The Role of the Therapeutic Regimen in Dosage Design. Part II

Krüger-Thiemer, Ekkehard; Bünger, Paul

doi:10.1159/000220402

Cited by 26 publications

(13 citation statements)

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“…In the case of bacteriostatic agents such as sulphormethoxine and Chlortetracycline, it can be clearly correlated with the length of the LRP, especially when the concentrations of active sub-stance in the serum during this critical period are considered [Sack mann, 1968[Sack mann, , 1971. The results of these studies are consistent with the hypothesis that adequate concentrations of bacteriostatic substances must be maintained uninterruptedly in the organism [Krüger-Thiemer and Bünger, 1965].…”

supporting

confidence: 84%

The Serum Concentration of Bactericidal Antibiotics (Rifampicin, Cephaloridine) in Relation to the Low Resistance Period in Experimental Infections

Sackmann¹

1971

Chemotherapy

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The minimum inhibitory concentration of bactericidal as opposed to bacteriostatic agents does not necessarily have to be maintained in the blood for the full duration of the low resistance period (LRP). Even brief exposure to concentrations which are bactericidal or high enough to induce bacteriopause can effectively suppress the infection. The longer the LRP, the more sustained must be the antibacterial effect. The relations between these factors are examined with reference to the effect of single doses of rifampicin and cephaloridine in a series of experimental infections in the mouse.

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supporting

confidence: 84%

The Serum Concentration of Bactericidal Antibiotics (Rifampicin, Cephaloridine) in Relation to the Low Resistance Period in Experimental Infections

Sackmann¹

1971

Chemotherapy

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“…This could introduce additional errors due to the use of different bacterial strains and culture media. How ever, for those compounds tested by different au thors [1,7,8] the MIC values were consistent within experimental error. The molar refractivity was calculated as the sum of bond refractivities after Vogel et al [12].…”

Section: Methodssupporting

confidence: 53%

“…For this purpose, 16 most widely used sulphonamides have been chosen whose bio logical parameters [1,7,8] have been com monly accepted in those studies [6,9]. For the sake of comparison, also the parent compound, sulphanilamide, and sulphacarbamide (sulphonylurea) have been included.…”

mentioning

confidence: 99%

<i>In vitro</i> Activity of Sulphonamides as a Function of Their Molar Refractivity

1979

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A significant correlation has been found between the in vitro activity of 16 commonly employed sulphonamides and their molar refractivity. The molar refractivity has been shown to be a superior parameter for the description of the activity of sulphonamides than the sum of electronegativities of atoms making up a heterocyclic substituent in the sulphonamide molecule and molecular weight of the substituent.

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“…It is possible that the sensitivity of certain strains of bacteria is such that SM is effective but the lower doses of SD are not. Their number is not likely to be high [5,10] and actually this amount of SM has also been regarded as an unnecessary overdose [9]. In urine, the concentrations of all the drugs studied were more than satisfac tory.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic Studies with Trimethoprim and Different Doses of Sulfadiazine in Healthy Human Subjects

Männistö¹,

Tuomisto²,

Saris³

et al. 1973

Chemotherapy

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Concentrations of sulfadiazine were compared with those of sulfamethoxazole after combination treatment of sulfonamide plus trimethoprim. Sulfadiazine was used in doses of 1.6, 1.0 or 0.6 g ini, and thereafter half of the initial dose twice daily. The initial dose of sulfamethoxazole was 1.6 g and the subsequent doses 0.8 g twice daily. All of these preparations contained the same amount of trimethoprim, 320 mg initially and then 160 mg twice daily. In plasma the free minimum concentrations of sulfadiazine were more than 10 mg/l even after the lowest dose, and both after the initial dose and after subsequent doses. Because of the more favorable MIC of sulfadiazine, these are more effective free concentrations than those obtained after conventional doses of sulfisoxazole. The free minimum concentrations of sulfamethoxazole were over 15 mg/l, which were approximately the same as those after the highest dose of sulfadiazine. In urine the free effective concentrations after sulfamethoxazole and even the lowest dose of sulfadiazine were well over 100 mg/l. The apparent half-lives of sulfamethoxazole and sulfadiazine were 13.4 ± 2.8 h and 14.9 ± 8.7 h, respectively. The minimum concentrations of trimethroprim were higher than 1 mg/l on an average. There were no differences between different combinations in this respect. It is concluded that on the pharmacokinetic basis, sulfadiazine appears to be as good a choice for combinations with trimethoprim as is sulfamethoxazole. Theoretically, it is effective at the same dosage level as sulfamethoxazole. This is due to its favorable pharmacokinetic properties, namely low protein-binding and relatively low degree of metabolism. As compared with sulfisoxazole, both of these sulfonamides are overdosed, and clinical trials by using a lower dosage appear feasible.

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The Role of the Therapeutic Regimen in Dosage Design. Part II

Cited by 26 publications

References 0 publications

The Serum Concentration of Bactericidal Antibiotics (Rifampicin, Cephaloridine) in Relation to the Low Resistance Period in Experimental Infections

The Serum Concentration of Bactericidal Antibiotics (Rifampicin, Cephaloridine) in Relation to the Low Resistance Period in Experimental Infections

<i>In vitro</i> Activity of Sulphonamides as a Function of Their Molar Refractivity

Pharmacokinetic Studies with Trimethoprim and Different Doses of Sulfadiazine in Healthy Human Subjects

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