FLUOROURACIL INJECTION USP SOLUTION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

FLUOROURACIL

Available from:

ACCORD HEALTHCARE INC

ATC code:

L01BC02

INN (International Name):

FLUOROURACIL

Dosage:

50MG

Pharmaceutical form:

SOLUTION

Composition:

FLUOROURACIL 50MG

Administration route:

INTRAVENOUS

Units in package:

100ML

Prescription type:

Prescription

Therapeutic area:

ANTINEOPLASTIC AGENTS

Product summary:

Active ingredient group (AIG) number: 0107505001; AHFS:

Authorization status:

APPROVED

Authorization date:

2013-10-04

Summary of Product characteristics

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