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Biomedical subjects

A Escousse

Publications and source records attributed to A Escousse.

At least 37 records · Page 2Linked to original sources
PubMed1989

Variations of sotalol kinetics in renal insufficiency.

Decreased elimination of sotalol (160 mg) is found in patients with renal insufficiency. Simulation of plasma concentrations at steady-state exhibits moderately higher concentrations when creatinine clearance is between 10 and 30 ml/min and very high plasma concentrations when creatinine clearance is less than 10 ml/min suggesting, if treatment is absolutely necessary, monitoring in these cases and the reduction of the dose in major renal insufficiency.

Arrhythmias, Cardiac↗
PubMed1988

Inductive effects of fenofibrate and metabolism of phenobarbital.

The inductive effects of fenofibrate (FF) and phenobarbital (PB) were investigated in male Wistar rats. FF treatment produced an inductive effect on liver weight, cytochrome P450 content, and aniline hydroxylase (AH) and bilirubin UDP-glucuronosyltransferase (UDP-GT) activities in liver microsome fraction. PB and FF inductive effects were additive on liver weight but were not additive on P450 microsomal concentrations. On the contrary, FF administration decreased the inductive effect of PB on bilirubin UDP-GT activity. When FF and PB treatment were coupled, plasma and liver PB concentrations were not affected, whereas OHPB concentrations, especially in liver homogenate, were greatly decreased. Thus it can be concluded that the production of OHPB from PB was probably not accelerated, but the elimination of OHPB, the main metabolite of PB, was considerably enhanced. These results are to be compared with recent reports of structure-dependent induction of bilirubin glucuronidation by arylcarboxylic acids chemically related to clofibrate.

Animals↗
PubMed1988

[Ingestion of soybean epoxide oil. Effects on monooxygenases, epoxide hydrolase and activities of UDP glucuronosyltransferases in hepatic microsomes of the rat].

The effect of peroxidized soybean oil in the diet of male Wistar rats was studied on hepatic drug metabolizing enzymes and their phenobarbital induction and compared to that of natural soybean diet in the same conditions. No hepatomegaly or increase in serum transaminases occurred, however growth was inhibited after ingestion of peroxidized soybean oil. In addition, the protein biosynthesis of epoxide hydrase determined by immunochemistry was largely stimulated by this treatment; but the corresponding activity measured with benzo(a)pyrene 4-5 oxide as a substrate was increased in weaker proportions. This induction was limited to epoxide hydrolase only, since the enzymes of phase one were not affected and UDP glucuronosyltransferase activities toward group I substrates were randomly activated. The induction of epoxide hydrolase may affect only one or several isoforms of the membrane enzyme which are not necessarily specific to benzo(a)pyrene 4-5 oxide activity determination of the enzyme.

Animals↗
PubMed1988

[Effects of 3,5,3'-triiodo-L-thyronine on the enzymes responsible for the metabolism of xenobiotics in the rat after increase in the dietary supply of cholesterol].

A cholesterol rich diet fed to rats was found to increase the cytochrome P 450 content in hepatic microsomes. Furthermore, the variations of the same parameters promoted by 3,5,3'-triiodo-L-thyronine were strongly reduced in cholesterol supplemented rats. Cholesterol prevented the inducing effects of phenobarbital but did not oppose its decreasing effect on maximal fluorescence of ANS and PNA introduced into the microsome suspensions.

Animals↗
PubMed1988

[Influence of 3,5,3'-triiodo-L-thyronine on the hepatic enzyme activities responsible for the metabolism of xenobiotics during the development of the chick embryo].

The influence of thyroid hormones on microsomal drug metabolizing enzymes was studied in hypothyroid newborn rats and chick embryos. Administration of 3,5,3'-triiodo-L-thyronine strongly decreased the microsomal cytochrome P 450 content in hypothyroid new-born rats and thus could render the rat pup more susceptible to hepatotoxicity from drugs. The drug metabolizing system in 20 days old chick embryos was less sensitive to the effects of thyroid hormone, but administration of phenobarbital was accompanied by a strongly induction effect on microsomal enzyme activities.

7-Alkoxycoumarin O-Dealkylase↗
PubMed1987

[Effects of the ingestion of oxidized fish oils on hepatic microsomal enzyme activities and membrane fluidity in rats. Influence of tocopherol overload].

Rats fed a dietary peroxidized fish oil showed an increase in cytochrome P-450 content and ethoxy-coumarin deethylase (ECDE) activity in liver microsomes. Administration of DL-alpha-tocopherol led to different effects according to the extent of the peroxidation in the fish oil. In rats fed a de-peroxidized oil, the inductive effect of phenobarbital on UDP-glucuronosyltransferase (UDGPT) activity was depressed by tocopherol. By the same time, induction of P-450 and ECDE remained unchanged, that of epoxide hydrase slightly increased. By contrast tocopherol strongly potentiated the inductive effect of phenobarbital toward UDPGT activity (group I substrates) in rats fed the peroxidized fish oil. The modification of the inductive effect of phenobarbital in combination with tocopherol on UDPGT activities was concomitant with an increase in seric transaminase activity and with a reverse effect as revealed from the study of the rate of fluorescent probes penetration in microsomes. The possible toxicity of the strong dose of tocopherol is discussed.

Animals↗
PubMed1987

Pharmacokinetics of bupivacaine after axillary brachial plexus block.

Severe cardiovascular complications have been associated with regional anesthesia using bupivacaine. Furthermore, in our practice, axillary brachial plexus block is commonly used for surgical emergencies of the hand in out-patients. The pharmacokinetics parameters: peak height (Cmax), peak time (tmax), half life of plasma elimination (t1/2), total apparent clearance (Cl), mean time of plasma retention (t) were studied in 20 male and female patients (mean age 35 and 32 years) receiving axillary local anesthesia by bupivacaine (BU) only (A group = 100 mg), B group BU = 200 mg, or BU + lidocaine (LI) (C group = BU 100 mg + LI 200 mg), plasmatic BU and LI were simultaneously measured by HPLC method. There were no significant differences in the pharmacokinetic data observed in groups A, B and C; total apparent clearances and half times of plasma elimination of BU after brachial plexus block are similar compared to those observed after i.v. administration. Absorption of BU seems to be total while the value of Cmax are very low compared to usual neurotoxic plasma levels, but near that of plasma concentrations observed in cardiac complications. All the tmax observed were under 2 h and the dose independence of the kinetic of BU is not admissible in this study. The association of LI induce no modification of the kinetic of BU. This work concludes that in this way of administration, the absorption of BU seems to be total. Pharmacokinetics of BU is dose dependent and the association of LI induces no significant modification of BU kinetics.

Adolescent↗
PubMed1986

Urinary beta 2-microglobulin: early indicator of high dose cisdiamminedichloroplatinum nephrotoxicity? Influence of furosemide.

To evaluate the efficacy of beta 2-microglobulin as an indicator of cisplatinum nephrotoxicity, creatinine clearance and urinary beta 2-microglobulin were measured in 19 patients during 5 h after administration of a single dose of 80 mg/m2 cisplatinum. Eleven patients received furosemide as a concomitant therapy. Serum creatinine and beta 2-microglobulin remained unchanged. A decrease of creatinine clearance was observed. Urinary beta 2-microglobulin increased between 1 and 3 h after administration. This suggests transient tubular damage immediately after the treatment course. The concomitant administration of furosemide does not modify these results. However, patients who developed long-term nephrotoxicity had no early rise of urinary beta 2-microglobulin excretion; thus, it is not possible to predict cumulative nephrotoxicity by measuring beta 2-microglobulin immediately after the first course of high-dose cisplatinum.

Cisplatin↗
PubMed1986

[Effects of ingestion of oxidized fish oils on membrane fluidity, and the activity of hepatic microsome enzymes in rats. Influence of vitamin A overload].

Oxidized fish oil (OFO) feeding is followed in the rat by the increase of vitamin A plasmatic level, and modifications of microsomal membranes (decrease of fluorophore ANS fixation). This inhibit the microsomal increase of cytochrome P 450, mixed function oxidase (MFO), any UDP-glucuronosyl transferases (group I) induced by phenobarbital treatment. On the other hand, vit A over load modify the microsomal structure of the opposite way (increase of ANS fixation). This effect is enlarged when OFO is added. In this case cyt P 450 is decreased. It seems that the magnification of vit. A effect is similar to increased microsomal membrane lability by oxidized fish oil addition.

Animals↗
PubMed1985

[Local anesthetics: simultaneous HPLC determination of lidocaine (Xylocaine) and bupivacaine (Marcaine) in human serum].

In order to monitor loco-regional anaesthesia in the upper limbs with a combination of two anaesthetics, the authors participated in a clinical pharmacology study. They describe a method of simultaneous assay of bupivacaine and lignocaine by direct phase HPLC. In particular, the use of heptane sulfonic acid (counter-ion) in the mobile phase allows the elution of the local anaesthetics to be controlled. The criteria of reliability studied enable this technique to be considered for routine use.

Anesthesia, Conduction↗
PubMed1985

Model independent pharmacokinetic study of cis-dichlorodiammineplatinum (II).

The disposition of cis-dichlorodiammineplatinum (CDDP) was evaluated in 8 patients with cancer. They received 80 mg/m2 of CDDP as a 20 min i.v. infusion. Sixteen blood samples and sixteen urine samples were obtained over 6 hours following the completion of cis-platinum infusion and were assayed for total platinum by flameless atomic absorption spectrometry. There was a great variation among maxima urinary concentrations (123 to 1436 mumol . l-1) and an important decrease of diuresis appeared 3 hours after the infusion. Model independent pharmacokinetic parameters: distribution volume and renal elimination clearance were determined. The calculated distribution volumes suggest an extremely rapid diffusion of CDDP into the peripheral compartment. The ratio of total platinum clearance to creatinine clearance decreased 75 min after infusion, this being the consequence of the variation of protein binding or nephrotoxicity.

Adult↗
PubMed1983

Liver microsome phospholipids and cytochrome P.450 concentration in phenobarbital treated rats fed on different diets.

Liver microsomal concentration of cytochrome P.450 is increased in animals which are fed diets rich in polyunsaturated fatty acids. On the other hand, the effects of phenobarbital are more important when the dietary fat is more unsaturated. The unsaturation index in liver microsomal phosphatidylcholines depends on the unsaturation of the dietary fats. The treatment with phenobarbital constantly results in a decrease of the unsaturation index of fatty acids both in lecithins and cephalins. The importance of the liver microsomal cytochrome P.450 increase and the importance of the unsaturation index decrease in liver microsomal lecithins, both promoted by phenobarbital, are in good agreement.

Animals↗
PubMed1983

[Inductive effects of N-(benzoyloxy-2-ethyl)norfenfluramine (benfluorex) on hepatic microsomal enzymes in rats].

Male Wistar rate were treated with benfluorex, 50 mg/kg/p.p. daily for 7 days. The administration of benfluorex markedly increased the activity of ethoxycoumarin deethylase without increase of cytochrome P 450 levels in hepatic microsomes. The activity of bilirubin glucuronosyl transferase is so much increased with benfluorex than phenobarbital but this effects are not additive. Benfluorex alone affected the fatty acid composition of microsomal lecithins and when given with phenobarbital benfluorex modified the phenobarbital-induced changes in the fatty acid composition of microsomal lecithins. Electrophoresis of microsomal proteins showed non sensitive induction of any proteins with benfluorex.

7-Alkoxycoumarin O-Dealkylase↗
PubMed1983

[Effect of carbamate pesticides on the induction of hepatic enzymes of the rat and on the microsomal phospholipid changes].

The influence of two carbamine pesticides i.e., manebe and carbaryl upon the hepatic microsomal enzymes induction in the rat was studied. Both substances, when administered by themselves, affect only slightly liver weight, P 450 cytochrome rates and bilirubin glucuronosyltransferase, in the microsome fraction of the hepatic homogenate. It seems, however, that carbaryl is involved in producing a slight induction, whereas manebe acts inversely. Yet, manebe changes largely the induction effects of phenobarbital when associated with the latter. In the animal treated simultaneously with manebe and phenobarbital, the increase in the rate of hepatic microsomal P 450 cytochrome as well as the variations in the distribution of fatty acids in phospholipids, are significantly lower than in the animal solely treated with phenobarbital.

7-Alkoxycoumarin O-Dealkylase↗