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At least 19 recordsLinked to original sources
PubMed1984

Ergoloid mesylates for senile dementias: unanswered questions.

Ergoloid mesylates has been used for 30 years to treat patients with senile dementia. Indications for this drug include hypertension, peripheral vascular disease, and senile dementia of the Alzheimer type. Formerly classified as a cerebral vasodilator, ergoloid mesylates is now considered a metabolic enhancer, but how this action pertains to treatment of senile dementia is uncertain. Prescribed doses of the drug range from 1.5 mg/d to as much as 12 mg/d, but the optimal dose is unknown. Although there is evidence of the short-term efficacy of ergoloid mesylates from numerous controlled trials, many clinicians still consider it to be a placebo. No alternative drug treatments have been proved better. The crucial decision a physician must make is whether to try specific drug therapy or rely solely on supportive care and symptomatic drug treatment. The increasing prevalence of senile dementia has renewed interest in discovering more effective drug treatments for this condition.

Alzheimer Disease↗
PubMed2006

The effects of ergoloid mesylates and ginkgo biloba on the pharmacokinetics of ticlopidine.

Ticlopidine is sometimes coadministered with ergoloid mesylates or ginkgo biloba in clinical situations. Our objective was to examine the effect of ergoloid mesylates and ginkgo biloba on ticlopidine pharmacokinetics. Ticlopidine, ergoloid mesylates, and ginkgo biloba significantly inhibited the organic anion transporting polypeptide (OATP-B)-mediated uptake of [(3)H]-estrone-3-sulfate in a concentration-dependent manner. When ergoloid mesylates was coadministered with ticlopidine, the ticlopidine area under the plasma drug concentration-time profile (AUC) from 0 to 12 hours was decreased 30% and the peak plasma drug concentration (C(max)) was decreased 29%, compared with ticlopidine administration alone. There were no significant changes in the pharmacokinetic parameters of ticlopidine when it was coadministered with ginkgo biloba. In summary, ergoloid mesylates is a more potent inhibitor of OATP-B than is ginkgo biloba, and it can reduce the oral bioavailability of drugs transported by OATP-B. Ergoloid mesylates markedly decreased the AUC and C(max) of ticlopidine, probably by inhibiting the OATP-B-mediated uptake of ticlopidine during the intestinal absorption phase. The results support a new model of intestinal drug-drug interaction.

Adult↗
PubMed1986

Effects of long-term ergoloid mesylates ('Hydergine') administration in healthy pensioners: 5-year results.

Five-year results are reported of a controlled long-term comparative study to assess the effects of ergoloid mesylates (1.5 mg 3-times daily) and placebo on medical, psychological and electrophysiological variables. Initially, 148 healthy elderly volunteers of both sexes were included. Eighty-nine subjects (48 on ergoloid mesylates and 41 on placebo) are still in the double-blind study; 39 subjects have left the trial for various reasons (6 deaths, 25 drop-outs due to disease, and 8 withdrawals) and 20 subjects are participating under 'open' conditions. Formal statistical comparison of the two groups in terms of 10 medical and psychometric outcome variables did not produce significant differences. However, a number of relevant findings and trends with regard to the effects of ergoloid mesylates were established: the drug was well tolerated objectively and subjectively; subjective complaints such as frequent dizziness, cardiac symptoms and leg cramps were improved; there was less increase than on placebo in the number of subjects with pathological ECG findings; there was less increase than on placebo in the number of subjects taking digitalis; fewer subjects than in the placebo group had an increase in the number of major diagnoses; the decrease in some lipid fractions was more pronounced than on placebo; and performance in some psychometric tests (WAIS Vocabulary, WAIS Performance) was better in the ergoloid mesylates group. None of these findings, by itself, would be evidence of a dramatic effect of ergoloid mesylates on the participants in the double-blind trial. Taken together, however, they fall into a pattern, suggesting that ergoloid mesylates was partly effective in maintaining physical and mental health in these healthy elderly individuals. The finding of more disease-related and symptom-related drop-outs in the placebo group (25 vs. 20 in the ergoloid mesylates group) supports this assumption. Furthermore, the fact that a number of subjects who had left the double-blind trial for medical reasons improved on subsequent ergoloid mesylates administration may be seen as a further argument in favour of a prophylactic effect of ergoloid mesylates on pathological concomitants of ageing.

Aged↗
PubMed1983

A controlled long-term study with ergoloid mesylates (Hydergine) in healthy, elderly volunteers: results after three years.

A long-term clinical comparison of the effects of ergoloid mesylates and placebo on 148 healthy elderly volunteers of both sexes was analyzed after three years of study. At that point, 99 subjects (53 receiving ergoloid mesylates and 46, placebo) were still being treated under double-blind conditions, while the remainder either had dropped out or continued to participate under open conditions. Many subjects in both groups were healthier after the three years than they had been at the onset of the study: subjective symptoms such as tiredness and dizziness were reduced, performances on tests of intelligence were improved, and some abnormal laboratory values had normalized. Blood pressures increased on the average during the investigational period and pulse rates became slower. The ergoloid mesylate regimen was well tolerated objectively and subjectively. Additional medical and psychologic improvements were noted in the group treated with ergoloid mesylates concerning cardiovascular parameters, cholesterol levels, subjective symptoms, and performances on tests of intelligence. These intermediate findings are interpreted as showing a preventive effect of ergoloid mesylates against some of the debilitating physical and psychologic concomitants of aging.

Aged↗
PubMed1985

Bioavailability of ergoloid mesylates liquid capsule.

Bioavailability of two formulations of ergoloid mesylates was compared in 18 healthy men. In a randomized, crossover design, each subject received a single oral dose of six liquid capsules and six oral tablets, each capsule or tablet containing 1 mg of the active ingredient. A one-week washout period intervened between the two doses. Blood samples were drawn at intervals up to ten hours after drug ingestion and were assayed for plasma concentrations of ergoloid mesylates by a specific radioimmunoassay. The liquid capsule produced mean peak concentrations and areas under the curve (AUC) that were about 12% higher than those produced by the oral tablet; these differences were statistically significant (P less than 0.05). No statistically significant differences were observed for the other pharmacokinetic parameters, namely, time to peak concentration, apparent rate constants for absorption and elimination, and lag time. As the differences in peak concentration and AUC were less than 20%, even though they were statistically significant, the two formulations were considered bioequivalent according to FDA guidelines for bioequivalence. The therapeutic benefit that might derive from greater bioavailability of the liquid capsule has not been established.

Administration, Oral↗
PubMed1996

Posttranslational changes in band 3 in adult and aging brain following treatment with ergoloid mesylates, comparison to changes observed in Alzheimer's disease.

Band 3, the most heavily used anion transport system in vertebrates, ages as cells and tissues age. Posttranslational changes in band 3 in adult and aging brain were investigated following treatment with ergoloid mesylates and compared to changes observed in Alzheimer's disease (AD). The study was conducted in a double blind fashion and was decoded only after the study was completed. The following posttranslational changes in brain band 3 occur with age: increased breakdown of band 3; decreased phosphorylation; and decreased anion transport. Autoantibodies to senescent cell antigen (SCA) synthetic peptides residue 538-554 and 812-827 increase with age, but antibodies to the former peptide are significantly reduced in ergoloid mesylate treated old mice. This is a critical transport region of band 3. Results showed the aged/altered band 3 increased in Alzheimer's disease (AD) as determined by quantitative antibody binding. Ergoloid mesylates altered the age-related posttranslational changes as follows: the observed age-related decrease in brain band 3 was partially reversed and anion transport was increased. This is consistent with the data indicating decreased autoantibodies to a critical anion transport segment of band 3. Aging appears to result in damage to a critical transport region of the anion transporter which is reflected by decreased anion transport, increased breakdown, alteration of the molecule itself, and an increase in autoantibodies to the region. Ergoloid mesylates seem to protect against this damage.

Aging↗
PubMed1989

Ergoloid mesylates ('Hydergine') in the treatment of mental deterioration in the elderly: a 6-month double-blind, placebo-controlled trial.

A double-blind, placebo-controlled trial was carried out in 97 elderly patients with age-related mental deterioration to assess the efficacy of ergoloid mesylates in improving their symptoms. Patients were allocated at random to receive either 4.5 mg ergoloid mesylates per day or a matching placebo tablet and were followed-up for 6 months after the start of treatment. Clinical examinations were performed by the doctor, using the EACG rating scale (a French version of the Sandoz Clinical Assessment Geriatric scale), and by the nurse, using the NOSIE scale, when patients entered the trial and repeated after 2, 4 and 6 months. Changes in the factors (symptom groups) covered by these scales were subjected to statistical analysis. After 6-months' treatment, a statistically significant difference in favour of the ergoloid mesylates group was observed for cognitive deficits (p less than 0.05), anxiety and mood depression (p less than 0.01), unsociability (p less than 0.01), retardation (p less than 0.05) and irritability (p less than 0.001). Treatment was very well tolerated. It was also observed that there was a progressive increase in efficacy throughout the trial; this indicates that treatment with ergoloid mesylates in patients with mental deterioration should be long-term.

Aged↗
PubMed1989

Ergoloid mesylates and ECT.

Amnesia is the most common adverse effect among patients receiving electroconvulsive therapy. In a double-blind pilot study, patients receiving bilateral ECT were pretreated with ergoloid mesylates (N = 5) or placebo (N = 5). Consistent with the hypothesis that ergoloid mesylates might protect against ECT-associated amnesia, nonsignificant trends on some memory tests showed better performance for patients receiving active treatment. Unexpectedly, patients treated with ergoloid mesylates had a significantly better antidepressant response.

Amnesia↗
PubMed1984

Double-blind clinical and psychologic study of ergoloid mesylates (Hydergine) in subjects with senile mental deterioration.

A double-blind study of 24 weeks' duration was conducted to investigate the effects of ergoloid mesylates (Hydergine) on symptoms of senile mental deterioration. Fifty-eight residents of old people's homes were included in the trial. Thirty were treated with ergoloid mesylates and 28 with placebo, and the effects of treatment were determined by means of medical and psychological examinations. On the Sandoz Clinical Assessment Geriatric Scale, the group receiving ergoloid mesylates showed significant improvement in all items. The group receiving placebo showed slight deterioration. Psychological examination showed that no changes were observed for either group in quantitative psychometric test results, although qualitative aspects of performance such as attention and concentration did improve. There was a close correlation between improved cognitive function scores on the SCAG and improved evaluations of behavior during the psychological examinations. There were marked individual differences in the degrees of improvement.

Aged↗
PubMedDate not supplied

Pharmacokinetics and bioavailability of ergoloid mesylates.

The pharmacokinetics and bioavailability of ergoloid mesylates following single administrations of various dose levels (3-9 mg), dosage forms (oral swallow and sublingual tablets, solution) and under different dosing conditions (fasted, with meal) were studied in young healthy volunteers. Male and female subjects showed a similar rate and extent of bioavailable ergoloid after drug treatment. The absorption of ergoloid using either the tablet dosage forms or the drug administered as a solution was rapid, with peak levels of about 60-80 pg ml-1 mg-1 dose achieved after 0.6 to 1.3 h. The elimination half-life for ergoloid in plasma was 2-5 h. Administration of drug with food had no effect on the extent of absorption (AUC) but lowered the absorption rate. This resulted in a reduction of (by 25 per cent) and delay in (by 1 h) achieving peak levels (Cmax). Increasing the ergoloid dose caused a proportional increase in the AUC, but a smaller than proportional increase for Cmax. The tablet formulations provided similar AUCs as the solution; the objective of the sublingual tablet formulation to provide improved bioavailability over the swallow tablet via circumvention of first-pass metabolism was therefore not realized. Transient decreases in blood pressure after ergoloid treatment paralleled the plasma level profiles. Higher ergoloid levels were paired with the larger pressure decreases.

Administration, Oral↗
PubMed1986

Combination therapy with lecithin and ergoloid mesylates for Alzheimer's disease.

A 10-week placebo-controlled double-blind crossover protocol of combination therapy with lecithin and ergoloid mesylates was conducted in seven patients with presenile and senile dementia, Alzheimer's type. The patients' abilities to detect spatial arrangements, to recognize faces, and to identify new words on the Delayed Recognition Span Test were not significantly improved. Dementia Rating Scale scores before treatment were not significantly different from those after treatment.

Aged↗
PubMed1985

CSF levels of neurotransmitters in Alzheimer-type dementia. Effects of ergoloid mesylate.

The cerebrospinal fluid level of homovanilic acid (HVA), 5 hydroxyindolacetic acid (5HIAA) and 3 methoxy-4-hydroxy phenylglycol (MHPG) was determined twice at 12 to 15-day intervals in 23 patients with Alzheimer-type dementia (ATD). No correlation was found with the degree of dementia as assessed by psychometric testing. In most of the patients, the CSF levels of 5HIAA, MHPG and to a lesser extent HVA were found to be rather stable within a period of 2 weeks. The observation of a decrease in the concentration of HVA but not of 5HIAA or MHPG in 10 out of 12 patients treated with ergoloid mesylate may therefore be of interest in elucidating the mechanism of action of this drug in ATD.

Aged↗
PubMedDate not supplied

The ergoloid mesylate dihydroergotoxine: radioimmunoassay measurements on plasma and blood-pressure-lowering activity.

Dihydroergotoxine plasma concentrations determined using a newly developed radioimmunoassay method and corresponding blood-pressure-lowering effects have been measured in normotensive subjects after intravenous injection (0.6 mg) and administration of an oral solution (4.5 mg). Plasma concentrations in the range 0.2-1 ng/ml dihydroergotoxine produced clinically significant reductions of up to 15% in systolic and diastolic standing and supine blood pressures, while no significant changes occurred in pulse rate.

Adult↗
PubMed1986

Drug therapy of Alzheimer's disease: realistic or not?

Drug therapy of Alzheimer's disease is either symptomatic, directed against behavioral manifestations, or specific, presumably directed against some hypothetical pathogenetic mechanism. Symptomatic treatment involves the use of antipsychotic drugs, alone or combined with benzodiazepines, to curb disturbed behavior, restore a normal sleep-wake cycle and improve self-care. Antidepressants can be used cautiously when indicated. Specific treatment has employed many different drugs over the years, including stimulants, cerebral vasodilators, drugs for certain hypothesized causes of the disorder, and drugs assumed to enhance metabolism of the brain, or to protect it against various insults. Of the metabolic enhancing drugs, ergoloid mesylates, nafronyl and piracetam are of the greatest current interest. Ergoloid mesylates have been the most extensively studied, but many questions about this drug, such as its mechanism of action, its proper dose, the proper duration of treatment, and the proper goals of treatment, remain unanswered. Symptomatic treatment is essential, both of the sake of patients and those who attend them. Specific treatment is more controversial. If specific treatment is warranted, ergoloid mesylates might be a reasonable first-choice. A number of experimental approaches aimed at enhancing deficient neurotransmission, or remedying deficient neuropeptides, are currently being investigated. Meanwhile, it is realistic to attempt to do the best one can for the afflicted patients.

Alzheimer Disease↗
PubMed1994

Overview of clinical trials of hydergine in dementia.

OBJECTIVE: To assess the overall effect of Hydergine (a combination drug called ergoloid mesylates) on patients with possible dementia and to investigate potential moderators of an effect. DATA SOURCES: MEDLINE, EMBASE, and two proprietary databases were searched for reports of clinical trials. STUDY SELECTION: Included were randomized, placebo-controlled, double-blind, parallel-group trials in subjects with symptoms consistent with dementia performed with specified outcome instruments and sufficient statistical information to calculate effect sizes. Forty-seven (31%) of 151 trials reviewed met selection criteria. DATA EXTRACTION: Potential moderating variables were extracted from each trial: sample size, inpatient-outpatient status, trial duration, age, gender, medication dose, publication year, and diagnostic grouping. Outcome measures were extracted with their associated statistics. DATA SYNTHESIS: The overall combined treatment effects ("adjusted d") for three types of outcome measures were calculated. Overall, Hydergine was more effective than placebo as assessed by comprehensive ratings (d = 0.47; 95% confidence interval [CI], 0.38 to 0.56; P = .0001), clinical global ratings (d = 0.56; 95% CI, 0.44 to 0.68; P = .0001), and combined neuropsychological measures (d = 0.27; 95% CI, 0.22 to 0.32; P = .0001). Inpatient status, daily doses of 4 mg or more, and vascular dementia were generally associated with larger effects. The effect in patients with possible Alzheimer's dementia was significant only for combined neuropsychological measures in five trials (d = 0.30; 95% CI, 0.16 to 0.44; P = .0001; and with a dose-response, P = .001). CONCLUSIONS: Overall, ergoloid mesylates were more effective than placebo. However, the effect in patients with possible Alzheimer's dementia was very modest at best. The dose-response relation suggests that potentially effective doses may be higher than the currently approved. The circumstances of the efficacy of Hydergine remain inadequately defined.

Alzheimer Disease↗
PubMed1990

Lack of efficacy of hydergine in patients with Alzheimer's disease.

BACKGROUND: There is no effective pharmacologic treatment for Alzheimer's disease, the most common dementing illness in the United States. Hydergine, a combination of ergoloid mesylates, is the only approved medication for Alzheimer's disease, but despite widespread use its efficacy remains to be established. We conducted a clinical trial of Hydergine-LC, a newer preparation of ergoloid mesylates in the form of a liquid in a capsule (LC) that may have greater bioavailability, to determine its value in patients with Alzheimer's disease. METHODS AND RESULTS: Eighty older adults with probable Alzheimer's disease participated in this double-blind, placebo-controlled trial of Hydergine-LC for 24 weeks. The recommended dose of 1 mg orally three times daily was used. Cognition and behavior were evaluated before and after the trial, and the patients were monitored for adverse effects. The medication was safe and well tolerated. The Hydergine-LC group did not perform better after treatment than the placebo group on any test, and its performance was worse (P less than 0.01 and P less than 0.02, respectively) on one cognitive measure (Wechsler Adult Intelligence Scale Digit Symbol Substitution Task) and on one behavioral scale (the Geriatric Evaluation by Relatives Rating Instrument). CONCLUSIONS: Hydergine-LC appears to be ineffective as a treatment for Alzheimer's disease.

Aged↗