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Transcranial magnetic stimulation was used to probe the acute effect of a single oral dose of various dopaminergic (levodopa, selegiline, bromocriptine) and antidopaminergic drugs (sulpiride, haloperidol) on motor cortex excitability in healthy volunteers. Motor threshold, intracortical inhibition and intracortical facilitation were tested in the abductor digiti minimi muscle. The latter two parameters were studied in a conditioning-test paired stimulus paradigm. The principal findings were an increase in intracortical inhibition by bromocriptine, and, conversely, a decrease in intracortical inhibition and an increase in intracortical facilitation by haloperidol. Effects peaked at delays consistent with the pharmacokinetics of the two drugs and were fully reversible. In conclusion, dopamine receptor agonists and antagonists can be considered inverse modulators of motor cortex excitability: the former enhance inhibition while the latter reduce it. The relation of the present findings to current models of motor excitability abnormalities in movement disorders will be discussed.
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After previous demonstration of paradoxical GH responses to TRH and oral glucose loading tests in some constitutionally tall adolescents, we studied the effects of a small dose of bromocriptine (5 mg/day) on GH secretion and adult height prediction. In 10 patients, each of whom had a substantial plasma GH increase after TRH injection, bromocriptine reduced or suppressed this abnormal response. In 4 of these patients who also had paradoxical GH increases after glucose loading, bromocriptine suppressed this abnormality in 2. Predicted adult height was reduced in 10 of the 12 patients after 6-12 months of treatment. This reduction resulted either from a decrease in growth velocity, an increase in skeletal maturation rate, or both. Since no side effects were noticed we suggest that bromocriptine may be a valuable alternative to sex steroid treatment to limit final height in excessively tall adolescents.
Acromegaly is very often accompanied by impaired glucose tolerance or a manifest diabetes mellitus, with increased immunoreactive insulin (IRI) levels whose response during oral glucose tolerance tests (OGTT) is quite often exaggerated. When the dopaminergic drug bromocriptine is administered to acromegalics, their elevated growth hormone (GH) levels very often decrease, their impaired glucose tolerance (as manifested in OGTT) improves and their exaggerated IRI response becomes more normal. Eighteen patients were treated with bromocriptine. They were followed-up repeatedly during their treatment of varying duration for up to 6 years. These results indicate that raised GH levels are not the only factor that impairs glucose tolerance in acromegalics. During bromocriptine administration, impaired glucose tolerance improved and abnormal IRI levels (OGTT) became more normal even without any decrease in the high GH levels. In non-diabetic acromegalics, when bromocriptine was administered, there was not only an average decrease in the elevated GH values during OGTT, but a normalization of increased IRI values as well, without any major change in the corresponding blood glucose levels. During insulin tolerance tests (ITT), after i.v. insulin, the IRI levels after 30 and 60 min were markedly higher in acromegalics on bromocriptine than in the same patients before its administration, without any significant change in the corresponding blood glucose values. In 2 diabetic acromegalics, bromocriptine administration re-established their lost ability to increase IRI levels during OGTT. This was accompanied by a marked improvement in their glucose tolerance. It is probable that bromocriptine decreases glucagon levels in acromegalics, or at least in some of them. It is suggested that bromocriptine could protect the beta-cells of acromegalics from "exhaustion'.
Drugs able to mimic or to antagonize the action of catecholamines have been implanted bilaterally into the basomedial region of the amygdala of adult castrated female rats. The animals were killed at different intervals after the implantation of the different drugs, and serum levels of LH and FSH were measured by radioimmunoassay. The results have shown that the intra-amygdalar implantation of the alpha-adrenergic blocker phenoxybenzamine induces a significant increase of the release both of LH and FSH. The implantation of the beta-adrenergic blocker propranolol brings about a rise of LH only. The dopamine receptor blocker pimozide stimulates the release of LH and exerts a biphasic effect (stimulation followed by inhibition) of FSH secretion. The alpha-receptor stimulant clonidine and the dopaminergic drug 2-Br-alpha-ergocryptine were without significant effects. From these observations it is suggested that the adrenergic signals reaching the basomedial area of the amygdala (possibly from the brain stem) may be involved in the modulation of gonadotrophin secretion.
A patient with a macroprolactinoma was treated with bromocriptine 15 mg daily. Both the size of the tumour as shown by computed tomography and the serum prolactin concentration decreased over several months but then increased. The dose of bromocriptine was increased to 40 mg daily but tumour growth continued, and the tumour was resected. Production of prolactin by cultured cells was not inhibited by high concentrations of bromocriptine, suggesting that regrowth of the tumour was due to cells resistant to dopamine agonist action. This case of regrowth of a prolactinoma during bromocriptine treatment after an initial reduction in size indicates the need for close surveillance especially of patients whose serum prolactin concentration fails to fall into the normal range with bromocriptine treatment.
Bromocriptine, a long acting dopamine agonist, has been used to treat 73 patients with active acromegaly for between 3 and 25 months. Clear clinical improvement occurred in 71 patients (97%). This included improvement in facial appearance, reduction in hand and foot size and sweating, relief of headaches and increased energy and libido. Abnormal visual fields became normal in two patients, but one of these was given concomitant radiotherapy. A significant reduction in growth hormone occurred in 58 patients (79%), but only 15 patients had levels persistently below 5microgram/l. Carbohydrate tolerance improved with the reduction in growth hormone and of 23 patients with diabetes mellitus before treatment, glucose tolerance became normal in 15 and improved in a further 5. Administration of bromocriptine should begin slowly in order to minimise early side effects. Long term side effects have been minor to date and the deaths of two patients whilst taking the drug were not considered to have been caused by it. Bromocriptine offers a major advance in the management of acromegaly, but further careful follow-up is required to determine whether serious side effects will be a problem with the long term use of high doses.
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These findings indicate that oral bromocriptine administration could represent a new therapy to reduce intraocular pressure in humans.
To investigate the mechanism of reversing multidrug resistance of hepatocarcinoma by bromocriptine (BCT) in vitro and in vivo.
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We aimed to explore the pattern of DA AE reporting over two decades.
This study was conducted to determine whether the acute administration of bromocriptine, a dopamine agonist, modulates the acute pharmacologic effects of i.v. cocaine in humans. Eight current users of i.v. cocaine who were not seeking treatment for their cocaine abuse completed the study while they were inpatients on a research unit. Twelve drug conditions were tested in all subjects in randomized order under double-blind, double-dummy conditions and included cocaine (0, 12.5, 25 and 50 mg, i.v.) in combination with bromocriptine (0, 1.2 and 2.5 mg given orally 2 hr before the cocaine injection). Physiologic and subject- and observer-rated responses were measured. Cocaine alone significantly increased pupil diameter, heart rate and blood pressure, and ratings of drug effect, good effects, liking and rush. Bromocriptine alone significantly increased pupil diameter and heart rate, decreased blood pressure and had only minor effects on subjective measures. There were significant cocaine/bromocriptine interactions on diastolic and mean arterial blood pressure, with combinations producing significantly smaller increases compared to cocaine alone, and on heart rate, with combinations producing significantly larger increases compared to cocaine alone. The physiologic and subjective effects of cocaine were not modified by pretreatment with bromocriptine in any other way that might indicate either a therapeutic benefit or a safety concern. However, bromocriptine alone produced undesirable effects (fainting) that should be considered before administration to outpatient cocaine abusers. Any possible therapeutic benefits of acute administration of bromocriptine in cocaine abuse are not likely to be due directly to modulation of the acute effects of cocaine.
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PRL enhanced RA synovial cell proliferation. Production of proinflammatory cytokine and MMP was augmented and production of tissue inhibitor of metalloproteinases (TIMP)-1 was inhibited by PRL treatment of RA synovial cells, suggesting that PRL enhances total collagenase activity in the joints. PRLR was exclusively expressed on fibroblast-like synovial cells and lymphocytes infiltrating into the synovium in patients with RA. Both synovium infiltrating T lymphocytes and, to a lesser extent, fibroblast-like synovial cells synthesized PRL, suggesting that PRL acts as a paracrine as well as autocrine activator of RA synovial cell functions. Stimulation of synovial cells by PRL induced rapid translocation of STAT-5 from cytoplasm into nuclei of RA synovial cells, suggesting that transcriptional regulation of RA synovial cell functions by PRL affects STAT-5. Inhibitors of PRL release, such as bromocriptine, inhibited proliferation of proinflammatory cytokines and collagenases by RA synovial cells.
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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.
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We investigated the frequency of headaches in women with menstrual abnormalities and hyperprolactinemia. Twenty-seven of 46 (58%) women with hyperprolactinemia indicated that headache episodes occur once or more per week; patients with sellar abnormalities (macroadenoma) or previous cranial or pituitary operation were excluded from this group of hyperprolactinemic patients. The headache episodes occurred significantly more frequently than in the control group (N = 56), where 27% indicated one or more headaches per week (p less than 0.01). In the vast majority of the women with hyperprolactinemia, headaches had preceded the finding of elevated prolactin levels for years and had not developed after the patients had become concerned about the pituitary gland. The clinical impression was that the headaches of these patients typically lack features of prodromal signs and unilaterality and resemble, in general, tension headaches; they may last for hours and often require medication. We could not demonstrate a relationship between prolactin levels and frequency or severity of these headache episodes. The etiology of these headaches is unclear. The therapeutic effect of bromocriptine deserves further investigation. In conclusion, we present data to suggest that headaches are commonly an associated finding in hyperprolactinemic women who have no evidence of significant pituitary enlargement.
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Akinetic mutism (AM) is a behavioral disorder characterized by impossibility to move or speak in awake patients. lt has been typically described as a transient disorder following posterior fossa tumour resection. Besides, AM may also appear after recurrent shunt failures in hydrocephalic patients, with no tendency towards improvement, either spontaneously or with shunt revisions. However successful treatment of this second type of AM has been achieved with bromocriptine. We present a patient who developed AM after a posterior fossa surgery complicated by ventriculitis and multiple hydrocephalic events. AM only improved with bromocriptine. We review AM pathophysiology. Although not well known, it appears to be quite different, depending on its cerebellar or hydrocephalic origin. Damage to dentate nucleus or its efferents (mainly of glutamate) should promote AM of cerebellar origin, while damage to paraventricular monoaminergic pathways could explain AM related to repeated shunt failures which has successful response to bromocriptine treatment. However, a more complete study of this disorder is required to ascertain its aetiology.
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Inbred male WF rats were castrated at 40 days of age and divided into 5 groups. Group I was given no further treatment. Groups III, IV, and V received pellet implants of 5.0 mg diethylstilbestrol (DES) concurrently with castration. At 50-55 days of age, groups II, IV, and V were given drinking water containing 5.0 mg N-nitrosobutylurea (NBU) per day for 30 days (subthreshold dose). At the termination of NBU treatment, group V further received daily sc injections of 2-bromoergocryptine (CB-154; 0.4 mg/100 g body wt) four times a week throughout the experiment. None of castrated rats or rats castrated and treated with NBU alone developed hepatic tumors (HT) and pituitary tumors (PT). Incidences of HT and PT in groups III, IV, and V were 4/9 (44%) and 7/9 (78%), 15/17 (88%) and 12/17 (71%), and 17/20 (85%) and 4/20 (20%), respectively. The treatment of DES alone resulted in the concurrent development of HT and PT in castrated male rats (group III), and further NBU treatment significantly increased the incidence of HT (group IV). CB-154 treatment did not change the incidence of HT, the number of HT per rat, and the liver weight, although it significantly reduced the incidence of PT, the pituitary weight, and the serum prolactin level in castrated male rats given DES and NBU (group V). These results indicate that DES itself had a direct carcinogenic effect on the liver; this effect was not mediated by prolactin, and NBU increased the effect of DES in this process.
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Reported herein is the possible interaction between two drugs used to treat a man with a large prolactin-secreting pituitary adenoma. The patient had a long history of schizophrenia that was treated with many different medications, including phenothiazines. Evaluation of progressive lethargy led to the discovery of a large parasellar tumor and a prolactin level of 7,981 ng/ml. His serum prolactin level fell to the 400 ng/ml range during bromocriptine therapy but rose whenever the antipsychotic thioridazine was added to his regimen. A marked deterioration of his visual fields was noted after 3 months' therapy with both drugs, and this abnormality resolved five days after the thioridazine was stopped. The use of dopamine antagonists such as thioridazine in patients with prolactinoma may interfere with bromocriptine's action, resulting in potentially serious complications.
The risk for developing visual loss during single or multiple pregnancies in patients with microadenomas was small. Six of eight pregnant women with macroadenomas, however, developed visual field loss during pregnancy.
To explore the basis of apparent conformational heterogeneity of cytochrome P450 3A4 (CYP3A4), the kinetics of dithionite-dependent reduction was studied in solution, in proteoliposomes, and in Nanodiscs. In CYP3A4 oligomers in solution the kinetics obeys a three-exponential equation with similar amplitudes of each of the phases. Addition of substrate (bromocriptine) displaces the phase distribution toward the slow phase at the expense of the fast one, while the middle phase remains unaffected. The fraction reduced in the fast phase, either with or without substrate, is represented by the low-spin heme protein only, while the slow-reducible fraction is enriched in the high-spin CYP3A4. Upon monomerization by 0.15% Emulgen-913, or by incorporation into Nanodiscs or into large proteoliposomes with a high lipid-to-protein (L/P) ratio (726:1 mol/mol), the kinetics observed in the absence of substrate becomes very rapid and virtually monoexponential. In Nanodiscs and in lipid-rich liposomes bromocriptine decreases the rate of reduction via appearance of the second (slow) phase, the amplitude of which reaches 100% at saturating bromocriptine. In contrast, in P450-rich liposomes (L/P = 112 mol/mol), where the surface molar density of the enzyme is comparable to that observed in liver microsomes, CYP3A4 behaves similarly to that observed in solution. These results suggest that in CYP3A4 oligomers in solution and in the membrane the enzyme is distributed between two persistent conformers with different accessibility of the heme for the reductant (SO*-(2) anion monomer). One of the apparent conformers exists in a substrate-dependent equilibrium between two states with different rate constants of reduction by dithionite, while the second conformer shows no response to substrate binding.
A 34-year-old woman presented with secondary infertility and hyperprolactinemia.
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Type 2 diabetes mellitus (DM) is a chronic metabolic disorder in which prevalence has been increasing steadily all over the world. As a result of this trend, it is fast becoming an epidemic in some countries of the world with the number of people affected expected to double in the next decade due to increase in ageing population, thereby adding to the already existing burden for healthcare providers, especially in poorly developed countries. This review is based on a search of Medline, the Cochrane Database of Systemic Reviews, and citation lists of relevant publications. Subject heading and key words used include type 2 diabetes mellitus, prevalence, current diagnosis, and current treatment. Only articles in English were included. Screening and diagnosis is still based on World Health Organization (WHO) and American Diabetes Association (ADA) criteria which include both clinical and laboratory parameters. No cure has yet been found for the disease; however, treatment modalities include lifestyle modifications, treatment of obesity, oral hypoglycemic agents, and insulin sensitizers like metformin, a biguanide that reduces insulin resistance, is still the recommended first line medication especially for obese patients. Other effective medications include non-sulfonylurea secretagogues, thiazolidinediones, alpha glucosidase inhibitors, and insulin. Recent research into the pathophysiology of type 2 DM has led to the introduction of new medications like glucagon-like peptide 1 analogoues: dipeptidyl peptidase-IV inhibitors, inhibitors of the sodium-glucose cotransporter 2 and 11ß-hydroxysteroid dehydrogenase 1, insulin-releasing glucokinase activators and pancreatic-G-protein-coupled fatty-acid-receptor agonists, glucagon-receptor antagonists, metabolic inhibitors of hepatic glucose output and quick-release bromocriptine. Inhaled insulin was licensed for use in 2006 but has been withdrawn from the market because of low patronage.
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Based on previous reports that bromocriptine, a postsynaptic dopamine agonist, reduced cocaine craving and prevented relapse in cocaine-dependent subjects, effects of the drug were evaluated in 20 cocaine-dependent males in an inpatient drug rehabilitation programme. The subjective and physiologic effects of exposure to both cocaine-associated and neutral stimuli, presented using videotapes, were measured at one-week intervals. Between laboratory sessions subjects received either bromocriptine (1.25 mg bid) or a matched placebo, administered in double-blind fashion. Compared with the neutral videotape, the cocaine videotape elicited both a greater desire to use cocaine and more symptoms associated with cocaine self-administration. These results support an appetitive conditioning model of cocaine effects. Bromocriptine, however, had no effect on the cocaine-cue-associated reactivity, which declined over the 1-week interval in both treatment groups. Methodological differences among studies that have examined the effects of bromocriptine in cocaine-dependent subjects may explain the variable findings observed.
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A preliminary randomized comparative study.
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Seven patients affected by Huntington's chorea were given an acute administration of 2-Br-alpha-ergocryptine (CB 154, Sandoz), a direct agonist at dopamine receptor sites. Seven nonobese hospitalized patients were used as controls. Oral administration of CB 154 (2.5 mg) induced a more prompt and consistent rise in plasma growth hormone (GH) levels in patients than in controls. GH levels rose from baseline values of 0.3+/-0.1 ng/ml to mean peak values of 20.4+/-5.1 ng/ml (120-270 min) in choreic subjects and from baseline values of 1.0+/-0.4 ng/ml to mean peak values of 5.7+/-1.6 ng/ml (180-300 min) in control subjects (P less than 0.02). Baseline plasma prolactin (PRL) values were significantly higher in choreic than in control subjects (22.1+/-6.6 ng/ml vs. 8.1+/-1.4 ng/ml, respectively, P less than 0.02); administration of CB 154 induced a more consistent PRL decrease in control than in choreic subjects. Collectively, these results suggest the existence of an abnormal regulation of GH and PRL secretion in Huntington's chorea, probably due to alterations in central dopaminergic neurotransmission.
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The present literature concerning sexual dysfunction in Parkinson's disease and dopaminergic therapy is discussed. Doctors who treat these patients should be aware of the problem of hypersexuality associated with dopaminergic therapy.