1990s and has since become the first-line medical treatment for prolactinomas according to the Endocrine Society Clinical Practice Guidelines (2011, updated 2023). Compared to older dopamine agonists such as bromocriptine, cabergoline offers superior efficacy, better tolerability, and more convenient dosing.
What Should You Know Before Taking Dostinex?
Before starting Dostinex, your doctor must assess your medical history, particularly for fibrotic disorders, cardiovascular disease, and psychiatric conditions. Dostinex is contraindicated in patients with a history of cardiac valvular disease, pulmonary or retroperitoneal fibrosis, pre-eclampsia, and severe hepatic impairment.
Contraindications
You should not take Dostinex if any of the following apply to you:
- Allergy to cabergoline or other ergot alkaloids – if you have ever experienced an allergic reaction to cabergoline or to any ergot-derived medication, you must not take Dostinex
- History of fibrotic disorders – if you have or have previously had fibrotic reactions (scar tissue formation) affecting the heart, lungs, or abdomen, including cardiac valvular fibrosis, pulmonary fibrosis, or retroperitoneal fibrosis
- Severe psychiatric disorders – a history of or current severe psychotic disorder, as cabergoline may exacerbate psychiatric symptoms
- Pre-eclampsia or postpartum hypertension – Dostinex must not be used in women who have had pregnancy-induced high blood pressure (pre-eclampsia/eclampsia) or who develop high blood pressure after delivery
- Severe hepatic impairment – as the liver is the primary site of cabergoline metabolism, significant liver disease can lead to dangerously elevated drug levels
Warnings and Precautions
Talk to your doctor or pharmacist before taking Dostinex if you have or have had any of the following conditions:
- Cardiovascular disease – including heart failure, coronary artery disease, or Raynaud's phenomenon. Dostinex can cause a blood-pressure-lowering effect, particularly during the first few days of treatment, which may exacerbate cardiovascular symptoms
- Peptic ulcer disease or gastrointestinal bleeding – cabergoline may worsen gastrointestinal conditions. If you have a history of stomach ulcers, your doctor should carefully weigh the benefits and risks
- Kidney disease – while cabergoline is primarily eliminated through the liver, impaired renal function may affect drug clearance and require dose adjustment
- Raynaud's disease – cabergoline, as an ergot derivative, can potentially exacerbate vasospastic symptoms in patients with Raynaud's phenomenon
If you have recently given birth, you may be at increased risk of certain serious medical problems when taking Dostinex. These include high blood pressure, heart attack, seizures, stroke, and psychiatric disturbances. Your doctor must monitor your blood pressure regularly during and after treatment. Contact your doctor immediately if you experience high blood pressure, chest pain, or unusually severe or persistent headache (with or without vision problems).
Impulse Control Disorders
Dopamine agonists, including cabergoline, have been associated with impulse control disorders (ICDs). These are behavioural changes where patients develop an inability to resist the urge to perform actions that may be harmful to themselves or others. Reported impulse control disorders include:
- Pathological gambling – compulsive gambling despite serious personal or financial consequences
- Hypersexuality – abnormally increased sexual drive or thoughts that cause distress
- Compulsive spending – an uncontrollable urge to buy things and spend money
- Binge eating – consuming large quantities of food in a short period, or eating more than normally needed
Tell your doctor if you or your family members notice the development of any unusual compulsive behaviours. Your doctor may need to adjust your dose or discontinue treatment. These behaviours typically resolve once the dose is reduced or the medication is stopped.
Cardiac Valve Monitoring
Long-term use of cabergoline has been associated with fibrotic changes affecting the heart valves. This is a class effect of ergot-derived dopamine agonists. Before starting long-term Dostinex therapy, your doctor should:
- Perform a baseline echocardiogram (heart ultrasound) to assess the heart, lungs, and kidneys
- Conduct regular follow-up echocardiograms at intervals determined by clinical judgement (typically every 6–12 months)
- Monitor for early symptoms of fibrosis, including shortness of breath, chest or back pain, and swollen legs
If echocardiographic evidence of valvular fibrosis is detected, treatment with Dostinex will be discontinued. The Endocrine Society recommends that the risk of cardiac valve disease be weighed against the benefits of prolactin normalisation, particularly at doses below 2 mg per week where the risk is considered lower.
Pregnancy and Breastfeeding
The effects of Dostinex on the human foetus are not fully established. If you are pregnant or suspect you may be pregnant, you should inform your doctor immediately. In most cases, Dostinex should be discontinued upon confirmation of pregnancy, unless there is a compelling medical reason to continue (such as a large or growing macroprolactinoma threatening the optic chiasm).
Women of childbearing potential should use effective contraception during treatment with Dostinex and for at least one month after the last dose. It is important to note that Dostinex can restore fertility in women with prolactin-related infertility. Therefore, women who do not wish to become pregnant should be advised to use reliable contraception throughout treatment.
It is unknown whether cabergoline passes into breast milk. Because Dostinex suppresses lactation, you should not breastfeed while taking this medication.
Driving and Operating Machinery
Dostinex can impair your ability to react, which should be taken into account when alertness is required, such as when driving or operating precision machinery. Cabergoline may cause somnolence (excessive drowsiness) and sudden onset of sleep without warning. Patients who experience these effects should not drive or engage in activities where impaired alertness could be dangerous. If you experience drowsiness or sudden sleep episodes, consult your doctor immediately.
How Does Dostinex Interact with Other Drugs?
Dostinex can interact with antipsychotic medications, antiemetics, certain antibiotics, and other ergot alkaloids. Drugs that block dopamine receptors (dopamine antagonists) may reduce the effectiveness of Dostinex, while concurrent use of other ergot derivatives increases the risk of ergotism and fibrosis.
Cabergoline exerts its therapeutic effect by stimulating dopamine D2 receptors. Therefore, medications that block dopamine receptors can directly antagonise the effects of Dostinex, reducing its ability to lower prolactin levels. Conversely, combining Dostinex with other ergot-derived medications or drugs that increase serotonergic activity can increase the risk of serious adverse effects including vasoconstriction, fibrosis, and serotonin syndrome.
It is essential that you inform your doctor about all medications you are currently taking, including prescription drugs, over-the-counter medicines, and herbal supplements. The following tables summarise the most clinically important drug interactions with Dostinex.
Major Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Haloperidol | Antipsychotic (D2 antagonist) | Blocks dopamine D2 receptors, directly opposing the prolactin-lowering action of cabergoline | Avoid combination; alternative antipsychotic strategies should be considered |
| Chlorpromazine | Antipsychotic (phenothiazine) | Potent dopamine receptor blockade reduces cabergoline efficacy | Avoid combination; discuss alternative treatment options with your doctor |
| Other ergot alkaloids | Ergot derivatives (e.g., ergotamine, dihydroergotamine) | Additive risk of ergotism (vasoconstriction), fibrosis, and cardiovascular toxicity | Contraindicated; do not use cabergoline with other ergot derivatives |
| Metoclopramide | Antiemetic (D2 antagonist) | Antagonises the dopaminergic effect of cabergoline, reducing prolactin suppression | Avoid combination; use alternative antiemetics such as ondansetron if needed |
Moderate Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Domperidone | Antiemetic / prokinetic | Peripheral dopamine D2 antagonist that may partly reduce cabergoline's effects on prolactin | Use with caution; monitor prolactin levels if co-administered |
| Erythromycin / Clarithromycin | Macrolide antibiotics | May increase cabergoline plasma levels through CYP3A4 inhibition, though cabergoline is primarily metabolised by hydrolysis | Monitor for increased side effects during concurrent use |
| Antihypertensive medications | Blood pressure-lowering drugs | Additive hypotensive effect, particularly during the first days of cabergoline therapy | Monitor blood pressure closely; dose adjustment of antihypertensives may be needed |
| Risperidone / Olanzapine | Atypical antipsychotics | May partially antagonise cabergoline via D2 receptor blockade, though to a lesser degree than typical antipsychotics | Monitor prolactin levels; consult specialist if both drugs are necessary |
While there is no specific pharmacokinetic interaction between cabergoline and alcohol, both substances can lower blood pressure and cause drowsiness. Drinking alcohol while taking Dostinex may increase the risk of dizziness, light-headedness, and fainting, particularly when standing up. It is advisable to limit alcohol consumption during treatment.
What Is the Correct Dosage of Dostinex?
The dosage of Dostinex depends on the indication. For lactation inhibition, a single dose of 1 mg (two tablets) is taken within 24 hours of delivery. For hyperprolactinaemia, the starting dose is typically 0.5 mg per week, which may be gradually increased based on prolactin response. Always take Dostinex with food.
Dostinex should always be taken exactly as prescribed by your doctor. The tablets should be taken with a meal to reduce the risk of gastrointestinal side effects such as nausea, vomiting, and abdominal pain. Do not exceed the prescribed dose without consulting your doctor.
Lactation Inhibition (Prevention)
Preventing breast milk production after delivery
The standard dose is 1 mg (two 0.5 mg tablets) taken as a single dose within 24 hours of delivery. This single dose is usually sufficient to prevent the onset of lactation. No further doses are typically required.
Lactation Suppression (Already Established)
Stopping breast milk production after breastfeeding has begun
The recommended dose is 0.25 mg (half a 0.5 mg tablet) taken every 12 hours for two days, giving a total dose of 1 mg. This dose should not be exceeded for this indication.
Hyperprolactinaemia (Elevated Prolactin)
Long-term treatment for excess prolactin
The initial recommended dose is 0.5 mg per week, administered as a single weekly dose or divided into two doses (e.g., 0.25 mg on Monday and Thursday). Your doctor will check your prolactin levels regularly and may gradually increase the dose in increments of 0.5 mg per week at monthly intervals until optimal prolactin suppression is achieved. The usual therapeutic dose ranges from 0.25 mg to 2 mg per week, although some patients may require higher doses. The maximum dose should not normally exceed 4.5 mg per week.
| Indication | Dose | Frequency | Duration |
|---|---|---|---|
| Lactation inhibition | 1 mg (2 tablets) | Single dose | One-off |
| Lactation suppression | 0.25 mg (half tablet) | Every 12 hours | 2 days |
| Hyperprolactinaemia (initial) | 0.5 mg | Once weekly | Ongoing (with monitoring) |
| Hyperprolactinaemia (maintenance) | 0.25–2 mg | Weekly (1–2 doses) | Long-term |
Missed Dose
If you forget to take a dose of Dostinex, take it as soon as you remember unless it is almost time for your next scheduled dose. In that case, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a forgotten one. If you are unsure about what to do, contact your doctor or pharmacist for advice.
Overdose
If you take more Dostinex than prescribed, or if someone else accidentally takes your medication, contact your doctor, go to the nearest emergency department, or call your local poison control centre immediately. Symptoms of overdose may include severe nausea, vomiting, abdominal pain, a significant drop in blood pressure (hypotension), confusion, psychosis, or hallucinations. Overdose requires prompt medical attention as supportive care may be needed to stabilise blood pressure and manage symptoms.
What Are the Side Effects of Dostinex?
Like all medicines, Dostinex can cause side effects, but not everybody gets them. The most common side effects include dizziness, headache, nausea, and fatigue. When used for lactation inhibition (short-term), about 14% of patients experience some form of side effect. With long-term use for hyperprolactinaemia, side effects are more common (affecting approximately 70% of patients) but typically diminish within the first two weeks.
The likelihood and severity of side effects depend on the dose and duration of treatment. Short-term use for lactation inhibition is generally well tolerated, while long-term therapy for hyperprolactinaemia carries a higher risk of side effects, particularly at higher doses. It is important to report any new or worsening symptoms to your doctor, who can adjust your treatment plan accordingly.
Very Common
- Dizziness and vertigo
- Headache
- Nausea
- Dyspepsia (indigestion)
- Abdominal pain
- Gastritis (inflammation of the stomach lining)
- Fatigue and asthenia (weakness)
- Cardiac valve changes and related disorders (e.g., pericarditis, pericardial effusion) – with long-term use
Common
- Somnolence (excessive drowsiness)
- Hypotension (low blood pressure), particularly orthostatic (on standing)
- Depression and depressed mood
- Vomiting
- Constipation
- Hot flushes
- Breast pain
Uncommon
- Visual disturbances
- Epistaxis (nosebleed)
- Dyspnoea (difficulty breathing)
- Pulmonary fibrosis (scar tissue in the lungs)
- Pleural effusion (fluid around the lungs)
- Increased libido
- Syncope (fainting)
- Paraesthesia (tingling or prickling sensation)
- Palpitations
- Muscle cramps (fingers and calves)
- Raynaud's phenomenon (cold, pale fingers and toes)
- Peripheral oedema (swelling of legs, feet, or fingers)
- Hair loss (alopecia)
- Skin rash
- Decreased haemoglobin values in women with amenorrhoea during the first months after menstruation resumes
Rare / Frequency Not Known
- Allergic reactions
- Aggression
- Delusions and psychotic disorder
- Liver function abnormalities
- Respiratory failure
- Pleuritis (inflammation of the lung lining)
- Chest pain and angina
- Sudden sleep onset (sleep attacks)
- Tremor
- Impulse control disorders (pathological gambling, hypersexuality, compulsive spending, binge eating)
Difficulty breathing, shortness of breath, chest pain, back pain, or swollen legs – these may be early signs of cardiac valve disease, pericarditis, pericardial effusion, or pulmonary fibrosis. These conditions require prompt medical evaluation and may necessitate discontinuation of Dostinex.
How Should You Store Dostinex?
Store Dostinex at or below 25°C (77°F), in a dry place, out of the sight and reach of children. Do not use the tablets after the expiry date printed on the packaging.
Dostinex tablets should be stored in their original container to protect them from moisture and light. The expiry date refers to the last day of the stated month. Once the expiry date has passed, do not take the medication, even if the tablets appear unchanged.
Do not dispose of Dostinex via household waste or by flushing down the toilet. Return any unused or expired tablets to your pharmacist for safe disposal. Proper medication disposal helps protect the environment and prevents accidental ingestion by others.
What Does Dostinex Contain?
Each Dostinex tablet contains 0.5 mg of cabergoline as the active substance. The inactive ingredients (excipients) are lactose (75.9 mg per tablet) and leucine.
Dostinex 0.5 mg tablets are white, flat, oblong-shaped tablets with a score line on one side to allow easy splitting for half-dose administration. The tablets are available in glass or plastic containers containing either 2 or 8 tablets. Not all pack sizes may be available in every market.
Dostinex contains lactose (75.9 mg per tablet). If you have been told by your doctor that you have an intolerance to some sugars, including lactose, contact your doctor before taking this medicine. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption should not take Dostinex.
Dostinex is manufactured by Pfizer, a multinational pharmaceutical company. The medication is distributed and available in numerous countries worldwide under the brand name Dostinex. Generic cabergoline formulations are also available from other manufacturers, containing the same active ingredient in equivalent doses.
Frequently Asked Questions About Dostinex
Dostinex (cabergoline) is a dopamine agonist used primarily to treat hyperprolactinaemia – a condition where the body produces abnormally high levels of the hormone prolactin. This can be caused by a prolactin-secreting pituitary tumour (prolactinoma) or other conditions. Dostinex is also used to inhibit or suppress breast milk production (lactation) when breastfeeding needs to be stopped for medical reasons. By stimulating dopamine D2 receptors in the pituitary gland, Dostinex effectively reduces prolactin secretion.
For lactation inhibition (when taken within 24 hours of delivery), Dostinex typically prevents breast milk production within 24 to 48 hours. For suppression of established lactation (when breastfeeding has already started), the 2-day course usually reduces milk production significantly within 2 to 3 days, with complete suppression occurring within about one week. The prolactin-lowering effect of a single dose can persist for up to 2 to 3 weeks due to cabergoline's long half-life.
Yes, Dostinex can restore fertility in patients whose infertility is caused by hyperprolactinaemia. Elevated prolactin levels can disrupt ovulation in women and reduce sperm production and testosterone levels in men. By normalising prolactin levels, Dostinex can restore normal menstrual cycles and ovulation in women, and improve fertility parameters in men. For this reason, women of childbearing potential who do not wish to become pregnant should use effective contraception during treatment with Dostinex.
The duration of Dostinex treatment for hyperprolactinaemia varies depending on the underlying cause and individual response. Many patients require long-term treatment, often for several years. Current Endocrine Society guidelines suggest that withdrawal of cabergoline may be considered after at least 2 years of treatment, provided that prolactin levels have been normal for at least 2 years and any prolactinoma has significantly shrunk. If prolactin levels rise again after discontinuation, treatment may need to be restarted. Your doctor will guide you on the appropriate duration based on your specific situation.
Clinical studies and systematic reviews have shown that cabergoline (Dostinex) is generally superior to bromocriptine for the treatment of hyperprolactinaemia. Cabergoline achieves prolactin normalisation in a higher percentage of patients (approximately 85–90% vs. 60–80% for bromocriptine), is better tolerated with fewer gastrointestinal side effects, and requires less frequent dosing (once or twice weekly vs. two or three times daily). For these reasons, the Endocrine Society Clinical Practice Guidelines recommend cabergoline as the first-line dopamine agonist for most patients with prolactinomas.
Cabergoline belongs to the ergot-derived class of dopamine agonists, which have been associated with fibrotic changes in the heart valves (cardiac valvulopathy). This is thought to occur through stimulation of serotonin 5-HT2B receptors on cardiac valve tissue. Although the risk is dose-dependent and appears to be lower at the doses typically used for hyperprolactinaemia compared to those used in Parkinson's disease, regular echocardiographic monitoring is recommended as a precautionary measure. Your doctor will perform a baseline echocardiogram before starting long-term treatment and repeat it at regular intervals (typically every 6–12 months).
References
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About Our Medical Editorial Team
This article was written and medically reviewed by the iMedic Medical Editorial Team, comprising board-certified specialists in endocrinology, clinical pharmacology, and reproductive medicine. Our team follows the GRADE evidence framework and adheres to guidelines issued by the Endocrine Society, the European Medicines Agency (EMA), the World Health Organization (WHO), and the British National Formulary (BNF).
All medical claims are supported by Level 1A evidence from systematic reviews, randomised controlled trials, and international clinical practice guidelines.
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