Dostinex
Dostinex: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Dostinex
ATX code: G02CB03
Active ingredient: cabergoline (cabergoline)
Producer: Pfizer Italia SrL (Italy)
Description and photo update: 2019-16-08
Prices in pharmacies: from 610 rubles.
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Dostinex is an inhibitor of prolactin secretion.
Release form and composition
Dosage form - tablets: flat oblong, white, marked on one side "P" and "U", separated by a notch, on the other - short notches on the bottom and top of the number "700" (2 or 8 pcs. In dark vials glass, in a cardboard box 1 bottle).
The active ingredient is cabergoline, in 1 tablet - 0.5 mg.
Auxiliary components: leucine, anhydrous lactose.
Pharmacological properties
Pharmacodynamics
Cabergoline is a dopaminergic derivative of ergoline and has a pronounced and prolonged prolactin-lowering effect, which is explained by the direct stimulation of D 2 -dopamine receptors localized in the lactotropic cells of the pituitary gland. Also, in contrast to taking Dostinex in order to reduce the level of prolactin in the blood plasma, taking it in higher doses causes the central dopaminergic effect of cabergoline due to the stimulation of D 2 receptors.
A decrease in the content of prolactin in the blood plasma is observed within 3 hours after taking Dostinex and persists for 7-28 days in patients with hyperprolactinemia and healthy volunteers and up to 14-21 days in women who have just survived childbirth. Cabergoline is characterized by a strictly selective action and does not alter the basal secretion of cortisol and other pituitary hormones. The active component of Dostinex reduces the production of prolactin, and this effect is dose-dependent both in terms of severity and prolonged action.
The pharmacodynamic effect of cabergoline, which is not related to its therapeutic properties, is expressed exclusively in lowering blood pressure. A single dose of Dostinex leads to the maximum hypotensive effect, which is observed during the first 6 hours and depends on the dose.
Pharmacokinetics
Cabergoline is absorbed from the gastrointestinal tract at a high rate, and its maximum plasma level is recorded 0.5-4 hours after ingestion. The degree of binding to blood plasma proteins reaches approximately 41-42%. The half-life of cabergoline is determined by the rate of excretion through the kidneys: it is equal to 63–68 hours in healthy volunteers and 79–115 hours in women suffering from hyperprolactinemia. Since the drug is excreted from the body for a long time, the equilibrium concentration of the active substance in the body is reached approximately 4 weeks after the start of treatment.
10 days after the start of the course of therapy, 72% and 18% of the dose of cabergoline taken, respectively, are found in feces and urine, and the proportion of cabergoline in unchanged form excreted through the kidneys is no more than 2–3%. The main metabolite detected in urine is 6-allyl-8β-carboxy-ergoline, the concentration of which is 4–6% of the dose of cabergoline taken. Also, urine contains 3 additional metabolites of lesser clinical significance, the content of which does not exceed 3% of the dose of Dostinex taken. The results of clinical studies confirm that drug metabolites suppress prolactin synthesis much weaker compared to cabergoline itself. Food intake does not change the degree of absorption and distribution of the active component of Dostinex.
Indications for use
- Suppression of established postpartum lactation;
- Prevention of physiological postpartum lactation;
- Prolactin-secreting pituitary adenomas (macro- and microprolactinoma), idiopathic hyperprolactinemia, combination of the syndrome of "empty Turkish saddle" with hyperprolactinemia;
- Therapy of disorders associated with hyperprolactinemia, including galactorrhea, anovulation, amenorrhea and oligomenorrhea.
Contraindications
- Age under 16;
- Breastfeeding period (for women who do not want to stop lactation);
- Hypersensitivity to the components of the drug and ergot alkaloids.
According to the instructions, Dostinex is recommended to be used with caution: in severe cardiovascular diseases, Raynaud's syndrome; with severe hepatic impairment (lower doses should be prescribed); with gastrointestinal bleeding, peptic ulcer; in the case of arterial hypertension that developed during pregnancy (preeclampsia or postpartum arterial hypertension), the appointment is possible only if the potential benefit significantly outweighs the likely risk; with severe cognitive or psychotic impairment (including information in history); with simultaneous use with antihypertensive drugs (there is a risk of orthostatic hypotension), with symptoms, including a history of functional respiratory and heart disorders due to fibrotic changes.
Instructions for the use of Dostinex: method and dosage
Dostinex tablets are recommended to be taken orally, with meals.
Recommended dosage for Dostinex:
- Suppression of established lactation: 0.25 mg (1/2 tab.) 2 times a day. The course of therapy is 2 days with a total dose of 1 mg. Exceeding the specified dose may cause the development of orthostatic hypotension;
- Prevention of lactation: once 1 mg (2 tablets) on the first day after childbirth;
- Treatment of disorders associated with hyperprolactinemia: 0.5 mg per week, with a gradual increase (no more than 0.5 mg over 4 weeks) until a therapeutically effective weekly dose is reached, which can range from 0.25 to 2 mg … Depending on the tolerance of Dostinex, the dose can be taken once or divided into several doses in equal shares (for example, on Monday and Thursday). To reduce the risk of side effects in patients with hypersensitivity to dopaminergic drugs, it is recommended to start therapy with a dose of 0.25 mg once a week with a gradual increase to the optimal dose of treatment. The maximum weekly dose for patients with hyperprolactinemia should not exceed 4.5 mg. When prescribing a dose of 1 mg per week or more, it is recommended to take it, proportionally divided into several doses during the week. If the patient develops severe side effects, a temporary decrease in the weekly dose is allowed, an increase in which is then carried out by 0.25 mg 1 time in 2 weeks.
Side effects
Based on clinical studies, the use of Dostinex can cause the development of side effects:
- From the digestive system: pain in the epigastric region, nausea, vomiting, abdominal pain, gastritis, constipation, dyspepsia;
- On the part of the cardiovascular system: palpitations; rarely - a decrease in blood pressure (asymptomatic) in the first 3-4 days after childbirth (systolic decreases by more than 20 mm, diastolic - by more than 10 mm Hg), orthostatic hypotension (against the background of prolonged therapy, the drug has a hypotensive effect);
- From the nervous system: increased fatigue, dizziness (vertigo), fainting, drowsiness, headache, depression, paresthesia, asthenia;
- On the part of laboratory parameters: rarely - a decrease in the level of hemoglobin in patients with amenorrhea was observed during the first months after the restoration of the menstrual cycle;
- Others: hyperemia, mastodynia, transient hemianopsia, epistaxis, leg muscle cramps, vasospasm of the fingers (the drug has a vasoconstrictor property).
Usually, side effects are transient in nature and in most patients disappear as treatment continues, and their severity usually depends on the Dostinex dose.
Based on post-marketing studies, the use of cabergoline can cause side effects in the form of: alopecia, increased activity of creatine phosphokinase (CPK) in the blood, dyspnoea, mania, edema, fibrosis, liver dysfunction, liver function abnormalities, rash, hypersensitivity reactions, respiratory disorders, valvulopathy, respiratory failure.
Overdose
Overdose of Dostinex causes hyperstimulation of dopamine receptors, the symptoms of which include orthostatic arterial hypotension, dyspeptic disorders, nausea, vomiting, hallucinations, confusion, psychosis. In this case, it is necessary to carry out additional therapeutic measures to remove unabsorbed cabergoline (mainly gastric lavage) and, if necessary, normalize blood pressure. Dopamine antagonists are also allowed.
special instructions
The appointment of Dostinex for the treatment of disorders associated with hyperprolactinemia is based on data from a complete study of the function of the pituitary gland.
Each dose increase should be carried out under the supervision of the attending physician to determine the lowest effective dose necessary to achieve a therapeutic effect. After establishing the dosage regimen, studies should be carried out at least 1 time per month to determine the level of concentration in the blood serum of prolactin, its normalization occurs within 2-4 weeks of therapy.
Usually, after discontinuation of Dostinex, patients experience a relapse of hyperprolactinemia, but in some cases, persistent containment of prolactin levels occurs over the next months. After stopping Dostinex, ovulatory cycles in most women persist for at least 6 months.
In women with hyperprolactinemic hypogonadism, Dostinex restores fertility and ovulation. Since fertilization can occur during the period of amenorrhea, pregnancy tests should be performed at least 1 time per month, after the restoration of the menstrual cycle - at each delay of menstruation for more than 3 days. Patients wishing to avoid pregnancy should use barrier methods of contraception during treatment and after discontinuation of the drug until anovulation recurs. For the timely detection of symptoms of an enlarged pituitary gland, women with a pregnancy should be constantly monitored by a doctor, since during this period an increase in the size of existing pituitary tumors is possible.
It is recommended to prescribe lower doses for long-term therapy in patients with severe hepatic impairment.
Dostinex tablets are recommended to be taken with caution in patients with clinical symptoms and / or existing signs of cardiac dysfunction, and if these conditions are present in the anamnesis. Patients with a diagnosis of valvulopathy, fibrinous pleurisy, or pleural effusion experienced an improvement in well-being after discontinuation of the drug.
Patients with Parkinson's disease who fall asleep suddenly while taking the drug are advised to reduce the dose or cancel the treatment.
Studies on the therapeutic use of the drug in elderly patients have not been conducted.
The efficacy and safety of the drug in patients under 16 years of age has not been established.
Dostinex can cause drowsiness, therefore, during the period of treatment, you should refrain from driving vehicles and mechanisms.
Application during pregnancy and lactation
Since controlled clinical studies of the use of Dostinex in pregnant women have not been conducted, the drug can be taken by patients from this category only after a thorough study of the benefit / risk ratio for the woman and the fetus and only in case of emergency.
If pregnancy occurs during treatment with Dostinex, consultation with a specialist is necessary, who will assess the feasibility of discontinuing the drug, weighing the potential benefits of treatment and possible risks to the fetus.
Available data confirm that taking Dostinex at a dose of 0.5-2 mg weekly in connection with disorders caused by hyperprolactinemia does not lead to an increase in the frequency of miscarriages, congenital malformations, the onset of multiple pregnancies or premature birth.
There is no information about the penetration of cabergoline into breast milk, however, if the effect of the drug, aimed at preventing or suppressing lactation, is minimal, nursing mothers are advised to stop breastfeeding. For disorders provoked by hyperprolactinemia, the drug is contraindicated in women planning breastfeeding.
Drug interactions
The simultaneous long-term use of cabergoline with other preparations of ergot alkaloids is not recommended.
You can not simultaneously prescribe the drug with dopamine antagonists, such as phenothiazine, butyrophenone, thioxanthene, metoclopramide, since they can weaken the prolactin-lowering effect of Dostinex.
The combination with macrolide antibiotics (erythromycin) can lead to an increase in the action of cabergoline.
Analogs
Dostinex analogs are: Agalates, Bergolak, Cabergoline.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Dostinex
Reviews about Dostinex are quite numerous, but it is difficult to make an unequivocal opinion about whether the drug helps in reducing prolactin. Many patients take it to stop lactation and report its high efficacy and low risk of side effects. However, some women note that Dostinex had practically no effect on them, while causing side reactions such as headaches, loss of consciousness, etc. The opinions of experts also differ, therefore, the use of the drug must be approached individually.
Dostinex price in pharmacies
The approximate price for Dostinex in pharmacy chains is 579-912 rubles (for a pack containing 2 tablets) or 1499-2070 rubles (for a pack containing 8 tablets).
Dostinex: prices in online pharmacies
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Drug name Price Pharmacy |
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Dostinex 0.5 mg tablets 2 pcs. RUB 610 Buy |
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Dostinex tablets 0.5mg 2 pcs. 778 RUB Buy |
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Dostinex 0.5 mg tablets 8 pcs. 2000 RUB Buy |
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Dostinex tablets 0.5mg 8 pcs. 2702 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
