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PubMed1993

Luteotrophic action of prolactin in dogs and the effects of a dopamine agonist, cabergoline.

The purposes of this study were (1) to evaluate the effects of cabergoline (1.65 micrograms kg-1 injected subcutaneously for 5 days) on plasma progesterone concentrations in the pregnant bitch; (2) to assess its clinical value in terminating pregnancy in the bitch, and (3) to evaluate its side effects. Cabergoline, given to pregnant bitches, had an anti-prolactinic action and induced abortion. Plasma progesterone concentrations were reduced to below that value necessary to maintain pregnancy (2 ng ml-1 in all cases when the treatment was given 40 days after the first mating, and in four out of six cases when given from 30 days after mating). Fetal resorption occurred in 75% of cases, without clinical sign other than some vaginal discharge. The efficiency of cabergoline treatment can be monitored by plasma progesterone determination: concentrations < 2 ng ml-1 5 days after the start of treatment indicate success; in the event of failure, another treatment can be started. Ultrasonography was not always useful in predicting abortion, as in some cases this was not preceded by signs of fetal distress. The use of cabergoline as an abortifacient in the bitch appears to be of interest. Its efficacy in the second half of gestation, which is attributable to its antiprolactinic action, has been widely demonstrated and the probable multifactorial regulation of corpus luteum activity during the first half of gestation has suggested that earlier luteolysis could certainly be obtained without any side effects through a multiple approach, using different, mutually potentiating, luteolytic agents.(ABSTRACT TRUNCATED AT 250 WORDS)

Abortifacient Agents↗
PubMed1993

Abortion induction in the cat using prostaglandin F2 alpha and a new anti-prolactinic agent, cabergoline.

This study in cats compared the effects of a natural prostaglandin F2 alpha (PGF2 alpha) and cabergoline, administered on and after day 30 after mating, with regard to the plasma progesterone concentration, the induction of abortion and the side effects of each regimen. PGF2 alpha, through a direct luteolytic action, induced abortion by an abrupt and rapid (24 h) decline in the plasma progesterone concentration. Using doses (2 mg per cat) comparable to the ones selected in a previous study, 100% of abortions (4/4) in cats treated from day 33 of gestation were obtained. Cabergoline (1.65 micrograms kg-1 day-1, administered subcutaneously for 5 days), through its antiprolactinic action induced abortion in 80% (4/5) of the cats treated on day 30 of gestation. The abortion was initiated by means of a reduction in plasma progesterone concentration to < 1 ng ml-1. This reduction was not as rapid (3-4 days), however, as that obtained with PGF2 alpha (24 h). Prostaglandins always induced significant side effects such as nausea, prostration, vomiting and diarrhoea, within 10 min following injection, whereas cabergoline never induced side effects or behavioural disturbances. In addition, cabergoline usually induced abortion through fetal resorption (75% of cases), without any clinical sign other than some vaginal discharge.

Abortifacient Agents↗
PubMed1995

Cabergoline improves motor disability without modifying L-dopa plasma levels in fluctuating Parkinson's disease patients.

Studies on the influence of some dopamine agonists, particularly bromocriptine, on the pharmacokinetics of L-dopa have furnished contrasting results. Thus, any possible pharmacokinetic interaction should be taken into consideration when adding a new dopamine agonist to L-dopa treatment. In 12 Parkinson's disease (PD) patients with motor fluctuations, cabergoline was added in an 8-week study to their usual L-dopa/carbidopa therapy. Cabergoline was administered once a day at increasing doses of 0.5, 1, 2, and 3mg/day for a period of one week per dose, and 4mg/day for three weeks. Motor performance was assessed weekly evaluating the motor examination of the Unified Parkinson's Disease Rating Scale (UPDRS) and the patients' diaries of daily on-off time. Blood levels of both L-dopa and 3-O-methyldopa (3-OMD) were assayed by HPLC in two different days, over an 8-hour period, before initiating cabergoline and at the end of the study. The results of this study confirm that cabergoline is effective in the management of PD motor fluctuations without modifying L-dopa and 3-OMD pharmacokinetics.

Analysis of Variance↗
PubMed1997

Termination of pregnancy in cats using a combination of cabergoline, a new dopamine agonist, and a synthetic PGF2 alpha, cloprostenol.

The objective of this study was to increase efficacy of treatment with the dopamine agonist, cabergoline, for inducing abortion in cats by combining it with a synthetic PGF2 alpha analogue, cloprostenol. Side effects of cloprostenol were avoided by using low doses. An oral formulation of cabergoline was chosen to facilitate administration. Cabergoline was given daily (5 micrograms kg-1 day-1) while s.c. injections of cloprostenol were administered every 2 days (5 micrograms kg-1) (2 days)-1). Plasma concentrations of progesterone, side effects and pregnancy outcome were compared with those of five untreated pregnant queens. The treatment was administered from day 30 after first mating in five queens confirmed as pregnant and lasted a mean of 11 +/- 1 days. All treated animals aborted in 9 +/- 1 days without any side effect, except a mild haemorrhagic vulvar discharge. Subsequent fertility of the queens was not compromised. Abortion was mediated by an abrupt and constant decrease in plasma concentrations of progesterone. Progesterone concentrations were lower than 1 ng ml-1 from day 38 onwards in all treated animals and remained at this value thereafter, except for one queen which showed a further increase in plasma progesterone concentration from day 44 without any clinical consequence. In conclusion, a combination of daily oral administration of cabergoline and cloprostenol injections every 2 days appears to be a reliable, safe and practical method for terminating pregnancy in cats at day 30 of pregnancy, when a diagnosis of pregnancy by palpation or ultrasonography can easily be made.

Abortion, Induced↗
PubMed1995

Long-term tolerability and efficacy of cabergoline, a new long-acting dopamine agonist, in Parkinson's disease.

Motor fluctuations constitute a severe complication of chronic levodopa therapy. The addition of dopamine agonists may partially alleviate these responses; however, due to the short half-life of these drugs, several daily doses are required. Cabergoline is a new dopamine agonist with a long half-life and can be given in a single daily dose. Seventeen patients with severe fluctuations were treated with cabergoline, seven of them for > 1 year (up to 39 months). The motor status ameliorated and the percentage of "off" hours significantly decreased in the first year and did not increase significantly later during long-term follow-up. Cabergoline is a promising treatment for parkinsonian patients with motor fluctuations.

Aged↗
PubMed2000

Reduction of lipid peroxidation in different rat brain areas after cabergoline treatment.

Oxidative stress and mitochondrial damage are involved in Parkinson's disease (PD). Several drugs used for PD treatment have demonstrated antioxidant properties. To evaluate the antioxidant efficacy of cabergoline, an ergot derivative with a long plasma half-life, male Wistar rats were treated with vehicle or with 2.5 mg kg(-1)and 10 mg kg(-1)of the drug three, six, or 10 times at 48-h intervals. Cabergoline decreased basal lipid peroxide levels (LPO) in the hippocampus of rats given 10 mg kg(-1)10 times, and in the striatum of rats given the same dose six or 10 times. Spontaneous LPO was inhibited in the hippocampus of rats given 10 mg kg(-1)10 times. Stimulated LPO was decreased in the striatum of rats given 10 mg kg(-1)six times and in rats given 2.5 and 10 mg kg(-1)10 times. The ability of cabergoline to reduce LPO suggests its anti-lipoperoxidative properties.

Animals↗
PubMed1996

Double-blind study of the activity and tolerability of cabergoline versus placebo in parkinsonians with motor fluctuations.

The use of a dopamine agonist with a long duration of action has theoretical advantages in attempting to reduce the motor fluctuations in Parkinson's disease. We report the results of a double-blind controlled study of adding cabergoline, an ergot derivative with potent long-lasting high affinity for the D2 receptor, to levodopa therapy in 37 patients with severe fluctuations in response to treatment. Increasing dosages of cabergoline (19 patients) or placebo (18 patients) were added to each patient's stable levodopa regime. The two patient groups were similar at baseline in terms of age, disease duration, duration of levodopa treatment, and average hours "off" per day. Following incremental dose titration, patients in the cabergoline group had a significant reduction in hours "off" per day from 5.0 (SD 2.1) to 3.0 (SD 2.5), but there was no change in this measure in the placebo group [4.0 (2.2) and 3.3 (2.3) respectively]. This was not at the expense of a significant increase in dyskinesia. However, there was no difference between the groups when comparing their average Hoehn and Yahr stage of disease, and Schwab and England activities of daily living index.

Adult↗
PubMed2000

A giant prolactinoma presenting with unilateral exophthalmos: effect of cabergoline and review of the literature.

We report the case of a 45-year-old male presenting with unilateral exophthalmos due to a large tumoral mass invading the skull base. Ophthalmologic examination did not show any visual field defects. Imaging techniques demonstrated extension of a huge tumor (approx. 8x8x8 cm) into the right orbit and nasopharynx. Endocrine work-up revealed grossly elevated serum prolactin (PRL) levels (26,466 microg/l, nl. < 12), pointing to a large, invasive macroprolactinoma. Stimulation tests indicated associated partial adrenal and growth hormone deficiencies. Planned surgery was abandoned, and the patient was instead treated with the long-acting dopamine agonist, cabergoline. Over a period of one year, serum PRL dropped to 131 microg/l, while the tumor mass shrank to less than 50% of its original volume (with 3.5 mg/week of cabergoline). The exophthalmos disappeared, and the patient did not develop rhinorrhea or any other side effects from treatment with cabergoline. The efficacy was maintained throughout the second year (ultimate serum PRL 74 microg/l, and final size less than 10% of the original). With reference to this case, we review other macroprolactinomas reported in the recent literature for associated exophthalmos, grossly elevated serum PRL levels (> or = 15,000 microg/l), and/or "giant" size (> or = 4 cm in maximum diameter). We highlight the use of dopamine agonists in the treatment of prolactinomas with such unusual characteristics.

Cabergoline↗
PubMed2004

Effect of cabergoline treatment on Cushing's disease caused by aberrant adrenocorticotropin-secreting macroadenoma.

The present case involves a 47-yr-old woman with Cushing's disease due to pituitary macroadenoma. The patient had suffered from hypertension and obesity for two yr. Her serum cortisol levels were moderately elevated throughout the observation period, and dexamethasone failed to suppress the cortisol secretion. Plasma ACTH levels were markedly high (>100 pg/ml) and did not respond to CRH provocation. Gel filtration analysis of the patient's plasma detected the existence of big ACTH molecules, which eluted with a peak of authentic 1-39 ACTH. Cranial magnetic resonance imaging (MRI) revealed a 3 cm pituitary tumor occupying the sellar region and right cavernous sinus with diffuse enhancement by gadolinium. The pituitary mass was removed by transsphenoidal surgery, and was pathologically identified as compatible to ACTH-producing pituitary adenoma by immunohistochemistry. RT-PCR analysis of total cellular RNA extracted from the resected adenoma revealed a relatively high expression level of dopamine D2 receptor (D2R) mRNA. Therefore, a long-acting D2R agonist, cabergoline (0.25 to 0.5 mg/week), was administered for the remnant adenoma, which gradually reduced ACTH levels in 90 days. In addition, cranial MRI exhibited shrinkage of the remnant pituitary mass after a 6-month treatment with cabergoline. This case demonstrates the efficacy of cabergoline to treat Cushing's disease caused by pituitary macroadenoma secreting aberrant ACTH molecules.

Adenoma↗
PubMed2001

A study of excessive daytime sleepiness and its clinical significance in three groups of Parkinson's disease patients taking pramipexole, cabergoline and levodopa mono and combination therapy.

OBJECTIVE: To determine if therapy with an ergot and a non-ergot dopamine agonist and levodopa confers an increased risk of excessive daytime sleepiness and secondary "sleep attacks" in Parkinson's disease (PD). METHODS: Comparative study of three clinical groups taking, pramipexole (Group 1, n = 19, 8 monotherapy), cabergoline (Group 2, n = 22, 10 monotherapy), and levodopa monotherapy (Group 3, n = 14). Clinical and demographic characteristics, occurrence of "sleep attacks", and assessment of daytime sleepiness [using the Epworth Sleepiness Scale (ESS)], recorded. RESULTS: No patients reported "sleep attacks". Mean ESS scores: Group 1 (pramipexole) 8.0 +/- 4.5 (range 0-16), Group 2 (cabergoline) 8.1 +/- 3.9 (range 0-19), Group 3 (levodopa), 8.1 +/- 5.5 (range 1-18). There was no significant difference between groups (p = 0.897). Scores of > or = 16 indicating excessive daytime sleepiness (EDS) were evenly distributed throughout treatment groups, particularly in older patients with more advanced disease. CONCLUSIONS: a) EDS is not unique to pramipexole therapy and occurs with both cabergoline and levodopa. b) Increasing age, advanced disease, and higher treatment dose appear important predictors for EDS. c) Driving regulations should be reviewed accordingly.

Adult↗
PubMed2006

Clinical and biochemical stabilization of Nelson's syndrome with long-term low-dose cabergoline treatment.

We report the results of long-term (6-year) treatment of Nelson's syndrome with the long-acting dopamine agonist, cabergoline, in a 55-year-old woman. The disease presented 26 years after bilateral adrenalectomy and radiation treatment for Cushing's disease, followed by glucocorticoid and mineralocorticoid replacement therapy. Signs of Nelson's syndrome included skin and mucosal hyperpigmentation accompanied by elevated plasma levels of adrenocorticotropic hormone (ACTH) (984 pmol/l; normal, 2.0-11.5 pmol/l). Magnetic resonance imaging of the pituitary demonstrated sellar enlargement with a 15 mm macroadenoma. The patient was initially treated with bromocriptine (10 mg/d) which had no effect on either ACTH level or tumor mass. Because of visual loss, transsphenoidal surgery was performed, with partial excision of the adenoma and chiasmal decompression, followed by radiosurgery. However, ACTH levels improved only temporarily, and then increased to previous levels. Therefore, cabergoline treatment (1.5 mg/week) was initiated. ACTH levels decreased dramatically from 1050 to 132 pmol/l, accompanied by clinical improvement. Repeated imaging studies demonstrated a stable residual pituitary tumor. This case demonstrates that long-term cabergoline treatment may be efficient in patients with Nelson's syndrome.

Cabergoline↗
PubMed1992

Determination of cabergoline in plasma and urine by high-performance liquid chromatography with electrochemical detection.

A sensitive and selective high-performance liquid chromatographic method for the determination of cabergoline in plasma and urine has been developed. After buffering plasma and urine samples, cabergoline was extracted with a methylene chloride-isooctane mixture, back-extracted into 0.1 M phosphoric acid, then analysed by reversed-phase high-performance liquid chromatography. Quantitation was achieved by electrochemical detection of the eluate. The linearity, precision and accuracy of the method were evaluated. No interference from the biological matrices (human plasma and urine) was observed. The assay was still inadequate in terms of sensitivity for the quantitation of cabergoline plasma concentrations after a single oral dose of 1 mg of the drug to humans, but was successfully used in the determination of the urinary excretion of the drug.

Cabergoline↗
PubMed2004

Cabergoline protects SH-SY5Y neuronal cells in an in vitro model of ischemia.

Dopamine receptor agonists are protective in different models of neurodegeneration by both receptor-dependent and -independent mechanisms. We used SH-SY5Y cells, differentiated into neuron-like type, to evaluate if cabergoline, a dopamine D2 receptor agonist endowed with anti-oxidant activity, protects the cells against ischemia (oxygen-glucose deprivation model). Cabergoline protected the cells from ischemia-induced cell death in a concentration-dependent manner (EC(50)=1.2 microM), as demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, lactate dehydrogenase (LDH) release, and fluorescein diacetate-propidium iodide staining. This effect, observed even when the drug was added after oxygen-glucose deprivation, was not mediated by either dopamine D2 receptor activation or anti-apoptotic Bcl-2 protein over-expression (Western blotting analysis), but was linked to a reduction in cellular free radical loading (2',7'-dichlorodihydrofluorescein diacetate (DCFH-DA) staining) and membrane lipid peroxidation (thiobarbituric acid-reacting test). In conclusion, cabergoline protects in vitro neurons against ischemia-induced cell death, suggesting its possible use in the therapy of other neurodegenerative diseases in addition to Parkinson's disease.

Animals↗
PubMed2002

Cabergoline prevents necrotic neuronal death in an in vitro model of oxidative stress.

To study if cabergoline, a long-lasting specific dopamine D2 receptor agonist, has neuroprotective effects against oxidative stress, we exposed (3 h) SH-SY5Y human neuroblastoma cells to tert-butylhydroperoxide (t-BOOH; 500 microM). t-BOOH caused a 42+/-4% neuronal death, which was prevented by cabergoline (2 h before) in a concentration-dependent manner (EC(50): 1.24 microM). This effect was not antagonised by haloperidol (concentration up to 10 microM), and was associated with an increased availability of intracellular GSH contents (+30+/-11%) and a decrease in the membrane lipid peroxidation (-23+/-9%). Our data suggest that cabergoline has neuroprotective effects useful for Parkinson's disease therapy.

Cabergoline↗
PubMed2003

Effects of dopamine agonists bromocriptine, pergolide, cabergoline, and SKF-38393 on GDNF, NGF, and BDNF synthesis in cultured mouse astrocytes.

We examined the stimulatory effects of the dopamine agonists bromocriptine, pergolide, cabergoline, and SKF-38393 on the synthesis and secretion of neurotrophic factors (nerve growth factor, NGF; brain-derived neurotrophic factor, BDNF; and glial cell line-derived neurotrophic factor, GDNF) in cultured mouse astrocytes, and clarified the role of dopamine D1 and D2 receptors in these effects. Bromocriptine, a D2 agonist, elevated NGF levels in the culture medium 6.8-fold vs. control, and significantly decreased GDNF and BDNF levels, at 24 h. Both pergolide, a D1/D2 agonist, and cabergoline, a D2/weak D1 agonist, rapidly elevated NGF and GDNF levels at 4-6 h, respectively to 21- and 1.5-fold, respectively, and 84- and 9-fold, respectively, of control levels at 24 h. SKF-38393, a D1 agonist, elevated NGF and GDNF levels to 20- and 2.8-fold of controls, respectively, at 24 h. Relative levels of NGF and GDNF mRNA detected by Northern blot analysis or semiquantitative reverse transcriptase-polymerase chain reaction confirmed that increases in levels of the 2 proteins in culture medium were due to overexpression as opposed to leakage from cells. Cabergoline rapidly increased GDNF mRNA expression at 4 h, producing a potent and long-lasting increase in GDNF levels. Bromocriptine significantly suppressed GDNF synthesis. These findings suggest that stimulation of dopamine D1 receptors may be required for GDNF synthesis and secretion, and that concurrent stimulation of dopamine D1 and D2 receptors may augment synthesis and secretion of NGF and GDNF. These dopamine agonists may play a role in neuronal survival by stimulating NGF and GDNF synthesis in the brain, and as drugs are good candidates as NGF and GDNF inducers.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed2001

Successful treatment of a large macroprolactinoma with cabergoline during pregnancy.

We report a pregnant woman with a large macroprolactinoma successfully treated with cabergoline after a suboptimal response to bromocriptine. A 7 week pregnant woman with a history of a prolactinoma presented to the endocrine clinic with the complaints of headaches and nausea. She had a prolactin level of 65 microg/L 1 1/2 weeks following her last menstrual period. Bromocriptine was discontinued at 6 weeks gestation when pregnancy was confirmed. A PRL concentration was 1899 microg/L (non-pregnant normal range 1.39-24.20 microg/L, the mean peak levels during pregnancy reported from the literature are 200-210 microg/L) at 7 weeks gestation, and a repeat was 2197 microg/L. An MRI showed a 3 x 2.2 x 2.5 cm seller mass abutting the optic chiasm and displacing the optic nerves superiorly; the visual field testing was normal. Bromocriptine was reinitiated and the patient responded initially with decreasing headaches and declining PRL concentrations to 1488 microg/L at 15 weeks gestation. However, PRL increased to 1836 microg/L at 16 weeks and remained elevated despite bromocriptine 2.5 mg three times a day; in addition, she complained of severe nausea, vomiting, and persistent headaches. Cabergoline was added at 18 weeks gestation. PRL decreased dramatically from 1710 to 859 microg/L in 1 week, and to 488 microg/L within 4 weeks. A repeat MRI showed more than 30% reduction in tumor size. Bromocriptine was discontinued at 24 weeks gestation; she was maintained on cabergoline 0.5 mg twice a week without complaints. PRL levels ranged from 190 to 278 microg/L during the last 10 weeks of pregnancy. She had a C-section electively at 37 weeks gestation and delivered a healthy baby. Management options in this patient and during pregnancy are discussed.

Adult↗
PubMed2006

A mechanistic account of striatal dopamine function in human cognition: psychopharmacological studies with cabergoline and haloperidol.

The authors test a neurocomputational model of dopamine function in cognition by administering to healthy participants low doses of D2 agents cabergoline and haloperidol. The model suggests that DA dynamically modulates the balance of Go and No-Go basal ganglia pathways during cognitive learning and performance. Cabergoline impaired, while haloperidol enhanced, Go learning from positive reinforcement, consistent with presynaptic drug effects. Cabergoline also caused an overall bias toward Go responding, consistent with postsynaptic action. These same effects extended to working memory and attentional domains, supporting the idea that the basal ganglia/dopamine system modulates the updating of prefrontal representations. Drug effects interacted with baseline working memory span in all tasks. Taken together, the results support a unified account of the role of dopamine in modulating cognitive processes that depend on the basal ganglia.

Adolescent↗
PubMed2001

Effectiveness of cabergoline for termination of pregnancy in silver fox (Vulpes vulpes fulva).

Red foxes (Vulpes vulpes) are a major pest species in Europe and Australia. Traditional methods of control such as hunting or poisoning are no longer sufficient or feasible. As with domestic dogs and cats, prolactin (PRL) in the vixen is an essential luteotropin during the second half of gestation. Hence, PRL inhibitors such as cabergoline have been used to induce abortions. Eighteen mated silver fox vixens (three groups of six foxes each) were treated orally with a placebo of paraffin oil (I), or with 15 microg/kg cabergoline in feed once (11) or twice (III), on day 30 (I and II) or days 30 and 32 (III) post-coitum. Blood samples were taken prior to and after treatments and concentrations of PRL and progesterone (P4) were determined. Normal parturitions were observed in five of six, five of six and two of six vixens in groups I, II and III, respectively. In group III plasma concentrations of PRL and P4 decreased significantly but only temporarily. This drop in hormone concentrations was more pronounced in the vixens that did not carry to term. In conclusion, doses in excess of 15 microg/kg of cabergoline are likely to prevent the development of fetuses to term in pregnant vixens.

Abortifacient Agents↗