Mechlorethamine hydrochloride

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Mechlorethamine hydrochloride
(Nitrogen mustard)

Mechlorethamine hydrochloride (Mustargen)
Nitrogen mustard (Mustargen)
Mechlorethamine hydrochloride
(meh-klor- ETH-ah-meen)
Pregnancy Category: D Mustargen (Rx)

Classification: Antineoplastic, alkylating agent

See Also: See also Antineoplastic Agents and Alkylating Agents .

Action/Kinetics: Cell-cycle nonspecific. Forms an unstable ethylenimmonium ion, which then alkylates or binds with various compounds, including nucleic acids. Cytotoxic activity is due to cross-linking of DNA and RNA strands and protein synthesis. When used for intracavitary tumors, exerts both an inflammatory reaction and sclerosis on serous membranes, which causes adherence of the drug to serosal surfaces. Reacts rapidly with tissues and within minutes after administration the active drug is no longer present. Metabolites are excreted through the urine.

Uses: IV: Bronchogenic carcinoma; CLL and CML; palliative treatment of stages III and IV of Hodgkin's disease, polycythemia vera, mycosis fungoides, lymphosarcoma. Intracavity: Intrapericardial, intraperitoneal, or intrapleural: Metastatic carcinoma resulting in effusion. Investigational: Topical: Cutaneous mycosis fungoides.

Contraindications: Lactation. During infectious disease.

Special Concerns: Extravasation into SC areas causes painful inflammation and induration. Use in children has been limited although the drug has been used in MOPP (mechlorethamine, Oncovin, procarbazine, prednisone) therapy.

Additional Side Effects: High incidence of N&V. Amyloidosis, hyperuricemia, petechiae, SC hemorrhages, tinnitus, deafness, herpes zoster, or temporary amenorrhea. Extravasation into SC tissue causes painful inflammation.

Drug Interactions: Amphotericin B: Combination possibility of blood dyscrasias.

How Supplied: Powder for injection: 10 mg

Adults, children: a total dose of 0.4 mg/kg per course of therapy given as a single dose or in two to four divided doses of 0.1-0.2 mg/kg over 2-4 days. Depending on blood cell count, a second course may be given after 3 weeks.
?Intrapleural, Intraperitoneal, Intrapericardial
0.4 mg/kg (0.2 mg/kg has been used intrapericardially).
?Topical Ointment, Solution
Apply to entire skin surface once daily until 6-12 months after a complete response is obtained; then, use once to several times a week for up to 3 years.

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