Mechlorethamine HCl (Mustargen)
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Mechlorethamine HCl (Mustargen)

MUSTARGEN®
(mechlorethamine HCl) for Injection

WARNINGS

MUSTARGEN (Mechlorethamine HCl) should be administered only under the supervision of a physician who is experienced in the use of cancer chemotherapeutic agents.

This drug is HIGHLY TOXIC and both powder and solution must be handled and administered with care. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Avoid exposure during pregnancy. Due to the toxic properties of mechlorethamine (e.g., corrosivity, carcinogenicity, mutagenicity, teratogenicity), special handling procedures should be reviewed prior to handling and followed diligently.

Extravasation of the drug into subcutaneous tissues results in a painful inflammation. The area usually becomes indurated and sloughing may occur. If leakage of drug is obvious, prompt infiltration of the area with sterile isotonic sodium thiosulfate (1/6 molar) and application of an ice compress for 6 to 12 hours may minimize the local reaction. For a 1/6 molar solution of sodium thiosulfate, use 4.14 g of sodium thiosulfate per 100 mL of Sterile Water for Injection or 2.64 g of anhydrous sodium thiosulfate per 100 mL or dilute 4 mL of Sodium Thiosulfate Injection (10%) with 6 mL of Sterile Water for Injection.

DRUG DESCRIPTION

MUSTARGEN (mechlorethamine hcl) , an antineoplastic nitrogen mustard also known as HN2 hydrochloride, is a nitrogen analog of sulfur mustard. It is a light yellow brown, crystalline, hygroscopic powder that is very soluble in water and also soluble in alcohol.

Mechlorethamine hydrochloride is designated chemically as 2-chloro-N-(2-chloroethyl)-N-methylethanamine hydrochloride. The molecular weight is 192.52 and the melting point is 108-111°C. The empirical formula is C5H11Cl2N•HCl, and the structural formula is: CH3N(CH2CH2Cl)2•HCl.

Trituration of MUSTARGEN (mechlorethamine hcl) is a sterile, light yellow brown crystalline powder for injection by the intravenous or intracavitary routes after dissolution. Each vial of MUSTARGEN (mechlorethamine hcl) contains 10 mg of mechlorethamine hydrochloride triturated with sodium chloride q.s. 100 mg. When dissolved with 10 mL Sterile Water for Injection or 0.9% Sodium Chloride Injection, the resulting solution has a pH of 3-5 at a concentration of 1 mg mechlorethamine HCl per mL.

What are the possible side effects of mechlorethamine (Mustargen)?

If you experience any of the following serious side effects, seek emergency medical attention or contact your doctor immediately:

  • an allergic reaction (shortness of breath; closing of your throat; difficulty breathing; swelling of your lips, face, or tongue; or hives);
  • blood in the urine;
  • black or tarry stools;
  • signs of infection such as fever; chills, or sore throat;
  • joint pain and stiffness similar to gout (high levels of uric acid in the blood);
  • jaundice (yellowing of the skin or eyes);or
  • unusual bleeding or...

Read All Potential Side Effects and See Pictures of Mustargen »

What are the precautions when taking mechlorethamine hcl (Mustargen)?

Before receiving mechlorethamine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood/bleeding disorders (e.g., anemia, low blood cell counts), gout, current infection, kidney disease, liver disease, radiation treatment.

Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose. Wash your hands well to prevent the spread of infections.

To lower your...

Read All Potential Precautions of Mustargen »

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

Before using MUSTARGEN see CONTRAINDICATIONS, WARNINGS, PRECAUTIONS, ADVERSE REACTIONS, DOSAGE AND ADMINISTRATION, and HOW SUPPLIED, Special Handling.

MUSTARGEN (mechlorethamine hcl) , 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.

MUSTARGEN (mechlorethamine hcl) , administered intrapleurally, intraperitoneally, or intrapericardially, is indicated for the palliative treatment of metastatic carcinoma resulting in effusion.

DOSAGE AND ADMINISTRATION

Not for oral administration

Intravenous Administration

The dosage of MUSTARGEN (mechlorethamine hcl) varies with the clinical situation, the therapeutic response and the magnitude of hematologic depression. 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. The presence of edema or ascites must be considered so that dosage will be based on actual weight unaugmented by these conditions.

The margin of safety in therapy with MUSTARGEN (mechlorethamine hcl) is narrow and considerable care must be exercised in the matter of dosage. Repeated examinations of blood are mandatory as a guide to subsequent therapy. (See OVERDOSAGE.)

Within a few minutes after intravenous injection, MUSTARGEN (mechlorethamine hcl) undergoes chemical transformation, combines with reactive compounds, and is no longer present in its active form in the blood stream. Subsequent courses should not be given until the patient has recovered hematologically from the previous course; this is best determined by repeated studies of the peripheral blood elements awaiting their return to normal levels. It is often possible to give repeated courses of MUSTARGEN (mechlorethamine hcl) as early as three weeks after treatment.

Preparation of Solution for Intravenous Administration

This drug is HIGHLY TOXIC and both powder and solution must be handled and administered with care. (See Boxed Warning and DOSAGE AND ADMINISTRATION, Special Handling.) Since MUSTARGEN (mechlorethamine hcl) is a powerful vesicant, it is intended primarily for intravenous use, and in most cases is given by this route. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Appropriate protective equipment should be worn when handling MUSTARGEN (mechlorethamine hcl) . Should accidental eye contact occur, copious irrigation for at least 15 minutes with water, normal saline or a balanced salt ophthalmic irrigating solution should be instituted immediately, followed by prompt ophthalmologic consultation. Should accidental skin contact occur, the affected part must be irrigated immediately with copious amounts of water, for at least 15 minutes while removing contaminated clothing and shoes, followed by 2% sodium thiosulfate solution. Medical attention should be sought immediately. Contaminated clothing should be destroyed. (See DOSAGE AND ADMINISTRATION, Special Handling.)

Each vial of MUSTARGEN (mechlorethamine hcl) contains 10 mg of mechlorethamine hydrochloride triturated with sodium chloride q.s. 100 mg. In neutral or alkaline aqueous solution it undergoes rapid chemical transformation and is highly unstable. Although solutions prepared according to instructions are acidic and do not decompose as rapidly, they should be prepared immediately before each injection since they will decompose on standing. When reconstituted, MUSTARGEN (mechlorethamine hcl) is a clear colorless solution. Do not use if the solution is discolored or if droplets of water are visible within the vial prior to reconstitution.

Using a sterile 10 mL syringe, inject 10 mL of Sterile Water for Injection or 10 mL Sodium Chloride Injection into a vial of MUSTARGEN (mechlorethamine hcl) . With the needle (syringe attached) still in the rubber stopper, shake the vial several times to dissolve the drug completely. The resultant solution contains 1 mg of mechlorethamine hydrochloride per mL.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.

Special Handling

Animal studies have shown mechlorethamine to be corrosive to skin and eyes, a powerful vesicant, irritating to the mucous membranes of the respiratory tract and highly toxic by the oral route. It has also been shown to be carcinogenic, mutagenic and teratogenic. Due to the drug's toxic properties, appropriate precautions including the use of appropriate safety equipment are recommended for the preparation of MUSTARGEN (mechlorethamine hcl) for parenteral administration. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Avoid exposure during pregnancy. The National Institutes of Health presently recommends that the preparation of injectable antineoplastic drugs should be performed in a Class II laminar flow biological safety cabinet.17 Personnel preparing drugs of this class should wear chemical resistant, impervious gloves, safety goggles, outer garments and shoe covers. Additional body garments should be used based upon the task being performed (e.g., sleevelets, apron, gauntlets, disposable suits) to avoid exposed skin surfaces and inhalation of vapors and dust. Appropriate techniques should be used to remove potentially contaminated clothing.

Several other guidelines for proper handling and disposal of antineoplastic drugs have been published and should be considered.18-23

Accidental Contact Measures

Should accidental eye contact occur, copious irrigation for at least 15 minutes with water, normal saline or a balanced salt ophthalmic irrigating solution should be instituted immediately, followed by prompt ophthalmologic consultation. Should accidental skin contact occur, the affected part must be irrigated immediately with copious amounts of water, for at least 15 minutes while removing contaminated clothing and shoes, followed by 2% sodium thiosulfate solution. Medical attention should be sought

immediately. Contaminated clothing should be destroyed. (See PRECAUTIONS, General and DOSAGE AND ADMINISTRATION, Preparation of Solution for Intravenous Administration.)

Technique for Intravenous Administration

Withdraw into the syringe the calculated volume of solution required for a single injection. Dispose of any remaining solution after neutralization (see below). Although the drug may be injected directly into any suitable vein, it is injected preferably into the rubber or plastic tubing of a flowing intravenous infusion set. This reduces the possibility of severe local reactions due to extravasation or high concentration of the drug. Injecting the drug into the tubing rather than adding it to the entire volume of the infusion fluid minimizes a chemical reaction between the drug and the solution. The rate of injection apparently is not critical provided it is completed within a few minutes.

Intracavitary Administration

Nitrogen mustard has been used by intracavitary administration with varying success in certain malignant conditions for the control of pleural,4-13 peritoneal,5,6,9,11-16 and pericardial,5,11-13 effusions caused by malignant cells.

The technique and the dose used by any of these routes varies. Therefore, if MUSTARGEN (mechlorethamine hcl) is given by the intracavitary route, the published articles concerning such use should be consulted. Because of the inherent risks involved, the physician should be experienced in the appropriate injection techniques, and be thoroughly aware of the indications, dosages, hazards, and precautions as set forth in the published literature. When using MUSTARGEN (mechlorethamine hcl) by the intracavitary route, the general precautions concerning this agent should be borne in mind.

As a general guide, reference is made especially to the techniques of Weisberger et al.5,11-13 Intracavitary use is indicated in the presence of pleural, peritoneal, or pericardial effusion due to metastatic tumors. Local therapy with nitrogen mustard is used only when malignant cells are demonstrated in the effusion. Intracavitary injection is not recommended when the accumulated fluid is chylous in nature, since results are likely to be poor.

Paracentesis is first performed with most of the fluid being removed from the pleural or peritoneal cavity. The intracavitary use of MUSTARGEN (mechlorethamine hcl) may exert at least some of its effect through production of a chemical poudrage. Therefore, the removal of excess fluid allows the drug to more easily contact the peritoneal and pleural linings. For intrapleural or intrapericardial injection nitrogen mustard is introduced directly through the thoracentesis needle. For intraperitoneal injection it is given through a rubber catheter inserted into the trocar used for paracentesis or through a No. 18 gauge needle inserted at another site. This drug should be injected slowly, with frequent aspiration to ensure that a free flow of fluid is present. If fluid cannot be aspirated, pain and necrosis due to injection of solution outside the cavity may occur.5,11-13 Free flow of fluid also is necessary to prevent injection into a loculated pocket and to ensure adequate dissemination of nitrogen mustard.

The usual dose of nitrogen mustard for intracavitary injection is 0.4 mg/kg of body weight, though 0.2 mg/kg (or 10 to 20 mg) has been used by the intrapericardial route.5,11-13 The solution is prepared, as previously described for intravenous injection, by adding 10 mL of Sterile Water for Injection or 10 mL of Sodium Chloride Injection to the vial containing 10 mg of mechlorethamine hydrochloride. (Amounts of diluent of 50 to 100 mL of normal saline have also been used.4,5) The position of the patient should be changed every 5 to 10 minutes for an hour after injection to obtain more uniform distribution of the drug throughout the serous cavity. The remaining fluid may be removed from the pleural or peritoneal cavity by paracentesis 24 to 36 hours later. The patient should be followed carefully by clinical and x-ray examination to detect reaccumulation of fluid.

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. Death, possibly accelerated by nitrogen mustard, has been reported following the use of this agent by the intracavitary route.9 Although absorption of MUSTARGEN (mechlorethamine hcl) when given by the intracavitary route is probably not complete because of its rapid deactivation by body fluids, the systemic effect is unpredictable. The acute side effects such as nausea and vomiting are usually mild. Bone marrow depression is generally milder than when the drug is given intravenously. Care should be taken to avoid use by the intracavitary route when other agents which may suppress bone marrow function are being used systemically.

Neutralization of Equipment and Unused Solution

To clean rubber gloves, tubing, glassware, etc., after giving MUSTARGEN (mechlorethamine hcl) , soak them in an aqueous solution containing equal volumes of sodium thiosulfate (5%) and sodium bicarbonate (5%) for 45 minutes. Excess reagents and reaction products are washed away easily with water. Any unused injection solution should be neutralized by mixing with an equal volume of sodium thiosulfate/sodium bicarbonate solution. Allow the mixture to stand for 45 minutes. Vials that have contained MUSTARGEN (mechlorethamine hcl) should be treated in the same way with thiosulfate/bicarbonate solution before disposal.

HOW SUPPLIED

No. 7753 — Trituration of MUSTARGEN (mechlorethamine hcl) is a light yellow brown crystalline powder, each vial containing 10 mg of mechlorethamine hydrochloride with sodium chloride q.s. 100 mg, and is supplied as follows:

NDC 0006-7753-31 in treatment sets of 4 vials.

Storage

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.

REFERENCES

4. Bass, B.H.: Nitrogen mustard in the palliation of lung cancer, Brit. Med. J. 1: 617-620, Feb. 27, 1960.

5. Bonte, F.J.; Storaasli, J.P.; Weisberger, A.S.: Comparative evaluation of radioactive colloidal gold and nitrogen mustard in the treatment of serous effusions of neoplastic origin, Radiol. 67: 63-66, July 1956.

6. Fullerton, C.W.; Reed, P.I.: Nitrogen mustard in treatment of pleural and peritoneal effusions, Can. Med. Ass. J. 79: 190-191, Aug. 1, 1958.

7. Harris, M.S.: The use of chemotherapy for carcinoma of the lung, J. Int. Coll. Surg. 34: 666-673, Nov. 1960.

8. Hepper, N.G.G.; Carr, D.T.: Intrapleural use of nitrogen mustard in malignant pleural effusion, Minn. Med. 43: 374-376, June 1960.

9. Levison, V.B.: Nitrogen mustard in palliation of malignant effusions, Brit. Med. J. 1: 1143-1145, Apr. 22, 1961.

10. Taylor, L.: A technique for intrapleural administration of nitrogen mustard compounds, Amer. J. Med. Sci. 233: 538-541, May 1957.

11. Weisberger, A.S.: Direct instillation of nitrogen mustard in the management of malignant effusions, Ann. N.Y. Acad. Sci. 68: 1091-1096, Apr. 24, 1958.

12. Weisberger, A.S.; Bonte, F.J.; Suhrland, L.G.: Management of malignant serous effusions, Geriat. 11: 23-30, Jan. 1956.

13. Weisberger, A.S.; Levine, B.; Storaasli, J.P.: Use of nitrogen mustard in treatment of serous effusions of neoplastic origin, J. Amer. Med. Ass. 159: 1704-1707, Dec. 31, 1958.

14. Brown, F.E.; Wright, H.K.: Hypovolemia following intraperitoneal nitrogen mustard therapy, Surg. Gynecol. & Obstet. 121: 528-530, Sept. 1965.

15. Greenwald, E.S.: Cancer chemotherapy, N.Y. Med. J. 66: 2532-2548, Oct. 1, 1966.

16. Rohn, R.J.; Bond, W.H.: Some indications for the use of chemotherapy in neoplastic disorders, J. Ind. Med. Ass. 50: 417-428, Apr. 1957.

17. Recommendations for the Safe Handling of Parenteral Antineoplastic Drugs, NIH Publication No. 83-2621. For sale by the Superintendent of Documents, U.S. Government Printing Office, Washington, DC 20402.

18. AMA Council Report: Guidelines for Handling Parenteral Antineoplastics, JAMA 253: 1590-1592, 1985.

19. National Study Commission on Cytotoxic Exposure-Recommendations for Handling Cytotoxic Agents. Available from Louis P. Jeffrey, Sc. D., Chairman, National Study Commission on Cytotoxic Exposure, Massachusetts College of Pharmacy and Allied Health Sciences, 179 Longwood Avenue, Boston, Massachusetts 02115.

20. Clinical Oncological Society of Australia: Guidelines and recommendations for safe handling of antineoplastic agents, Med. J. Australia 1: 426-428, 1983.

21. Jones, R.B., et al: Safe handling of chemotherapeutic agents: A report from the Mount Sinai Medical Center, Ca - A Cancer Journal for Clinicians Sept/Oct, 258-263, 1983.

22. American Society of Hospital Pharmacists: Technical assistance bulletin on handling cytotoxic and hazardous drugs, Am. J. Hosp. Pharm. 47: 1033-1049, 1990.

23. Controlling Occupational Exposure to Hazardous Drugs (OSHA Work-Practice Guidelines), Am. J. Health-Syst. Pharm. 53: 1669-1685, 1996.

Merck& Co., Inc., Whitehouse Station, NJ 08889, USA.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Clinical use of MUSTARGEN (mechlorethamine hcl) usually is accompanied by toxic manifestations.

Local Toxicity

Thrombosis and thrombophlebitis may result from direct contact of the drug with the intima of the injected vein. Avoid high concentration and prolonged contact with the drug, especially in cases of elevated pressure in the antebrachial vein (e.g., in mediastinal tumor compression from severe vena cava syndrome).

General: Hypersensitivity reactions, including anaphylaxis, have been reported. Nausea, vomiting and depression of formed elements in the circulating blood are dose-limiting side effects and usually occur with the use of full doses of MUSTARGEN (mechlorethamine hcl) . Jaundice, alopecia, vertigo, tinnitus and diminished hearing may occur infrequently. Rarely, hemolytic anemia associated with such diseases as the lymphomas and chronic lymphocytic leukemia may be precipitated by treatment with alkylating agents including MUSTARGEN (mechlorethamine hcl) . Also, various chromosomal abnormalities have been reported in association with nitrogen mustard therapy.

MUSTARGEN (mechlorethamine hcl) is given preferably at night in case sedation for side effects is required. Nausea and vomiting usually occur 1 to 3 hours after use of the drug. Emesis may disappear in the first 8 hours, but nausea may persist for 24 hours. Nausea and vomiting may be so severe as to precipitate vascular accidents in patients with a hemorrhagic tendency. Premedication with antiemetics, in addition to sedatives, may help control severe nausea and vomiting. Anorexia, weakness and diarrhea may also occur.

Hematologic: The usual course of MUSTARGEN (mechlorethamine hcl) (total dose of 0.4 mg/kg either given as a single intravenous dose or divided into two or four daily doses of 0.2 or 0.1 mg/kg, respectively) generally produces a lymphocytopenia within 24 hours after the first injection; significant granulocytopenia occurs within 6 to 8 days and lasts for 10 days to 3 weeks. Agranulocytosis appears to be relatively infrequent and recovery from leukopenia in most cases is complete within two weeks of the maximum reduction. Thrombocytopenia is variable but the time course of the appearance and recovery from reduced platelet counts generally parallels the sequence of granulocyte levels. In some cases severe thrombocytopenia may lead to bleeding from the gums and gastrointestinal tract, petechiae, and small subcutaneous hemorrhages; these symptoms appear to be transient and in most cases disappear with return to a normal platelet count. However, a severe and even uncontrollable depression of the hematopoietic system occasionally may follow the usual dose of MUSTARGEN (mechlorethamine hcl) , particularly in patients with widespread disease and debility and in patients previously treated with other antineoplastic agents or x-ray. Persistent pancytopenia has been reported. In rare instances, hemorrhagic complications may be due to hyperheparinemia. Erythrocyte and hemoglobin levels may decline during the first 2 weeks after therapy but rarely significantly. Depression of the hematopoietic system may be found up to 50 days or more after starting therapy.

Integumentary: Occasionally, a maculopapular skin eruption occurs, but this may be idiosyncratic and does not necessarily recur with subsequent courses of the drug. Erythema multiforme has been observed. Herpes zoster, a common complicating infection in patients with lymphomas, may first appear after therapy is instituted and on occasion may be precipitated by treatment. Further treatment should be discontinued during the acute phase of this illness to avoid progression to generalized herpes zoster.

Reproductive: Since the gonads are susceptible to MUSTARGEN (mechlorethamine hcl) , treatment may be followed by delayed catamenia, oligomenorrhea, or temporary or permanent amenorrhea. Impaired spermatogenesis, azoospermia, and total germinal aplasia have been reported in male patients treated with alkylating agents, especially in combination with other drugs. In some instances spermatogenesis may return in patients in remission, but this may occur only several years after intensive chemotherapy has been discontinued. Patients should be warned of the potential risk to their reproductive capacity.

Read the Mustargen (mechlorethamine hcl) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

No information provided.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Before using MUSTARGEN (mechlorethamine hcl) , an accurate histologic diagnosis of the disease, a knowledge of its natural course, and an adequate clinical history are important. The hematologic status of the patient must first be determined. It is essential to understand the hazards and therapeutic effects to be expected. Careful clinical judgment must be exercised in selecting patients. If the indication for its use is not clear, the drug should not be used.

As nitrogen mustard therapy may contribute to extensive and rapid development of amyloidosis, it should be used only if foci of acute and chronic suppurative inflammation are absent.

Usage in Pregnancy

Mechlorethamine hydrochloride can cause fetal harm when administered to a pregnant woman. MUSTARGEN (mechlorethamine hcl) has been shown to produce fetal malformations in the rat and ferret when given as single subcutaneous injections of 1 mg/kg (2-3 times the maximum recommended human dose). There are no adequate and well-controlled studies in pregnant women. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should be advised to avoid becoming pregnant.

PRECAUTIONS

General

This drug is HIGHLY TOXIC and both powder and solution must be handled and administered with care. (See Boxed Warning and DOSAGE AND ADMINISTRATION, Special Handling.) Since MUSTARGEN (mechlorethamine hcl) is a powerful vesicant, it is intended primarily for intravenous use, and in most cases is given by this route. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Appropriate protective equipment should be worn when handling MUSTARGEN (mechlorethamine hcl) . Should accidental eye contact occur, copious irrigation for at least 15 minutes with water, normal saline or a balanced salt ophthalmic irrigating solution should be instituted immediately, followed by prompt ophthalmologic consultation. Should accidental skin contact occur, the affected part must be irrigated immediately with copious amounts of water, for at least 15 minutes while removing contaminated clothing and shoes, followed by 2% sodium thiosulfate solution. Medical attention should be sought immediately. Contaminated clothing should be destroyed. (See DOSAGE AND ADMINISTRATION, Special Handling.)

Because of the toxicity of MUSTARGEN (mechlorethamine hcl) , and the unpleasant side effects following its use, the potential risk and discomfort from the use of this drug in patients with inoperable neoplasms or in the terminal stage of the disease must be balanced against the limited gain obtainable. These gains will vary with the nature and the status of the disease under treatment. The routine use of MUSTARGEN (mechlorethamine hcl) in all cases of widely disseminated neoplasms is to be discouraged.

The use of MUSTARGEN (mechlorethamine hcl) in patients with leukopenia, thrombocytopenia, and anemia, due to invasion of the bone marrow by tumor carries a greater risk. In such patients a good response to treatment with disappearance of the tumor from the bone marrow may be associated with improvement of bone marrow function. However, in the absence of a good response or in patients who have been previously treated with chemotherapeutic agents, hematopoiesis may be further compromised, and leukopenia, thrombocytopenia and anemia may become more severe and lead to the demise of the patient.

Tumors of bone and nervous tissue have responded poorly to therapy. Results are unpredictable in disseminated and malignant tumors of different types.

Precautions must be observed with the use of MUSTARGEN (mechlorethamine hcl) and x-ray therapy or other chemotherapy in alternating courses. Hematopoietic function is characteristically depressed by either form of therapy, and neither MUSTARGEN (mechlorethamine hcl) following x-ray therapy nor x-ray therapy subsequent to the drug should be given until bone marrow function has recovered. In particular, irradiation of such areas as sternum, ribs, and vertebrae shortly after a course of nitrogen mustard may lead to hematologic complications.

MUSTARGEN (mechlorethamine hcl) 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 (mechlorethamine hcl) . The problem of urate precipitation should be anticipated, particularly in the treatment of the lymphomas, and adequate methods for control of hyperuricemia should be instituted and careful attention directed toward adequate fluid intake before treatment.

Since drug toxicity, especially sensitivity to bone marrow failure, seems to be more common in chronic lymphatic leukemia than in other conditions, the drug should be given in this condition with great caution, if at all.

Extreme caution must be used in exceeding the average recommended dose. (See OVERDOSAGE.)

Laboratory Tests

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.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Therapy with alkylating agents such as MUSTARGEN (mechlorethamine hcl) may be associated with an increased incidence of a second malignant tumor, especially when such therapy is combined with other antineoplastic agents or radiation therapy.

The International Agency for Research on Cancer has judged that mechlorethamine is a probable carcinogen in humans. This is supported by limited evidence of carcinogenicity in humans and sufficient evidence of carcinogenicity in animals. Young-adult female RF mice were injected intravenously with four doses of 2.4 mg/kg of mechlorethamine (0.1% solution) at 2-week intervals with observations for up to 2 years. An increased incidence of thymic lymphomas and pulmonary adenomas was observed. Painting mechlorethamine on the skin of mice for periods up to 33 weeks resulted in squamous cell tumors in 9 of 33 mice.

Mechlorethamine induced mutations in the Ames test, in E. coli, and Neurospora crassa. Mechlorethamine caused chromosome aberrations in a variety of plant and mammalian cells. Dominant lethal mutations were produced in ICR/Ha Swiss mice.

Mechlorethamine impaired fertility in the rat at a daily dose of 500 mg/kg intravenously for two weeks.

Pregnancy

Pregnancy Category D. See WARNINGS.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from MUSTARGEN (mechlorethamine hcl) , a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established by well-controlled studies. Use of MUSTARGEN (mechlorethamine hcl) in pediatric patients has been quite limited. MUSTARGEN (mechlorethamine hcl) has been used in Hodgkin's disease, stages III and IV, in combination with other oncolytic agents (MOPP schedule). The MOPP chemotherapy combination includes mechlorethamine, vincristine, procarbazine, and prednisone or prednisolone.2,3

Geriatric Use

Clinical studies of MUSTARGEN (mechlorethamine hcl) did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

REFERENCES

2. Kolygin, B.A.: Combination chemotherapy of Hodgkin's disease in children, Cancer Philadelphia 38: 1494-1497, Oct. 1976.

3. Young, R.C.; DeVita, V.T.; Johnson, R.E.: Hodgkin's disease in childhood, Blood 42: 163-174, Aug. 1973.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

With total doses exceeding 0.4 mg/kg of body weight for a single course, severe leukopenia, anemia, thrombocytopenia and a hemorrhagic diathesis with subsequent delayed bleeding may develop. Death may follow. The only treatment in instances of excessive dosage appears to be repeated blood product transfusions, antibiotic treatment of complicating infections and general supportive measures.

The intravenous LD50 of MUSTARGEN (mechlorethamine hcl) is 2 mg/kg and 1.6 mg/kg in the mouse and rat, respectively. The oral LD50 for mechlorethamine hydrochloride is 20 mg/kg and 10 mg/kg in the mouse and rat, respectively.

CONTRAINDICATIONS

The use of MUSTARGEN (mechlorethamine hcl) is contraindicated in the presence of known infectious diseases and in patients who have had previous anaphylactic reactions to MUSTARGEN (mechlorethamine hcl) .

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Mechlorethamine, a biologic alkylating agent, has a cytotoxic action which inhibits rapidly proliferating cells.

Pharmacokinetics and Metabolism

In water or body fluids, mechlorethamine 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.1

REFERENCES

1. Calabresi, P.; Parks, R.E., Jr.: Antiproliferative agents and drugs used for immunosuppression, in "The Pharmacological Basis of Therapeutics", L.S. Goodman; A. Gilman (eds.), Ed. 6, New York, Macmillan, 1980, p. 1263.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

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PATIENT INFORMATION

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last reviewed on RxList: 5/21/2009
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Mustargen Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

MECHLORETHAMINE - INJECTION

(MEH-klor-ETH-uh-meen)

COMMON BRAND NAME(S): Mustargen

WARNING: Mechlorethamine must be handled and used very carefully. Direct contact with the skin, nose, mouth, or eyes may cause severe damage. Precautions (e.g., wearing a mask/outer garment/gloves) should be taken to prevent direct contact or breathing the dust/vapors from this medication.

Mechlorethamine is usually given by injection into a vein. If this medication accidentally leaks into the skin/muscle around the injection site, it may cause severe damage. Tell your doctor immediately if you notice hardening/peeling of the skin, redness, pain, or swelling at or near the injection site. Prompt treatment (e.g., ice compress, thiosulfate solution) may lessen damage.

USES: Meclorethamine is used to treat various types of cancer (e.g., Hodgkin's disease, non-Hodgkin's lymphoma). It works by slowing or stopping the growth of cancer cells.

HOW TO USE: This medication is usually given by injection into a vein by a health care professional, as directed by your doctor. It may also be given by placing within certain parts of the body (e.g., chest, abdomen) or applying to the skin (for certain skin conditions). Dosage is based on your medical condition, body size, and response to treatment.

If this medication touches your skin, immediately remove any clothing/shoes that may have been in contact with the medication, and wash the area well with water for at least 15 minutes. Then apply a certain solution (thiosulfate) to help reduce skin damage. If this medication gets in your eye, open the eyelid and flush well with water or balanced salt solution for 15 minutes, then seek immediate medical attention.

Drink plenty of fluids while using this medication unless otherwise directed by your doctor. Doing so may help decrease the risk of certain side effects (e.g., increased uric acid).

Disclaimer

Mustargen Consumer (continued)

SIDE EFFECTS: See also Warning section.

Nausea, vomiting, loss of appetite, diarrhea, headache, confusion, drowsiness, metallic taste in the mouth, or weakness may occur. Nausea and vomiting can be severe. In some cases, your doctor may prescribe medication to prevent or relieve nausea and vomiting. Eating several small meals, not eating before treatment, or limiting activity may help lessen some of these effects. If these effects persist or worsen, tell your doctor or pharmacist promptly.

Severe nausea, vomiting, and diarrhea may infrequently result in a loss of too much body water (dehydration). Contact your doctor promptly if you notice any symptoms of dehydration such as unusual decreased urination, unusual dry mouth/increased thirst, lack of tears, dizziness/lightheadedness, or pale/wrinkled skin.

Temporary hair loss may occur. Normal hair growth should return after treatment has ended.

Many people using this medication have serious side effects. However, your doctor has prescribed this drug because he or she has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.

Tell your doctor right away if you have any serious side effects, including: hearing changes (decreased hearing, ringing in ears), menstrual changes (e.g., stopped periods), numbness/tingling, unusual bleeding/bruising (e.g., small red spots on the skin, black/bloody stools, bloody urine, vomit that looks like coffee grounds), urination changes (e.g., decreased/painful urination).

This medication can lower the body's ability to fight an infection. Tell your doctor promptly if you develop any signs of an infection such as fever, chills, or persistent sore throat.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the Mustargen (mechlorethamine hcl) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before receiving mechlorethamine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood/bleeding disorders (e.g., anemia, low blood cell counts), gout, current infection, kidney disease, liver disease, radiation treatment.

Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose. Wash your hands well to prevent the spread of infections.

To lower your risk of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.

Before having surgery, tell your doctor or dentist that you are using this medication.

This drug may make you drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

Very rarely, people with cancer who are treated with this type of medication have developed other cancers (e.g., secondary tumor). The risk may be increased when this medication is given with certain other anti-cancer drugs (especially in high doses) or radiation treatment. Consult your doctor for more details.

This medication may affect the production of sperm, increasing the risk of fathering a child with birth defects. Therefore, men receiving treatment with this drug should use reliable forms of birth control (e.g., condoms). Consult your doctor for details and to discuss effective forms of birth control.

This medication is not recommended for use during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, tell your doctor immediately. To avoid pregnancy, both males and females using this drug should use reliable form(s) of birth control (e.g., birth control pills, condoms) during treatment. Consult your doctor for details and to discuss effective forms of birth control.

It is not known whether this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

Disclaimer

Mustargen Consumer (continued)

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Some products that may interact with this drug include: other anti-cancer drugs, nalidixic acid.

A certain spice (turmeric) may decrease the effect of mechlorethamine. Avoid using turmeric in your diet while receiving treatment with this medication. Consult your doctor or pharmacist for more details.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Laboratory and/or medical tests (e.g., complete blood counts, kidney/liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: For the best possible benefit, it is important to receive each scheduled dose of this medication as directed. If you miss a dose, contact your doctor to establish a new dosing schedule. Do not double the dose to catch up.

STORAGE: Not applicable. This medication is given in a clinic and will not be stored at home.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-800-854-1166 (USA) or 1-800-668-1507 (Canada).

Information last revised November 2010. Copyright(c) 2010 First Databank, Inc.

Mustargen Patient Information Including Side Effects

Brand Names: Mustargen

Generic Name: mechlorethamine (Pronunciation: mech klor EH tha meen)

What is mechlorethamine (Mustargen)?

Mechlorethamine is a cancer (antineoplastic) medication. Mechlorethamine interferes with the growth of cancer cells and slows their growth and spread in the body.

Mechlorethamine is used to treat several types of cancer, such as Hodgkin's Disease, lymphosarcoma, chronic myelocytic or chronic lymphocytic leukemia, lung cancer and mycosis fungoides. Mechlorethamine is also used to treat certain other blood disorders (polycythemia vera) and is sometimes injected into body spaces, such as the chest, abdomen or the sack containing the heart, to stop the accumulation of fluids caused by cancer.

Mechlorethamine may also be used for purposes other than those listed in this medication guide.

What are the possible side effects of mechlorethamine (Mustargen)?

If you experience any of the following serious side effects, seek emergency medical attention or contact your doctor immediately:

  • an allergic reaction (shortness of breath; closing of your throat; difficulty breathing; swelling of your lips, face, or tongue; or hives);
  • blood in the urine;
  • black or tarry stools;
  • signs of infection such as fever; chills, or sore throat;
  • joint pain and stiffness similar to gout (high levels of uric acid in the blood);
  • jaundice (yellowing of the skin or eyes);or
  • unusual bleeding or bruising.

Other less serious side effects may be more likely to occur. Talk to your doctor if you experience:

  • nausea, vomiting, or decreased appetite;
  • mouth sores;
  • a sensation of spinning or dizziness (vertigo);
  • diarrhea;
  • temporary hair loss;
  • rash;
  • a ringing in the ears or decreased ability to hear; or
  • weakness.

In some cases, second malignancies have been reported to occur during and following treatment with mechlorethamine. Talk to your doctor about the risks and benefits of this medication.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

Read the Mustargen (mechlorethamine hcl) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about mechlorethamine (Mustargen)?

Mechlorethamine should only be administered under the supervision of a qualified healthcare provider experienced in the use of cancer chemotherapeutic agents.

Serious side effects have been reported with the use of mechlorethamine including: allergic reactions (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives); decreased bone marrow function and blood problems (extreme fatigue; easy bruising or bleeding; black, bloody or tarry stools; fever or chills; or signs of infection such as fever; chills, or sore throat); severe nausea, vomiting, diarrhea, and loss of appetite; and others. Talk to your doctor about the possible side effects from treatment with mechlorethamine.

Mechlorethamine is highly toxic and both the powder and solution must be handled with care. Inhalation of dust or vapors and contact with skin or mucous membranes (eyes, nose and mouth) must be avoided.

Side Effects Centers

Mustargen Patient Information including How Should I Take

Who should not take mechlorethamine (Mustargen)?

Before taking mechlorethamine, tell your doctor if you

  • have had recent vaccinations;
  • have any type of infection;
  • have bone marrow problems;
  • have had radiation or x-ray therapy; or
  • have been treated with other cancer (chemotherapy) medicines.

You may not be able to take mechlorethamine, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Mechlorethamine is in the FDA pregnancy category D. This means that mechlorethamine is known to cause birth defects in an unborn baby. Do not take mechlorethamine without first talking to your doctor if you are pregnant or could become pregnant during treatment. Contraceptive measures are recommended during treatment with mechlorethamine.

It is not known whether mechlorethamine passes into breast milk. Do not take mechlorethamine without first talking to your doctor if you are breast feeding a baby.

How should I take mechlorethamine (Mustargen)?

Mechlorethamine should only be administered under the supervision of a qualified healthcare provider experienced in the use of cancer chemotherapeutic agents.

Your doctor will determine the correct amount and frequency of treatment with mechlorethamine depending upon the type of cancer being treated and other factors. Talk to your doctor if you have any questions or concerns regarding the treatment schedule.

Your doctor will probably want you to have regularly scheduled blood tests and other medical evaluations during treatment with mechlorethamine to monitor progress and side effects.

Mechlorethamine is highly toxic and both the powder and solution must be handled with care. Inhalation of dust or vapors and contact with skin or mucous membranes (eyes, nose and mouth) must be avoided. Should accidental contact occur, rinse the area with water and seek emergency medical attention.

Your healthcare provider will store mechlorethamine as directed by the manufacturer.

Side Effects Centers

Mustargen Patient Information including If I Miss a Dose

What happens if I miss a dose (Mustargen)?

Contact your doctor if you miss a dose of mechlorethamine injection.

What happens if I overdose (Mustargen)?

If for any reason an overdose of mechlorethamine is suspected, seek emergency medical attention or contact your healthcare provider immediately.

Symptoms of a mechlorethamine overdose tend to be similar to side effects caused by the medication, although often more severe.

What should I avoid while taking mechlorethamine (Mustargen)?

Mechlorethamine can lower the activity of your immune system making you susceptible to infections. Avoid contact with people who have colds, the flu, or other contagious illnesses and do not receive vaccines that contain live strains of a virus (e.g., live oral polio vaccine) during treatment with mechlorethamine. In addition, avoid contact with individuals who have recently been vaccinated with a live vaccine. There is a chance that the virus can be passed on to you.

Mechlorethamine is highly toxic and both the powder and solution must be handled with care. Inhalation of dust or vapors and contact with skin or mucous membranes (eyes, nose and mouth) must be avoided.

What other drugs will affect mechlorethamine (Mustargen)?

Do not receive "live" vaccines during treatment with mechlorethamine. Administration of a live vaccine may be dangerous during treatment with mechlorethamine.

Other drugs may interact with mechlorethamine. Talk to your doctor and pharmacist before taking any other prescription or over-the-counter medicines, including herbal products, during treatment with mechlorethamine.

Where can I get more information?

Your pharmacist has additional information about mechlorethamine written for health professionals that you may read.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 1.05. Revision date: 12/15/2010.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

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Side Effects Centers

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