Bromocriptine and Levodopa (With or Without Carbidopa) in Parkinsonism

Kartzinel, Ronald; Teychenne, Paul F.; Gillespie, Marjorie; Perlow, Mark J.; Gielen, Andrea Carlson; Sadowsky, Doris A.; Calne, Donald B.

doi:10.1016/s0140-6736(76)90728-5

Cited by 88 publications

(25 citation statements)

References 13 publications

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“…However, the therapeutic efficacy of bromocriptine in a maximum dose of 30 mg daily was less than that of levodopa (800 mglday) in combination with benserazide (200 mg/day). A similar finding has been reported by Gerlach [lo], but Kartzinel et a1 [13] and Lieberman et a1 [14] have found bromocriptine to be superior to levodopa alone ,or combined with carbidopa. One reason for this discrepancy in results may be the difference in dosage of bromocriptine, because in Gerlach's study and in ours, a lower daily dose of bromocriptine was used than in Kartzinel's and Lieberman's series.…”

Section: Discussionsupporting

confidence: 78%

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Brain dopamine receptor stimulation and the relief of parkinsonism: Relationship between bromocriptine and levodopa

Rinne

Marttila

1978

Annals of Neurology

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The relationship between dopamine receptor stimulation by bromocriptine or levodopa and the relief of parkinsonism was studied in 24 patients with Parkinson disease. Bromocriptine, 30 mg daily for 20 weeks, elicited an improvement in the parkinsonian clinical features, but this was less than the subsequent improvement with levodopa and benserazide, 800 mg and 200 mg daily, respectively. There was a negative correlation between the pretreatment severity of the disease or changes in cerebrospinal fluid homovanillic acid (HVA) and improvement in parkinsonian disability during bromocriptine treatment. Futhermore, it was found that clinical improvement and HVA responses in the cerebrospinal fluid after dopamine receptor stimulation by bromocriptine may predict the clinical response to levodopa.

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Section: Discussionsupporting

confidence: 78%

“…Recent evidence indicates that drugs stimulating brain dopamine receptors directly could be beneficial in the treatment of patients with Parkinson disease [4,6,13,191. Among these agents, bromocriptine has been proved to be superior to levodopa [ 13, 141, although contrary results have also been described [lo, 161.…”

mentioning

confidence: 99%

Brain dopamine receptor stimulation and the relief of parkinsonism: Relationship between bromocriptine and levodopa

Rinne

Marttila

1978

Annals of Neurology

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“…Several studies have demonstrated the capacity of bromocriptine, used as an adjunct to levodopa, to improve parkinsonian disability and reduce dyskinesia and motor fluctuations in patients with advanced PD. [317][318][319] Pergolide is also an ergot agent with D2 receptor agonist properties but differs from bromocriptine in that it is a weak agonist at the D1 receptor. A large, prospective, multicenter, double-blind, placebo-controlled trial in levodopa-treated patients demonstrated that the addition of pergolide improved motor and ADL scores, decreased "off " time, and provided a levodopa-sparing effect.…”

Section: No Dyskinesias Up To 6 Monthsmentioning

confidence: 99%

The scientific and clinical basis for the treatment of Parkinson disease (2009)

Olanow¹,

Stern²,

Sethi³

2009

Neurology

759

658

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Parkinson disease (PD) is an age-related neurodegenerative disorder that affects as many as 1-2% of persons aged 60 years and older. With the aging of the population, the frequency of PD is expected to increase dramatically in the coming decades. Current therapy is largely based on a dopamine replacement strategy, primarily using the dopamine precursor levodopa. However, chronic treatment is associated with the development of motor complications, and the disease is inexorably progressive. Further, advancing disease is associated with the emergence of features such as freezing, falling, and dementia which are not adequately controlled with dopaminergic therapies. Indeed, it is now appreciated that these nondopaminergic features are common and the major source of disability for patients with advanced disease. Many different therapeutic agents and treatment strategies have been evaluated over the past several years to try and address these unmet medical needs, and many promising approaches are currently being tested in the laboratory and in the clinic. As a result, there are now many new therapies and strategic approaches available for the treatment of the different stages of PD, with which the treating physician must be familiar in order to provide patients with optimal care. This monograph provides an overview of the management of PD patients, with an emphasis on pathophysiology, and the results of recent clinical trials. It is intended to provide physicians with an understanding of the different treatment options that are available for managing the different stages of the disease and the scientific rationale of the different approaches. 1 PD is the second most common neurodegenerative disorder, with an average age at onset of about 60 years. An estimated 5 million people throughout the world have PD, with 1 million individuals each in the United States and in Europe with the disorder. PD affects approximately 0.3% of the population and 1% to 2% of those older than 60 years.2 With the aging of the population and the substantial increase in the number of at-risk individuals older than 60 years, it is anticipated that the prevalence of PD will increase dramatically in the coming decades.

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“…The potency of pergolide was compared with that of bromocriptine (2-bromo-a-ergocriptine), another ergot derivative currently used in the treatment of parkinsonism (7,8). The long duration of action of pergolide as an agonist (9, 10) prompted us to investigate its therapeutic effectiveness in parkinsonism patients.…”

mentioning

confidence: 99%

Interaction of pergolide with central dopaminergic receptors.

Goldstein¹,

Lieberman²,

Lew³

et al. 1980

Proc. Natl. Acad. Sci. U.S.A.

100

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The activity of pergolide, an N-propylergoline derivative, has been tested for stimulation of central dopaminergic receptors. Binding to dopamine receptors shows that pergolide acts as an agonist with respect to these receptors. GTP decreases the potencies of dopamine agonists and of pergolide, It is now established that the major abnormality in parkinsonism is the degeneration of the nigrostriatal 3,4-dihydroxyphenylethylamine (dopamine) neurons. The effectiveness of 3,4-dihydroxyphenylalanine (L-dopa) in parklnsonism is dependent on the capacity of the remaining nigrostriatal dopamine neurons to synthesize dopamine from administered L-dopa. It has become apparent that therapeutic response diminishes after prolonged treatment with L-dopa (1, 2). This decrease might be due to progressive degeneration of the nigrostriatal dopamine neurons or to a decreased sensitivity of dopamine receptors in the striatum. It was therefore of interest to investigate the effectiveness of drugs that directly stimulate dopamine receptors in the brain. Among various dopamine agonists tested, certain ergot alkaloids were found to stimulate dopamine receptors (3, 4), and their therapeutic effectiveness in parkinsonism was investigated (5, 6).We now describe dopamine agonist properties of a semisynthetic ergoline derivative, pergolide (8fl-[8-(methylthio)-methyl]-6-propylergoline), tested both in vitro and in two animal models that simulate certain features of parkinsonism. The potency of pergolide was compared with that of bromocriptine (2-bromo-a-ergocriptine), another ergot derivative currently used in the treatment of parkinsonism (7,8). The long duration of action of pergolide as an agonist (9, 10) prompted us to investigate its therapeutic effectiveness in parkinsonism patients. Preliminary reports on this study have been presented (9,11,12). MATERIALS AND METHODSNPA) (75 Ci/nmol) were purchased from New England Nuclear (1 Ci = 3.7 X 1010 becquerels). Pergolide was a gift from Eli Lilly, and bromocriptine from Sandoz Pharmaceutical.Binding Assay. Preparation of bovine or rat membranes and the ensuing binding assay were carried out as described (13). For routine assay each tube contained 1.8 ml. of membrane suspension (5 mg of wet tissue), 0. Values for the mean inhibitory concentration, ICso, were derived by log probit analysis. Values for the dissociation constant, Kd, for each radioactive ligand were determined from the corresponding Scatchard plots, and values for the inhibitor constant, Ki, were determined according to the equation Ki =

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Bromocriptine and Levodopa (With or Without Carbidopa) in Parkinsonism

Cited by 88 publications

References 13 publications

Brain dopamine receptor stimulation and the relief of parkinsonism: Relationship between bromocriptine and levodopa

Brain dopamine receptor stimulation and the relief of parkinsonism: Relationship between bromocriptine and levodopa

The scientific and clinical basis for the treatment of Parkinson disease (2009)

Interaction of pergolide with central dopaminergic receptors.

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