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At least 19 recordsLinked to original sources
PubMed1976

A comparison of the effects of CB-154 and lergotrile mesylate on prolactin and growth hormone secretion in mice.

The influence of 2-bromo-alpha-ergocryptine (CB-154) and 2-chloro-6-methyl-ergoline-8beta-acetonitrile methanesulfonate (lergotrile mesylate) on prolactin (PRL) and growth hormone (GH) secretion in mice was investigated. Both drugs inhibited the nursing-induced rise in serum PRL in lactating mice, CB-154 being effective at a somewhat lower dosage than lergotrile mesylate. Both drugs reduced basal concentrations of serum PRL by more than 90% within an hr after administration, but the effect of CB-154 lasted for several hr longer than that of lergotrile mesylate. CB-154 did not change the resting concentrations of GH in mice, but it promoted the induction of GH release by nursing; injection of lergotrile mesylate, on the other hand, seemed to enhance the basal concentrations of GH in lactating mice that were separated from their young for 12 hr. The results show that both drugs can be used successfully for reducing PRL secretion in the mouse.

Acetonitriles↗
PubMed1975

Inhibition of prolactin secretion by lergotrile mesylate: mechanism of action.

Lergotrile mesylate (2-chloro-6-methylergoline-8beta-acetonitrile, methane-sulphate salt) was shown to be a potent inhibitor of prolactin secretion in vivo and in vitro. The dopamine receptor blocker, pimozide, was able to reverse the inhibitory effect of lergotrile mesylate (LM) on prolactin release from rat pituitaries in vitro. Alpha-adrenergic or beta-adrenergic receptor blockers were unable to antogonize the action of LM on prolactin release. These findings indicate that ergolines such as LM inhibit prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. LM is currently undergoing clinical trial as a prolactin inhibitor and a dopamine agonist.

Acetonitriles↗
PubMed1978

Effect of the dopamine agonist, lergotrile mesylate, on circulating anterior pituitary hormones in man.

The effects of the ergoline derivative, lergotrile mesylate, on the serum levels of PRL, GH, TSH, LH, FSH, cortisol, and blood sugar were studied in six normal males. The effects of lergotrile mesylate on the serum levels of GH and PRL were also studied in eight patients with acromegaly and in two with idiopathic hyperprolactinemia. In the normal subjects, 2 mg oral lergotrile lowered basal PRL levels after 90 min and markedly impaired the PRL response to TRH (200 micrograms iv); the mean peak value +/- SE was 8.3 +/- 1.1 micrograms/liter, compared to the control value of 66.6 /+- 11.3 micrograms/liter. Lergotrile raised serum GH levels in five of the six subjects to peaks of 8-49 micrograms/liter, compared to 2-8 micrograms/liter after placebo. In three subjects, the GH response to lergotrile was attenuated by the prior administration of the dopamine antagonist, metoclopramide (10 mg orally). Lergotrile had no effect on FSH and LH levels under basal conditions or after the gonadotrophin-releasing hormone (GnRH; 100 micrograms iv). Circulating TSH levels were unaltered basally but impaired after TRH. Blood sugar levels were unaltered; serum cortisol was elevated in five of six subjects; there was a brief depression of diastolic blood pressure, but no change in pulse rate. The side effects after lergotrile were variable, with drowsiness as a consistent feature. These actions are similar to those of bromocriptine (an ergot derivative treatment of hyperprolactinemia and acromegaly, to suppress PRL and GH secretion, and in parkinsonism. Therefore, it may be expected that lergotrile could fulfill these clinical uses; however, in the studies comparing the effects of single oral doses of lergotrile (2 mg) and bromocriptine (2.5 mg) on GH and PRL secretion in patients with acromegaly and hyperprolactinemia, lergotrile in the dose used has been found to have an earlier onset and shorter duration of action.

Acromegaly↗
PubMed1977

Treatment of Parkinson's disease with lergotrile mesylate.

Lergotrile mesylate, an ergot alkaloid derivative and putative dopamine agonist, was effective in the majority of patients with Parkinson's disease who were showing signs of disease progression despite treatment with levodopa combined with a peripheral decarboxylase inhibitor (carbidopa). Among 20 patients completing a six-month trial, there was a significant (P less than .01) reduction in rigidity, tremor, bradykinesia, gait disturbance, and total score when lergotrile was added to levodopa plus carbidopa. Mean daily dose of lergotrile mesylate was 52 mg, and the mean daily dose of levodopa was reduced by 15%. Abnormal involuntary movements were decreased on addition of lergotrile and reduction in levodopa while mental changes and orthostatic hypotension were increased. Elevations in serum transaminase levels were noted in three patients. The ergot alkaloids promise to be an important new class of antiparkinsonian drugs.

Acetonitriles↗
PubMed1975

Pralidoxime mesylate absorption and heart rate response to atropine sulphate following intramuscular administration of solution mixtures.

1. The oxime pralidoxime mesylate (P2S) and atropine sulphate, alone and mixed, have been administered intramuscularly to forty-four human subjects. Doses of 750 mg and 500 mg P2S and 2.0 mg atropine sulphate were used. 2. The presence of P2S had no significant influence, as judged by effect on heart rate, on the absorption of atropine although there was a tendency for atropine to exert its effects more rapidly when administered mixed with P2S. 3. No significant difference in the rate of uptake of P2S as judged by plasma levels following injection, between a combined (plus atropines) and single (P2S alone) intramuscular injection was found.

Absorption↗
PubMed1979

Reduction in blood pressure in normal and spontaneously hypertensive rats by lergotrile mesylate.

The acute administration of lergotrile mesylate to normal or spontaneously-hypertensive rats (SHR) causes a prompt reduction in blood pressure. In SHR, doses as small as 0.05 mg kg-1 are effective; maximal reductions in blood pressure are obtained at a dose of 0.25 mg kg-1. Lergotrile may be administered intraperitoneally or orally. Its efficacy as an antihypertensive agent in rats does not diminish significantly when administered twice daily for 7 days. Although lergotrile has been reported to be a dopamine agonist, the present data do not establish the mechanism by which the drug lowers blood pressure.

Animals↗
PubMed1979

Desferoxamine mesylate (Desferal): a contrast-enhancing agent for gallium-37 imaging.

Desferal (desferoxamine mesylate) was investigated as a contrast-enhancing agent for tumor and abscess imaging with 67Ga-citrate. Tumor studies were performed in mice with Cloudman S-91 melanoma. Abscess studies were performed with a subcutaneous abscess model in rabbits. When Desferal is administered 16 to 18 hours after injection of 67Ga, rapid blood clearance of 67 Ga occurs with only slight (tumor) or no (abscess) loss of activity from the lesion. Retention in other organs is variable. Tumor-to-blood ratios are improved eightfold in tumor and fourfold in abscess in studies performed with single Desferal injections of 150 mg/kg. Blood and total body clearance studies in rabbits reveal that maximum Desferal effect is achieved in the 17 to 50 mg/kg dose range and that only minimal improvement occurs at higher doses.

Abscess↗
PubMed1978

Effects of dihydroergotoxine mesylate on aging neurons in vitro.

C1300 mouse neuroblastoma cells gradually accumulate lipofuscin-like pigment when they are maintained in culture. Pigment was demonstrated by positive straining for acid phosphatase and with periodic acid-Schiff stain. Pigment was formation in cells was reduced by exposure of the cells to lower doses of dihydroergotoxine mesylate which also induced neurite formation and increased protein synthesis. Since lipofuscin appears to originate as a result of wear and tear within the cells, the drug probably exerts its beneficial effects by reducing the rate of intracellular wear and tear associated with aging.

Animals↗
PubMed1978

The influence of dihydroergotoxine mesylate on the low-Km phosphodiesterase of cat and rat brain in vitro.

Dihydroergotoxine mesylate (DHET; active substance of Hydergine) was shown to be a stronger inhibitor of the low-Km than of the high-Km phosphodiestrase (PE) in cat and rat brain homogenates. The inhibition due to DHET was greater when a purified low-Km PE preparation originating from a sonicated pellet (100,000 g) of rat brain tissue was used. The drug alters the kinetic properties of the enzyme, producing a lowering of the negative cooperativity effect. This kind of PE inhibition is of particular importance at normal cellular cAMP levels, but does not interfere with cAMP production by hormonal stimulation.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1978

Effect of dopamine agonist (Lergotrile mesylate) therapy on twenty-four hour secretion of prolactin in treated Parkinson's disease.

Plasma PRL was measured at 20-min intervals in six patients with Parkinson's disease under various treatment protocols. In addition, 24-h mean GH levels were measured. The results of these studies showed that two untreated patients with Parkinson's disease had normal 24-h mean PRL levels with the normal increase during sleep. During chronic treatment with L-dopa-carbidopa (Sinemet), the 24-h PRL level was 12.8 +/- 4.9 ng/ml (mean +/- SD) and there was persistence of augmented PRL secretion during sleep. The 24-h mean GH level ranged from 1.5-4.4 ng/ml, with a mean of 2.5 ng/ml. The addition of a dopamine agonist (Lergotrile mesylate) resulted in a significant (P less than 0.01) suppression of the 24-h mean PRL levels and abolition of the normal sleep augmentation after 2 weeks of therapy. This suppression was maintained in one patient who was restudied 4 months after the addition of dopamine agonist therapy to L-dopa-carbidopa. The 24-h mean GH levels did not change significantly after the addition of the dopamine agonist when compared to L-dopa-carbidopa alone. These results suggest a dichotomy between the PRL and GH responses to combined L-dopa-carbidopa and dopamine agonist therapy. In addition, the preservation of normal PRL regulation in the two untreated patients with Parkinson's disease suggests that dopaminergic neurons are not universally affected in this disorder.

Adult↗
PubMed1977

The effect of 2-bromo-alpha-ergocryptine and 2-chloro-alpha-methylergoline-8beta-acetonitrile (lergotrile mesylate) on the prolactin secretion of the ewe.

The effects of two ergot alkaloids, 2-bromo-alpha-ergocryptine methane-sulphonate (CB154, Sandoz) and lergotrile mesylate (LM, E. Lilly & Co.), on the basal secretion of prolactin and on the prolactin response to TRH or the milking stimulus was investigated in the sheep. Both CB154 (c. 0.5 mg/kg) and LM (c. 0.75 mg/kg) markedly reduced basal levels of prolactin and inhibited the TRH-induced prolactin release in ewes in the mid-luteal phase of the oestrous cycle. Both compounds also suppressed basal levels of prolactin in lactating ewes and inhibited the prolactin response to the milking stimulus in lactating ewes.

Acetonitriles↗
PubMed1978

Effects of bromocriptine mesylate on the composition of the mammary secretion in non-breast-feeding women.

A double-blind trial was performed on 26 women, who had elected not to breast-feed their infants, to determine the effect of bromocriptine mesylate (2.5 mg twice daily for 14 days postpartum) on the composition of the mammary secretion during lactogenesis. Mammary secretion (less than 5.0 ml) was collected from each breast of each woman at daily intervals during the 14-day treatment period and the progressive changes in the concentration of the milk constituents, lactose, alpha-lactalbumin, serum albumin, total protein, lactoferin, IgA, IgG, sodium and potassium were determined. The degree of milk leakage and breast engorgement were also assessed. Both the subjective assessments and the changes in the concentration of the milk constituents demonstrated that lactogenesis occurred between about Day 2 and Day 5 postpartum in the placebo group (in the absence of the suckling stimulus) but was suppressed in the bromocriptine-treated group.

Breast↗
PubMed1978

Pituitary and adrenal function in normal women after treatment with Lergotrile mesylate.

We studied the effects of a dopaminergic agonist, 2-chloro-6-methyl-ergoline-8-beta-acetonitrile methanesulfonate (LERGOTRILE mesylate), on the pituitary and adrenal function of five normal women. No changes were observed in basal serum luteinizing hormone (LH), follicle-stimulating hormone (FSH), growth hormone (GH) and cortisol levels, in LH and FSH levels after luteinizing hormone-releasing hormone (LH-RH) stimulation, or in GH and cortisol levels during insulin-induced hypoglycemia. Lergotrile treatment produced a fall in basal prolactin and thyrotropin (TSH) levels and there was dissociation in the responses of the women to thyrotropin-releasing hormone: attenuation of TSH release, but retention of prolactin release.

Acetonitriles↗
PubMed1979

Acute confusional states and depression treated with maprotiline mesylate. Report of 4 patients successfully treated in an intensive care unit.

Four patients admitted to hospital with multiple injuries developed psychiatric symptoms after an initially favourable response to intensive therapy. Alterations in the level of consciousness and behavioural pattern were observed, associated with the presence of acute depression, possibly endogenous in origin. Within 24--48 hours of intravenous administration of maprotiline mesylate (Ludiomil, Ciba), a tetracyclic antidepressant drug, considerable improvement was noted in all 4 patients, with regard to both the depressive state and the clouding of consciousness. The importance of recognizing psychiatric disorders in severely ill patients in an intensive therapy environment is stressed.

Anthracenes↗
PubMed1978

The treatment of hyperprolactinemia with a new ergot derivative, lergotrile mesylate.

Lergotrile mesylate is an ergot alkaloid derivative modified to eliminate the vasoconstrictive properties of the parent compound while preserving the properties that inhibit pituitary secretion. Administration of the drug to women with amenorrhea-galactorrhea resulted in the lowering of serum prolactin concentrations. The duration of action was short, so that prolactin levels were near base line 6 to 8 hours after a 2.0-mg dose and morning prolactin concentrations were not persistently suppressed. Initial therapy was accompanied by the development of postural hypotension. Tolerance to this side effect of the drug developed after several days of treatment with gradually increasing doses. In one patient, long-term treatment resulted in reduction of breast secretions, resumption of menses, and conception.

Acetonitriles↗
PubMed1978

Failure to detect dominant-lethal mutations and effects on reproductive capacity in mice exposed to dihydroergotoxine mesylate.

Triethylenemelamine (TEM), a known chemical mutagen, and dihydroergotoxine mesylate (DHETM, Hydergin), an ergot derivative, were tested for mutagenic effects by means of the dominant-lethal test in male mice and the total reproductive capacity test in female mice. In contrast to TEM, which proved to be strongly effective in these test systems, DHETM did not show any effect. It is concluded that this drug, at both subtoxic and pharmacologically active dose-levels, has no potential to affect spermatogenic and oogenic cells.

Animals↗
PubMed1979

Dopamine agonist-induced hyperglycemia in rats: effects of lergotrile mesylate.

Lergotrile and apomorphine, two direct-acting dopamine agonists, caused marked hyperglycemia in fasted rats, while compounds which release endogenous dopamine (amphetamine, methylphenidate) or inhibit dopamine reuptake (LR5182), failed to elevate blood glucose. The effect of lergotrile was dose dependent, causing blood glucose to rise 3-fold above resting levels at 5 mg/kg (i.p.). Blood glucose increased prior to the onset of the behavioral signs of dopamine stimulation. The effect of lergotrile was attenuated by phentolamine, propranolol or butaclamol. Adrenalectomy also prevented lergotrile-induced hyperglycemia. These data indicate that hyperglycemia is not a property of all compounds that cause dopaminergic effects. The action of lergotrile might be indirect, perhaps mediated through release of catecholamines from the adrenal glands.

Adrenalectomy↗