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lomustine (Rx)Brand and Other Names:Gleostine, CCNU

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 5mg
  • 10mg
  • 40mg
  • 100mg
more...

Brain Tumors

130 mg/m² PO once q6week 

Round dose to nearest 5 mg

Compromised bone marrow: 100 mg/m² PO once q6week

Hodgkin Lymphoma

130 mg/m² PO once q6week 

Round dose to nearest 5 mg

Compromised bone marrow: 100 mg/m² PO once q6week

Dosage Modifications

For SI Units, convert full U.S. value by x 10^6/L

Do not repeat course until platelets >100000/mm³ and leukocytes >4000/mm&sup3/

Give full dose if

  • Leukocytes >3000/mm³
  • Platelets >75000/mm³

Give 70% if

  • Leukocytes: 2000-2999/mm³
  • Platelets: 25000-74999/mm³

Give 50% if

  • Leukocytes <1999/mm³
  • Platelets <24999/mm³

Renal impairment

  • CrCl >50 mL/min: Administer full dose
  • CrCl 10-50 mL/min: Administer 75% of regular dose
  • CrCl <10 mL/min: Administer 25-50% of regular dose

Hepatic impairment

  • Use caution, not studied

Monitor

CBC, pulmonary function, LFTs, renal function

Adjust dose based on WBC counts; do not repeat dose until WBC >4000/mm³ & Plts >100000/mm³

Other Indications & Uses

Malignant gliomas

Off-label: pancreatic, liver, gastric, colorectal cancer; multiple myeloma; mycosis fungoides, psoriasis (topical)

Dosage Forms & Strengths

capsule

  • 5mg
  • 10mg
  • 40mg
  • 100mg
more...

Brain Tumors

130 mg/m² PO once q6week 

Round dose to nearest 5 mg

Compromised bone marrow: 100 mg/m² PO once q6week

Hodgkin Lymphoma

130 mg/m² PO once q6week 

Round dose to nearest 5 mg

Compromised bone marrow: 100 mg/m² PO once q6week

Dosing Considerations

Pediatric use, including dose, is not based on adequate and well-controlled clinical studies, although it has approved indications for brain tumors and Hodgkin lymphoma

Dosage Modifications

For SI Units, convert full U.S. value by x 10^6/L

Do not repeat course until platelets >100000/mm³ and leukocytes >4000/mm&sup3/

Give full dose if

  • Leukocytes >3000/mm³
  • Platelets >75000/mm³

Give 70% if

  • Leukocytes: 2000-2999/mm³
  • Platelets: 25000-74999/mm³

Give 50% if

  • Leukocytes <1999/mm³
  • Platelets <24999/mm³

Renal impairment

  • CrCl >50 mL/min: Administer full dose
  • CrCl 10-50 mL/min: Administer 75% of regular dose
  • CrCl <10 mL/min: Administer 50% of regular dose

Hepatic impairment

  • Use caution, not studied

Monitor

CBC, pulmonary function, LFTs, renal function

Adjust dose based on WBC counts; do not repeat dose until WBC >4000/mm³ & Plts >100000/mm³

Next

Interactions

Interaction Checker

lomustine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
             activity indicator 
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            Adverse Effects

            >10%

            Nausea (54%)

            Vomiting (54%)

            1-10%

            Neurotoxicity

            Myelosuppression (delayed 4-5 weeks)

            Frequency Not Defined

            Ataxia

            Lethargy

            Disorientation

            Stomatitis

            Mucositis

            Pulmonary fibrosis (rare)

            Pulmonary toxicity

            Elevated LFTs

            Leukemia

            Renal toxicity

            Hepatic toxicity

            Infertility

            Alopecia

            Optic atrophy (rare)

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            Warnings

            Black Box Warnings

            Myelosuppression is delayed, dose-related, and cumulative; thrombocytopenia is generally more severe than leukopenia; may occur 4-6 weeks after drug administration and persist for 1- 2 weeks; thrombocytopenia and leucopenia may contribute to bleeding and overwhelming infections in an already compromised patient; monitor blood counts weekly for 6 or more weeks after a dose; do not give therapy more frequently than every 6 weeks; bone marrow toxicity is cumulative; adjust dose based on nadir blood counts from prior dosage

            Therapy should be administered by experienced cancer physician; prescribe, dispense, and administer enough capsules for one dose; fatal toxicity occurs with overdosage; prescribe, dispense, and administer only enough capsules for one dose; both physician and pharmacist should emphasize to patient that only one dose of the drug is taken every 6 weeks

            Contraindications

            Hypersensitivity

            Cautions

            Causes myelosuppression that can result in fatal infections and bleeding; monitor blood counts for at least 6 weeks after each dose; do not give more frequently than q6wk due to delayed myelosuppression

            Avoid pregnancy; can cause fetal harm; advise males and females of reproductive potential of potential risk to fetus and to use effective contraception; advise males with female partners of reproductive potential to use effective contraception during treatment and for 3.5 months after the final dose; therapy may result in reduced fertility in males and females of reproductive potential

            Hepatotoxicity reported; increased levels of transaminases, alkaline phosphatase and bilirubin can occur; monitor liver function

            Can cause renal failure; monitor renal function

            Delayed pulmonary toxicity may occur; pulmonary infiltrates and/or fibrosis may occur; perform pulmonary function tests prior to treatment and repeat frequently; permanently discontinue therapy in patients diagnosed with pulmonary fibrosis

            Secondary malignancies reported; acute leukemia and myelodysplasia can occur with long-term use

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            Pregnancy & Lactation

            Pregnancy Category: D

            Lactation: Unknown if metabolites present in breast milk; avoid nursing during treatment and for 2 weeks after final dose

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Not completely understood

            Inhibition of DNA & RNA synthesis resulting from carbamylation of DNA polymerase, alkylation of DNA, and alteration of RNA proteins

            Pharmacokinetics

            Half-Life Elimination (biphasic): 16-24 hr (parent drug); 16-48 hr (active metabolite)

            Peak plasma time: ~3 hr

            Metabolism: Liver

            Duration: 5-6 weeks (bone marrow recovery)

            Excretion: Urine (50%); feces (<5%)

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            Administration

            Oral Administration

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • Compare formulary status to other drugs in the same class.
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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.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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