Mechlorethamine Hydrochloride

Trade Names:
Mustargen
- Powder for injection 10 mg

Pharmacology

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An alkylating agent with cytotoxic, mutagenic, and radiomimetic actions that inhibit rapidly proliferating cells.

Pharmacokinetics

Metabolism

Mechlorethamine is rapidly inactivated in body fluids or water within a few minutes.

Elimination

Apparently eliminated renally.

Onset

Onset happens within a few seconds or minutes.

Indications and Usage

Hodgkin disease (stage III and IV), lymphosarcoma, chronic myelocytic or lymphocytic leukemia, polycythemia vera, mycosis fungoides (topical), bronchogenic carcinoma; palliative treatment of malignant effusion (intrapleural, intraperitoneal, or intrapericardial use only).

Contraindications

Infectious disease; previous anaphylactic reactions to the drug.

Dosage and Administration

IV Total dose of 0.4 mg/kg of body weight for each course (as single dose or divided doses of 0.1 to 0.2 mg/kg/day). Dose based on ideal dry body weight. May repeat courses as early as 3 wk after treatment.

General Advice

• For IV and intracavitary administration only. Not for intradermal, subcutaneous, IM, intraarterial, or oral administration.
• Examine vial before reconstitution. Do not use if droplets of water are visible.
• Reconstitute powder with 10 mL sterile water for injection or sodium chloride injection. Resulting solution contains 1 mg/mL of mechlorethamine.
• Do not administer if particulate matter, cloudiness, or discoloration noted.
• Premedicate patient with antiemetics and sedatives as ordered by health care provider.
• If possible, administer at night when sedation for adverse reactions is required.
• To reduce risk of extravasation, inject prescribed dose into the rubber or plastic tubing of a freely flowing IV infusion set.
• To reduce loss of potency, administer prescribed dose immediately after reconstitution by IV infusion over a few minutes. Do not add to entire volume of infusion solution.
• Dispose of mechlorethamine vials and any remaining solution after neutralizing with an equal volume of sodium thiosulfate 5% and sodium bicarbonate 5% solution. Allow mixture to stand for 45 min.
• Decontaminate administration equipment (eg, rubber gloves, tubing, glassware) by soaking in solution containing equal volumes of sodium thiosulfate 5% and sodium bicarbonate 5% for 45 min.

Storage/Stability

Store unopened vials at controlled room temperature (59° to 86°F). Protect from light and humidity. Administer solution immediately after reconstitution.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Dermatologic

Alopecia; erythema multiforme; herpes zoster; maculopapular eruptions.

EENT

Diminished hearing; tinnitus; vertigo.

GI

Anorexia; diarrhea; nausea; vomiting.

Genitourinary

Azoospermia; total germinal aplasia; impaired spermatogenesis; amenorrhea; delayed menses; oligomenorrhea; hyperuricemia.

Hematologic

Agranulocytosis; granulocytopenia; hematopoietic depression; hyperheparinemia; lymphocytopenia; thrombocytopenia; hemolytic anemia; pancytopenia.

Hepatic

Jaundice.

Local

Extravasation; thrombosis; thrombophlebitis.

Miscellaneous

Chromosomal abnormalities; anaphylaxis.

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy in children not established.

Hypersensitivity

Reactions, including anaphylaxis, have occurred.

Carcinogenesis

Therapy with nitrogen mustard may be associated with an increased incidence of second malignant tumor.

Fertility

Impaired spermatogenesis, azoospermia, and total germinal aplasia have occurred in men.

Amyloidosis

Nitrogen mustard therapy may contribute to extensive and rapid development of amyloidosis; use only if foci or acute and chronic suppurative inflammation are absent.

Chronic lymphatic leukemia

Drug toxicity, especially sensitivity to bone marrow failure, appears to be more common in chronic lymphatic leukemia than in other conditions; administer with great caution in this condition, if at all.

GI

Nausea and vomiting usually begins 1 to 3 h after use. Vomiting may persist for the first 8 h, nausea for 24 h.

Hematologic

The usual course of treatment produces lymphocytopenia within 24 h after the first injection; significant granulocytopenia occurs within 6 to 8 days and lasts for 10 days to 3 wk. Severe thrombocytopenia may lead to bleeding from the gums and GI tract, petechiae, and small subcutaneous hemorrhages. Erythrocyte and hemoglobin levels may decline, but rarely significantly, during the first 2 wk after therapy. Depression of the hematopoietic system may occur up to 50 days or more after starting therapy.

Herpes zoster

Herpes zoster, common with lymphomas, may first appear after therapy is instituted and may be precipitated by treatment.

Hyperuricemia

Urate precipitation may develop during therapy, particularly in the treatment of lymphomas.

Intercavitary administration

Pain occurs rarely with intrapleural use; it is common with intraperitoneal injection and is often associated with nausea, vomiting, and diarrhea of 2 to 3 days' duration. Transient cardiac irregularities may occur with intrapericardial injection.

Tumors

Tumors of bone and nervous tissue respond poorly to therapy.

Overdosage

Symptoms

Severe leukopenia, anemia, thrombocytopenia, hemorrhagic diathesis, death.

Patient Information

• Advise patient, family, or caregiver that medication will be prepared and administered by health care provider in a health care setting.
• Advise patient, family, or caregiver that medication may be used in combination with other agents, including antiemetics and sedatives, to achieve max benefit possible.
• Advise patient, family, or caregiver to immediately report any of the following to health care provider: rash; hives; difficulty breathing; fever, chills, or other signs of infection; unusual bleeding or bruising; pain, redness, or swelling at injection site.
• Advise patient, family, or caregiver to report any of the following to health care provider: persistent nausea, vomiting, diarrhea, or appetite loss; persistent or worsening general body weakness.
• Caution women of childbearing potential to avoid becoming pregnant during therapy.
• Advise men that therapy may temporarily or permanently impair fertility.
• Advise patient, family, or caregiver that, following discharge, frequent follow-up visits and laboratory tests will be required to monitor therapy and to keep appointments.

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