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PubMed1986

Inhibition of SKF 38393- and pergolide-induced circling in rats with unilateral 6-OHDA lesion is correlated to dopamine D-1 and D-2 receptor affinities in vitro.

The effects of 30 dopamine (DA) antagonists, including 4 as stereoisomeric pairs, on circling behaviour induced by the D-1 agonist SKF 38393 and the D-2 agonist pergolide in rats with unilateral 6-hydroxy-DA lesions have been studied. SKF 38393-induced circling was selectively blocked by the specific D-1 antagonists SCH 23390 and SKF 83566, and was furthermore blocked by other DA antagonists with potencies correlating to their affinities to D-1 receptors labelled by 3H-SCH 23390 in vitro. Pergolide-antagonistic potencies in contrast correlated to affinities to D-2 receptors labelled by 3H-spiperone in vitro. Pergolide-induced circling was selectively blocked by the specific D-2 antagonists in the benzamide series. No interaction between D-1 and D-2 antagonists was observed in combination experiments with SCH 23390 and YM 09151-2 in both circling models. Among other reference neurotransmitter antagonists acting on alpha- and beta-adrenoceptors, histamine, serotonin and muscarinic receptors, only the alpha 1-adrenoceptor antagonist prazosin was effective in high doses. In contrast, the alpha 2- and beta-adrenoceptor agonists clonidine and clenbuterol as well as the muscarinic agonist RS 86 inhibited circling induced by SKF 38393 as well as pergolide. The 5-HT1A agonist 8-OHDPAT inhibited pergolide-induced circling only. It is concluded that these two behavioural models are selective in vivo measures of relative D-1 and D-2 receptor activity of DA antagonists.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed1990

Antagonism by domperidone of the ocular hypotensive effect of pergolide.

1. The effect of pre-dosing with 15 mg domperidone, a relatively selective dopamine 2-receptor antagonist, on the ocular hypotensive action of a single oral dose of 25 micrograms pergolide, a dopamine 2-receptor agonist, was studied in 9 normal human volunteers, using a non-invasive method. 2. Compared with domperidone followed after 1 h by placebo, placebo followed after 1 h by pergolide had an ocular hypotensive effect in both eyes. Domperidone followed after 1 h by pergolide had no effect on intraocular pressure in both eyes. 3. The results of this study showed that domperidone inhibited the ocular hypotensive action of pergolide, suggesting that pergolide reduces intraocular pressure by the stimulation of the peripheral dopamine 2-receptors.

Adult↗
PubMed2004

Pergolide effect on cognitive functions in early-mild Parkinson's disease.

In the present study, we evaluated the effect of pergolide, a mixed D1/D2 agonist, on cognitive function in mild Parkinson's disease (PD). After a two-week wash-out phase, twenty patients with a Hoehn and Yahr score </=2.5 entered a 16-week, cross-over study in which the order of administration of pergolide or 1-dopa was randomly assigned. Cognitive assessment was performed after the wash-out phase and repeated after eight weeks (before patients were switched to the other drug) and at the end of the study. There were no significant differences in test scores among the three experimental modalities (off-treatment vs. l-dopa, off-treatment vs. pergolide, pergolide vs. l-dopa). In another cohort of comparably mild PD patients we had previously demonstrated that pramipexole, a mixed D2/D3 agonist, slightly but significantly worsened verbal fluency in comparison to l-dopa; moreover, pramipexole impaired short term verbal memory and attentional-executive functions in comparison to both l-dopa and the off-treatment condition. Taken together, these findings suggest that dopamine agonists may influence cognition in PD according to their pharmacological characteristics. Unlike the D2/D3 agonist pramipexole, pergolide and l-dopa, both of which stimulate D1- and D2-receptor subtypes, do not appear to impair cognitive function.

Aged↗
PubMed1991

Effects of oral pergolide mesylate on nociceptive spinal cord reflexes in rats.

The effects of orally administered pergolide mesylate on the flexor reflex were evaluated in chronic spinal rats. The mixed D1/D2 agonist pergolide (0.1 to 3.0 mg/kg) produced a dose-related decrease in the magnitude of the flexor reflex elicited by a tetanic stimulus. The effects of pergolide were blocked by haloperidol, demonstrating that the effects of pergolide were mediated through dopamine receptors. In contrast, the selective D2 agonist bromocriptine (3.0 to 30 mg/kg) had no effect on the flexor reflex. The present results are consistent with the interpretation that pergolide produces an antinociceptive action at the spinal cord level by stimulating both D1 and D2 dopamine receptors.

Animals↗
PubMed1995

Pergolide interactions with nicotine and pilocarpine in rats on the radial-arm maze.

Antagonists of nicotinic and muscarinic acetylcholinergic (ACh) receptors have significant interactions with dopaminergic (DA) ligands with regard to radial-arm maze choice accuracy. The current studies examined the interactions of agonists of nicotinic and muscarinic ACh receptors with the DA agonist pergolide. Pergolide given in a range from 0.03-1.0 mg/kg had no detectable effect on radial-arm maze choice accuracy when given alone. With this dose range there was a linear increase in response latency. Pergolide had significant interactive effects with the nicotinic and muscarinic agonists nicotine and pilocarpine. Given together with nicotine, pergolide produced a significantly elevated linear increase in accuracy relative to when it was given alone. With pilocarpine, pergolide had an inverted U-shaped effect improving choice accuracy at low to moderate doses of 0.03 and 0.1 mg/kg. These results support previous findings of DA-ACh interactions with regard to radial-arm maze choice accuracy. Combined DA-ACh treatment may be a useful treatment of cognitive dysfunction.

Animals↗
PubMed1988

Further characterization of tolerance to the corticosterone-elevating effect of pergolide in rats.

Four daily injections of pergolide, an ergoline dopamine agonist, made male rats tolerant to the corticosterone-elevating effects of an acute injection of pergolide on the fifth day. This tolerance occurred not only to acute treatment with pergolide, but also to other dopamine agonists differing in structure, potency and receptor subtype selectivity. Plasma corticosterone was elevated following administration of opioid or serotonin agonists in both vehicle- and pergolide-pretreated rats. The current findings strengthen the conclusion that tolerance to the acute elevation of corticosterone by pergolide is not due to impairment of pituitary-adrenocortical function but instead to changes in dopamine receptors that initiate the response.

Animals↗
PubMed2004

Effects of pergolide on nocturia in Parkinson's disease: three female cases selected from over 400 patients.

We started the subject screening from over 400 patients with Parkinson's disease using strict selection criteria to identify the patients with nocturia who would allow accurate and efficient evaluation of the pergolide effects. The subjects were confined to female patients to exclude patients with potential prostate hypertrophy. The patients treated with bromocriptine at 7.5-15 mg/day adjunctive to l-dopa were selected to replace bromocriptine with pergolide of the equivalent dosage approved in Japan. The nocturia was defined as having more than two episodes of urination during sleep per night on average. The subjects received the urinary sediment test before and during the study for screening urinary tract infection and the study was discontinued when urinary tract infection was found. As a result, we identified total 11 patients with nocturia and three of those completed the 12-week study of switching dopamine agonist from bromocriptine to pergolide. We observed a decrease in nocturia frequency in all three patients, a decrease in irritative urinary symptoms in two and an improvement of sleep QOL in two. The effect of pergolide on nocturia was independent of improvement of parkinsonian symptoms, suggesting a distinct mechanism from that of anti-parkinsonian effects. Our study also suggests that switching from bromocriptine to pergolide improves nocturia, thereby improving sleep status of patients with Parkinson's disease.

Aged↗
PubMed2005

The long-lasting improvement of sexual dysfunction in patients with advanced, fluctuating Parkinson's disease induced by pergolide: evidence from the results of an open, prospective, one-year trial.

Fourteen male patients suffering from Parkinson's disease, each of whom had been treated with L-DOPA, and in whom additional treatment with oral dopamine agonist (DA) was needed, were followed for a period of one year. Pergolide mesylate (Permax) was given to each patient, and titrated to a total daily dose of 3 mg. All of the patients were taking L-DOPA. The assessments performed before the start of pergolide treatment consisted of neurological examination, unified Parkinson's disease rating scale (UPDRS) III and IV subscales scoring, mini mental state examination (MMSE) scoring, the neuropsychological examination including Zung scale scoring, biochemical and hematological examinations including prolactine serum levels; and a sexological examination during which the patients filled-in the international index of erectile function (IIEF) questionnaire. These examinations were repeated during the control assessments at months 1, 3, 6 and 12. ANOVA, non-parametric Friedmann's ANOVA and Tukey post hoc tests were used for the statistical analysis. There were statistically significant differences between the values of UPDRS III motor subscale and all subscales of IIEF when months 0 and 1 were compared with the results obtained at months 3, 6 and 12. Pergolide mesylate, when added to L-DOPA, significantly improved all sexual functions in younger male Parkinsonian patients who were still interested in sexual activities. The treatment with pergolide in these cases might be more beneficial than with short-acting PDE-5 inhibitor sildenafile. Nevertheless, the relationship between pergolide treatment and incidence of restrictive valvular heart disease must be considered.

Aged↗
PubMed2005

High-dose treatment with pergolide in Parkinson's disease patients with motor fluctuations and dyskinesias.

Motor complications arising after long-term treatment with levodopa remain one of the main challenges in the treatment of patients with Parkinson's disease (PD). Monotherapy with dopamine agonists may delay the onset of motor complications or reduce their severity when added to levodopa treatment. Here, we retrospectively analyzed data from 62 patients with advanced PD who presented with moderate to severe response fluctuations in whom we increased the dose of oral treatment with pergolide beyond 4.5mg daily. Patients had been treated with levodopa for 10.7+/-4.8 years. Pergolide was increased to 8.2+/-4.3 mg per day over a median titration period of 13.5 weeks. Mean daily dose of levodopa prior to pergolide high-dose treatment was 733+/-468 mg and decreased to 348+/-186 mg after pergolide titration. The duration of OFF times decreased from 7.3+/-3.8 to 1.7+/-0.9 h per day (p < 0.001) measured by patients' diaries. Dyskinesias, present for 5.0+/-3.3 h per day at baseline, were reduced to 1.4+/-0.8 h per day (p < 0.001) and the total daily duration of motor fluctuations (off-time duration plus dyskinesia duration) decreased from 10.5+/-7.0 to 2.8+/-2.2 h (p < 0.001). There was a significant improvement in parkinsonian symptoms (baseline to endpoint reduction of UPDRS III from a median of 36 to 8; p < 0.001). To reduce gastrointestinal side effects 23 patients required concomitant treatment with domperidone. Seven patients developed hallucinations during the titration period, six patients required treatment with clozapine. Our data indicate that increasing the dose of pergolide above 5mg per day can dramatically reduce the need for levodopa, motor fluctuations and severity of clinical symptoms. Controlled trials are needed to further substantiate the efficacy and safety of this treatment strategy.

Adult↗
PubMed2005

[Pergolide associated valvulopathy: critical analysis of the literature and practical recommendations].

INTRODUCTION: Pergolide is a widely used antiparkinsonian dopamine agonist. Following occasional case reports, two studies recently suggested potentially frequent and severe valvular disease associated with pergolide intake. STATE OF ART: Although there is now strong evidence to consider that pergolide may induce valvulopathy, incidence, severity, and risk factors for this adverse effect remain to be clarified. Valvular disease associated with pergolide consists in fibrosis and resembles conditions described in carcinoid carcinoma and in patients taking fenfluramine therapy. The mechanisms leading to valvular fibrosis are unknown but involvement of 5-HT(2B) receptors, especially expressed in valvular fibroblasts, is suspected. PERSPECTIVES AND CONCLUSIONS: Following the recommendations of the Agence Française de Sécurité Sanitaire des Produits de Santé, we describe a clinical practice attitude for pergolide therapy in Parkinson's disease.

Antiparkinson Agents↗
PubMed2000

A double-blind, placebo-controlled outpatient trial of pergolide for cocaine dependence.

Results of preclinical studies suggest that pergolide, a mixed D(1)/D(2) dopamine receptor agonist, may be useful in treating cocaine dependence. To empirically investigate this possibility, we conducted a 5-year, double-blind, placebo-controlled clinical trial of two doses of pergolide (0.05 and 0.25 mg bid) in subjects with cocaine dependence and combined cocaine/alcohol dependence. Data analysis was performed on an intent to treat population (N=358) and a per protocol population (N=108) with urine drug screens (UDS) used as the main outcome measure. There were no significant effects on UDS at either pergolide dose. Pergolide had no significant effect on alcohol use in the comorbid alcohol/cocaine dependence group. Pergolide does not appear to have clinical value in the treatment of cocaine dependence or in decreasing alcohol use in cocaine-dependent individuals at the presently studied doses.

Adolescent↗
PubMed2000

Effects of chronic levodopa and pergolide treatment on cortical excitability in patients with Parkinson's disease: a transcranial magnetic stimulation study.

OBJECTIVES: Transcranial magnetic stimulation was used to assess the effects of chronic levodopa and pergolide treatment on motor cortex excitability in Parkinson disease (PD). METHODS: Motor thresholds, intracortical inhibition and facilitation were studied at baseline and after 6 and 12 months of therapy in 10 PD patients and compared to 7 age-matched controls. RESULTS: At baseline, there was significantly less intracortical inhibition with only a slight reduction of intracortical facilitation in PD as compared to controls. Relative to pretreatment condition, levodopa restored intracortical inhibition for 12 months while pergolide did not. Intracortical facilitation was always within the normal range. Motor thresholds were unchanged in both groups of patients over 12 months. Clinically, levodopa and pergolide improved motor Unified Parkinson's disease rating scale (UPDRS) scores at 6 months but only levodopa maintained benefit at 12 months as compared to baseline. CONCLUSIONS: Levodopa and pergolide differentially affected cortical inhibitory circuits at 12 months. The progressive deterioration of restored intracortical inhibition with pergolide may be due to the development of tolerance and down-regulation of dopamine receptors.

Aged↗
PubMed1982

The use of pergolide, a potent dopamine agonist, in Parkinson's disease.

Pergolide, a semisynthetic ergoline and a potent long-acting adenylcyclase-linked dopamine agonist, was given to 40 patients with advanced Parkinson's disease whose response to levodopa had diminished considerably. The group included 31 patients with marked diurnal oscillations in performance ("wearing off" and/or "on-off" phenomena). Pergolide alone (7 patients) or combined with levodopa (33 patients), resulted in a reduction in disability (P less than or equal to 0.01) as assessed in both the patients' "on" and "off" periods. Pergolide also resulted in an increase (P less than or equal to 0.001) in the number of hours in which patients were on from 3.8 (+/-0.4) to 11.9 (+/-0.9). The mean daily dose of pergolide was 2.4 mg (range 0.1 to 10.0). The mean duration of the study was 12 mo (range 1 to 24). Pergolide is effective in Parkinson's disease and will change the management of patients whose response to levodopa has diminished.

Adult↗
PubMed2003

[Tardive dyskinesia: pergolid, a possible therapeutic option].

OBJECTIVE: There's still no effective treatment established for Tardive Dyskinesia. Aim of the study was to analyse the effect of pergolide, a D1 and D2 receptor agonist with prevalence for presynaptic auto receptors, in oro-facial tardive dyskinesia by means of a double-blind, placebo controlled cross-over study. Low-dose pergolide should activate presynaptic auto receptors, decrease dopamintransmission and reduce tardive dyskinesia. METHOD: Assessment of dyskinesia was performed with the computer-assisted technique Digital-Imaging-Processing in addition to the clinical scale AIMS (Abnormal-Involuntary-Movement-Scale). 10 patients with oro-facial dyskinesia were examined for alteration to dyskinesia, psychopathology, vital functions and laborchemical parameter. RESULTS: Dyskinesia decreased 25 % for relax and 17 % for task conditions under pergolide treatment. Low-dose pergolide showed no side effects or worsening of the psychopathological state. Results of the Digital-Imaging-Processing correlated significantly with the results of clinical AIMS scale, but the computer-assisted technique gives more detailed information about degree and type of the movement disorder. CONCLUSION: Results suggest a therapeutic effect of pergolide in tardive dyskinesia, this has to be verified with a larger study population and longer observation. Assessment of dyskinesia is rater independent and more significant with the computer-assisted technique.

Adult↗
PubMed1983

Pergolide for the treatment of pituitary tumors secreting prolactin or growth hormone.

We gave pergolide mesylate, a new long-acting ergot derivative with dopaminergic properties, to 47 patients with hypersecretion of prolactin or growth hormone. Single doses produced long-lasting reductions of serum prolactin levels; after 24 hours, the values remained depressed at a mean of 28.8 per cent of the base-line value. Among 41 patients (22 women and 19 men) with hyperprolactinemia who took pergolide for three months or more, prolactin levels fell to normal in 37 and remained slightly elevated in 2. In the two patients in whom the levels fell to only 38 to 52 per cent of base line, treatment was regarded as a failure. The level of growth hormone fell to a mean of 52.8 per cent of base line in patients with acromegaly who were taking 100 micrograms of pergolide per day. Among patients for whom adequate CT scans were available, definite tumor shrinkage occurred in 10 of 13 with macroadenomas and definite or probable shrinkage in 5 of 9 with microadenomas. Menses returned in 76 per cent of treated women and testosterone levels rose in 10 of 14 men. We conclude that pergolide reduces hypersecretion and shrinks most prolactin-secreting macroadenomas. In some patients long-term pergolide therapy may be superior to surgery and x-ray treatment.

Acromegaly↗
PubMed1999

Pergolide mesylate for cocaine abuse: a controlled preliminary trial.

A small, controlled study was conducted to assess whether pergolide mesylate has clinical promise as a treatment for cocaine abuse prior to embarking on a larger, randomized, double-blind, controlled trial. Fourteen individuals were placed on placebo for 2 weeks, followed by a 24-week single-blind study in which they were placed on pergolide for 12 weeks, followed by placebo for 12 weeks. Another 14 patients received single-blind placebo for two weeks and then were randomized into a 24-week double-blind, placebo-controlled, multiple baseline design. Initially, patients enrolled in the study were placed on risperidone (n = 9) or placebo (n = 5). During the first 12 weeks, retention was worse for those receiving pergolide compared to risperidone or placebo. Neither risperidone nor pergolide were more efficacious in reducing cocaine use than placebo. Although earlier open studies found pergolide to show promise as a treatment for cocaine abuse, this study did not support these earlier findings. Comparing an agent to both an active control and placebo group may better predict whether a promising new agent will have clinical utility compared to the standard open trial.

Adult↗
PubMed1997

Pergolide in the management of restless legs syndrome: an extended study.

Twenty patients with problematic restless legs syndrome (RLS) were treated with pergolide. Efficacy, dosage, side effects, and tolerance were analyzed. Fifteen patients continued treatment for a median study time of 2 years. Five patients discontinued treatment after a mean of 4.2 months. Pergolide resulted in complete or near complete control of symptoms in 45% and moderate control in 50% of patients studied. Levodopa-induced daytime augmentation resolved in all patients in whom it had been present. The mean total daily maintenance dose of pergolide was 0.23 mg. Forty percent required an additional afternoon dose. Side effects developed in 12 patients (60%) and necessitated discontinuation of treatment in five. Common side effects were nausea, dizziness, and insomnia. Daytime augmentation occurred in 27% of patients, but this was mild and usually easily controlled with a supplementary afternoon dose of pergolide. Tolerance did not develop. We conclude that pergolide is an effective second-line agent for RLS, especially following levodopa-induced daytime augmentation.

Adult↗
PubMed1986

Long-term efficacy of pergolide in patients with Parkinson's disease.

We report the clinical course of 35 patients with Parkinson's disease who experienced an initially favorable response to pergolide and who were taking the drug for at least 6 months. The duration of pergolide treatment was 6-50 (25 +/- 16 SD) months. Of the 14 patients who remained on pergolide for over 2 years, 12 remained less disabled for 26 +/- 17 SD months, seven enjoyed increased "on" time for 39 +/- 8 SD months, and nine had a lower Hoehn-Yahr stage for 25 +/- 17 SD months. Pergolide was discontinued after 5-39 months in eight patients; six patients then deteriorated. Pergolide can remain efficacious in the treatment of Parkinson's disease for up to 50 months.

Aged↗