Intrinsic absolute bioavailability prediction in rats based on in situ absorption rate constants and/or in vitro partition coefficients: 6-fluoroquinolones.

A preliminary study attempting to predict the intrinsic absolute bioavailability of a group of antibacterial 6-fluoroquinolones-including true and imperfect homologues as well as heterologues-was carried out. The intrinsic absolute bioavailability of the test compounds, F, was assessed on permanently cannulated conscious rats by comparing the trapezoidal normalized areas under the plasma concentration-time curves obtained by intravenous and oral routes (n = 8-12). The high-performance liquid chromatography analytical methods used for plasma samples are described.

[Expression of oncogenes (c-myc-neu) and prolactin receptor (PRLr) in tissues of women with endometriosis].

Endometriosis is a disease of unknown ethology; there are several theories that are unproven. It is known that women with such disease present with infertility, and that recurrence is very high, and apparently not depending of estrogenic stimulus. This phenomenon has been contributed to other growth factors and some oncogens.

[Reduced neuronal nitric oxide synthetase and c-protein kinase levels in Alzheimer's disease].

Introduction: Alzheimer's disease is characterized by a general and progressive dementia and by the presence of beta-amiloide deposits.

Objective: The levels of neuronal nitric oxide synthase (NOS) and protein kinase C (PKC), and the relationship between these proteins, the free-radical theory and the high level of beta-amiloide in Alzheimer's disease, have been studied.

Material And Methods: The study has been performed in samples of Alzheimer's disease (superior, medial and inferior regions of temporalis gyrus) from control individuals and patients.

Preliminary vocal repertoire and vocal communication of wild bonobos (Pan paniscus) at Lilungu (Democratic Republic of Congo).

Vocal communication in bonobos, Pan paniscus, has been studied mainly in captive groups. The few studies carried out in the wild are on only specific aspects of their behaviour. The aim of this study is to give a preliminary description of the vocal repertoire and a qualitative account of the contextual use of the vocalizations described.

Pharmacokinetics, bioavailability and absorption of flumequine in the rat.

The study demonstrates that the oral extent of bioavailability of flumequine in the rat, relative to the intravenous injection, is complete (0.94 +/- 0.04) and not significantly different from that found by the intraduodenal route (0.

[Effect of antiinflammatory agents on the accumulation of ofloxacin in human polymorphonuclear leukocytes].

The uptake of quinolones is a recently defined pharmacokinetic parameter which is increasing in importance in clinical practice, especially for immunocompromised patients whose polymorphonuclear leukocytes (PMNLs) have their bactericidal systems impaired, or in infections due to bacteria able to survive in the phagocytes. In both situations, antibiotics able to penetrate and be active in the phagocytes are required. The simultaneous administration of an antibiotic and an antiinflammatory drug is frequent, and previous studies have described interactions between the intracellular activity of the quinolones and the presence of phenylbutazone.

Effects of ethanol on intestinal absorption of drugs: in situ studies with ciprofloxacin analogs in acute and chronic alcohol-fed rats.

Background: Previous work from our laboratory on the effect, in rats, of chronic ethanol intake on the intestinal absorption of ciprofloxacin analogs suggested an increased polarity of the lipoidal membrane constituents without effects on the aqueous environment. The aim of the present study was to investigate the influence of acute ethanol intake on the absorption of the same series of compounds.

Methods: The effects of in situ ethanol exposure on intestinal absorption were determined in rats fed either a standard liquid diet or a 5% (w/v) ethanol-containing liquid diet.

Validation of a biophysical drug absorption model by the PATQSAR system.

Absorption rate constants (in situ rat gut technique) and in vitro antibacterial activities of twenty fluoroquinolones have been evaluated. A biophysical model that relates the absorption of the compounds with their lipophilicity was fitted. The model considers the absorption process from the intestinal lumen as the sum of two resistances in series: aqueous diffusional barrier and lipoidal membrane.

Expression of IkappaBalpha in the nucleus of human peripheral blood T lymphocytes.

According to current models the inhibitory capacity of I(kappa)B(alpha) would be mediated through the retention of Rel/NF-kappaB proteins in the cytosol. However, I(kappa)B(alpha) has also been detected in the nucleus of cell lines and when overexpressed by transient transfection. To gain better insight into the potential role of nuclear I(kappa)B(alpha) in a physiological context we have analysed its presence in the nucleus of human peripheral blood T lymphocytes (PBL).

[Sensitivity of group A beta-hemolytic Streptococcus isolated from pediatric pharyngotonsillitis to erythromycin and clarithromycin: a primary care multicenter study].

Background: The recent increase in the prevalence of macrolide-resistant group A beta-haemolytic Streptococcus (BHSGA) strains reported in some areas in Spain and several neighboring countries underscores the need to perform a periodic surveillance, with the adequate methodology, of the level of its susceptibility to these antimicrobials which are frequently used in our country for the treatment of acute streptococcal pharingotonsillitis and respiratory tract infections.

Patients And Methods: The susceptibility of 293 isolates of BHSGA to the macrolides erythromycin and clarithromycin was evaluated by the broth microdilution procedure recommended by the NCCLS (1997). The isolates were prospectively obtained from children with acute pharyngotonsillitis (n = 757) who were seen at primary care centers in ten Spanish cities.

[Incidence and clinical features of splenic abscesses, with special reference to tuberculous etiology in a general hospital].

Background: The aim of this revision is to know the incidence of splenic abscess (SA) in our hospital, its etiology, with special reference to tuberculosis, and clinical characteristics.

Patients And Methods: Abdominal CT-scan performed during the period 1987-1997, with the diagnosis of splenic abscess were reviewed. Etiologic diagnosis standed on blood or sputum cultures, PAAF and/or histologic study of lymph nodes.

Activation of blood T lymphocytes down-regulates CXCR4 expression and interferes with propagation of X4 HIV strains.

The chemokine receptor CXCR4 serves as a coreceptor for HIV-1 entry into CD4+ cells, in particular for strains emerging late in the infection. Cell surface expression of CXCR4 has, therefore, important implications for HIV-1 pathogenesis. Using blood lymphocytes cultured under various conditions, we studied the expression and regulation of CXCR4.

A comparative study on the efficacy of the new quinolone alatrofloxacin in the treatment of experimental legionellosis in guinea pigs.

The in vivo efficacy of trovafloxacin, intraperitoneally administered as alatrofloxacin (CP-116,517), was assessed and compared with that of erythromycin, alone or in combination with rifampicin, in a model of Legionella pneumophila pneumonia in guinea pigs. Trovafloxacin (5 mg/kg administered as alatrofloxacin once daily for 7 days) gave a survival rate of 100% in infected animals. Clearance of bacteria and of bacteria-induced lesions from lungs was achieved by day 6 post-inoculation.

Quantitative alterations of the functionally distinct subsets of CD4 and CD8 T lymphocytes in asymptomatic HIV infection: changes in the expression of CD45RO, CD45RA, CD11b, CD38, HLA-DR, and CD25 antigens.

We determined the representation in asymptomatic human immunodeficiency virus (HIV) infection of the CD45RO+ and CD45RO- CD45RA+ subsets of CD4+ and CD8+ T lymphocytes, CD11b+ and CD11b- subsets of CD8+ T cells, and activated populations of these subsets. Three-color flow cytometry was used to quantitate the different CD4+ and CD8+ T cell populations in 116 asymptomatic HIV+ individuals. In asymptomatic HIV+ infection there was a significant relative increase in the CD4+ CD45RO+ and CD8+ CD45RO+ T cell subsets, which express CD38 and DR antigens, that correlated strongly with the decline in total CD4+ T cells.

Antimicrobial susceptibility of Streptococcus pneumoniae isolated from pediatric carriers in Spain.

The in vitro activity of several beta-lactam agents, macrolides, and cotrimoxazole was investigated against 53 Streptococcus pneumoniae isolates recovered from healthy children. The rates of resistance to penicillin or amoxicillin, cefaclor, and cefuroxime were 30%, 51%, and 37%, respectively. No cefotaxime-resistant isolates were found.

[Activity of erythromycin and clarithromicin against isolates of Streptococcus pneumoniae with decreased sensitivity to penicillin obtained from healty carriers. Spanish Collaborative Group].

Background: Empirical treatment of pneumococcal upper and lower respiratory infections must be chosen on the basis of the susceptibility patterns of nasopharyngeal colonizing strains isolated from healthy carriers.

Methods: The susceptibility to erythromycin and clarithromycin was investigated by a conventional microdilution method among 103 pneumococci isolates recovered from healthy children (n = 63) and adults (n = 40) exhibiting decreased susceptibility to penicillin (MIC > or = 0.12 mg/l).

Subclinical impairment of distal renal acidification induced by low-dose cyclosporin A therapy.

Twenty-nine psoriasis patients on 5 mg/kg cyclosporin A (CyA) therapy were studied for 3 months using the furosemide test. Five of them (17%) showed an abnormal renal acidification capacity after furosemide administration: The urinary pH did not sink under 5.3 after furosemide, while the ammonium and titrable acid levels were significantly low.

Lichen planus with simultaneous involvement of the oral cavity and genitalia.

Five women with reticular and/or erosive lichen planus of the oral cavity associated with mucous involvement of the genitalia are reported. The presence of a typical lesion in one of these sites requires search for other common sites of involvement as well as manifestations of systemic diseases. Early management and careful follow-up of patients with chronic erosive and atrophic lesions of the vulva should be instituted to prevent dyspareunia.