RESUMEN
The MICs of evernimicin at which 90% of Borrelia burgdorferi patient isolates were inhibited ranged from 0.1 to 0.5 microg/ml. Evernimicin was as effective as ceftriaxone against B. burgdorferi in a murine model of experimental Lyme disease. As assessed by culturing the urinary bladders of infected C3H mice, no live Borrelia isolates were recoverable following antibiotic treatment.
Asunto(s)
Aminoglicósidos , Antibacterianos/uso terapéutico , Grupo Borrelia Burgdorferi/efectos de los fármacos , Enfermedad de Lyme/tratamiento farmacológico , Animales , Antibacterianos/farmacología , Ceftriaxona/farmacología , Ceftriaxona/uso terapéutico , Cefalosporinas/farmacología , Cefalosporinas/uso terapéutico , Modelos Animales de Enfermedad , Femenino , Ratones , Ratones Endogámicos C3H , Pruebas de Sensibilidad Microbiana , Resultado del TratamientoRESUMEN
SCH 39304 was compared with fluconazole and ketoconazole in a systemic Candida albicans infection in mice (10(6) CFU per mouse). Results were based on survival rates and CFU in kidneys following once-daily oral treatment of 2, 5, or 10 days duration. In normal mice, SCH 39304 (dose to reduce kidney counts by 4 log units, 0.5 mg/kg of body weight) was 3 and 200 times more active than fluconazole and ketoconazole, respectively. In immunocompromised mice (gamma irradiation, 600 rads), SCH 39304 (dose to reduce kidney counts by 4 log units, 1.3 mg/kg) was 35 and greater than 100 times more active than fluconazole and ketoconazole, respectively. In normal mice, when the infecting inoculum varied from 10(5) to 10(7) CFU, only a fivefold increase in the dose to reduce kidney counts by 4 log units was observed with SCH 39304. Excellent protection was also seen when mice were treated with a single oral dose of SCH 39304 up to 24 h prior to infection with C. albicans. Studies in a systemic C. albicans infection model indicated that SCH 39304 is equally efficacious following either oral or intravenous administration. In a systemic Aspergillus flavus infection, mice treated with SCH 39304 (5 mg/kg) survived twice as long (16 days) as those treated with fluconazole (50 mg/kg) or controls did.
Asunto(s)
Antifúngicos/uso terapéutico , Aspergilosis/tratamiento farmacológico , Candidiasis/tratamiento farmacológico , Fluconazol/uso terapéutico , Cetoconazol/uso terapéutico , Triazoles/uso terapéutico , Administración Oral , Animales , Antifúngicos/administración & dosificación , Evaluación Preclínica de Medicamentos , Fluconazol/administración & dosificación , Inyecciones Intravenosas , Cetoconazol/administración & dosificación , Riñón/efectos de los fármacos , Riñón/microbiología , Riñón/efectos de la radiación , Masculino , Ratones , Triazoles/administración & dosificaciónRESUMEN
The authors performed the experimental model of infarct-like myocardial lesions in rats treated with large doses of ISP. Myocardial necrosis was assessed on the basis of serum enzyme changes as well as of gross and microscopic findings. The infarct size was measured by a direct enzymatic method assaying creatine kinase (CK) depletion in infarcted myocardium. Pretreatment of the infarcted rats with antiplatelet (Lysin Acetyl Salicylate) or calcium antagonist drugs (Verapamil or Nifedipine) allowed the reduction of the necrotic area. Since a smaller size of infarct was achieved through different types of interventions it should be suggested that ISP-myocardial damage is due to several effects of the drug involving metabolic, vascular and/or coagulative patterns.