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Antineoplastics generally have _____ therapeutic ranges. -ANSWER✅✅✅Narrow
Is blood/serum concentration of the drug the same as the drug concentration in the
tissues? -ANSWER✅✅✅It is not always the same
What type of dosing does carboplatin use? -ANSWER✅✅✅Unique AUC-based dosing
Therapeutic drug monitoring is used for which antineoplastics? -ANSWER✅✅✅-High
dose methotrexate
-High dose busulfan
-Fluorouracil (not routine)
What is an example in which a clinical condition may affect the pharmacokinetics of an
antineoplastic? -ANSWER✅✅✅Third spacing and methotrexate
What are three examples of pharmacogenomic profiles that reduce the metabolism of
antineoplastics and increases the risk for toxicity? -ANSWER✅✅✅-Dihydropyrimidine
dehydrogenase deficiency (5-fluorouracil/capecitabine) (now BBW)
-UGT1A1*28 homozygosity (irinotecan)
-Thiopurine S-methyltransferase deficiency (mercaptopurine and thioguanine)
What are two examples of platinum agents? -ANSWER✅✅✅-Cisplatin
-Carboplatin
What is the mechanism of action of platinum agents? -ANSWER✅✅✅They covalently
bind to DNA which produces interstrand DNA cross-links. This causes a kink in the DNA
and DNA double strand breaks which cannot be repaired. This interferes with the
function of DNA. They are not cell cycle specific.
What are the pharmacokinetics of carboplatin? -ANSWER✅✅✅-Metabolism: Minimal
hepatic metabolism to aquated and hydroxylated compounds
-Excretion: Urine (~70% as unchanged drug within 24 hours)
-Half-life with normal renal function: 2.6 to 5.9 hours