Drug information of Mechlorethamine

Mechlorethamine

Drug group:

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. 

Mechanism of effect

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.

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. Mechlorethamine 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.

Pharmacokinetics

Absorption

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

Volume of distribution

Not Available

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.

Route of elimination

Not Available

Half-life

15 minutes

Clearance

Not Available

Drug indications

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.

Dosage

Leukemia/Lymphomas/Polycythemia Vera/Mycosis Fungoides/Bronchogenic Carcinoma

0.4 mg/kg IV divided over 2 or 4 days  

Combo treatment (MOPP regimen): 6 mg/m²/day IV days 1 and 8 q4Weeks

Do not repeat course until WBC >1000/mm³ & platelets >50 k/mm³

Metastatic Carcinoma

Intracavitary: 0.4 mg/kg once  

Intrapericardial: 0.2 mg/kg once

Drug contraindications

Hypersensitivity, history of anaphylaxis

Active infection

Side effects

  • Nausea and vomiting.  Usually occurs within first 3 hours after drug administration.  You will be given anti-nausea medication before receiving drug.
  • Hair loss
  • Mouth sores
  • Darkening of veins used for infusion
  • Redness, dryness, irritation with topical use
  • Loss of fertility.  Meaning, your ability to conceive or father a child may be affected by mechlorethamine.  Discuss this issue with your health care provider.
  • Fever
  • Diarrhea
  • Poor appetite
  • Taste changes (metallic taste)
  • Ringing in the ears (tinnitus) (see hearing problems)
  • Abnormal blood tests: increased uric acid levels

Alerts

  • Before starting mechlorethamine treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.).   Do not take aspirin, or products containing aspirin unless your doctor specifically permits this.
  • Do not receive any kind of immunization or vaccination without your doctor's approval while taking mechlorethamine.
  • Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Pregnancy category D (mechlorethamine may be hazardous to the fetus.  Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus).
  • For both men and women: Do not conceive a child (get pregnant) while taking mechlorethamine. Barrier methods of contraception, such as condoms, are recommended. Discuss with your doctor when you may safely become pregnant or conceive a child after therapy.
  • Do not breast feed while taking this medication.
  • If redness or swelling is noted at the IV infusion site, apply ice and notify your health care professional immediately.
  • Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
  • You may be at risk of infection so try to avoid crowds or people with colds and those not feeling well, and report fever or any other signs of infection immediately to your health care provider.
  • Wash your hands often.
  • To help treat/prevent mouth sores, use a soft toothbrush, and rinse three times a day with 1/2 to 1 teaspoon of baking soda and/or 1/2 to 1 teaspoon of salt mixed with 8 ounces of water.
  • Use an electric razor and a soft toothbrush to minimize bleeding.
  • Avoid contact sports or activities that could cause injury.
  • To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals. 
  • Avoid sun exposure.  Wear SPF 15 (or higher) sunblock and protective clothing.
  • In general, drinking alcoholic beverages should be kept to a minimum or avoided completely.  You should discuss this with your doctor.
  • Get plenty of rest. 
  • Maintain good nutrition.
  • If you experience symptoms or side effects, be sure to discuss them with your health care team.  They can prescribe medications and/or offer other suggestions that are effective in managing such problems.

Pregnancy level

D group

Related drugs

Lomustine


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