Experiment 1142695

Details

PropertyValue
Pharmacology
Administration routeORAL
OrganismEmpty organism
CitationSTEWART,DJ: NUNDY,D: MAROUN,JA: TETREAULT,L: PRIOR,J:. (1985). BIOAVAILABILITY, PHARMACOKINETICS, AND CLINICAL EFFECTS OF AN ORAL PREPARATION OF ETOPOSIDE.. 69(3)
Amount utilized
Compound isolated
DiseaseBIOAVAILABILITY AND PHARMACOKINETICS OF ORAL ETOPOSIDE WAS STUDIES IN 13 PATIENTS WITH ADVANCED LUNG CANCER. PATIENTS WERE GIVEN AN INITIAL COURSE BY IV 1-HOUR INFUSION AT A DOSE OF 100/MG/SQ.M. DAY FOR 4 DAYS. FOR THE SECOND COURSE OF TREATMENT 3 WEEKS LATER, 3 PATIENTS RECEIVED 150, 175 AND 200 MG/SQ.M./DAY P.O. FOR 4 DAYS. THE TEN ADDITIONAL PATIENTS WERE RANDOMIZED TO RECEIVE THE DRUG ORALLY AT 200 MG/SQ.M./DAY OR BY IV 1-HOUR INFUSION AT 100MG/SQ.M./DAY FOR 4 DAYS. PLASMA LEVEL ANALYSIS USING HPLC SHOWED THAT 52% (RANGE OF 17-72%) OF THE ORALLY ADMINISTERED DOSE WAS ABSORBED, (ABSORPTION OF OVER 40% WAS SEEN IN ONLY ONE PATIENT). THE MEAN PEAK PLASMA LEVEL WAS 9.6 UG/ML ORALLY AND 13.0 UG/ML BY IV ADMINISTRATION. OTHER PARAMETERS BY ORAL OR IV ADMINISTRATION RESPECTIVELY,WERE: MEAN ALPHA HALF LIFE OF 0.96 AND 0.82 HOUR,MEAN BETA HALF LIFE OF 7.2 AND 6.8 HOURS,MEAN C X T VALUES OF 75.9 AND 75.3 MG/L/HR,AND MEAN PLASMA CLEARANCES OF 1.44 AND 1.45 L/HOUR/SQ.M. THE MEAN EXTRAPOLATED VOLUMES OF DISTRIBUTION FOR ORALLY AND IV ADMINISTERED ETOPOSIDE WERE 15.2 AND 16.9 L/SG.M. RESPECTIVELY.
Dose amountVAR
Number1
Qualitative resultACTIVE
AnimalHUMAN ADULT
Dose expressionDOSE