chlorambucil (Rx)

Brand and Other Names:Leukeran
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 2mg

Chronic Lymphatic (Lymphocytic) Leukemia

0.1 mg/kg/day for 3-6 weeks or  

0.4 mg/kg (increased by 0.1 mg/kg/dose until response/toxicity observed) biweekly or

0.4 mg/kg (increased by 0.1 mg/kg/dose until response observed) monthly or

0.03-0.1 mg/kg/day continuously

Reduce initial dose if administered within 4 weeks after a full course of radiation/myelosuppressive therapy or patients with bone marrow disease

Not to exceed 0.1 mg/kg/day if bone marrow infiltrated with lymphocytes

Hodgkin's Lymphoma

0.2 mg/kg/day for 3-6 weeks or  

0.4 mg/kg (increased by 0.1 mg/kg/dose until response/toxicity observed) biweekly or

0.4 mg/kg (increased by 0.1 mg/kg/dose until response or toxicity observed) monthly or

0.03-0.1 mg/kg/day continuously

Reduce initial dose if administered within 4 weeks after a full course of radiation/myelosuppressive therapy or patients with bone marrow disease

Not to exceed 0.1 mg/kg/day if bone marrow infiltrated with lymphocytes

Renal Impairment

<1% (including metabolites) excreted in urine; no dose adjustment required

Hepatic Impairment

Primarily metabolized in liver; dose reduction may be required

Monitor

CBC

Discontinue if WBC <3000/mm³ or platelets <150,000/mm³

Other Indications & Uses

Malignant lymphomas (lymphosarcoma, giant follicular lymphoma)

Off-label: Uveitis & meningoencephalitis associated with Behcet's disease; other NHL; idiopathic membranous nephropathy; RA

Dosage Forms & Strengths

tablet

  • 2mg

Chronic Lymphatic (Lymphocytic) Leukemia (Off-label)

Safety and efficacy not established, but has been used unlabeled

0.1-0.2 mg/kg PO qDay

Chronic Lymphatic (Lymphocytic) Leukemia

0.1 mg/kg/day for 3-6 weeks or  

0.4 mg/kg (increased by 0.1 mg/kg/dose until response/toxicity observed) biweekly or

0.4 mg/kg (increased by 0.1 mg/kg/dose until response observed) monthly or

0.03-0.1 mg/kg/day continuously

Reduce initial dose if administered within 4 weeks after a full course of radiation/myelosuppressive therapy or patients with bone marrow disease

Not to exceed 0.1 mg/kg/day if bone marrow infiltrated with lymphocytes

Hodgkin's Lymphoma

0.2 mg/kg/day for 3-6 weeks or  

0.4 mg/kg (increased by 0.1 mg/kg/dose until response/toxicity observed) biweekly or

0.4 mg/kg (increased by 0.1 mg/kg/dose until response or toxicity observed) monthly or

0.03-0.1 mg/kg/day continuously

Reduce initial dose if administered within 4 weeks after a full course of radiation/myelosuppressive therapy or patients with bone marrow disease

Not to exceed 0.1 mg/kg/day if bone marrow infiltrated with lymphocytes

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Interactions

Interaction Checker

and chlorambucil

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            Contraindicated (0)

              Serious - Use Alternative (5)

              • adenovirus types 4 and 7 live, oral

                chlorambucil decreases effects of adenovirus types 4 and 7 live, oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressives may diminish therapeutic effects of vaccines and increase risk of adverse effects (increased risk of infection). Live-attenuated vaccines should be avoided for at least 3mo after cessation of immunosuppressive therapy.

              • influenza virus vaccine quadrivalent, adjuvanted

                chlorambucil decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.

              • influenza virus vaccine trivalent, adjuvanted

                chlorambucil decreases effects of influenza virus vaccine trivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.

              • palifermin

                palifermin increases toxicity of chlorambucil by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

              • tofacitinib

                chlorambucil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              Monitor Closely (31)

              • acalabrutinib

                acalabrutinib, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.

              • belatacept

                belatacept and chlorambucil both increase immunosuppressive effects; risk of infection. Use Caution/Monitor.

              • bendamustine

                bendamustine, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • busulfan

                busulfan, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • carboplatin

                carboplatin, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • carmustine

                carmustine, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • cholera vaccine

                chlorambucil decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.

              • cisplatin

                chlorambucil, cisplatin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • cyclophosphamide

                chlorambucil, cyclophosphamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • dacarbazine

                chlorambucil, dacarbazine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • dengue vaccine

                chlorambucil decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.

              • denosumab

                chlorambucil, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.

              • fingolimod

                chlorambucil increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .

              • hydroxyurea

                chlorambucil, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.

              • ifosfamide

                chlorambucil, ifosfamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • influenza A (H5N1) vaccine

                chlorambucil decreases effects of influenza A (H5N1) vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.

              • influenza virus vaccine (H5N1), adjuvanted

                chlorambucil decreases effects of influenza virus vaccine (H5N1), adjuvanted by pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.

              • isavuconazonium sulfate

                chlorambucil and isavuconazonium sulfate both decrease immunosuppressive effects; risk of infection. Use Caution/Monitor.

              • lomustine

                chlorambucil, lomustine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • mechlorethamine

                chlorambucil, mechlorethamine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • meningococcal group B vaccine

                chlorambucil decreases effects of meningococcal group B vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Individuals with altered immunocompetence may have reduced immune responses to the vaccine.

              • obinutuzumab

                chlorambucil increases toxicity of obinutuzumab by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reported to cause thrombocytopenia and subsequent hemorrhage that may require blood product support.

              • ofatumumab SC

                ofatumumab SC, chlorambucil. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

              • olaparib

                chlorambucil and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.

              • oxaliplatin

                oxaliplatin, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • siponimod

                siponimod and chlorambucil both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • sipuleucel-T

                chlorambucil decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

              • streptozocin

                chlorambucil, streptozocin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • thiotepa

                chlorambucil, thiotepa. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.

              • trastuzumab

                trastuzumab, chlorambucil. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • trastuzumab deruxtecan

                trastuzumab deruxtecan, chlorambucil. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              Minor (2)

              • vitamin A

                vitamin A, chlorambucil. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin A enhance the efficacy, and reduce toxicity, of antineoplastic drugs.

              • vitamin E

                vitamin E, chlorambucil. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin E enhance the efficacy, and reduce toxicity, of antineoplastic drugs.

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              Adverse Effects

              >10%

              Neutropenia (25-33%)

              Anemia

              Leukopenia

              Thrombocytopenia

              Frequency Not Defined

              Seizures

              Hallucinations

              Peripheral neuropathy

              Nausea

              Vomiting

              Pulmonary fibrosis

              GI effects

              Leukemia

              Myelosuppression

              Hyperuricemia

              Infertility

              Hepatotoxicity & jaundice

              Type I hypersensitivity

              Rash

              Stevens-Johnson syndrome (rare)

              Toxic epidermal necrosis (rare)

              Urticaria

              Erythema multiforme (rare)

              Secondary malignancies

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              Warnings

              Black Box Warnings

              Severe bone marrow suppression can occur with chlorambucil

              Chlorambucil is a carcinogen. Chronic therapy may produce myelocytic leukemia and secondary malignancies

              Chlorambucil may cause infertility. It is teratogenic and mutagenic

              Contraindications

              Hypersensitivity or resistance; demonstrated resistance to chlorambucil previously

              Cautions

              History of seizures; head trauma; those receiving other potentially epileptogenic drugs

              Potentially mutagenic, carcinogenic & teratogenic; avoid pregnancy

              Can cause infertility

              Severely myelosuppressive

              May need lower dosages in liver failure

              Beware of cross-hypersensitivity w/ other alkylating agents

              Reduce dose in preexisting myelosuppressive situations or if WBC/Plt counts fall below normal

              If used within 4 week of radiation/cytotoxic chemotherapy

              Avoid pregnancy

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              Pregnancy & Lactation

              Pregnancy Category: D

              Lactation: not known if excreted in breast milk; do not nurse

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Alkylating agent of nitrogen mustard family, crosslinks DNA and interferes with DNA replication and RNA transcription; cell cycle nonspecific

              Absorption

              Bioavailability: 70-80%

              Peak Plasma Time: 1 hr

              Distribution

              Protein Bound: 99%

              Vd: 0.3 L/kg

              Metabolism

              Liver

              Metabolites: phenylacetic acid mustard

              Elimination

              Half-Life: 1.5 hr (chlorambucil); 2.5 hr (phenylacetic acid mustard)

              Clearance: 492 ±160 ng/mL (chlorambucil); 306±73 ng/mL (phenylacetic acid mustard)

              Excretion: Urine (20-60% metabolites)

              Dialyzable: No

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Leukeran oral
              -
              2 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              chlorambucil oral

              CHLORAMBUCIL - ORAL

              (klor-AM-bue-sil)

              COMMON BRAND NAME(S): Leukeran

              WARNING: Although chlorambucil is used to treat cancer, it may rarely increase your risk of developing other cancers. Also, chlorambucil may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you develop unusual growths or lumps, swollen glands, signs of infection (such as a sore throat that doesn't go away, fever, chills), easy bruising/bleeding, or unusual tiredness.Taking chlorambucil during pregnancy may increase the risk of birth defects. Also, it may make it harder for men or women to have a child (decreased fertility) after treatment.Talk with your doctor about the risks and benefits of treatment with this medication.

              USES: This medication is used to treat certain types of cancer (such as leukemia, lymphoma). Chlorambucil belongs to a class of drugs known as alkylating agents. It works by slowing or stopping the growth of cancer cells.

              HOW TO USE: Take this medication by mouth as directed by your doctor, usually once daily. Unless otherwise directed by your doctor, drink plenty of fluids to help prevent side effects.The dosage is based on your medical condition, weight, and response to treatment. Do not increase your dose or take this medication more often than directed. Your condition will not improve any faster and your risk of side effects will increase.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

              SIDE EFFECTS: See also Warning section.Rarely, nausea, vomiting, stomach upset, or diarrhea may occur. 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 any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, such as: easy bleeding/bruising, mouth sores, shaking/tremors, muscle problems (such as twitching, stiffness, weakness), numbness/tingling of the hands or feet, mental/mood changes (such as confusion, hallucinations), signs of liver problems (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), stopped menstrual periods (women).Get medical help right away if you have any very serious side effects, such as: seizures.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: 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 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking chlorambucil, tell your doctor or pharmacist if you are allergic to it; or to other alkylating agents (such as busulfan, cyclophosphamide); 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: gout, bleeding/blood problems, liver disease.Chlorambucil can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance 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 about all the products you use (such as prescription drugs, nonprescription drugs, and herbal products).Children may be more sensitive to the side effects of this drug, especially infertility later in life or seizures.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while you are using chlorambucil. Chlorambucil may harm an unborn baby. If you become pregnant while using chlorambucil, talk to your doctor right away about its risks and benefits.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.It is unknown if 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.

              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 (such as 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.A product that may interact with this drug is: nalidixic acid.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: seizures.

              NOTES: Do not share this medication with others.Lab and/or medical tests (such as complete blood counts, uric acid levels) should be done while you are taking this medication. Keep all medical and lab appointments.

              MISSED DOSE: It is important to take each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule. Do not double the dose to catch up.

              STORAGE: Store in the refrigerator away from light and moisture. Do not freeze. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

              Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

              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.

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              Formulary

              FormularyPatient Discounts

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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              NC NOT COVERED – Drugs that are not covered by the plan.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.