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At least 145 records · Page 8Linked to original sources
PubMed1997

Dopamine agonist treatment of Tourette disorder in children: results of an open-label trial of pergolide.

This exploratory study was meant to determine the effect of the dopamine (DA) agonist pergolide on Gilles de la Tourette syndrome (GTS) in children and adolescents and to ascertain correlates of pergolide response. Thirty-two outpatients, aged 7-19 years, were systemically assessed in a neuropsychiatric clinic for the presence of GTS and comorbid disorders. After a 6-week open-label, fixed-flexible dosing schedule, response to pergolide on standard GTS severity outcome measures was assessed. Overall, 75% of patients (24/32) had a > 50% drop in their tic severity rating from baseline with a mean treatment dosage of 177 +/- 61 micrograms/day. Highly significant (p = 0.0001) baseline to week 6 differences were demonstrated in all tic symptom measures. The presence of restless legs syndrome (RLS) comorbidity (59%) was highly associated with a positive response. These results suggest DA agonism as a strategy, and pergolide in particular, may be a practical form of therapy for GTS. Response predictors of patient comorbid RLS argue for its further study with regard to GTS.

Adolescent↗
PubMed1984

Pergolide therapy in Parkinson's disease.

A total of 26 patients were treated with pergolide mesylate, a semi-synthetic ergot derivative with the property of direct dopamine activity. Of these patients, 18 suffered from late failure of L-dopa, while the remaining 8 had never before been treated with L-dopa. The aim of the trial was to study the activity of pergolide, either by giving it to untreated patients or by reducing as much as possible the L-dopa given in patients with parkinsonism. Adverse effects and failure rate were reduced by slowly increasing the daily dosage, by giving considerable dose flexibility whenever side-effects were manifest, and by the use of relatively low doses (mean of 3.8 mg in the L-dopa-group and 2.9 in the other group). At present, from 26 patients, 13 (50%) still remain in the study for an average treatment period of 16 months (3 weeks to 25 months for the group as a whole). All patients experienced a beneficial effect from pergolide, especially during the first months of treatment, in selfcare, rigidity, gait and automatic movements. Slight or no improvement was seen in tremor, speech and posture. The most frequent side-effects were nausea and vomiting (in the initial phase of the treatment), insomnia and psychotoxic reactions (mostly periods of confusion accompanied by visual hallucinations and paranoid illusions). The study indicated that pergolide mesylate is a useful additive for treatment of parkinsonism, but special attention should be paid to the important psychotoxic adverse effects that may appear, even at a low dose.

Aged↗
PubMed1986

The effect of the dopamine agonist pergolide on tyrosine hydroxylase activity in rat striatal and limbic miniprisms in vitro: a model for the dopamine autoreceptor?

A method for the assay of tyrosine hydroxylase activity in rat striatal and limbic (nucleus accumbens + olfactory tubercle) brain miniprisms is described. The dopamine agonists apomorphine (1 mumol/l) and pergolide (0.01-100 mumol/l) inhibited the tyrosine hydroxylase activity in both regions. The inhibition produced by 1 mumol/l pergolide was antagonised partially in striatal miniprisms and completely in limbic miniprisms by 1 mumol/l haloperidol. The dopamine D2-selective antagonist raclopride, at concentrations up to 300 nmol/l, did not antagonise the inhibition produced by pergolide in striatal miniprisms, but appeared partially to antagonise the inhibition in limbic miniprisms. It is concluded that whilst pergolide potently inhibits tyrosine hydroxylase activity in striatal and limbic miniprisms, the inhibition is of doubtful value as a predictive model of dopamine autoreceptor function in striatal miniprisms, but may be useful when limbic miniprisms are used.

Animals↗
PubMed1985

Inhibitory effects of apomorphine and pergolide on neurogenic vasoconstriction in the hindquarters of the rat.

The effects of locally administered apomorphine and pergolide were studied in the isolated autoperfused hindquarters of the rat, in an attempt to assess the possible role of presynaptic dopamine receptors at that level in the hypotensive effect of these dopamine agonists. Local infusion of apomorphine (1 micrograms . kg-1 . min-1 for 5 min) or pergolide (1 micrograms . kg-1 . min-1 for 5 min) [into the hindquarters] did not alter perfusion pressure per se, but reduced the pressor response to electrical stimulation of the lumbar sympathetic chains for the whole frequency range used during a cumulative frequency-response curve (0.25-16 Hz, 1 ms, supramaximal voltage). Apomorphine and pergolide reduced the pressor response elicited by 4 Hz electrical stimulation (applied until maximum response was reached) to 54.8 +/- 7.1% and 53.9 +/- 1.7% respectively, but they did not modify similar increases of perfusion pressure produced by locally administered noradrenaline. The inhibition by apomorphine and pergolide of the 4 Hz stimulation-evoked pressor response was completely antagonized by local administration of the dopamine antagonist haloperidol (1 microgram . kg-1), but was not influenced by the alpha 2-antagonist rauwolscine (100 micrograms . kg-1). This dose of rauwolscine antagonized the inhibitory effect of the alpha 2-agonist UK-14,304, which was not influenced by haloperidol. Local administration of rauwolscine increased the pressor response to stimulation at 4 Hz by 37.4-46.2%. In contrast, local administration of haloperidol did not influence the 4 Hz stimulation-evoked pressor response.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1980

Stimulation of adenylate cyclase in rat striatum by pergolide: influence of GTP.

Pergolide stimulates adenylate cyclase activity in homogenates of rat striatum. In contrast, bromocriptine and lisuride are inactive. GTP enhances the stimulation produced by pergolide and has no effect on the other ergots tested. The stimulation produced by pergolide is inhibited by haloperidol but not by molindone. It is concluded that pergolide acts as an agonist at dopaminergic receptors coupled to adenylate cyclase in rat striatum.

Adenylyl Cyclases↗
PubMed1982

Dopaminergic inhibition of cardiac sympathetic nerve function by pergolide.

The effect of pergolide, a dopaminergic ergoline, on cardiac sympathetic neurotransmission was examined in pentobarbital-anesthetized dogs. Positive chronotropic responses to right postganglionic cardioaccelerator nerve stimulation were significantly reduced following infusion of pergolide, 1.25 microgram/kg per min for 10 min, whereas positive chronotropic responses to exogenous norepinephrine were unchanged. Pretreatment with sulpiride but not with yohimbine completely antagonized the inhibitory effect of pergolide. These results demonstrate that pergolide inhibits sympathetic neurotransmission to the heart by a specific activation of presynaptic dopamine receptors.

Animals↗
PubMed1983

Comparative study of central dopaminergic properties of RU 29717 (N-propyl-9-oxaergoline) and pergolide.

RU 29717, a 9-oxaergoline derivative, has been compared with pergolide in a variety of biochemical and behavioural tests indicative of dopaminergic (DAergic) activity. RU 29717 and pergolide have a similar affinity for DA receptors labelled by [3H]spiroperidol or [3H]dihydroergocryptine ( [3H]DHEC) by using striatal or anterior pituitary membranes respectively. Both compounds stimulate the striatal DA-sensitive adenylate cyclase and inhibit the activity of this enzyme in dispersed cells from the neurointermediate lobe of the pituitary gland. In anterior pituitary cells in primary culture, they decrease prolactin release with the same efficacy. In vivo, they exert a long-lasting inhibition of the reserpine-induced hyperprolactinemia. They equally retard the alpha-MPT-induced disappearance of striatal DA and increase striatal acetylcholine levels. In behavioural models, the similarity between RU 29717 and pergolide is also evident: they induce contralateral circling in animals lesioned unilaterally with 6-OHDA, produce stereotyped behaviour and have emetic activity within the same dose range. Therefore, RU 29717, like pergolide, is a potent direct acting DAergic agonist. In experimental models used to investigate this activity at the striatal or the anterior pituitary levels the compounds present a similar profile of action.

Acetylcholine↗
PubMed1984

Central dopamine receptors mediating pergolide-induced elevation of serum corticosterone in rats. Characterization by the use of antagonists.

Fourteen dopamine antagonists were compared for their ability to antagonize the elevation of the concentration of serum corticosterone in rats by pergolide, a dopamine agonist. Clozapine did not antagonize the effect of pergolide at the largest dose (10 mg/kg) that could be tested without alteration of basal levels of corticosterone. For the other antagonists, calculation of ED50 values [dose antagonizing by 50% the elevation of corticosterone caused by a 0.3 mg/kg (i.p.) dose of pergolide mesylate] revealed the following order of potency: spiperone greater than loxapine greater than fluphenazine greater than perphenazine greater than flupentixol greater than haloperidol greater than cyclophenazine greater than zotepine greater than flumezapine greater than molindone greater than metoclopramide greater than chlorpromazine greater than sulpiride. All of these compounds caused increases in the concentration of the dopamine metabolites, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA), in the brains of rats. The dose that increased the concentration of DOPAC to 200% of the control value (ED200) was calculated for each compound. The ratio of the ED50 value for antagonism of the elevation of corticosterone induced by pergolide to the ED200 value for the elevation of DOPAC in brain varied, probably related to differing selectivity for pre- versus postsynaptic dopamine receptors between the compounds.(ABSTRACT TRUNCATED AT 250 WORDS)

3,4-Dihydroxyphenylacetic Acid↗
PubMedDate not supplied

Developmental toxicity of the dopamine agonist pergolide mesylate in CD-1 mice. II: Perinatal and postnatal exposure.

Pergolide mesylate is a dopamine agonist and, therefore, reduces prolactin secretion. In Experiment I, pregnant mice were given oral doses of 0, 0.1, 0.3, 1.0 or 3.0 mg/kg/day pergolide on GD 15 through PD 10 or 20 to identify a tolerated dose which would not markedly reduce offspring survival during late gestational and lactational exposure. Offspring survival was not affected at any dose, but dose-related decreases in progeny body weights occurred at weaning. On PD 10, suckling-induced increases in maternal serum prolactin concentrations did not occur in dams treated with 3.0 mg/kg/day. In Experiment II, pregnant mice were given oral doses of 0, 0.002, 0.1 or 3.0 mg/kg/day pergolide on GD 15 through PD 20. Dams were allowed to deliver and maintain their offspring throughout a 21-day lactation period. Growth and behavioral performance of one F1 male and one F1 female per litter were monitored, followed by a reproduction trial and terminal organ weight measurements. There were no treatment-related effects on maternal body weights, food consumption, or terminal organ weights and pathology. Three dams showed overt signs of mammary inflammation and lactational insufficiency and mean progeny survival was decreased slightly in the 3.0 mg/kg/day group. There were no adverse effects on growth, development or reproductive performance in the F1 treatment-derived generation. Neonatal negative geotaxis, 1-h activity levels at 30 and 60 days of age, auditory startle habituation at 55 days of age, and two-way active avoidance performance at 65 days of age were not affected significantly by treatment. Thus doses of pergolide that did not inhibit lactation completely in the F0 dams were found to have no enduring effects on offspring development.

Abnormalities, Drug-Induced↗
PubMed2005

High doses of pergolide improve clinical global impression in advanced Parkinson's disease:- a preliminary open label study.

We evaluated the efficacy and safety of high-dose pergolide treatment in patients with moderate to severe Parkinson's disease (PD) in an open-label multicenter clinical trial. The primary objective was to assess the amount of reduction in levodopa, the improvement in Unified Parkinson's Disease Rating Scale (UPDRS) and adverse reactions. We treated 32 patients with PD presenting with motor fluctuations. Pergolide treatment started with a dose escalation period of 12 weeks followed by a 12-week continuation period. Pergolide doses were increased up to a maximum of 12 mg/day in combination with a simultaneous decrease of levodopa doses in 100mg steps. Levodopa was reduced from 500 mg/day (median) to 250 mg/day. Mean UPDRS part III improved significantly (p=0.01). Clinical global impression improved significantly after 24 weeks (p<0.01). Most frequent adverse events were hallucinations, asthenia, anxiety, abdominal pain, and peripheral edema. Twenty-two patients finished the complete study according to protocol. A possible relationship to the study medication was assumed for two serious adverse events reporting psychosis. We conclude that high doses of pergolide are efficacious in advanced stages of PD if given in appropriate regimens.

Adult↗
PubMed2006

A functional magnetic resonance imaging study of the effects of pergolide, a dopamine receptor agonist, on component processes of working memory.

Working memory is an important cognitive process dependent on a network of prefrontal and posterior cortical regions. In this study we tested the effects of the mixed D1-D2 dopamine receptor agonist pergolide on component processes of human working memory using functional magnetic resonance imaging (fMRI). An event-related trial design allowed separation of the effects on encoding, maintenance, and retrieval processes. Subjects were tested with spatial and object memoranda to investigate modality-specific effects of dopaminergic stimulation. We also measured baseline working memory capacity as previous studies have shown that effects of dopamine agonists vary with working memory span. Pergolide improved reaction time for high-span subjects and impaired reaction time for low-span subjects. This span-dependent change in behavior was accompanied by span-dependent changes in delay-related activity in the premotor cortex. We also found evidence for modality-specific effects of pergolide only during the response period. Pergolide increased activity for spatial memoranda and decreased activity for object memoranda in task-related regions including the prefrontal and parietal cortices.

Adult↗
PubMed2000

Effects of sub-chronic combined treatment with pergolide and caffeine on contralateral rotational behavior in unilateral 6-hydroxydopamine-denervated rats.

We studied the synergistic effects of pergolide and bromocriptine with caffeine on turning behavior in 6-OHDA denervated rats. Both pergolide and bromocriptine were synergistic with caffeine, and prevented tolerance to caffeine-induced turning. When caffeine was removed, tolerance to bromocriptine effects was observed for 1 day only, while no tolerance was observed to pergolide. These results suggest that caffeine could be useful in the treatment of Parkinson's disease, preferentially as an adjuvant of mixed dopaminergic agonists like pergolide.

Animals↗
PubMed1987

Effect of topical pergolide on aqueous dynamics in normal and glaucomatous monkeys.

The effects of pergolide mesylate, an ergoline derivative, were studied on intraocular pressure (IOP), outflow facility, aqueous humor flow, and pupil size in monkeys. Unilateral topical administration of two 20-microliters drops of 0.1% pergolide significantly lowered IOP in the treated- and contralateral eye in both normal- and glaucomatous monkeys. In 12 normal monkeys, the baseline IOP of 18.3 +/- 0.4 mmHg [mean +/- S.E.(M.)] was maximally reduced to 14.4 +/- 0.7 mmHg in the treated eye (P less than 0.001) and 14.6 +/- 0.6 mmHg in the contralateral eye (P less than 0.001) at 2 hr after drug administration. In 10 monkeys made bilaterally glaucomatous by argon laser treatment of the trabecular meshwork, the baseline IOP of 33.9 +/- 3.0 mmHg [mean +/- S.E.(M.)] in the treated eyes and 31.7 +/- 3.3 mmHg in the untreated eyes maximally decreased to 23.9 +/- 2.2 mmHg (P less than 0.05) and 26.2 +/- 3.3 mmHg (P less than 0.005), respectively, at 5 hr. No significant change (P greater than 0.7) in outflow facility occurred in either eye of 11 normal monkeys 2 hr after unilateral 0.1% pergolide treatment. In six normal monkeys, the baseline aqueous humor flow of 1.58 +/- 0.20 microliter min-1 in treated eyes and 1.44 +/- 0.18 microliter min-1 in untreated eyes was reduced to 0.92 +/- 0.08 microliter min-1 (P less than 0.02) and 1.09 +/- 0.11 microliter min-1 (P greater than 0.10), respectively, from 0.5- to 3.5 hr after drug administration. A mydriatic response was observed in both eyes after unilateral treatment from 1- to 2 hr in eight normal monkeys. By the third day of treatment, bilateral twice a day 0.1% pergolide drops in eight glaucomatous monkey eyes no longer significantly (P greater than 0.05) decreased IOP.

Administration, Topical↗
PubMed2000

Open pergolide treatment of tricyclic and heterocyclic antidepressant-resistant depression.

BACKGROUND: Recently, a dopamine hypothesis of depression was put forward, and several studies have demonstrated that direct and indirect dopamine agonists have antidepressant effects. METHODS: Using Clinical Global Impressions, we evaluated the efficacy of 4-week treatment of pergolide as an antidepressant adjuvant involving 20 unipolar depressed patients who were refractory to standard treatment with antidepressants. RESULTS: One patients (5%) were very much improved, seven (35%) much improved, four (20%) minimally improved, six (30%) no change or worse, and two (10%) not assessed. There was no significant difference in any clinical factors between the pergolide responder and non-responder group. LIMITATIONS: This study was a non-blind open trial, and pergolide was added to tricyclic and heterocyclic antidepressants. CONCLUSION: Pergolide may be useful as an antidepressant adjuvant, suggesting a potential role for dopamine-2 stimulation in the antidepressant response.

Adult↗
PubMed2006

Cardiac valvulopathy associated with pergolide use.

OBJECTIVE: To review the risk of pergolide associated cardiac valvulopathy in patients with Parkinson's disease. DATA SOURCES: MEDLINE, Embase, and the Cochrane Library. Reference lists were reviewed and librarians were consulted to identify additional trials. STUDY SELECTION: All studies and case reports in the English literature on pergolide and cardiac valvulopathy. DATA EXTRACTION: Demographics of patients, study duration, dose and duration of pergolide use, echocardiogram results, length of follow-up, and clinical outcome. RESULTS: Twenty-two published articles were identified. There were no randomized controlled trials. Follow-up time varied between a few months and four years. Three case reports and four studies (three case control and one observational) assessed 246 patients. Evidence for valvulopathy was found in all studies. Variable methods were used to assess the degree of valvular regurgitation making comparisons between studies difficult. Little clinical correlation is available for echocardiogram results. Variable improvement was shown in the few patients in whom the drug was stopped. There is insufficient data to determine whether dose and duration or other comorbities have an effect on the risk of developing cardiac valvulopathy. CONCLUSION: Pergolide therapy is associated with an increased risk of developing cardiac valvulopathy but the true incidence and importance of this remains unknown. Further prospective studies are needed with standardized assessments of echocardiograms.

Antiparkinson Agents↗
PubMed1997

Pergolide to augment the effectiveness of antidepressants: clinical experience and a small double-blind study.

To attempt to confirm a prior report that pergolide can augment the efficacy of antidepressants in refractory patients, pergolide was administered to 12 patients receiving antidepressants. Eight patients were involved in a placebo-controlled evaluation of pergolide; the others were prescribed pergolide clinically. Results showed no evidence of benefit, so the double-blind study has been discontinued.

Adjuvants, Pharmaceutic↗
PubMed2003

The pharmacokinetics of pergolide in Parkinson's disease.

Three decades of research have led to a fuller understanding of the pharmacokinetics of pergolide. Pergolide is rapidly absorbed following oral dosing, reaching peak plasma concentrations within 2-3 h. It is about 90% protein bound yet has negligible drug interactions. Pergolide undergoes extensive first-pass metabolism and is completely eliminated within 4-5 days. The metabolism/elimination profile varies between patients but is consistent within the individual, highlighting the importance of careful titration to an effective dose. Pergolide has a long half-life of about 21 h; this has interesting implications, as it should produce a more physiological or continuous stimulation of dopamine receptors, avoiding or delaying the induction of dyskinesia.

Animals↗
PubMed2003

Appropriate dosing of pergolide in monotherapy and adjunctive therapy in Parkinson's disease.

Pergolide is one of the most well-tested and widely used dopamine agonists for the treatment of Parkinson's disease; however, there is worrying evidence that sub-therapeutic dosing of pergolide is widespread in clinical practice. Clinical studies in Caucasians suggest that a pergolide dose of 3 mg/day provides the optimal efficacy to tolerability ratio and that, in Japanese patients, a dose in excess of 2.25 mg/day may be ideal. Whether pergolide is used early in patients with de-novo Parkinson's disease or as adjunctive therapy later in the disease, in order to optimize its clinical efficacy, it is recommended that practitioners aim to achieve at least these doses, or higher ones, if the drug is well tolerated.

Antiparkinson Agents↗