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1.
Arzneimittelforschung ; 44(12A): 1495-8, 1994 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-7857350

RESUMEN

A multicentre double-blind placebo-controlled study was conducted in order to assess the effects of pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6), a new synthetic biological response modifier, on the clinical picture of bacterial exacerbations of chronic bronchitis. Seven centres of respiratory diseases participated in the trial. A total of 137 patients, 103 males and 34 females (mean age: 65.0 years) were admitted to the study. The trial was subdivided into 3 phases. During the first 8-day phase (D0-D8), 68 patients received 800 mg pidotimod orally (one sachet) twice daily and an antibiotic treatment (amoxycillin plus clavulanic acid: 1 g twice daily), while 69 patients received placebo (one sachet) and antibiotic according to the same dosage schedule. In the second 7-day phase (D8-D15), while the double-blind therapy proceeded, the antibiotic treatment was stopped. The third phase (D15-D45) consisted of a 30-day follow-up period. Five clinical observations, at D0, D4, D8, D15 and D45, were scheduled. The Skin test, to evaluate immunocompetence, was carried out at D0, D15 and D45. The faster improvement of symptomatology (dyspnoea, cough, sputum, hyperpyrexia) in the patients in the pidotimod group compared with the placebo group was reflected in recovery time: mean 8.9 days in the pidotimod group versus 10.7 days in the placebo group (p < 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)


Asunto(s)
Bronquitis/complicaciones , Factores Inmunológicos/uso terapéutico , Ácido Pirrolidona Carboxílico/análogos & derivados , Infecciones del Sistema Respiratorio/complicaciones , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Tiazoles/uso terapéutico , Adulto , Anciano , Bronquitis/inmunología , Bronquitis/microbiología , Enfermedad Crónica , Método Doble Ciego , Femenino , Humanos , Factores Inmunológicos/efectos adversos , Masculino , Persona de Mediana Edad , Ácido Pirrolidona Carboxílico/efectos adversos , Ácido Pirrolidona Carboxílico/uso terapéutico , Recurrencia , Infecciones del Sistema Respiratorio/microbiología , Pruebas Cutáneas , Esputo/microbiología , Linfocitos T Colaboradores-Inductores/efectos de los fármacos , Linfocitos T Colaboradores-Inductores/inmunología , Linfocitos T Reguladores/efectos de los fármacos , Linfocitos T Reguladores/inmunología , Tiazoles/efectos adversos , Tiazolidinas
2.
Arzneimittelforschung ; 44(12A): 1499-502, 1994 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-7857351

RESUMEN

The efficacy and safety of pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl)carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6), a new oral synthetic immunostimulating agent, were investigated in a multicentre study, performed in 10 university and hospital centres of pneumophthisiology and respiratory physiopathology, according to a double-blind vs. placebo experimental design. Primary objective of the investigation was to verify the efficacy of pidotimod against infectious exacerbations in patients affected with chronic bronchitis. 181 inpatients or outpatients (117 male, 64 female; mean age: 62.5 years), affected with chronic bronchitis, were enrolled in the study. Pidotimod 800 mg/die or placebo sachets were administered by oral route for 60 consecutive days, followed by a 60-day follow-up period. Clinical observations were performed at baseline (D 0), after 30 (D 30) and 60 (D 60) days of treatment, as well as at the end of the follow-up (D 120). Time and frequency of infectious relapses were considered as the target variable for the evaluation of the efficacy of the drug. Clinical picture, expectoration characteristics, spirometric parameters and laboratory tests were monitored to evaluate patients' conditions. The results indicate that pidotimod is significantly more effective than placebo against infectious relapses in patients suffering from chronic bronchitis. During the first month, 9% of patients treated with pidotimod were affected with an infectious relapse vs. 39.5% of patients treated with placebo (chi 2, p < 0.001). In the second month, infectious episodes were reported by 1.2% of patients treated with the drug vs. 46.1% of patients treated with placebo (chi 2, p < 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)


Asunto(s)
Infecciones Bacterianas/tratamiento farmacológico , Bronquitis/tratamiento farmacológico , Factores Inmunológicos/uso terapéutico , Ácido Pirrolidona Carboxílico/análogos & derivados , Tiazoles/uso terapéutico , Adulto , Anciano , Anciano de 80 o más Años , Infecciones Bacterianas/complicaciones , Infecciones Bacterianas/microbiología , Bronquitis/complicaciones , Bronquitis/microbiología , Enfermedad Crónica , Método Doble Ciego , Femenino , Estudios de Seguimiento , Humanos , Masculino , Persona de Mediana Edad , Ácido Pirrolidona Carboxílico/uso terapéutico , Pruebas de Función Respiratoria , Tiazolidinas
3.
J Int Med Res ; 18(2): 164-70, 1990.
Artículo en Inglés | MEDLINE | ID: mdl-2140330

RESUMEN

The efficacy and safety of 500 mg clarithromycin and 1000 mg josamycin both given twice daily for a maximum of 14 days were compared in the treatment of 72 hospitalized patients with bacterial pneumonia. The predominant pathogens isolated were Streptococcus pneumoniae and Staphylococcus aureus. Clinical success was reported for 91.5% of patients treated with clarithromycin and for 87.0% of those treated with josamycin. Eradication of the causative pathogen was noted in 85.7% of patients receiving clarithromycin and in 90% of those receiving josamycin. Adverse events considered probably to relate to therapy were experienced by 2% of patients treated with clarithromycin and by 12.5% of those treated with josamycin; one patient treated with josamycin was withdrawn because of severe nausea and moderate vomiting. Treatment with clarithromycin at half the dosage of josamycin was found to have comparable efficacy and to be associated with a lower incidence of adverse events.


Asunto(s)
Infecciones Bacterianas/tratamiento farmacológico , Eritromicina/análogos & derivados , Josamicina/uso terapéutico , Neumonía/tratamiento farmacológico , Adolescente , Adulto , Factores de Edad , Anciano , Anciano de 80 o más Años , Claritromicina , Tos/tratamiento farmacológico , Disnea/tratamiento farmacológico , Eritromicina/efectos adversos , Eritromicina/uso terapéutico , Femenino , Humanos , Josamicina/efectos adversos , Masculino , Persona de Mediana Edad , Ruidos Respiratorios/efectos de los fármacos , Infecciones Estafilocócicas/tratamiento farmacológico , Streptococcus pneumoniae/efectos de los fármacos
4.
Respiration ; 57(1): 28-36, 1990.
Artículo en Inglés | MEDLINE | ID: mdl-2359893

RESUMEN

Alveolar macrophages, lymphocyte and granulocyte percentages, together with OKT3+, OKT4+, OKT8+ lymphocyte subsets and OKT4+/OKT8+ ratio, were evaluated in bronchoalveolar lavage (BAL) fluid and in peripheral venous blood (PVB) of neoplastic and nonneoplastic subjects, in order to assess these aspects of immunity in neoplastic disease and to find out if the modifications in the bronchoalveolar environment are correlated to the ones in the circulation blood. BAL was performed in 30 patients undergoing fiberoptic bronchoscopy to ascertain the presence of lung cancer. Twelve of them had positive findings for epidermoid bronchogenic carcinoma, while in the remaining subjects the diagnosis was not confirmed. The 30 examined subjects were then grouped according to their smoking habit. In PVB, no significant difference was seen between neoplastic and nonneoplastic subjects, whereas in BAL the neoplastic patients showed a significant increase of lymphocytes OKT3+ and OKT8+. This tends to confirm that PVB is not a good indicator of organ immunity and may justify the reduced activity of alveolar macrophages in subjects affected by bronchogenic neoplasia. Between smokers and nonsmokers, lymphocyte subsets showed more significant differences than between neoplastic and nonneoplastic subjects (decrease of T4+ lymphocytes, increase of T8+ lymphocytes and, therefore, reduction of T4/T8 ratio); there were also scalar variations in the three groups (smokers with cancer, smokers without cancer and nonsmokers without cancer). Thus, the possible autonomous role of cigarette smoke and the presence of neoplasia in the immunity alterations of the alveolar environment with final joint effects were confirmed. These data may indicate a possible correlation between cigarette smoking, immunological alterations in BAL and the onset of bronchogenic carcinoma.


Asunto(s)
Líquido del Lavado Bronquioalveolar/inmunología , Carcinoma Broncogénico/inmunología , Carcinoma de Células Escamosas/inmunología , Neoplasias Pulmonares/inmunología , Linfocitos/inmunología , Adulto , Anciano , Antígenos de Diferenciación de Linfocitos T/análisis , Carcinoma Broncogénico/patología , Carcinoma de Células Escamosas/patología , Femenino , Granulocitos/inmunología , Granulocitos/patología , Humanos , Neoplasias Pulmonares/patología , Linfocitos/patología , Macrófagos/inmunología , Macrófagos/patología , Masculino , Persona de Mediana Edad , Alveolos Pulmonares/inmunología , Alveolos Pulmonares/patología , Fumar
5.
Respiration ; 57(4): 248-53, 1990.
Artículo en Inglés | MEDLINE | ID: mdl-2095607

RESUMEN

Four subjects working in sharpening and grinding operations of hard metal tools were examined. Only 1 worker, a 37-year-old female exposed for 7 years to hard metal dusts, developed hard metal pneumoconiosis, which rapidly progressed to death. Cytology of the bronchoalveolar lavage (BAL) showed a high number of eosinophils, more than 30% of the cell population. Biopsy of the lung revealed interstitial fibrosis with hyperplasia of the pneumocytes of the second type and inflammatory cellular infiltration of the interstitium. High tungsten (W) and tantalum concentrations were determined in the admission BAL and in the biopsy 4 months later by neutron activation analysis while cobalt (Co) levels were near to normal values. The content of Co and W in blood and urine and particularly in pubic hair and toe nails of the patients was significantly higher than the normal values. This suggests that these biological specimens could be used as indicators of chronic exposure to hard metal dusts.


Asunto(s)
Metalurgia , Exposición Profesional , Neumoconiosis/etiología , Tantalio , Tungsteno , Adulto , Líquido del Lavado Bronquioalveolar/patología , Cobalto , Femenino , Humanos , Italia/epidemiología , Masculino , Neumoconiosis/epidemiología
7.
Int J Clin Pharmacol Res ; 9(1): 43-7, 1989.
Artículo en Inglés | MEDLINE | ID: mdl-2651331

RESUMEN

The present report concerns an open clinical trial aimed to investigate the efficacy and safety of enoxacin (Zami 8401), a new quinolone drug, in bacterial infections of the lower respiratory tract. A total of 30 hospital in patients, 25 males and 5 females, of a mean age of 67 years (range 39-84 years), suffering from bronchopneumonia, or acute exacerbation of chronic bronchitis, were treated. Enoxacin was administered at the dose of 800 mg twice daily by the oral route. As a rule the patients received the drug for ten days. Efficacy was assessed on the basis of radiological, bacteriological and clinical changes. Tolerance was monitored by the daily recording of any sign or symptom possibly related with the drug as well as by laboratory tests performed before, during and after the treatment. Efficacy was excellent in 80%, good in 17%, poor in 3% of the patients. Tolerance was excellent in all except one patient. Enoxacin appears a very effective and safe drug in the treatment of the infections of the lower respiratory tract.


Asunto(s)
Bronquitis/tratamiento farmacológico , Bronconeumonía/tratamiento farmacológico , Enoxacino/uso terapéutico , Adulto , Anciano , Ensayos Clínicos como Asunto , Enoxacino/farmacología , Femenino , Humanos , Masculino , Persona de Mediana Edad
8.
Int J Clin Pharmacol Res ; 9(3): 175-82, 1989.
Artículo en Inglés | MEDLINE | ID: mdl-2744910

RESUMEN

The rheological properties of bronchial mucus samples, collected from randomly selected patients with chronic bronchitis by protected expectoration, under steady-state conditions without any exacerbation, were investigated in a double-blind multicentre study before and after five days of treatment with 4.5 g/day carbocysteine or with glucose as a placebo. Viscous and elastic properties of the mucus were measured with a rheometer fitted with coaxial cylinders set up in an oscillating instead of a rotating mode. The shapes of the ellipses obtained characterized the rheological properties of each bronchial mucus sample before and after treatment. Two different rheological patterns were observed. In the group of patients with initial viscosity greater than or equal to 10,000 mPa.s-1, carbocysteine treatment reduced viscosity and elasticity more than those of the placebo-treated patients. In the group of patients with viscosity lower than 10,000 mPa.s-1, the rheological modifications were the same for both groups. These results are discussed in terms of both the efficacy of carbocysteine and the necessity of rheological characterization of the patients before treatment into different groups, according to the rheological properties of their secretions, for better and targetted therapy with mucus modifying drugs.


Asunto(s)
Bronquitis/diagnóstico , Moco/fisiopatología , Adulto , Anciano , Bronquitis/terapia , Carbocisteína/farmacología , Elasticidad , Humanos , Persona de Mediana Edad , Reología , Viscosidad
9.
Drugs Exp Clin Res ; 14(8): 547-53, 1988.
Artículo en Inglés | MEDLINE | ID: mdl-3248508

RESUMEN

The pharmacokinetic profile of cefotetan was studied in a group of hospitalized patients. The absorption of the molecule (after a single dose of 2 g/i.m.) was good and the drug was found to diffuse satisfactorily in the lungs, prostatic tissue, kidney and in the female genitalia.


Asunto(s)
Cefotetán/farmacocinética , Adulto , Anciano , Bronquios/análisis , Cefotetán/administración & dosificación , Cefotetán/sangre , Femenino , Genitales Femeninos/análisis , Humanos , Absorción Intestinal , Riñón/análisis , Pulmón/análisis , Enfermedades Pulmonares Obstructivas/metabolismo , Masculino , Persona de Mediana Edad , Próstata/análisis , Distribución Aleatoria , Factores de Tiempo , Distribución Tisular
10.
Int J Clin Pharmacol Ther Toxicol ; 25(11): 638-42, 1987 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-3429068

RESUMEN

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.


Asunto(s)
Bronquitis/tratamiento farmacológico , Penicilina G/análogos & derivados , Piperacilina/farmacocinética , Sulbenicilina/farmacocinética , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Piperacilina/sangre , Piperacilina/uso terapéutico , Esputo/análisis , Sulbenicilina/sangre , Sulbenicilina/uso terapéutico
12.
Chemotherapy ; 33(2): 85-92, 1987.
Artículo en Inglés | MEDLINE | ID: mdl-3568801

RESUMEN

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.


Asunto(s)
Antibacterianos/metabolismo , Esputo/metabolismo , Anciano , Aminoglicósidos/administración & dosificación , Aminoglicósidos/sangre , Aminoglicósidos/metabolismo , Antibacterianos/administración & dosificación , Antibacterianos/sangre , Bronquitis/tratamiento farmacológico , Bronquitis/metabolismo , Femenino , Gentamicinas , Semivida , Humanos , Inyecciones Intramusculares , Cinética , Masculino , Persona de Mediana Edad
13.
Int J Clin Pharmacol Res ; 7(2): 129-33, 1987.
Artículo en Inglés | MEDLINE | ID: mdl-3495498

RESUMEN

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.


Asunto(s)
Aminoácidos Sulfúricos/uso terapéutico , Bronquitis/inmunología , Fagocitosis/efectos de los fármacos , Linfocitos T/efectos de los fármacos , Tiopronina/uso terapéutico , Anciano , Anticuerpos Monoclonales , Bronquitis/tratamiento farmacológico , Enfermedad Crónica , Femenino , Humanos , Macrófagos/efectos de los fármacos , Masculino , Persona de Mediana Edad , Alveolos Pulmonares/inmunología
14.
Int J Clin Pharmacol Res ; 7(1): 63-71, 1987.
Artículo en Inglés | MEDLINE | ID: mdl-3583489

RESUMEN

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.


Asunto(s)
Ciprofloxacina/metabolismo , Enfermedades Respiratorias/metabolismo , Adulto , Anciano , Bronquitis/metabolismo , Bronquitis/microbiología , Enfermedad Crónica , Ciprofloxacina/sangre , Ciprofloxacina/orina , Humanos , Cinética , Pulmón/metabolismo , Masculino , Persona de Mediana Edad , Enfermedades Respiratorias/microbiología , Esputo/microbiología
15.
Chemotherapy ; 33(5): 309-15, 1987.
Artículo en Inglés | MEDLINE | ID: mdl-3665628

RESUMEN

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.


Asunto(s)
Cinoxacino/farmacocinética , Cistitis/tratamiento farmacológico , Piridazinas/farmacocinética , Uretritis/tratamiento farmacológico , Administración Oral , Anciano , Anciano de 80 o más Años , Cinoxacino/uso terapéutico , Cistitis/orina , Femenino , Humanos , Masculino , Tasa de Depuración Metabólica , Uretritis/orina
16.
Chemotherapy ; 32(3): 192-9, 1986.
Artículo en Inglés | MEDLINE | ID: mdl-3709267

RESUMEN

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.


Asunto(s)
Ceftriaxona/metabolismo , Oído Medio/metabolismo , Sistema Respiratorio/metabolismo , Ceftriaxona/sangre , Ceftriaxona/orina , Esquema de Medicación , Oído Medio/cirugía , Humanos , Cinética , Premedicación , Sistema Respiratorio/cirugía , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Infecciones del Sistema Respiratorio/metabolismo , Esputo/metabolismo , Distribución Tisular
17.
Chemotherapy ; 32(3): 200-4, 1986.
Artículo en Inglés | MEDLINE | ID: mdl-3709268

RESUMEN

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.


Asunto(s)
Ceftriaxona/uso terapéutico , Otitis/tratamiento farmacológico , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Tonsilitis/tratamiento farmacológico , Adolescente , Adulto , Anciano , Ceftriaxona/administración & dosificación , Ceftriaxona/efectos adversos , Niño , Diarrea/inducido químicamente , Esquema de Medicación , Femenino , Humanos , Masculino , Persona de Mediana Edad
18.
Int J Clin Pharmacol Res ; 5(5): 331-40, 1985.
Artículo en Inglés | MEDLINE | ID: mdl-4066083

RESUMEN

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.


Asunto(s)
Amoxicilina/uso terapéutico , Bronquios/metabolismo , Bronquitis/tratamiento farmacológico , Carbocisteína/uso terapéutico , Cisteína/análogos & derivados , Pulmón/patología , Anciano , Amoxicilina/administración & dosificación , Bronquios/irrigación sanguínea , Bronquitis/microbiología , Bronquitis/patología , Carbocisteína/administración & dosificación , Interacciones Farmacológicas , Quimioterapia Combinada , Femenino , Humanos , Masculino , Persona de Mediana Edad , Moco/metabolismo
19.
Int J Clin Pharmacol Res ; 4(5): 361-5, 1984.
Artículo en Inglés | MEDLINE | ID: mdl-6519850

RESUMEN

Mezlocillin is an expanded spectrum semisynthetic penicillin for parenteral administration, with a good activity against a wide range of pathogenic bacteria including most anaerobes. The pharmacokinetic parameters of mezlocillin were determined in serum and sputum at the first and the seventh day of treatment with 1 g/im/12 h in patients suffering from bronchopulmonary infections. In a second group of volunteer patients who had to undergo surgery for lung cancer, mezlocillin levels in pulmonary tissue and the corresponding serum levels were determined at different times after drug administration. The data obtained made it possible to obtain information on the penetration and clearance of this drug in the bronchopulmonary tract in comparison with that of the serum. The pharmacokinetic behaviour of mezlocillin ensures an efficient antibacterial action in the respiratory tract.


Asunto(s)
Bronquios/metabolismo , Pulmón/metabolismo , Mezlocilina/metabolismo , Humanos , Cinética , Mezlocilina/sangre , Factores de Tiempo
20.
Respiration ; 44(2): 109-17, 1983.
Artículo en Inglés | MEDLINE | ID: mdl-6403977

RESUMEN

Reduction in non-specific bronchial hyperreactivity has been reported in atopic asthmatic patients as a consequence of long-term treatment with sodium cromoglycate. As bronchial hyperreactivity is an undesirable feature in other forms of obstructive airways disease, we examined the effect of regular treatment with sodium cromoglycate (20 mg, 4 times daily, for 30 days) in a group of non-atopic bronchitic subjects who showed a significant bronchoconstrictor response to the inhalation of ultrasonically nebulised distilled water (fog challenge). After 30 days treatment with sodium cromoglycate, there was a significant reduction in response to fog challenge, compared with pretreatment values. There was a washout period of 12 h between the administration of the last dose of sodium cromoglycate and the second fog challenge. The possible mechanisms involved and the clinical significance of these findings are discussed.


Asunto(s)
Enfermedades Bronquiales/prevención & control , Bronquitis/tratamiento farmacológico , Cromolin Sódico/uso terapéutico , Hipersensibilidad/prevención & control , Adulto , Anciano , Albuterol/inmunología , Pruebas de Provocación Bronquial , Femenino , Humanos , Masculino , Persona de Mediana Edad , Premedicación , Factores de Tiempo
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