Active Substance: Cabergoline
Analogs: Drugs containing bromocriptine (Cycloset, Parlodel)
Drug form: Tablets 0.25, 0.5mg
Other names: Cabergoline (generic Dostinex)
What is Dostinex?
Dostinex is a drug based on the active ingredient cabergoline, belonging to the category of Antiparkinson’s and specifically prolactin inhibitors. This drug belongs to the family of dopaminergic derivatives of ergot rye. It has the property of curbing the cells of the pituitary that secrete the hormone of lactation, prolactin.
Indications
It is used in the treatment of disorders due to an excess of prolactin in the blood (hyperprolactinemia). Dostinex (cabergoline) is thus indicated for the treatment of hyperprolactinemic disorders, as well as idiopathic or consecutive to a pituitary adenoma.
In other cases, Dostinex (cabergoline) is indicated to prevent the onset of physiologic lactation (inhibition of physiological lactation) during postpartum for clearly defined medical reasons. These medical reasons may include the birth of a stillborn baby, neonatal mortality, conditions affecting breastfeeding (cleft lip or cleft palate in babies), serious acute or chronic mental or physical illnesses, or a disease of the mother that can be passed on to the baby with the milk and / or that requires the use of drugs excreted in breast milk. Dostinex is not indicated to inhibit postpartum lactation that is already established.
Dostinex is used for regulating conditions caused by excessive production of prolactin, including erectile problems in males and overweight in both male and female patients.
How Dostinex works
Dostinex prevents physiological lactation through inhibition of prolactin secretion. In controlled clinical trials it was shown that Dostinex, administered as a single dose of 1 mg on the first post-partum day, proved to be effective in preventing prolactin production, as well as reducing congestion and breast pain in 70% to 90% of women. Only a fraction of the patients had recurrent breast symptoms, generally of a minor nature, at the third week after delivery.
The suppression of milk secretion and the improvement of symptoms related to breast congestion and pain following the milk supply are achieved in about 85% of women receiving a total of 1 mg of cabergoline, administered in four divided doses over the arc two days. The return of breast symptoms after 10 days is rare.
Dostinex is prescribed for patients with a number of conditions linked to hyperprolactinaemia such as amenorrhea, oligomenorrhea, anovulation and galactorrhoea. The drug is administered in order to address the following issues: prolactin-secreting pituitary microprolactinoma and prolactin-secreting pituitary macroprolactinoma, idiopathic hyperprolactinemia, and empty saddle syndrome associated with hyperprolactinemia, fundamental diseases in the clinical manifestations mentioned above.
Dostinex administered at doses of 1 – 2 mg weekly as chronic therapy yielded meaningful health results in 84% of trial cases; the trials were made in individuals with hyperprolactinemia. Dostinex effectively restored normal levels of serum prolactin and helped recover regular cycles in 83% of previously amenorrheic women. Based on the monitoring of progesterone levels, determined during the luteal phase, ovulation re-established in 89% of the treated women, the galactorrhea disappeared in 90% of the treated cases. In 50%-90% of men and women alike diagnosed with pituitary adenoma there was a decrease in tumor mass.
Dosage and administration
The starting dose is 0.5 mg per week in a single dose, ie 1 tablet per week. The blood test for the determination of prolactin should be made the day before taking the tablet.
This dosage of 0.5 mg per week should be maintained for 4 weeks and then adapted according to the prolactinemia dosage to be performed the day before taking a tablet. The dosage should be maintained or increased in increments of 0.5 mg as a function of prolactin, measured at most every 4 weeks until an optimal response to treatment is obtained.
After equilibration of the dosage, a quarterly dose of prolactin is sufficient. Most patients are controlled by a dose less than or equal to 1 mg / week. In this case, a single weekly catch is sufficient. The dosage can range from 0.25 to 2 mg or even up to 4.5 mg per week. When the dosage exceeds 1 mg, it is recommended to split the weekly dose into two or more doses depending on the patient’s tolerance.
To improve tolerance, the medication should be given in the middle of the meal, preferably in the evening, or at bedtime with a light snack.
Storage
Keep this medicine out of the reach and sight of children. Do not store at temperatures above 25 ° C. Keep this medicine in its packaging in order to protect from light.
Do not use after the expiry date which is stated on the package. The expiration date is the last day of the specified month. After expiry date, do not expose of drugs using your garbage bin or the drain. Ask your pharmacist for instructions on how to dispose of the pills that are not going to be used in an environmentally conscious way.
Warnings
Decreases in blood pressure (orthostatic hypotension) are sometimes observed at the beginning of treatment. Blood pressure monitoring is recommended during the first few days of treatment. Before starting long-term treatment, your doctor may need to assess how well your lungs, kidneys, and heart work. Regular medical supervision, including an echocardiogram, is required during treatment.
If you experience pain in the abdomen, an unexplained respiratory difficulty, or a persistent urge to cough during treatment, seek prompt medical attention.
Precautions are necessary in cases of severe hepatic insufficiency, a history of mental disorders (confusion, hallucinations) and cardiovascular diseases (arteritis, angina pectoris, Raynaud’s disease).
Tell your doctor if you feel drowsy during the day: dose adjustment or discontinuation may be necessary.
The dopaminergic drugs expose to a risk of compulsive or repetitive behavior disorders: pathological gambling, compulsive spending, bulimia, significant increase in libido. In case of such disorders, do not hesitate to talk to your doctor without shame or guilt. A change in treatment should be considered.
This drug can restore fertility in infertile women by excess prolactin. If pregnancy is not desired, contraception is necessary. The pill cannot be used because it is contraindicated in cases of prolactin excess.
This medication may be responsible for dizziness or decreased alertness during driving or operating machinery.
In addition, dopaminergic drugs may, in rare cases, cause sudden drowsiness during the day without warning signs. Driving and using dangerous machines are not recommended during treatment. They are contraindicated in people who have had an urge to sleep under treatment.
This drug should not be associated with neuroleptics: risk of cancellation of their effects.
It can also interact with antibiotics of the macrolide family and with vasoconstrictors, particularly those derived from ergot of rye.
Pregnancy:
The effect of this medicine during pregnancy is poorly known: only your doctor can evaluate the possible risk of its use in your case.
Breastfeeding:
This medicine blocks lactation.
Hyperprolactinemia results in variable symptoms: absence of menstruation, disorders of the cycle, infertility in women; decreased libido, impotence and, more rarely, increased breast volume in humans. The doctor looks for the cause before starting treatment.
