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Cabergoline is a synthetic ergoline which shows high specificity and affinity for the dopamine D2 receptor. It is a potent and very long-acting inhibitor of prolactin secretion. Prolactin-lowering effects occur rapidly and, after a single dose, were evident at the end of follow up (21 days) in puerperal women, and up to 14 days in patients with hyperprolactinaemia. In the only comparative study to date, cabergoline 0.5 to 1.0 mg twice weekly was more effective than bromocriptine 2.5 to 5.0 mg twice daily in the treatment of hyperprolactinaemic amenorrhoea, restoring ovulatory cycles in 72% of women and normalising plasma prolactin levels in 83%, compared with 52 and 58%, respectively, for bromocriptine. In the prevention of puerperal lactation, a single dose of cabergoline 1.0mg was as effective as bromocriptine 2.5mg twice daily for 14 days. A significantly lower incidence of rebound lactation in the third postpartum week was seen with cabergoline. Unpublished data suggest cabergoline 0.25mg twice daily for 2 days is effective in suppressing established puerperal lactation in about 85% of women. Nausea, vomiting, headache and dizziness are characteristic adverse events of the dopaminergic ergot derivatives. Cabergoline appears to be better tolerated than bromocriptine in both patients with hyperprolactinaemia and postpartum women. Most patients intolerant of other ergot derivatives can tolerate cabergoline. Bromocriptine use in the puerperium has been associated with an increased risk of serious thromboembolic events. However, there are no such reports with cabergoline and whether these events will become associated with other dopaminergic agents is unknown. The teratogenic potential of cabergoline has not been extensively investigated in humans. Ten congenital abnormalities have been reported in 199 cabergoline-associated pregnancies. Although there is no pattern to these abnormalities, the limited experience with cabergoline in pregnancy means the drug cannot be considered as a first-line therapy for the treatment of infertility associated with hyperprolactinaemia. At this stage of its development, cabergoline will prove useful in patients with hyperprolactinaemia who have failed treatment with, or are intolerant of, other dopamine agonists such as bromocriptine. If drug treatment is required for the prevention or suppression of puerperal lactation, cabergoline offers significant advantages over bromocriptine and should become the drug treatment of first choice for this indication.
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PMID:Cabergoline. A review of its pharmacological properties and therapeutic potential in the treatment of hyperprolactinaemia and inhibition of lactation. 772 32

Pituitary apoplexy results from necrosis or haemorrhage of a pituitary adenoma. This rare complication occurs in 2 to 10% of operated adenomas. The acute form results from massive intrapituitary bleeding leading to violent headache, meningeal signs, impaired conscience and ophthalmology signs, basically bilateral blindness. Associated signs are frequent including paralysis of the oculomotor nerves, epilepsy seizure, hemiplegia. Diabetes insipidis is exceptional. In less acute forms, the sudden nature of the headache and ophthalmology signs can suggest diagnosis. Standard X-ray reveals destruction of the sella turcica. Computed tomography shows either a haematoma or a cystic cavity in the pituitary gland which must be perfectly described together with the integrity of the bone structures due to the risk of lysis. Magnetic resonance imaging is an essential technique which can be used to describe the volume and suprasellar extension of the tumour, its texture, possible compression of adjacent structures and determine the age of the haemorrhage. This imaging technique can also isolate rare optochiasmatic apoplexia requiring intracranial evacuation. Emergency surgery is mandatory for most all authors. Rhinal-septal decompression is usually used, but the intracranial route may be preferred for very large suprasellar tumours. Medical treatment alone may be successful for small prolactin adenomas. Outcome depends on the time lapse to decompression. Optic nerve recovery is usually possible if the delay is less than 7 days. Cranial nerve recovery is less dependent on the time interval. In all cases hormone substitution is required.
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PMID:[Pituitary apoplexy]. 854 41

In an open, non-randomized prospective phase-III-study the clinical and endocrine efficacy as well as the safety of leuprorelin acetate depot (Enantone-Gyn Monats-Depot) were investigated. The therapeutic results of 198 patients, gathered from 5 university institutions and two city hospitals, are reported. Endometriosis was classified by the revised American Fertility Society score (r-AFS) before and at the end of treatment. Serum levels of LH, FSH, prolactin, estradiol, progesterone, androstenedione, testosterone and leuprorelin acetate were determined by radioimmunoassay. The mean total r-AFS score changed as follows: before surgical intervention during first-look laparoscopy 21 +/- 24 at the end of first-look laparoscopy 15 +/- 19 at the end of the GnRH-treatment 8 +/- 14 During leuprorelin acetate treatment the r-AFS stages changed as follows: [table; see text] Using the scoring system 85.2% of the patients improved. Relief of dysmenorrhoea could be achieved in 95.4%, relief of dyspareunia in 64% and of pelvic pain in 69.4% of patients. Baseline hormone levels dropped sharply during treatment. [table; see text] Androstenedione, testosterone, blood pressure, body weight, haematological parameters, liver enzymes, creatinine, electrolytes and HDL-/LDL-cholesterin remained more or less unchanged. Side effects being hot flushes, sweating, sleeplessness, headache, nausea, depression and vaginal dryness were due to estradiol deprivation. In 135 patients resumption of menstruation occurred in 95.6% within the first three months post-treatment. 23 patients of whom 21 were judged as infertile, became pregnant immediately after treatment was finished. The study results confirm the efficacy of leuprorelin acetate depot in the treatment of even advanced stages of endometriosis.
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PMID:[Treatment of endometriosis with the GnRH agonist leuprorelin acetate depot (Enatone-Gyn monthly depot): a multicenter study]. 784 80

The authors examined clinically 1710 women. Among them 199 women with symptoms of menopause were selected and divided into two groups: group I (control) included 80 women without contact with carbon disulphide and group II (examined) included 119 women chronically exposed to carbon disulphide at a concentration of 9.36-23.4 mg/m3. Menopause was present in 16.59% of women chronically exposed to CS2 as compared with 8.05% of the normal population. The mean age at menopause was 48.1 years in group I and 43.9 in group II. Significantly more frequent headaches, weight gain and loss of libido (p < 0.01) were observed in women chronically exposed to CS2. While in the control group fatigue, palpitations and hot flushes were more often (p < 0.001). The concentrations of estrone (p < 0.01), estradiol, progesterone, 17-hydroxy-progesterone, testosterone and dehydroepiandrosterone sulphate (DHAS) were significantly decreased in women chronically exposed to CS2 (p < 0.001). No difference in the level of dehydroepiandrosterone was found. The daily excretion of adrenaline and noradrenaline in urine and concentrations of dopamine in plasma of women chronically exposed to CS2 were lower (p < 0.001), while the concentrations of serotonin and prolactin in plasma were higher (p < 0.001). No differences in the level of FSH or LH were noted between the two groups. Significant negative linear correlations between serotonin and FSH (r = -0.45; p < 0.01) serotonin and daily excretion of adrenalin (r = -0.43; p < 0.01) or noradrenalin (r = -0.58; p < 0.001) were found in the exposed group.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Effect of carbon disulfide on menopause in women]. 799 46

63 cases of hyperprolactinaemia (55 women and 8 men) were studied. Of the 55 women, 39 presented with infertility, while five were unmarried and had menstrual abnormalities. All eight men were partners of an infertile union. The principal modes of presentation of hyperprolactinaemia in women were infertility (74.6%) and menstrual disorders (27.6%). Galactorrhoea was evident in 28.6% and 10.7% had headache. There was no significant correlation between the level of prolactin and the duration of amenorrhoea. Changes in pituitary gonadotrophin levels were observed in 30.2% of cases, the common feature being an elevated LH level. Treatment with bromocriptine restored normal cycles, and the incidence of pregnancies was 38.5%. 14 normal infants were born and one patient miscarried.
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PMID:Hyperprolactinaemia and reproductive failure. 814 34

The phenomenon of clinical improvement of diabetes mellitus after occurrence of pituitary insufficiency has been reported occasionally in the medical literature, as a human counterpart of Houssay's experiment with hypophysectomized diabetic animals. We report the case of a 76-year-old woman who developed diabetes in 1928, at the age of 14, and was treated with low doses of insulin. At the age of 29, during the 7th month of her second pregnancy, she suddenly developed severe headaches and soon afterwards an intense polyuria which subsided under treatment with posterior pituitary extract. Her pregnancy followed to term but uterine stimulants had to be used at delivery because of lack of contractions. She was unable to nurse her baby and a permanent amenorrhea ensued. She continued using the posterior pituitary powder for several years, after which she discontinued it without adverse effects. The dose of insulin was decreased gradually until its replacement by chloropropamide in 1967 and glibenclamide in 1970. The present dose of glibenclamide is 2.5 mg daily, on which she has occasional mild hypoglycemic reactions. When the medication was discontinued for 5 days glycemia rose to 450 mg/dl but responded immediately to 2.5 mg of the drug with a mild hypoglycemia. She never required thyroid hormone therapy. Glucocorticoid substitution was instituted recently because of evidence of mild adrenocortical insufficiency. Basal hormone levels were normal for thyroxin, thyrotropin, FSH, LH, prolactin, hGH and cortisol; the responses to pituitary stimulation with TRH and LHRH were subnormal or nil. Cortisol stimulation with ACTH was normal. Insulin levels rose moderately after stimulation with glucagon, and with glibenclamide, with simultaneous marked decrease in glycemia.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Houssay's phenomenon in man]. 820 16

The cause of cluster headache remains to be determined. The involvement of peripheral neurovascular structures can explain the pain and autonomic signs of a cluster attack, but not its rhythmicity. The central theory of cluster headache attributes the cyclic recurrence to involvement of the hypothalamus. To evaluate hypothalamic dysfunction a number of hormone studies have been carried out on cluster headache patients. Alterations in plasma melatonin, cortisol, testosterone, gonadotrophins, prolactin, growth hormone and thyrotropin have been documented, some only in the cluster period but others in the remission phase of the illness. We believe that the hormonal abnormalities in cluster headache support disorders of hypothalamic function.
Cephalalgia 1993 Oct
PMID:A review of hormonal findings in cluster headache. Evidence for hypothalamic involvement. 824 22

The serotonin receptor agonist m-chlorophenylpiperazine (m-CPP) stimulates the release of cortisol and prolactin, and induces migraine-like headaches. We have studied the neuroendocrine and headache responses to m-CPP in 8 subjects with migraine and 10 normal subjects. Each subject underwent two challenge tests, one with 0.25 mg/kg PO of m-CPP and the other with placebo, administered in a double-blind crossover format. Serial measurements of serum cortisol, prolactin, and m-CPP levels were made at 30-min intervals for 210 min following ingestion of the medication. The incidence and severity of headache was assessed by a structured telephone interview after each test. We confirmed that m-CPP stimulates the release of cortisol and prolactin, and may induce headache, in both migraine subjects and normal controls. The cortisol response as well as ratings of headache severity and duration directly correlated with plasma levels of m-CPP. There were highly significant associations between the cortisol response and both headache severity and duration, independent of m-CPP plasma levels. We did not find statistically significant differences between the migraine and normal subjects in terms of their neuroendocrine or headache responses to m-CPP.
Cephalalgia 1993 Dec
PMID:Headache and cortisol responses to m-chlorophenylpiperazine are highly correlated. 831 48

We evaluated the effect of l-deprenyl, a drug that increases the availability of endogenous dopamine, on the plasma levels of prolactin and growth hormone in 10 female patients with migraine and in 10 control subjects matched for age and menstrual phase. The patients showed a significant decrease in prolactin levels at 30, 60 and 120 min after the oral administration of 5 mg of l-deprenyl when compared with the values obtained in controls (p < 0.001). The effects of l-deprenyl on growth hormone plasma levels were not significantly different between patients and controls. These data suggest that l-deprenyl inhibits prolactin release in migraine patients, but not in control subjects. This differential sensitivity could be explained by dopamine receptor supersensitivity in migraine patients.
Cephalalgia 1993 Dec
PMID:l-deprenyl test in migraine: neuroendocrinological aspects. 831 54

A case of actinomycotic granuloma of the optic chiasma and the optic nerve is reported. A 53-year-old man was admitted to our hospital with headache and vomiting on September 25, 1989. General physical and neurological examination on admission revealed no remarkable findings. CT-scan demonstrated almost normal pictures. On the 17th hospital day, his temperature was 38 degrees C and white blood cell (WBC) count was 12000 cumm. And he presented right abducens palsy. MRI demonstrated no abnormal findings then. After antibiotic therapy of penicillin intravenously for 4 days, his temperature returned to normal and abducens palsy disappeared for two weeks. He was discharged 43 days after admission. But one year after discharge he developed progressive impairment of right visual acuity. He was admitted to our hospital again on January 19, 1991. His neurological examination revealed severe impairment of right visual acuity and bitemporal hemianopsia. WBC count was 5400 and CRP was negative and temperature was 36.2 degrees C. CT-scan and MRI demonstrated a suprasellar enhancing mass lesion. Serum prolactin was 38 ng/ml. A diagnosis of pituitary adenoma was considered and a right frontotemporal craniotomy was performed. At operation, abnormally swelled right optic nerve and chiasma were found and the swelled chiasma only was resected. Histological examination showed an abscess containing necrotic tissues and actinomycotic granules with radiating filaments. The patient was given penicillin intravenously for 37 days and orally for two months. At that time, MRI revealed no abnormal enhancing lesion, and his visual acuity improved gradually. Actinomycosis of the optic nerve and chiasma is very rare.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Actinomycotic granuloma of the optic chiasma: a case report]. 832 54


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