Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Bromocriptine”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 379 records · Page 21Linked to original sources

Regulation of body temperature in postmenopausal women: interactions between bromocriptine and the endogenous opioid system.

The role exerted by the endogenous opioid system on thermoregulation has been studied in nine postmenopausal women before and after the chronic administration of the dopamine agonist bromocriptine (5 mg/day). These women randomly received an infusion of the opioid antagonist naloxone (1.6 mg/h for 4 h) or saline on two consecutive days, before and after 30 days of bromocriptine administration. Body temperature as evaluated by rectal temperature, did not vary during saline infusion performed both before and after 30 days of bromocriptine administration. In untreated women naloxone infusion significantly reduced body core temperature. The hypothermic response to naloxone was significantly greater following chronic bromocriptine administration. These results indicate that bromocriptine seems to increase the activity of the endogenous opioid system on the mechanisms which regulate body temperature in postmenopausal women.

Body Temperature Regulation↗

Bromocriptine treatment of acromegaly.

Bromocriptine at a dose of 7.5-30 mg/day was given to 12 acromegalics for 6 mo. Mean serum growth hormone (GH) levels during a glucose tolerance test (GTT) were significantly lowered by the drug. In four patients the serum GH response during a GTT was suppressed to normal (i.e. less than or equal to 5 mlU/liter). If bromocriptine had not brought the serum GH response to a GTT to normal at a dose of 20 mg/day, this effect was not achieved by raising the dose to 30 mg/day. Bromocriptine was effective for the duration of treatment. On discontinuing therapy there was an increase in serum GH levels. No obvious clinical changes in the acromegalic features were noted. One patient with impaired glucose tolerance and one with established diabetes had normal glucose tolerance while on bromocriptine and another two patients with impaired glucose tolerance showed no obvious changes while on the drug. Side effects were minor. X-rays of the pituitary fossa before starting and at the end of treatment showed no significant change. We conclude that although bromocriptine is the most promising form of medical treatment for acromegaly to date, it is fully effective only in a minority of patients.

Acromegaly↗

Failure of bromocriptine to alter the qualitative characteristics of human growth hormone in acromegaly.

The role of bromocriptine as a therapeutic agent for acromegaly is uncertain. In the present study we have attempted to determine whether bromocriptine therapy causes qualitative changes in plasma human growth hormone (hGH) in acromegaly. When eight paired samples obtained before and during bromocriptine therapy were filtered over Sephadex G-100 there was no difference in the elution profiles. When the "little" hGH peak from each of the eight paired samples was pooled, lyophilized, and assayed in both radioreceptor assay (RRA) and radioimmunoassay (RIA), the RRA/RIA before treatment was not different than during treatment. When bromocriptine in pharmacologically significant concentrations was incubated with cultured human lymphocytes in vitro, there was no alteration in hGH binding properties. These results demonstrate directly that bromocriptine does not change the form or receptor-reactive properties of plasma hGH and, further, that the drug does not alter at least one form of human growth-hormone receptor.

Acromegaly↗

CV 205-502, a new dopamine agonist, versus bromocriptine in the treatment of hyperprolactinaemia.

Forty-seven hyperprolactinaemic patients with serum prolactin (PRL) concentrations persistently above 1500 mU/l were treated with the new dopamine agonist CV 205-502 or bromocriptine in a prospective, randomized and double-blind fashion during a 24-week period. Two women had to be excluded because of poor compliance in the first month. Therefore 45 patients remained for evaluation. 81% of the patients in the CV 205-502 group and 70% of the patients in the bromocriptine group normalized their prolactin levels within the study period with a treatment dose as permitted in this protocol. In general serum prolactin normalized within 8 to 12 weeks of treatment. There were no differences between the two tested drugs regarding restoration of the menstrual cycle or disappearance of galactorrhoea. Both drugs gave rise to adverse reactions, especially during the initiation of therapy. However, the adverse reactions reported during CV 205-502 treatment were less severe and persistent than those attributed to bromocriptine. Patient acceptance of the new drug with regard to tolerability was judged by 90% of the women in that treatment group as very good or good, while 75% of those treated with bromocriptine evaluated its tolerability as very good or good. We conclude that CV 205-502 is highly effective in the treatment of hyperprolactinaemia with concomitant restoration of gonadal function and prevention of galactorrhoea. The tolerability of the drug seems better than of bromocriptine and therefore this drug is of value in the treatment of hyperprolactinaemic patients.

Adolescent↗

Effects of bromocriptine pretreatment on subjective and physiological responses to i.v. cocaine.

We studied the effect of pretreatment with single doses of bromocriptine on the pattern of subjective and physiologic responses to single doses of intravenous (IV) cocaine. Placebo, bromocriptine 2.5 mg and, in five subjects only, 5 mg were administered orally 120 minutes before a dose of placebo or cocaine 40 mg IV to 9 male cocaine-using volunteers. Bromocriptine pretreatment diminished blood pressure generally, including cocaine-induced blood pressure increases, and augmented the heart rate after cocaine. It caused virtually no change in either augmentation or diminution of subjective responses including "rush" and "good feeling" scores, and scores for the MBG of the Addiction Research Center Inventory (ARCI), all measures of euphoria. However, a trend for the scores for the item "Would a dose of drug (cocaine) make you feel better?," suggested that bromocriptine may decrease the urge to use cocaine that was evoked by cocaine itself. However, this decreased desire was associated with a trend toward an increase in dysphoria as measured on the LSD scale of ARCI. These data support the view that euphoria and some forms of craving may be pharmacologically separable. We found no potentially toxic interactions of bromocriptine with cocaine in these single dose experiments.

Blood Pressure↗

European multicentre trial of bromocriptine in cyclical mastalgia.

In a randomised parallel-block trial in thirteen European centres bromocriptine 2.5 mg twice a day was compared with placebo therapy for cyclical mastalgia. 272 patients were enrolled into the study. Linear analogue charts and diary pain cards were used for assessment of response. Reduction in breast pain, heaviness, tenderness, and serum prolactin after 3 and 6 months' therapy were significantly greater with bromocriptine than with placebo. Improvement in symptoms with bromocriptine was maintained for at least 6 months after therapy. Overall 29% of patients dropped out while on therapy, more from the bromocriptine than from the placebo group. Adverse effects, especially nausea and dizziness, were commoner among the bromocriptine-treated patients, but blood pressure was unaffected.

Adult↗

Bromocriptine and amantadine in cocaine detoxification.

The effects of bromocriptine and amantadine in treating cocaine withdrawal were compared. Withdrawal symptoms are thought to be due to central dopamine depletion. Both bromocriptine and amantadine are dopamine agonists previously reported to diminish withdrawal symptoms. Thirty subjects were withdrawn for 30 days with amantadine, bromocriptine, or placebo. Bromocriptine and amantadine were more effective than placebo for 15 days. Amantadine's effectiveness then declined so that it was no more effective than placebo by experiment's end. Bromocriptine was significantly more effective than both throughout the latter phase of the study. Amantadine's decline in effectiveness is hypothesized to be due to stimulation of dopamine release.

Adult↗

Effect of bromocriptin treatment on prolactin and steroid receptor levels in human breast cancer.

We have investigated the effect of bromocriptin, a prolactin-lowering drug, on prolactin, estradiol and progesterone receptors in breast cancers. Doses of 2.5 mg per os of bromocriptin were given twice daily for 4 days before surgery. The efficiency of the treatment was evaluated by assaying the plasma prolactin level. The results obtained for the treated population (n = 30) was compared to those obtained for an untreated one (n = 120) during the same period. Bromocriptin does not increase the available prolactin receptors in breast cancer specimens. Unmasking in vitro receptors with MgCl2 3 M leads in both cases to an increase in prolactin receptors. The number of positive estradiol receptor tumors was increased after bromocriptin treatment. Neither the rate of positivity nor the level of progesterone receptors is changed by the treatment. This study demonstrates clearly the inefficiency of bromocriptin in unmasking in vivo prolactin receptors in breast cancer.

Breast Neoplasms↗

Effects of bromocriptine on receptor binding of methionine-enkephalin.

Bromocriptine inhibited the binding of methionine-enkephalin (ENK) to rat striatal synaptic membranes in a dose-dependent fashion. The bromocriptine IC50 was 16 micrometers. hill coefficients of bromocriptine were 0.7 and 0.3, suggesting that an allosteric effect was involved in bromocriptine inhibition of ENK binding to its receptor. These data suggest that at least a part of the therapeutic antiparkinsonian effect f bromocriptine is its allosteric effects on the ENK receptor, which influences the function of striatal dopamine neurons and/or of striatal cholinergic neurons.

Animals↗

Bromocriptine stimulates Na+, K(+)-ATPase in renal proximal tubules via the cAMP pathway.

The present study was undertaken to examine the effect of dopamine D2 receptor activation on Na+,K(+)-ATPase activity in rat renal proximal tubule suspension. Bromocriptine, a dopamine D2 receptor agonist, produced a concentration (10(-9)-10(-5) M) dependent stimulation of Na+,K(+)-ATPase activity which was antagonized by pretreating the tubules with domperidone (1 microM), a dopamine D2 receptor antagonist. Forskolin (1 microM), a direct activator of adenylyl cyclase, inhibited Na+ K(+)-ATPase activity and reversed the stimulation of Na+,K(+)-ATPase activity induced by bromocriptine. Pertussis toxin (200 ng/ml) treatment also abolished the bromocriptine-induced stimulation of Na+,K(+)-ATPase activity. Bromocriptine attenuated forskolin-stimulated cAMP accumulation which was blocked by pertussis toxin treatment of the tubules. The data suggest that dopamine D2 receptor activation by bromocriptine leads to stimulation of Na+,K(+)-ATPase activity which may be mediated through a pertussis-sensitive G protein and inhibition of adenylyl cyclase in rat renal proximal tubules.

Animals↗

Effects of Ca2+ channel blockers on apomorphine, bromocriptine and morphine-induced locomotor activity in mice.

The effects of L-type voltage-dependent Ca2+ channel blockers on apomorphine, bromocriptine and morphine-induced changes in locomotor activity were examined in mice. Apomorphine (4 mg/kg) and morphine (20 mg/kg) produced locomotor stimulation. Bromocriptine (8 mg/kg) produced a biphasic effect on motor behaviour, an early depressant phase, followed by locomotor stimulation. Amlodipine (2.5 mg/kg), nicardipine (10 mg/kg), diltiazem (10 mg/kg) and verapamil (10 mg/kg), which by itself did not affect locomotor activity, inhibited the stimulant phase of bromocriptine without altering the depressant phase, while they did not affect apomorphine- and morphine-induced locomotor stimulation. Apomorphine, bromocriptine and morphine-induced locomotor stimulation was decreased by SCH 23390 (R-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7- ol) (0.05 mg/kg) or haloperidol (0.1 mg/kg). These results indicate that L-type voltage-dependent Ca2+ channels are involved in the motor stimulant effect of bromocriptine, but not in apomorphine- and morphine-induced locomotor stimulation. The effects of Ca2+ channel blockers on the dopaminergic system appears not to be directly related to dopamine receptor blockade.

Amlodipine↗

Bromocriptine in the treatment of hyperolactinemic amenorrhea.

Thirty women with secondary amenorrhea and hyperprolactinemia were studied; galactorrhea was present in 25 of them, and 18 were infertile. Serum prolactin (PRL) levels were high in all cases, between 26 and 120 ng/ml. All women were treated with bromocriptine in increasing doses from 2.5 to 5.0 or 7.5 mg daily, according to the response obtained, for 4 months. In 27 patients a PRL determination was performed during treatment; values returned to normal (up to 20 ng/ml) in 23 women and remained high in 4. Galactorrhea disappeared in 21 of 25 women. Ovulatory menses were re-established in 17 patients (56.6%). Seven women became pregnant (38.8%), one of them after bromocriptine and clomiphene were given simultaneously in the same cycle. According to our results and a literature review the following conclusions may be drawn: (1) bromocriptine is a useful therapeutic tool for re-establishing menstruation and inducing ovulation in patients with the hyperprolactinemic-amenorrhea syndrome; (2) the association of bromocriptine and clomiphene could be the next step in the treatment of patients who fail to ovulate with bromocriptine alone.

Adolescent↗

Restoration of ovarian function by low nocturnal single daily doses of bromocriptine in patients with the galactorrhea-amenorrhea syndrome.

Eighteen hyperprolactinemic patients with either amenorrhea or both galactorrhea and amenorrhea were treated with 2.5 mg of bromocriptine per day supplied at night. Ovulation occurred in 16 patients, and 8 wishing to conceive became pregnant. One of these patients became pregnant for a second time at a bromocriptine dose as low as 1.25 mg/day. Normal ovulatory cycles in four women receiving 2.5 mg of bromocriptine per day could also be maintained at 1.25 mg, despite the differences in the degree of prolactin (PRL) inhibition. Progesterone and luteinizing hormone levels measured for both bromocriptine levels were consistent with ovulatory cycles. The low, single dose of bromocriptine per day supplied at night decreased PRL levels, but normalization of blood levels did not always occur. Eighty percent of the patients ovulated with prolactin values over 25 ng/ml (normal value = less than 20 ng/ml).

Adolescent↗

Hyperprolactinemic response after bromocriptine withdrawal in women with prolactin-secreting pituitary tumors.

In patients with prolactin (PRL)-secreting tumors, plasma PRL concentrations after discontinuation of bromocriptine therapy have been used clinically as an index of tumor activity. To investigate the pattern of PRL response under these conditions, seven women on chronic bromocriptine therapy for PRL-producing pituitary tumors were followed with serial PRL determinations for 2 months after bromocriptine withdrawal. In these patients, peak PRL concentrations were achieved 28.1 days (mean; range, 14 to 49 days) after bromocriptine discontinuation. However, PRL concentrations did not usually plateau until at least 40 days after cessation of therapy, and the pattern of PRL response was highly variable. Because of the inconsistent pattern of serum PRL response during the first 40 days after discontinuation of bromocriptine, decisions regarding tumor activity based on PRL concentrations should not be made until at least 6 weeks after withdrawal of the drug.

Adenoma↗

The effect of bromocriptine on the motility of human spermatozoa and its capacity to penetrate the cervical mucus.

We investigated the direct effects of bromocriptine on the motility of the human ejaculated spermatozoa and its capacity to penetrate the cervical mucus (CM) in vitro. Washed sperm were incubated with a wide range of bromocriptine concentrations (0.005 to 5 mM). Progressive and total motility was evaluated after 15, 30, 60, and 180 minutes. No reduction of motility was observed at any concentration tested. Similar results were observed with semen samples. Failure to alter sperm motility was evident in samples with either good or reduced motility. Also, CM penetration as measured after 90 minutes by Penetrak assay (Serono Diagnostics, Randolph, MA) was not impaired by a concentration as high as 5 mM bromocriptine. We conclude that bromocriptine in a wide range of concentrations does not inhibit sperm motility nor does it impair the capability of the sperm to penetrate the CM. These data support the therapeutic use of daily vaginal bromocriptine for the treatment of infertility.

Animals↗

Macroprolactinomas with suprasellar extension: effect of bromocriptine withdrawal during one or more pregnancies.

OBJECTIVE: To investigate the effects of bromocriptine withdrawal during one or more pregnancies in patients who presented with pituitary macroprolactinomas with suprasellar extension. DESIGN: Four infertile patients presenting with a macroprolactinoma with suprasellar extension conceived during treatment with bromocriptine on 10 occasions resulting in eight full-term normal deliveries. Treatment was withheld shortly after conception in each pregnancy. RESULTS: Serum prolactin (PRL) levels fell initially from a mean of 2,776 (range 1,682 to 4,515) to 27 micrograms/L (range 1 to 71) with the development of a partially empty sella in all patients. Recovery of visual field defects occurred in the only affected individual. In case 1, PRL levels remained within the normal range, after bromocriptine withdrawal in the first pregnancy, with the development of an empty sella. Prolactin levels, however, increased substantially in cases 2 to 4. An asymptomatic suprasellar tumor extension returned in cases 2 and 3. After two or more pregnancies (cases 1, 3, and 4), there was a progressive decline in the serum PRL levels. Although still elevated in cases 3 and 4, the PRL levels were considerably below those obtained at presentation or in the first pregnancy. Tumor regression with the development of an empty sella was observed in both these patients as well in their pregnancy or postpartum period. CONCLUSIONS: Bromocriptine may be safely withdrawn during pregnancy in patients presenting with a macroprolactinoma. With multiple bromocriptine induced pregnancies, PRL levels and tumor size may progressively decrease with the eventual development of an empty sella.

Adult↗

A novel method of ovarian stimulation for in vitro fertilization: bromocriptine-rebound method.

OBJECTIVE: To examine whether a new method of ovarian stimulation, bromocriptine-rebound method, improves IVF outcomes compared with the conventional long protocol of GnRH agonist and hMG regimen. DESIGN: A prospective clinical trial. SETTING: In vitro fertilization program at a university hospital. PATIENTS: Endocrine-normal ovulatory women less than 40 years of age, with normal male partners and previous failed IVF-ET using long protocol. INTERVENTIONS: Patients were assigned to either bromocriptine-rebound method (group 1) or long protocol (group 2). The bromocriptine-rebound method was the same as the long protocol, except that bromocriptine was administered daily from day 4 of the preceding cycle until 7 days before hMG stimulation. MAIN OUTCOME MEASURES: The number of cleaved and morphologically superior embryos, pregnancy rate per oocyte pick-up, and serum PRL concentrations during administrations of hMG. RESULTS: Significantly more embryos were cleaved and had superior morphology in group 1 than group 2. Clinical and ongoing pregnancy rates per oocyte pick-up were significantly higher in group 1 (42% and 38%, respectively) than group 2 (24% and 21%, respectively). The mean PRL concentration was significantly higher in the group 1 than group 2. A significant correlation between the number of superior embryos and PRL concentrations was observed in group 1, but not in group 2. CONCLUSION: The bromocriptine-rebound method enhanced embryonic development, resulting in an increased pregnancy rate compared with the long protocol.

Adult↗

Terguride--a new dopamine agonist drug: a comparison of its neuroendocrine and side effect profile with bromocriptine.

Terguride, the C9-10 dihydrogenated derivative of lisuride, is a new drug which inhibits pituitary prolactin (PRL) secretion. It has mixed dopaminergic-antidopaminergic and alpha 2-antiadrenergic activity, and has proved useful in the clinical management of hyperprolactinemia. However, no trial comparing its use with the standard dopamine agonist bromocriptine has been reported. We have therefore compared three doses of terguride with bromocriptine 2.5 mg and placebo in a randomized double-blind crossover trial in eight normal volunteers. Terguride showed a potent dose-dependent PRL-inhibiting and growth hormone (GH)-releasing effect, while no significant changes were observed in thyroid-stimulating hormone (TSH), follicle-stimulating hormone (FSH), or luteinizing hormone (LH) in comparison to placebo. The neuroendocrine profile of terguride 1 mg was identical to that of bromocriptine, with a significant reduction in PRL still evident at 24 hours. However, in this small group of normal subjects, the side effects experienced at any dose of terguride were significantly less than with bromocriptine. Terguride 1 mg was always preferred to bromocriptine, while the lower doses were indistinguishable from placebo. Terguride is therefore likely to play an important role in the treatment of hyperprolactinemia.

Adult↗