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Biomedical subjects

F Fraschini

Publications and source records attributed to F Fraschini.

At least 145 records · Page 8Linked to original sources

Depressant effects of suprofen, a new non-steroidal anti-inflammatory drug on thalamic evoked neuronal firing in arthritic rats.

The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of which is mainly antinociceptive, were compared with those of aspirin (as a reference drug) in a study of spontaneous and evoked firing of thalamic neurons (nucleus lateralis and ventrobasalis) in rats rendered arthritic by injection of Freund's adjuvant into the paw. Suprofen (3.7 mg/kg, i.v.) induced a marked decrease in the firing evoked in arthritic rats by ankle mobilization. This effect, after a rapid onset, lasted on the average for 60 min. A similar effect was obtained with aspirin, but with 54 mg/kg (i.v.) (14 times more than suprofen). With increasing doses of suprofen, it was possible to obtain an increased long-lasting inhibition of the evoked activity, with a significant dose-effect linear regression. The possibility that there are both CNS and peripheral effects of suprofen is discussed in relation to the possible role of aspirin (the reference standard for NSAIDs) in enhancing presynaptic inhibition, thus reducing the effectiveness of incoming sensory stimuli.

Animals↗

Human pharmacokinetics and distribution in various tissues of ceftriaxone.

Multiple-dose pharmacokinetics of ceftriaxone were investigated in 7 patients with bronchopneumonia using an intramuscular regimen of 1 g given every 24 h for 7 days. Serum, sputum, and urine samples were collected serially following the first dose (day 1) and last dose (day 7). Mean peak serum concentrations of ceftriaxone occurred at 2 h on both days and were 67.8 and 75.1 micrograms/ml, respectively, on day 1 and day 7. Ceftriaxone had a half-life of 6.9 h on day 1 and 7.4 h on day 7. The half-life of ceftriaxone in sputum was 5.9 and 6.6 h, respectively, on days 1 and 7. Approximately 50% of the dose of ceftriaxone was recovered in the urine within 24 h on day 1, 60% on day 7. Tissue distribution of ceftriaxone was determined in 103 patients following intramuscular administration of a single 1-gram dose at different times up to 24 h prior to surgery. High concentrations of ceftriaxone were found in lung, tonsil, middle ear mucosa, and nasal mucosa, and therapeutic levels of ceftriaxone persisted for 24 h after administration.

Ceftriaxone↗

Ceftriaxone therapy in otolaryngological and pulmonary infections.

The efficacy of ceftriaxone, 1 g given intramuscularly once daily, was evaluated in 38 patients with pneumonia (n = 11), pulmonary empyema (n = 2), bronchitis (n = 4), tonsillitis (n = 9), sinusitis (n = 7), and otitis (n = 5). Causative organisms were Streptococcus pneumoniae (n = 11), viridans type streptococcus (n = 1), Haemophilus influenzae (n = 6), group A streptococcus (n = 10), Staphylococcus aureus (n = 3), Klebsiella pneumoniae (n = 2), Pseudomonas aeruginosa (n = 1), Escherichia coli (n = 2), Proteus mirabilis (n = 1), and Proteus vulgaris (n = 1). Sterilization of infected foci was obtained in 89.4% of those treated, with clinical recovery in 86.8%. The ceftriaxone regimen was well tolerated.

Adolescent↗

Evaluation of the immunostimulating activity of erythromycin in man.

The effects of erythromycin on the immune system have been studied in healthy volunteers and patients suffering from chronic bronchopneumonial diseases, by means of the following assays: phagocytosis, natural killer activity and superoxide anion production. The tests were performed before and after oral administration of 1 g of erythromycin. The findings suggest that erythromycin enhances phagocytosis by means of increasing ingestion of microorganisms, superoxide anion (O2-) production as well as natural killer activity. Under the experimental conditions described these effects appear 4-6 h after drug intake and reach their maximum around the 8th hour.

Adult↗

Effects of cephacetrile on reproduction cycle.

The research of possible effects of cephacetrile (Celospor) on the reproductive function was carried out on two animal species, rats and rabbits. The animals were divided into experimental groups, each treated subcutaneously with different amounts of cephacetrile (50, 100 and 500 mg/kg/die), control group receiving physiological solution. Effects of the preparation on fertility and post-natal growth in rats were analyzed, and trials were performed to test perinatal toxicity and teratogenesis in rabbits. From the observation of the experimental data collected it can be assumed that cephacetrile, administered subcutaneously in the given doses--1, 2 and 10 times, respectively, higher than the maximum therapeutic dose advisable--does not alter fertility, gestation and post-natal development of term foetuses of rats and fertility and gestation of rabbits.

Animals↗

Differentiated distribution of norfloxacin in the medullary-cortical part of the kidney in man.

Norfloxacin administered orally in a single dose of 400 mg, rapidly reaches high levels in the renal tissues, and provides an effective therapeutic action against sensitive pathogen germs. Twelve hours after administration, the drug is still detectable in the renal tissue; particularly, it was evidenced a positive tropism in the medullary part of renal parenchyma, where they were found norfloxacin levels far higher than those of cortical parts.

Female↗

Use of aztreonam in patients suffering from urinary tract infections with contraindications for the use of aminoglycosides.

The clinical efficacy and safety of aztreonam were studied in 30 patients suffering from urinary tract infections caused by gram-negative bacteria. Aztreonam was given in a dose of 1 g i.m. at intervals of 12 or 24 hours. Duration of therapy was 2-8 days. Bacteria isolated in urine cultures were: Escherichia coli (60%); Proteus mirabilis (10%); Pseudomonas aeruginosa and Citrobacter sp. (7%); Proteus vulgaris, Serratia marcescens; Klebsiella pneumoniae and Pseudomonas species (3%). At completion of therapy and at follow-up all patients were bacteriologically and clinically cured. No significant side effects or toxicity were observed in all patients treated. It is concluded from these data that aztreonam is highly effective and well tolerated in patients affected either by upper or lower urinary tract infections.

Adult↗

Pharmacokinetic studies on ceftezole.

The adult volunteers were given 1 g of ceftezole as a single intramuscular dose to investigate the pharmacokinetic profile of this new cephalosporin. The peak average serum concentration, reached 2 h after injection, was 22.5 micrograms/ml, and the t1/2 beta was 1.5 h; urinary recovery was over 80% within 24 h, the majority of injected ceftezole being excreted within 3 hours.

Adult↗

Effects of melatonin on PRL secretion during different photoperiods of the day in prepubertal and pubertal healthy subjects.

The effect of melatonin on PRL secretion has not been established yet. In an attempt to establish whether PRL response to melatonin changes in relation to the photoperiods of the day and pubertal maturation, we evaluated PRL plasma levels after melatonin administration in 19 prepubertal and pubertal healthy subjects of both sexes in two different periods of the day: in the morning, when the sensitivity to melatonin is low, and in the afternoon, when the responsiveness to melatonin is higher. Melatonin was given im at a dose of 0.2 mg/kg BW PRL plasma levels were determined with double antibody RIA method. When melatonin was administered in the morning, all pubertal subjects and 7 of 9 prepubertal ones showed no significant variation of PRL levels; a significant decrease was observed in the other 2 prepubertal subjects. On the contrary, when melatonin was given in the afternoon, a significant increase in PRL plasma levels was seen in all pubertal subjects; no significant changes were found in 6 prepubertal ones, while in the other 3 a marked decrease could be observed. The results reveal that the response of PRL to melatonin depends upon the times of day of administration and on pubertal development.

Adolescent↗

Penetration of erythromycin into tonsillar tissue.

A study was carried out to investigate serum levels and tonsillar tissue penetration of erythromycin in 80 children suffering from chronic tonsillitis who had to undergo tonsillectomy. Oral erythromycin ethyl succinate (1 g twice daily) was given for the 2 days preceding surgery, the last dose scheduled for 2, 3, 4 or 6 hours before the start of the operation and the withdrawal of blood and tissue samples. The results showed that erythromycin penetrated quickly into tonsillar tissue and the levels were higher in tissue than in serum at all time points. Mean levels of erythromycin were consistently greater than the minimum inhibitory concentrations for most common Gram-positive oro-pharyngeal pathogens and H. influenzae.

Administration, Oral↗

Relative bioavailability in humans for oral tablets and solutions of lormetazepam.

A study was carried out to estimate the relative bioavailability of 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1-methyl-1, 3-dihydro-1H-1,4-benzodiazepine-2-one (lormetazepam, Minias) in humans after administration of oral tablets and solutions. Plasma concentration of the drug was measured by gaschromatography with electron capture detector. Six healthy males were each given both formulations. With the oral solution higher plasma peak concentration and a shorter peak time were observed than with tablets. Also the elimination half-life was shorter with the oral solution, while no difference was found with the AUC.

Administration, Oral↗

Flumethasone pivalate (Locorten) in the treatment of oral diseases.

The combination flumethasone pivalate + iodochlorohydroxychinoline drops was used in 40 patients, 24 males and 16 females, mean age 42.6 years, suffering from infectious enanthema (35%), periodontitis (30%), aphthous stomatitis (25%) and abscess due to prosthesis (10%). After application of 2-3 drops of the combination t.i.d. for 2-7 days, satisfactory results were obtained in all the patients. Tolerance was good; mild unwanted effects occurred in 2 patients (5.0%). Thus the combination flumethasone pivalate + iodochlorohydroxychinoline appears to be very effective in the treatment of oral diseases because its action is more rapid and stronger than that of other currently used drugs.

Abscess↗

Comparative study on the electrophysiological responses at thalamic level to different analgesic peptides.

Using electrophysiological methods to detect the extracellular activity of single neurons in the thalamus of anaesthetized rats, their response to mechanical and thermal noxious stimuli were assessed before and after administration of 4 analgesic peptides of various types. Dermophin, a peptide extracted from frog's skin, was found to have an opioid-like antinociceptive activity antagonized by naloxone. Caerulein, which has a similar origin, failed to suppress the nociceptive responses of thalamic neurons evoked by peripheral stimuli. Calcitonin, a peptide found at brain level, induced an alteration of the increased firing characteristic of noxious stimuli, and its action was not reversed by naloxone. FK 33-824, a synthetic peptide, induced a morphine-like action when injected i.c.v. at a dosage 1000 times lower than that of morphine on a molar basis. It is concluded that electrophysiological investigations on peptides endowed with analgesic activity contribute greatly to a more precise profile of the peptides as candidate drugs in pain control.

Analgesics↗

Comparison between penetration of amoxicillin combined with carbocysteine and amoxicillin alone in pathological bronchial secretions and pulmonary tissue.

Patients with chronic bronchitis were treated orally with either amoxicillin (500 mg) alone or in combination with carbocysteine (150 mg), thrice daily for five days, in order to assess whether the combination allows higher antibiotic levels to be obtained in bronchial mucus than those obtained from amoxicillin alone. Serum and mucus levels were determined for each patient at first and fifth day of the two drug regimens. The levels of amoxicillin in the lung tissue collected in patients undergoing pulmonary surgery were also determined after a single oral dose of amoxicillin (1 g) or of amoxicillin (1 g) plus carbocysteine (300 mg). In the bronchial secretions, at the same plasma concentrations, amoxicillin levels were statistically higher after administration of combined substances. These findings indicate the presence of a pharmacokinetic synergism between these compounds, which allows amoxicillin to penetrate more easily through the hemato-bronchial barrier. The association of amoxicillin and carbocysteine, determining an increase of the quantitative levels of antibiotic in the bronchial secretion (also if it is purulent), performs a sterilizing action in a short time with significant therapeutic advantages.

Aged↗

Dermorphin, a new peptide from amphibian skin, inhibits the nociceptive thalamic neurons firing rate evoked by noxious stimuli.

Dermorphin is the representative of a new class of potent opioid peptides occurring in amphibian skin and possesses the unique feature of having a D-Ala residue incorporated in the peptide molecule. The effect of dermorphin on the spontaneous and evoked neuronal activity by a nociceptive stimulus was studied in the nucleus lateralis anterior and ventrobasal complex of the rat thalamus. The high firing frequency induced by nociceptive stimuli was blocked when dermorphin was injected intraperitoneally at the dose of 1.5 mg/kg. The action starts about 10 min after injection and lasts on average for 120 min. Naloxone, a specific opioid antagonist, injected i.p. at a dose of 1 mg/kg antagonized the effect of dermorphin. The dermorphin time-course is about twice that of morphine (1.5 mg/kg i.p.) under the same experimental conditions.

Action Potentials↗