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PubMedDate not supplied

Dopamine agonist pergolide prevents levodopa-induced quinoprotein formation in parkinsonian striatum and shows quenching effects on dopamine-semiquinone generated in vitro.

The neurotoxicity of dopamine (DA) quinones that appears in dopaminergic neuron-specific oxidative stress has recently been shown to play a role in the pathogenesis and/or progression of Parkinson disease. To clarify the effects of a DA agonist, pergolide, on the levodopa-induced elevation of quinones, the authors examined striatal changes in quinoprotein using a hemi-parkinsonian mouse model. The level of striatal quinoprotein was significantly elevated specifically on the parkinsonian side, but not on the control side, after repeated levodopa administration. This levodopa-induced increase in striatal quinoprotein was almost completely suppressed by adjunctive administration with pergolide on the lesioned side. Furthermore, it was clarified that pergolide scavenged DA-semiquinones generated in vitro in a dose-dependent manner. These suppressive and quenching effects of pergolide against cytotoxic DA quinones may play a key role in its neuroprotective mechanism in the parkinsonian brain.

Animals↗
PubMed2005

A randomly assigned double-blind cross-over study examining the relative anti-parkinsonian tremor effects of pramipexole and pergolide.

This study examined the relative anti-Parkinson's disease (PD) tremor potencies of pergolide and pramipexole in people with PD, using a 3-month double-blind cross-over design. Patients were randomly assigned to receive either pergolide and then pramipexole (n=9) or vice versa (n=8). The dose of the respective dopamine agonist was increased according to a titration schedule up to a maximum 1.5 mg t.d.s., with cross-over at 10 weeks. Assessments were performed at baseline, 4, 8 and 12 weeks. The primary outcome measures were the differences in the clinical (rest and postural) tremor scores on pergolide versus pramipexole. Seventeen PD patients (11 females and six males) with a mean age 68.4 years (range: 55-84 years) and a mean disease duration of 3.9 years (range: 2 months to 13 years) participated in the study. Twelve of the patients were taking other anti-parkinsonian medications. Two patients dropped out of the study whilst on pergolide. Fifteen of 16 patients were able to cross-over from one dopamine agonist to the other, without major retitration. There were no significant differences between the effects of the two drugs on the primary outcome measures, suggesting that the anti-PD tremor efficacies of dopaminergic medications are not dependent on differential affinities for dopamine receptor types.

Aged↗
PubMed1985

Rotational behaviour elicited by intracerebral injections of apomorphine and pergolide in 6-hydroxy-dopamine-lesioned rats. II: The striatum of the rat is heterogeneously organized for rotational behaviour.

The present study compares the role of the nucleus accumbens and the striatum, as well as various regions of the striatum, in the ability of intracerebral injections of the dopamine agonists apomorphine and pergolide to elicit rotational behaviour in 6-hydroxy-dopamine-lesioned rats. We found that apomorphine and pergolide elicit rotational behaviour when injected into the denervated striatum, but not when injected into the ipsilateral nucleus accumbens. The striatum seems heterogeneously organized as regards rotational behaviour since maximal-apomorphine rotation was elicited from the corpus of the striatum as compared to the effects produced by injections into the head and the tail of the striatum. This topographical distribution is similar to the distribution of dopamine-stimulated cyclic AMP. The pergolide response is more evenly distributed in the striatum. It is suggested that the difference in the topographical distribution of the ability of apomorphine and pergolide to elicit rotational behaviour reflects a regional distribution of dopamine receptors in the striatum of the rat.

Animals↗
PubMed1982

Reduction in size of prolactin-secreting tumours in men treated with pergolide.

The effect of pergolide mesylate was studied in two previously untreated men with large prolactinomas and exceptionally high prolactin concentrations. The study was designed to determine whether pergolide would be effective in alleviating symptoms, correcting hormonal abnormalities and shrinking the tumour. Starting with 50 micrograms daily the dose of pergolide was slowly increased over 10 weeks to 1 mg once daily, when repeat assessment was performed. Both patients reported complete relief of symptoms, with no side effects. Serum prolactin concentration was suppressed to normal in both subjects, and evidence to suggest tumour shrinkage was observed. Pergolide appears to be effective treatment for men with large prolactinomas.

Antineoplastic Agents↗
PubMed1983

Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia.

Twenty five patients with hyperprolactinaemia were treated with pergolide mesylate, a new dopamine receptor agonist. Twenty three received treatment for six to 20 months, and in all serum prolactin concentrations were considerably reduced. In most patients prolactin concentrations were maintained in the normal range by a low, once daily dose of pergolide and reversal of associated reproductive disorders was observed. Tumour volume as assessed by computed tomography decreased considerably during treatment in three out of four patients with a pituitary tumour. The drug was well tolerated. Side effects were similar to those of bromocriptine, but four out of eight patients who had been forced to stop taking bromocriptine because of untoward effects were subsequently able to tolerate treatment with pergolide. Pergolide mesylate promises to be a useful addition to the currently available long acting dopamine agonists in the management of hyperprolactinaemia.

Adult↗
PubMed1988

Parkinson's disease: an open label trial of pergolide in patients failing bromocriptine therapy.

Sixty-three patients with Parkinson's disease who failed bromocriptine therapy for various reasons were treated in an open-label trial of pergolide. The data were evaluated in a retrospective manner. Forty-six percent had a good response and tolerated the pergolide. A comparison of the outcomes regarding response and toxicity revealed that bromocriptine and pergolide act differently in individual patients. A trial of pergolide in Parkinsonian patients failing bromocriptine therapy may be therapeutically useful.

Adult↗
PubMed1986

Efficacy of pergolide and mesulergine.

The activity of pergolide, a clavine ergolene, and mesulergine, an 8-alpha amino ergoline, were compared in 18 patients with advanced Parkinson's disease. All of the patients were no longer satisfactorily responding to levodopa, and 16 patients had diurnal oscillations in performance. Pergolide, mean dose 2.7 mg, when added to levodopa resulted in a significant (27%) decrease in Parkinson disability and a significant improvement in diurnal oscillations in performance (136% increase in hours 'on'). Twelve of the 18 patients (67%) improved. However, after 2 years pergolide was discontinued in all of the patients because of decreased efficacy, adverse effects, or both. At this time, mesulergine, mean dose 9.3 mg., when added to levodopa resulted in a significant (37%) decrease in Parkinson disability and a significant improvement in diurnal oscillations (61% increase in hours 'on'). Twelve of the 18 patients (67%) improved. Adverse effects (dyskinesias) were less with mesulergine than with pergolide. A declining response to one agonist does not preclude a successful response to another agonist of a different class.

Aged↗
PubMed2005

Nocturnal activity with nighttime pergolide in Parkinson disease: a controlled study using actigraphy.

Pergolide is a dopamine agonist that improves Parkinson disease but is associated with dose-dependent sleepiness. This study evaluates the effect of a nighttime dose of 1 mg of pergolide on actigraphic measures of sleep using a randomized, double-blind, placebo-controlled study design. The pergolide group (n = 10) worsened in actigraphic measures of sleep efficiency and sleep fragmentation vs the placebo group (n = 12). Side effects were more frequent in the pergolide group.

Age Factors↗
PubMed1982

Pergolide mesylate and idiopathic Parkinson disease.

We studied the effects of pergolide mesylate in an open trial of 23 patients with idiopathic Parkinson disease (PD). All had suffered from loss of efficacy or dose-limiting side effects on current antiparkinsonian regimens. On pergolide therapy, improvement, which was maintained for 6 months, was noted in some parkinsonian features in all 23 patients. All patients suffering from on-off phenomenon were helped by pergolide. Significant side effects were not encountered. Pergolide is useful in the treatment of PD.

Adolescent↗
PubMed1983

Controlled trial of pergolide mesylate in Parkinson's disease and progressive supranuclear palsy.

We evaluated pergolide in 22 patients with Parkinson's disease and 3 with progressive supranuclear palsy (PSP). After achieving an optimal dose of pergolide and Sinemet, a matching placebo was substituted in double-blind manner. The mean dose of levodopa (in Sinemet) was reduced by 68%; in eight patients, pergolide completely replaced levodopa. In parkinsonian patients, the mean Hoehn-Yahr stage decreased from 3.2 to 1.6, and the mean total disability score decreased from 48.3 to 17.8. In 10 patients with on-off phenomenon, the time on increased 174% with pergolide. There was little effect in PSP. Postural light-headedness and reversible mental changes were seen.

Adult↗
PubMed2006

Pergolide-associated valvular heart disease.

Pergolide is an ergot derivative dopamine agonist used in the treatment of Parkinson's disease and restless legs syndrome. Ergot derivatives are known to be associated with fibrotic conditions, including a carcinoid-like, fibrotic, valvular heart disease (VHD). Recently, pergolide was identified in association with the development of VHD. This article includes a summary of the literature published on pergolide-associated VHD, a description of the potential mechanisms of drug-induced VHD, and the clinical implications for the management of patients taking pergolide.

Dopamine Agonists↗
PubMedDate not supplied

Modification of dopamine D2 receptor activity by pergolide in Parkinson's disease: an in vivo study by PET.

It is well known that chronic administration of pergolide and other dopamine agonists may induce a downregulation of dopamine D2 receptors in the rat model of Parkinson's disease (PD). To our knowledge, this effect has not been demonstrated in vivo in patients with PD. At present, the status of striatal dopamine D2 receptors can be studied with use of positron emission tomographic (PET) technology. Five patients with PD chronically treated with levodopa were studied with use of PET and [11C]-raclopride before and after 6 months of pergolide treatment (dose range = 4.5-7.5 mg/d). We found a slight reduction in the specific striatal [11C]-raclopride uptake index (mean reduction 14% in putamen and 9% in caudate) after pergolide treatment. This reduction appears to be related to downregulation of the receptor, although competitive binding of pergolide at the D2 receptor cannot be excluded.

Antiparkinson Agents↗
PubMed1992

General pharmacology of pergolide in animals. 2nd communication: gastrointestinal, renal and miscellaneous studies.

Pergolide mesylate ((8 beta)-8-[(methylthio)methyl]-6-propylergoline monomethanesulfonate, LY 127809, CAS 66104-23-2) is a novel and potent dopamine agonist marketed for treating the symptoms of Parkinson's disease. The potential secondary pharmacological effects of this agent on the gastrointestinal and renal systems, as well as effects on local anesthesia, hemolysis, platelet aggregation, circulating blood glucose, primary antibody production, and the acute inflammatory response were examined. Pergolide exhibited significant pharmacological effects in gastrointestinal, renal and anti-inflammatory tests at high oral doses. Pergolide was essentially inactive in blood hemolysis, platelet aggregation, primary antibody production and local anesthesia testing. In summary, these studies confirm the pharmacological selectivity of pergolide, and indicate a low potential for secondary pharmacological side effects upon the functions tested at clinically relevant doses.

Anesthetics, Local↗
PubMed1986

Control of hyperprolactinemia with pergolide.

Ten patients with clinical, laboratory and radiographic evidence compatible with the diagnosis of prolactinoma were treated with two dopamine agonists. One group (N = 6) took bromocriptine and the other group (N = 4) used pergolide, a longer-acting agent. Both medications were found to reduce prolactin levels significantly from baseline, but an oscillatory pattern with significant fluctuation was seen in the mean prolactin levels in the patients taking bromocriptine. Three patients did not achieve euprolactinemia on bromocriptine, 2.5 mg qid, the maximum dose used in this study. All of the study group taking pergolide became euprolactinemic rapidly; no more than a single dose of 100 micrograms/day was required. Tumor reduction was noted in two patients taking bromocriptine and two taking pergolide. The duration of side effects was shorter and compliance was improved on pergolide therapy.

Bromocriptine↗
PubMed1987

Effects of pergolide on the cardiovascular responses to sinoaortic deafferentation in dogs with intact or surgically decentralized adrenal glands.

In pentobarbital-anesthetized dogs with decentralized adrenal glands, sinoaortic baroreceptor deafferentation produced an increase in mean aortic blood pressure which reached a maximum (42 +/- 5 mm Hg, n = 6) within 5 min and then waned entirely within the subsequent 25 min. In contrast, in sham-operated dogs, the maximal pressor response due to deafferentation was of greater magnitude (63 +/- 6 mm Hg, n = 8) and of much longer duration (44 +/- 4 mm Hg, 60 min after deafferentation). Heart rate was only augmented slightly in both preparations. A marked elevation of epinephrine plasma concentration occurred 5 min after deafferentation and the magnitude of this effect was 8 times greater in dogs with innervated than denervated adrenal glands. Norepinephrine plasma concentration increased moderately and similarly in the two preparations. Administration of pergolide (30.0 micrograms/kg i.v.) 15 min before undertaking the deafferentation procedure induced a small, short-lasting increase in blood pressure and a small fall in heart rate in dogs in which the innervation to the adrenal glands was left either intact (sham-operated) or removed surgically. In dogs with adrenal gland denervated, pergolide blocked entirely the pressor response and the small elevation in plasma concentration of catecholamines evoked by sinoaortic deafferentation in the matched, saline-pretreated group. However, in sham-operated dogs (intact adrenal innervation), pergolide reduced partially (by 41%) the increase in blood pressure and plasma epinephrine concentration caused by deafferentation. The decrease in heart rate, produced by pergolide, was abolished by deafferentation in sham-operated and adrenal decentralized dogs.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenal Glands↗
PubMed1985

Effects of pergolide on diethylstilbestrol-induced rat pituitary hyperplasia.

Hyperplastic anterior pituitary glands were produced in female rats by treatment with 10 mg of diethylstilbestrol in Silastic tubing. This led to increased numbers of immunoreactive prolactin cells and increased serum prolactin levels. After 6 weeks of diethylstilbestrol treatment, one group of rats was treated with daily injections of pergolide for 3 weeks. Pergolide produced a significant decrease in pituitary gland weight and in serum prolactin levels but did not change the percentage of prolactin cells significantly, compared with that of control rats. Ultrastructural studies showed a significant increase in the numbers of prolactin secretory granules and numerous large intracellular bodies with associated secretory granules in pituitaries from rats treated with pergolide. In one group of rats in which the diethylstilbestrol was discontinued for 3 weeks after 6 weeks of treatment there was a significant decrease in pituitary gland weight and serum prolactin and a significant decrease in the percentage of prolactin cells, compared with values in the rats treated with diethylstilbestrol for 9 weeks. These results indicate that pergolide causes decreased release of prolactin from secretory granules in anterior pituitary prolactin cells and an increase in the numbers of PRL secretory granules per cell but does not change the percentage of prolactin-producing pituitary cells after 3 weeks of treatment.

Animals↗
PubMedDate not supplied

The long-acting dopamine agonist pergolide mesylate for treatment of hyperprolactinaemia.

Seven hyperprolactinaemic women were treated with the new, long-acting dopamine agonist pergolide mesylate. The treatment resulted in normalization of the prolactin secretion in four of the seven women and six of them experienced regular uterine bleedings. Four of the patients had previously discontinued bromocriptine because of adverse effects but had no problems to tolerate pergolide. One bromocriptine-resistant woman was unresponsive also to pergolide therapy. Reported side-effects in the seven women were mild and transient. Pergolide mesylate may be a valuable alternative to bromocriptine in the management of patients with hyperprolactinaemia.

Adult↗
PubMed1984

Pergolide and lisuride in advanced Parkinson's disease.

In a retrospective study, treatment with lisuride was compared to pergolide in 25 patients with advanced PD in whom the response to levodopa had diminished. Sixteen patients had wearing off and/or ON-OFF phenomena. Lisuride or pergolide, when added to levodopa, resulted in comparable and significant decreases in disability in both ON and OFF periods; pergolide resulted in a greater increase in the number of hours in which patients were ON. Adverse reactions were comparable on both drugs. However, patients who developed an adverse reaction on one drug did not necessarily develop the same reaction on the other drug. Both lisuride and pergolide are effective anti-Parkinson drugs.

Aged↗