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Dostinex

Dostinex
Dostinex is used to prevent physiological postpartum lactation immediately after childbirth or to suppress existing lactation.

Brand: Cabergoline

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: October 2023
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Dostinex 0.25 mg
32 pills - 0.25 mg
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$117.57 $3.67 $72.63 Add to cart
24 pills - 0.25 mg $94.68 $3.95 $47.97 Add to cart
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12 pills - 0.25 mg $59.99 $5.00 $11.34 Add to cart
8 pills - 0.25 mg $47.55 $5.94 No Add to cart
Dostinex 0.5 mg
48 pills - 0.5 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$359.55 $7.49 $288.33 Add to cart
32 pills - 0.5 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$248.99 $7.78 $182.93 Add to cart
24 pills - 0.5 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$192.73 $8.03 $131.21 Add to cart
16 pills - 0.5 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$137.99 $8.62 $77.97 Add to cart
12 pills - 0.5 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$109.95 $9.16 $52.02 Add to cart
8 pills - 0.5 mg $81.33 $10.17 $26.65 Add to cart
4 pills - 0.5 mg $53.99 $13.50 No Add to cart

Product description

Pharmacological action of Dostinex

Buy Dostinex in Canada

Cabergoline is a dopaminergic derivative of ergoline, characterized by a pronounced and prolonged prolactin-lowering effect due to direct stimulation of dopamine D2receptors of pituitary lactotropic cells. In addition, when taken in doses in excess of those to reduce the concentration of prolactin in the blood plasma, cabergoline has a central dopaminergic effect due to the stimulation of dopamine D2receptors.

A decrease in the concentration of prolactin in blood plasma is noted 3 hours after taking the drug and persists for 7-28 days in healthy volunteers and patients with hyperprolactinemia, and up to 14-21 days in women in the postpartum period.

Cabergoline has a strictly selective effect, does not affect the basal secretion of other pituitary hormones and cortisol. The prolactin-lowering effect of cabergoline is dose-dependent in terms of both severity and duration of action.

The pharmacological effects of cabergoline, not associated with a therapeutic effect, include only a decrease in blood pressure. With a single dose of the drug, the maximum hypotensive effect is observed during the first 6 hours and is dose-dependent.

Pharmacokinetics

Absorption and distribution

After oral administration, cabergoline is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is achieved in 0.5-4 hours. Plasma protein binding is 41-42%. Css is achieved after 4 weeks of therapy due to prolonged T1/2.

Food intake does not affect the absorption and distribution of cabergoline.

Metabolism

The main metabolic product of cabergoline identified in urine is 6-allyl-8β-carboxy-ergoline at a concentration of up to 4-6% of the dose taken. The content of 3 additional metabolites in urine does not exceed 3% of the dose taken. It was found that metabolic products have a significantly lower effect in suppressing the secretion of prolactin in comparison with cabergoline.

Elimination

T1/2, assessed by the rate of excretion by the kidneys, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia.

10 days after taking cabergoline, 18% and 72% of the dose taken, respectively, are found in urine and feces, and the proportion of unchanged cabergoline in urine is 2-3%.

Indications for Dostinex®

Dostinex drug appearance

  • prevention of physiological postpartum lactation;

  • suppression of established postpartum lactation;

  • treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation and galactorrhea;

  • prolactin-secreting pituitary adenomas (micro- and macroprolactinomas), idiopathic hyperprolactinemia, syndrome of "empty" Turkish saddle in combination with hyperprolactinemia.

Dosage regimen of Dostinex

Is taken orally, with meals.

Prevention of lactation: 1 mg (2 tablets) once on the first day after childbirth.

Suppression of established lactation: 0.25 mg (1/2 tab.) 2 times / day every 12 hours for 2 days (total dose is 1 mg). To reduce the risk of development of orthostatic hypotension in breastfeeding mothers single dose Dostinexformulation® should not exceed 0.25 mg.

Treatment of disorders associated with hyperprolactinemia: the recommended starting dose is 0.5 mg per week in 1 (1 tab.) Or 2 doses (1/2 tab., For example, on Monday and Thursday). An increase in the weekly dose should be carried out gradually - by 0.5 mg with an interval of 1 month until the optimal therapeutic effect is achieved. The therapeutic dose is usually 1 mg per week, but can range from 0.25 mg to 2 mg per week. The maximum dose for patients with hyperprolactinemia is 4.5 mg per week.

Depending on the tolerance, the weekly dose can be taken once or divided into 2 or more doses per week. The division of the weekly dose into several doses is recommended when prescribing the drug at a dose of more than 1 mg per week.

In patients with increased sensitivity to dopaminergic drugs likelihood of side effects can be reduced by starting therapy with Dostinex® at a lower dose (0.25 mg of 1 times a week), followed by a gradual increase to achieve its therapeutic dose. To improve the tolerance of the drug in the event of severe side effects, a temporary decrease in the dose is possible, followed by a gradual increase, for example, by 0.25 mg per week every 2 weeks.

Contraindications for use

  • hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids;

  • dysfunction of the heart and respiration due to fibrotic changes or the presence of such conditions in history;

  • with long-term therapy: anatomical signs of the pathology of the valve apparatus of the heart (such as thickening of the valve leaflet, narrowing of the valve lumen, mixed pathology - narrowing and stenosis of the valve), confirmed by echocardiographic examination (EchoCG) performed before the start of therapy;

  • lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

  • children and adolescents up to 16 years of age (safety and efficacy have not been established).

Dostinex® should be prescribed with caution in the following conditions and / or diseases:

  • arterial hypertension that developed during pregnancy, for example, preeclampsia or postpartum arterial hypertension (Dostinex® is prescribed only in cases where the potential benefit from the use of the drug significantly outweighs the possible risk);

  • severe cardiovascular disease, Raynaud's syndrome;

  • peptic ulcer, gastrointestinal bleeding;

  • severe hepatic impairment (lower doses are recommended);

  • severe psychotic or cognitive impairment (including a history);

  • simultaneous use with drugs that have an antihypertensive effect (due to the risk of orthostatic hypotension).

Application during pregnancy and lactation

Since there have been no controlled clinical trials with the use of Dostinex® in pregnant women, the administration of the drug during pregnancy is possible only in cases of extreme necessity, taking into account the benefit / risk ratio for the woman and the fetus.

If pregnancy occurs during treatment with Dostinex®, the advisability of discontinuing the drug should be considered, also taking into account the benefit / risk ratio.

According to the available data, the use of Dostinex at a dose of 0.5-2 mg per week for disorders associated with hyperprolactinemia was not accompanied by an increase in the frequency of miscarriages, premature birth, multiple pregnancies and congenital malformations.

There is no information on the excretion of the drug in breast milk, however, in the absence of the effect of using the drug Dostinex® to prevent or suppress lactation, breastfeeding should be abandoned. For disorders associated with hyperprolactinemia, Dostinex® is contraindicated in patients planning breastfeeding.

Application for violations of liver function

The caution drug is used within severe liver failure (lower doses are recommended).

Use in children

Contraindication: children and adolescents under 16 years of age (safety and efficacy have not been established).

Special instructions

Before prescribing Dostinex® for the treatment of disorders associated with hyperprolactinemia, it is necessary to conduct a complete study of the pituitary gland function.

In addition, an assessment of the state of the cardiovascular system, including echocardiography, should be carried out in order to identify asymptomatic dysfunction of the valve apparatus.

As with other ergot derivatives, patients with long-term use of cabergoline have had pleural effusion / pleural fibrosis and valvulopathy. In some cases, patients have received prior therapy with dopamine ergotonin agonists. Therefore Dostinex® should not be used in patients with current symptoms and / or clinical symptoms of cardiac or respiration functions associated with fibrotic changes or such states in the history. You should stop taking the drug if signs of the appearance or worsening of blood regurgitation, narrowing of the lumen of the clans or thickening of the valve leaflets are detected.

It was found that ESR increases with the development of pleural effusion or fibrosis. If an unexplained increase in ESR is found, a chest X-ray is recommended. In making a diagnosis, the study of the concentration of creatinine in the blood plasma, an assessment of renal function can also help. After discontinuation Dostinex® in patients with pleural effusion / fibrosis or pleural valvulopatii noted improvement in symptoms.

It is not known whether cabergoline can worsen patients with signs of blood regurgitation. Cabergoline should not be used in the detection of fibrotic lesions of the heart valve apparatus.

Fibrotic disorders can be asymptomatic. In this regard, you should regularly monitor the condition of patients receiving long-term therapy with cabergoline and pay special attention to the following symptoms:

  • pleuro-pulmonary disorders: such as shortness of breath, difficulty breathing, persistent cough or chest pain;

  • renal failure or obstruction of the vessels of the ureters or abdominal organs, which may be accompanied by pain in the side or in the lumbar region and edema of the lower extremities, any swelling or pain on palpation in the abdomen, which may indicate the development of retroperitoneal fibrosis;

  • pericardial fibrosis and fibrosis of the valve cusps often present with heart failure. In this regard, it is necessary to exclude fibrosis of the valves of the heart valves (and constrictive pericarditis) when symptoms of heart failure appear.

The patient's condition should be regularly monitored for the development of fibrotic disorders. The first time EchoCG should be performed 3-6 months after the start of therapy. Then this study should be carried out depending on the clinical assessment of the patient's condition, paying special attention to the symptoms described above, at least every 6-12 months of therapy.

The need for other monitoring methods (eg, physical examination, including cardiac auscultation, radiography, computed tomography) is assessed individually for each patient.

When the dose is increased, patients should be under medical supervision in order to establish the minimum effective dose that provides a therapeutic effect.

After an effective dosing regimen is selected, it is recommended to carry out regular (once a month) determination of the concentration of prolactin in serum. Normalization of prolactin concentration is usually observed within 2-4 weeks of treatment.

After discontinuation of Dostinex® , a relapse of hyperprolactinemia is usually observed, however, some patients experience persistent suppression of prolactin concentration for several months. In most women, ovulatory cycles persist for at least 6 months after discontinuation of the drug Dostinex®.

Dostinex® restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before menstruation is restored, it is recommended to carry out pregnancy tests at least once every 4 weeks during the period of amenorrhea, and after menstruation is restored - every time there is a delay in menstruation by more than 3 days. Women wishing to avoid pregnancy should use barrier methods of contraception during treatment with Dostinex®, as well as after discontinuation of the drug until anovulation recurs. Women who have become pregnant should be under the supervision of a doctor for the timely detection of symptoms of an enlarged pituitary gland, since during pregnancy, an increase in the size of already existing pituitary tumors is possible.

Dostinex® should be prescribed in lower doses to patients with severe hepatic impairment (class C according to the Child-Pugh classification) for whom long-term drug therapy is indicated. With a single use of the drug in such patients at a dose of 1 mg, there was an increase in AUC compared to healthy volunteers and patients with less severe hepatic impairment.

The use of cabergoline causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists can induce sudden sleep. In such cases, it is recommended to reduce the dose of Dostinex® or discontinue therapy.

Studies on the use of the drug in elderly patients with disorders associated with hyperprolactinemia have not been conducted.

Use in Pediatrics

The safety and efficacy of the drug in children and adolescents under 16 years of age has not been established.

Influence on the ability to drive vehicles and control mechanisms

Patients taking Dostinex®should refrain from driving vehicles and mechanisms and other potentially dangerous activities that require concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms (more likely symptoms of dopamine receptor hyperstimulation): nausea, vomiting, dyspeptic symptoms, orthostatic arterial hypotension, confusion, psychosis, hallucinations.

Treatment: measures should be taken to remove the unabsorbed drug (gastric lavage) and, if necessary, to maintain blood pressure. Dopamine antagonists are recommended.

Drug Interactions

There is no information on the interaction of cabergoline and other ergot alkaloids; therefore, the simultaneous use of these drugs during long-term therapy with Dostinex® is not recommended.

Since cabergoline has a therapeutic effect by directly stimulating dopamine receptors, the drug should not be administered concurrently with drugs acting as dopamine antagonists (including phenothiazines, butyrophenones, thioxanthenes, metoclopramide). they can weaken the effect of cabergoline in decreasing prolactin concentration.

Like other ergot derivatives, cabergoline should not be used concomitantly with macrolide antibiotics (for example, with erythromycin), since this may lead to an increase in the systemic bioavailability of cabergoline.


Side effects

During clinical studies using the drug Dostinex® to prevent physiological lactation (1 mg once) and to suppress lactation (0.25 mg every 12 hours for 2 days), side effects were observed in approximately 14% of women. When using the drug Dostinex® for 6 months at a dose of 1-2 mg per week, divided into 2 doses, for the treatment of disorders associated with hyperprolactinemia, the frequency of adverse reactions was 68%. Adverse events occurred mainly during the first 2 weeks of treatment and in most cases, disappeared with continued therapy or a few days after discontinuation of the drug Dostinex®.Adverse reactions were usually transient, mild or moderate in severity and dose-dependent. At least once during therapy, severe side effects were observed in 14% of patients; due to adverse reactions, treatment was discontinued in about 3% of patients.

The most common adverse reactions are presented below.

On the part of the cardiovascular system: palpitations; in some cases - orthostatic hypotension (with prolonged use, Dostinex® usually has a hypotensive effect); possible asymptomatic decrease in blood pressure during the first 3-4 days after childbirth (systolic - not less than 20 mm Hg, diastolic - not less than 10 mm Hg).

From the nervous system: dizziness / vertigo, headache, fatigue, drowsiness, depression, asthenia, paresthesia, fainting, nervousness, anxiety, insomnia, impaired concentration.

From the digestive system: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia, dryness of the oral mucosa, diarrhea, flatulence, toothache, irritation of the pharyngeal mucosa.

Others: mastodynia, epistaxis, "hot flushes" of blood to the skin of the face, transient hemianopsia, vasospasm of the fingers, muscle cramps of the lower extremities (like other ergot derivatives, Dostinex® can have a vasoconstrictor effect), visual impairment, flu-like symptoms, malaise, periorbital and peripheral edema, anorexia, acne, pruritus, joint pain.

During long-term therapy with Dostinex®, deviation from the norm of standard laboratory parameters was observed rarely; women with amenorrhea experienced a decrease in hemoglobin levels during the first few months after menstruation was restored.

In a post-marketing study, the following adverse reactions associated with the use of cabergoline were recorded: alopecia, increased CPK activity in the blood, mania, dyspnea, edema, fibrosis, liver dysfunction, liver function abnormalities, hypersensitivity reactions, rash, respiratory disorders, respiratory failure, valvulopathy, pathological addiction to gambling, hypersexuality, increased libido, aggressiveness, psychotic disorders, pericarditis, attacks of sudden falling asleep, weight loss or increase, nasal congestion.