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Mechlorethamine


ACCESSION NB: DB00888 (APRD00249)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
A vesicant and necrotizing irritant destructive to mucous membranes. It was formerly used as a war gas. The hydrochloride is used as an antineoplastic in Hodgkin's disease and lymphomas. It causes severe gastrointestinal and bone marrow damage. [PubChem]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Alkylating Agents Antineoplastic Agents, Alkylating Irritants Chemical Warfare Agents

ABSORPTION: Partially absorbed following intracavitary administration, most likely due to rapid deactivation by body fluids.

INDICATION:
For the palliative treatment of Hodgkin's disease (Stages III and IV), lymphosarcoma, chronic myelocytic or chronic lymphocytic leukemia, polycythemia vera, mycosis fungoides, and bronchogenic carcinoma. Also for the palliative treatment of metastatic carcinoma resulting in effusion.

PHARMACODYNAMICS:
Mechlorethamine also known as mustine, nitrogen mustard, and HN2, is the prototype anticancer chemotherapeutic drug. Successful clinical use of mechlorethamine gave birth to the field of anticancer chemotherapy. The drug is an analogue of mustard gas and was derived from toxic gas warfare research. It belongs to the group of nitrogen mustard alkylating agents. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.

MECHANISM OF ACTION:
Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations. Mechlorethamine is cell cycle phase-nonspecific.

PROTEIN BINDING:
Not Available

METABOLISM:
Undergoes rapid chemical transformation and combines with water or reactive compounds of cells, so that the drug is no longer present in active form a few minutes after administration.

TOXICITY:
Symptoms of overexposure include severe leukopenia, anemia, thrombocytopenia, and a hemorrhagic diathesis with subsequent delayed bleeding may develop. Death may follow. The intravenous LD50 is 2 mg/kg and 1.6 mg/kg in mouse and rat, respectively.

AFECTED ORGANISMS:
Humans and other mammals