trimethoprim--sulfamethoxazole-drug-combination and brodimoprim

Brodimoprim is a new diaminopyridine derivative suitable for oral therapy which shows good in-vitro activity against most Gram-positive and Gram-negative pathogens. The efficacy and tolerability of brodimoprim in acute lower respiratory tract infections was tested in controlled clinical trials in comparison with different classes of antibiotics. Acute bacterial infections or infective exacerbations of chronic obstructive bronchitis were included in the studies. Brodimoprim in a single dose was compared to different oral treatments which included co-trimoxazole (trimethoprim 160 mg+sulphamethoxazole 800 mg every 12 hours) and erythromycin (600 mg three times a day). In the studies criteria of efficacy such as daily temperature curve, intensity and frequency of cough, degree of dyspnea, intensity of thoracic pain, difficulty of expectoration, sputum production, thoracic semiology were examined. Brodimoprim was more effective than cotrimoxazole and erythromycin at the end of the treatment, induring a more significant and prompt reduction of axillary temperature, daily sputum volume, degree of dyspnea. There was no difference among treatments in the mean period of therapy to obtain the resolution of the infective process (8 days on average). Brodimoprim had a significantly lower percentage of side effects during the treatment in comparison with cotrimoxazole or erythromycin. Hence brodimoprim was better accepted by patients.

Topics: Adult; Erythromycin; Female; Gram-Negative Bacterial Infections; Humans; Male; Middle Aged; Respiratory Tract Infections; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

160 children with an average age of 9 years (range 6-15) affected by acute bacterial tonsillitis, were selected and assigned, following an open, parallel group design to: a) brodimoprim at the dose of 10 mg/kg on the first day, in single administration, and of 5 mg/kg on the following days; b) cotrimoxazole suspension, at the dosage of 6 mg of trimethoprim/kg/day, in two daily administrations; c) amoxicillin with clavulanic acid suspension (amoxi-clavulanate) 50 mg/kg every 12 hours. Quantity of pharynx and tonsillar exudate, pharynx pain, dysphonia and dysphagia were checked at the basal time, 3rd, 7th and at the last day of therapy. These symptoms were evaluated using a four-step rating scale. The evolution of body temperature was measured at two different times (1 and 5 o'clock p.m.), until the end of treatment, foreseen five days after disappearance of fever. Microbiological evaluation through a pharynx swab was performed at the beginning and at the end of therapy. Side-effects were registered during all the observation period. Lab-tests were carried out at the enrollment and at the end of treatment. The frequency and intensity of symptoms decreased significantly in all treatment groups. In comparison with amoxi-clavulanate, the brodimoprim group showed an earlier improvement (3rd day) of the clinical situation and a significantly better regression of pharynx exudate (p < 0.01), pharynx pain (p < 0.05) and dysphonia (p < 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Adolescent; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Child; Child, Preschool; Clavulanic Acids; Drug Therapy, Combination; Humans; Pharyngitis; Suspensions; Tonsillitis; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

The efficacies of trimethoprim (TMP)-sulfamethoxazole (SMZ), TMP-dapsone, dapsone, and pentamidine were compared for the prevention of Pneumocystis carinii pneumonia in the corticosteroid-treated-rat model. While 11 (73%) of 15 untreated control animals had P. carinii pneumonia after 10 weeks of immunosuppression, none of the animals given 125 mg of dapsone per kg daily, weekly, biweekly, or monthly had evidence of infection. Of the 10 rats given a single dose of dapsone 23 and 50 days after immunosuppression was started, 5 (50%) had P. carinii pneumonia. When three drugs were given separately to groups of 10 rats in single doses biweekly, P. carinii pneumonia occurred in 40% of those treated with TMP-SMZ and in none of those treated with TMP-dapsone; although only 2 of those treated with pentamidine survived for evaluation, both had P. carinii pneumonia. The experiments showed that dapsone is highly effective in chemoprophylaxis for P. carinii pneumonia when given at monthly intervals or more frequently and that dapsone and TMP-dapsone are more effective than is TMP-SMZ when given at biweekly intervals. It seems reasonable to expect that biweekly doses of dapsone or TMP-dapsone would provide an effective and reasonably safe chemoprophylaxis regimen for patients at high risk for P. carinii pneumonia, and studies to test such a scheme are justifiable. Biweekly doses are preferred over monthly doses to allow for occasional inadvertent omission of doses expected from patients.

Topics: Amidines; Animals; Anti-Infective Agents; Dapsone; Drug Administration Schedule; Drug Combinations; Immunosuppression Therapy; Male; Pentamidine; Pneumonia, Pneumocystis; Rats; Rats, Inbred Strains; Sulfamethoxazole; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination