Dostinex – cabergoline, a dopaminergic agent, an ergoline derivative. Has a long and pronounced effect of reducing prolactin. Acts due to blockade of prolactin secretion as a result of direct stimulation in lactotrophic cells of the pituitary D2-dopamine receptors. When high doses are used, there is also a central stimulating dopaminergic effect on D2 receptors. This property differs from other prolactin-lowering agents.
Just 3 hours after taking Dostinex in the blood, a decrease in the level of prolactin is observed, which persists for 7 to 28 days in healthy individuals and patients with high prolactin levels. The effect when used in the period of postpartum lactation lasts up to 2-3 weeks. From the digestive tract is absorbed quickly. The maximum plasma concentration is reached in 0,5-4 hours after internal reception of a preparation. The half-life was evaluated by the rate of elimination of cabergoline in the urine – it was 63-68 hours in healthy individuals, 79-115 hours in patients with hyperprolactinaemia. Due to the significant half-life of cabergoline, the equilibrium concentrations of the drug are reached after 28 days. About 41-42% of cabergoline binds plasma proteins.
Indications for use Dostinex:
Indications for the use of the drug Dostinex are:
• In women – treatment of hyperprolactinaemia, which manifests in infertility, a violation of the menstrual cycle (oligomenorrhoea, amenorrhea, anovulatory menstrual cycles), galactorrhea;
• in men – treatment of hyperprolactinaemia, which manifests itself by a decrease in libido or impotence;
• Prolactin-secreting adenoma of the pituitary gland (micro- or macro-prolactinoma);
• Syndrome of an empty Turkish saddle;
• to suppress physiological lactation after childbirth if the woman is unwilling or unable to breastfeed, or if there are contraindications to feeding by the child or the mother;
• to prevent lactation after childbirth in case of abortion or stillbirth.
Method of application:
The preparation Dostinex used for suppression of lactation postpartum
On ½ tablet (0.25 mg) every 12 hours for 2 days.
To prevent lactation
One time on 1 mg in the first day after birth.
In the treatment of hyperprolactinemia
The mode of taking the prescribed dosage is 1-2 times a week on certain days (for example, every Tuesday at the regime of once a week or every Tuesday-Friday at a mode of 2 times a week). First, it is recommended to take lower doses of the drug – 1/2-1 tablet (0.25-0.5 mg) 1 time per week. If necessary, gradually increase the dose, depending on the tolerability and therapeutic response. Dosage regimen: 0.5 mg every month of admission.
The average therapeutic dose of Dostinex is 1 mg / week. Usually, for the treatment of hyperprolactinemia, the maximum dose of the drug is 4.5 mg / week. If a dose of more than 2 mg / week is used, then it is divided into 2 divided doses. As soon as the optimal dosing regimen is selected, it is necessary to once a month to determine the content of prolactin in the blood. On the average, the normalization of prolactin levels is observed after 0.5-1 months of treatment.
Side effects of Dostinex:
Usually the drug is well tolerated. If Dostinex is prescribed to prevent lactation or to suppress it, dizziness, hypotension, insomnia, headache, nausea, and abdominal pain are often observed. These signs are weakly expressed and quickly pass. If the drug is used to treat hyperprolactinaemia, dizziness, headache, nausea, dyspepsia, abdominal pain, gastritis, constipation, general weakness, breast tenderness, depression, hot flushes to the face, hypotension, paresthesia are possible. These signs are weak or moderately expressed and pass quickly. The most common side effects occur within the first 14 days of taking Dostinex.
Adverse effects of Dostinex are additive, so when developing strong effects, it is recommended first to reduce the dosage, then try to increase it again if necessary (by 0.25 mg per week for 2 weeks). If the side effects are severe, which requires withdrawal, the symptoms disappear after 1-2 days.
Contraindications to the use of the drug Dostinex are: liver failure; late gestosis; increased sensitivity to ergot alkaloids, cabergoline or other components of Dostinex; anamnestic indication of postpartum psychosis.
Dostinex is not intended for the treatment of pregnant women. Before prescribing the drug, it is recommended to exclude pregnancy. After the end of taking the drug, adequate contraception is necessary for 1 month, after which it is possible to become pregnant. In the case of inefficiency Dostinex for suppressing lactemia, breastfeeding is discontinued. If there was conception on the background of the drug, Dostinex is canceled.
Interaction with other drugs:
Interactions between Dostinex and methylergonovine maleate was not detected. Nevertheless, it is necessary to refrain from using a combination of cabergoline and ergot alkaloids. Against the background of the drug should not be prescribed dopamine antagonists (butyrophenones, phenothiazines, metoclopramide, thioxanthenes). Since cabergoline stimulates receptors for dopamine, dopamine antagonists can cause clinical inefficiency of the drug.
Side effect of cabergoline is arterial hypotension, therefore it is not recommended to prescribe other drugs with hypotensive effect on the background of taking the drug.
With an accidental overdose of Dostinex possible vomiting, nausea, dyspeptic phenomena, impaired consciousness (hallucinations, psychosis), arterial hypotension. For treatment, it is recommended that conventional measures be taken to remove unabsorbed cabergoline from the digestive tract. Possible use of dopamine antagonists. In the future, symptomatic therapy (normalization of blood pressure).
The drug Dostinex should be stored at room temperature.
Tablets of 0.5 mg. In the package – 8 tablets.
Active substance: cabergoline.
Inactive substances: leucine and lactose.
Efficiency and safety issues were not studied Dostinex in patients with renal or hepatic insufficiency. The main way of eliminating cabergoline is excretion with bile, so for serious violations of liver function the drug is not recommended. It is used with caution in patients with cardiovascular pathology, liver disease, Raynaud’s syndrome, duodenal ulcer or stomach ulcer, kidney failure, mental illness (including past illnesses), and bleeding from the gastrointestinal tract.
If Dostineks is used in a long-term regime, periodic gynecological examination is necessary, which includes histological examination of the endometrium and mucosal cervical canal. Cabergoline, like other ergot remedies, is strictly not allowed to use to prevent lactation in women who have experienced pre-eclampsia or have postpartum hypertension. It was found that with the use of Dostinex to suppress physiological lactation in a dose of 0.5 mg, an increase in the risk of side effects is observed in 2 times. Therefore, it is not recommended for this purpose to use the dosage of the drug more than 0.25 mg.
Before taking the drug to treat hyperprolactinemia, it is necessary to diagnose the pituitary gland to determine the possible development of a tumor of pituitary origin. The pituitary tumor is most often associated with infertility, galactorrhea and amerorrhea. In women with hypogonadism of hyperprolactinemic origin, Dostinex restores fertility and ovulation. Therefore, it is necessary to conduct a regular pregnancy test every month, to carry out a pregnancy test (if the drug is used in the presence of amenorrhea). After the restoration of fertility and menstruation to prevent pregnancy, it is necessary to use mechanical contraception. If during pregnancy Dostineksom becomes pregnant, the drug is canceled and observed for the pituitary, since it is possible to resume clinical symptoms of the pituitary tumor.
The drug has a long half-life, so after the resumption of regularity of the menstrual cycle, it is necessary to cancel Dostinex one month before the expected conception. This is necessary to prevent the influence of cabergoline on the developing fetus. If on a background of reception of a preparation conception all the same comes, Dostineks cancel. In experiments on rats it was established that cabergoline is excreted in breast milk. Despite the fact that the study in humans was not conducted, it is recommended that if the drug is taken during breastfeeding, stop lactation. The efficacy and safety of the drug in children (up to 16 years of age) have not been studied. In the first days of taking the drug, it is necessary to carefully manage the vehicles and work in production with installations that require close attention.