国: カナダ
言語: 英語
ソース: Health Canada
FLUOROURACIL
ACCORD HEALTHCARE INC
L01BC02
FLUOROURACIL
50MG
SOLUTION
FLUOROURACIL 50MG
INTRAVENOUS
100ML
Prescription
ANTINEOPLASTIC AGENTS
Active ingredient group (AIG) number: 0107505001; AHFS:
APPROVED
2013-10-04
PRODUCT MONOGRAPH PR FLUOROURACIL INJECTION USP 50 MG / ML (5 g / 100 mL) STERILE SOLUTION Antineoplastic Agent Accord Healthcare Inc. 3535 Boul. St-Charles, Suite 704 Kirkland, QC H9H 5B9 Canada CONTROL # : 232735 DATE OF REVISION: October 30, 2019 _Fluorouracil Injection USP 50 mg/mL, 100 mL - Accord Healthcare Inc._ _Page 2 of 21_ PRODUCT MONOGRAPH PR FLUOROURACIL INJECTION USP 50 MG / ML (5 g / 100 mL) Antineoplastic agent CAUTION FLUOROURACIL IS A POTENT DRUG AND SHOULD BE ADMINISTERED BY, OR UNDER SUPERVISION OF, A PHYSICIAN, WHO IS EXPERIENCED IN CANCER CHEMOTHERAPY. ACTIONS AND CLINICAL PHARMACOLOGY There appears to be two mechanisms of action of fluorouracil which result in cytotoxic effects. One is the competitive inhibition of thymidylate synthetase, the enzyme catalyzing the methylation of deoxyuridylic acid to thymidylic acid. The consequent thymidine deficiency results in inhibition of deoxyribonucleic acid (DNA) synthesis, thus inducing cell death. A second mechanism of action is evidenced by the moderate inhibition of ribonucleic acid (RNA) and incorporation of fluorouracil into RNA. The predominant mechanism of antitumour action appears to be dependent, at least in part, on individual tumour intracellular metabolism. The effects of DNA and RNA deprivation are most significant on those cells which are most rapidly proliferating. Following intravenous injection, fluorouracil is cleared rapidly from the plasma (half-life about 10 to 20 minutes), and distributed throughout body tissues including the cerebrospinal fluid and malignant effusions, exhibiting a volume of distribution equivalent to the total body water. Plasma concentrations fall below measurable levels within 3 hours. Oral administration of fluorouracil has shown marked variability in its bioavailability, from 28% to 100%. Constant intravenous infusion for 96 hours showed constant plasma drug levels and significantly less drug (50 to 1000 fold) in the bone marrow. Fluorouracil is converted to active nucleotide metabolites, 5-fluorouridine 完全なドキュメントを読む