trimethoprim--sulfamethoxazole-drug-combination and sulfadiazine--tetroxoprim-drug-combination

127 outpatients, 78 with acute purulent sinusitis and 49 with acute tonsillitis, were treated for 7 days with a benzylpyrimidine -sulphonamide combination. In this double-blind and randomized study 59 patients received co- tetroxazine (100 mg tetroxoprim and 250 mg sulphadiazine) b.i.d., whilst the reference substance, co-trimoxazole (160 mg trimethoprim and 800 mg sulphamethoxazole) was given to the remaining 68 patients b.i.d. The test criteria were the therapeutic efficacy and both subjective and objective tolerance. An improvement in clinical symptoms and signs occurred in both conditions under each therapeutic regimen. Clinical therapeutic success was rated very good or good in 96.6% treated with co- tetroxazine and in 97.1% of patients treated with co-trimoxazole. In the former group therapy failed in 1 patient with sinusitis and in 1 with acute tonsillitis . In 98.3% of patients treated with co- tetroxazine the tolerance was very good or good, whilst the respective figure for co-trimoxazole was only 91.2%. 6 patients suffered from side effects ( gastric spasm, gastralgia , nausea, vomiting, diarrhoea) which were so severe in 2 cases that treatment had to be prematurely terminated. The generally good tolerance to both preparations was confirmed by the results of the laboratory investigations.

Topics: Acute Disease; Adult; Clinical Trials as Topic; Drug Combinations; Female; Humans; Male; Middle Aged; Pyrimidines; Sinusitis; Sulfadiazine; Sulfamethoxazole; Tonsillitis; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

Following a single dose of co-trimoxazole or co-tetroxazine, the plasma and urine levels of intact trimethoprim (TMP) and sulphamethoxazole (SMZ) and of tetroxoprim and sulphadiazine (SDZ) were determined in six geriatric patients in a cross-over design by high pressure liquid chromatography. The pharmacokinetic analysis showed a plasma elimination half-life in the terminal phase of 10.39 h for TMP, 11.79 h for SMZ, 6.55 h for TXP and 10.46 h for SDZ. The resulting distribution volumes Vd beta and total plasma clearance values corresponded with the data obtained in young patients or volunteers. Recovery in urine, measured for up to 96 h, was 49.2% (TMP), 19.8% (SMZ), 57.03% (TXP) and 61.1% (SDZ). In contrast to young volunteers, geriatric patients experienced a slight prolongation of renal excretion for both sulphonamides. In this group of patients the renal clearance was 2.42 ml/min for SMZ and 10.7 ml/min for SDZ.

Topics: Absorption; Aged; Aging; Anti-Infective Agents, Urinary; Drug Combinations; Female; Half-Life; Humans; Kinetics; Male; Pyrimidines; Sulfadiazine; Sulfamethoxazole; Sulfonamides; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

In patients with chronic obstructive airway disease, the elimination half-lives of tetroxoprim (TXP) and sulfadiazine (SDZ) were found to be 8.6-9.0 h and 7.9-8.5 h, respectively, after administration of a single dose. The corresponding values for trimethoprim (TMP) and sulfamethoxazole (SMZ) were found to be 13.7 and 15.7 h, respectively. In the case of therapeutic multiple dosing, TMP and SMZ accumulate in patients' serum (tau = 12 h). Over a 10-day period of investigation, the serum levels measured were used to calculate half-life values of 12.9 h for TMP and 10.7 h for SMZ. Under the conditions of steady state, half-lives of 5.0 and 5.6 h were calculated for TXP and SDZ, respectively, which in the case of TXP might be explained kinetically. Due to the parallel change in the elimination-rate constants, no accumulation of TXP and SDZ in patients' serum (tau = 12 h) can occur.

Topics: Drug Combinations; Half-Life; Humans; Kinetics; Male; Middle Aged; Pyrimidines; Sulfadiazine; Sulfamethoxazole; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

Topics: Drug Combinations; Humans; Microbial Sensitivity Tests; Pyrimidines; Sulfadiazine; Sulfamethoxazole; Sulfamoxole; Sulfanilamides; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination