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Biomedical subjects

F Borsa

Publications and source records attributed to F Borsa.

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

Comparative pharmacokinetics of tromethamine fosfomycin and calcium fosfomycin in young and elderly adults.

The pharmacokinetics of two oral forms of fosfomycin, tromethamine (trometamol) salt and calcium salt, were studied in five young (age, 29 +/- 3 [standard deviation] years) and eight elderly (age, 72 +/- 6 years) adults. The subjects received a single 40-mg/kg (body weight) (approximately equal to 3-g) calcium fosfomycin dose and a 25-mg/kg (approximately equal to 2-g) tromethamine fosfomycin dose in fosfomycin acid form. Blood and urine samples were collected for 24 h. Antibiotic concentrations in serum and urine were measured by microbiological assay. In all subjects, the peak levels of the calcium salt in serum were two- to fourfold lower than those of the tromethamine salt (6 to 7 and 18 to 22 micrograms/ml, respectively), indicating poor intestinal absorption of the calcium form. The elimination half-life of the two oral forms was about 5 h in young adults, and the half-life was only moderately longer in elderly subjects, with large individual variations: 8.28 +/- 5.51 h for tromethamine fosfomycin and 11.80 +/- 6.86 h for calcium fosfomycin. In elderly subjects, absorption of the tromethamine salt form was not modified, but the time to peak level was delayed for the calcium salt (2.58 +/- 0.54 h versus 1.41 +/- 0.67 h in young adults). Pharmacokinetic elimination of the two forms of fosfomycin was only moderately affected in elderly subjects; we observed lower urinary elimination, about 58 versus 28% of the dose in 24-h urines for the tromethamine salt and decreased renal clearance of both forms. However, the dosages of tromethamine and calcium fosfomycin need not be adjusted for elderly subjects who have endogenous creatinine clearances above 50 ml/min per 1.73 m2.

Adult↗
PubMed1987

Acquired immunodeficiency syndrome after travelling in Africa: an epidemiological study in seventeen Caucasian patients.

Seventeen Caucasian patients with acquired immunodeficiency syndrome (AIDS) contracted after long stays in Africa are reported. Central Africa was concerned in all cases. Men are particularly exposed to AIDS whatever their occupation. This study suggests that the risk of contracting AIDS in Africa is high; the transmission of the virus was related to sexual contact, particularly with prostitutes, in Africa in most of the cases. It suggests also that Caucasians who travel in Africa spread the virus throughout the world by means of their heterosexual relations.

Acquired Immunodeficiency Syndrome↗
PubMed1986

[Urinary excretion of phospholipids: index of aminoglycoside nephrotoxicity].

Aminoglycosides have a low molecular weight and bind weakly to proteins. They are easily filtered through the glomeruli, bind to phospholipid receptors located on the brush border of proximal tubule cells, and penetrate within the cells by endocytosis. Aminoglycosides decrease lysosomal A and C phospholipase and sphingomyelinase activities. This impairs the degradation of phospholipids, with formation of abnormal intralysosomal structures called myeloid bodies as a result. These myeloid bodies are gradually eliminated from the cells into the lumen of the tubule and excreted in the urine. We studied the urinary excretion of phospholipids following 1, 3, 5 and 10 days of treatment with gentamicin (3 mg/kg/day) or tobramycin (3 mg/kg/day) in patients with acute pyelonephritis. Infection-free, non-treated subjects were used as controls. Patients with a urinary tract infection treated by a quinolone made up a third group. Urinary N-acetyl-beta-D-glucosaminidase (NAG), an indicator of epithelial necrosis, was also evaluated. Results were expressed per ml urine, per mg creatinine and per 24 hours. Only the results expressed per mg creatinine appeared valid. No significant increase in serum creatinine or urinary NAG was found in patients under gentamicin. In the patients with a urinary tract infection not treated with an aminoglycoside, urinary phospholipid excretion on D1 was decreased as compared to controls (p less than 0.01). Urinary phospholipid excretion was never found to be increased in patients under aminoglycosides. No significant difference was found between males and females. Mistaken interpretations occurred if urinary excretion of phospholipids or NAG was not expressed per mg creatinine.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1984

Pharmacokinetic study of cefmenoxime (SCE 1365-CMX) in healthy adults.

Cefmenoxime pharmacokinetics were investigated in six healthy volunteers after intravenous and intramuscular administration of 0.5, 1, and 2 g. Blood and urine samples were analyzed by reversed-phase high-pressure liquid chromatography using ultraviolet detection at 275 nm. The assay is precise and linear up to 200 micrograms/ml-1, with 0.02 micrograms/ml-1 as the limit of detection. Linearity of cefmenoxime kinetics was demonstrated because the area under the plasma concentrations is proportional to studied doses. Eight hours after 1 g of cefmenoxime intramuscularly, mean plasma concentrations are, respectively, 0.6 +/- 0.1 and 0.3 +/- 0.1 microgram/ml-1. Intramuscular cefmenoxime is rapidly absorbed (Ka = 7.28 hours-1) with complete bioavailability (F = 0.99); apparent volume of distribution is 0.35 liters/kg-1 and elimination half-life 1.5 hours. The fraction of cefmenoxime excreted unchanged in the urine after intramuscular administration is 0.72, indicating a major contribution of renal clearance in total clearance. Experimental data after intramuscular administration were well fitted with a two-compartment model.

Adult↗
PubMed1984

Pharmacokinetics of ceftazidime in normal and uremic subjects.

The pharmacokinetics of ceftazidime, administered as a single intravenous dose of 15 mg/kg given in a bolus injection over 3 min, were investigated in 5 normal subjects and in 19 uremic patients. The subjects studied were divided into five groups according to values for endogenous creatinine clearance (CLCR): group I, five subjects with CLCR greater than 80 ml/min; group II, five patients with CLCR = 30 to 80 ml/min; group III, six patients with CLCR = 10 to 30 ml/min; group IV, four patients with CLCR = 2 to 10 ml/min; and group V, four anuric patients on hemodialysis. A two-compartment open model was used to calculate the pharmacokinetic parameters. In normal subjects, the mean apparent elimination half-life was 1.57 +/- 0.13 h. The central distribution volume and the apparent volume of distribution were 0.127 +/- 0.023 and 0.230 +/- 0.015 liter/kg, respectively. Of the injected dose, 83.6 +/- 3.6% was eliminated in the urine as parent drug within 24 h. The terminal half-life increased with impairment of renal function to about 25 h in severely uremic patients. Impairment of function did not significantly modify the half-life at alpha phase, central distribution volume, or apparent distribution volume. A 6- to 8-h hemodialysis procedure reduced concentrations of ceftazidime in plasma by approximately 88%, and the elimination half-life was 2.8 +/- 0.2 h. There was no evidence of accumulation of ceftazidime in four patients with severe and chronic impairment of function who received doses of 0.5 to 1.0 g every 24 h for 10 days.

Adult↗
PubMed1983

Pharmacokinetics of temocillin (BRL 17421) in subjects with normal and impaired renal function.

The pharmacokinetics of temocillin were investigated in five normal subjects and in 20 uraemic patients. Normal subjects were given single intravenous doses of 3.75, 7.5 and 15 mg/kg of temocillin and a single intramuscular dose of 7.5 mg/kg. Patients with renal impairment were given 7.5 mg/kg of the antibiotic intravenously. A three-compartment open model was used to calculate kinetic data after iv administration. Pharmacokinetic parameters of temocillin were similar both for the three iv doses and for the im dose. The terminal serum half-lives (T1/2 beta) averaged 4.75-5.88 h. The central distribution volume (Vc) and the apparent volume of distribution (Vd area) were 0.093-0.111 and 0.268-0.303 l/kg, respectively. Renal and total body clearances were within 27.4-34.1 and 40.2-47.8 ml/min/1.73 m2, respectively. 67.4-71.5% of the dose was recovered unchanged in urine over 24 h. Intramuscular dosing of 7.5 mg/kg gave a mean peak level of 26.71 mg/l at 1.67 h. In uraemic patients, similar maximum serum concentrations were found after a single 7.5 mg/kg iv dose. The terminal half-life increased according to the degree of renal failure, from 5 h in normal subjects to about 30 h in severe uraemic patients. Renal impairment did not significantly modify Vd area, fractional clearance (Cr/GFR) and non renal clearance. 65.2% of the antibiotic was removed during haemodialysis. Dosage adjustments of temocillin in uraemic patients are proposed.

Adult↗
PubMed1983

[Evaluation of the clinical activity of cefotiam (SCE 963). Multicentric study in 7 centers].

Cefotiam (SCE 963), a new, broad-spectrum, third generation cephalosporin was used in the treatment of 136 patients suffering from respiratory tract infections, urinary tract infections, septicemia, meningitis, biliary tract infections and osteoarthritis infections. Cefotiam was administered in monotherapy to 98 patients at the mean posology of two grams per day (extreme doses: 1 to 6 g). The following clinical effectiveness was noted: 83 successes and 18 failures on 101 available clinical reports. The general, biological tolerance and renal tolerance was good in all patients.

Adolescent↗
PubMed1982

[Pharmacokinetics of dibekacin in subjects with normal renal function].

The principal pharmacokinetic parameters of dibekacin were studied in five adult subjects with normal renal function after IM and IV injection of a single dose of 1 mg/kg. The results obtained showed that the pharmacokinetics of dibekacine were independent of the dose (T1/2: 2.1 h; distribution volume: 14-161; renal clearance: congruent to 70 ml/min; urinary excretion in 24 hours congruent to 80%) and very similar to those of other aminoglycosides of the deoxystreptamine group.

Adult↗
PubMed1981

[Diclofurime: a new antihypertensive agent. Effectiveness and kidney tolerance].

Diclofurime is a non-inotropic arterial vasodilator and an antagonist to calcium transport. We studied its antihypertensive effect in 16 hypertensive subjects. When given alone at an average dose of 240 mg/day, it induced an overall significant diminution of systolic and diastolic arterial pressure. Among the 16 subjects studied, diclofurime lowered arterial pressure below 150/90 mm Hg in seven, induced an improvement in arterial pressure in six, and showed no effect in three. When hypertension is not controlled with 450 mg diclofurime in 3 doses/day, it may be given in association with acebutolol. Diclofurime is well tolerated. The most troublesome side effects noted were headache, cardiac erethism, asthenia and edema in the lower limbs. These clinical signs were usually transient. Among these 32 patients side effects required interruption of treatment in three. Laboratory follow-up was made on day 78 and 180 after initiation of treatment. No significant change in results was noted. Renal function was studied in seven patients having normal renal function and in six chronic renal failure patients whose inulin clearance was about 30 ml min-I. It was observed that in the normal subject, the injection of a loading dose of 40 mg diclofurime followed by a maintenance dose of 80 mg during one hour induced a slight increase in glomerular filtration and a greater increase in renal blood flow; the filtered fraction was thus diminished. Diclofurime induced a clear and sustained increase in excretion of water and sodium chloride without modifying urinary excretion of potassium. In severe renal failure, no significant changes in glomerular filtration, renal blood flow or electrolyte excretion were observed with diclofurime.

Adult↗