EFFECTS OF INHIBITORS OF SULFANILAMIDE ACETYLATION ON SULPHONAMIDE BLOOD CONCENTRATIONS

1955 ◽  
Vol 33 (4) ◽  
pp. 523-529 ◽  
Author(s):  
Willard Johnson

The effect of inhibitors of sulphanilamide acetylation on free and total sulphonamide blood levels has been investigated. p-Aminosalicylic acid hydrazide, administered to rabbits in combination with sulphanilamide, produced a twofold increase in the blood level of free sulphanilamide six hours after a single oral dose. Similarly, p-aminosalicylate and p-(dipropylsulphamyl)-benzoic acid together were responsible for a twofold increase in free-sulphonamide blood level six hours after a single oral dose of a triple sulphonamide mixture. Salicylamide and 5-bromosalicylamide were ineffective. The significance of these results is discussed.

1955 ◽  
Vol 33 (1) ◽  
pp. 523-529 ◽  
Author(s):  
Willard Johnson

The effect of inhibitors of sulphanilamide acetylation on free and total sulphonamide blood levels has been investigated. p-Aminosalicylic acid hydrazide, administered to rabbits in combination with sulphanilamide, produced a twofold increase in the blood level of free sulphanilamide six hours after a single oral dose. Similarly, p-aminosalicylate and p-(dipropylsulphamyl)-benzoic acid together were responsible for a twofold increase in free-sulphonamide blood level six hours after a single oral dose of a triple sulphonamide mixture. Salicylamide and 5-bromosalicylamide were ineffective. The significance of these results is discussed.


1986 ◽  
Vol 31 (4) ◽  
pp. 299-303 ◽  
Author(s):  
Lawrence H. Rockland

Gas chromatography and radioreceptor assay technologies made possible the measurement of nanogram quantities of neuroleptic in the blood. They revealed large differences in blood concentrations among patients receiving the same oral dose. This led to the hope that measuring neuroleptic concentrations would allow more effective oral dosing for individual psychotic patients. Early attempts to study neuroleptic concentration/clinical response patterns, using chlorpromazine, produced confusing results. Many of the studies had serious design flaws, and were complicated by the many active metabolites of chlorpromazine. Adequate blood level/response studies should use fixed drug dosage schedules, drug-responsive patients, and neuroleptics without active metabolites. Brain concentration of drug is probably better reflected by erythrocyte than by plasma concentration. Therefore, recent investigators have usually used erythrocyte haloperidol or butaperazine concentrations to study level/response relationships. These recent studies strongly suggest an “optimal concentration” level/response pattern for haloperidol and butaperazine. Patients tend to respond best to moderate concentrations of neuroleptic, and non-response can be due to either too low or too high concentrations. In the latter case, decreasing the oral dose should be seriously considered. Blood level findings remain preliminary. The clinician should continue to fine-tune his clinical skills, using neuroleptic blood concentrations to complement his clinical judgment, in the attempt to determine the lowest effective dose for the individual patient.


1962 ◽  
Vol 13 (2) ◽  
pp. 307 ◽  
Author(s):  
RL Reid

Acetone comprised 0–40% (average 18%) of the acetoacetic acid plus acetone fraction in sheep blood, in which the level of this fraction was 0.6–5.2 mg % (as acetone). Acetoacetic acid was largely converted to acetone during storage of blood at –20°C, with intermittent thawing for analysis. Concentrations of acetoacetic acid in red cells were similar to those in plasma, but those of ß-hydroxybutyric acid were considerably lower. In contrast to acetoacetic acid, ß-hydroxybutyric acid was virtually absent from foetal blood and from brain tissue. Concentrations of both ketone fractions in liver and muscle tissue were about one-half the blood concentrations. The renal clearance of acetoacetic acid plus acetone in hyperketonaemic pregnant ewes was independent of blood level up to 20 mg % and was little affected by rate of urine flow. Clearance values were in the range of 4–9 ml per min, which indicates that most of the acetoacetic acid filtered at the glomeruli is absorbed by the renal tubules. Renal clearance of ß-hydroxybutyric acid was dependent on blood level and was more affected by rate of urine flow than that of acetoacetic acid. Very little ß-hydroxybutyric acid appeared in the urine when blood levels were below 15 mg %. Clearance increased as blood concentration rose above this level, and reached maximum values, mostly of 3–5 ml per min, at blood levels exceeding 30 mg %.


1973 ◽  
Vol 92 (10) ◽  
pp. 263-263
Author(s):  
R. Medd ◽  
I. Burrows ◽  
D. Ross

1973 ◽  
Vol 12 (03) ◽  
pp. 218-224
Author(s):  
Elli Lakka - Papadodima ◽  
Constantin Ntalles ◽  
Denis Ikkos

Des mesurages répétés de la fixation thyroïdienne de 10 minutes du 132I injecté intraveineusement on été effectués sur 55 malades euthyroïdiens sans et avec goitre et sur 16 malades hyperthyreoïdiens par 4 jours consécutifs. Immédiatement après le premier mesurage tous les malades recevaient une dose unique oral de 100 μg de Triiodothyronine (T3). Les valeurs de fixation 24, 48 et 72 heures après le T3 (moyen ± déviation standard) étaient de 75 ± 1,7, 64 ± 1,8, et 67 ± 1,9 dans le groupe euthyroïdien et le 106 ± 2,6, 104 ± 2,2 et 108 ± 4,0 dans le groupe hyperthyroïdien, exprimés en pourcentage du groupe controle. 48 heures après T3 tous les personnes euthyroïdiens, sauf une, avaient des valeurs en dessous de 88% tandis que la valeur la plus basse des personnes hyperthyroïdiens ce jour était de 93%. La séparation des valeurs 48 heures des deux groupes était complète après avoir respecté l’influence de la première fixation sur la valeur 48 heures. On peut donc supposer q’un test thyroïdien de suppression utilisable en clinique peut-être effectué en 48 heures après une administration oral de 100 μg de T3 et mesurage de la fixation 10 minutes après l’injection du radioisotope.


1973 ◽  
Vol 30 (03) ◽  
pp. 494-498 ◽  
Author(s):  
G de Gaetano ◽  
J Vermylen

SummaryThrombelastograms of both native blood and re-calcified platelet-rich plasma samples taken from subjects given a single oral dose of aspirin (1 gram) were not significantly different from the pretreatment recordings. Aspirin also did not modify the thrombelastogram when preincubated in vitro with platelet-rich plasma at concentrations inhibiting the platelet “release reaction” by collagen. Thrombelastography therefore cannot evaluate the effect of aspirin on platelet function.


1970 ◽  
Vol 31 (2) ◽  
pp. 281-287 ◽  
Author(s):  
Paul D. Altland ◽  
Benjamin Highman ◽  
Milton G. Parker ◽  
Michael P. Dieter

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