FLUOROURACIL INJECTION SOLUTION

Maa: Kanada

Kieli: englanti

Lähde: Health Canada

Aktiivinen ainesosa:

FLUOROURACIL

Saatavilla:

SANDOZ CANADA INCORPORATED

ATC-koodi:

L01BC02

INN (Kansainvälinen yleisnimi):

FLUOROURACIL

Annos:

50MG

Lääkemuoto:

SOLUTION

Koostumus:

FLUOROURACIL 50MG

Antoreitti:

INTRAVENOUS

Kpl paketissa:

10ML

Prescription tyyppi:

Prescription

Terapeuttinen alue:

ANTINEOPLASTIC AGENTS

Tuoteyhteenveto:

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

Valtuutuksen tilan:

APPROVED

Valtuutus päivämäärä:

2005-06-01

Valmisteyhteenveto

_Fluorouracil Injection _
_Page 1 of 19 _
_ _
PRODUCT MONOGRAPH
FLUOROURACIL INJECTION
5-fluorouracil Ph.Eur.
50 mg/mL Injection USP
Antineoplastic Agent
Sandoz Canada Inc.
Date of Revision: April 3, 2012
145 Jules-Léger
Boucherville, QC
J4B 7K8
Submission Control No: 145218
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_Fluorouracil Injection _
_Page 2 of 19 _
Fluorouracil Injection
(5-fluorouracil Ph.Eur.)
THERAPEUTIC CLASSIFICATION
Antineoplastic
CAUTION:
FLUOROURACIL (5-FLUOROURACIL) IS A POTENT DRUG AND SHOULD
BE PRESCRIBED ONLY BY PHYSICIANS EXPERIENCED WITH CANCER
CHEMOTHERAPEUTIC DRUGS (SEE WARNINGS AND PRECAUTIONS). BLOOD
COUNTS AS WELL AS RENAL AND HEPATIC FUNCTION TESTS SHOULD BE
PERFORMED REGULARLY. DISCONTINUE THE DRUG IF THERE IS SIGNIFICANT
LEUKOPENIA (UNDER 3 000/mm
3
) OR GRANULOCYTOPENIA (UNDER 1 500/mm
3
).
ACTIONS AND CLINICAL PHARMACOLOGY
Fluorouracil (5-fluorouracil) is a fluorinated pyrimidine
antimetabolite which is structurally
similar to uracil, one of the necessary building blocks in cellular
division and growth.
Figure 1
Its usefulness is based on uracil being utilized preferentially for
nucleic acid biosynthesis in
some tumors. 5-fluorouracil is metabolized to 5-fluorouridine
triphosphate (F-UTP),
2-deoxyfluorouridine monophosphate (Fd-UMP), and 2-deoxyfluorouridine
triphosphate
(Fd-UTP) in cells to concentrations that result in both DNA-directed
and RNA-directed
cytotoxicities (see Figure 1). Fd-UMP is the intracellular cytotoxic
form of 5-fluorouracil. It
competes with the natural substrate d-UMP (deoxyuridine monophosphate)
for the catalytic site
_ _
_Fluorouracil Injection _
_Page 3 of 19 _
on thymidylate synthetase (a key enzyme in DNA synthesis), forming a
covalent complex with
the enzyme that is unable to undergo the normal catalytic reaction of
converting d-UMP to
d-TMP. The presence of a reduced folate cofactor is required for tight
binding of Fd-UMP to
thymidylate synthetase. Folinic acid (leucovorin), which is
metabolized to 5,10-methylene-
tetrahydropteroylglutamine (a reduced folate), is able to modulate the
ant