Caberlin 0.5 Mg (Cabergoline)

About

Cabergoline is an ergot-derived drug that is used to treat Prolactinoma, Cushing’s disease and other pituitary adenomas. It is a dopamine receptor agonist on D₂ receptors. Due to its inhibitory effect on prolactin cells, it is successfully used to treat disorders of increased prolactin levels. Since its inception in 1981 it has replaced bromocriptine as the first-line drug in the treatment of Prolactinoma due to less severe side effects and higher affinity for dopamine D₂ receptors.

Classification and mechanism of action

Prolactin is released by the anterior pituitary gland under the influence of dopamine. Cabergoline is a dopamine receptor agonist on D₂ receptors, although it also has a lower affinity for dopamine D₁, 5HT1 and 5HT2 serotonin, α1 and α2- adrenergic agonist. Cabergoline has also an inhibitory effect on pituitary lactotroph cells that release prolactin. In this way, they reduce the secretion of prolactin and help to shrink a Prolactinoma.

Looking after Caberlin 0.5 Mg

• Cabergoline should be stored at room temperature of 20-25 ^oC or 68-77 ^oF.
• Store in a cool, dry place, away from the reach of children and pets.

How to take Caberlin 0.5 Mg

Cabergoline should be taken by mouth with water twice a week, or as suggested by your doctor. It is advised to mark on your calendar when you have to take the medicine so you do not forget it and notice if the symptoms improved, persisted or got worse.

Dosage

Cabergoline is given orally 0.25 mg twice a week as starting dose. If the prolactin levels are really high, or if despite the starting dose the symptoms did not improve, the dose can be increased to up to 1-2 mg twice a week. It is advised to check cardiac activity and do echocardiography before initiating the dose and continue that periodically once the treatment is going on for a long term. There are no food interactions; you can take it with or without food.

Overdose

Contact your emergency if you develop symptoms like nasal congestion, fainting, hallucination and loss of consciousness.

Missed Dose

If you miss a dose of Cabergoline take the missed pill right away, but if it is just about the time to take your next dose then take the scheduled dose instead and skip the missed dose. Do not take double doses. Inform your doctor for further suggestion.

Warnings and precautions
Care should be advised to patients if:

• A dose of more than 1 mg is given as Cabergoline can cause dizziness and drowsiness
• The mother is lactating or planning to nurse
• The patient is a child, the lowest possible dose is given
• The patient is on other antihypertensive drugs
• The patient has Raynaud’s disease, gastroduodenal ulcer, hypotension or gastrointestinal bleeding.
• Because Cabergoline is extensively metabolized in the liver, it should be cautiously given to patients who have hepatic impairment
• Patients should undergo periodic cardiac assessments for valvulopathy by echocardiography.

When Caberlin 0.5 Mg should not be used

Cabergoline is contraindicated in patients who have:

• Uncontrolled hypertension
• Patients who are allergic to ergot-derived drugs (ergotamine)
• Women planning pregnancy
• Severe hepatic impairment
• Severe pre-eclampsia
• Known history of fibrotic disorders or valvular heart diseases
• You have taken or will be taking a sumatriptan within 24 hours of taking Cabergoline
• Concomitantly taking haloperidol, metoclopramide, chlorpromazine, or any thioxanthene.

How long should you take Caberlin 0.5 Mg?

Cabergoline should be taken for as long as your doctor has prescribed, increasing the dose if required after every 4 weeks. Once the prolactin levels have been maintained for 6 months the drug can be discontinued, with regular monitoring of prolactin levels to see if the treatment needs to be restarted. If, despite increased dosage no improvement in symptoms is seen, the lowest dose of the drug should be given that gives therapeutic results and other management options should be considered.

Possible side effects
More common

• Nausea
• Headache
• Dizziness
• Constipation

Less common

• Asthenia
• Fatigue
• Somnolence
• Dyspepsia
• Abdominal pain
• Depression
• Postural hypotension
• Paresthesia, numbness, tingling or pins and needles sensation
• Breast tenderness
• Dysmenorrheal
• Hot flushes
• Nervousness
• Abnormal vision

Rare

• Epistaxis
• Increased libido
• Difficulty concentrating