BUY-DOSTINEX.COM
Cheap Discreet
U.S. & Worldwide Delivery   Genuine
Dostinex (Cabergoline)
Also known as Cabergoline, Cabaser

DOSTINEX (cabergoline)
Research & Medical References

The medical community raves about Dostinex (cabergoline).
Read what latest research and what doctors are saying about Dostinex



 
Discreet
Cheap
Worldwide Delivery
The ORIGINAL Dostinex
Order Dostinex here

Buy Dostinex
Dostinex
(cabergoline 0.5 mg)
8 tablets
(1 bottle)
$109
SALE
Buy Now
Dostinex
(cabergoline 0.5 mg)
16 tablets
(2 bottles)
$199
SALE
Buy Now
Dostinex
(cabergoline 0.5 mg)
24 tablets
(3 bottles)
$279
SALE
Buy Now
Cabaser
(cabergoline 1 mg)
20 tablets
LOW Available! Contact us

We offer the ORIGINAL legitimate version of
DOSTINEX™ and CABASER™

 
Dostinex (Cabergoline) articles hyperprolactinemia for the treatment of pituitary adenomas prolactinoma, pituitary tumours:

The assessment of cabergoline (Dostinex) efficacy and tolerability in patients with pituitary adenomas prolactinoma type.

Bolko P, Jaskula M, Wasko R, Wolun M, Sowinski J.
Department of Endocrinology, Internal Diseases and Metabolism, Karol Marcinkowski University of Medical Sciences, Poznan, Poland. May 2003



Prolactinoma is the most frequent type of secreting pituitary tumours. In the treatment, pharmacotherapy with dopamine agonists is considered the first-line option. For many years Bromocriptine (parlodel), a D1 and D2 dopamine receptor agonist, has been the standard medicine for hyperprolactinemic patients. However, the treatment is frequently associated with intolerance or resistance. Recently cabergoline (dostinex), a long acting, ergoline-derived, selective D2 agonist has become available and has been promoted as the initial treatment.

Therefore the object of four studies was to assess the efficacy and tolerability of cabergoline dostinex in patients with prolactin-secreting pituitary adenomas. 17 patients, 13 women at the age of 21-55 years (average 37.1) and 4 men at the age of 29-45 years (average 36.3), with pathological hyperprolactinemia due to pituitary tumours were involved in the study. In all patients the increased pretreatment concentration of PRL was observed, ranging from 1047 to 1678 mlU/ml (mean 1369 mlU/ml). MRI scans revealed microprolactinomas in 11 (64.7%) cases and macroadenomas in 6 (35.3%) cases. None of the patients had previously undergone pituitary surgery and all of them were newly diagnosed, previously untreated. The patients were treated with cabergoline for 6 months.

Cabergoline therapy was started at a dose of 0.5 mg twice a week for the first two months, then the dose was decreased to a 0.25 mg twice a week and finally maintained at 0.25 mg a week. After 6 months of the therapy, the normalization of serum PRL concentrations (from mean 1358 mlU/ml to mean 420 mlU/ml; p < 0.001) was achieved in 13 (76.5%) patients (8 with microprolactinoma and 5 with macroprolactinoma). In the remaining 4 patients PRL levels remained elevated but were decreased from mean 1403 mIU/ml to mean 812 mIU/ml. There were no differences, regarding CAB efficacy in lowering PRL levels, between patients with micro- and macroadenomas (p > 0.05). About 90% women resumed menstrual cycles in our study. All the other clinical pretreatment symptoms disappear in the course of the therapy.

The tumour shrinkage, confirmed by control MRI was noted in 2 patients (33%) with macroprolactinoma. Cabergoline (Dostinex) was tolerated satisfactorily by all our patients. The results have confirmed a high efficacy and a very good tolerability of Cabergoline (Dostinex) in the treatment of patients with pituitary adenomas. Together with a very convenient administration, such therapy can provide a very good patient compliance thus should be considered the first line option in patients with prolactinomas.


Giant prolactinomas in men: efficacy of cabergoline (Dostinex) treatment.

Corsello SM, Ubertini G, Altomare M, Lovicu RM, Migneco MG, Rota CA, Colosimo C.
Institute of Endocrinology, Catholic University School of Medicine, Rome, Italy. May 2003

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, cabergoline (Dostinex) represents a first-line therapy effective in reducing PRL levels and determining tumour shrinkage.

Dopamine receptor agonists for treating prolactinomas.

Colao A, di Sarno A, Pivonello R, di Somma C, Lombardi G.
Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, via S. Pansini 5, 80131 Naples, Italy. June 2002

Prolactinomas are the most common hormone-secreting pituitary tumours and cause infertility and gonadal and sexual dysfunction in both sexes. The approach to prolactinomas has changed in the last 25 years thanks to the availability of dopaminergic drugs characterised by a potent prolactin-inhibitory effect, a tumour shrinking effect associated with a satisfactory tolerability. In more recent years, cabergoline 1-[(6-allelylergolin-8beta-yl)carbonyl]-1-[3-(dimethylamino) propyl]-3-ethyl-urea an ergoline derivative with potent, selective and long-lasting inhibitory activity on prolactin release, has been used to suppress prolactin secretion in women with hyperprolactinaemia. Cabergoline (Dostinex) was shown to be significantly more effective than Bromocriptine in inducing a complete biochemical response and clinical efficacy and was better tolerated than Bromocriptine in the majority of patients. Notable tumour shrinkage until tumour disappearance was observed during cabergoline treatment in most patients with macroprolactinoma and it was also proven effective in patients resistant to or with a poor response to Bromocriptine .

In view of the limited data on cabergoline-associated pregnancies and the long half-life of the drug, it is currently recommended that women hoping to become pregnant, once ovulatory cycles have been established, should discontinue cabergoline therapy 1 month before they intend to conceive. However, no data concerning negative effects on pregnancy or offspring have been reported. The great efficacy of this compound together with its excellent tolerability makes this drug the current treatment of choice for the majority of patients with hyperprolactinaemic disorders.

Minor tumour shrinkage in nonfunctioning pituitary adenomas by long-term treatment with the dopamine agonist cabergoline (Dostinex)

Lohmann T, Trantakis C, Biesold M, Prothmann S, Guenzel S, Schober R, Paschke R.
Department of Internal Medicine III, University of Leipzig, Germany. Tobias. August 2001



OBJECTIVE: The purpose of this study was to define safety and efficacy of medical therapy in the treatment of nonfunctioning pituitary tumours. DESIGN: We studied thirteen patients with a clinically nonfunctioning pituitary macroadenoma for response to cabergoline treatment for 1 year. Twelve/13 patients were already operated and had residual or recurrent tumours. METHODS: We determined the outcome of treatment by visual perimetry, computed tumour size measurement in MRI and hormonal response (changes in pituitary function, reduction of alpha-subunit). RESULTS: Seven/13 patients on cabergoline had a tumour shrinkage above 10% of the initial tumour volume. In 4 patients, this tumour shrinkage was correlated to an increasing distance of the tumour to the optic chiasm. Only 2/9 patients with visual field defects before therapy showed improvements in visual acuity under cabergoline.

No significant side effects of the therapeutical regimens were observed. Neither LH and/or FSH expression in the tumour cells nor the reduction of the alpha-subunit serum levels by medical therapy was correlated to tumour shrinkage. CONCLUSION: Given that these patients had advanced disease which makes it difficult to find significant therapeutic effects, medical therapy with potent dopamine agonists such as cabergoline (Dostinex) may evolve as a novel therapeutic option in a subgroup of patients with clinically nonfunctioning tumours declining operation and radiotherapy.

The novel use of very high doses of cabergoline (Dostinex) and a combination of testosterone and an aromatase inhibitor in the treatment of a giant prolactinoma.

Gillam MP, Middler S, Freed DJ, Molitch ME.
Division of Endocrinology, Metabolism, and Molecular Medicine, Northwestern University, The Feinberg Medical School, Chicago, Illinois 60611, USA. October 2002



Most prolactinomas respond rapidly to low doses of dopamine agonists. Occasionally, stepwise increases in doses of these agents are needed to achieve gradual prolactin (PRL) reductions. Approximately 50% of treated men remain hypogonadal, yet testosterone replacement may stimulate hyperprolactinemia. A 34-yr-old male with a pituitary macroadenoma was found to have a PRL level of 10,362 micro g/liter and testosterone level of 3.5 nmol/liter. Eleven months of dopamine agonist therapy at standard doses lowered PRL levels to 299 micro g/liter.

Subsequent stepwise increases in cabergoline (3 mg daily) further lowered PRL levels to 71 micro g/liter, but hypogonadism persisted. Initiation of testosterone replacement resulted in a rise and discontinuation in a fall of PRL levels. Aromatization of exogenous testosterone to estradiol and subsequent estrogen-stimulated PRL release was suspected. Concomitant use of cabergoline (Dostinex) with the aromatase inhibitor anastrozole after resuming testosterone replacement resulted in the maintenance of testosterone levels and restoration of normal sexual function, without increasing PRL. Ultimately, further reduction in PRL on this therapy permitted endogenous testosterone production. Thus, novel pharmacological maneuvers may permit successful medical treatment of some patients with invasive macroprolactinomas.

Withdrawal of long-term cabergoline (Dostinex) therapy for tumoral and nontumoral hyperprolactinemia.

Colao A, Di Sarno A, Cappabianca P, Di Somma C, Pivonello R, Lombardi G.
Department of Molecular and Clinical Endocrinology and Oncology, Section of Endocrinology, Federico II University of Naples, Naples, Italy. Nov 2003

BACKGROUND: Whether the withdrawal of treatment in patients with nontumoral hyperprolactinemia, microprolactinomas, or macroprolactinomas is safe and effective has been unclear. We performed an observational, prospective study of cabergoline (Dostinex a dopamine-receptor agonist) withdrawal in such patients. METHODS: The study population included 200 patients--25 patients with nontumoral hyperprolactinemia, 105 with microprolactinomas, and 70 with macroprolactinomas.

Withdrawal of cabergoline was considered if prolactin levels were normal, magnetic resonance imaging (MRI) showed no tumor (or tumor reduction of 50 percent or more, with the tumor at a distance of more than 5 mm from the optic chiasm, and no invasion of the cavernous sinuses or other critical areas), and if follow-up after withdrawal could be continued for at least 24 months. RESULTS: Recurrence rates two to five years after the withdrawal of cabergoline were 24 percent in patients with nontumoral hyperprolactinemia, 31 percent in patients with microprolactinomas, and 36 percent in patients; with macroprolactinomas.

Renewed tumor growth did not occur in any patient; in 10 female patients (22 percent) and 7 male patients (39 percent) with recurrent hyperprolactinemia, gonadal dysfunction redeveloped. In all diagnostic groups, prolactin levels at the time of recurrence were significantly lower than at diagnosis (P<0.001). The Kaplan-Meier estimated rate of recurrence at five years was higher among patients with macroprolactinomas and those with microprolactinomas who had small remnant tumors visible on MRI at the time of treatment withdrawal than among patients whose MRI scans showed no evidence of tumor at the time of withdrawal (patients with macroprolactinomas, 78 percent vs. 33 percent, P=0.001; patients with microprolactinomas, 42 percent vs. 26 percent, P=0.02). CONCLUSIONS: Cabergoline (Dostinex) can be safely withdrawn in patients with normalized prolactin levels and no evidence of tumor. However, because the length of follow-up in our study was insufficient to rule out a delayed increase in the size of the tumor, we suggest that patients be closely monitored, particularly those with macroprolactinomas, in whom renewed growth of the tumor may compromise vision. Copyright 2003 Massachusetts Medical Society

Six months of treatment with cabergoline (dostinex) restores sexual potency in hyperprolactinemic males: an open longitudinal study monitoring nocturnal penile tumescence.

De Rosa M, Zarrilli S, Vitale G, Di Somma C, Orio F, Tauchmanova' L, Lombardi G, Colao A.
Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, 80131 Naples, Italy. Feb 2004

This open longitudinal study investigated the prevalence of depressed sexual potency by monitoring erectile dysfunction using nocturnal penile tumescence (NPT) in 51 consecutive men with hyperprolactinemia (41 macroprolactinomas and 10 microprolactinomas) and evaluated potential reversibility of sexual failure after 6 months of treatment with cabergoline (dostinex). Fifty-one healthy men served as controls. Compared with controls, the patients with either micro- or macroprolactinoma had low testosterone levels with severe alterations of erectile function.

Testosterone deficiency was present in 73.2% of macro- and 50% of microprolactinomas; reduced libido and sexual potency were referred by 53.6% of macroprolactinomas, 50% of microprolactinomas, and none of controls. Fewer than three erectile events per night by NPT were found in 96.7% of patients and 13.7% of controls (P < 0.0001). After 6 months of cabergoline (dostinex) treatment, prolactin levels normalized in 74.5% of patients: 73.2% of macroprolactinomas and 80% of microprolactinomas. Testosterone levels normalized in 68.6% of patients, whereas NPT normalized in 60.6% of patients who had normalized prolactin levels and in 7.7% of patients who did not. In conclusion, at study entry, 50% of the patients complained of sexual disturbances, 96.7% of whom had an impairment of erectile events per night compared with 13.7% of controls. Six months of treatment with cabergoline normalized testosterone levels in most cases, thus restoring and maintaining during treatment the capability of normal sexual activity in hyperprolactinemic males.

Cabergoline (Dostinex) and hyperprolactinaemia: new preparation. Better than Bromocriptine .

Feb 2000

Cabergoline, a dopamine agonist already marketed in about 40 countries, is indicated in France for the treatment of hyperprolactinaemia (idiopathic or caused by a pituitary microadenoma). The reference drug in this setting is Bromocriptine . (2) The clinical file on cabergoline is methodologically sound, albeit limited mainly to women with amenorrhoea. (3) Two partially blinded comparative trials have shown that cabergoline is significantly more effective than Bromocriptine in restarting ovulatory cycles with menstruation. (4) In these trials the incidence of nausea was significantly lower on cabergoline than on Bromocriptine . Other adverse events seem to be equally frequent with the two drugs. (5) Cabergoline is effective when taken once or twice a week, while Bromocriptine needs to be taken several times a day.

Comparison of the effects of cabergoline and Bromocriptine on prolactin levels in hyperprolactinemic patients.

Sabuncu T, Arikan E, Tasan E, Hatemi H.
Harran University, Medical Faculty, Department of Endocrinology and Metabolism, Sanliurfa, Turkey. Sep 2001

OBJECTIVE: It is well known that Bromocriptine has a suppressive effect on the prolactin release in hyperprolactinemic patients. But it also has some adverse effects. The new, long-acting dopaminergic drug, cabergoline, has been reported to be an effective agent in these patients. However, there are relatively few reports comparing the beneficial and adverse effects of these drugs in the treatment of hyperprolactinemic patients. Therefore, here we studied and compared the efficacy and tolerability of cabergoline with Bromocriptine in hyperprolactinemic patients. PATIENTS: Seventeen patients (7 with microprolactinoma, 4 with macroprolactinoma, 6 with idiopathic hyperprolactinemia) were given Bromocriptine at a dose of 2.5 mg (or 5 mg for macroprolactinomas) twice daily, and 17 patients (8 with microprolactinoma, 4 with macroprolactinoma, 5 with idiopathic hyperprolactinemia) were given cabergoline at a dose of 0.5 mg twice weekly for 12 weeks.

RESULTS: At the end of the study, the prolactin reduction was significantly greater in the cabergoline group than in the Bromocriptine group (-93 vs. -87.5 %, respectively, p < 0.05). Normalization of prolactin levels was achieved in 10 of 17 patients (59%) in the Bromocriptine group, and in 14 of 17 patients (82%) in the cabergoline group (p = 0.13). Two patients (50%) with macroprolactinoma in the Bromocriptine group and three patients (75%) with macroprolactinoma in the cabergoline group demonstrated a normalization of their serum prolactin levels. Adverse events were noted in 53% of Bromocriptine patients and in 12% of cabergoline patients (p < 0.01). CONCLUSION: These data indicate that cabergoline is a very effective agent for lowering the prolactin levels in hyperprolactinemic patients and that it appears to offer considerable advantage over Bromocriptine in terms of efficacy and tolerability.


 
 
Top

Dostinex (Cabergoline) articles in the treatment of Parkinson's Desease:

Efficacy of cabergoline (Dostinex) in long-term use: results of three observational studies in 1,500 patients with Parkinson's disease.

Baas HK, Schueler P.
Department of Neurology, Central Hospital Hanau, Germany. 2001



The tetracyclic ergoline derivative cabergoline was investigated in three studies to test its efficacy in treating the motor symptoms of Parkinson's disease. In two studies, it was used as an add-on agent to the previous medication regimen that included other parkinsonian drugs, including levodopa. In the third study, cabergoline was switched from another dopamine agonist. All studies proved this drug's effectiveness in treating such motor symptoms as akinesia, dyskinesia, and nocturnal akinesia.

Quality of life and disability in activities of daily living assessments were measured by PDQ 39 or UPDRS VI. Treatment with cabergoline (Dostinex) showed higher efficacy and greater safety than other parkinsonian drugs. Copyright 2001 S. Karger AG, Basel

The effect of cabergoline on sleep, periodic leg movements in sleep, and early morning motor function in patients with Parkinson's disease.

Hogl B, Rothdach A, Wetter TC, Trenkwalder C.
Max Planck Institute of Psychiatry, Department of Neurology, Munich, Germany. Oct 2003

To investigate the effect of the dopamine D2 and D1 receptor agonist cabergoline on sleep, periodic leg movements (PLMs) in sleep, and early morning motor performance in patients with Parkinson's disease (PD). It was hypothesized that cabergoline had long-lasting beneficial effects on sleep and PLMs in sleep in patients with PD, after a single evening intake. A total of 15 patients with idiopathic PD underwent two nights of polysomnography and motor tests (UPDRS, tapping test) before and after 6-8 weeks of treatment with cabergoline (dosage: 3-6 mg/day). Additionally, patients completed a subjective sleep visual analog scale (VAS) before and during cabergoline treatment. Compared to baseline values, treatment with cabergoline did not change sleep efficiency or the amount of stage 1 and stage 2 sleep. The number of awakenings (22.4+/-10.1 vs 32.5+/-13.3, p<0.05) and stage shifts (119+/-42 vs 148+/-46, p<0.05) were increased during treatment with cabergoline, and PLMs in sleep were reduced (PLM index 34.9+/-44.9 vs 6.7+/-4.2 per hour, p<0.05). Cabergoline (Dostinex) significantly improved early morning motor function, and in spite of increased phase shifts and awakenings, patients felt significantly more refreshed in the morning during cabergoline therapy. Cabergoline slightly fragmented sleep, without altering its total amount. The functional significance of this finding is uncertain. The subjective quality of sleep improved, and periodic limb movements in sleep decreased.

Cabergoline (Dostinex) in the treatment of Parkinson's disease

Pastor P, Tolosa E.
Unidad de Parkinson y Movimientos Anormales Servicio de Neurologia, Institut Clinic de Malaties del Sistema Nervios, IDIBAPS, Hospital Clinic, Facultad de Medicina de la Universidad de Barcelona, Barcelona, Spain. May 2003

Cabergoline (also known as Dostinex) (1-[(6-allelylergolin-8 beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethyl-urea) is a new agonist of the D2 dopaminergic receptors used in the treatment of Parkinson's disease. Cabergoline is characterized by unique pharmacologic properties, such as its long plasma half-life (about 68 hours), which allows for once a day administration. Cabergoline is well tolerated, as has been shown in several clinical trials. Based on the information available, we suggest that cabergoline produces an improvement in the symptoms of Parkinson's disease similar to those produced by other dopaminergic agonists. Cabergoline monotherapy, when used in previously untreated patients, is an appropriate option for the symptomatic treatment of Parkinson's disease. Cabergoline improves motor symptoms, delays the presentation of levodopa-induced motor complications, and diminishes the amount of levodopa required for the control of the symptoms. We suggest that cabergoline (Dostinex) is an adequate adjuvant treatment for Parkinson' disease. There is improvement in motor symptoms (without substantially increased dyskinesias), reduced severity and duration of the wearing-off period, and diminished need for levodopa. Cabergoline can also be useful in the treatment of sleep disturbances associated with advanced Parkinson's disease such as nocturnal akinesia and dystonia. However, additional studies on cabergoline's effects in nocturnal disturbances associated with Parkinson's disease are still required. Cabergoline is a well tolerated drug. Its side effects are seen mainly in the digestive and nervous system (central and peripheral). The efficacy of cabergoline in comparison to other dopaminergic agonists should be tested in future clinical studies.

Combination of two different dopamine agonists in the management of Parkinson's disease.

Stocchi F, Berardelli A, Vacca L, Thomas A, De Pandis MF, Modugno N, Valente M, Ruggieri S.
Department of Neurosciences, La Sapienza University, Viale dell'Universita 30, I-00185 Rome, Italy. Sep 2002

 An alternative approach to the symptomatic treatment of parkinsonian patients with and without motor fluctuations is to use dual dopamine agonists. The aim of this study was to investigate the symptomatic effect of administrating a second dopamine agonist to parkinsonian patients already assuming pramipexole or ropinirole. As the second dopamine agonist we chose cabergoline, a drug with a long half life, whose pharmacological profile differs from that of the newer non-ergot-derived dopamine-receptor agonists. In this pilot study we enrolled 27 patients: 21 patients had motor fluctuations and were receiving levodopa plus a dopamine agonist, and 6 patients without motor fluctuations were receiving a dopamine agonist without levodopa.

This open study shows that dual dopamine agonist therapy (cabergoline plus pramipexole or ropinirole) may be used in the symptomatic treatment of patients with Parkinson's disease receiving therapy with or without levodopa.

Use of the dopamine agonist cabergoline (Dostinex) in the treatment of movement disorders.

Marco AD, Appiah-Kubi LS, Chaudhuri KR.
Movement Disorders Unit, Mapother House, King's College Hospital, Denmark Hill, London, UK. Oct 2002



Cabergoline is an ergot-derived dopamine agonist used in the treatment of Parkinson's disease (PD). Both ergot and non-ergot-derived dopamine agonists directly stimulate dopamine receptors, unlike levodopa, which must undergo presynaptic breakdown to dopamine beforehand.

Cabergoline has the longest half-life of the dopamine agonists currently available and is effective when given once-daily. It has been proposed that therapy with cabergoline may mimic physiological dopaminergic stimulation in PD by providing striatal intrasynaptic dopamine replacement. Its long half-life is likely to result in sustained rather than pulsatile dopaminergic stimulation, the preferred manner of treating PD. Placebo-controlled trials using cabergoline as an adjunctive therapy in PD have shown that it significantly reduces 'off' time, improves motor function and reduces levodopa requirements. Cabergoline has been shown to be as effective as other dopamine agonists in improving motor function as monotherapy in early PD, and a 5-year levodopa-controlled study indicates the superiority of cabergoline over levodopa in reducing dyskinesias.

The efficacy of cabergoline (Dostinex) in PD patients with nocturnal disabilities, restless leg syndrome and augmentation has also been demonstrated. Audits of the clinical efficacy of cabergoline indicate that it is well-tolerated and has an acceptable side effect profile.

The dopamine agonist cabergoline (Dostinex) provides neuroprotection by activation of the glutathione system and scavenging free radicals.

Yoshioka M, Tanaka K, Miyazaki I, Fujita N, Higashi Y, Asanuma M, Ogawa N.
Department of Brain Science, Graduate School of Medicine and Dentistry, Okayama University, 2-5-1 Shikatacho, Japan. July 2002



Free radicals are involved in the pathogenesis and/or progression of Parkinson's disease (PD). Several ergot derivative dopamine (DA) agonists have been reported to scavenge free radicals in vitro and to show a neuroprotective effect in vivo. We investigated the in vitro free radical scavenging and antioxidant activities of cabergoline, a long-acting ergot DA agonist, as well as its ability to activate glutathione (GSH), catalase (Cat) and superoxide dismutase (SOD) activating effects and its in vivo neuroprotective properties against 6-hydroxydopamine (6-OHDA) intracerebroventricularly (i.c.v.) in mice.

The striatal DA turnover induced by i.c.v. injection of 6-OHDA was completely normalized by pretreatment with cabergoline. Moreover, cabergoline scavenged free radicals in vitro and significantly reduced lipid peroxidation in vitro and in vivo. Furthermore, daily administration of cabergoline to mice significantly increased striatal GSH levels by activation of RNA expressions of GSH-related enzymes, although striatal Cat and SOD activities did not change. In addition, our present results suggest that repeated administration of cabergoline attenuates both 6-OHDA-induced nigrostriatal DAergic dysfunction and DA neuronal cell death, since cabergoline also had a neuroprotective effect in the immunohistochemical experiment.

In conclusion, our findings indicate that the multiple antioxidant mechanisms of cabergoline (Dostinex), such as activation of the GSH system and the direct free radical scavenging activity, may explain the neuroprotective effect of this ergot DA agonist.

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

Lombardi G, Varsaldi F, Miglio G, Papini MG, Battaglia A, Canonico PL.
DISCAFF Department, University of Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy. Dec 2002



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.

Chronic treatment with small doses of cabergoline (Dostinex) prevents dopa-induced dyskinesias in parkinsonian monkeys.

Belanger N, Gregoire L, Tahar AH, Bedard PJ.
Department of Medicine and Neuroscience Unit, Laval University and Research Center, Ste-Foy, Quebec, Canada. Dec 2003

Levodopa continues to be the most effective agent for the symptomatic treatment of Parkinson's disease (PD). But over time, initial benefits decline in efficacy because of a rise in adverse effects such as dyskinesias.

The pathophysiology of levodopa-induced dyskinesias (LID) is not completely understood, but it appears to result from deficient regulation by dopamine of corticostriatal glutamatergic inputs leading to a cascade of neurochemical changes in the striatum and the output pathways. In the present study, we examined if the addition of small doses of cabergoline (Dostinex a long-acting D(2) receptor agonist) to levodopa could prevent LID. The major hypothesis is that sustained activation of postsynaptic D(2) receptors on medium spiny neurons even by small doses of cabergoline could prevent or reduce LID. The minor hypothesis, and the more controversial of the two, is that the long-acting stimulation by small doses of cabergoline could diminish the release of glutamate by the corticostriatal pathway and prevent LID.

Eight MPTP-treated monkeys with a long-standing and stable parkinsonian syndrome and having never received dopaminergic agents were used. Two groups of four were treated for 1 month with levodopa/benserazide administered orally (100 mg/25 mg). The second group received in addition a threshold dose of cabergoline (dose ranging from 0.015 to 0.035 mg/kg, SC). During the treatment, we observed LID in the levodopa group but not in the group receiving levodopa+cabergoline.

Furthermore, the combination produced a comparable antiparkinsonian effect in terms of quality but prolonged the duration (by 1 to 2 hours) and increased the locomotion (mean for 2 weeks congruent with 104%). Our data suggest that a small dose of a long-acting D(2) agonist combined with high doses of levodopa could be preventive of LID in patients with PD and could be an alternative to using antiglutamatergic agents for this purpose. Copyright 2003 Movement Disorder Society


 
Top

Dostinex (Cabergoline) articles on effects on Sexual activity:

Six months of treatment with cabergoline (dostinex) restores sexual potency in hyperprolactinemic males: an open longitudinal study monitoring nocturnal penile tumescence.

De Rosa M, Zarrilli S, Vitale G, Di Somma C, Orio F, Tauchmanova' L, Lombardi G, Colao A.
Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, 80131 Naples, Italy. Feb 2004

This open longitudinal study investigated the prevalence of depressed sexual potency by monitoring erectile dysfunction using nocturnal penile tumescence (NPT) in 51 consecutive men with hyperprolactinemia (41 macroprolactinomas and 10 microprolactinomas) and evaluated potential reversibility of sexual failure after 6 months of treatment with cabergoline (dostinex). Fifty-one healthy men served as controls. Compared with controls, the patients with either micro- or macroprolactinoma had low testosterone levels with severe alterations of erectile function.

Testosterone deficiency was present in 73.2% of macro- and 50% of microprolactinomas; reduced libido and sexual potency were referred by 53.6% of macroprolactinomas, 50% of microprolactinomas, and none of controls. Fewer than three erectile events per night by NPT were found in 96.7% of patients and 13.7% of controls (P < 0.0001). After 6 months of cabergoline (dostinex) treatment, prolactin levels normalized in 74.5% of patients: 73.2% of macroprolactinomas and 80% of microprolactinomas. Testosterone levels normalized in 68.6% of patients, whereas NPT normalized in 60.6% of patients who had normalized prolactin levels and in 7.7% of patients who did not. In conclusion, at study entry, 50% of the patients complained of sexual disturbances, 96.7% of whom had an impairment of erectile events per night compared with 13.7% of controls. Six months of treatment with cabergoline normalized testosterone levels in most cases, thus restoring and maintaining during treatment the capability of normal sexual activity in hyperprolactinemic males.


 
Top

Dostinex (Cabergoline) articles in the treatment of Restless Legs Syndrom (RLS):

Role of dopamine receptor agonists in the treatment of restless legs syndrome.

Happe S, Trenkwalder C.
Department of Clinical Neurophysiology, University of Gottingen, Gottingen, Germany 2004


The restless legs syndrome (RLS) is defined by four essential criteria obligatory for clinical diagnosis which were established, and recently revised, by the International RLS Study Group. These are (i) the urge to move the legs, usually accompanied or caused by uncomfortable and unpleasant sensations in the legs, which are (ii) worse during rest/inactivity, (iii) partially or totally relieved by movement and (iv) worse at night/in the evening. Treatment with levodopa leads to symptom relief, but augmentation (occurrence of symptoms before levodopa administration in the evening) may occur, limiting the long-term use of this drug.

This article gives an overview of the treatment in general and the role of dopamine receptor agonists in the therapy of RLS and periodic limb movements (PLMs). Dopamine receptor agonists are widely used as an effective treatment for RLS and PLMs, presumably because of their longer half-lives, lower likelihood of augmentation and good tolerability compared with levodopa. It was shown that, for example, pergolide, ropinirole, pramipexole and cabergoline (dostinex) alleviated RLS symptoms in 70-90% of patients. A new non-oral (transdermal) formulation of one dopamine receptor agonist, rotigotine, has recently been developed and shown to be efficacious in RLS. Further research should focus on long-term observations and comparisons of different dopamine receptor agonists in RLS.

Cabergoline (Dostinex) is an effective single-drug treatment for restless legs syndrome: clinical and actigraphic evaluation.

Zucconi M, Oldani A, Castronovo C, Ferini-Strambi L.
Sleep Disorders Center, Department of Neurology, H San Raffaele Scientific Institute and Hospital, Universita Vita-Salute San Raffaele, Milan, Italy. Nov 2003

STUDY OBJECTIVES: To evaluate the efficacy and the safety of cabergoline (Dostinex), a dopamine-receptor agonist with a long half-life, in restless legs syndrome (RLS). DESIGN: A 2 month, single blind, open labeled clinical trial. Patients were evaluated with polysomnography at baseline (B), following 1 week of placebo (T0), and after 1 week (T1) and 2 months (T2) of cabergoline treatment. The clinical global impression was assessed using International RLS Study Group Rating Scale and nocturnal actigraphy. SETTING: Sleep Disorders Center. PATIENTS: Twelve patients with moderate to severe RLS (mean age 56.6 years) who were naive to treatment with dopaminergic agents. INTERVENTIONS: Upward titration of cabergoline (from 0.5 mg to 2 mg) in a single evening dose.

MEASUREMENTS AND RESULTS: Ten patients completed the study (mean dose, 1.1 mg), and all showed an improvement of RLS symptoms. The results from the International RLS Study Group Rating Scale showed similarities between B (24.3+/-2.9) and T0 (23.1+/-5.9; P=0.6), with significant improvement at T1 (12.5+/-6.0; P=0.01 vs B and T0) and T2 (9.8+/-6.9; P=0.001 vs B and P=0.005 vs T0). The mean nocturnal activity value measured by actigraphy during week 1 decreased from T0 (19.8+/-9.3) to T1 (13.6+/-6.4) and dropped significantly at T2 (8.5+/-5.3; P=0.05). Nine patients continued the treatment up to 12 months with consistent efficacy, few side effects, and no augmentation.

CONCLUSIONS: Low doses of cabergoline (Dostinex) showed effectiveness and safety in patients with moderate to severe RLS, with no appearance of augmentation phenomenon. Double blind, crossover, polysomnographic studies are necessary to confirm this preliminary data.

Clinical data on restless legs syndrome: a dose-finding study with cabergoline (Dostinex)

Stiasny K.
Department of Neurology, Center of Nervous Diseases, Marburg, Germany. 2001

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. Copyright 2001 S. Karger AG, Basel


 
Top

Dostinex (Cabergoline) for the arrest of lactation

Arrest of lactation after 2nd trimester abortion with a single dose of cabergoline (Dostinex) in comparison with 10-day administration of teguride

Pavlista D, Calda P, Zivny J.
Gynekologicko-porodnicka klinika 1. LF UK a VFN v Praze. Jan 2003

Mother breast feeding - arrest of lactation OBJECTIVE: The objective of the work was to compare the effectiveness and tolerance of a single administration of 1 mg cabergoline and 10-day administration of 1.5 mg terguride divided into three doses after 8-hour intervals, in the indication of arrest of lactation after an abortion during the second trimester. TYPE OF STUDY: Prospective clinical study. NAME AND PLACE OF DEPARTMENT: Gynaecological and Obstetric Clinic. First Medical Faculty, Charles University and General Faculty Hospital Prague, Apolinarska 18, Prague 2. METHOD: During the period between January and October 2000 to 41 patients after abortion induced during the 2nd trimester terguride, 0.5 mg after 8-hour intervals, was administered for a 10-day period. During the subsequent period from November 2000 to September 2001 to 43 patients cabergoline was administered in a single dose within 12 hours after the abortion.

During hospitalization the patients were asked daily for their subjective evaluation of the effect of treatment (vertigo, palpitations, headache, nausea, vomiting, abdominal pain, sleepiness, secretion from the breast, tension in the breasts) and the doctor evaluated the success of treatment objectively. Within 21 days after the abortion the patients were addressed over the phone on subjective and objective effects of treatment. For statistical evaluation Fisher's exact bilateral test was used. RESULTS: The "cabergoline" group displayed, as compared with the "terguride" group, significantly fewer undesirable effects (p < 0.01). No significant difference was found between groups (p = 0.1) as regards the necessity to repeat administration of the drug. None of the undesirable effects were so serious to call for interruption of treatment. CONCLUSION: Arrest of lactation during the second trimester of gestation is an integral part of care of the patient. Symptoms associated with lactation are adversely accepted by the patient.

The incidence of undesirable effects after a single dose of cabergoline is significantly lower as compared with 10-day administration of terguride. A single dose of cabergoline (Dostinex) during hospitalization improves the patients' compliance and thus the effect of treatment. Cabergoline (Dostinex)can be used as the drug of first choice for arrest of lactation after abortion during the second trimester of pregnancy.

Dostinex - the most effective medicine for inhibition of postpartal lactation

Bozhinova S, Porozhanova V, Penkov V. 2001

The aim of the authors is to confirm the efficiency of the Dostinex for prevention an inhibition of the puerparal Lactation. Dostinex is a dopamine ergoline derivation that strongly decrease the Prolactin secretion and has a long-lasting effect. 20 parturients were treated with Dostinex and the most common indication was: death fetus (12 cases), disorders of the nipples (2 cases) and 1 occasion with epilepsy, thrombophlebitis and thromboembolic disease of the V. ileofemoralis, polymastia and polythelia and fetal malformations and in 2 women with hypergalactemy was given for inhibition of the lactation (1/2 table. For 4 days).

The treatment is based on two tablets daily in the first 24 h. after delivery in 6 cases and for the other--2 x 1/2 table. daily for 2 days. Our conclusion is that Dostinex is the most effective agent for prevention of the postpartal lactation given once a day (2 table.) in the first 24 h. post delivery. We read good effect when the medicine was taken twice daily x 1/2 table. for 2 days. Dostinex shows vary good compliance and low rate of relapse of the Lactation.


 
Top

Dostinex (Cabergoline) for the treatment of depression

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

Takahashi H, Yoshida K, Higuchi H, Shimizu T, Inoue T, Koyama T.
Department of Neuro-Psychiatry, Akita University School of Medicine, 1-1-1 Hondo, Akita, Japan. Sep-Oct 2003

We illustrate 2 patients with depression who attained dramatic improvement of energy loss and fatigue when treated with cabergoline (Dostinex), 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.


Top

Dostinex (Cabergoline) in the treatment of acromegaly

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

Marzullo P, Ferone D, Di Somma C, Pivonello R, Filippella M, Lombardi G, Colao A.
Department of Molecular and Clinical Endocrinology and Oncology, Federico II University, Naples, Italy. 1999

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.

Top

The information presented on this site is non professional and non medical
You must consult and get your doctor's approval before using any prescription medication
Please make sure to read and agree to the disclaimer before making a purchase or using info
Dostinex & Cabaser are trademarks and property of Pharmacia & Upjohn
Parlodel is a trademark and property of Novartis
All trademarks and copyrights belong to their respective owners and are acknowledged.
You need to have a prescription to order for more info check order page
Buy-Dostinex.com site is independent and is not affiliated in any way with any pharmaceutical companies
Policies