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mechlorethamine; nitrogen mustard (Mustargen, Nor-mustard, Chlorethazine)

Tradename: Mustargen. Indications: 1) brain tumors 2) Hodgkin's disease 3) non-Hodgkin's lymphoma 4) chronic leukemias 5) malignant effusions (intracavitary injections) - malignant ascites 6) mycosis fungoides 7) palliative treatment of: a) bronchogenic carcinoma b) breast carcinoma c) ovarian carcinoma 8) polycythemia vera Contraindications: 1) severe myelosuppression 2) infection Dosage: 1) Hodgkin's lymphoma: 6 mg/m2 IV on days 1 & 8, repeated monthly 2) as single agent: 0.4 mg/kg/month 3) intracavitary: 0.4 mg/kg 4) topically: 0.17 mg/mL applied daily Powder for injection: 10 mg. Pharmacokinetics: 1) rapidly deactivated in blood 2) 1/2life is 12-15 minutes Adverse effects: 1) common (> 10%) - bone marrow suppression (dose-related) - leukopenia & thrombocytopenia may be severe - onset: 4-7 days - nadir: 14 days - recovery: 21 days - moderate to severe nausea/vomiting - reproductive dysfunction - amenorrhea (may be temporary or pemanent) - impaired spermatogenesis (may return to normal after several years) - chromosomal abnormalities - precipitation of Herpes zoster (shingles) - ototoxicity 2) less common (1-10%) - thrombosis, diarrhea, anorexia, metallic taste, secondary malignancies*, thrombophlebitis, tissue necrosis with extravasation# 3) uncommon (< 1%) - allergic reactions, hepatotoxicity, peptic ulcer, peripheral neuropathy, vertigo, tinnitus, rash, hemolytic anemia, weakness, hypersensitivity 4) other - stomatitis * secondary malignancies occur in 1-6% of patients after several years # sodium thiosulfate is a specific antidote for nitrogen mustard extravasations Test interactions: increases serum K+ Mechanism of action: 1) alkylating agent 2) interferes with DNA & RNA synthesis Mechanism of drug resistance: - defective transport via the choline transporter Notes: - not related to the mustard plant [5]

Interactions

drug adverse effects of alkylating agents

Related

choline transporter

General

alkylating agent nitrogen mustard

Properties

MISC-INFO: elimination route PLASMA pregnancy-category X safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 533
  4. Deprecated Reference
  5. Wikipedia: Nitrogen Mustard http://en.wikipedia.org/wiki/Nitrogen_mustard

Component-of

estramustine (Emcyt) nitrogen mustard/vincristine (Oncovin)/prednisone/ procarbazine (MOPP)