Chemical formula: C₉H₁₆ClN₃O₂ Molecular mass: 233.695 g/mol PubChem compound: 3950
Lomustine interacts in the following cases:
Co-administration of antiepileptic medicinal products and chemotherapeutic medicinal products including lomustine can lead to complications secondary to pharmacokinetic interaction between the medicinal products.
Lomustine can have a mutagenic effect. Men treated with lomustine are therefore advised not to father children during treatment and for up to 6 months afterwards, and to seek advice regarding sperm conservation before the start of treatment given the possibility of irreversible infertility caused by lomustine therapy.
Pretreatment with phenobarbital can lead to a reduced antitumour effect of lomustine due to an accelerated elimination caused by induction of microsomal liver enzymes.
Lomustine in combination with theophylline or with the H2 receptor antagonist cimetidine may potentiate bone marrow toxicity.
Since lomustine may cause liver dysfunction, it is recommended that liver function tests be monitored periodically.
Lomustine is contraindicated during pregnancy. Safe use in pregnancy has not been established. Animal studies have shown reproductive toxicity. If this medicinal product is used during pregnancy, or if the patient becomes pregnant while taking (receiving) this medicinal product, the patient should be apprised of the potential hazard to the foetus. Women of childbearing potential should be advised to avoid becoming pregnant.
Lomustine is contraindicated during breastfeeding. Due to the lipophilic nature of lomustine, it is likely to be excreted in human milk. As a risk to the nursing child potentially exists, a decision must be made whether to discontinue breastfeeding or to discontinue/abstain from lomustine therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
Lomustine can have a mutagenic effect. Men treated with lomustine are therefore advised not to father children during treatment and for up to 6 months afterwards, and to seek advice regarding sperm conservation before the start of treatment given the possibility of irreversible infertility caused by lomustine therapy.
No studies on the effects on the ability to drive and use machines have been performed.
Lomustine capsules can impair the ability to drive and use machines, e.g. because of nausea and vomiting.
The list is presented by system organ class and frequency: Very common (≥1/10)
Common (≥1/100 to <1/10), Uncommon (≥1/1,000 to <1/100), Rare (≥1/10,000 to <1/1,000), Very rare (<1/10,000), Not known (cannot be estimated from the available data).
Not known: Acute leukaemia, myelodysplastic syndrome
Very common: Leukopenia
Not known: Bone marrow failure, thrombocytopenia, anaemia
Not known: Coordination abnormal, disorientation, lethargy, dysarthria
Not known: Pulmonary fibrosis, lung infiltration
Not known: Nausea, vomiting, stomatitis
Not known: Transaminases increased, blood bilirubin increased
Not known: Alopecia
Not known: Renal failure, azotaemia, renal atrophy, renal injury
Not known: Blood alkaline phosphatase increased
The principal adverse effect is marrow toxicity of a delayed or prolonged nature. It usually occurs four to six weeks after administration of the medicinal product and is dose-related. Thrombocytopenia appears about four weeks after a dose of Lomustine “medac” and lasts one or two weeks at a level around 80-100,000/mm³. Leucopenia appears after five to six weeks and persists for one or two weeks at about 4-5,000/mm³.
The haematological toxicity may be cumulative, leading to successively lower white cell and platelet counts with successive doses of the medicinal product. Approximately 65% of patients receiving 130 mg/m² develop white blood cell counts below 5,000 WBC/mm³. Thirty-six percent developed white blood cell counts below 3,000/mm³. Thrombocytopenia is generally more severe than leukopenia. However, both may be dose-limiting toxicities.
The occurrence of acute leukaemia and bone marrow dysplasia have been reported in patients following long-term nitrosourea therapy.
Anaemia also occurs, but is less frequent and less severe than thrombocytopenia or leukopenia.
Nausea and vomiting usually occur four to six hours after a full single dose of Lomustine “medac” and last for 24–48 hours, followed by anorexia for two or three days. The effects are less troublesome if the 6-weekly dose is divided into three doses given on each of the first three days of the six week period. Gastrointestinal tolerance is usually good, however, if prophylactic antiemetics are given (e.g. metoclopramide or chlorpromazine). Disorders of liver function have been reported commonly. They are mild in most cases. In rare cases a cholestatic jaundice occurs. Transient elevation of liver enzymes (SGOT, SGPT, LDH or alkaline phosphatase) are occasionally observed.
More rarely patients are troubled by stomatitis and diarrhoea.
Mild neurological symptoms, like e.g. apathy, disorientation, confusion and stuttering can occur uncommonly in combination therapy with other antineoplastic medicinal products or radiation.
Interstitial pneumonia or lung fibrosis have been reported rarely.
Renal failure, decrease in kidney size, and progressive azotaemia have been reported in single cases after prolonged treatment with lomustine and related nitrosoureas reaching a high cumulative total dose. Therefore it is recommended not to exceed a maximum cumulative total lomustine dose of 1,000 mg/m².
Kidney damage has also been reported occasionally in patients receiving lower total doses.
Loss of scalp hair has been reported rarely.
In single cases an irreversible vision loss has been reported after a combined therapy of lomustine with radiation.
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