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Seromycin (Cycloserine) - Description and Clinical Pharmacology

 
 



DESCRIPTION

Seromycin(Cycloserine Capsules, USP), 3-isoxazolidinone, 4-amino, (R)is a broadspectrum antibiotic that is produced by a strain of Streptomyces orchidaceus and has also been synthesized. Cycloserine is a white to offwhite powder that is soluble in water and stable in alkaline solution. It is rapidly destroyed at a neutral or acid pH.
Cycloserine has a pH between 5.5 and 6.5 in a solution containing 100 mg/mL. The molecular weight of cycloserine is 102.09, and it has an empirical formula of C3H6N2O2. The structural formula of cycloserine is as follows:





CLINICAL PHARMACOLOGY

After oral administration, cycloserine is readily absorbed from the gastrointestinal tract, with peak blood levels occurring in 4 to 8 hours. Blood levels of 25 to 30can generally be maintained with the usual dosage of 250 mg twice a day, although the relationship of plasma levels to dosage is not always consistent. Concentrations in the cerebrospinal fluid, pleural fluid, fetal blood, and mother's milk approach those found in the serum. Detectable amounts are found in ascitic fluid, bile, sputum, amniotic fluid, and lung and lymph tissues. Approximately 65% of a single dose of cycloserine can be recovered in the urine within 72 hours after oral administration. The remaining 35% is apparently metabolized to unknown substances. The maximum excretion rate occurs 2 to 6 hours after administration, with 50% of the drug eliminated in 12 hours.

Microbiology
Cycloserine inhibits cellwall synthesis in susceptible strains of grampositive and gramnegative bacteria and in Mycobacterium tuberculosis.

Susceptibility Tests
Cycloserine clinical laboratory standard powder is available for both direct and indirect methods1 of determining the susceptibility of strains of mycobacteria. Cycloserine MICs for susceptible strains are 25or lower.

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