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Biomedical subjects

D Lamiable

Publications and source records attributed to D Lamiable.

At least 55 records · Page 3Linked to original sources
PubMed1988

Severe ethylene glycol butyl ether poisoning. Kinetics and metabolic pattern.

A case of severe poisoning with ethylene glycol butyl ether (EGBE) after massive ingestion is described. Deep coma, metabolic acidosis, hypokalaemia, haemoglobinuria, oxaluria and a transitory rise in the serum creatinine level were observed. The elimination of the various metabolites butoxyacetic acid and oxalate was assessed in urine and a metabolic pattern for EGBE is suggested.

Creatine↗
PubMed1987

Troleandomycin-triazolam interaction in healthy volunteers: pharmacokinetic and psychometric evaluation.

Seven healthy volunteers received a single oral dose of triazolam 0.25 mg after 7 days on troleandomycin 2 g/day p.o. or placebo in a double-blind cross-over study. Plasma triazolam and psychometric and memory tests (including Critical Flicker Fusion threshold, Choice Reaction Time, Digit Symbol Substitution and Self-Rating Scales) were assessed at regular intervals after the final treatment. Troleandomycin was found to prolong the psychomotor impairment and amnesia produced by triazolam. There was a significant enhancement of the AUC, the peak concentration and the delay to tmax of triazolam after 7 days treatment with troleandomycin compared to placebo. Thus, there is a pharmacokinetic interaction, and the combination of triazolam and troleandomycin should be avoided or the dose of triazolam should be adjusted. The most likely mechanism is a diminished hepatic first-pass effect, and a decrease in the apparent oral clearance of triazolam.

Adult↗
PubMed1986

[Plasma levels of clomipramine and declomipramine in patients with depression: a study of its correlation with therapeutic efficacy].

Twenty four in-patients with an endogenous or non endogenous depressive syndrome (9 and 15, respectively) were treated in hospital for 21 days with various dosages regimens of clomipramine. Plasma concentrations of clomipramine and demethylclomipramine were determined once a week in blood samples. Therapeutic effects were assessed with Hamilton Rating Scale. At day 21, optimal therapeutic effect was observed when the sum of clomipramine and demethylclomipramine plasma levels was situated between 200-400 ng/ml.

Adolescent↗
PubMed1984

Evaluation of 4-aminopyridine and 3,4-diaminopyridine penetrability into cerebrospinal fluid in anesthetized rats.

4-aminopyridine (4-AP) and 3,4-diaminopyridine (3,4-DAP) when injected intracisternally to anesthetized rats induced qualitatively similar central nervous system stimulant and convulsant effects at equimolar concentrations. Overall penetrability into cerebrospinal fluid of 4-AP is significantly higher than that of 3,4-DAP after single i.v. administration as evaluated by a high-performance liquid chromatographic determination. The present results can account for the lower central nervous system toxicity of 3,4-DAP when compared to 4-AP previously described after systemic administration.

4-Aminopyridine↗
PubMed1984

[Bone and blood levels of azlocillin after intra-arterial injection in the dog].

Pharmacokinetic values of azlocillin--a semisynthetic penicillin of the ureidopenicillin family--were determined in dogs after injection of the drug into the right femoral artery by measuring plasma concentrations in the right femoral artery and left femoral vein and tissue concentrations in ipsi- and contralateral bones. Two different doses of azlocillin were administered, one group of dogs receiving 100 mg X kg-1 by fast (1 min) bolus injection and the other group receiving 250 mg X kg-1. The drug was assayed by high performance liquid chromatography in reverse phase, which proved to be the simplest, most rapid and most sensitive method. Changes in plasma and bone tissue concentrations after intra-arterial injection were interpreted as order one kinetics with a two-compartment open model. Following the 100 mg/kg dose, concentrations versus time corresponded to the following equations: --Arterial blood (mg/l) = 7570 e-0.15 t (min) + 240 e-0.017 t --Venous blood (mg/l) = 553 e-0.13 t + 222 e-0.016 t --Bone tissue (micrograms/g) = 15 e-0.0115 t (elimination phase). Distribution and elimination constants were identical in arterial and venous blood. Distribution half-life was 5 +/- 1 min in arterial blood and biological half-life was 42 +/- 11 min. However, bioavailability was comparatively lower in veins due to higher levels in arteries during the distribution phase. Bone tissue concentrations were much lower than plasma concentrations and were identical on both sides despite high arterial levels on the ipsilateral side during the distribution phase. Bone concentrations diminished rapidly and elimination kinetic values were the same in bone and in plasma. It is concluded that bone tissue concentrations of azlocillin after intra-arterial injection are highest during the distribution phase.

Animals↗
PubMed1983

Pharmacokinetic study of two pharmaceutical preparations containing alkaloid vincamine administered orally to human subjects.

In a crossover study of six healthy volunteers the pharmacokinetics and the bioavailability of vincamine were studied after administration of two oral forms. All subjects received an oral dose of 60 mg vincamine. The plasma concentrations of the drug were determined by a specific and sensitive gas chromatographic method. In this kind of subject the drug generally follows a one-compartment kinetic model. The average value of Tmax is 1.4 +/- 0.5 h-1 with the tablets and 1 +/- 0.6 h-1 with the solution; the Cmax are, respectively, 155 +/- 82 micrograms . 1(-1) and 133 +/- 104 micrograms . 1(-1). The AUC are 443 +/- 156 micrograms . 1(-1) h with the tablets and 315 +/- 178 micrograms . 1(-1) h with the solution. The short elimination phases, 1.43 +/- 0.80 h with the tablets and 1.55 +/- 0.78 h with the solution should be taken into account during chronic administration.

Administration, Oral↗
PubMedDate not supplied

Intranuclear concentration measurements of doxorubicin in living leucocytes from patients treated for a lympho-proliferative disorder.

The accumulation of doxorubicin (DOX) in white blood cells of treated patients has been studied by quantitative microspectrofluorometry. From blood samples of treated patients, leucocyte subpopulations were separated by the gradient method. Emission fluorescence spectra from a microvolume of a single living cell nucleus were analysed in terms of spectral shape and fluorescence yield between free and DNA-bound doxorubicin. With this non-destructive analysis technique, intranuclear doxorubicin concentrations were determined within +/- 10%. Doxorubicin concentrations were measured in patients treated with bolus injection. After an accumulation of DOX in leucocytes during the first 30 min, intranuclear doxorubicin concentration did not vary significantly for 24 h, whereas its concentration in plasma decreased. Despite large differences between patients, monocytes accumulated significantly more doxorubicin than granulocytes or lymphocytes did.

Aged↗
PubMedDate not supplied

Induction and inhibition of cicletanine metabolism in cultured hepatocytes and liver microsomes from rats.

Cicletanine, a racemic furopyridine derivative synthesized as racemate, is used as an antihypertensive agent. Its two enantiomers are involved in the pharmacological effects of the drug. Cicletanine is metabolized by conjugation enzyme systems (phase II) into sulfoconjugated or glucuroconjugated enantiomers. This study reports on the use of both the induction with 3-methylcholanthrene (3-MC) or phenobarbital (PB) and inhibition with selective compounds to determine and identify UGT isoenzymes involved in the metabolism of cicletanine enantiomers. PB and 3-MC both enhanced the cicletanine enantiomer glucuronidation. These two compounds being known as inducing agents of UGT2B1 and UGTIA6 isoforms, respectively, this suggests an implication of UGT2B1 and UGT1A6 isoforms in the metabolism of the two cicletanine enantiomers: ( + )-cicletanine and ( - )-cicletanine. The use of selective compounds for inhibition study evidenced, in addition to UGT2B1 and UGT1A6 isoforms, the involvement of other UGT isoforms such as UGT1A1, UGT2B7 and UGT2B15 in cicletanine metabolism.

Animals↗
PubMedDate not supplied

The effects of 5-fluorouracil on contractility and oxygen uptake of the isolated perfused rat heart.

Clinical cardiotoxicity related to 5-fluorouracil (5-FU) simulates either myocardial ischemia or left ventricular dysfunction. In order to characterize the changes occurring in the heart following 5-FU administration, the isovolumic perfused rat heart model according to Langendorff has been used. Particular emphasis was laid on contractility and oxygen uptake. Perfusion of isolated hearts with 1 mg/L 5-FU for 80 minutes failed to show any differences in contractility and oxygen consumption in comparison with the control group. On the contrary, 5-FU pretreatment of Wistar rats (50 mg/kg I.P. for 5 consecutive days) led to a decrease in inotropism without any change in maximum relaxation rate. The most significant finding was the consistent increase in oxygen consumption throughout the 80 minutes of perfusion (p less than 0.05) associated with a decrease in the fractional extraction of oxygen. Mean coronary flow was consistently increased in the 5-FU-pretreated group. Lactate release and CK Leakage did not differ in the two groups. In the 5-FU-pretreated group the ratio of oxygen consumption to rate-pressure product remained significantly elevated throughout 80 minutes of perfusion in comparison with the control group (p less than 0.05). Inappropriately high oxygen uptake could be a reflection of cellular metabolic disturbances responsible for post-ischemic dysfunction.

Animals↗
PubMedDate not supplied

[Chronopharmacokinetics of dexamethasone in young subjects].

Dexamethasone chronopharmacokinetics was studied in six young subjects 20 to 30 years old. The randomized cross-over study consisted of evening (11.00 p.m.) or morning (08.00 a.m.) dose separated by a period of one week. After the evening administration of the drug, only Tmax (1.77 +/- 0.74 à 11.00 p.m. and 0.99 +/- 0.64 à 08.00 a.m.) and Cmax/Tmax were higher than those determined at 08.00 a.m. This difference might be related to a cyclic variation of the absorption phase of dexamethasone. Thus, in our study, the time of administration has only a weak effect on the pharmacokinetics of dexamethasone.

Adult↗
PubMedDate not supplied

[Pharmacokinetics of dexamethasone administered orally in obese patients].

Dexamethasone pharmacokinetics was studied after oral administration of two Décadron tablets in six healthy controls and in eight obese patients whose weight was at least 20% above that of the ideal body weight. The absorption (0.30 +/- 0.09 h and 0.29 +/- 0.08 h) and elimination (4.52 +/- 0.57 h and 3.71 +/- 1.05 h) half-lives were not significantly different. Maximum plasma concentrations were similar (11.95 +/- 1.00 micrograms/l and 10.93 +/- 0.94 micrograms/l) but the lag-time was significantly higher in the obese patients (0.49 +/- 0.12 h and 0.13 +/- 0.04 h). A positive correlation was observed between the AUC and the total body weight (r = 0.738, p less than 0.01). Mean predexamethasone cortisol level was significantly lower in the obese patients (189.20 +/- 52.7 micrograms/l and 256.90 +/- 58 micrograms/l). The pharmacokinetics modifications were not sufficient to explain the increased false positive frequency in the dexamethasone suppression test of the hypothalamic-pituitary-adrenal axis in obesity.

Administration, Oral↗