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brand gleostine 40 mg capsule

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Brain Tumors

Lomustine is used as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures for the palliative treatment of primary and metastatic brain tumors.

Malignant Gliomas

Astrocytic Tumors

Lomustine is used in combination with procarbazine and vincristine as adjuvant therapy following surgery and radiation therapy for astrocytic tumors (e.g., glioblastoma multiforme, anaplastic astrocytoma) in adults.

The benefit of adjuvant chemotherapy for the treatment of malignant gliomas has not been established. Analysis of pooled data from the reported results of several published randomized studies suggests that the use of adjuvant chemotherapy prolongs survival in adults with malignant gliomas. However, in a large randomized trial, the addition of combination chemotherapy with lomustine, procarbazine, and vincristine (PCV) to radiation therapy did not prolong median survival or increase the survival rate in patients with high-grade astrocytoma. Retrospective review of cases suggests that the PCV regimen and single-agent therapy with carmustine are associated with similar survival in patients with anaplastic astrocytoma. In another randomized trial, the addition of lomustine alone to radiation therapy did not affect median survival in adult patients with supratentorial gliomas.

Combination therapy with lomustine, vincristine, and prednisone administered during and following radiation therapy has been used as postoperative adjuvant therapy for glioblastoma multiforme in children. Because of the debilitating effects of radiation on growth and neurologic development, the use of postoperative chemotherapy to delay, modify, or possibly avoid the need for radiation therapy in children younger than 3 years of age is being studied.


Lomustine is used in combination regimens (e.g., lomustine, cisplatin and vincristine; lomustine, vincristine, and prednisone) as adjuvant therapy following surgical resection and radiation therapy for the treatment of medulloblastoma, the most common malignant childhood brain tumor. Such adjuvant chemotherapy has been shown to increase progression-free survival in patients with poor prognostic factors (i.e., younger than 3 years of age, metastatic disease and/or subtotal resection with greater than 1.5 cm of residual disease and/or nonposterior fossa location), but the role of adjuvant chemotherapy in children with average-risk medulloblastoma has not been established. Because of the debilitating effects of radiation on growth and neurologic development, the use of postoperative chemotherapy to delay, modify, or possibly avoid the need for radiation therapy in children younger than 3 years of age is being studied. (Also see for further discussion of the treatment of medulloblastoma in children.)


Lomustine is used in combination with procarbazine and vincristine as adjuvant therapy following surgery and radiation therapy for anaplastic oligodendroglioma, a uniquely chemosensitive form of glioma.

Hodgkin's Disease

Although lomustine is labeled for use in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease, combination regimens containing other agents currently are preferred for this cancer.

Dosage and Administration


Lomustine is administered orally. Lomustine is commercially available in 3 strengths of capsules, enabling the pharmacist to select the proper combination of capsules to supply the patient with the prescribed dose within 10 mg. The pharmacist should instruct the patient regarding the differences in appearance of the capsules and explain that all the capsules dispensed are to be consumed in one dose.


The usual dosage of lomustine for adults and children is 130 mg/m administered as a single dose. If lomustine is administered in conjunction with other myelosuppressive drugs, dosage should be reduced accordingly. Clinicians should consult published protocols for the dosage of lomustine and other chemotherapeutic agents and the method and sequence of administration. Patients who have compromised bone marrow function (such as those who have received prior extensive radiation therapy or chemotherapy) should receive reduced doses of 100 mg/m. Subsequent dosage must be determined by the clinical and hematologic response and tolerance of the patient in order to obtain optimum therapeutic results with minimum adverse effects. Because of the delayed and cumulative myelosuppressive effects, the drug is given at intervals of at least 6 weeks. However, repeat doses of lomustine should not be administered until leukocyte and platelet counts have returned to acceptable levels (usually 4000/ mm and 100,000/ mm, respectively) with an adequate number of neutrophils present on a peripheral blood smear. The manufacturer suggests that dosage subsequent to the initial dose may be adjusted according to the schedule in the table that follows; however, some clinicians believe the manufacturer's recommendations could result in overdosage and advocate dosage reductions of 25% when platelet nadirs are 50,000-74,999/ mm, 50% when platelet nadirs are 25,000-49,999/ mm, and 75% when platelet nadirs are less than 25,000/ mm.

Nadir After Prior Dose (cells/ mm3) Percentage of Prior Dose to Be Given Leukocytes Platelets
>4000 >100,000 100%
3000-3999 75,000-99,999 100%
2000-2999 25,000-74,999 70%
<2000 <25,000 50%


Hematologic Effects

The major and dose-limiting adverse effect of lomustine is delayed hematologic toxicity. Thrombocytopenia and leukopenia, which may contribute to bleeding and overwhelming infections in an already compromised patient, are the most common and severe adverse effects of lomustine. Delayed myelosuppression usually occurs 4-6 weeks after administration of the drug and is dose-related. Leukopenia generally occurs about 5-6 weeks after an oral dose of lomustine and persists for 1-2 weeks. An earlier nadir at about 15 days has been reported in some patients. Although the degree of leukopenia varies with the dose of lomustine and previous exposure to chemotherapy or radiation therapy, the manufacturer states that approximately 65% of patients develop leukocyte counts less than 5000/mm and 36% develop leukocyte counts less than 3000/mm following administration of a usual dose of the drug. Thrombocytopenia generally occurs at about 4 weeks after an oral dose of lomustine and persists for 1-2 weeks. Thrombocytopenia generally is more severe than leukopenia, but either may be a dose-limiting toxicity. Decreases in hematocrit, reaching a nadir at 4-7 weeks, and mild anemia have also been reported. Anemia generally occurs less frequently and is less severe than thrombocytopenia or leukopenia. When lomustine therapy is continued for longer than 1 year, refractory anemia and thrombocytopenia are common; mild pancytopenia has also been reported. Lomustine has some tendency toward cumulative hematologic toxicity (manifested by more depressed indices or longer duration of suppression following repeated doses); the manufacturer reports that this usually has not been a major factor in the success or failure of treatment to date.

Myelosuppression has been reported following topical application of lomustine for the treatment of psoriasis and mycosis fungoides.

Respiratory Effects

Pulmonary toxicity, sometimes fatal, has occurred rarely in patients receiving lomustine. Pulmonary toxicity characterized by pulmonary infiltrates and/or fibrosis has occurred at 6 months or longer following initiation of lomustine therapy in patients typically receiving cumulative doses exceeding 1100 mg/m; however, pulmonary fibrosis has occurred with lower total doses.

Delayed onset of pulmonary fibrosis occurring up to 17 years after treatment has been reported in patients receiving related nitrosoureas combined with cranial radiation therapy for intracranial tumors during childhood and adolescence (age 1-16 years). Late onset of reduction in pulmonary function was observed in all long-term survivors. Nitrosourea-induced pulmonary fibrosis may be slowly progressive and can cause death. In a long-term study of carmustine, all children who received initial treatment at less than 5 years of age died of delayed pulmonary fibrosis.

GI Effects

Nausea and vomiting occur in 45-100% of patients within 45 minutes to 6 hours after ingestion of an oral dose of lomustine. Although these symptoms are not severe and usually abate within 24 hours, they may persist up to 36 hours and are often followed by 2-3 days of anorexia. The frequency and duration of nausea or vomiting reportedly can be reduced by fasting or by administration of antiemetics. Stomatitis has occurred infrequently.

Renal Effects

A decrease in kidney size, progressive azotemia, and renal failure have occurred in patients who received large cumulative doses after prolonged therapy with lomustine; renal damage also has occurred occasionally in patients receiving lower total doses.

Hepatic Effects

Hepatic toxicity, manifested by increased serum concentrations of transaminase, alkaline phosphatase, and bilirubin, has been reported in a small percentage of patients receiving lomustine and usually is reversible.

Nervous System Effects

Adverse nervous system effects, including disorientation, lethargy, ataxia, and dysarthria have been reported in some patients receiving lomustine; however, a causal relationship to the drug has not been established.

Ocular Effects

Optic atrophy, and visual disturbances, including blindness, have been reported infrequently in patients receiving lomustine.

Dermatologic Effects

Alopecia has been reported infrequently in patients receiving lomustine.

Adverse dermatologic effects resulting from topical application of lomustine for the treatment of psoriasis and mycosis fungoides include contact dermatitis, short-term hyperpigmentation, long-term telangiectasia, cutaneous pain, pruritus, and a Nikolsky-like epidermal separation in inflamed, uninvolved skin.

Precautions and Contraindications

Lomustine is a highly toxic drug with a low therapeutic index, and a therapeutic response is not likely to occur without some evidence of toxicity. The drug must be used only under constant supervision by clinicians experienced in cancer chemotherapy.

For each patient, the possible benefit of lomustine therapy must be weighed carefully against the risk of toxic effects or adverse reactions. If prompt action is taken, including reduction of dosage or discontinuance of therapy and appropriate corrective measures as clinically indicated, most adverse reactions associated with lomustine are reversible. The clinician should carefully consider the need for further therapy with lomustine in patients who have experienced adverse effects requiring discontinuance of the drug; reinstitution of lomustine therapy should be undertaken with caution and careful monitoring for possible recurrence of toxicity.

Patients who receive myelosuppressive drugs experience an increased frequency of infections as well as possible hemorrhagic complications. Because these complications are potentially fatal, the patient should be instructed to notify the physician if fever, chills, sore throat, or unusual bleeding or bruising occurs. Other serious adverse effects may occur, and patients also should be informed to notify the clinician promptly if shortness of breath, dry cough, swelling of the feet or lower legs, mental confusion, or yellowing of the eyes or skin develop.

The patient's hematologic status must be carefully monitored. Although the manufacturer recommends that blood counts be performed weekly during and for at least 6-8 weeks after discontinuance of lomustine therapy, some experts advocate performing the first blood count 2-3 weeks after the first dose with subsequent blood counts performed as indicated by prior toxicity.

Pulmonary function tests should be conducted before initiation of therapy and at frequent intervals during treatment in patients receiving lomustine. Patients with a forced vital capacity or carbon monoxide diffusing capacity below 70% of the predicted value at baseline testing are particularly at risk for pulmonary toxicity associated with lomustine therapy.

Because lomustine may cause hepatic dysfunction, the manufacturer recommends periodic monitoring of liver function.

Renal function should be monitored periodically in patients receiving lomustine.

Patients receiving lomustine should be informed that lomustine is an anticancer drug that belongs to the group of medicines known as the alkylating agents. Patients should be made aware that to provide the proper dose of this medication there may be two or more different types and colors of capsules in the container dispensed by the pharmacist. Patients should be informed that lomustine is given as a single oral dose and that the dose will not be repeated for 6 weeks. Patients should be told that, although loss of appetite may last for several days, nausea and vomiting associated with lomustine therapy usually lasts less than 24 hours.

Lomustine is contraindicated in patients who have demonstrated previous hypersensitivity to the drug.


Lomustine has been shown to be carcinogenic in animals. In addition, acute leukemia and bone marrow dysplasias have been reported in humans following long-term nitrosourea therapy.

Pregnancy, Fertility, and Lactation


Lomustine may cause fetal harm when administered to a pregnant woman, but potential benefits from use of the drug may be acceptable in certain conditions despite possible risks to the fetus. Lomustine has been shown to be embryotoxic and teratogenic in animal studies, and safe use of the drug during pregnancy has not been established.

There are no adequate and well-controlled studies to date using lomustine in pregnant women. Lomustine should be used during pregnancy only in life-threatening situations or for disease for which safer drugs cannot be used or are ineffective. When lomustine is used during pregnancy or if the patient becomes pregnant while receiving the drug, the patient should be apprised of the potential risks. Women of childbearing potential should be advised to avoid becoming pregnant during therapy with lomustine.


Lomustine adversely affects fertility in male rats at doses somewhat higher than human doses.


Because some lomustine metabolites are present in milk, women receiving the drug probably should not nurse their infants.



Lomustine is rapidly absorbed from the GI tract; the drug is also absorbed following topical application. Peak plasma concentrations of metabolites occur within 1-6 hours following administration of an oral dose of lomustine.


Lomustine is reported to be widely distributed. Lomustine and/or its metabolites cross the blood-brain barrier and are rapidly transported into cells due to their high lipid solubility. Although intact lomustine is not detectable in the CSF, active metabolites of the drug appear in substantial concentrations within 30 minutes after oral administration of lomustine. CSF concentrations of metabolites have been reported to be 15-50% or greater than concurrent plasma concentrations. Lomustine metabolites are present in milk, but in concentrations less than those in maternal plasma.


Virtually all of a dose of lomustine is metabolized within 1 hour after oral administration. The half-life of lomustine metabolites is biphasic; although the initial plasma half-life is 6 hours, the second phase plasma half-life is 1-2 days, and 15-20% of the metabolites remain in the body 5 days after administration of lomustine. Prolongation of plasma concentrations is thought to reflect a combination of protein binding and enterohepatic circulation of metabolites.

Although the metabolic fate of lomustine has not been completely elucidated, some of the metabolites are known to be active. Lomustine is excreted primarily in the urine as metabolites. Following oral administration of C-labeled lomustine, about 50% of the radioactivity is excreted within 12 hours and about 75% within 4 days.

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