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Chlorambucil: Uses, Mechanism, and Formulation

Chlorambucil, marketed as Leukeran, is an alkylating agent used primarily for treating various cancers, including chronic lymphatic leukemia and lymphomas. Its mechanism of action involves damaging DNA through cross-linking and inducing mutations, leading to the prevention of DNA synthesis. The drug is administered orally and has specific side effects, including unusual bleeding and respiratory issues.

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50 views1 page

Chlorambucil: Uses, Mechanism, and Formulation

Chlorambucil, marketed as Leukeran, is an alkylating agent used primarily for treating various cancers, including chronic lymphatic leukemia and lymphomas. Its mechanism of action involves damaging DNA through cross-linking and inducing mutations, leading to the prevention of DNA synthesis. The drug is administered orally and has specific side effects, including unusual bleeding and respiratory issues.

Uploaded by

alaaeletre312
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd

CHLORAMBUCIL

PHARMACEUTICAL CHEMISTRY DEPARTMENT


KEROLOS MAGED SAMI, ABDELRAHMAN MEDHAT HASHEM, ALAA ELDIN MELEGY ELETRE.
[Link]/ GAMAL ABU-RAHMA [Link]/NAWAL EL-KOUSSI [Link]/SALAH ABDEL-AZIZ

GENERIC & TRADE MECHANISM OF SYNTHESIS OF CHLORAMBUCIL:


 GENERIC:
NAME ACTION: AGENT WORK
 ALKYLATING
CHLORAMBUCIL BY 3 DIFFERENT WAYS:
 Trade name: II. SECOND
leukeran  DNA damage via the
MECHANISM:
formation of cross-links
(bonds between atoms
in the DNA).
 which prevents DNA
from being separated for
synthesis or
III. THIRD MECHANISM:
transcription.
 the induction of
mispairing of the
Chemical structure nucleotides leading to
& mutations.
nomenclature……….
 CHEMICAL STRUCTURE:
SIDE EFFECT:
•Black, tarry stools.
•bleeding gums.
•blood in the urine or
stools.
•chest pain.
 NOMENCLATURE: •swollen glands.
•troubled breathing with
4-(4-(bis(2- exertion.
chloroethyl)amino)phenyl) •unusual bleeding or
butanoic acid. bruising.
•unusual tiredness or
MEDICINAL USES: Quantize
weakness METHODS OF
 USED FOR TTT OF: Less common.
structure activity ASSAY:
 High
 chronic lymphatic performance liquid chromatography
relationship:GROUP:
 MECHLORETHAMINE
with ultra-violet detection (HPLC-UV) and
(lymphocytic) leukemia.
 childhood minimal-change • Responsible gas chromatography–mass spectrometry
nephrotic syndrome. for binding (GC-MS) methods were developed and
 malignant lymphomas. and validated for the determination of
 Lymphosarcoma. crosslinking chlorambucil (CLB) in plasma, as a part of
 giant follicular lymphoma. with the experiments on their anticancer activity in
 BUTYRIC
 Hodgkin's disease. DNA. chronic lymphocytic leukemia (CLL).
 non-Hodgkin's ACID:  CLB was extracted from 250 µL of plasma
lymphomas. • Modificatio with methanol, using simple protein
 Waldenström’s. n site. precipitation and filtration.
 Macroglobulinemia.
MECHANISM OF  CH2OH CHAIN:
ACTION: AGENT WORK
 ALKYLATING • The alkyl chain
BY 3 DIFFERENT WAYS: length
influenced the
I. FIRST MECHANISM: antiproliferative
 activity.
Cl group modification:
 attachment of alkyl
Modification of
groups to DNA bases. the 2 Cl group
must be avoided
 resulting in the DNA as it may result
being fragmented by in potent
DRUG
repair enzymes in their chemotherapeuti
attempts to replace DRUG cs. FORMULATIONS:
LEUKERAN is
the alkylated bases. The ELIMINATION:
pharmacokinetic data supplied as brown,
suggests that oral chlorambucil film-coated, round,
 preventing DNA undergoes rapid biconvex tablets
gastrointestinal absorption containing 2 mg
synthesis and RNA
and plasma clearance and that chlorambucil in
transcription from the it is almost completely amber glass bottles

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