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At least 937 records · Page 52Linked to original sources
PubMed1986

In vitro binding study of gemfibrozil to human serum proteins and erythrocytes: interactions with other drugs.

The binding of gemfibrozil to human serum, isolated proteins and erythrocytes was studied in vitro by equilibrium dialysis. Our results show that this drug is highly bound to serum (99%) at therapeutic levels. Human serum albumin was shown to be mainly responsible for this binding (98.6%) with a saturable process characterized by two binding sites with a moderate affinity. Like many acidic drugs with a carboxylic acidic group, gemfibrozil showed none or negligible binding to alpha 1 acid glycoprotein, lipoproteins and gamma-globulins. The drug binding to erythrocytes is very low (0.8%). The unbound fraction in blood remains constant (0.8%) within the range of therapeutic concentrations. Moreover, interactions were studied with bilirubin and palmitic acid at pathophysiological concentrations and acenocoumarol, salicylic acid, valproic acid, furosemide, phenylbutazone, tolbutamide, warfarin and sulfamethoxazol at therapeutic concentrations. Neither endogenous compounds nor the other drugs studied altered gemfibrozil binding in serum. Likewise, the binding of warfarin to serum and to human serum albumin (600 microM) is not influenced by gemfibrozil.

Blood Proteins↗
PubMed1985

Determination of gemfibrozil in plasma by high performance liquid chromatography.

A sensitive and specific method for the determination of 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid (gemfibrozil, Gevilon) at therapeutic concentrations in plasma is described. The method is based on high performance liquid chromatography and the use of ibuprofen as internal standard. Gemfibrozil and the internal standard are extracted from acidified plasma into cyclohexane and the resulting residue is analyzed on a commercial reversed phase column with acetonitrile/water 1:1 and 0.2% phosphoric acid as mobile phase. The eluted peaks are detected by UV-absorption at 225 nm. The sensitivity is approx. 50 ng/ml plasma using a 0.5-ml sample. The applicability to pharmacokinetic studies of gemfibrozil is demonstrated.

Chromatography, High Pressure Liquid↗
PubMedDate not supplied

[Neonatal form of isovaleric acidemia. Apropos of a new case].

The case reported concerns a 18 day-old girl who was hospitalized for severe toxemia. The nauseous smell, and significant ketonuria led us to suspect a disorder in amino-acids metabolism. Diagnosis was proven by gas chromatography. With adequate diet, evolution was favourable and the child had a normal psycho-motor development.

Amino Acid Metabolism, Inborn Errors↗
PubMed1978

[Chemical modification of epsilon-NH2 groups of lysine residues in horseradish peroxidase. Accessibility of these groups to different modifying agents].

Modification of epsilon-NH2 groups of lysine residues in horseradish peroxidase by acetic, propionic, butyric, valeric and succinic anhydrides and trinitrobenzenesulfonic acid (TNBS) is carried out. All the anhydrides modify at 0 degrees C four epsilon-NH2 lysine groups, and TNBS--three groups. TNBS modifies all 6 peroxidase epsilon-NH2 groups at 40 degrees C. Possible spacing of lysine epsilon-NH2 groups in the enzyme molecule is discussed.

Anhydrides↗
PubMed1980

The treatment of hyperlipoproteinaemia with gemfibrozil compared with placebo and clofibrate.

In a single-blind study the lipid-lowering drug gemfibrozil was compared at fixed dosage of 1600 mg daily with placebo and other drugs (mainly clofibrate) over a nine month period in 33 patients with hyperlipidaemia. Two patients were withdrawn from the study because of gastrointestinal symptoms attributable to gemfibrozil. The drug significantly lowered plasma cholesterol and triglycerides compared to the placebo. The drug also significantly lowered plasma cholesterol and triglycerides compared to the placebo. The drug also significantly lowered very low density lipoprotein (VLDL) triglycerides and raised high density lipoprotein (HDL) cholesterol levels but a previously significant inverse relationship between VLDL triglyceride and HDL cholesterol on placebo disappeared with gemfibrozil treatment.

Adult↗
PubMed1977

Organic acidosis in infants.

Any child or adult who has persistent acidosis after apparently adequate treatment should be suspected of having an organic aciduria, as should any person with a large anion gap and acidosis. The possibility that some can presently be treated, makes early diagnosis urgent. Acidosis occurs in hypoperfused states, and treatment of the hypoperfusion with half- to two-thirds-strength of physiological saline with 40 mEq/1 of potassium may correct the acidosis without there being any need to use bicarbonate.

Acidosis↗
PubMed2006

Low-temperature inactivation of fecal coliforms in sludge digestion.

The goal of this research was to demonstrate the ability to achieve Class A pathogen standards in nonthermophilic acid digesters. It was proposed that the key mechanism responsible for fecal coliform inactivation was the presence of un-ionized volatile fatty acids. Lab-scale acid digesters were assembled and operated in a batch mode for 5 days at mesophilic (38 degrees C) and low-mesophilic (21 degrees C) temperatures and at different solids concentrations. The key factor recognized for successful pathogen inactivation was pH, which is also the main factor driving the shift in organic acids toward the un-ionized form. Compared to conventional mesophilic acid digestion, low-mesophilic acid digestion was effective in fecal coliform inactivation because the process maintained lower pH throughout the duration of the experiment, offered continuous release of organic acids, and showed higher concentrations of organic acids in un-ionized form, including acetate, propionate, butyrate, and valerate.

Acids↗
PubMed1980

Effect of five anti-inflammatory steroids on collagen and glycoaminoglycan synthessis in vitro.

The effect of five anti-inflammatory corticosteroids, i.e. hydrocortisone, hydrocortisone 17-butyrate, betamethasone 17-valerate, nicocortonide acetate and nicocortonide, on the synthesis of hyaluronic acid, sulphated glycosaminoglycans and collagen by cultured skin fibroblasts was studied. As inhibitors of all these parameters the steroids could be arranged in order hydrocortisone < hydrocortisone 17-butyrate < betamethasone 17-valerate, nicocortonide acetate and nicocortonide. The corticosteroid concentrations required for inhibition of hyaluronic acid were very low as compared to those required for inhibition of sulphated glycosaminoglycan and collagen synthesis.

Anti-Inflammatory Agents↗
PubMed1985

Contractile effect of short-chain fatty acids on the isolated colon of the rat.

The contractile effect of short-chain fatty acids on proximal, middle and distal segments of the rat colon was studied in vitro. A single contraction of the longitudinal muscle of the everted preparation of the middle and distal but not the proximal colon was induced by mucosal application of propionate, butyrate or valerate. Sigmoid dose-responses were observed between contraction and log dose of propionate, butyrate and valerate. The threshold concentration of short-chain fatty acids was between 0.02 and 0.04 mM. A maximal contraction was induced with 0.1 mM-propionate, butyrate and valerate. While acetate (up to 10 mM) and lactate (up to 30 mM) had no contractile effect at all. Serosal application of short-chain fatty acids was without effect, while the contractile response with up to 10 mM-propionate was abolished in both the middle and distal colon by scraping away the mucosa. Cumulative addition of short-chain fatty acids to the organ bath (without wash-out of the first dose) caused adaptation of the contractile response; thus, the effect of propionate (1 mM) was abolished by prior addition of acetate (10 mM) or lactate (30 mM) or propionate (1 mM) or butyrate (1 mM) or valerate (1 mM). The contractile effect of propionate was also inhibited by atropine (1 microM), procaine (0.4 mM) and tetrodotoxin (3 microM); was unaffected by hexamethonium (0.1 mM) and enhanced by eserine (10 nM). The results suggest that short-chain fatty acids, which are normal constituents of the colon, have the ability to stimulate colonic contractions, probably via an enteric reflex involving local sensory and cholinergic nerves.

Adaptation, Physiological↗