Chlormethine
Chlormethine Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
Chlormethine 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. Chlormethine is a nitrogen mustard alkylating agent. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.
| Trade Name | Chlormethine |
| Availability | Discontinued |
| Generic | Mechlorethamine |
| Mechlorethamine Other Names | Chlormethine, Chlormethinum, Clormetina, Mechlorethamine, Mustine, Nitrogen mustard |
| Related Drugs | prednisone, methotrexate, dexamethasone, Decadron, carboplatin, fluorouracil, doxorubicin, cyclophosphamide, Deltasone, vincristine |
| Type | |
| Formula | C5H11Cl2N |
| Weight | Average: 156.054 Monoisotopic: 155.026854771 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Chlormethine is an antineoplastic agent used to treat Hodgkin's disease, lymphosarcoma, and chronic myelocytic or lymphocytic leukemia.
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.
Chlormethine is also used to associated treatment for these conditions: Carcinoma, Bronchogenic, Chronic Lymphocytic Leukaemia (CLL), Hodgkins Disease (HD), Lymphoma, Diffuse, Mycosis Fungoides (MF), Polycythemia Vera (PV), Stage I Mycosis Fungoides, Malignant effusion
How Chlormethine works
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. Chlormethine is cell cycle phase-nonspecific.
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 ulceration or blistering, and hyperpigmentation. The oral LD50 for a rat is 10 mg/kg.
Food Interaction
No interactions found.Chlormethine Drug Interaction
Moderate: fluorouracil, fluorouracil, bleomycin, bleomycin, daunorubicin, daunorubicin, cytarabine, cytarabineUnknown: risedronate, risedronate, doxorubicin, doxorubicin, aspirin, aspirin, pentosan polysulfate sodium, pentosan polysulfate sodium, estramustine, estramustine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids
Chlormethine Disease Interaction
Elimination Route
Partially absorbed following intracavitary administration, most likely due to rapid deactivation by body fluids. When it is topically administered, systemic exposure was undetectable.
Half Life
15 minutes
Innovators Monograph
You find simplified version here Chlormethine
