Search PubMed⌕ Search

Biomedical subjects

A Eschalier

Publications and source records attributed to A Eschalier.

At least 145 records · Page 8Linked to original sources

Chronopharmacokinetic and bioequivalence studies of two formulations of trimipramine after oral administration in man.

The bioavailability of two oral formulations of trimipramine, tablets and solution, was performed in twelve healthy volunteers, in a cross-over study. Each formulation was administered in the morning after a fasted period, and in the evening after a meal, in order to evaluate the role of both administration time and food consumption on the plasma kinetic parameters, under usual therapeutic conditions. A high interindividual variability of data was found. First, the extent of bioavailability was identical for the two formulations but the rate of bioavailability seemed to be different, with the p.o. solution, being more rapidly absorbed (tmax = 1.50 h). The effect of administration time was more obvious for the solution as shown by a lower quantitative absorption as well as a delay in time to reach the maximal concentration. Regardless of formulation and administration time, the t1/2 beta was about 10 hours and the mean MRT value was 11 hours.

Administration, Oral↗

Application of HPLC with silica-phase and reversed-phase eluents for the determination of clomipramine and demethylated and 8-hydroxylated metabolites.

A rapid and efficient high-performance liquid chromatographic method using a reversed-phase eluent of methanol-water with butylamine on a silica column was developed for the separation and quantitation of clomipramine (CMI), its demethylated metabolites (desmethyl-clomipramine and didesmethyl-clomipramine [DDCMI]), and its hydroxylated metabolites (8-hydroxy-clomipramine and 8-hydroxy-desmethylclomipramine). A liquid-liquid extraction procedure, which involved an alkaline extraction with heptane-isoamyl alcohol, first from a 1-mL serum sample and then from the acidic back extract, was used. The chromatographic separation was rapid (20 min), and the ultraviolet detection (at 254 nm) was sufficiently sensitive (limit of detection, 5-10 ng/mL). Except for DDCMI, the calibration was linear (r > 0.99, n = 5), and within-day and day-to-day coefficients of variation remained less than 11%. The method was used to analyze CMI and its metabolites in the serum of depressive patients and to determine their hydroxylation and demethylation capacities.

Adult↗

Another use of silica gel and aqueous eluent for HPLC analysis of clozapine and desmethylclozapine.

A procedure that involves a high-performance liquid chromatographic system with silica-bonded columns and reversed-phase eluents was fitted from a previously described method to measure clozapine and desmethylclozapine plasma levels. Clozapine and its demethylated metabolite were extracted from alkalinized serum by a liquid-liquid extraction, separated in 10 min, then quantitated at 254 nm at a minimum concentration of 20 ng/mL. The standard curves were linear over the range of 50-3000 ng/mL (r > 0.99) both for clozapine and desmethylclozapine and the assay had good sensitivity and recovery. Intra- and interday coefficients of variation for 200 and 800 ng/mL controls were less than 11.5% for clozapine and desmethylclozapine. This simple and efficient assay was used to monitor clozapine and desmethylclozapine levels from some treatment-refractory schizophrenic patients.

Antipsychotic Agents↗

Pain and Alzheimer's disease.

Literature on pain management in Alzheimer's disease is slowly emerging and this review deals with different aspects of pain in this growing population. Clinical pain, experimental pain and assessment of pain in cognitively impaired patients are presented. Treatment of pain is also discussed. This review calls for more studies and clinical trials with a view to improve the comfort and quality of life of patients suffering from Alzheimer's disease.

Aged↗

A comparison of central and peripheral effects of cetirizine and loratadine.

In a double-blind, crossover, randomized clinical pharmacological study performed on 10 healthy volunteers, peripheral and central effects of 10 mg cetirizine and 10 and 40 mg loratadine were compared. Cetirizine (10 mg) significantly (P less than 0.001) inhibited 10 or 100 mg/ml histamine-induced weals 2 and 6 h after drug intake. Cetirizine was more potent than 10 mg loratadine after 2 and 6 h, and was even more potent than 40 mg loratadine after 6 h. Neither drug affected subjective evaluation of central effects and cetirizine was completely devoid of electro-encephalographic (EEG) changes, whereas 10 and 40 mg loratadine induced only slight and limited EEG changes.

Adult↗

A comparison of the electroencephalographic spectral modifications induced by diazepam and by hydroxyzine.

A double-blind, randomized controlled trial using an electroencephalograph computerized analysis and cartography was carried out to investigate the spectral modifications induced by diazepam and hydroxyzine. Without monitoring response to stimulation, the spectra found for diazepam and for hydroxyzine were qualitatively very similar, showing increase of the slow waves, reduction of the alpha rhythm and accentuation of the beta 1 rhythms. These traces suggested strongly that both drugs had produced a sedative, anti-anxiety effect. The intensity of the effect produced by 50 mg of hydroxyzine appeared to be less than that produced by 10 mg diazepam. After monitoring response to stimulation, the spectra were modified and the reactivity of the two drugs differed with regard to the slow delta, theta and alpha 1 frequency bands. It was possible to distinguish between the sedative and anti-anxiety effects of both diazepam and hydroxyzine. Even if the two drugs had some similar effects, the mode of action in the central nervous system was certainly different, as can be seen from the characteristics of distribution of the slow waves, their reactivity and, with regard to frequency, the fluctuation of the dominant frequency of rapid rhythms.

Adult↗

[Therapeutic drug monitoring: a challenge for biologists].

Therapeutic drug monitoring may be a precious help for the clinician especially if rigorously performed, and it is used for many drugs. The leading role of biologists in the development of new tests is strengthened by the coming-up of new drugs, the increasing demands for clinical trials to study the concentration-clinical effects of drugs and the development of pharmacogenetics. These represent stimulating challenges to optimise therapeutic drug monitoring and favour collaboration between biologists and clinicians so as to improve the care quality of the patient.

Biology↗

[Interest of the use of pindolol in the treatment of depression: review].

The principal stakes of depression treatment are to accelerate and enhance the clinical effects of antidepressant drug. The onset of antidepressant action of Serotonin (5HT) selective reuptake inhibitors (SSRIs) was attributed in part to the decrease in firing activity of serotonin neurons produced by the activation of raphe 5HT1A autoreceptors at the time of treatment initiation. Pindolol, an antagonist at somatodendritic pre-synaptic 5HT1A receptors has been investigated as a potential accelerator or potentialisator of antidepressant response. Six open label studies and 12 controlled studies were identified for revue. The first open-label pilot study was conducted by Artigas et al. They showed promising results with pindolol, both in the acceleration of antidepressant response and in improving the efficacy of antidepressant. On the basis of these results five open-label studies were conducted. The open label studies suggest that pindolol accelerate the antidepressant response of serotoninergics therapeutics. The augmentation of antidepressant response was not clearly demonstrated by these studies particularly in the treatment of refractory depression. For example, Dinan et Scott that found the addition of pindolol in association with SSRI therapy had a poor efficacy. In the twelve controlled studies, 4 tried to underscore the shortening of the onset and the augmentation of efficacy of SSRI by pindolol [Berman et al., Maes et al., Perez et al., Tome et al. ], 3 tried to underscore shortening of the onset [Bordet, Zanardi ] and 3 tried to underscore the augmentation of efficacy [Maes et al., Moreno et al., Perez et al. ]. One study tried to underscore the augmentation of efficacy of sleep deprivation by pindolol and another one the shortening of the onset of ECT. Six studies included depressive resistant patients. Three studies were carried out with fluoxetine, 1 with fluvoxamine, 3 with paroxetine, 1 with trazodone. Two -studies were investigated with several antidepressant treatments. The results of the studies indicate one acceleration of antidepressant response in 6 studies, one augmentation of efficacy in 5 studies. Two studies clearly demonstrate that pindolol may -augment and accelerate antidepressant response. Three studies did not confirm these observations. Several points can be examined. For pindolol: 3 authors have demonstrated that the effect of pindolol did not rely upon small antidepressant effect mediated by b-blockers properties, because anxiety was not predominantly improved by pindolol plus SSRI while depressive symptoms were clearly improved. On the basis of data issues from recent positron emission tomography (PET) studies, several authors suggested that the dose of pindolol used in most clinical trials (3 yen 2,5 mg day-1) might be insufficient to induce a substantial occupancy of 5-HTA receptors (Rabiner et al. It is possible that higher doses will show a more evident benefit. On the whole, pindolol seemed to be well tolerated. Adverse effects most commonly reported were increased irritability, insomnia and nausea. Pindolol had poor adverse effects in cardiovascular functions. The variation of the results of the controlled studies can be explained by different points: Firstly by difficulty to determine good criterion of resistance. The most simplistic definition of treatment resistance is the failure to achieve and sustain euthymia with adequate antidepressant treatment. Secondly by the fact that depressive patients who present antecedents of depressive illness seem to be worst responders to the association pindolol/serotoninergic antidepressant than patients suffering of first episode of depression. We observed one antecedent of depression in the group of resistant patients who were good responders to the association pindolol/antidepressant therapy. We observed three anterior episodes of depression in negatives studies of the association pindolol/antidepressant therapy. Thirdly by the fact that the failure of the antidepressant treatment at the time of earlier (or actual) episode seems to be a criterion for less responsiveness to the association of this antidepressant treatment with pindolol. In fact, the open label studies who demonstrated efficacy of the association between pindolol and serotoninergic therapy in major resistant depression were realized with new antidepressant molecule for the episode. Other controlled trials could confirm these facts. Most of the studies failed to retrace clearly the historicity of depression, and it may be interesting in future investigations to analyze the response of the association -compared to the status of the patient with the antidepressant therapy. Further perspective could be envisaged especially in the utilization of pindolol for the treatment of pathologies which are usually treated with a serotoninergic antidepressant -therapy. For example, the antagonist 5HT(1A) Way 100635 was experimented with success in animals in order to augment the efficacy of clomipramine in the treatment of chronic pain. In other respects several psychopharmacogenetics studies could be investigated to examine, for instance, the role of the 5-HT transporter and its implication in the response to pindolol and antidepressant association. In summary, pindolol accele-rates, and in some cases enhances the clinical action of antidepressant drugs. It appears that this augmentation strategy has more limited effect on treatment resistant patient but there is experimental evidence for using higher doses in future augmentation trial.

Major Depressive Disorder↗

[Salsolinol, an endogenous molecule. Possible implications in alcoholism, Parkinson's disease and pain].

Salsolinol can be formed either by condensation of dopamine with acetaldehyde, or by condensation of dopamine with pyruvic acid followed by decarboxylation. Salsolinol has a complex pharmacologic profile. Its opium-like activity may be related to alcohol dependency and to the effectiveness of naloxone during acute alcohol intoxication. Because they had noticed that alcoholism and Parkinson's disease rarely coexist, the authors undertook a study to confirm this fact and attempt to explain it by implicating salsolinol. Urinary excretion of salsolinol was found to increase following ingestion of alcohol, as well as in Parkinson patients under L-dopa treatment. The authors also found that urinary salsolinol was very low in untreated patients with Parkinson's disease. Salsolinol was detected in a number of foods and beverages. Separate assays of enantiomeres showed that the S enantiomere predominates in some foods whereas the R enantiomere is more abundant in humans. Lastly, the antinociceptive effects of salsolinol and its enantiomeres were studied in mice and antidepressant effects were evidenced using predictive tests.

Aged↗

Lack of importance of caffeine as an analgesic adjuvant of dipyrone in mice.

The analgesic effect of caffeine used alone and in combination with dipyrone and butalbital was evaluated after oral administration in mice, using two different pain tests: the hot plate test and the phenylbenzoquinone-induced writhing test. Neither caffeine (5 to 200 mg/kg) nor butalbital (10 and 20 mg/kg) (20 mg/kg was the highest dose that did not induce sleep) produced a significant antinociceptive effect, whereas dipyrone was active from 400 mg/kg in the hot plate test and from 50 mg/kg in the writhing test. The scores obtained with the combinations were not different from those of the dipyrone-treated group, except for the butalbital-dipyrone combination. Thus caffeine is not an analgesic adjuvant in mice; its presence in the combination studied appears to be justifiable only insofar as it inhibited the sedative effect of butalbital.

Aminopyrine↗

[Drugs against pain].

Explore the source record for details and available documents.

Analgesics, Opioid↗

[Drugs against pain].

Explore the source record for details and available documents.

Anti-Inflammatory Agents, Non-Steroidal↗

[Plasma concentrations of clomipramine and its desmethyl metabolite in man. Methodologic limits].

The purpose of the present work was to study the correlations between clinical response and plasma concentrations of clomipramine or desmethylclomipramine, using two different methods of dosage: radio-immunoassay and high pressure liquid chromatography, compared with mass spectrometry method. The results vary according to the method used, suggesting that methodological problems might explain, at least partly, the discrepancies observed in the literature.

Chromatography, High Pressure Liquid↗

[Dexamethasone test in cluster headache].

Cluster headache and manic depressive illness share in common similarities like: periodic symptomatology, accessibility to lithium therapy, abnormalities in circadian rhythm of cortisol. Though, in contrast to periodic depression, D.S.T. was found normal in 9 patients with cluster headache.

Cluster Headache↗