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Biomedical subjects

F Fraschini

Publications and source records attributed to F Fraschini.

At least 73 records · Page 4Linked to original sources

Effects of lincomycin on the immune system.

The effects of lincomycin on the immune system were studied on patients suffering from chronic bronchitis by means of phagocytosis, chemotaxis and natural-killer tests. The tests were performed before and 2, 4, 8, 12 and 24 h after administration of 600 mg lincomycin i.m. in a single dose. The results indicate that lincomycin stimulates phagocytosis, expressed as enhanced superoxide production (O2-), chemotaxis and the activity of natural killer cells, measured on the basis of their ability to perform a lysis on the K562 tumoral target labelled with 51Cr. The stimulating effects on chemotaxis appear already 2 h after the administration of the drug, while the same effect on phagocytosis and natural-killer activity occurs after 4 h. The maximal stimulating activity on all three parameters can be shown at 8 h and disappears at 24 h.

Adult

Multiple-dose pharmacokinetics in serum and sputum of sagamicin administered intramuscularly to patients.

Sagamicin is an aminoglycosidic antibiotic produced by Micromonospora sagamiensis, chemically related with gentamicin. Single- and multiple-dose pharmacokinetics have been investigated in patients affected by bronchopulmonary infections treated with 60 mg sagamicin i.m. every 12 h. The two concentration-time curves for sputum and serum are parallel; while there is no evidence of accumulation in the serum at the 7th day of treatment, sagamicin concentrations in the sputum are significantly higher on the 7th day, and this is also confirmed by a remarkable difference between the two AUC values. The good penetration power of sagamicin into sputum makes this antibiotic useful for the treatment of infections of the respiratory tract.

Aged

Kinetics of cefatrizine penetration into gynaecological tissues after oral administration.

Twenty-four patients, hospitalized in order to undergo radical gynaecological surgery, were orally administered cefatrizine in a single dose of 1 g at different times before surgery. The tissue levels determined in the organs considered (uterus, ovary, tubae, vagina) proved that cefatrizine possesses good absorption in the genital tract, reaching concentrations near to the MICs of most gram-negative and gram-positive sensitive bacteria lasting even 12 h after administration.

Administration, Oral

Pharmacokinetics of cinoxacin in elderly patients following repeated oral administration.

Cinoxacin is an antibacterial drug belonging to the quinolone class used in the treatment of urinary tract infections due to common gram-negative pathogens. Considering the high frequency of urinary tract infections in elderly people where aging represents a physiopathological condition frequently requiring an adjustment of the dosage regimen, the pharmacokinetic behaviour of cinoxacin (500 mg/12 h) in aged patients was investigated to find out if age-dependent differences may be established. The main differences detected were a shift to 4 h of the Tmax and a partly reduced clearance in comparison with data referred to younger people. On the other hand the findings showed that no accumulation occurred. High urinary concentrations of cinoxacin, exceeding the MICs for most urinary tract pathogens were found up to the 12th hour after administration.

Administration, Oral

Comparison between sulbenicillin and piperacillin levels in serum and in bronchial secretions--a pharmacokinetic study.

In order to assess pharmacokinetic differences between sulbenicillin (S) and piperacillin (P), two penicillin derivatives, 24 in-patients, 12 males and 12 females mean age 59.4 years, suffering from recurrent bronchial infections were enrolled. Patients were randomly allocated to S (12 patients) and to P (12 patients) and were given 2 g i.m. every 12 h of the awarded antibiotic, for a 7-day period. At the first and 7th day blood samples (0.25, 0.5, 1, 2, 4, 6, 8 and 12 h after dosing) as well as sputum samples (1, 2, 4, 8, 12 h after dosing) and urine samples (3, 6, 9 and 12 h after dosing) were collected, and the levels of S or P were determined by bacillus subtilis test. The pharmacokinetic analysis was performed by a standard program. On day 1 and 7 the mean peak serum concentration occurred at the first hour for S (39.9 +/- 5.2; 40.9 +/- 5.1 mcg/ml, respectively) and for P (32.2 +/- 5.4; 33.1 +/- 5.4 mcg/ml, respectively). Serum AUC0-12 and AUC0-00 (mg/l.h) levels of S were significantly higher (p less than 0.01 or less) than those of P on day 1 and 7. Similarly MRT (8 h) and Cmax (mg/l) where higher but only on day 7. Sputum AUC0-12 (mg/l.h) level of S was significantly higher (p less than 0.05) than that of P on day 1 and 7. In conclusion serum and sputum S appear to have a different pharmacokinetic profile in respect to P. However, when compared to the AUC, both drugs reach antibacterial levels.

Aged

Distribution of ceftriaxone in the tissues of the female genital system.

Twenty-nine patients, hospitalized in order to undergo gynaecological surgery involving organ removal, were treated with a single intramuscular administration of 1 g ceftriaxone before surgery. The tissue levels of the drug determined in the organs considered: uterus, ovary, fallopian tubes, vagina, proved to be comparable and to guarantee its satisfactory and uniform penetration into the tissues of the female genital system at a slowly decreasing rate. The high levels observed 12 h and 24 h after administration (2.24 +/- 0.74 mcg/g; 3.58 +/- 0.60 mcg/g; 0.70 +/- 0.45 mcg/g; 1.20 +/- 0.57 mcg/g in the ovaries and myometrium respectively) suggest a possible application of ceftriaxone in presurgical prophylaxis also in cases of female genital surgery.

Adolescent

Some aspects of "deep lung" cellular immunity in chronic bronchitis before and after therapy with tiopronin.

Fifteen patients suffering from obstructive chronic bronchopneumonia in a clinical steady-state phase received 0.6 g of tiopronin once a day during 10 days per os. The lymphocyte subsets (OKT3, OKT4 and OKT8) have been identified in peripheral blood and in bronchoalveolar lavage liquid (BAL) before and after treatment and phagocytosis has been evaluated in pulmonary alveolar macrophages (PAM) (phagocytosis index, phagocytosis percentage, superoxide-ion production). A highly significant improvement in the phagocytosis process has been observed in the PAM, as well as an increase in the number of lymphocytes T3 and in the T4/T8 ratio (due to an increase in T4 lymphocytes) in the BAL; while in peripheral blood T3 and T4 lymphocytes and the T4/T8 ratio only showed a nonsignificant increase after treatment. The possible mechanisms on which these variations are based have been investigated.

Aged

Study on pulmonary, prostatic and renal (medulla and cortex) distribution of sagamicin at different time intervals.

In order to assess the therapeutic activity of an antibiotic, not only its serum kinetics but also its kinetics in the peripheral tissues must be determined, thus evaluating the specific power of penetration of the drug. Sagamicin is an aminoglycosidic basic antibiotic closely related to gentamicin and its penetration rate into lungs, kidney and prostate, together with its serum concentrations time-course, were investigated. The findings obtained showed that this antibiotic attained a good distribution in the peripheral tissues, where it easily reached therapeutic levels.

Aminoglycosides

Ciprofloxacin: multiple-dose pharmacokinetic and clinical results in patients with hypercrinic bronchopulmonary diseases.

Ciprofloxacin, a 4-quinolone derivative with a wider spectrum of activity as compared to classic quinolones employed in the therapy of urinary tract infections, was studied in view of its possible application in the therapy of bronchopulmonary infections. An oral dose of 500 mg every 12 h was administered and both the clinical response and the pharmacokinetic profile were investigated. A complete recovery was reached in 87.5% of patients and an improvement in 12.5%; no failure was recorded. A very good penetration in sputum was confirmed by the sputum/serum area under curve ratio, providing evidence for a high bioavailability in bronchial secretion. Lung tissue concentrations confirmed the good peripheral distribution of ciprofloxacin. A twelve-hour administration schedule allows high peripheral concentrations to be obtained superior or equal to the minimum inhibitory concentrations for many pathogens.

Adult

Eseroline depresses the responses of dorsal horn neurons to C-fiber afferents in the spinal rat.

Eseroline not only has some structural features in common with morphine but also has a specific antinociceptive action like opioid drugs. The effects of eseroline on the responses of rat dorsal horn lamina V neurons to C-fiber-related noxious stimuli were investigated. The data obtained showed that 15 min after eseroline administration, the neuronal responses to C-fiber-related afferents were almost totally suppressed. Morphine was used as reference drug. The postulated action of eseroline on opioid receptors was confirmed by reversal of eseroline-driven cell activity after naloxone injection.

Action Potentials

A clinical study on the relationship between the pineal gland and the opioid system.

Recent reports point to a link between the pineal gland and the opioid system. In order to investigate this relationship, two separate studies were performed on humans. Beta-endorphin plasma levels were determined after melatonin administration (0.2 mg/kg b.w. i.m. at 2 p.m.). Melatonin serum values were evaluated after administration of FK 33-824, a met-enkephalin analogue (0.3 mg i.v. infusion at 9 a.m.). A significant decrease of beta-endorphin plasma levels was observed 120 minutes after melatonin injection. Melatonin release was stimulated by FK 33-824, with a peak at 30 minutes. The present results provide evidence of the inhibitory effect of melatonin on beta-endorphin secretion and the stimulatory action of the opioid peptides on the pineal gland. However, further studies will be required to clarify the relationship between the opioid system and the pineal gland.

Adolescent

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