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PubMedDate not supplied

Pregnancy outcome after treatment with the ergot derivative, cabergoline.

The goal of this article is to assess the reproductive safety of cabergoline, a new ergot derivative proposed in hyperprolactinemic disorders. Investigated in different animal species, the drug showed no teratogenic or embryotoxic effects on rabbits. Considering the dose envisaged for humans, large safety margins exist. Our sample consists of 226 pregnancies occuring in 205 women. Follow-up is available for 204. There were 24 miscarriages and three abortions induced because of major malformations (one Down syndrome in a 42-year-old woman, one limb-body wall complex, one hydrocephalus). Two of the 148 single liveborn infants had significant malformations: one megaureter, one scaphocephaly. This series shows no increase in miscarriage rate, a distribution of birthweights and sex ratio within the expected range, and no increased rate of congenital malformations. Follow-up of babies, limited to 107 cases, thus far indicates normal physical and mental development.

Abnormalities, Drug-Induced↗
PubMed2006

Mitral heart disease due to cabergoline.

The case of a restrictive valve disease associated with cabergoline, an ergot alkaloid agonist used in the treatment of Parkinson's disease, is described. Cardiovascular and periodical follow-up assessment may be required when these drugs are prescribed.

Antiparkinson Agents↗
PubMed1994

Effectiveness of cabergoline in reducing follicle-stimulating hormone and prolactin hypersecretion from pituitary macroadenoma in an infertile woman.

Dopaminergic drugs have been reported to be effective in the treatment of FSH-secreting adenomas. We describe the case of a young woman suffering from amenorrhea with radiologic signs of pituitary macroadenoma. The enlargement of both ovaries with hemorrhagic and serous cysts suggest that FSH was active biologically. The short-term (13 weeks) chronic treatment with 0.5 mg cabergoline one time per week, a dopaminergic drug with long-lasting effect, was effective in reducing FSH and PRL hypersecretion and restoring the function of the pituitary ovarian axis, as confirmed by the occurrence of pregnancy.

Adenoma↗
PubMed2002

A practical synthesis of cabergoline.

Cabergoline is an N-acylurea derived from 9,10-dihydrolysergic acid, which is a potent prolactin inhibitor. It is marketed by Pharmacia as Dostinex for the treatment of hyperprolactinemia and is currently under active development for the treatment of a variety of CNS disorders. In the existing process, the N-acylurea is formed by the reaction of an amide with a large excess of ethyl isocyanate at elevated temperatures. An improved process was developed that eliminates this hazardous reaction. The amide is reacted with phenyl chloroformate and then with ethylamine, which provides a mild and efficient means of forming the unsymmetrical N-acylurea.

Cabergoline↗
PubMed2000

Cabergoline as a first-line treatment in newly diagnosed macroprolactinomas.

There are few long-term studies of cabergoline (CAB) administration in patients with macroprolactinomas. All of these studies included different type of patients, such as patients with idiopathic hyperprolactinemia, microprolactinomas and previously treated or untreated macroprolactinomas. We report a study of CAB treatment conducted exclusively in patients with newly diagnosed, untreated, macroprolactinomas. Twelve patients (6 M, 6 F) with macropolactinomas were investigated prospectively for 12 months to determine the effects of prolonged treatment with CAB on serum PRL levels, tumor size, visual fields and prevalence of side effects. Nine of these patients continued therapy and follow-up for 6 or more additional months of CAB administration. Our results demonstrated that CAB decreased the volume of the tumor in all patients investigated 3 months after the initiation of treatment. Specifically, mean tumor volume was 11,327 +/- 25,187 mm3 before the study and decreased to 4281 +/- 8465 mm3 and 1544 +/- 2118 mm3 in the second and last measurement, respectively. However, these changes were not statistically significant, most probably due to the very high SD. As far as the maximum diameter is concerned, mean values was 22.8 +/- 16.9 mm before the study and decreased to 16.6 +/- 10.9 mm and 13.4 +/- 7.5 mm in the 3 months and last examination, respectively. These changes were statistically significant (p = 0.005 and p = 0.007). The mean percentage decrease of the tumor volume and maximum tumor diameter was 42.4 +/- 14.0% and 24.7 +/- 4.8% respectively in the third month and 67.2 +/- 17.3% and 35.9 +/- 11.8% in the last estimation. These differences were statistically significant, (p < 0.01 and p < 0.001, respectively). The same was also true for PRL levels, the mean of which was 14,719 +/- 20,616 before treatment and became normal in the third month (153.3 +/- 63.4) and continued to be throughout the study. Four patients had visual field defects, which improved or even completely resolved during the treatment period. Finally, the CAB doses used were particularly small, i.e., 0.5-2 mg per week. All the patients recovered from their clinical problems and symptoms. This remarkable improvement was associated with an excellent tolerability of the long-term treatment due to the low incidence of side effects. In conclusion, the results of the present study demonstrated that CAB produced tumor shrinkage and normalized PRL levels in all the patients studied. Also, clinical symptoms disappeared and visual fields improved. These beneficial effects were associated with a very high compliance rate and minimal side effects. Thus, CAB can be considered a first-line pharmacological treatment of macroprolactinomas.

Adolescent↗
PubMed1999

Efficacy of combined treatment with lanreotide and cabergoline in selected therapy-resistant acromegalic patients.

The aim of this study was to evaluate the efficacy of a 6-month treatment with lanreotide (LAN) (60-90 mg/month) alone and combined with cabergoline (CAB) (1.5-3 mg/week) in 10 acromegalic patients previously demonstrated to be poor responders to octreotide (OCT) (0.6 mg/day) alone and combined with quinagolide (CV) (0.6 mg/day). All patients had previously undergone unsuccessful surgery and none of them received radiotherapy. Immunohistochemistry showed intense positive GH staining in all adenomas, positive PRL staining in 5 adenomas and faint ACTH or FSH/LH positive staining in other 2 adenomas. Moderately elevated serum PRL levels (35 and 47 ng/ml) were recorded in two patients. Fasting plasma IGF-I and serum GH levels were assayed at baseline and 30, 60, 90 and 120 days after each treatment. Gallbladder ultrasonography and sellar MRI were performed before and after 6 months of OCT and LAN treatments. After OCT treatment circulating GH and IGF-I levels remained elevated in all patients, while after 3 months of combined OCT + CV treatment, serum GH levels were suppressed (below 2.5 ng/ml) in only 1 patient. Significant increase of the percent GH (83.9 +/- 4.3 vs. 70.3 +/- 5.6%, p < 0.01) and IGF-I suppression (54 +/- 4.4 vs. 45.3 +/- 5.7, p < 0.01) and decrease of the nadir of GH (8.5 +/- 1.2 vs. 14.6 +/- 1.9 ng/ml, p < 0.01) and IGF-I (400.9 +/- 32.8 vs. 462.1 +/- 45.1 ng/ml) were obtained with the combined treatment when compared to OCT treatment alone. After a 15-30 days wash-out, circulating GH and IGF-I levels significantly increased up to pretreatment level in all patients. After 6 months of treatment with LAN, suppression of serum GH was achieved in 1 patient, but no difference in GH (66.3 +/- 6.3%) and IGF-I (43.9 +/- 4.6%) suppression was recorded in comparison to OCT treatment. After 3 months of treatment with LAN combined with CAB, suppression of serum GH and normalization of plasma IGF-I levels was achieved in 4 and 5 patients, respectively. Percent suppression of GH (88.1 +/- 2.1%) and IGF-I (57.5 +/- 2.8%) was significantly greater with the combined treatment than with LAN treatment alone. In the 7 patients with evident residual mass no change was documented by magnetic resonance imaging (MRI). None of the patients withdrew LAN + CAB treatment for poor tolerance, one patient had mild hypotension. Sludge was shown after 6 months of LAN treatment in one patient without notable change after 3 months of LAN + CAB treatment. In conclusion, the treatment with dopaminergic drugs such as CV and CAB, significantly increased the efficacy of somatostatin analogs, and can be used in combined therapy in poorly responsive patients.

Acromegaly↗
PubMed2001

In vivo and in vitro effects of octreotide, quinagolide and cabergoline in four hyperprolactinaemic acromegalics: correlation with somatostatin and dopamine D2 receptor scintigraphy.

OBJECTIVE: GH and PRL cosecretion frequently occurs in acromegaly and the sensitivity of both hormones to somatostatin analogs (SA) and dopamine agonists (DA) alone or in combination, is still debated. This study was designed to evaluate the in vivo and in vitro sensitivity to SA and/or DA and correlate the response in terms of hormone suppression to the results of in vivo somatostatin and dopamine receptor scintigraphy and to the immunohistochemical findings. DESIGN AND PATIENTS: Scintigraphy using 111In-DTPA-D-Phe(1)-OCT (111In-OCT) and 123I-methoxybenzamide (123I-IBZM) was performed in four patients with acromegaly and high circulating GH, PRL and IGF-I levels. The results were correlated with the response to long-term treatment with octreotide (OCT), quinagolide (QN) and/or cabergoline (CAB), to the in vitro hormone suppression by OCT and DA in primary cultures from the pituitary tumors and to the immunohistochemical findings. RESULTS: The first patient showed high tumour uptake of 111In-OCT and 123I-IBZM, the second high uptake of only 111In-OCT, while the third one showed faint tumour uptake of only 123I-IBZM, and the fourth a faint uptake of 111In-OCT. In the first and in the fourth patients OCT or CAB administered alone failed to normalize hormone levels while the combined treatment induced circulating GH, IGF-I and PRL normalization. In the second patient OCT administered alone normalized hormone levels while QN reduced PRL levels only. In the third patient both OCT and QN, alone or in combination, failed to normalize hormone levels. However, in this patient GH and PRL suppression was significantly greater after QN than OCT treatment. After medical therapy, all the patients were operated on. Immunohistochemistry showed diffuse GH and focal PRL staining in the first patient, while diffuse GH and PRL staining in the remaining three. In vitro, OCT significantly suppressed GH secretion in the four primary pituitary tumor cultures, while PRL secretion was significantly suppressed only in the second and the fourth cases. Dopamine agonists (DA) significantly suppressed PRL release in all the cultures, while GH secretion was significantly suppressed in three out of four. CONCLUSIONS: These four acromegalics, presenting similar clinical findings and comparable peripheral hormone levels, showed different responsiveness to SA and DA. Moreover, during the in vitro study on primary tumor cell cultures, OCT and DA displayed an inhibiting activity on GH and PRL secretion positively correlated with the response observed in vivo. This evidence together with the in vivo receptor imaging study suggest the existence of somatostatin and/or dopamine D2 receptor heterogeneity in this class of pituitary tumors. The new potent DA might be primarily considered in the medical treatment of hyperprolactinemic acromegalics, while SA alone or in combination with DA in case of ineffective hormone suppression.

Acromegaly↗
PubMed2003

Giant prolactinomas in men: efficacy of cabergoline treatment.

OBJECTIVE: The term 'giant prolactinoma' can be used for tumours larger than 4 cm in diameter and/or with massive extrasellar extension. Cabergoline (CAB), a long-lasting dopamine agonist (DA), safe and well tolerated, is effective in normalizing PRL levels and inducing tumour shrinkage in micro- and macroprolactinomas. The purpose of this prospective study was to evaluate the efficacy and safety of CAB also for giant prolactinomas. PATIENTS AND METHODS: Ten men with giant prolactinomas with a median age of 44.8 years were treated with CAB. Before CAB, four patients had previously undergone transsphenoidal surgery without modifying the parasellar extension of the tumour or their visual defects. Pretreatment serum prolactin (PRL) levels ranged between 1230 and 22 916 micro g/l (mean +/- SEM: 5794 +/- 1996) and tumour volume was between 21.8 and 105.5 cm3 (mean +/- SEM: 50.7 +/- 8.8). CAB was administered at an initial low dose of 0.5 mg three times a week and, in five patients who did not achieve serum PRL normalization, the dose was progressively increased up to 10.5 mg/week. The duration of treatment was 13-68 months (mean 38.9). PRL levels and pituitary target organ hormones were assayed before, after 30 days and then every 3 months after the beginning of CAB treatment. Magnetic resonance imaging (MRI) was carried out before, after 1-3 months, after 6 months and then every 10-12 months to evaluate tumour shrinkage. RESULTS: In every patient, a significant PRL decrease (P = 0.0086) of at least 96% of the pretreatment values occurred (from 5794 +/- 1996 to 77 +/- 38, mean +/- SEM); a persistent normalization of PRL levels was achieved in five out of 10 patients (50%) beginning from the first 3-6 months of CAB treatment (only one patient needed 12 months of therapy). A significant tumour shrinkage (P = 0.0003) was achieved after 12 months of therapy in nine out of 10 patients (90%), with a volume reduction greater than 95% in three, of 50% in four and 25% in two patients. Tumour volume decreased from 50.7 +/- 8.8 to 28.6 +/- 9.4 and then to 22.3 +/- 8.8 cm3 (mean +/- SEM) after 6 and 12 months of CAB treatment, respectively. An improvement of visual field defects (VFD) was obtained in six of the seven patients presenting visual impairment before CAB treatment. Among the eight patients presenting libido and potency (L-P) failure, five normalized their PRL levels. In two of these a complete restoration of libido and potency was observed. Three patients with secondary hypoadrenalism and a patient with secondary hypothyroidism were treated with substitutive therapy during all the study time. The drug was well tolerated by all patients and no one discontinued the therapy. CONCLUSIONS: These data suggest that, in giant, aggressive prolactinomas, CAB represents a first-line therapy effective in reducing PRL levels and determining tumour shrinkage.

Adrenal Glands↗
PubMed2001

Bait-delivered cabergoline for the reproductive control of the red fox (Vulpes vulpes): estimating mammalian non-target risk in south-eastern Australia.

Cabergoline (CAB) is a potent dopamine agonist and an inhibitor of prolactin (PRL). In red foxes (Vulpes vulpes), a single oral dose of 100 microg kg(-1) CAB can cause abortions and postnatal cub mortality from at least Day 21 of the 52-day pregnancy. The abortifacient activity of CAB is owing to the suppression of PRL, which is essential for luteotrophic support in some eutherian species. Postnatal cub mortality probably results from a reduction in the development of the mammary ductile system, which is also partially dependant on PRL during pregnancy. This paper investigates the potential risks faced by non-target mammalian species that may consume CAB baits intended for fox control. Baiting with CAB is proposed from 1 August until 1 October each year, to correspond with the time that most vixens are pregnant in south-eastern Australia. Thirty-four endemic mammals in south-eastern Australia (9 eutherians and 25 marsupials) are considered to be potentially bait-consuming (PBC) species. The percentage overlap of pregnancy and birth periods for each PBC species was compared with the duration of the proposed CAB baiting period. Only Antechinus (3 species) and Sminthopsis leucopus have greater than 40% overlap, whereas overlap in endemic rodents ranges from 0% to 22%. Overall, most PBC rodent populations appear to face little risk from CAB baiting, as their period of pregnancy does not overlap significantly with the proposed CAB baiting period. The Antechinus species, Phascogale tapoatafa and Dasyurus maculatus, are the only PBC mammals that are seasonally mono-oestrous and are thus probably more susceptible to disruption of breeding compared with polyoestrous species that may breed many times a year. At a baiting density of 8 baits km(-2), theoretical bait availability for small dasyurids, rodents and peramelids is low. This suggests a low potential for affecting these populations if CAB was indiscriminate in affecting reproductive success in all mammal groups. Presently, studies in a limited range of marsupials suggest that, unlike eutherians, the marsupial corpus luteum is independent of pituitary control and thus suppression of PRL is not likely to cause abortions in marsupials. As yet, CAB has not been shown to be orally active in any PBC species other than rodents and carnivores. Oral doses of CAB given post partum have not been found to affect lactation in Sminthopsis crassicaudata, Trichosurus vulpecula, Macropus eugenii and Setonix brachyurus. Further studies are required in order to assess the potential for high doses of oral CAB to affect pre-partum mammary development and early lactation post partum, especially in peramelids and larger dasyurids. Highly target-specific baiting techniques, may eliminate most PBC species from being exposed to CAB and these are briefly discussed.

Abortifacient Agents↗
PubMed1998

In vitro production of progesterone and estradiol by rat granulosa cells regulated by cabergoline and prolactin.

Cabergoline (CG), a dopamine agonist, and prolactin (PRL) added in vitro to isolated granulosa cells from immature rats cultured in serum-free medium inhibited FSH-stimulated production of progesterone. The lowest effective concentrations of CG and PRL were 10(-8)M and 1 ng/mL, respectively. In combination, the inhibitory activities were additive. CG at 10(-8) M also suppressed estradiol production by isolated rat granulosa cells; whereas PRL did not. In conclusion, CG inhibits FSH-stimulated progesterone and estradiol production by rat granulosa cells.

Animals↗
PubMedDate not supplied

Addition of a dopamine agonist, cabergoline, to a serotonin-noradrenalin reuptake inhibitor, milnacipran as a therapeutic option in the treatment of refractory depression: two case reports.

We illustrate 2 patients with depression who attained dramatic improvement of energy loss and fatigue when treated with cabergoline, a dopamine agonist, and milnacipran, a serotonin-noradrenalin reuptake inhibitor. Although the biologic basis of energy, motivation, and fatigue in association with depression remains unknown, some reports suggest that the decrease of noradrenalin and dopamine in the brain are particularly related to these symptoms. Therefore, treatment strategy that enhances these two monoamine neurotransmissions may be appropriate for getting a boost in energy and eliminating fatigue in patients with depression. These cases suggest that further studies are warranted to confirm the potential benefit of this strategy in the treatment of patients with depression who failed to attain complete remission due to residual symptoms including energy loss and fatigue refractory to previous treatments.

Adrenergic Uptake Inhibitors↗
PubMed1989

Effect of subacute cabergoline treatment on prolactin, thyroid stimulating hormone and growth hormone response to simultaneous administration of thyrotrophin-releasing hormone and growth hormone-releasing hormone in hyperprolactinaemic women.

It is known that dopaminergic neurotransmission is involved in the control of PRL, TSH and GH secretion. Cabergoline (CAB) is a new ergolinic derivative with a long-acting dopaminergic activity. We evaluated 11 women with pathological hyperprolactinaemia before and during sub-acute CAB treatment (0.8-1.2 mg/p.o.; 8 weeks). Simultaneous administration of TRH (200 micrograms i.v.) and GHRH 1-44 (50 micrograms i.v.) were carried out before and after 4, 8 and 10 week intervals from the beginning of CAB treatment. Basal PRL levels (2453.5 +/- S.E. 444.5 mU/l) were significantly reduced during CAB administration (week 4: 164.5 +/- 66.5 mU/l; week 8: 168.0 +/- 66.5 mU/l; P less than 0.01) and no variations were observed 2 weeks after drug discontinuation (week 10: 210.0 +/- 98.0 mU/l). PRL percentage change after TRH was increased by CAB (P less than 0.05). No variation in basal and TRH-stimulated TSH levels was found during CAB administration. A slight increase in GH basal levels (3.0 +/- 0.6 mU/l) was found after weeks 4 (6.4 +/- 2.0 mU/l) and 10 (5.8 +/- 1.6 mU/l) (P less than 0.05). GH response to GHRH was significantly enhanced (ANOVA: P less than 0.01) during sub-acute CAB treatment. A positive correlation was found between GH secretory area and weeks of CAB therapy (P less than 0.01). Our data show that CAB is very effective in lowering PRL secretion in hyperprolactinaemia, and is able to modify PRL and GH responses after TRH and GHRH. The increasing trend in GH basal and GHRH-stimulated GH levels seems to indicate that CAB can override the central dopaminergic tone which is operative in hyperprolactinaemia.

Adult↗
PubMed1997

Effect and mechanisms of the anti-prolactin drug cabergoline on pseudopregnancy in the bitch.

A potent anti-prolactin drug, cabergoline, administered orally for five days, was clinically successful in treating three different clinical manifestations of pseudopregnancy in referred bitches. The clinical conditions treated were categorised as standard pseudopregnant bitches (n = 8), those previously unsuccessfully treated with hormones (n = 10) and those which had behavioural pseudopregnancy following ovariohysterectomy (n = 8). The number of bitches whose owners reported a 'good' response was seven out of eight, six out of 10 and six out of eight, respectively. There were very few side effects in that only one bitch vomited following treatment. The clinical response did not necessarily appear to be related to an alteration in circulating prolactin concentrations, suggesting that the drug may have a direct effect on the tissues as well as in most cases reducing the plasma prolactin concentrations.

Animals↗
PubMed2004

Massive reduction of tumour load and normalisation of hyperprolactinaemia after high dose cabergoline in metastasised prolactinoma causing thoracic syringomyelia.

In 1970 a 20 year old woman presented with a pituitary chromophobe adenoma for which she underwent transfrontal pituitary surgery. In 1978 she had to be reoperated on because of local tumour recurrence, resulting in hypopituitarism. Bromocriptine (5 mg/day) was given for 15 years, but the plasma prolactin levels remained elevated. In 2000 the patient presented with signs and symptoms suggestive of a spinal cord lesion at the mid-thoracic level. A magnetic resonance imaging (MRI) scan showed an extensive leptomeningeal mass extending from the brainstem to L5, with a thoracic syringomyelia at the T7-T8 level. The plasma prolactin level was very high (5114 microg/l). A biopsy showed the presence of a metastasised prolactinoma. On administration of high dose cabergoline, 0.5 mg twice a day orally, the plasma prolactin levels decreased within one month and then normalised within 26 months. Tumour load reduced considerably but unfortunately, her signs and symptoms did not improve. This case illustrates that a high dose dopamine agonist might be an important therapeutic option in patients with a metastasised prolactinoma.

Adult↗
PubMed1999

Giant prolactinoma presented as unilateral exophthalmos in a prepubertal boy: response to cabergoline.

We report the case of a giant prolactinoma in a 7-year-old boy, which was complicated by unilateral exophthalmos. The initial levels of prolactin (PRL) were about 80,000 microU/ml. Treatment with cabergoline (CAB) resulted in rapid normalization of serum PRL (6 weeks after initiation of treatment) and reduction of tumor size. In particular, magnetic resonance imaging (MRI), which was done 2.5 months after the patient was put on CAB, revealed tremendous improvement with a decrease in the size of the tumor which now showed no extrasellar extension. Subsequent MRI studies demonstrated further improvement. Exophthalmos, anisocoria and visual fields improved. In summary, this patient represents the first report of the therapeutic use of CAB as the primary mode of treatment in a 7-year-old boy with infiltrative giant prolactinoma complicated by unilateral exophthalmos. It is a noninvasive treatment that can preserve and restore vision, as well as pituitary function, and is preferable to surgery or radiation in the treatment of prolactin-secreting macroadenoma in childhood and adolescence.

Antineoplastic Agents↗
PubMed2001

Clinical data on restless legs syndrome: a dose-finding study with cabergoline.

Current treatment options for restless legs syndrome (RLS), based on the American Academy of Sleep Medicine practice parameters, favor dopaminergic agents. The drug of first choice is levodopa, which is now licensed for RLS in two European countries. However, the short duration of action and augmentation of symptoms under therapy may limit the clinical use of levodopa, especially in severely affected patients. An open pilot study shows that the long-acting dopamine agonist cabergoline is a promising new tool in the treatment of RLS. Results of a double-blind, controlled trial are pending.

Adult↗