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Cabergoline for men & women: Dostinex (Know Your Medicine)

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Postural hypotension can occur following administration of cabergoline. Care should be exercised when administering cabergoline concomitantly with other drugs known to lower blood pressure. As expected for dopamine agonists, dose response for both efficacy and side effects appears to be linked to individual sensitivity. Optimization of dose should be obtained through slow initial dose titration, from starting doses of 1 mg daily. The dosage of concurrent levodopa may be gradually decreased, while the dosage of cabergoline is increased, until the optimum balance is determined. In view of the long half-life of the compound, increments of the daily dose of 0.5-1 mg should be done at weekly (initial weeks) or bi-weekly intervals, up to optimal doses.

As cabergoline suppresses milk production, you should not take it whilst breast feeding. It is often helpful to see whether your periods start again when you have stopped breast feeding, and reassess your prolactin levels, before deciding whether or not to resume cabergoline treatment. Sometimes microprolactinomas resolve after a pregnancy. Rarely, women with large macroprolactinomas will be advised to continue cabergoline treatment and not to breast feed. Your endocrinologist will discuss these decisions with you. Are there any medicines I should avoid when taking cabergoline? The pharmacokinetics of cabergoline seem to be dose-independent both in healthy volunteers (doses of 0.5-1.5 mg) and parkinsonian patients (steady state of daily doses up to 7 mg/day). On the basis of the elimination half-life, steady state conditions should be achieved after 4 weeks, as confirmed by the mean peak plasma levels of cabergoline obtained after a single dose (37 ± 8 pg/ml) and after a 4 week multiple regimen (101 ± 43 pg/ml).The pharmacokinetic and metabolic profiles of cabergoline have been studied in healthy volunteers of both sexes , in female hyperprolactinemic patients and in parkinsonian patients. After oral administration of the labelled compound, radioactivity was rapidly absorbed from the gastrointestinal tract as the peak of radioactivity in plasma was between 0.5 and 4 hours. Ten days after administration about 18/20% and 55/72% of the radioactive dose ( 3H-cabergoline/ 14C-cabergoline) was recovered in urine and faeces, respectively. Unchanged drug in urine accounted for 2-3% of the dose. Cabergoline crosses the placenta in rats, although it is unknown whether this is also true for humans. Animal studies have shown no embryo or foetal toxicity (Briggs, 2011) In controlled clinical trials, cabergoline given as a single 1 mg administration during the first day post-partum, was effective in inhibiting milk secretion, as well as breast engorgement and pain in 70 - 90% of the women. Less than 5% of women experienced rebound breast symptomatology during the third post-partum week (which was usually mild in severity).

Cabergoline has been associated with somnolence. Dopamine agonists can be associated with sudden sleep onset episodes in patients with Parkinson's disease. Sudden onset of sleep during daily activities, in some cases without awareness or warning signs, has been reported uncommonly. Patients must be informed of this and advised to exercise caution while driving or operating machines during treatment with cabergoline. Patients who have experienced somnolence and/or an episode of sudden sleep onset must refrain from driving or operating machines. Furthermore a reduction in dosage or termination of therapy may be considered. (See section 4.7) The recommended therapeutic dosage is 2 mg to 3 mg/day for patients with signs and symptoms of Parkinson's disease. Cabergoline should be given as a single daily dose.Cabergoline is a tablet treatment used to reduce the production of a hormone called prolactin by the pituitary gland (a gland at the base of the brain). If you have a prolactinoma (overproduction of prolactin by a cluster of cells in the pituitary), cabergoline treatment is also used to shrink the size of the swelling on the pituitary gland. How should I take cabergoline? Cardiac failure: cases of valvular and pericardial fibrosis have often manifested as cardiac failure. Therefore, valvular fibrosis (and constrictive pericarditis) should be excluded if such symptoms occur. The tablets should be taken with meals to reduce certain side effects such as nausea, vomiting and stomach pains. serious chest complaint (e.g. pain in the chest when breathing, fluid in the lungs, inflammation or infection of the lungs). Advise patients that side effects including excessive daytime sleepiness or sudden onset of sleep and hypotensive reactions may occur and that they should exercise caution when driving or operating machinery. They should be informed to refrain from driving or operating machinery until the effects have stopped recurring.

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