N(1)-acetyl sulfisoxazole (N1AS), a dihydropteroate synthase inhibitor is known to be biotransformed primarily to sulfisoxazole, partly to N(4)-acetyl sulfisoxazole (N4AS), and likely also to diacetyl sulfisoxazole (DAS) and other compounds. Although its clinical use has been limited due to urolithiasis, some countries still use the drug in combination with trimethoprim in cattle. A liquid chromatographic method using ultraviolet detection was developed for the simultaneous determination of four substances for the first time. Four analytes and sulfamethoxazole (IS) were separated on a reversed-phase column with gradient elution of a mobile phase. Because DAS and N1AS in plasma were changed very quickly into N4AS and sulfisoxazole, respectively, and esterase inhibitors (sodium fluoride and eserine) could not prevent the transformation, sulfisoxazole and N4AS were monitored in rat plasma following a single oral administration of N1AS and sulfisoxazole in five rats. The relative bioavailability of N1AS to sulfisoxazole was about two, indicating that a half-dose of N1AS would be equivalent to a dose of sulfisoxazole to achieve the same systemic exposure to sulfisoxazole.

01 Sep 2006·Journal of AOAC INTERNATIONALQ4 · AGRICULTURAL & FORESTRY SCIENCE

A Validated Spectrofluorometric Assay for the Determination of Certain Macrolide Antibiotics in Pharmaceutical Formulations and Spiked Biological Fluids

Q4 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: El-Rabbat, Nawal ; Askal, Hassan F ; Khashaba, Pakinaz Y ; Attia, Noha N

AbstractThis paper describes a simple spectrofluorometric method for the analysis of 4 macrolide antibiotics. The method is based on the condensation of 10% (w/v) malonic acid and acetic acid anhydride under the catalytic effect of tertiary amine groups of the studied macrolides. The relative fluorescence intensity of the condensation product was measured at 397/452 nm (excitation/emission) for azithromycin dihydrate and at 392/445 nm (for clarithromycin, erythromycin ethylsuccinate, and roxithromycin. All variables affecting the reaction conditions were studied. The effects of potential interference due to common excipients, such as starch, lactose, sucrose, glucose, gum acacia, and magnesium stearate, as well as trimethoprim and sulfisoxazole acetyl formulated in primomycin capsules and pediazole oral suspension, respectively, were studied. A validation study for the proposed method was carried out according to U.S. Pharmacopeia 2002. The linearity ranges were 380 ng/mL for all of the cited macrolides. The limit of detection range was 0.741.20 ng/mL, while the limit of quantitation range was 2.474.02 ng/mL. The method was applied for the assay of the studied macrolides in pure pharmaceutical formulations and in spiked biological fluids. Results were compared with those obtained from the reported method, where calculated t- and F-values indicated high accuracy and good precision for the proposed method.

01 Dec 1994·Journal of EndourologyQ3 · MEDICINE

Urolithiasis as a Hazard of Sulfonamide Therapy

Q3 · MEDICINE

Article

Author: Prien, E L ; Galal, H A ; Albala, D M

We identified 40 patients (25 men and 15 women) who developed calculi composed totally or partially of sulfonamides (acetylsulfamethoxazole, sulfadiazine, and acetylsulfisoxazole) between 1980 and 1987. The incidence of sulfonamide stones is less than 1% of stones. Patient characteristics were determined from questionnaires sent to the patients and attending physicians. The majority of patients developed symptoms 1 to 4 weeks after beginning sulfonamide therapy. The bladder was the most common stone location. Obstruction of the urinary system by the acetyl derivatives of the drug is the most serious consequence of sulfonamide therapy. Early recognition of drug-related stones is essential to protect patients from recurrences, reduce the risk of renal complications, and avoid continuing ineffective therapeutic regimens.

100 Deals associated with Sulfisoxazole Acetyl

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KEGG	Wiki	ATC	Drug Bank
D05956	-	S01AB02 J01EB05	DB14033

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