Description

Simple

A medication used to treat a number of cancers.

Clinical

An antineoplastic agent used to treat Hodgkin's disease, lymphosarcoma, and chronic myelocytic or lymphocytic leukemia.

Overview

A vesicant and necrotizing irritant destructive to mucous membranes, mechlorethamine is an alkylating drug. 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]

The FDA granted marketing approval for the orphan drug Valchlor (mechlorethamine) gel on August 23, 2013 for the topical treatment of stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma (CTCL) in patients who have received prior skin-directed therapy. Each tube of Valchlor contains 0.016% of mechlorethamine which is equivalent to 0.02% mechlorethamine HCL.

Pharmacology

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.

Pharmacodynamic

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.... Read more

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 form... Read more

Absorption

Partially absorbed following intracavitary administration, most likely due to rapid deactivation by body fluids. When it is topically administered, systemic exposure was undetectable.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

15 minutes

Route of elimination

Information currently not available.

Toxicity

Symptoms of overexposure include severe leukopenia, anemia, thrombocytopenia, and a hemorrhagic diathesis with subsequent delayed bleeding may develop. Death may follow. The most common adverse reactions (≥5%) of the topical formulation are dermatitis, pruritus, bacterial skin infection, skin ulcer... Read more

Adverse Effects

Contraindications

  • Route:
    • Intravenous
    • Intracavitary
  • Dose Form:
    • Injection
  • Hypersensitivity:
    • mechlorethamine
  • Regions: US
  • Route:
    • Intravenous
    • Intracavitary
  • Dose Form:
    • Injection
  • Regions: US
  • Patient Conditions:
      • Name: Infectious Diseases
      • Drugbank Id: DBCOND0028267

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Mechlorethamine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding can be increased when (R)-warfarin is combined with Mechlorethamine.
(S)-Warfarin
The risk or severity of bleeding can be increased when (S)-Warfarin is combined with Mechlorethamine.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with 2-Methoxyethanol.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Mechlorethamine.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abatacept
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Mechlorethamine.
Abetimus
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Abetimus.
Acebutolol
Mechlorethamine may increase the bradycardic activities of Acebutolol.
Acenocoumarol
The risk or severity of bleeding can be increased when Acenocoumarol is combined with Mechlorethamine.
Acetylcholine
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Acetylcholine.
Acetyldigitoxin
Acetyldigitoxin may decrease the cardiotoxic activities of Mechlorethamine.
Acetyldigoxin
Acetyldigoxin may decrease the cardiotoxic activities of Mechlorethamine.
Acetylsalicylic acid
The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Mechlorethamine.
Aclidinium
The therapeutic efficacy of Aclidinium can be decreased when used in combination with Mechlorethamine.
Acteoside
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Acteoside.
Adalimumab
The risk or severity of adverse effects can be increased when Adalimumab is combined with Mechlorethamine.
Adenovirus type 7 vaccine live
The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Mechlorethamine.
Afelimomab
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Afelimomab.
Agmatine
The therapeutic efficacy of Agmatine can be decreased when used in combination with Mechlorethamine.