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CABERGOLIA Acceptance

PHARMA ACTION

A dopamine-stimulating agent, an ergoline derivative, reduces the hypersecretion of growth hormone, suppresses the secretion of prolactin. Stimulates dopamine D2 receptors of lactotropic pituitary cells; in high doses, it has a central dopaminergic effect. Normalizes the content of prolactin in the blood, restores the menstrual cycle and fertility. By reducing the concentration of prolactin in the blood in women, the pulsating secretion of gonadotropins and the release of LH in the middle of the cycle are restored, anovulatory cycles are eliminated and the concentration of estrogen in the body increases, the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism and others) symptoms. In men, it reduces the decrease in libido caused by hyperprolactinemia, impotence (with a decrease in the concentration of prolactin, the level of testosterone increases), gynecomastia, reduction and softening of the testicles, lactorrhea. The macroadenomas of the pituitary gland and the associated symptoms (headache, impaired fields and visual acuity, functions of the cranial nerves and the anterior pituitary gland) undergo regression. Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter – without reducing the size of the pituitary adenoma). Suppresses the release of growth hormone by pituitary adenoma and reduces visual impairment, neurological disorders and severe headaches, inhibits the progression of acromegaly. In 70-90% of patients, it causes a clinical improvement, however, at the end of the course, the content of STH in the blood increases again. Stimulation of dopamine receptors restores the neurochemical balance in the area of ​​the striatum and the black nucleus of the brain, which contributes to the weakening of depressive symptoms, tremor and rigidity, and the acceleration of movements in all stages of Parkinson’s disease. A decrease in the concentration of prolactin is observed 3 hours after administration and persists for 7-28 days in patients with hyperprolactinemia and 14-21 days – with suppression of postpartum lactation. Normalization of the concentration of prolactin occurs within 2-4 weeks. treatment. Normalization of the concentration of prolactin occurs within 2-4 weeks. treatment. Normalization of the concentration of prolactin occurs within 2-4 weeks. treatment.

INDICATIONS

Postpartum lactation (prevention or suppression);
treatment of disorders associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, galactorrhea),
prolactin-secreting pituitary adenomas (micro- and macroprolactinomas);
idiopathic hyperprolactinemia;
syndrome of “empty” Turkish saddle in combination with hyperprolactinemia.

CONTRAINDICATIONS

Hypersensitivity (including to other ergot derivatives), lactation period.
Carefully. Severe cardiovascular disease, Raynaud’s syndrome, severe liver failure, peptic ulcer, gastrointestinal bleeding, severe psychotic and cognitive impairment (including history), arterial hypertension that developed during pregnancy (preeclampsia) and postpartum arterial hypertension, children age (up to 16 years – safety and efficacy have not been established).

DOSING

Inside, during meals. To prevent postpartum lactation – on the first day after birth, 1 mg once. To suppress established lactation – 0.25 mg 2 times a day for 2 days.
Treatment of hyperprolactinemia – 0.5 mg in 1-2 doses per week. Therapeutic dose – 0.25-2 mg / week, the average therapeutic dose – 1 mg / week for 2 doses. The weekly dose can be increased at a rate not exceeding 0.5 mg/month. The maximum weekly dose is 4.5 mg.
Cabergoline should be given at lower doses to patients with severe hepatic impairment who are eligible for long-term therapy with the drug.

SIDE EFFECTS

Moderately expressed, appear during the first 2 weeks and disappear on their own.
From the nervous system: dizziness, vertigo, headache, fatigue, drowsiness, depression, asthenia, paresthesia, fainting.
From the digestive system: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia. From the CCC: asymptomatic decrease in blood pressure (during the first 3-4 days after birth), palpitations; rarely – orthostatic hypotension. Others: mastodynia, epistaxis, “flushing” of blood to the skin of the face, transient hemianopsia, vasospasm of the fingers, muscle cramps of the lower extremities, alopecia, increased CPK activity, mania, dyspnea, edema, pleural fibrosis, pleural effusion, valvulopathy, respiratory disorders ( including respiratory failure), impaired liver function.
Allergic reactions: skin rash,
Overdose. Symptoms: nausea, vomiting, abdominal pain, constipation, decreased blood pressure, orthostatic hypotension, headache, cramps in the calf muscles, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations, impaired consciousness.
Treatment: gastric lavage, blood pressure control, administration of dopamine antagonists (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide).

INTERACTION

Macrolides (including erythromycin) increase the risk of side effects (increase the concentration of the drug in plasma).
Derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide reduce the effect.
The combination with ergot alkaloids and their derivatives is not recommended.

Updated: 21/04/2023 — 11:05 am

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