Dostinex 0.5mg 8 tablets — Made in Italy — Free Delivery

(Dostinex 0.5mg)
Dostinex 0.5mg  8 tablets — Made in Italy — Free Delivery
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Description Dostinex 0.5mg 8 tablets — Made in Italy — Free Delivery

Pharmacological properties

Pharmacodynamics. Cabergoline is a dopaminergic ergot derivative with strong and prolonged prolactin-lowering activity. the preparation directly stimulates d2-dopamine receptors on the surface of pituitary lactotropic cells, thus inhibiting the secretion of prolactin. this substance reduces the secretion of prolactin in rats when administered orally at a dose of 3–25 μg / kg and in vitro at a concentration of 45 pg / ml. in addition, cabergoline exerts a central dopaminergic effect through the stimulation of d2 receptors at oral doses in excess of those that are effective in reducing plasma prolactin levels. the long-term effect of the preparation dostinex on the reduction of prolactin levels is probably associated with its long-term persistence in the target organ, as indicated by the low rate of elimination of total radioactivity from the pituitary gland after a single oral dose in rats (m½ is approximately 60 h).

Pharmacodynamic effects were studied in healthy volunteers, postpartum women and patients with prolactinemia. After a single dose of the preparation in a dose of 0.3–1.5 mg, a significant decrease in plasma prolactin levels is noted in each of the studied populations. This effect develops rapidly - within 3 hours after administration of the preparation and persists for 7-28 days in healthy individuals and patients with hyperprolactinemia and within 14-21 days - in women after childbirth. The extent and duration of the decrease in prolactin levels is dose dependent.

Regarding the endocrine effects of Dostinex, which are not associated with antiprolactinemic action, there are data from studies involving humans, confirming the experimental results obtained in animal studies and showing that the test substance is characterized by a high selective effect and does not affect the basal level of secretion of other pituitary hormones and cortisol. ... The pharmacodynamic effect of Dostinex did not correlate with the therapeutic effect of blood pressure reduction alone. The maximum hypotensive effect of the preparation in a single dose is usually achieved within the first 6 hours after taking the preparation and depends on the dose for both maximum reduction and frequency of occurrence.

Pharmacokinetics. The pharmacokinetics and metabolic profiles of Dostinex were studied in healthy volunteers of both sexes and in female patients with hyperprolactinemia.

After ingestion of a substance labeled with a radioactive label, it was rapidly absorbed in the gastrointestinal tract, and the peak of radioactivity in blood plasma was reached after 0.5–4 hours.

10 days after administration of the preparation, about 18 and 72% of the radioactive dose was excreted in the urine and feces, respectively. The content of unchanged preparation in urine was 2–3% of the administered dose.

The main metabolite identified in urine was 6-allyl-8β-carboxy-ergoline, which accounted for 4–6% of the preparation dose. Three additional metabolites were identified in urine, which in total amounted to less than 3% of the preparation dose. The in vitro activity of metabolites in suppressing the secretion of prolactin is significantly lower than that of cabergoline. The metabolism of cabergoline was also studied in the blood plasma of healthy male volunteers treated with [14C] -cabergoline: it was found that cabergoline is subject to rapid and significant biotransformation.

The low level of excretion in the urine of unchanged cabergoline was also confirmed in studies using a non-radioactive preparation. T½ of cabergoline, which was determined by the rate of excretion of the preparation in the urine, is long: 63–68 hours in healthy volunteers (using radioimmunoassay) and 79–115 hours in patients with hyperprolactinemia (using high performance liquid chromatography).

Taking into account T½, the equilibrium state should be achieved after 4 weeks, which is confirmed by the average Cmax values ​​of cabergoline in blood plasma after a single use (37 ± 8 pg / ml) and after 4 weeks with repeated use (101 ± 43 pg / ml).

The results of in vitro experiments showed that the preparation  at concentrations of 0.1–10 ng / ml binds by 41–42% to blood plasma proteins. Food does not affect the absorption and distribution of the preparation.

Indications

Inhibition or suppression of physiological lactation

Prevention of physiological postpartum lactation immediately after childbirth or to suppress existing lactation in such cases: after childbirth, if the mother decided not to breastfeed the baby or when breastfeeding is contraindicated for the mother or child for medical reasons; after the birth of a dead fetus or after an abortion.

Treatment of hyperprolactinemia

Disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, and galactorrhea. Treatment of patients with prolactin-secreting pituitary adenomas (micro- and macroprolactinomas), idiopathic hyperprolactinemia or empty Turkish saddle syndrome with associated hyperprolactinemia, which are the main pathological conditions that cause the aforementioned clinical manifestations.

Application

Dostinex is intended for oral administration. since in clinical trials dostinex was used mainly with food and the tolerance of this class of preparations when taken with food improves, the preparation is recommended to be taken with food for all therapeutic indications.

Inhibition / suppression of physiological lactation. Dostinex should be used within 1 day after childbirth. The recommended therapeutic dose is 1 mg (2 tablets of 0.5 mg), which is taken once.

To suppress the already established lactation, the recommended therapeutic dosage regimen is 0.25 mg (½ tablet of 0.5 mg) every 12 hours for 2 days (total dose - 1 mg). Such a dosing regimen for suppressing lactation is better tolerated by women than taking a single dose, and is accompanied by a lower incidence of adverse events, especially symptoms of arterial hypotension.

Treatment of hyperprolactinemic conditions. The recommended starting dose of Dostinex is 0.5 mg once a week or ½ a 0.5 mg tablet 2 times a week (for example, on Monday and Thursday). The increase in the weekly dose should be carried out gradually, preferably increasing it by 0.5 mg / week every month until optimal therapeutic efficacy is achieved. Typically, the therapeutic dose is 1 mg / week and can range from 0.25 to 2 mg / week. For the treatment of patients with hyperprolactinemia, Dostinex was used in doses up to 4.5 mg / week.

The maximum dose of the preparation should not exceed 3 mg / day.

The weekly dose of the preparation can be taken 1 time or divided into 2 or more doses per week, depending on the patient's tolerance to the preparation. If the prescribed doses exceed 1 mg / week, it is recommended to divide the weekly dose into several doses, since the tolerability of the preparation in a dose exceeding 1 mg when taken as a single weekly dose has been assessed in only a few patients.

When the dose is increased, the patient should be examined to determine the minimum dose of the preparation that has a therapeutic effect. After an effective therapeutic dosing regimen has been selected, it is recommended to carry out regular (monthly) determination of plasma prolactin levels, since the normalization of these levels usually occurs within 2 or 4 weeks.

After discontinuation of Dostinex, a relapse of hyperprolactinemia usually develops. However, in some patients, prolactin levels persisted for several months. In 23 of 29 women in the follow-up group, ovulatory cycles lasted longer than 6 months after discontinuation of Dostinex.

Elderly patients. The experience of using the preparation in elderly patients is very limited due to the proposed indications for the use of Dostinex. Available data indicate no particular risk.

Contraindications

Hypersensitivity to cabergoline, any excipients of the preparationor ergot alkaloids. uncontrolled ag. a history of fibrotic diseases of the lungs, pericardium and retroperitoneal space. for long-term treatment: signs of damage to the heart valves, which are determined using echocardiography before starting treatment (see special instructions).

Side effects

In general, adverse events depend on the dose of the preparation. in patients with known intolerance to dopaminergic preparations, the likelihood of adverse events can be reduced by starting treatment with Dostinex with reduced doses, for example 0.25 mg once a week, followed by a gradual increase until the therapeutic dose is reached. in the event of persistent or severe side effects, a temporary decrease in the dose followed by a more gradual increase, for example, by 0.25 mg / week every 2 weeks, can improve the tolerability of the preparation.

During treatment with Dostinex, the following adverse reactions were noted and reported with the following frequency: very often ≥1 / 10; often: ≥1 / 100 and 1/10; infrequently ≥1 / 1000 and 1/100; rarely ≥1 / 10,000 and 1/1000; very rarely 1 / 10,000; the frequency is unknown (cannot be estimated from the available data).

common data

From the side of the vessels: often - Dostinex as a whole causes a hypotensive effect in patients receiving long-term treatment; postural arterial hypotension; infrequently - peripheral vasospasm, loss of consciousness.

From the musculoskeletal system and connective tissue: infrequently - cramps in the lower extremities; rarely - muscle weakness.

On the part of the skin and subcutaneous tissues: infrequently - skin reactions, such as alopecia, itching, rash; rarely - allergic skin reactions.

Laboratory tests: infrequently - in women with amenorrhea, a decrease in hemoglobin levels was noted during the first few months after menstruation.

Hyperprolactinemic conditions

From the side of the psyche: often - depression, sleep disturbance; the frequency is unknown - aggression, hypersexuality, pathological addiction to gambling, increased libido.

From the nervous system: very often - dizziness / vertigo, headache; infrequently - paresthesia; frequency unknown - sudden falling asleep, fainting.

From the side of the vessels: often - hot flashes.

From the digestive system: very often - abdominal pain, dyspepsia, gastritis, nausea; often constipation, vomiting.

From the reproductive system and mammary glands: often - pain in the mammary glands.

General disorders and reactions at the injection site: very often - asthenia, increased fatigue.

Inhibition / suppression of lactation

From the nervous system: often - dizziness / vertigo, headache, drowsiness; infrequently - fainting.

From the side of the cardiovascular system: very often - lesions of the heart valves (including regurgitation) and similar disorders (pericarditis and pericardial effusion); infrequently - heart palpitations, nosebleeds, decreased hemoglobin levels in women with amenorrhea after menstruation has been restored. Asymptomatic decrease in blood pressure can usually occur once during the first 3-4 days after delivery.

From the respiratory system, chest and mediastinal organs: infrequently - pleural effusion, pulmonary fibrosis.

From the digestive system: often - abdominal pain, nausea; infrequently - vomiting; rarely - pain in the epigastric region.

Laboratory tests: often - asymptomatic decrease in blood pressure (≥20 mm Hg - systolic and ≥10 mm Hg - diastolic).

From the vascular system: often - hot flashes.

General disorders and reactions at the injection site: infrequently - asthenia.

From the side of the organ of vision: infrequently - transient hemianopsia; frequency unknown - visual impairment.

Post-marketing observations

From the immune system: frequency unknown - hypersensitivity reaction.

From the side of the psyche: infrequently - increased libido; frequency is unknown - nonsense.

From the side of the heart: very often - valve damage (including regurgitation) and similar disorders (pericarditis and pericardial effusion).

From the respiratory system, chest and mediastinal organs: the frequency is unknown - shortness of breath, respiratory failure, respiratory failure, pleural effusion, pulmonary fibrosis.

From the hepatobiliary system: the frequency is unknown - impaired liver function.

Skin and subcutaneous tissue disorders: infrequently - alopecia, rash.

General disorders and reactions at the injection site: frequency unknown - edema.

Laboratory tests: the frequency is unknown - an increased level of CPK in the blood.

Violation of impulse control. Pathological gambling, increased libido, hypersexuality, compulsive desire to spend and buy, bulimia and binge eating disorder may occur in patients treated with dopamine agonists, including Dostinex.

Also during clinical trials, adverse reactions were noted such as nervousness, dysmenorrhea, acne, pain, arthralgia, rhinitis, dry mouth, diarrhea, bloating, throat irritation, toothache, symptoms similar to colds, periorbital edema, peripheral edema, anorexia, insomnia, weight gain / loss, impaired concentration, agitation.

special instructions

General. the safety and efficacy of Dostinex has not yet been established in patients with kidney and liver disease. Like other ergot derivatives, Dostinex should be used with caution in patients with severe cardiovascular disease, Raynaud's syndrome, renal failure, ulcer or gastrointestinal bleeding, as well as a history of serious, especially psychotic, mental disorders. you should be especially careful if patients are taking a psychotropic preparation at the same time.

In patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption, this preparation should not be used.

Symptomatic arterial hypotension can develop when using Dostinex for any indication. Dostinex should be used with caution along with other preparations that lower blood pressure.

The effect of alcohol on the overall tolerability of the preparation is currently unknown.

Before using the preparation Dostinex, pregnancy should be excluded, and after the end of treatment, pregnancy should be prevented for at least 1 month.

Liver failure. Consideration should be given to the use of the preparation in low doses for patients with severe hepatic impairment receiving long-term treatment with Dostinex. In patients with severe hepatic impairment (class C on the Child-Pugh scale) who received a single dose of the preparation (1 mg), there was an increase in AUC compared to healthy volunteers and patients with less severe hepatic impairment.

Postural hypotension. After using the preparation Dostinex, orthostatic arterial hypotension may occur. Caution should be exercised when using this preparation simultaneously with other preparations that lower blood pressure.

Sleepiness / sudden falling asleep. Dostinex has been associated with drowsiness. Dopamine agonists can be the cause of falling asleep episodes in patients with Parkinson's disease. Infrequent cases of sudden falling asleep during daily activities have been reported, sometimes without realizing it or without warning signs. The above information should be provided to patients and advised to be careful when driving or working with other automated systems during the period of treatment with cabergoline. Patients who experience drowsiness and / or episodes of sudden falling asleep should refrain from driving vehicles or working with other automated systems. In addition, in these cases, the advisability of reducing the dose of the preparationor discontinuing treatment may be considered (see Ability to influence the reaction rate when driving or operating other mechanisms).

Violation of impulse control. The condition of patients should be systematically monitored for the occurrence of impulse control disorders. Patients and caregivers should be advised that behavioral symptoms of impulse control disorders, in particular pathological gambling, increased libido, hypersexuality, compulsive spending and buying, bulimia and binge eating disorder, may occur in patients. receiving treatment with dopamine agonists, in particular cabergoline. In case of development of such symptoms, the possibility of dose reduction / gradual discontinuation of the dpreparation should be considered.

Inhibition / suppression of physiological lactation. Like other ergot derivatives, Dostinex should not be used in women with pregnancy-related hypertension, such as preeclampsia or postpartum hypertension, unless the potential benefit is considered to outweigh the potential risk.

In studies of the use of the preparation Dostinex in the postpartum period, the decrease in blood pressure was predominantly asymptomatic and often a single dose 2–4 days after the start of treatment. Since a decrease in blood pressure is often noted in the postpartum period, regardless of preparation treatment, it is likely that a significant number of reported cases of a decrease in blood pressure after taking Dostinex are not due to the effect of the preparation. However, periodic monitoring of blood pressure is recommended, especially during the first few days after taking cabergoline.

To avoid possible postural hypotension, a single dose of Dostinex should not exceed 0.25 mg for women who are breastfeeding and taking a preparation to suppress established lactation. In a clinical study to assess the efficacy and tolerability of a single dose of Dostinex 0.5 mg to suppress lactation, it was found that the risk of side effects in this indication is approximately doubled if the preparation is used as a single dose of 0.5 mg.

Treatment of hyperprolactinemic conditions. Before starting treatment with Dostinex, a complete examination of the pituitary gland is shown, since hyperprolactinemia, accompanied by amenorrhea / galactorrhea and infertility, can be caused by a pituitary tumor.

Dostinex restores ovulation and fertility in women with hyperprolactinemic hypogonadism.

Since pregnancy can occur before the menstrual cycle is restored, it is recommended that a pregnancy test be performed at least every 4 weeks during the amenorrhea period, and after menstruation has been restored, with a delay of more than 3 days. Women who want to avoid pregnancy should be advised to use mechanical contraception during treatment with Dostinex and after stopping treatment with this preparation until anovulation reappears. As a precaution, women who become pregnant should be monitored for signs of enlargement of the pituitary gland, since there is the possibility of an increase in the volume of an already existing pituitary tumor during pregnancy.

Before using the preparation Dostinex, it is necessary to exclude the presence of pregnancy. Women wishing to become pregnant are advised to discontinue treatment with Dostinex 1 month before the planned fertilization when a regular ovulatory cycle appears as a precautionary measure, since clinical experience with the preparation is still quite limited and the preparation is characterized by a long T½. If pregnancy occurs during treatment, cabergoline should be discontinued.

It is recommended to conduct regular gynecological examinations, in particular cytological examinations of the cervix and endometrium, in patients taking Dostinex for a long period.

Fibrosis, valvular heart disease and possible similar clinical events. Fibrous and serous inflammatory disorders such as pleurisy, pleural effusion, pleural fibrosis, pulmonary fibrosis, pericarditis, pericardial effusion, damage to one or more heart valves (aortic, mitral, and tricuspid), or retroperitoneal fibrosis have occurred after prolonged use of spinal alkaloids with an agonistic effect on the 5HT2B serotonin receptor, such as Dostinex. In some cases, symptoms or manifestations of lesions of the heart valves may decrease after you stop taking Dostinex.

In combination with pleural effusion / fibrosis, an excessive increase in ESR occurred. In the case of an increase in ESR of unknown etiology, which deviates significantly from the norm, it is recommended to conduct an X-ray examination of the chest organs.

Valve lesions are associated with preparation buildup, and patients should be treated with low effective doses. At each visit, the safety profile of patients treated with Dostinex should be re-evaluated to determine the appropriateness of continuing treatment.

Before starting long-term treatment, all patients should undergo a cardiovascular examination, in particular echocardiography, to determine the possible presence of asymptomatic heart disease. Before starting treatment, it is also advisable to determine the indicators of the initial level of ESR or other markers of inflammation, pulmonary function / chest x-ray and renal function. It is not known whether treatment with cabergoline can worsen disease in patients with valvular regurgitation. If a patient has fibrotic heart valve disease, it is not recommended to continue treatment with Dostinex (see CONTRAINDICATIONS).

During long-term treatment, fibrotic diseases can develop asymptomatically, therefore, patients should be regularly monitored for possible manifestations of fibrosis progression. So, during treatment, you should pay attention to the following signs and symptoms:

diseases of the lungs and pleura such as dyspnea, shortness of breath, persistent cough, or chest pain;

renal failure or obstruction of the ureteral / abdominal vessels, which may manifest as lower back / side pain and swelling of the lower extremities, as well as any possible abdominal mass or tenderness that may indicate retroperitoneal fibrosis;

heart failure: Cases of valvular or pericardial fibrosis often manifest as heart failure. In this regard, when such symptoms appear, the presence of valvular fibrosis (and constrictive pericarditis) should be excluded.

Conducting clinical diagnostic monitoring of the development of fibrotic diseases in the prescribed manner is mandatory. The first echocardiogram should be done within 3–6 months after starting treatment, after which the frequency of echocardiographic examinations should be determined by appropriate individual clinical examination, with particular attention to the above signs and symptoms, but at least every 6–12 months.

Dostinex should be discontinued if the echocardiogram shows signs of new or worsening existing valvular regurgitation, valve restriction or valve leaflet hardening (see CONTRAINDICATIONS).

The need for other clinical examinations (for example, physical examination, including cardiac auscultation, radiography and computed tomography) should be determined individually for each patient.

Appropriate additional studies, including ESR and plasma creatinine levels, should be performed as needed to confirm the diagnosis of fibrotic disease.

During pregnancy and breastfeeding. Before starting the use of Dostinex, pregnancy should be excluded, and after the end of treatment, pregnancy should be prevented for at least 1 month.

When a regular ovulatory cycle appears, women wishing to become pregnant should stop treatment with cabergoline 1 month before the planned fertilization. This will prevent the possible effect of the preparation on the fetus and will not interfere with the possibility of fertilization, since ovulatory cycles continue in some cases for 6 months after the preparation is discontinued. If fertilization occurs during treatment, the preparation should be discontinued as soon as pregnancy is confirmed in order to limit the effect of the preparation on the fetus.

Mothers should be advised not to breastfeed if Dostinex did not inhibit / suppress lactation. Since the preparation prevents lactation, Dostinex should not be used in mothers with hyperprolactinemic conditions who wish to breastfeed.

Children. The safety and efficacy of Dostinex in patients under the age of 16 has not been studied.

The ability to influence the reaction rate when driving or operating machinery. During the first days of using Dostinex, patients should be warned against engaging in activities that require quick and accurate responses, such as driving or working with other automated systems.

Patients taking Dostinex and who develop drowsiness should be advised to refrain from driving or from activities in which a lack of vigilance could expose themselves and others to the danger of serious injury or death (work with automated systems), unless patients are able to overcome drowsiness.

Interactions

Concomitant use of the preparation dostinex with other preparations, especially with ergot alkaloids, in the postpartum period was not associated with obvious interactions that altered the efficacy and safety of this preparation.

Despite the fact that there is no data on the interaction of cabergoline with other ergot alkaloids, the simultaneous use of these preparations during long-term treatment with Dostinex is not recommended.

Since Dostinex realizes its therapeutic effect by direct stimulation of dopamine receptors, its simultaneous use with dopamine receptor antagonists (for example, phenothiazines, butyrophenones, thioxanthenes and metoclopramide) is not recommended, since these preparations can reduce the prolactin-lowering effect of cabergoline.

Like other ergot derivatives, Dostinex should not be used with macrolide antibiotics (eg erythromycin) due to the increased systemic bioavailability of cabergoline.

Overdose

Overdose symptoms may be similar to those resulting from overstimulation of dopamine receptors (eg, nausea, vomiting, stomach upset, postural hypotension, confusion / psychosis, or hallucinations).

If necessary, supportive measures should be taken to remove any residual unabsorbed preparation and maintain blood pressure. In addition, it may be advisable to administer preparations of the dopamine antagonist group.

Storage conditions

At a temperature not exceeding 25 ° c.

Tags: Dostinex

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