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2 X 0.5 mg
8 X 0.5 mg
General: Dostinex is to be administered by the oral route. Since the tolerability of this class of compounds is improved with food, it is recommended that Dostinex be preferably taken with meals for all the therapeutic indications. In patients known to be intolerant to dopaminergic drugs, the likelihood of adverse events may be lessened by starting therapy with DOSTINEX at reduced doses (e.g., 0.25 mg once a week) with subsequent gradual increase until the therapeutic dosage is reached. If persistent or severe adverse events occur, temporary reduction of dosage followed by a more gradual increase (e.g., increments of 0.25 mg per week every two weeks) may increase tolerability.
Inhibition/suppression of physiological lactation: For inhibition of lactation: Dostinex should be administered during the first day post-partum. The recommended therapeutic dosage is 1 mg (two 0.5 mg tablets) given as a single dose.
For suppression of established lactation: The recommended therapeutic dosage regimen is 0.25 mg (one half 0.5 mg tablet) every 12 hours for two days (1 mg total dose).
Treatment of hyperprolactinemic disorders: The recommended initial dosage of Dostinex is 0.5 mg per week given in one or two (onehalf of one 0.5 mg tablet) doses (e.g. on Monday and Thursday) per week. The weekly dose should be increased gradually, preferably by adding 0.5 mg per week at monthly intervals until an optimal therapeutic response is achieved. The therapeutic dosage is usually 1 mg per week and ranges from 0.25 mg to 2 mg per week. Doses of Dostinex up to 4.5 mg per week have been used in hyperprolactinemic patients. The weekly dose may be given as a single administration or divided into two or more doses per week according to patient tolerability. Division of the weekly dose into multiple administrations is advised when doses higher than 1 mg per week are to be given since the Dostinex, Israel 14 July 2010 tolerability of doses greater than 1 mg taken as a single weekly dose has been evaluated only in a few patients. Patients should be evaluated during dose escalation to determine the lowest dose that produces the therapeutic response. Monitoring of serum prolactin levels at monthly intervals is advised since, once the effective therapeutic dosage regimen has been reached, serum prolactin normalization is usually observed within two to four weeks. After Dostinex withdrawal, recurrence of hyperprolactinemia is usually observed. However, persistent suppression of prolactin levels has been observed for several months in some patients. In most women, ovulatory cycles persist for at least 6 months after Dostinex discontinuation.
Patients with Severe Hepatic Insufficiency: Lower doses of DOSTINEX should be considered in patients with severe hepatic insufficiency.
Children: Safety and efficacy of Dostinex has not been established in patients younger than 16 years.
Elderly: Dostinex has not been formally studied in elderly patients with hyperprolactinemic disorders.
For full details see prescribing information.
Hyperprolactinemia disorders, inhibition and and suppression of lactation.
Hypersensitivity to any ergot alkaloid, uncontrolled hypertension. History of pulmonary, pericardial and retroperitoneal fibrotic disorders. Anatomical evidence of cardiac valvulopathy of any valve (e.g., ECG showing valve leaflet thickening, valve restriction, valve mixed restriction-stenosis).
General: As with other ergot derivatives, Dostinex should be given with caution to subjects with severe cardiovascular disease, Raynaud’s syndrome, peptic ulcer or gastrointestinal bleeding, or with a history of serious, particularly psychotic, mental disorders. Particular care should be taken when patients are taking concomitant psychoactive medication. Before Dostinex administration, pregnancy should be excluded and after treatment pregnancy should be prevented for at least one month.
Hepatic Insufficiency: Lower doses should be considered in patients with severe hepatic insufficiency who receive prolonged treatment with DOSTINEX. Compared to normal volunteers and those with lesser degrees of hepatic insufficiency, an increase in AUC has been seen in patients with severe hepatic insufficiency (Child-Pugh Class C) who received a single 1 mg dose.
Postural Hypotension: Symptomatic hypotension can occur with Dostinex administration. Care should be exercised when administering Dostinex concomitantly with other drugs known to lower blood pressure.
Fibrosis/Valvulopathy: As with other ergot derivatives, pleural effusion/pulmonary fibrosis and valvulopathy have been reported following long-term administration of cabergoline. Some reports were in patients previously treated with ergotinic dopamine agonists. Therefore, Dostinex should be used with caution in patients with a history of, or current signs and/or clinical symptoms of, respiratory or cardiac disorders linked to fibrotic tissue. Erythrocyte sedimentation rate (ESR) has been found to be abnormally increased in association with pleural effusion/fibrosis. Chest x-ray examination is recommended in cases of unexplained ESR increases to abnormal values. Serum creatinine measurements can also be used to help in the diagnosis of fibrotic disorder Following diagnosis of pleural effusion/pulmonary fibrosis or valvulopathy, the discontinuance of cabergoline has been reported to result in improvement of signs and symptoms.
For full details see prescribing information.
Dizziness/vertigo, headache, nausea, abdominal pain. Somnolence/sudden sleep onset. May act as a vasoconstrictor. Digital vasospams and leg cramps have been reported.
Neuroleptics, dopamine antagonists, ergot alkaloids, macrolides, antihypertensives.
Pregnancy and Lactation
Studies in animal models have not demonstrated any teratogenic effect or effects on overall reproductive performance. However, there are no adequate and well-controlled studies in pregnant women. Dostinex should be used during pregnancy only if clearly needed. If conception occurs during therapy with Dostinex, discontinuation of treatment should be considered, after careful evaluation of the risks and benefits to mother and fetus. Pregnancy should be avoided for at least one month following discontinuation of treatment with Dostinex due to the long half-life of the drug and the limited data on in utero exposure, although the use of Dostinex at 0.5 to 2 mg/week for hyperprolactinemic disorders does not appear to be associated with an increased risk of abortion, premature delivery, multiple pregnancy or congenital abnormalities. In rats, cabergoline and/or its metabolites are excreted in milk. No information is available on the excretion in breast milk in humans; however, mothers should be advised not to breast-feed in case of failed lactation inhibition/suppression by Dostinex. Since it prevents lactation, Dostinex should not be administered to mothers with hyperprolactinemic disorders who wish to breast-feed their infants.
There is no experience in humans of overdose with Dostinex in the proposed indication: it is likely to lead to symptoms due to over-stimulation of dopamine receptors. These might include nausea, vomiting, gastric complaints, postural hypotension, confusion/psychosis or hallucinations. General supportive measures should be undertaken to remove any unabsorbed drug and maintain blood pressure if necessary. In addition, the administration of dopamine antagonist drugs may be advisable.