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Biomedical subjects

E Singlas

Publications and source records attributed to E Singlas.

At least 73 records · Page 4Linked to original sources
PubMed1983

[Human pharmacokinetics of molsidomine].

Molsidomine is well absorbed by the gastro-intestinal tract and is taken up by the liver during the first passage. Its bioavailability is 60 per cent. Digestive or sublingual absorption is rapid: maximal plasma concentrations are obtained 0.5 to 1.0 hours after administration. Molsidomine is minimally bound by plasma proteins and is distributed in a volume of 1 litre/kg. The excretion is essentially extrarenal: less than 2 per cent of the administered dose is excreted in the form of unchanged molsidomine. Molsidomine is metabolized in the liver to two pharmacologically active metabolites which spontaneously and rapidly breakdown into inactive metabolites which are excreted by the kidneys. The plasma half-life of molsidomine is 1 to 2 hours: it is not modified in patients with renal failure, but it is prolonged in patients with hepatic failure. The kinetics are linear and independent of the route of administration and the dose. There is a correlation between the plasma concentration and the pharmacological effect: the minimal effective concentration is about 5 ng/ml. At the usual dose of 2 mg three times a day, there is no accumulation of the drug.

Biological Availability↗
PubMed1982

[Tissue distribution of mezlocillin (author's transl)].

Substantial amounts of mezlocillin are rapidly distributed in a wide range of tissues. After intravenous administration of doses ranging form 2 to 5 g, concentrations therapeutically active against most sensitive organisms were obtained in bone, prostate, skin, muscle and liver, as well as in wound exudates, pleural exudates, sputum and bronchial secretions. Mezlocillin did not easily cross the blood-brain barrier with normal meninges, but CSF concentrations when the meninges were inflamed. The antibiotic also crossed the placenta.

Bronchi↗
PubMed1982

Pharmacokinetics of sulfamethoxazole--trimethoprim combination during chronic peritoneal dialysis: effect of peritonitis.

The pharmacokinetics of the fixed combination trimethoprim sulfamethoxazole (TMP--SMZ), including peritoneal transfer, has been studied in patients with end-stage renal disease treated by peritoneal dialysis, intermittent in 18 cases and continuous ambulatory dialysis in 6 cases. After a single oral dose of TMP 4 mg and SMZ 20 mg per kg, peak serum levels of approximately 2.0 micrograms/ml TMP and 28 micrograms/ml SMZ were achieved at 4 hours for TMP, and at 6 hours for SMZ. The protein binding of TMP was 34.7 +/- 1.1% and its distribution volume was 2.2 +/- 0.51/kg. Total plasma clearance of TMP was 66.2 +/- 11.5 ml/min, peritoneal dialysance was 5.1 +/- 0.5 ml/min, and renal clearance was negligible. The protein binding of SMZ was 48.0 +/- 1.4% and the distribution volume was 0.55 +/- 0.071/kg. Total plasma clearance of SMZ was 26.2 +/- 5.7 ml/min, peritoneal dialysance was 1.2 +/- 0.2 ml/min, and renal clearance was negligible. The half lives of TMP and SMZ were 23.7 +/- 4.0 h and 18.1 +/- 3.5 h, respectively. The peritoneal dialysance both of TMP and SMZ after oral administration was very low. In contrast the absorption after intra-peritoneal administration is high. Peritoneal absorption was increased during peritonitis. In patients with peritonitis, the intra-peritoneal administration of TMP-SMZ resulted in an immediate high local concentration, and a serum concentration of both drugs in the therapeutic range within 6 to 12 h.

Administration, Oral↗
PubMed1982

[Plasma assay of clomipramine and demethylclomipramine by high performance liquid chromatography].

A technique for assay of clomipramine (Anafranil) and its demethylated metabolite by high performance liquid chromatography is described in this study. This technique utilizes an XoA 800 normal phase column and a quaternary solvent composed of dietylamine, water, acetonitrile, and ethanol. Plasma of patients was extracted with hexane in an alkaline medium (pH 10). The use of an internal standard seemed to improve the assay's repeatability. The simplicity and rapidity of this technique should make it a useful aid for determining optimal doses of Anafranil for patients with depression.

Chromatography, High Pressure Liquid↗
PubMed1980

[Plasma estimation of metronidazole by high performance liquid chromatography (author's transl)].

A rapid and sensitive analytic method for metronidazole (Flagyl) using high performance liquid chromatography is described; the use of a column filled with grafted silicium, lichrosorb RP 8, permits the direct injection of a plasma treated with perchloric acid and then centrifuged. The coefficients of capacity of metronidazole and of the internal standard solution were respectively 4,8 and 11,5. This technic permits one to carry out as a routine estimations of metronidazole, used in the treatment anaerobic gram negative septicemias.

Chromatography, High Pressure Liquid↗
PubMed1978

Pharmacokinetics of perhexiline maleate in anginal patients with and without peripheral neuropathy.

Perhexiline maleate (Pexid) which has been in general use in France with good results for the treatment of angina pectoris since 1973, may be associated with severe side effects including peripheral neuropathy. The present study is a comparison of the pharmacokinetics of perhexiline maleate in anginal patients with and without signs of peripheral neuropathy. Compared to the latter, those with neuropathy had higher plasma levels of perhexiline, slower hepatic metabolism and a longer plasma half-life. Thus, peripheral neuropathy associated with perhexiline maleate treatment appears to be a direct toxic effect due to accumulation of the drug. The accumulation might result either from a decreased volume of distribution secondary to a loss of body weight, possibly drug-induced, or to slow hepatic metabolism of perhexiline of genetic origin or due to hepatic disease, possibly drug-induced. The neuropathy is rarely an isolated event, as it is often associated with one or more adverse effects of perhexiline.

Aged↗
PubMed1978

[Perhexilline maleate: relationship between side-effects, plasma concentrations and rate of metabolism (author's transl)].

In three individuals (2 male and 1 female) with severe side-effects apparently related to the regular ingestion for a period of at least 5 months of perhexiline maleate, the authors studied the rate of fall in plasma levels of the drug, of its monohydroxylated metabolite, blood transaminase and glucose levels following the interruption of therapy. The relationship between these data would indicate two hypotheses which could be tested during future studies: the manner in which the body metabolises the drug would appear to vary in relation to plasma concentration and/or hepatic involvement.

Adult↗
PubMed1978

[Neurological disorders and perhexiline maleate therapy. Clinical study of 10 cases. Neuropathological, pharmacocinetic and biochemical studies (author's transl)].

Ten new cases of perhexiline induced peripheral neuropathies are reported. The authors emphasize the possible association of other neurological disorders: cerebellar symptoms in one case, complex tremor in two other cases, marked decrease of photomotor reflexes in one case and disgeusia in another one. The pharmacocinetic study of 4 cases revealed the presence of a low metabolism of the drug in one of them. Polymorphous inclusions have been seen in Schwann cell and endothelial cell cytoplasm in the three patients with electron microscopic study of the nerves. The pathological study of one case showed the demyelination of spinal cord posterior columns. In another case, who died from hepatic coma, the biochemical study of cerebral lipids revealed the low values of cerebrosides and sulfatides in cerebellum and cerebral white matter.

Cerebellar Diseases↗