Cabergoline

What is Cabergoline?

• Cabergoline (Dostinex) is a dopamine receptor agonist used to treat hyperprolactinemia.
• Cabergoline is also used in the treatment of Parkinson's disease.

Cabergoline

What are the uses of this medicine?

• Cabergoline (Dostinex) is used for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

How does this medicine work?

• A synthetic ergoline derivative and a long-acting dopamine receptor agonist with high affinity for the dopamine D2 receptor.
• The secretion of prolactin by the anterior pituitary is mainly under hypothalamic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons.
• Cabergoline exerts an inhibitory effect on prolactin secretion by acting on dopamine receptors present in pituitary lactotrophs.
• This drug also binds to dopamine D2 receptors in the corpus striatum, thereby mimicking the actions of dopamine on motor control.
• Cabergoline also possesses antioxidant and neuroprotective properties due to its free radical scavenging activity.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Uncontrolled hypertension or known hypersensitivity to ergot derivatives.
• History of cardiac valvular disorders.
• History of pulmonary, pericardial, or retroperitoneal fibrotic disorders.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antihistamines
• ergot medications such as dihydroergotamine (D.H.E. 45, Migranal), ergotamine (in Cafergot, in Ergomar), and methylergonovine (Methergine)
• haloperidol (Haldol)
• levodopa (in Parcopa, Sinemet, and Stalevo)
• medications for high blood pressure, mental illness, or nausea
• metoclopramide (Reglan)
• thiothixene (Navane)

Is this medicine FDA approved?

• Cabergoline was patented in 1980 and approved for medical use in 1993.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of cabergoline tablets for initiation of therapy is 0.25 mg twice a week. Dosage may be increased by 0.25 mg twice weekly up to a dosage of 1 mg twice a week according to the patient's serum prolactin level.
• After a normal serum prolactin level has been maintained for 6 months, cabergoline may be discontinued, with periodic monitoring of the serum prolactin level to determine whether or when treatment with cabergoline should be reinstituted.
• The durability of efficacy beyond 24 months of therapy with cabergoline has not been established.

Administration:

• Cabergoline comes as a tablet to take by mouth.
• It is usually taken with or without food two times a week.
• Your doctor will probably start you on a low dose of cabergoline and gradually increase your dose, not more often than once every 4 weeks.
• Do not stop taking cabergoline without talking to your doctor.
• Your doctor will probably decrease your dose gradually.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Cabergoline tablets, for oral administration, contain 0.5 mg of cabergoline

This medicine is available in fallowing brand namesː

• Dostinex

What side effects can this medication cause?

The most common side effects of this medicine include:

• Nausea
• Constipation
• Abdominal pain
• Dyspepsia
• Vomiting
• Headache
• Dizziness
• Paresthesia
• Vertigo
• Asthenia
• Fatigue
• Hot flashes
• Somnolence
• Depression
• Nervousness
• Postural hypotension
• Breast pain
• Dysmenorrhea
• Vision
• Abnormal vision

Less common side effects may include:

• Cardiovascular System: hypotension, syncope, palpitations
• Digestive System: dry mouth, flatulence, diarrhea, anorexia
• Metabolic and Nutritional System: weight loss, weight gain
• Nervous System: somnolence, nervousness, paresthesia, insomnia, anxiety
• Respiratory System: nasal stuffiness, epistaxis
• Skin and Appendages: acne, pruritus
• Special Senses: abnormal vision
• Urogenital System: dysmenorrhea, increased libido

What special precautions should I follow?

• All patients should undergo a cardiovascular evaluation, including echocardiogram to assess the potential presence of valvular disease. If valvular disease is detected, the patient should not be treated with cabergoline.
• Initial doses higher than 1.0 mg may produce orthostatic hypotension. Care should be exercised when administering cabergoline with other medications known to lower blood pressure.
• Cabergoline is not indicated for the inhibition or suppression of physiologic lactation. Use of bromocriptine, another dopamine agonist for this purpose, has been associated with cases of hypertension, stroke, and seizures.
• Since cabergoline is extensively metabolized by the liver, caution should be used, and careful monitoring exercised, when administering cabergoline to patients with hepatic impairment.
• Impulse control/compulsive behaviors, including pathological gambling, increased libido, and hypersexuality have been reported in patients treated with dopamine agonists including cabergoline. Prescribers should consider dose reduction or stopping the medication if a patient develops such urges while taking cabergoline.
• Patients should be instructed to notify their physician if they suspect they are pregnant, become pregnant, or intend to become pregnant during therapy.
• Patients should notify their physician if they develop shortness of breath, persistent cough, difficulty with breathing when lying down, or swelling in their extremities.
• Patients should be alerted to the possibility that patients may experience intense urges to spend money uncontrollably, intense urges to gamble, increased sexual urges, and other intense urges and the inability to control these urges while taking cabergoline. Advise patients to inform their healthcare provider if they develop new or increased uncontrolled spending, gambling urges, sexual urges, or other urges while being treated with cabergoline.
• The prolactin-lowering action of cabergoline suggests that it will interfere with lactation. Due to this interference with lactation, cabergoline should not be given to women postpartum who are breastfeeding or who are planning to breastfeed.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• nasal congestion, syncope, or hallucinations

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Measures to support blood pressure should be taken if necessary.

Can this medicine be used in pregnancy?

• There are, however, no adequate and well-controlled studies in pregnant women.
• Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• Safety and effectiveness of cabergoline in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• CABERGOLINE

Inactive ingredients:

• LEUCINE
• LACTOSE, UNSPECIFIED FORM

Who manufactures and distributes this medicine?

Distributed by:

• Greenstone llc

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 20° to 25°C (68° to 77°F).

• Dailymed label info on Cabergoline
• FDA Cabergoline

Cabergoline Resources
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