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PubMed2005

Long-term remission following withdrawal of dopamine agonist therapy in subjects with microprolactinomas.

OBJECTIVE: Reports suggest that up to 70% of patients with microprolactinomas treated with dopamine agonist therapy may achieve long-term normoprolactinaemic remission following drug withdrawal. Yet, there is no consensus on the duration of therapy nor is therapeutic interruption universally practised. We have assessed remission rates in a large cohort of treatment-naive subjects with microprolactinomas. Subjects received dopamine agonist (DA) therapy with either cabergoline or bromocriptine for a period of 2 to 3 years in the majority of cases, followed by a trial of treatment withdrawal. DESIGN: Retrospective analysis of clinic records of 89 patients (mean age 32.7 +/- 8.4 years, 84 women and 5 men) who had received either cabergoline (n = 67) (0.5-3 mg weekly) or bromocriptine (n = 22) (2.5-10 mg daily) for a mean duration of 3.1 years. RESULTS: Following withdrawal of therapy, 57 subjects developed recurrence (64%) and the mean time to recurrence was 9.6 months (range 1-44 months), while 32 subjects (36%) remained in remission beyond 1 year (mean 3.6 years, range 1-7 years). There was no difference in remission rates between subjects treated with cabergoline (n = 21) and bromocriptine (n = 11), but a direct relationship between pretreatment prolactin concentration and risk of recurrent symptomatic hyperprolactinaemia was observed. No subjects developed clinical features to suggest tumour expansion following therapeutic discontinuation. CONCLUSIONS: This study confirms that abrupt withdrawal of chronic dopamine agonist therapy, following 2 to 3 years of treatment is safe and associated with long-term remission in 30-40% of subjects with microprolactinomas. This therapeutic strategy is convenient and applicable in clinical practice.

Adolescent↗
PubMed2006

Somatostatin and dopamine-somatostatin multiple ligands directed towards somatostatin and dopamine receptors in pituitary adenomas.

AIM: We report the comparative efficacy of octreotide, cabergoline and multiple ligands directed towards the different somatostatin subtypes (ssts), such as BIM-23A779 and SOM-230, and of chimeric analogs which bind both somatostatin and the dopamine D2 receptors (D2R), such as BIM-23A760 and BIM-23A781, in cell cultures from human growth hormone (GH)-secreting pituitary adenomas. PROCEDURES: RT-PCR analysis of the quantitative expression of the different ssts and D2R mRNAs was performed on tumor fragments of 22 GH-secreting adenomas collected after surgery. Pharmacological studies, using the different ligands, were performed on cell cultures of such tumors. RESULTS: sst2, sst5 and D2R were constantly coexpressed in all tumors, in variable amounts. The levels of expression of sst2 and D2R mRNAs were significantly correlated with the maximal GH suppression by either octreotide or cabergoline (p < 0.001). In each tumor tested, 3 patterns of response, in terms of GH suppression, were observed. GH secretion was preferentially inhibited by the sst2 preferential compound octreotide in 61% of the tumors. In 19% of the tumors, the maximal inhibition of GH release was achieved with the sst5 preferential compound BIM-23268. The dopamine analog cabergoline was the most effective inhibitor of GH secretion in 21% of cases. Among the compounds tested, the most potent inhibitors of GH secretion were the sst2, sst5, D2R chimeric compound BIM-23A760, followed by the sst universal ligand SOM-230. CONCLUSIONS: The variable patterns of response to sst2, sst5 and dopamine D2 analogs may explain the greater efficacy of drugs which bind to the 3 receptors in suppressing GH secretion. The biological potency (EC50) and efficacy of the chimeric compound BIM-23A760 on GH secretion can be partly explained by its high affinity for sst2. The effect of multiple receptor activation on the functions of other pituitary tumor types, such as prolactinomas and corticotropinomas, is not presently analyzed, and the efficacy of multireceptor ligands remains to be elucidated.

Adenoma↗
PubMed1997

New pharmacotherapy for Parkinson's disease.

OBJECTIVE: To summarize the development, pharmacology, pharmacokinetics, efficacy, and safety of five investigational antiparkinsonian drugs that are in or have recently completed Phase III trials: three dopamine agonists, pramipexole, ropinirole, and cabergoline; and two catechol-O-methyltransferase (COMT) inhibitors, entacapone and tolcapone. The pathophysiology and the role of dopamine in Parkinson's disease are also reviewed. DATA SOURCES: A MEDLINE search of relevant English-language literature, clinical studies, abstracts, and review articles pertaining to Parkinson's disease was conducted. Manual searches of 1996/1997 meeting abstracts published by the American Academy of Neurology and the Movement Disorders Society were also performed. Manufacturers provided unpublished Phase III trial efficacy and pharmacokinetic data. STUDY SELECTION AND DATA EXTRACTION: Clinical trial investigations selected for inclusion were limited to human subjects. Interim analyses after 6 months for long-term clinical studies in progress were included. Pharmacokinetic data from animals were cited if human data were unavailable. Statistical analyses for all studies were evaluated. DATA SYNTHESIS: By selectivity targeting D2 receptors, the newer dopamine agonists (i.e., cabergoline, pramipexole, ropinirole) may delay the introduction of levodopa and thus the occurrence of levodopa-induced dyskinesias. In addition, they are efficacious as adjunctive therapies in patients with advanced Parkinson's disease. Unlike the currently available dopamine agonists, pramipexole and ropinirole are non-ergot derivatives and do not cause skin inflammation, paresthesias, pulmonary infiltrates, or pleural effusion. The COMT inhibitors, tolcapone and entacapone, improve the pharmacokinetics of levodopa by preventing its peripheral catabolism and increasing the concentration of brain dopamine; thus, these agents may reduce the incidence of "wearing-off" effects associated with the short half-life of levodopa and the progression of Parkinson's disease. CONCLUSIONS: Interim 6-month analyses of pramipexole, ropinirole, and cabergoline for symptomatic treatment of early Parkinson's disease have shown these drugs to be efficacious and relatively well-tolerated when used as monotherapy. Their role in delaying the development of motor fluctuations and delaying the addition of levodopa is the subject of long-term clinical studies. In advanced stages of Parkinson's disease, these medications were also efficacious; however, the main adverse effects included dyskinesias, somnolence, and hallucinations. The COMT inhibitors, entacapone and tolcapone, have also demonstrated efficacy in improving on-time in patients with stable disease. Tolcapone has also demonstrated efficacy in patients with motor fluctuations. Both drugs are relatively well-tolerated, with the exception of dyskinesias that require reduction of the levodopa dosage and occasional diarrhea.

Benzophenones↗
PubMed2006

Dopamine receptor expression and function in corticotroph ectopic tumors.

BACKGROUND: Dopamine receptor (DR) expression and dopamine agonist (DA) effectiveness have never been demonstrated in neuroendocrine tumors associated with ectopic ACTH syndrome (EAS). AIM: The aim of the current study was to evaluate DR and particularly D2 subtype expression in neuroendocrine tumors associated with EAS and to evaluate the in vivo effectiveness of the DA cabergoline in the treatment of EAS. PATIENTS AND METHODS: Six ACTH-secreting neuroendocrine tumors, including four lung, one pancreatic, and one thymic carcinoid, were used for the evaluation of D2 expression by immunohistochemistry. DR subtypes and D2 isoforms and number were evaluated by RT-PCR in three cases of persistent EAS after surgery. These patients were treated with cabergoline at the dose of 3.5 mg/wk for 6 months. Clinical parameters, hormonal levels, and tumor size were monitored during the treatment period. RESULTS: At immunohistochemistry, D2 was expressed in five (83.3%) tumors. At RT-PCR, D2 was confirmed in all three cases but at variable numbers, whereas D4 was expressed in two cases. D(2long) was expressed in all three cases, together with D(2short) in one case. A normalization of urinary cortisol levels was found in two patients (66.7%) after 3 months of treatment. However, treatment escape was demonstrated in one of these patients afterward. CONCLUSION: The results of this study demonstrated that DR are expressed in neuroendocrine tumors associated with EAS and that cabergoline treatment could be effective in controlling cortisol excess in a subgroup of patients with EAS. Further studies on a larger number of patients are mandatory to confirm the usefulness of DA in EAS.

ACTH Syndrome, Ectopic↗
PubMed1998

Bone marker and bone density responses to dopamine agonist therapy in hyperprolactinemic males.

The aim of this prospective study was to evaluate the bone mineral density (BMD) at lumbar spine and femoral neck levels and biochemical parameters of bone turnover in 20 consecutive hyperprolactinemic males before and after an 18-month treatment with different dopamine agonists. Six patients received bromocriptine at a dose of 2.5-10 mg/day; 7 patients received quinagolide at a dose of 0.075-0.3 mg/day; 7 patients received cabergoline at a dose of 0.5-1.5 mg/week. BMD, serum PRL, testosterone, dihydrotestosterone, and osteocalcin (OC), and urinary cross-linked N-telopeptides of type I collagen (Ntx) levels were measured before and every 6 months during treatment. At study entry, BMD values were lower in patients than controls at both lumbar spine (0.82 +/- 0.03 vs. 1.18 +/- 0.01 g/cm2; P < 0.001) and femoral neck (0.85 +/- 0.02 vs. 0.92 +/- 0.02 g/cm2; P < 0.05) levels. Osteopenia or osteoporosis was diagnosed in 16 patients at the lumbar spine and in 6 of them at the femoral neck level. A significant inverse correlation was found between lumbar spine and femoral neck BMD values and both PRL levels and disease duration (P < 0.01). In the 20 patients, serum OC levels were significantly lower (2.1 +/- 0.1 vs. 9.3 +/- 2.4 microg/L; P < 0.01), whereas Ntx levels were significantly higher (157.8 +/- 1.1 vs. 96.4 +/- 7.4 nmol bone collagen equivalent/mmol creatinine; P < 0.001) than control values. A significant inverse correlation was found between serum PRL and OC (P < 0.01), but not Ntx, levels. After 18 months of treatment, serum PRL levels were suppressed, and gonadal function was restored in all 20 patients, as shown by the normalization of serum T (from 2.2 +/- 0.2 to 5.0 +/- 0.2 microg/L) and dihydrotestosterone (0.3 +/- 0.02 vs. 0.5 +/- 0.01 nmol/L) levels, without any significant difference among groups. A progressive significant increase in serum OC levels together with a significant decrease in Ntx levels were observed after 6, 12, and 18 months of treatment in the 3 groups of patients. A slight, although significant, increase in BMD values was recorded in all patients after 18 months of bromocriptine, quinagolide, and cabergoline treatment, serum OC levels were normalized after treatment, whereas neither urinary Ntx levels nor BMD values were normalized by 18 months of treatment with dopaminergic agents. In conclusion, treatment with bromocriptine, quinagolide, and cabergoline for 18 months, although successfull in suppressing serum PRL levels and restoring gonadal function, was unable to restore lumbar spine and femoral neck BMD and normalize Ntx levels. However, BMD was slightly increased during treatment, suggesting that additional bone loss was prevented after treatment of hyperprolactinemia.

Adult↗
PubMed2006

Quinagolide--a valuable treatment option for hyperprolactinaemia.

Hyperprolactinaemia is characterised by gonadal dysfunction, including infertility and reduced libido and, if left untreated, is associated with an increased risk of long-term complications, such as osteoporosis. The first-line therapy for patients with hyperprolactinaemia is pharmacological intervention with a dopamine agonist. Currently, there are three dopamine agonists available for hyperprolactinaemia therapy: bromocriptine, quinagolide and cabergoline. Bromocriptine has a long history of use; however, a range of 5-18% of patients are reported to show bromocriptine resistance, with only partial lowering of plasma prolactin levels and an absence of tumour shrinkage. The newer dopamine agonists, quinagolide and cabergoline, offer improved efficacy over bromocriptine, with a lower incidence of adverse events. Quinagolide and cabergoline have also demonstrated efficacy in many patients intolerant or resistant to bromocriptine. Thus, the selection of dopamine agonists available provides more than one option for pharmacological intervention of hyperprolactinaemia. This review discusses the clinical use of quinagolide in comparison to other dopamine agonists for hyperprolactinaemia therapy. Quinagolide may improve patient compliance to treatment owing to its reduced side effect profile, simple and rapid titration over just 7 days, once-daily dosing regimen and easy to use starter pack (available in some countries). Quinagolide offers an additional benefit for patients wishing to become pregnant, as it can be used until the point of confirmation of pregnancy. Therefore, as a well tolerated and effective therapy, with a simple dosing regimen, quinagolide should be considered as a first-line therapy in the treatment of hyperprolactinaemia.

Administration, Oral↗
PubMed2003

Effects of acute prolactin manipulation on sexual drive and function in males.

The neuroendocrine response to sexual activity in humans is characterized by a pronounced orgasm-dependent increase of plasma levels of prolactin. In contrast to the well-known inhibitory effects of chronic hyperprolactinemia on sexual drive and function, the impact of acute prolactin alterations on human sexual physiology is unknown. Therefore, this study was designed to investigate the effects of acute manipulation of plasma prolactin on sexual behavior. Ten healthy males participated in a single-blind, placebo-controlled, balanced cross-over design. Prolactin levels were pharmacologically increased to high levels (protirelin, 50 micro g i.v.) or reduced to low physiological concentrations (cabergoline, 0.5 mg p.o.). Sexual arousal and orgasm were then induced by an erotic film and masturbation. In addition to continuous neuroendocrine and cardiovascular recordings, the quality and intensity of the acute sexual drive, arousal, orgasm and refractory period were assessed by extensive psychometric measures. Administration of cabergoline decreased prolactin levels and significantly enhanced all parameters of sexual drive (P<0.05), function (P<0.01) and positive perception of the refractory period (P<0.01). Administration of protirelin increased prolactin concentrations and produced small, but not significant reductions of sexual parameters. The sexual effects observed from cabergoline were completely abrogated by coadministration of protirelin. Although different pharmacological sites of action of prolactin-altering drugs have to be considered, these data demonstrate that acute changes in prolactin plasma levels may be one factor modulating sexual drive and function. Therefore, besides a neuroendocrine reproductive reflex, a post-orgasmic prolactin increase may represent one factor modulating central nervous system centers controlling sexual drive and behavior. These findings may offer a new pharmacological approach for the treatment of sexual disorders.

Adult↗
PubMed2006

[Constrictive pericarditis caused by carbergoline].

A 72-year-old male with paralysis agitans presented with symptoms and findings of constrictive pericarditis (CP). One year prior, he had a minor lateral MI. The patient had been treated with cabergoline for four years. At pericardiectomy, a thickened pericardium of 1-1,5 cm encased the right side of the heart. The pericardium was normal in the infarction area. Dopamine agonists pergolide and cabergoline for treatment of Parkinson s disease have been associated with development of CP. The absence of pericardial thickening in the infarction area suggests cabergoline as a probable cause.

Aged↗
PubMed2006

[Case of juvenile parkinsonism in pregnancy].

A 29-year-old woman with two sons developed a rest tremor and motor slowness in her right limbs. She was diagnosed as Parkinson's disease (PD) and was treated with anti-cholinergic drugs. After three years of taking a dopamine agonist (cabergoline, 4 mg per day), she became pregnant. The patient and her husband decided to have an abortion because they worried that the cabergoline might have harmed the fetus. The patient hoped to prepare for future planned birth, so we canceled the cabergoline and gradually increased her carbidopa/levodopa dose. Her motor disability gradually worsened during the pregnancy, and she developed prominent bradykinesia while taking a high dose of carbidopa/levodopa (1,000 mg per day) and a continuous infusion of levodopa. A cesarean section was performed, and the patient gave birth to a healthy baby. After the delivery, she was treated with pramipexole (2 mg per day), and her bradykinesia decreased. The initial anti-PD medication schedule for fertile female PD patients should be carefully considered to lessen the harm to the fetus, especially during organogenesis. Motor disability may worsen during pregnancy, and appropriate childcare support should be prepared.

Adult↗
PubMed1998

[Administration of combination therapy with synthetic pgf2alpha analogs and a dopamine agonist for the termination of unwanted pregnancy in pregnant dogs. A study of six cases].

Analogous to the study of Onclin and Verstegen of 1996 the combination of a dopamine agonist, cabergoline, and a synthetic analogue of prostaglandin F2 alpha, cloprostenol or dinoprost, was used to induce termination of pregnancy 25 (+/- 2) days after the first mating. The study was done in six bitches. Cabergoline was administered at a dose of 5 micrograms/kg daily over a period of nine days and cloprostenol was injected subcutaneously at 1-2 micrograms/kg (dinoprost at a dose of 25 micrograms/kg) every other day. Treatment efficacy was 100%. No side effects were observed. Pregnancy and its termination was diagnosed by ultrasonographic examination. The combination of cabergoline and cloprostenol offers a simple and safe procedure for the termination of unwanted pregnancy.

Abortifacient Agents↗
PubMed2003

Effects of acute administration of DA agonists on locomotor activity: MPTP versus neonatal intracerebroventricular 6-OHDA treatment.

The effects of several dopamine (DA) receptor agonists upon locomotor activity on adult MPTP-treated mice and postnatal 6-hydroxydopamine- (6-OHDA-) treated rats were assessed in ten experiments. C57 BL/6 mice were administered 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP, 2 x 40 mg/kg, s.c., 24-hr interval between injections) at 5-months-age, while 1-day-old male Wistar rat pups were given intracisternal 6-OHDA (50 mg, once following desipramine, 25 mg/kg). MPTP-treated mice were tested 4-5 weeks following MPTP injections whereas neonatal 6-OHDA rats were tested at 3-months-age. Locomotor activity was measured in respective activity test chambers following acute administration of DA receptor agonists. In MPTP-treated mice, apomorphine failed to elevate locomotor activity but instead further exacerbated (1.0 and 3.0 mg/kg, s.c.) the hypokinesia of these animals while inducing marked increases in control mice. Cabergoline (0.3 mg/kg, s.c.) and bromocriptine (3.0 mg/kg, s.c.) caused dose-specific elevations of locomotion in MPTP and control mice but suppressed activity at the highest doses. Quinpirole (0.2 mg/kg) and 7-hydroxydipropylaminotetralin (7-OH-DPAT; 300 nmole/kg) increased locomotion in hypokinesic MPTP-treated mice; in control mice, activity was elevated by quinpirole (0.2 and 0.7 mg/kg) and 7-OH-DPAT (100 and 300 nmole/kg), while higher doses suppressed activity. Neither SKF 38393 (1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol) nor FCE 23884 [4-(9,10-didehydro-6-methylergolin-8 beta-yl) methyl-piperazine-2,6-dione] affected locomotor activity. Apomorphine (0.3, 1.0 and 2.0 mg/kg), bromocriptine (3.0 mg/kg) and cabergoline (1.0 mg/kg) stimulated locomotion in sham-operated rats, and to a greater extent in the 6-OHDA-treated rats. Higher dose cabergoline (3.0 mg/kg) induced increased activity of similar extent in sham controls and 6-OHDA treated rats. Activity-enhancing effects of quinpirole (0.2, 0.7 and 2.1 mg/kg) in sham rats were attenuated in 6-OHDA treated rats. Both SKF 38393 (10 mg/kg) and FCE 23884 (0.3 and 1.0 mg/kg) induced locomotor activity increases in 6-OHDA, but not sham, rats. Finally, 7-OH-DPAT (1200 mg/kg) enhanced activity in 6-OHDA rats vs. shams. The effects of the DA agonists are discussed with regard to the putative antihypokinesic effects in MPTP mice and DA-receptor supersensitivity effects in neonatal 6-OHDA rats, pertaining to their more-or-less selective subreceptor profiles.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗
PubMed2003

Dual dopamine agonist treatment in Parkinson's disease.

We studied the effectiveness of cabergoline as an adjunct in patients with early Parkinson's disease receiving another dopamine agonist (pramipexole or ropinirole), at the maximal permitted dose. The study enrolled 47 patients: 35 had motor fluctuations and were receiving a dopamine agonist with levodopa; and 12, without motor fluctuations, were receiving a dopamine agonist without levodopa. These medications had in all cases failed to achieve adequate symptom control. In the 35 patients with motor fluctuations, when cabergoline was added to therapy, the time spent in the OFF period decreased by 65.6% (from 3.14+/-1.11 to 1.08+/-1.07 hours p<0.0001); and the Unified Parkinson's Disease Rating Scale (UPDRS) motor score decreased by 19.24% (from 41.68+/-12.6 to 33.66+/-10.22; (p<0.0001) during the OFF condition, and by 7.11% (from 17.01+/-6.63 to 15.8+/-7.22; p<0.001) during the ON condition. Nocturnal akinesia improved in all the patients except one. In the 12 patients without motor fluctuations, when cabergoline was added, the UPDRS score improved by 34.4% (from 23.5+/-5.3 to 15.5+/-4.7). This open study shows that dual dopamine agonist therapy can be useful in the symptomatic treatment of patients with early or more advanced Parkinson's disease receiving therapy with or without levodopa.

Adult↗
PubMed2000

Primary medical therapy of micro- and macroprolactinomas in men.

The presentation and long-term therapeutic responses of PRL-secreting pituitary tumors in men have been only partially studied. Gender-specific differences in tumor size at clinical presentation and possible differences in tumor biology in men compared to women make it important to determine treatment outcomes of male patients with prolactinomas. We performed a retrospective review of men with prolactinomas medically managed at Massachusetts General Hospital between 1980 and 1997. We identified 46 male patients with prolactinomas managed with medical therapy alone. Twelve patients had microadenomas, defined as a serum PRL level greater than 15 ng/mL and a normal pituitary scan or a tumor smaller than 1 cm. Thirty-four patients had macroprolactinomas, defined by a serum PRL greater than 200 ng/mL and pituitary adenoma larger than 1 cm. Bromocriptine, quinagolide, and/or cabergoline were administered as medical therapy. All patients had at least one follow-up visit, and the most recent serum PRL measurement after initiating dopamine agonist therapy was reported. Baseline clinical characteristics for patients with macroprolactinomas and microprolactinomas showed a larger proportion of patients with macroprolactinomas reporting a history of headache (74% vs. 0%), whereas the prevalence of sexual dysfunction and testosterone deficiency was similar between the two groups. Median serum PRL at presentation was 99 ng/mL (range, 16-385 ng/mL) vs. 1,415 ng/mL (range, 387-67,900 ng/mL), in the microprolactinoma and macroprolactinoma groups, respectively. A normal PRL level was achieved in a similar percentage of men with microprolactinomas vs. macroprolactinomas (83% vs. 79%, respectively). Although the majority of patients in both groups were treated with bromocriptine, a comparable number of patients with microprolactinomas vs. macroprolactinomas achieved a normal PRL level with cabergoline therapy. The response rates for bromocriptine and cabergoline were similar in both groups. No patient with a microprolactinoma required hormone replacement therapy, in contrast to patients with macroprolactinomas, who required thyroid, testosterone, and/or glucocorticoid replacement therapy. No patient had evidence of an increase in tumor size during therapy. In summary, we investigated the clinical presentation and treatment outcome in men with prolactinomas. We found that normalization of serum PRL levels occurs in approximately 80% of men with prolactinomas. Of importance, dopamine agonist administration yielded similar biochemical remission rates in men with microprolactinomas and macroprolactinomas.

Adult↗
PubMed1999

Guidelines for the diagnosis and treatment of hyperprolactinemia.

Hyperprolactinemia is the most common endocrine disorder of the hypothalamic-pituitary axis. While it can occur in men, it occurs more commonly in women. The prevalence of hyperprolactinemia ranges from 0.4% in an unselected normal adult population to as high as 9-17% in women with reproductive disorders. There are many possible causes of hyperprolactinemia, falling into three general categories: physiologic, pharmacologic and pathologic. When specific treatable underlying causes have been eliminated and in cases of severe hyperprolactinemia, the most likely cause is a prolactin (PRL)-secreting pituitary adenoma. Microadenomas should be treated medically, with a dopamine agonist, if there is an indication for therapy (such as amenorrhea, infertility or bothersome galactorrhea). If there is no indication for therapy, microadenomas may be followed conservatively, as growth is uncommon. Macroadenomas may grow larger; medical therapy is recommended initially, with neurosurgical evaluation reserved for specific clinical situations, such as failure of medical therapy and evidence of mass effect despite medical therapy. In the United States, the dopamine agonists indicated for treatment of hyperprolactinemia are bromocriptine and cabergoline. Bromocriptine is usually given once or twice daily, while cabergoline has a long duration of action and is given once or twice weekly. Results of comparative studies indicate that cabergoline is clearly superior to bromocriptine in efficacy (PRL suppression, restoration of gonadal function) and tolerability.

Adult↗
PubMed1999

Management of prolactinomas during pregnancy.

Infertility is a common problem for women presenting with hyperprolactinemia, and lowering of prolactin (PRL) levels to normal or near normal is often necessary to permit ovulation. Dopamine agonists are effective in a majority of women, with cabergoline somewhat more effective than bromocriptine. Bromocriptine use by the mother appears to be safe for the developing fetus when its use is discontinued four to six weeks after conception. For women with microadenomas, the subsequent risk of adenoma growth during pregnancy appears to be 1% after discontinuing the drug, and symptomatic follow-up each trimester appears to be reasonable in such patients. For women with macroadenomas, bromocriptine may be discontinued after diagnosis of pregnancy (23% risk of tumor enlargement) or continued throughout pregnancy with monthly visual field testing. Alternatively, prepregnancy debulking of the tumor may be undertaken with appropriate follow-up (2.8% risk of tumor enlargement). Although data are less extensive on cabergoline, preliminary evidence does not suggest any increase in adverse fetal outcomes. As such, therapeutic abortion is not warranted if pregnancy occurs during cabergoline treatment. The drug appears reasonably safe for continued use. Further accrual of safety data will clarify that issue.

Adult↗
PubMed2001

Prolactinomas in children and adolescents--consequences in adult life.

Prolactinomas in children and adolescents are rare. However, they represent, together with corticotropinomas, the most frequent types of pituitary tumors in adolescence. Most prolactin-secreting pituitary tumors are microprolactinomas but many, and particularly those in men, are macroadenomas. The clinical findings that would usually project into the adult life of patients, in other words the issue of transitory endocrinology from childhood to adulthood, are menstrual irregularities, infertility, short stature, osteopenia and/or osteoporosis, and sometimes psychometric abnormalities. The therapy of choice for both macro- and microprolactinomas is one of the new dopamine agonists, such as quinagolide or cabergoline. Recent evidence-based data have clearly promoted cabergoline as the first-line treatment. Cabergoline may normalize prolactin secretion, restore fertility in women and men. and induce tumor shrinkage. Today, transsphenoidal surgery should be considered only in patients with a large extrasellar extension.

Adolescent↗
PubMed2004

Prolactin excess: treatment and toxicity.

Dopamine agonists provide highly effective therapy for the treatment of hyperprolactinemia. As a result of their efficacy and tolerability, these agents are considered to be the initial therapy of choice in children, adolescents and adults with idiopathic hyperprolactinemia and prolactinomas. The four dopamine agonists, bromocriptine, pergolide, cabergoline and quinagolide, share a similar mechanism of action and side effect profile. Although studies of cabergoline have demonstrated the highest treatment efficacy and tolerability, all four of these agents are safe, effective and tolerable in children and adolescents. When fertility is desired, bromocriptine is generally preferable, but cabergoline is also likely safe; pergolide and quinagolide should not be used in this setting.

Adult↗
PubMed1995

Differential effects of three dopamine receptor agonists in MPTP-treated monkeys.

The behavioral effects of cabergoline, pergolide and bromocriptine were investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys with attention to the induction of hyperactivity, as evidenced by irritability, excitability and aggressiveness. All three drugs improved the parkinsonism in a dose-dependent fashion following a single injection. Among the three dopamine (DA) receptor agonists used, the antiparkinsonian effect of pergolide was the strongest and had an immediate effect, while cabergoline showed the longest duration of the antiparkinsonian effect and was least potent in inducing hyperactivity.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗