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Biomedical subjects

M Eandi

Publications and source records attributed to M Eandi.

At least 37 records · Page 2Linked to original sources

Changes of lymphocyte beta-adrenergic receptors after surgical stress.

In this study the authors' purpose was to observe the effects of surgical stress on the number of lymphocyte beta-adrenergic receptors in hypertensive and normotensive subjects. It was noticed that after surgery a significant reduction occurred in the number of binding sites of lymphocytes of both hypertensive and normotensive subjects. The time course of recovery to the pre-operative values of binding sites varied between the two groups, being slower in normotensive than in hypertensive patients. This might suggest a different pattern of regulation of the beta-adrenergic receptor between hypertensive and normotensive subjects.

Adult↗

Absolute bioavailability of paracetamol after oral or rectal administration in healthy volunteers.

The absolute bioavailability of paracetamol (Tachipirina) administered in single doses orally and rectally was studied in nine healthy adult volunteers. The results of the rapid intravenous injection of 600 mg show that the kinetics of paracetamol can be represented by an open two-compartment model with introduction and elimination occurring in the central compartment. The oral administration shows an absolute bioavailability of 60-70% independent of the pharmaceutical form and gastric contents. The rectal administration shows a lower absolute bioavailability (of about 30-40%) substantially independent of dose in the range under consideration. The pharmaceutical form, food and the route of administration modify the plasma concentration-time curves of free paracetamol and of its main metabolites. A moderate inter-individual variation in the kinetics and the bioavailability was observed.

Acetaminophen↗

[Ceftriaxone, a long-acting cephalosporin. Microbiological, kinetic and clinical study].

Ceftriaxone effectively inhibited 332 out of 452 (73.45%) bacterial strains in vitro tests. 291 out of 365 (79.69%) gram negative and 41 out of 87 (47.12%) gram positive strains were inhibited. The tests showed ceftriaxone to be more effective than cephalothin, cephotaxime, cephuroxime, cephamandol and cephoxitin. Kinetic tests showed that cephtriaxone has a plasmatic half life of 7.25 hrs. 24 hours after administration of a 1000 mg venous bolus the drug was still present in the blood. Urinary elimination over a 24 hr. period amounted to means 486.8 mg (48.68%). The drug has liquor transfer capacity. 37 of the 38 patients treated showed complete clinical or clinicobacteriological cure. Improvement was noted in the 38th.

Adolescent↗

[Microbiological, kinetic and clinical study on a new cephamycin: cefotetan].

Microbiological, kinetic and clinical studies were conducted on a new cephamycin, cephotetan. In vitro the antibiotic was found to be very effective against all strains tested. It had a particularly strong action against Gram negative bacteria too. Kinetically speaking, an intravenous bolus produced a high plasmatic concentration with a half life of about 4 hours. Elimination via the kidneys was fastest in the first 3 hours after administration (49.82%) and the slowed down. 82.76% of the dose administered was excreted within 24 hours. This antibiotics is particularly indicated in cases of urinary, respiratory and biliary infections.

Adolescent↗

Pharmacokinetics of norfloxacin in healthy volunteers and patients with renal and hepatic damage.

The pharmacokinetics of norfloxacin were studied in six healthy volunteers, and three patients each with moderate renal and hepatic damage. A new specific and sensitive high performance liquid chromatography method was set up to measure plasma and urine concentrations of norfloxacin. The mean urinary concentrations after a single oral dose of 400 mg norfloxacin exceeded many times the MIC and MBC values of most of the bacterial strains responsible for urinary tract infections. Results in the patients with hepatic and renal damage indicated slight and not statistically significant differences in comparison with healthy volunteers.

Adult↗

Toxic effects of some antibiotics on rabbit kidney cells.

The cellular toxicity of some antibiotics (cephaloridine, cefazolin, cefoperazone and gentamicin) was studied in vitro using rabbit kidney cell cultures. In order to evaluate the importance of the different factors causing toxic effects, the authors studied the correlations between toxicity and antibiotic concentration and between toxicity and period of contact. The toxic effects were measured by LDH release and by neutral red uptake inhibition. In both tests, gentamicin clearly showed curvilinear dose-toxicity and time-toxicity correlation but the cephalosporins did not do so in either test. However the antibiotics tested all showed various degrees of toxicity, suggesting that their specific toxic activity on renal cells was greater than that of aspecific variables linked to pharmacokinetic behaviour.

Animals↗

[Kinetic and clinical studies on a new cephalosporin: Cefotiam].

Kinetic and clinical evaluation of cefotiam, a new cephalosporin, is reported. It was found that the drug is rapidly distributed to the tissues. Equilibrium between tissues and plasma is reached in about an hour. Some 90-91% of the dose administered is excreted in the urine, and accumulation does not occur. A clinical cure was obtained in 27 of a series of 35 patients (77.1%). Improvement was observed in 7 cases (20%). The antibiotic proved ineffective in the remaining cases (2.8%). Tolerance was excellent and there were no side-effects worthy of note.

Adult↗

Pharmacokinetics of some cephalosporins in normal and nephrectomized rabbits.

We made a pharmacokinetic study of the cephalosporins cephazolin, cephaloridine, cefoperazone, and cefuroxime in the rabbit. We computed the pharmacokinetic parameters of a two-compartment open model from the plasma concentration time curves obtained at different increasing doses. Cephazolin, cephaloridine and cefoperazone demonstrated a dose dependent kinetics since the constants of apparent rate of elimination and apparent volume of distribution varied with the doses. In order to evaluate the extra-renal of elimination, we performed pharmacokinetic analysis on the same animals after nephrectomy. While cephazolin, cephaloridine and cefuroxime were eliminated primarily through the kidneys, cefoperazone was largely eliminated by extrarenal pathways.

Animals↗

[Pharmacokinetic and clinical evaluation of cefoxitin].

An investigation conducted on healthy volunteers showed that cefoxitin quickly reaches high plasma concentrations, and is almost completely excreted via the urine within 6 hours. In a series of 21 cases treated with 2 g i.v. in 100 ml of a 5% glucose solution two or three times a day, a clinical cure was achieved in 20, and marked improvement in the remaining patient.

Bacillus subtilis↗

[Kinetic and clinical study of bacampicillin].

A mean plasma concentration curve, with peaks within the first hour and moderate individual variations, was obtained after a single administration of 800 mg of bacampicillin to 5 healthy volunteers. An adequate antibiotic transfer from the circulation to the bronchial apparatus was demonstrated. Treatment of 34 patients suffering from ampicillin-sensitive bacterial diseases permitted clinical cure of all patients, without onset of side-effects. It is concluded that bacampicillin is preferable to oral ampicillin because of its kinetic and tolerance features.

Adolescent↗

[Pharmacokinetics of intravenous rifampicin (RMP) and its clinical evaluation in purulent bacterial meningitis].

A combined kinetic and clinical study showed that rifampicin displays good tissue diffusibility, though it may have a tendency to accumulate. A liquor transfer sufficient for the bacteria most commonly responsible for meningeal inflammation was observed; 15/18 cases of purulent bacterial meningitis treated were clinically cured without sequelae, while 1 displayed considerable improvement. Two patients died from unforseen, uncontrollable complications that were not related to administration of the drug.

Adolescent↗

[Clinical study on a new cephalosporin: CGP 9000 (cefroxadine)].

CGP 9000 (cefroxadine), a new cephalosporine derived from N-acyl-3-alkoxy-7-amino-3-cefem-4-carboxylic acid for exclusively oral use, has been experimented on 67 patients, 41 adults and 20 children. CGP 9000 appeared to possess good therapeutic activity, even in low doses: its rapid absorption and moderate sero-protein bond are a guarantee of an immediate and almost total bioavailability.

Adolescent↗

Meal stimulated response of serum bile acids levels in normal and altered bile acids enterohepatic circulation.

Sequential measurement of postprandial serum levels of bile acids was carried out in ten healthy controls and in four patients with different impairment of bile acids enterohepatic circulation. An enzymathic fluormetric method was used for SBA analysis. The peak of increase above fasting baseline in normal subjects was 11.8 +/- 1.2 microM/1 (mean +/- SD). In a cholecystectomized subject no SBA peak was observed. Two patients with mild and severe liver impairment (i.e. alcoholic steatosis and Summerskill-Walshe disease during an acute attack of jaundice) had postprandial SBA increase of 20 microM/1 and 70 microM/1 respectively. In a patient affected by Crohn's disease, with proved bile acids malabsorption, a negligible postprandial SBA increase was noted (6.65 microM/1). It is concluded that meal stimulated response of SBA levels might be useful index of altered hepatobiliary and intestinal function.

Adult↗

[Effect of a new beta-blocker (CM 6805) on the action potential of guinea pig atrial fiber].

CM6804 effect has been studied about some parameters of the intracellular action potential (AP) of guinea pig autorythmic auricle. Auricle was preserved alive under Tyrode oxygenated solution at 37 degrees C. AP is measured by a fluctuating intracellular glass microelectrode. At a concentration of 5 . 10(-5) M, CM doesn't alter the resting membrane potential, it causes a small overshoot reduction, it decreases the maximum depolarization rate and the heart rate, it increases the action potential duration. Overshoot and maximum depolarization rate decrease prove that CM modifies the membrane permeability probably by a diminution of the sodium rapid inward current. CM action is similar to others aryl-oxy-propyl propanolamine like propranolol.

Action Potentials↗

[Action of some psychotropic drugs on the electrmyographic response evoked by stretches of the gastrocnemius muscle of rats submitted to stress].

Electromyographic response evoked by stretches is registered in the rat gastrocnemius muscle. Stretch is caused by the forced flection of the paw on the leg by a solenoid. Intensity of the electromyographic signal is measured by an electronic integrator. We studied the dose/effect correlation of some psycotropic drugs on the stretch reflex in stressed rats by contention: Pentobarbital, Meprobamate, Chlorpromazine, Sulpiride, Amitriptyline, D-Amphetamine. Chlorpromazine abolishes the myoelectric stretch response while Meprobamate and Amitriptyline reduce it only a little. Pentobarbital and Sulpiride produce a biphasyc effect of opposite sign: at small doses Pentobarbital increases the stretch response while Sulpiride reduces it. At high doses we can see an opposite effect. Amphetamine, at least, at all studied doses decreases the myoelectric stretch response.

Amitriptyline↗

[Effect of some psychotropic drugs on spontaneous electromyographic activity in the stressed rat].

Electromyographic registration of a skeletal muscle allows to point out not only the phasic activation but also the tonic activity which otherwise is difficult to value. We registered the spontaneous electromyographic activity of the gastrocnemius muscle in stressed rats. The intensity of the electromyographic signal is measured by electronic rectification and integration. We studied the dose-effect correlation of some neurotropic drugs: Pentobarbital, Meprobamate, Chlorpromazine, Sulpiride, Amitriptyline, D-Amphetamine. Chlorpromazine progressively reduces the spontaneous mioelectric activity until the whole abolition. At the studied doses Meprobamate doesn't reduce completely the spontaneous activity. At small doses of Pentobarbitral the spontaneous activity increases while at high doses it's abolished. At small doses Amitriptyline becomes an exciting drug while at higher doses it reduces the spontaneous mioelectric activity. Sulpiride at small doses inhibits the spontaneous activity while at high doses it seems to increase it. At all tested doses D-amphetamine remarkably increases the spontaneous mioelectric activity.

Amitriptyline↗

[Pharmacokinetics and clinical studies of a new cephalosporin: cefamandole nafate].

The results of a pharmacokinetic and clinical study of cephamandol naphate indicated that the drug quickly reaches high plasma concentration after both i.m. and i.v. bolus administration. Urinary excretion of the biologically active form is as much as 84--90% of the total dose and mostly takes place in the first 6 hr. The therapeutic response was good: clinical cure in 90%, marked improvement in 6.6%, no change in 3.3%.

Adolescent↗