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PubMed2001

Resistance to cabergoline as compared with bromocriptine in hyperprolactinemia: prevalence, clinical definition, and therapeutic strategy.

To evaluate the prevalence of resistance to cabergoline treatment, we studied 120 consecutive de novo patients (56 macroadenoma, 60 microadenoma, 4 nontumoral hyperprolactinemia) treated with cabergoline (CAB) compared with 87 consecutive de novo patients (28 macroadenoma, 44 microadenoma, 15 nontumoral hyperprolactinemia) treated with bromocriptine (BRC) for 24 months. Resistance was evaluated as inability to normalize serum PRL levels (first end point) and to induce tumor shrinkage (second end point). After 24 months, PRL normalization and tumor shrinkage after CAB and BRC treatments, respectively, were obtained in 82.1% and 46.4% of macroprolactinomas (P < 0.001) and in 90% vs. 56.8% of microprolactinomas (P < 0.001). The median doses of CAB and BRC able to fulfill the two criteria of treatment success were 1 mg/wk and 7.5 mg/d in macroprolactinomas, 1 mg/wk and 5 mg/d in microprolactinomas, and 0.5 mg/wk and 3.75 mg/d in nontumoral hyperprolactinemia. Hyperprolactinemia persisted in 17.8% of macroprolactinomas, 10% of microprolactinomas, and after CAB at doses of 5-7 mg/wk and in 53.6% of macroprolactinomas, 43.2% of microprolactinomas, and 20% of nontumoral hyperprolactinemic patients, after BRC at doses of 15-20 mg/d. In these resistant macro- and microprolactinomas, the maximal tumor diameter was reduced by 43.7 +/- 3.6% and 22.1 +/- 3.7% and by 59.3 +/- 7.1% and 4.3 +/- 2.1% after CAB and BRC, respectively (P < 0.001). In conclusion, long-term CAB treatment induced the successful control of hyperprolactinemia associated with tumor shrinkage in a higher proportion of patients than did BRC treatment. In a small number of patients (i.e. 17.8% of macroprolactinomas and 10% of microprolactinomas), however, CAB treatment did not normalize serum PRL levels despite reducing tumor mass, even at very high doses. Therefore, an absence of tumor shrinkage cannot be considered as end point to indicate resistance to CAB, and increasing the dose of CAB higher than 3 mg/wk does not seem to be helpful in controlling PRL hypersecretion.

Adenoma↗
PubMed2004

Effective cabergoline treatment in idiopathic restless legs syndrome.

OBJECTIVE: To assess the efficacy and safety of the dopamine agonist cabergoline (CAB) in patients with restless legs syndrome (RLS). METHODS: Patients with moderate to severe RLS were randomized into four groups receiving placebo, 0.5 mg, 1 mg, or 2 mg CAB once daily in a double-blind, placebo-controlled, multicenter dose-finding trial followed by an open long-term extension trial of 47 weeks. Efficacy was assessed with the RLS-6 scales and International RLS Study Group severity scale (IRLS). RESULTS: A total of 85 patients (age 56 +/- 10 years, 71% females) were treated. Severity of RLS-6 scale symptoms during the night (the primary endpoint) was markedly improved by all CAB doses compared to placebo (placebo: -1.4 +/- 3.1, 0.5 mg CAB: -4.2 +/- 3.0 [p = 0.0082], 1.0 mg CAB: -4.0 +/- 2.9 [p = 0.0040], 2.0 mg CAB: -4.8 +/- 3.7 [p = 0.0026]). Similar results were found for the RLS severity at bedtime and during the day, IRLS, and satisfaction with sleep. A stable, clinically relevant improvement was achieved in all efficacy measures (severity during the night: change between last assessment and baseline: -5.6 +/- 2.5, rate of remission: 71.2%) throughout 1 year with a mean CAB dose of 2.2 mg per day. During long-term treatment, 6 of 66 treated patients were affected (n = 2) or possibly affected (n = 4) by mild augmentation. Under CAB therapy up to 1 year, 11 of 85 patients discontinued treatment due to a drug-related adverse event. CONCLUSIONS: Cabergoline is an efficacious and well-tolerated option for the treatment of restless legs symptoms during the night and the day.

Aged↗
PubMed1992

Excretion balance and urinary metabolic pattern of [3H]cabergoline in man.

After oral administration of [3H]cabergoline to man at a single nominal dose of 0.6 mg/subject radioactivity is mainly eliminated by the faecal route (72% of the dose after 10 days). Urine contains 18% of the dose after the same period. The unchanged drug and metabolites present in urine were identified by comparison with reference compounds and quantified by radio-TLC analysis. Cabergoline is extensively metabolized. Unchanged drug in 0-24 h urine represents less than 14% of urinary radioactivity, reaching 20% in 0-96 h urine. The acid derivative FCE 21589 is the main metabolite, amounting to 38% and 30% of the urinary radioactivity in 0-24 h and 0-96 h urine, respectively. The amide derivative FCE 21590 appears to be present in only a small amount, accounting for no more than 4% of the urinary radioactivity in the urine of the first 24 hours after administration and increasing to about 8% in the 0-96 h urine.

Adult↗
PubMedDate not supplied

LHRH-induced gonadotropin release before and after short-term therapy with cabergoline in hyperprolactinaemic patients.

Cabergoline is a new ergot derivative with long-lasting PRL lowering effect. Basal and LHRH stimulated (50 micrograms i.v.) gonadotropin secretion was evaluated before and during cabergoline treatment (0.5-2 mg/week) in 28 women with pathological hyperprolactinaemia. After 4 weeks, PRL and E2 were significantly (p less than 0.01) reduced and increased, respectively. Basal LH and FSH levels did not change. Both LH (p less than 0.05) and FSH (p less than 0.02) responsiveness to LHRH was decreased from the former to the latter test. The study underlines drug-induced variations in gonadotropin responsiveness to LHRH which are probably due to variations in the steroid milieu.

Adolescent↗
PubMed1995

X-ray crystal structure and conformational analysis of N-(3-dimethylaminopropyl)-N-(ethylaminocarbonyl)-6-(2-propenyl)er goline -8 beta-carboxamide (Cabergoline): comparison with bromocriptine and lisuride and a hypothesis for its high dopaminergic activity.

The crystal structure of Cabergoline, a potent and long lasting prolactin lowering agent interacting with the D2 dopamine receptors, has been determined by X-ray diffraction data. The structural data represent the starting point for a computational study, where the molecular mechanisms approach was used to explore the motion of all unconstrained torsion angles. Two different conformations related to energetic minima have been found, one of them in agreement with the experimental crystal structure. Both conformations are shape compared with Bromocriptine and Lisuride, two dopaminergic ergoline derivatives with C-8 beta and C-8 alpha substituents of the ergoline ring, respectively. We observe that the C-8 beta Cabergoline assumes the overall three-dimensional features of C-8-alpha-ergolines in one of its low-energy conformations.

Bromocriptine↗
PubMed1993

Reproduction in a feral cat population and its control with a prolactin inhibitor, cabergoline.

A feral cat population (12 females, 13 males) was observed almost daily for 6 years, at a location 40.53 degrees N and 74.29 degrees W. Cats were accustomed to twice-daily feeding. Oestrous behaviour was seasonal and started in early January, irrespective of climatic conditions, with peak levels of oestrous activities in late January and February. Of all 60 heat periods observed, and conceptions recorded, the percentage occurrence was 58 and 49 in the first quarter, and 29 and 33, 12 and 16 and 1 and 2 in the second, third and fourth quarter, respectively. Queens could be reliably identified as being pregnant by 31.5 +/- 5.82 days, and were subjected between days 36 and 57 of gestation to daily oral treatment with 5-15 micrograms cabergoline kg-1 placed on food. Treatments (n = 41) from days 36 +/- 6.17 to 40.8 +/- 6.96 resulted in abortion in all animals on day 40.5 +/- 6.19; if treatment started as late as day 48.5, and lasted 9 or more days, premature parturition occurred. As cabergoline had caused mammary gland regression within 36-48 h, litters could not be nursed and perished quickly. Five repeatedly aborted queens were subsequently allowed to go to term. Pregnancies, gestation length (64.5 days), parturitions, maternal care and lactations were normal. Of the 24 kittens born out of seven pregnancies, 16 were observed from 6 months to 3 years. Pubertal oestrus and first conceptions occurred at 189.9 days (range 150-214 days) and 212.0 days (155-277 days), respectively. Males were seen to achieve reproductive success in their third year only.

Abortifacient Agents↗
PubMed1997

Termination of dioestrus and induction of oestrus in dioestrous nonpregnant bitches by the prolactin antagonist cabergoline.

The effects of treatment with a dopamine agonist from day 30 after the LH surge of a nonpregnant oestrous cycle were analysed in five bitches previously demonstrated to be fertile. Five untreated nonpregnant bitches were studied as controls. Cabergoline was given (5 micrograms kg-1 body weight) daily from day 30 after the LH peak until +/- 2 days after the first sign of pro-oestrus. Cabergoline decreased progesterone concentrations to < 1 ng ml-1 within 15-20 days. Four of the five treated bitches came into pro-oestrus after a mean of 29.75 +/- 5 days of treatment, at 66.5 +/- 7.1 days after the previous LH surges. The previous and following interoestrous intervals in the treated and responding animals were 216 +/- 6 and 66.5 +/- 7.1 days, respectively, and were significantly different (P < 0.05). In untreated animals, interoestrous intervals were longer (P < 0.05) than in treated animals, and not different from previous interoestrous intervals. The duration of pro-oestrus and oestrus was normal in the induced oestrous cycle compared with previous or untreated cycles in both groups. Variations in progesterone in the induced cycles were not different from those in control cycles. Prolactin concentrations were lower (P < 0.05) in treated animals compared with untreated animals. All bitches mated. However, none of the treated bitches became pregnant at the induced oestrous cycle. Lack of fertility was presumably due to the inability of the uterus to receive the embryos and was related to insufficient uterine involution and regeneration. Nevertheless, this study demonstrates that it is possible to induce oestrus not only in anoestrus but also in dioestrous nonpregnant bitches using a D2 dopamine agonist.

Animals↗
PubMed1987

Inhibition of lactation in the Beagle bitch with the prolactin inhibitor cabergoline (FCE 21336): Dose response and aspects of long-term safety.

Sixteen healthy, lactating Beagle bitches with litters of three to six pups were assigned to four treatment groups for one daily oral treatment of cabergoline in an oily solution (0, 1.25, 2.50 or 5.0 mcg/kg body weight (BW) for 5 d, commencing on Day 8 of lactation. Bitches and all their puppies were weighed daily for 2 d before treatments started, and for 10 d thereafter. Technicians rated daily treatment effects on maternal health, maternal behavior and mammary glands, using a scoring system. Treatments had no effect on maternal health, maternal body weight, and maternal behavior. Treatments with the two higher doses caused a reaction and a regression of the mammary glands in a dose-related fashion, resulting in cessation of lactation with 5 mcg/kg BW. Maternal treatment did not adversely affect the puppies' health, and no puppy was lost during the trial. However, average daily weight gains of puppies declined with increasing levels of cabergoline, causing significant weight losses in the 2.5 and 5 mcg/kg treatment group. This became evident after 2 d of treatment. To save the puppies in the highest dosage group, hand-feeding, and later, crossfostering, had to be used with all litters, starting on Day 3 or 4 of treatment. Weight losses were dose-related with an ED(50) of 1.5 mcg/kg/d and persisted for at least 24 h after treatment had ceased. Since puppies were left with their mothers to provide a continued suckling stimulus, lactation rebounded in all bitches treated with 2.5 mcg/kg, but only in two of four bitches treated with 5 mcg/kg. All bitches returned to estrus at their normal intervals. Fertility and fecundity at the next breeding were undisturbed.

Journal Article↗
PubMed2005

Pleural effusion and thickening due to cabergoline use in a patient with Parkinson's disease.

A 62-year-old Caucasian man with a history of Parkinson's disease developed bilateral pleural thickening and a large, right-sided, exudative pleural effusion. Further investigations revealed a chronic inflammatory process involving the pleura as a result of exposure to cabergoline used to treat the Parkinson's disease. The inflammatory process reversed after the discontinuation of cabergoline.

Journal Article↗
PubMed1999

Cabergoline: a first-choice treatment in patients with previously untreated prolactin-secreting pituitary adenoma.

Cabergoline (CAB) treatment is an effective, safe and well tolerated approach for hyperprolactinemia. We investigated the efficacy of 24-month treatment with CAB in 37 patients with previously untreated PRL-secreting pituitary adenoma and evaluated the hormonal and neuroradiological changes after the discontinuation of long-term therapy. Eleven patients with macroprolactinoma (1M/10F) and 26 with microprolactinoma (4M/22F) started treatment taking 0.25 mg CAB twice a week for 4 weeks. The dose was increased stepwise in 0.5 mg increments until reaching lowest maximally effective and tolerated dose. CAB was withdrawn before the end of the study in 6 women who became pregnant and in one patient who showed a slight increase of the macroadenoma at MRI. During treatment, PRL levels decreased significantly in macro (11.1+/-1.1 vs 407.8+/-98.3 microg/l, p<0.001) and microprolactinomas (11.1+/-1.6 vs 193.8+/-23.4 microg/l, p<0.05) and normalized in all macro and in 23/26 microprolactinomas. In 3 cases PRL levels decreased but did not normalize because the appearance of side effects, such as nausea or hypotension, prevented the increase of the dose of CAB. The effective dose of drug correlated significantly with basal serum PRL levels (p<0.05) and with the pituitary tumor size (p<0.05). A significant decrease of the mean adenoma size was evident for macro (6.9+/-1.8 vs 16.0+/-1.8 mm, p<0.001) and microprolactinomas (3.0+/-0.5 vs 6.5+/-0.4 mm, p<0.001) at MRI. The tumor disappeared in 4 macroadenomas and in 11 microadenomas after 12 months of treatment. CAB withdrawal was followed by serum PRL increase in 13 cases after 3 months, in 6 after 6 months, in 2 after 9 months, and in one patient at the 12th month. Five patients showed normoprolactinemia with negative MRI after one year. Regular menses were restored in 7/10 macroprolactinomas and in all oligo-amenorrhoic patients with microadenoma; serum testosterone levels normalized in 2/3 hypogonadic men. Five out of 6 women become pregnant and had uneventful pregnancies which resulted in deliveries of normal babies. In conclusion, this study confirms the effectiveness and safety of CAB for patients with PRL-secreting pituitary adenoma and suggests that it can be considered a first choice treatment.

Adolescent↗
PubMedDate not supplied

A randomized cross-over study comparing cabergoline and quinagolide in the treatment of hyperprolactinemic patients.

Quinagolide (QUI) and cabergoline (CAB) are dopamine agonists recently introduced for the treatment of hyperprolactinemia. In the present study, these drugs have been compared in terms of effectiveness and tolerability. Twenty patients (18 females and 2 males) with hyperprolactinemia (8 with microprolactinomas, 6 with idiopathic hyperprolactinemia and 6 with empty sella turcica syndrome) were treated with oral QUI (75 microg once daily) and CAB (0,5 mg twice weekly), in a randomized cross-over trial with placebo between both drugs. Each drug was administered for 12 weeks, separated by other 12 weeks with placebo. PRL levels decreased with both drugs at 2 or 4 weeks of starting the treatment, without differences between both drugs at weeks 4, 8 and 12. At week 12, normal PRL levels (<20 ng/ml) were attained in 90% patients with CAB and only in 75% patients with QUI (p<0.05). After discontinuation of treatment, significant increase in serum PRL was higher after QUI withdrawal than after CAB. Clinical efficacy of both treatments was similar in terms of improvement amenorrhea, oligomenorrhea, galactorrhea, and impotence. All patients completed both cycles of treatment, and the most frequent side-effects were nausea, headache and dizziness, without significant differences between CAB (30%) and QUI (55%). Our study indicates that, at the doses employed here, CAB showed a high percentage of patients with normal PRL at the end of treatment and long-lasting efficacy in the levels of PRL. Clinical response and side-effects were similar in both drugs.

Adult↗
PubMed2002

Macroprolactinoma associated with Cushing's disease, successfully treated with cabergoline.

Multiple pituitary hormone hypersecretions have already been described, but the co-occurrence of PRL and ACTH excess is very rare. To our knowledge, medical treatment with cabergoline only, avoiding pituitary surgery and radiotherapy in this type of tumor has never been reported before. This case report deals with a 31-yr-old man affected with a macroprolactinoma associated with a florid clinical image of Cushing's disease. Normalization of the prolactin levels and the disappearance of clinical and biochemical features of Cushing's disease were obtained after administration of medical treatment only.

Adrenocorticotropic Hormone↗
PubMed1997

Use of cabergoline in the long-term treatment of hyperprolactinemic and acromegalic patients.

Cabergoline (Cab), a very potent and long-lasting dopaminergic compound, was administered to 26 women with pituitary microprolactinoma [mean serum PRL levels: 124.8 +/- 11.3 micrograms/l (+/- SE), range 62-300 micrograms/l] and 3 patients with GH-secreting pituitary adenoma (2 with associated PRL hypersecretion) for 12 and 24 months, respectively. In microprolactinomas, a stable normoprolactinemia was achieved in 96.1% of cases: in 13 women (50%) with the lowest dose of the drug (0.5 mg/week), and in other 12 patients (46.1%) with increasing doses up to 3 mg/week. All the oligomenorrheic/amenorrheic women, except one, restored regular and ovulatory menses. Two patients became pregnant. Pituitary abnormalities at high resolution-CT (HR-CT) scan disappeared in 13 of 19 patients (68.4%) after 12 months of therapy and this feature persisted in 8/13 cases (61.5%) 12 months after drug withdrawal. During Cab discontinuation (range: 3-60 months), mean serum PRL levels remained significantly lower than the basal ones. Six of 25 women are still without therapy. In 2 patients, normoprolactinemia persisted up to 38 and 60 months, respectively. Cab treatment was re-instituted in 13 patients because of the recurrence of hyperprolactinemia. Five patients were lost at follow up. In all the acromegalic patients, Cab (1-3 mg/week) normalized serum GH, IGF-I and PRL levels. A clear improvement in clinical symptoms was observed in all patients, but neuroradiological improvement in only one. Cab therapy was very well tolerated, as only seven patients complained of mild and transient side-effects and none had to stop treatment. In conclusion, Cab is an effective, safe, and well tolerated dopaminergic compound for the treatment of hyperprolactinemic disorders and the control of the clinical and hormonal features of dopamine-sensitive acromegalic patients.

Acromegaly↗
PubMed1997

Long-term treatment with cabergoline, a new long-lasting ergoline derivate, in idiopathic or tumorous hyperprolactinaemia and outcome of drug-induced pregnancy.

Cabergoline (CAB), a new long-acting ergoline derivative, was shown to be very effective in reducing PRL levels in normal volunteers and in hyperprolactinemic patients. We evaluated the hormonal changes after discontinuation of long-term therapy with CAB as well as the safety of drug exposure during pregnancy both for mothers and babies. We therefore studied 48 patients (47 females and one male) with pathological hyperprolactinaemia (mean +/- SE, 117.2 +/- 15.2: median 73.2 micrograms/l), treated for 1-82 months (mean +/- SE, 28.3 +/- 3; median 18). After long-term treatment, CAB was withdrawn in 11 patients and PRL levels were persistently normal for almost 15 days and significantly lower (p < 0.05) than basal at 30, 45, 60, 90, 120 days. Three patients had normal PRL levels still at 45 days after treatment discontinuation. Nine patients became pregnant after 1-37 months (mean 12.4) of therapy. In two patients the pregnancy was interrupted spontaneously in one case and voluntarily in the other. In all but one patients after delivery or three-month breast feeding, PRL levels trended towards reduction. In two cases (one with microadenoma and one with idiopathic hyperprolactinaemia) PRL remained in the normal levels for 1-3 years after delivery. In conclusion CAB is able to inhibit plasma PRL levels for long time (up to 120 days) after withdrawal in patients with pathological hyperprolactinaemia treated with long-term therapy.

Adenoma↗
PubMed2004

Usefulness of switching to cabergoline from other dopamine agonists in patients with advanced Parkinson's disease.

Problems associated with long-term treatment of advanced Parkinson's disease (PD) include motor complications and psychotic and autonomic symptoms. We switched patients from bromocriptine (BR) or pergolide (PER) to cabergoline (CB) therapy and investigated CB's usefulness in alleviating such problems. Subjects were 30 patients (mean age 68.2 years; 13 receiving BR, 17 PER) with PD complicated by effects of long-term treatment but in whom their dose of dopamine (DA) agonist was contraindicated due to adverse reactions. Patients were switched to CB over a 2-4-week period. Hoehn-Yahr and Unified Parkinson Disease Rating Scale (UPDRS) I-IV "on" and "off" scores improved in both the BR and PER groups. CB was not discontinued due to adverse reactions in any patient. In conclusion, switching to CB is useful in patients in whom it is problematic to increase their dose of DA agonist due to motor complications or psychotic symptoms of advanced PD.

Aged↗
PubMed2003

Bedtime cabergoline in Parkinson's disease patients with excessive daytime sleepiness induced by dopamine agonists.

Excessive daytime somnolence is a common adverse effect of dopamine-agonist treatment of Parkinson's disease (PD). Many factors, such as age and sleep disturbances, could be involved in the pathogenesis of this phenomenon. However, pharmacokinetic factors have never been considered. In this open, prospective, pilot study, nine consecutive non-demented PD patients in early disease stages on monotherapy treatment with dopamine agonists and with no significant sleep problems, were enrolled. They were selected based on the presence of excessive daytime sleepiness induced by the dopaminergic treatment. A fast switch-over from the dopamine agonist currently used to a single equivalent dose of cabergoline, a long-acting dopamine agonist, administered at bedtime was performed. All patients were evaluated by means of UPDRS and Epworth Sleepiness Scale (ESS). A significant 70% reduction of daytime sleepiness was observed during the 3-month study compared with baseline. Data from this study suggest that both pharmacodynamic and pharmacokinetic mechanisms are involved in the pathophysiology of dopamine agonist-induced sleepiness.

Aged↗
PubMed2004

Pituitary apoplexy during therapy with cabergoline in an adolescent male with prolactin-secreting macroadenoma.

Pituitary adenomas are rare in young patients. Prolactinomas are the most common type of pituitary adenomas in children older than 12 years, occurring more often in girls, at a 4.5:1 female-to-male ratio. The clinical presentation may vary according to the age and sex of the patient. Pituitary apoplexy is a rare life-threatening condition caused by a sudden infarction or hemorrhagic necrosis of the pituitary containing an adenoma. A wide variety of conditions can trigger apoplexy such as pituitary irradiation, general anesthesia, traumatic head injury, pituitary stimulatory tests and a wide variety of medications including bromocriptine. We report a case of a 16-year-old male patient with puberty arrest harboring a macroprolactinoma, who developed a sudden clinical picture of pituitary apoplexy during the 12th month of treatment with cabergoline.

Adenoma↗