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A significant fraction of the administered dose undergoes a first-pass effect. The elimination half-life of Cabergoline estimated from urinary data of 12 healthy subjects ranged between 63 to 69 hours. The prolonged prolactin-lowering effect of Cabergoline may be related to its slow elimination and long half-life. Distribution: In animals, based on total radioactivity, Cabergoline (and/or its metabolites) has shown extensive tissue distribution. Radioactivity in the pituitary exceeded that in plasma by >100-fold and was eliminated with a half-life of approximately 60 hours. This finding is consistent with the long-lasting prolactin-lowering effect of the drug. Whole body autoradiography studies in pregnant rats showed no fetal uptake but high levels in the uterine wall. Significant radioactivity (parent plus metabolites) detected in the milk of lactating rats suggests a potential for exposure to nursing infants. The drug is extensively distributed throughout the body. Cabergoline is moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner. Concomitant dosing of highly protein-bound drugs is unlikely to affect its disposition. Metabolism: In both animals and humans, Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety, bodybuilding supplements dubai online. Cytochrome P-450 mediated metabolism appears to be minimal. Cabergoline does not cause enzyme induction and/or inhibition in the rat. Hydrolysis of the acylurea or urea moiety abolishes the prolactin-lowering effect of Cabergoline, and major metabolites identified thus far do not contribute to the therapeutic effect. Excretion: After oral dosing of radioactive Cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine. Nonrenal and renal clearances for Cabergoline are about 3. Urinary excretion in hyperprolactinemic patients was similar. Renal Insufficiency: The pharmacokinetics of Cabergoline were not altered in 12 patients with moderate-to severe renal insufficiency as assessed by creatinine clearance. Hepatic Insufficiency: In 12 patients with mild-to-moderate hepatic dysfunction (Child-Pugh score ?10), no effect on mean Cabergoline C max or area under the plasma concentration curve (AUC) was observed. However, patients with severe insufficiency (Child-Pugh score >10) show a substantial increase in the mean Cabergoline C max and AUC, and thus necessitate caution. Elderly: Effect of age on the pharmacokinetics of Cabergoline has not been studied. In 12 healthy adult volunteers, food did not alter Cabergoline kinetics. Dose response with inhibition of plasma prolactin, onset of maximal effect, and duration of effect has been documented following single Cabergoline doses to healthy volunteers (0.
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Each tablet contains either 1 mg or 2 mg of cabergoline. Cabaser also contains the following inactive ingredients: lactose leucine, bodybuilding supplements from uk
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