Universal reference book for medicines

Active substance: lomustine

Type: Antitumor preparation

Manufacturer: medac (Germany)
Composition, form of production and packaging
Capsules hard gelatinous, size 3, body and cap of blue color; the contents of the capsules are a white or slightly yellowish powder.
1 caps.
lomustine 40 mg
Excipients: lactose, starch, talc, magnesium stearate, gelatin, titanium dioxide, indigocarmine.
20 pcs. - plastic cans (1) - packs of cardboard.
Description of the drug approved by the manufacturer for the printed edition of 2012.
Lomustine is an anticancer agent of the alkylating action from the group of nitrosoureas. The mechanism of action is the alkylation of DNA and RNA. The inhibition of DNA synthesis is due to carbamoylation of DNA polymerase and other DNA repair enzymes, and damage to the DNA matrix. The drug can also inhibit key enzymatic processes by changing the structure and function of many proteins and enzymes. Lomustine acts in the late phase of GI and the early S-phase of the cell cycle. The highest sensitivity to lomustine in cells in the stationary phase of growth (a factor determining activity in solid tumors with a low proliferative pool).
After oral administration, it is quickly and almost completely absorbed from the digestive tract. C max drug in the blood plasma is reached after 1-4 hours. Communication with plasma proteins is 50%. Penetrates through the blood-brain barrier and into breast milk. In cerebrospinal fluid, more than 50% of the concentration in the blood plasma is determined.
Metabolized in the liver with the formation of active metabolites (oxymethyldiazonium and isocyanate). Oxymethyldiazonium is ionized and converted to the methyl diazonium ion, which is transformed into a more stable tautomeric form (diazomethane), or decomposes into the methylcarbon ion and nitrogen. T 1/2 active metabolites ranges from 16 to 48 hours. It is excreted mainly by kidneys in the form of metabolites, less than 5% through the intestine.
Lomustine is used in monotherapy and in combination therapy of the following diseases:
- primary and metastatic brain tumors after surgical treatment and / or radiotherapy;
- lymphogranulomatosis (Hodgkin's disease) as second-line therapy;
- cancer of the stomach and intestines, small cell lung cancer, kidney cancer, multiple myeloma, malignant melanoma.
Lomustine should be taken orally in the evening, before going to bed or 3 hours after eating. The recommended dose of lomustine in adults and children is 130 mg / m 2 with a single intake every 6 weeks.
In patients with reduced bone marrow function, the dose can be reduced to 100 mg / m 2 while maintaining a six-week interval between doses.
In the case of combination therapy, the drug is used in a dose of 70-100 mg / m 2 .
Repeated courses should not be administered with platelet counts less than 100,000 / mm3 and leukocytes less than 4000 / mm3.
The total dose for all treatment courses should not exceed 1000 mg / m 2 .
Further doses of the drug should be selected depending on the patient's hematologic response to the previous dose. When selecting doses, you can focus on the following scheme:
Minimum values ​​after the previous dose The recommended next dose
Leukocytes / Ојl Platelets / ОјL (% of previous dose)
3000-4000 75000- 100000 100%
2000 - 2999 25000 - 74999 70%
less than 2000 less than 25000 50%
From the hemopoiesis: thrombocytopenia develops after 4 weeks, leukopenia 5-6 weeks after the application of the drug and can last 1-2 weeks. Usually, thrombocytopenia is more severe than leukopenia. Anemia and granulocytopenia are less common.
Lomustine can cause cumulative myelosuppression, and after taking repeated doses, there may be more marked suppression of the bone marrow, or the duration of myelosuppression may be longer.
On the part of the digestive organs: nausea and vomiting (3-6 hours after taking lomustine, usually lasting up to 24 hours), anorexia. The frequency and duration of these side effects can be reduced by the prophylactic use of antiemetics, and by administering lomustine to patients on an empty stomach. Rarely - diarrhea, stomatitis, increased activity of liver enzymes and bilirubin concentrations.
On the part of the respiratory system: rarely - cough, respiratory failure associated with the emergence of infiltrates and / or pulmonary fibrosis (reported after 6 months or longer after treatment with total doses of more than 1100 mg / m 2 . cumulative dose of 600 mg / m 2 ).
From the nervous system: disorientation, lethargy, ataxia, speech articulation disorder, increased fatigue.
From the urinary system: urinary retention, edema of the feet or lower limbs, azotemia, a decrease in the size of the kidneys (usually at high cumulative doses of the drug in conditions of prolonged treatment with lomustine and other nitrosoureas).
From the side of the reproductive system: azoospermia (in some cases irreversible), amenorrhea.
Other: rarely - alopecia, irreversible damage to the optic nerves, leading to blindness (when combined with radiation therapy of the brain). Reported acute leukemia and dysplasia of the bone marrow as a result of treatment with drugs nitrosourea.
- hypersensitivity to lomustine, other derivatives of nitrosourea or constituents of the drug;
- Pregnancy and the period of breastfeeding.
With caution: myelosuppression (including on the background of concomitant radiation or chemotherapy, intoxication); chicken pox (including recently transferred or after contact with the sick), surrounding herpes and other acute infectious diseases of a viral, fungal or bacterial nature; cachexia, intoxication, renal and / or hepatic insufficiency, respiratory failure, cytotoxic treatment, and radiation therapy in the anamnesis.
Contraindicated in pregnancy and during lactation.
With caution: kidney failure.
With caution: liver failure.
The application is possible according to the dosing regimen.
Lomustine should be used under the supervision of doctors who have experience with antitumor drugs.
A systematic (at least 1 time per week) control of the peripheral blood picture during therapy and within 6 weeks after the end of treatment is needed, as well as periodic monitoring of laboratory parameters of liver and kidney function.
Against the background of thrombocytopenia and leukopenia, weakened patients may experience bleeding and severe infections.
Before the start of therapy and during treatment, lung function should be evaluated. Patients with initially reduced vital capacity of the lungs are more susceptible to pulmonary toxicity of lomustine. It is not recommended to use the drug more than once every 6 weeks.
Men and women of childbearing age should, during treatment and at least 6 months afterwards, use reliable contraceptive methods.
Do not open capsules (powder has irritating effect), avoid getting powder on the skin and mucous membranes.
In case of an overdose, one should expect an increase in the severity of side effects - oppression of bone marrow hematopoiesis, gastrointestinal disorders and worsening liver function, and neurological disorders. The antidote is not known. Treatment is symptomatic.
Medicines that cause myelosuppression, as well as other cytotoxic drugs and radiotherapy, can increase leukopenia and thrombocytopenia caused by lomustine. The combined use of lomustine with amphotericin B increases the risk of nephrotoxic action, lowering blood pressure and bronchospasm.
A case of significant enhancement of leukopenia and neutropenia in the joint use of lomustine and cimetidine is described.
An increase in toxicity can be observed with simultaneous administration of lomustine and theophylline. Phenobarbital, which activates microsomal enzymes, can enhance the metabolism of lomustine. In patients receiving lomustine, there may be a weakening of the defense mechanisms of the body, which can cause a decrease in the formation of antibodies in the administration of antiviral vaccines. This condition lasts from 3 months to 1 year after the last course of chemotherapy. Particular care should be taken when using vaccines containing live viruses.
On prescription.
List B. Store at a temperature of no higher than 25 В° C in a place inaccessible to children.
Shelf life - 3 years. Do not use after the expiration date printed on the package.
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