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The pharmacodynamic actions of cabergoline not linked to the therapeutic effect relate only to blood pressure decrease. The maximal hypotensive effect of cabergoline as a single dose usually occurs during the first 6 hours after drug intake and is dose-dependent both in terms of maximal decrease and frequency. 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. Ten days after administration about 18/20% and 55/72% of the radioactive dose ( 3 H-cabergoline/ 14 C-cabergoline) was recovered in urine and faeces, respectively. Unchanged drug in urine accounted for 2-3% of the dose. In urine, the main metabolite identified was 6-allyl-8b-carboxy-ergoline, which accounted for 4-6% of the dose. Three additional metabolites were identified in urine, which accounted overall for less than 3% of the dose. The metabolites have been found to be much less potent than cabergoline as D 2 dopamine receptor agonists in vitro. The low urinary excretion of unchanged cabergoline has been confirmed also in studies with non-radioactive product. The elimination half-life of cabergoline, estimated from urinary excretion rates, is long (63-68 hours in healthy volunteers, 79-115 hours in hyperprolactinemic patients). The pharmacokinetics of cabergoline seem to be dose-independent both in healthy volunteers (doses of 0. 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). In vitro experiments showed that the drug at concentrations of 0. Food does not appear to affect absorption and disposition of cabergoline. While renal insufficiency has been shown not to modify cabergoline kinetics, hepatic insufficiency of severe degree (> 10 Child-Pugh score, maximum score 12) has been shown to be associated with an increase of AUC. Almost all the findings noted throughout the series of preclinical safety studies are a consequence of the central dopaminergic effects or the long-lasting inhibition of PRL in rodents with a specific hormonal physiology different to man. Preclinical safety studies of cabergoline indicate a consistent safety margin for this compound in rodents and in monkeys, as well as a lack of teratogenic, genotoxic or carcinogenic potential. undefined MULTILOAD Cu (Multiload Intrauterine Device) releases levonorgestrel into the uterus, but only small amounts of the hormone reach your blood stream, buy turbovital (igf-1 lr3) 100 mcg peptides. 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