Dostinex( cabergoline): treatment of hyperprolactinaemia, suppression of lactation - Causes, symptoms and treatment. MF.

Dostinex is a drug for the treatment of diseases caused or combined with hyperprolactinemia: amenorrhea, galactorrhea, infertility, prolactin-secreting pituitary adenoma, acromegaly. It is used to suppress lactation.

Latin name: Dostinex / Dostinex.

Structure and Composition: Dostinex tablets: in package 2 and 8 pcs.
1 tablet Dostinex contains cabergoline 500 mcg.

Active-active substance of the drug Dostinex: Cabergoline / Cabergoline.

Pharmacological action of the drug Dostinex:

Dostinex - dopamine-stimulating agent, ergoline derivative, reduces hypersecretion of STH, inhibits the secretion of prolactin. Stimulates dopamine D2 receptors of lactotrophic cells of the pituitary gland;in high doses has a central dopaminergic effect. Normalizes the content of prolactin in the blood, restores the menstrual cycle and fertility. Due to the decrease in prolactin levels in women, the pulsating secretion of gonadotropins and the release of LH in the middle of the cycle are restored, the anovulatory cycles are eliminated, the concentration of estrogen in the body is increased, the hypoestrogenic level is increased( weight gain, fluid retention, osteoporosis) and hyperandrogenic( acne, hirsutism, etc.).) of the symptoms. Reduction in prolactin levels is observed 3 hours after taking Dostinex and persists for 7-28 days in patients with hyperprolactinemia and up to 14-21 days - with suppression of postpartum lactation. Normalization of prolactin takes place within 2-4 weeks of treatment. In men, reduces the hyperprolactinemia-related decrease in libido, impotence( with a drop in prolactin levels, testosterone levels increase), gynecomastia, softening and softening of the testicles, lactorrhea. The macroadenoma of the pituitary gland and the associated symptoms( headache, disturbance of the fields and visual acuity, functions of the cranial nerves and the anterior lobe of the pituitary gland) are reversed. Reduces the content of prolactin in patients with prolactinoma and pseudoprolactinoma( in the latter without reducing the size of the pituitary adenoma).Inhibits the release of STH by the pituitary adenoma and reduces visual disturbances, neurological disorders and severe headaches, inhibits the progression of acromegaly. In 70-90% of patients causes clinical improvement, but at the end of the course the content of STG in the blood again increases. Stimulation of dopamine receptors restores the neurochemical balance in the region of the striatum and the black core of the brain, which contributes to weakening of depressive symptoms, tremors and rigidity, acceleration of movements at all stages of Parkinson's disease.

Pharmacokinetics of the drug Dostinex:

After oral administration, cabergoline is rapidly absorbed from the digestive tract. The intake of food does not affect the absorption and distribution of the active substance. Cmax in plasma is achieved in 0.5-4 h;the connection with proteins is 40-42%.
The equilibrium state is achieved after 4 weeks of therapy.
Binding to plasma proteins is 41-42%.Excretion of
T1 / 2 is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinaemia.
The state of equilibrium concentration is achieved after 4 weeks of therapy.
Cabergoline is excreted by the kidneys.

Indications for the drug Dostinex:

Prevention of physiological puerperal lactation or suppression of established lactation( including if the mother prefers not to breastfeed, or when breastfeeding is contraindicated to either the mother or the baby, with stillbirth or abortion);
treatment of dysfunctions caused or combined with hyperprolactinemia( including women - amenorrhea, oligomenorrhoea, anovulation, galactorrhea, infertility, in men - impotence, decreased libido);
treatment of prolactin-secreting adenomas of the pituitary gland( micro- and macro-prolactin);
idiopathic hyperprolactinaemia;
syndrome of the "empty" Turkish saddle;
acromegaly( maintenance therapy after surgery or radiation therapy).

Method of administration and dose of the drug Dostinex:

To prevent postpartum lactation, Dostinex is prescribed 1 mg once on the first day after childbirth.
To suppress the established lactation, Dostinex is prescribed 250 μg every 12 hours for 2 days. With this dosing regimen, side effects( especially arterial hypotension) are less frequent.
For the treatment of hyperprolactinemia, Dostinex is prescribed 1-2 times a week. The initial dose is 250 micrograms per week. If necessary, the dose may be increased depending on the therapeutic effect and tolerability. An increase in the weekly dose should be carried out gradually( 500 mcg with an interval of 1 month).The average therapeutic dose is 1 mg per week and can vary from 250 μg to 2 mg per week. When appointing the drug at a dose of 1 mg per week or more, it should be divided into 2 or more doses per week, depending on the tolerability.
Dostinex should be taken with meals.

Overdose of the drug Dostinex:

Symptoms of overdose: nausea, vomiting, abdominal pain, constipation, decreased blood pressure, headache, severe general weakness, sweating, drowsiness, psychomotor agitation, cramps in the calf muscles, impaired consciousness: psychosis, hallucinations. Treatment: gastric lavage and subsequent control of blood pressure;antagonists of dopamine.

Contraindications of the drug Dostinex:

Hypersensitivity( including other ergot derivatives);pregnancy, lactation;postpartum psychosis( in history);postpartum hypertension.
Precautions include cardiovascular disease, Raynaud's syndrome, renal insufficiency, hepatic insufficiency, peptic ulcer and duodenal ulcer, gastrointestinal bleeding, or a history of mental illness.

Use of the drug Dostinex in pregnancy and lactation:

Do not use Dostinex during pregnancy and during breastfeeding.
A woman should be warned that if Dostinex was appointed to suppress lactation, but the desired effect was not achieved, it is necessary to refrain from breastfeeding and consult a doctor.
Before beginning treatment with Dostinex, pregnancy should be excluded and mechanical methods of contraception should be used further. If pregnancy is established during treatment with Dostinex, it is necessary to stop taking the drug.
Since the half-life of cabergoline is long, after the restoration of the regular menstrual cycle, it is recommended to stop taking the drug 1 month before the expected conception to prevent the possible effects of the drug on the fetus.

Side effects of the drug Dostinex:

Often: decreased blood pressure, dizziness, nausea, headache, insomnia, abdominal pain.
With prolonged use - gastritis, weakness, drowsiness, constipation, vomiting, painful tension of the mammary glands, "tides" of blood to the skin of the face, depression, paresthesia. These symptoms are mild, appear within the first 2 weeks and pass on their own.

Special instructions and safety precautions : Dostinex is prescribed with caution to patients with cardiovascular diseases, Raynaud's syndrome, severe renal dysfunction, peptic ulcer and duodenal ulcer, gastrointestinal bleeding, or a history of mental illness.
With caution appoint Dostinex on the background of therapy with drugs that cause hypotensive effect.

After choosing an effective dosing regimen, it is recommended to conduct a regular( 1 time per month) determination of the serum prolactin level. Normalization of prolactin levels is usually observed within 2-4 weeks of treatment.
Before the beginning of treatment by Dodonexom, pregnancy is excluded and mechanical methods of contraception are used. If the pregnancy occurred during treatment, it is necessary to stop taking the drug and consult a doctor.

In the case of prolonged use of Dostinex, a regular gynecological examination is required, including a cervical histological examination and a histological study of the endometrium. After the restoration of the regular menstrual cycle for 1 month before the expected conception should stop taking the drug.

It is necessary to monitor blood pressure, GI functions( potential bleeding hazard).With an increase in blood pressure, the occurrence of persistent headaches or any signs of neurotoxicity, the reception of Dostinex is immediately stopped. To reduce nausea, reduce the dose, prescribe domperidone or cisapride.

Inefficiency of cabergoline testifies to the presence of other causes of hyperprolactinaemia( decreased prolactin clearance in liver diseases, chronic renal failure, especially in patients on hemodialysis).

Impact on ability to drive vehicles and control mechanisms:
Patients taking the drug should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interaction: With the simultaneous use of Dostinex with antibiotics from the macrolide group, the risk of side effects increases.
Derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide decrease the effectiveness of Dostinex.
Combination with ergot alkaloids and their derivatives, as well as with antihypertensive drugs, is not recommended.

Storage conditions: The drug should be stored at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
Release of the drug from the pharmacy - it is released on prescription.

Description of the drug Dostinex is not an instruction for self-treatment, it is necessary to consult a doctor.