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(1) A simple disc technic has been devised for determining concentrations of amethopterin in blood and urine. (2) This test has an accuracy which compares favorably with similar assay methods for antibiotics. (3) Amethopterin appeared in the blood and urine in detectable amounts 15 to 30 minutes after the ingestion of a 5 mg dose on a fasting stomach by 2 normal individuals, and 30 to 60 minutes after ingestion at the same dose by 4 normal non-fasting individuals. In some of the 6 it was still detectable at 6 hours, but in none after 24 hours. (4) Six normal adults excreted 40 to 57% of the ingested dose in the urine within 24 hours. (5) In one patient little difference in serum levels or total excretion could be demonstrated whether the drug was given by the oral or intramuscular route. (6) In a patient with impaired renal function, higher initial serum levels were obtained and detectable amounts were present in the blood serum 48 hours after ingestion of amethopterin.
Burchenal et al. (Thu,) studied this question.