Mechlorethamine

What is Mechlorethamine?

• Mechlorethamine (Mustargen), an antineoplastic nitrogen mustard also known as HN2 hydrochloride, Chlormethine, mustine and embikhin, is a nitrogen analog of sulfur mustard.

Mechlorethamine

Mechlorethamine 3D spacefill

Mechlorethamine 3D ball

What are the uses of this medicine?

• Mechlorethamine (Mustargen), administered intravenously, is indicated 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.
• Mechlorethamine (Mustargen), administered intrapleurally, intraperitoneally, or intrapericardially, is indicated for the palliative treatment of metastatic carcinoma resulting in effusion.

How does this medicine work?

• The hydrochloride salt of mechlorethamine, a nitrogen mustard and an analogue of sulfur mustard, with antineoplastic and immunosuppressive activities.
• Mechlorethamine is metabolized to an unstable, highly reactive ethyleniminium intermediate that alkylates DNA, particularly the 7 nitrogen of guanine residues, resulting in DNA base pair mismatching, DNA interstrand crosslinking, the inhibition of DNA repair and synthesis, cell-cycle arrest, and apoptosis.
• This agent also exhibits lympholytic properties.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• the presence of known infectious diseases and in patients who have had previous anaphylactic reactions to Mustargen.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Is this medicine FDA approved?

• Mechlorethamine was approved for use in the United States in 1949.
• Its major use has been as therapy of Hodgkin’s disease and lymphomas in a regimen with vincristine, procarbazine and prednisone, commonly referred to as MOPP.
• In recent years, mechlorethamine has been replaced by more stable alkylating agents such as cyclophosphamide (COPP).
• Current indications include Hodgkin's disease, lymphosarcoma, chronic leukemias, polycytehemia vera, mycosis fungoides and lung cancer.
• Mechlorethamine is available in 10 mg vials generically and under the brand name Mustargen.

How should this medicine be used?

Recommended dosage:

• A total dose of 0.4 mg/kg of body weight for each course usually is given either as a single dose or in divided doses of 0.1 to 0.2 mg/kg per day.
• Dosage should be based on ideal dry body weight.

Administration:

• Mechlorethamine comes as powder to be mixed with liquid to be injected intravenously (into a vein) by a doctor or nurse in a medical facility.
• It may also be injected intraperitoneally (into the abdominal cavity), [[]]intrapleurally (into the chest cavity), or intrapericardially (into the lining of the heart).
• The length of treatment depends on the types of drugs you are taking, how well your body responds to them, and the type of cancer or condition you have.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As powder to be mixed with liquid

This medicine is available in fallowing brand namesː

• Mustargen

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• vomiting
• loss of appetite
• diarrhea
• unusual tiredness or weakness
• dizziness
• painful, swollen joints
• ringing in ears and difficulty hearing

Less common, but serious side effects may include:

• Hypersensitivity reactions, including anaphylaxis
• Jaundice, alopecia, vertigo, tinnitus and diminished hearing
• hemolytic anemia
• chromosomal abnormalities
• maculopapular skin eruption
• Erythema multiforme
• delayed catamenia
• oligomenorrhea
• temporary or permanent amenorrhea
• spermatogenesis
• azoospermia
• total germinal aplasia

What special precautions should I follow?

• Tell your doctor if you have previously received or will be receiving radiation (x-ray) therapy or other chemotherapy and if you have or have ever had any medical conditions.
• Mechlorethamine may interfere with the normal menstrual cycle (period) in women, may stop sperm production in men, and may cause infertility (difficulty becoming pregnant). However, you should not assume that you or your partner cannot become pregnant.
• Tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. You should not become pregnant or breast-feed while you are receiving mechlorethamine injection. Mechlorethamine may harm the fetus.
• This drug is HIGHLY TOXIC and both powder and solution must be handled and administered with care.
• The use of Mustargen in patients with leukopenia, thrombocytopenia, and anemia, due to invasion of the bone marrow by tumor carries a greater risk.
• Mustargen has been reported to have immunosuppressive activity. Therefore, it should be borne in mind that use of the drug may predispose the patient to bacterial, viral or fungal infection.
• Hyperuricemia may develop during therapy with Mustargen. Adequate methods for control of hyperuricemia should be instituted and careful attention directed toward adequate fluid intake before treatment.
• Many abnormalities of renal, hepatic, and bone marrow function have been reported in patients with neoplastic disease and receiving mechlorethamine. It is advisable to check renal, hepatic, and bone marrow functions frequently.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• fever, chills, sore throat, ongoing cough and congestion, or other signs of an infection
• unusual bleeding or bruising
• bloody or black, tarry stools
• bloody vomit
• vomited material that looks like coffee grounds

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Pregnancy Category D.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established by well-controlled studies.
• Use of Mustargen in pediatric patients has been quite limited.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• mechlorethamine hydrochloride

Inactive Ingredients:

• sodium chloride

Who manufactures and distributes this medicine?

• Merck&co.,Inc.
• Whitehouse station, NJ, USA

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 15-30°C (59-86°F).
• Protect from light and humidity.
• Solutions of mechlorethamine HCl decompose on standing; therefore, solutions of the drug should be prepared immediately before use.

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• Dailymed label info on Mechlorethamine
• FDA Mechlorethamine

Mechlorethamine Resources
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