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Biomedical subjects

M Eandi

Publications and source records attributed to M Eandi.

At least 19 recordsLinked to original sources
PubMed1997

Preliminary pharmacokinetic study of ibuprofen enantiomers after administration of a new oral formulation (ibuprofen arginine) to healthy male volunteers.

The pharmacokinetics of ibuprofen enantiomers were investigated in a crossover study in which seven healthy male volunteers received single oral doses of 800 mg racemic ibuprofen as a soluble granular formulation (sachet) containing L-arginine (designated trade name: Spedifen), 400 mg (-)R-ibuprofen arginine or 400 mg (+)S-ibuprofen arginine. Plasma levels of both enantiomers were monitored up to 480 minutes after drug intake using an enantioselective analytical method (HPLC with ultraviolet detection) with a quantitation limit of 0.25 mg/l. Substantial inter-subject variability in the evaluated pharmacokinetic parameters was observed in the present study. After (+)S-ibuprofen arginine, the following mean pharmacokinetic parameters +/-SD were calculated for (+)S-ibuprofen: tmax 28.6 +/- 28.4 min; Cmax 36.2 +/- 7.7 mg/l; AUC 86.4 +/- 14.9 mg.h/l; t1/2 105.2 +/- 20.4 min. After (-)R-ibuprofen arginine, the following mean pharmacokinetic parameters were calculated for (+)S-ibuprofen and (-)R-ibuprofen, respectively: tmax 90.0 +/- 17.3 and 50.5 +/- 20.5 min; Cmax 9.7 +/- 3.0 and 35.3 +/- 5.0 mg/l; AUC 47.0 +/- 17.2 and 104.7 +/- 27.7 mg.h/l; t1/2 148.1 +/- 63.6 and 97.7 +/- 23.3 min. After racemic ibuprofen arginine, the following mean pharmacokinetic parameters were calculated for (+)S- and (-)R-ibuprofen, respectively: tmax 30.7 +/- 29.1 and 22.9 +/- 29.8 min; Cmax 29.9 +/- 5.6 and 25.6 +/- 4.4 mg/l; AUC 105.1 +/- 23.0 and 65.3 +/- 15.0 mg.h/l; t1/2 136.6 +/- 20.7 and 128.6 +/- 45.0 min. Tmax values of S(+)- and (-)R-ibuprofen after a single dose of 400 mg of each enantiomer did not differ significantly from the corresponding parameters obtained after a single dose of 800 mg of racemic ibuprofen arginine, indicating that the absorption rate of (-)R- and (+)S-ibuprofen is not different when the two enantiomers are administered alone or as a racemic compound. An average of 49.3 +/- 9.0% of a dose of the (-)R-ibuprofen arginine was bioinverted into its antipode during the study period (480 minutes post-dosing). The percent bioinversion during the first 30 minutes after (-)R-ibuprofen arginine intake averaged 8.1 +/- 3.9%. The mean AUC of (+)S-ibuprofen calculated after 800 mg racemic ibuprofen arginine (105.1 +/- 23.0 mg.h/l) was lower than the mean AUC value obtained by summing the AUCs of (+)S-ibuprofen after administration of 400 mg (+)S-ibuprofen arginine and 400 mg (-)R-ibuprofen arginine (133.4 +/- 26.6 mg.h/l). In conclusion, the administration of Spedifen resulted in very rapid absorption of the (+)S-isomer (eutomer) with tmax values much lower than those observed for this isomer when conventional oral solid formulations such as capsules or tablets of racemic ibuprofen are administered. This characteristic is particularly favourable in those conditions in which a very rapid analgesic effect is required.

Adult↗
PubMed1997

Pharmacoeconomic aspects of antibacterial treatment with cefotaxime.

Pharmacoeconomics is a relatively new discipline, which is becoming increasingly useful in the current climate of medical advances that continue despite limited access to healthcare resources. Pharmacoeconomics may be used as a tool, assisting healthcare decision makers to select clinically beneficial therapies and weigh clinical gain against expenditure. Cefotaxime has been shown in many studies to be a cost-effective antibiotic agent, its monetary value being augmented by its use in low dose, low frequency regimens. This cost-effectiveness, combined with a maintained broad spectrum of antibiotic activity, low propensity for selecting resistant bacterial strains and high therapeutic index, makes cefotaxime a suitable antibiotic agent in many indications involving mild-to-moderate infections by susceptible organisms.

Cefotaxime↗
PubMed1991

[Piroxicam in analgesia].

Piroxicam, a NSAID with a proved analgesic and antiphlogistic efficacy, largely used in rheumatic-orthopedic pathologies, has an antalgic action also in extra-rheumatic pathologies, such as postoperative and dental pain and primary dysmenorrhea. This is probably due both to a peripheral mechanism, at the injured site level, which is particularly widespread, and goes from prostaglandin inhibition to suppression of the synthesis of different algesiogenic substances (oxygen free radicals, lytic enzymes), and to a direct non endorphin-mediated action at central level. The data base considered in this review, concerning piroxicam in extra-rheumatic analgesia, is of about 2,500 patients, in 26 clinical studies, mostly with an experimental double-blind placebo-controlled design or vs other NSAIDs. The doses ranged from 5 to 40 mg in a single administration: the doses of 20 and 40 mg showed an immediate analgesic effect, with the onset of analgesia within 30 min./1 hour from the administration. Analgesic activity was intense, comparable or superior to that of other drugs (aspirin, codeine, other NSAIDs) and more prolonged, often lasting as long as 24 hours. Tolerability of this data base was very satisfactory and comparable to that of the placebo, incidence of side effects being negligible.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1990

[Ferroprotein succinylate: treatment of iron deficiency in obstetrics and gynecology].

Aim of this multicentric clinical trial was to evaluate the efficacy and tolerability of a new iron compound: iron proteinsuccinylate. 3,200 patients affected with iron deficiency due to obstetric or gynecologic etiology were treated with iron proteinsuccinylate, at a daily dose of 80 mg Fe3+, for at least 30 days. Iron proteinsuccinylate induced a statistically significant improvement (p less than 0.01) in mean values of hemoglobin and serum iron. The compound also caused a disappearance or improvement of subjective symptomatology (asthenia, anorexia) and of clinical conditions deriving from iron deficiency state (polypnea, cutaneous and mucous pallor). The treatment was well tolerated and caused a few slight side effects (diarrhea, epigastralgia, nausea) in 2.4% of patients.

Anemia, Hypochromic↗
PubMed1989

Pharmacokinetics, endocrine and antitumour effects of leuprolide depot (TAP-144-SR) in advanced prostatic cancer: a dose-response evaluation.

Twenty-two patients with advanced prostatic cancer and one with benign prostatic hypertrophy were given the GnRH analogue leuprolide in the form of a slow-release depot formulation by subcutaneous injection at doses of 3.75, 7.5, 15 or 30 mg. Following the first dose, drug levels were measured by a double-antibody RIA over an observation period of 5 weeks. Thereafter patients continued long-term subcutaneous treatment at the same dose every 4 weeks. Serum levels of leuprolide showed a rapid increase immediately after injection, reaching a peak proportional to dose within 3 h (range of mean values 13.1-54.5 ng/ml). Subsequently, mean drug levels declined to a plateau proportional to dose (0.49-1.99 ng/ml at 5 weeks). A significant dose-dependent increase in the area under the serum concentration-time curve from zero to 35 days (AUC0-35 days) from 541.7 to 1653.9 ng/ml.h was also noted (p less than 0.01). With all doses there was an initial rise in serum LH and FSH, followed by a rise in testosterone and dihydrotestosterone, then a sharp decrease within 3 weeks. FSH inhibition was achieved in all the 20 evaluable patients and was maintained in 17 of them (85%) over 5 weeks. Fifteen subjects (75%) had marked suppression of LH levels. In 13 of them (65%) this condition continued for the entire observation time. Castration levels of serum testosterone and dihydrotestosterone, however, were maintained in all patients for up to 5 weeks. Two of the 21 evaluable patients (10%) had a complete response; 15 a partial response (71%) and 3 stable disease (14%). No significant differences were observed in relation to dose. Clinical improvement and serum hormonal changes support this as a new and superior method of administration of leuprolide at a dose as low as 3.75 mg.

Aged↗
PubMed1989

[Clinico-pharmacologic study of a new sustained-release oral salbutamol preparation in patients with obstructive airway disease].

A new sustained release preparation of oral salbutamol (8 mg) was compared to salbutamol (8 mg) and placebo in 15 patients suffering from chronic obstructive airways disease in a randomized double-blind cross-over trial. Changes in airways resistance and amplitude of finger tremor as well as subjective assessment of side effects (tremors, unrest, palpitations) revealed a longer lasting effect following the sustained release preparation of salbutamol.

Adult↗
PubMed1988

Drug monitoring study of a product containing ferritin.

A drug monitoring study was carried out co-operatively by industry, a university department of clinical pharmacology and a randomly selected sample of general practitioners throughout Italy to collect case history and clinical data on over 10,000 patients with anaemia treated for 2 to 4 months with a preparation containing ferritin plus vitamin B12 co-enzyme and folinic acid. Analysis of the data generated, whilst confirming the effectiveness and tolerability of the study medication, highlighted the usefulness of the research methodology for describing the pattern of use of a drug widely prescribed in general medicine.

Adolescent↗
PubMed1987

Congenital deficiency of alpha-2-adrenoceptors on human platelets: description of two cases.

The biochemistry and functionality of platelets from two related subjects (mother and son) with alpha-2-adrenoceptor-deficient platelets has been evaluated. Radioligand binding experiments with the specific alpha-2-adrenergic-receptor antagonist, 3H-yohimbine, showed a drastic reduction of alpha-2-adrenoceptors in platelets from both subjects in comparison with the control values. Electron microscopy studies revealed a normal morphology and a normal number of alpha granules and dense bodies. Levels of adenine nucleotides; 5-hydroxytryptamine; B-thromboglobulin; platelet-factor-4 and thromboxane A2 production were within normal limits. Platelet aggregation and 5-hydroxytryptamine production in response to adrenalin (at concentrations up to 50 microM) were absent, whereas ADP, AA, PAF, collagen and thrombin-induced aggregation, secretion, Ca++ flux and thromboxane A2 production were normal. The inhibitory effect caused by different concentrations of prostacyclin on Ca++ flux, aggregation, secretion and thromboxane A2 production of platelet functionally lacking of alpha-2-adrenoceptor was not distinguishable from control platelets and platelets preincubated with yohimbine.

Adult↗
PubMed1985

[Cefoperazone: microbiological, kinetic and clinical studies].

In vitro cefoperazone proved more active against the tested gram-negative bacteria than either piperacillin or mezlocillin. When administered in 1 g venous bolus the antibiotic achieved high plasmatic concentrations that were still adequate after 8 hours. 33.2% was excreted by the kidneys and a considerable amount by the biliary way. Cefoperazone produced a clinical cure in 35/36 patients (97.22%). A disulfiram-like effect was noted in 18.18%.

Bacterial Infections↗
PubMed1984

[Antitubercular agents].

Author resume the most important stages of the antitubercular struggle. Then they consider the action mechanisms of single drugs, often not well known, such the action mechanism of pyrazinamide. At present, the criteria of effectiveness, tolerance, availability and economy allow to use rationally and not arbitrarily the antitubercular drugs and these criteria also assure the best therapeutic results.

Antimetabolites↗
PubMed1984

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↗
PubMed1984

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↗
PubMed1983

[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↗
PubMed1983

[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↗
PubMed1983

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↗
PubMed1983

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↗