DTI FOR INJECTION

Country: Malaysia

Language: English

Source: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)

Active ingredient:

DACARBAZINE

Available from:

FIRST PHARMACEUTICAL SDN. BHD.

INN (International Name):

DACARBAZINE

Units in package:

0.1 gm mcg/mL; 0.2 gm mcg/mL; 10Units Units

Manufactured by:

Korea United Pharm. Inc.

Summary of Product characteristics

DTI
FOR INJECTION
DACARBAZINE 100MG, 200MG
COMPOSITION
Each vial contains
Dacarbazine
··········································································
100 mg
Dacarbazine
······················································································
200 mg
DESCRIPTION
White to pale yellow, freeze-dried powder in an amber vial.
Dacarbazine is a structural analogue of
5-amino-imidazole-4-carboxamide which is an
intermediate in purine biosynthesis.
ACTIONS
Cytotoxic agent.
PHARMACOLOGY
Site and mode of action: This drug inhibits cell replication by an
unknown mechanism.
However, three possible mechanisms have been postulated:
Since dacarbazine is an analogue of 5-amino-imidazole-4-carboxamide,
an intermediate in
the de novo biosynthesis of purine, it might interfere with purine
biosynthesis and hence
DNA bio-synthesis. This appears to be true at high concentrations of
the drug, but low
concentrations appear to enhance DNA, RNA and protein biosynthesis.
One metabolite of dacarbazine, diazomethane, is an alkylating agent
and may act in the
same way as the nitrogen mustards.
The drug might act as a sulphydryl reagent since the inhibition of
bacterial growth by
dacarbazine can be prevented by glutathione.
PHARMACOKINETICS
Absorption : Dacarbazine is poorly absorbed from the GI tract. Peak
plasma concentrations
of about 8 µ
g
/mL are reached immediately following administration of dacarbazine
4.5
mg/kg
by IV push.
Distribution : The volume of distribution of dacarbazine exceeds total
body water content,
suggesting localization in some body tissue, probably the liver. The
drug is only slightly
bound to plasma proteins. Dacarbazine crosses the blood-brain barrier
to a limited extent;
CSF concentrations are reported to be about 14 % of plasma
concentrations. It is not known
if dacarbazine crosses the placenta or distributes into milk.
Elimination :