Active substanceLomustineLomustine
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  • Lomustine medak
    capsules inwards 
    medac GmbH     Germany
  • Dosage form: & nbspcapsules
    Composition:

    Each capsule contains

    Active substance: Lomustine - 40 mg.

    Excipients: lactose monohydrate 100 mg, wheat starch 40 mg, talc 16 mg, magnesium stearate 4 mg.

    Capsule shell: gelatin 49 mg, titanium dioxide (E171) 0.5 mg, indigocarmine (E132) 0.06 mg.

    Description:

    Hard gelatin capsules No. 3 with a casing and a lid of blue color. The contents of the capsule - powder from white to light yellow color, it is possible to have inclusions of yellow color.

    Pharmacotherapeutic group:An antitumour agent, an alkylating compound
    ATX: & nbsp

    L.01.A.D   Nitrosoureas derivatives

    L.01.A.D.02   Lomustine

    Pharmacodynamics:

    Lomustine is an antitumor drug of the alkylating action from the group of nitrosoureas. The mechanism of action is the alkylation of DNA and RNA, as well as the inhibition of individual steps in the synthesis of nucleic acids and the repair of individual DNA strand breaks. 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 G1 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).

    Pharmacokinetics:

    After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum concentration in the blood plasma (0.5-2 ng / ml) is achieved on average 3 hours after oral administration of the dose of the drug 30-100 mg / m2.

    Connection with plasma proteins - 50%. Penetrates through the blood-brain barrier. After oral administration of lomustine, labeled with a radioisotope label, the radioactivity in the cerebrospinal fluid is from 15 to 30% of the radioactivity measured in the plasma.

    Rapidly 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.

    The chloroethyl group is excreted from the plasma single-phase with a half-life of 72 hours.The elimination of the cyclohexyl group is biphasic with a half-life T1/2α= 4 hours and T1/2β = 50 hours. It is excreted mainly by kidneys in the form of metabolites, less than 5% - through the intestine. The active form of lomustine in urine is not detected.

    Indications:

    Lomustine is used in ionotherapy and combined therapy (including in combination with radiotherapy and surgical treatment) of the following diseases:

    - primary and metastatic brain tumors,

    - lung cancer (especially small cell),

    - lymphogranulomatosis (Hodgkin's disease), resistant to standard chemotherapy,

    Malignant metastatic melanoma.

    Lomustine medak can also be used in the therapy of multiple myeloma, stomach and intestinal cancer, kidney cancer.

    Contraindications:

    - Hypersensitivity to lomustine and other components of the drug, other derivatives of nitrosourea, including in the anamnesis;

    - Previously identified tumor resistance to nitrosoureas derivatives;

    - Pronounced suppression of bone marrow function;

    - Severe renal insufficiency;

    - Celiac disease or wheat allergy;

    - Co-administration with yellow fever vaccine or other livevaccines in patients with a decreased immune status;

    - Pregnancy and lactation.

    Carefully:In patients with myelosuppression and reduced concentration of platelets, leukocytes, red blood cells in the blood; 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, cytostatic therapy and radiation therapy in history, lactose intolerance, lactase deficiency, glucose-galactose malabsorption (since the drug contains lactose).
    Pregnancy and lactation:

    Pregnancy

    The drug is contraindicated in pregnancy. In preclinical studies lomustine manifested embryotoxic and teratogenic effects. Patients using the drug should be aware of the potential hazard to the fetus if the pregnancy occurs during treatment with Lomustine medak. Women of childbearing age should avoid pregnancy.In case of pregnancy on the background of taking the drug, the patient should inform his / her own doctor about this.

    Breastfeeding period

    As lomustine has lipophilic properties, there is reason to believe that it penetrates into breast milk. Given the risk of adverse effects on the child, the expected benefit of treatment for the mother and the potential risk to the child should be carefully weighed and decide whether to stop breastfeeding or stop using lomustine.

    Dosing and Administration:

    Lomustine should be taken orally in the evening, before going to bed or 3 hours after eating.

    For preventive purposes, the use of antiemetics with lomustine is recommended.

    The recommended dose of lomustine in adults and children with normal bone marrow function is 120-130 mg / m2 with a single oral intake every 6-8 weeks. This dose can be divided into three doses for three consecutive days.

    In patients with reduced bone marrow function, the dose can be reduced to 100 mg / m2 while maintaining a six-week interval between doses.

    Cumulative myelosuppression may require a longer interval between taking the drug.

    Before each next reception of lomustine, a general blood test should be performed and, if necessary, the dose should be adjusted.

    The dose should be reduced if:

    - the drug is used as part of a therapy regimen, which includes other drugs with myelosuppressive properties:

    - with leukopenia below 3000 / μL or thrombocytopenia below 75,000 / μl.

    R In the case of combination therapy, the drug is used in a dose of 70-100 mg / m2.

    When lomustine is used, the inhibition of bone marrow function is longer than after exposure to trichlorotriethylamine compounds, restoration of white blood cell and platelet counts can occur for 6 weeks or more. Repeated courses should not be assigned with a platelet count of less than 100,000 / μL and a white blood cell count of less than 4000 / μL. 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 (% of the previous dose)

    Leukocytes / μL

    Platelets / μL

    3000-4000

    75000-100000

    100%

    2000-2999

    25000-74999

    70%

    Less than 2000

    Less than 25,000

    50%

    Use in children

    The use of the drug for the treatment of children with cancer should only be carried out in specialized centers and only after assessing the ratio of the expected benefit of treatment to the potential risk.

    Side effects:

    The incidence of adverse reactions listed below is set out according to the following gradation: very often (≥ 1/10), often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), the frequency is unknown (can not be determined on the basis of available data).

    Violations of the blood and lymphatic system

    Often: oppression of bone marrow hematopoiesis, thrombocytopenia, leukopenia, anemia.

    Benign, malignant and unspecified neoplasms (including cysts and polyps)

    Frequency unknown: reported the development of acute leukemia and bone marrow dysplasia in patients who had received nitrosourea preparations for a long time.

    Disorders from the gastrointestinal tract

    Often: nausea, vomiting, anorexia.

    Rarely: diarrhea, stomatitis.

    Disturbances from the liver and bile ducts

    Often: violation of liver function (in most cases, mild degree of severity).

    Rarely: cholestatic jaundice, hepatic insufficiency.

    Disturbances from the respiratory system, chest and mediastinal organs

    Rarely: interstitial pneumonia, infiltrative processes, pulmonary fibrosis.

    Disturbances from the nervous system

    Rarely: impaired coordination, confusion, drowsiness, apathy, speech articulation disorder, stuttering (reported on development of these symptoms in combination therapy with other antitumor agents and radiation therapy).

    Disorders from the nochek and urinary tract

    Frequency unknown: renal failure, progressive azotemia, decrease in the size (atrophy) of the kidneys.

    Disorders from the rut and subcutaneous tissues

    Rarely: alopecia.

    Disturbances on the part of the organ of sight

    Rarely: defeat of the optic nerves (when combined with radiation therapy of brain tumors), irreversible loss of vision.

    Impact on the results of laboratory and instrumental studies

    Frequency unknown: increased activity of hepatic enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH), alkaline phosphatase), increased serum bilirubin concentration.

    The main undesirable side effect of lomustine is delayed or prolonged myelotoxicity, which usually manifests itself 4-6 weeks after taking the drug and is dose-dependent. Thrombocytopenia occurs approximately 4 weeks after taking a dose of lomustine and is usually stored on level of 80000 - 100000 / μL for 1-2 weeks. After 5-6 weeks, there is leukopenia (about 4000 - 5000 / μl), which persists for one or two weeks. Anemia is less common, however, compared with thrombocytopenia and leukopenia, it is less common and occurs in a less severe form.

    Hematologic toxicity can be cumulative, and after receiving repeated doses, there may be more pronounced suppression of bone marrow function. Approximately 65% ​​of patients receiving the drug at a dose of 130 mg / m2, the concentration of leukocytes decreased to levels less than 5000 / μl.In 36% of patients this figure was less than 3000 / μL. As a rule, thrombocytopenia is more severe than leukopenia; however, both types of toxicity may be dose-limiting.

    Nausea and vomiting usually appear 4-6 hours after the administration of a full single dose of lomustine and last 24-48 hours, anorexia usually lasts for 2-3 days. The severity of these side effects can be reduced by dividing the single dose, calculated for 6 weeks, the sodium intake in the first three days of each 6-week cycle. Usually the drug is well tolerated if its use is accompanied by a prophylactic intake of antiemetics (for example, metoclopramide or chlorpromazine).

    In isolated cases, after prolonged treatment with lomustine and other preparations of nitrosourea, when a high cumulative dose was reached, renal failure, progressive azotemia, diminishing the size (atrophy) of the kidneys were observed. In this regard, it is recommended not to exceed the maximum total cumulative dose of lomustine 1000 mg / m2. However, it must be borne in mind that kidney damage is also possible in patients who received lower cumulative doses of the drug.

    Overdose:

    Lomustine overdose, including fatalities, has been reported.

    Possible symptoms of overdose: myelotoxicity. hematological toxicity, abdominal pain, nausea, vomiting, diarrhea, anorexia, drowsiness, dizziness, dysfunction of the liver, cough, shortness of breath. The antidote is not known. In case of an overdose, immediately wash the stomach. Treatment is symptomatic. If there are clinical indications, measures should be taken to compensate for the loss of blood cells.

    Interaction:

    Lomustin myelotoxicity may be enhanced by its combined use with theophylline or cimetidine, which is an antagonist of H2receptors. Lomustine is characterized by cross-resistance with other derivatives of nitrosourea, which is not observed for other alkylating agents.

    Phenobarbital, which activates microsomal enzymes of the liver, can enhance the metabolism of lomustine and accelerate its excretion from the body, so the use of phenobarbital before lomustine can reduce the antitumor activity of the latter.

    The use of the yellow fever vaccine increases the risk of systemic post-vaccination complications, including fatal. Patients undergoing immunosuppressive therapy are not allowed to use live vaccines.

    Joint use of antiepileptic and chemotherapeutic drugs, including lomustine, can cause complications caused by pharmacokinetic interaction between drugs.

    The simultaneous use of lomustine with other cytostatic drugs and radiotherapy can enhance myelotoxicity of lomustine. Lomustine when combined with amphotericin B may increase the toxicity of the latter.

    Special instructions:

    Lomustin should be medicated by an oncologist who has experience in antitumor therapy.

    Patients should be sure to inform that a single dose of the drug should be taken orally once every 6 weeks, during which it is not possible to take repeated doses, as well as about the inadmissibility of taking the drug at doses exceeding those prescribed by the doctor.

    The most common and severe toxic effect of lomustine is a delayed suppression of bone marrow function,manifested primarily by thrombocytopenia and leukopenia, which can lead to the development of bleeding and infections in weakened patients. Therefore, before starting taking the drug and throughout the course of treatment (once a week for at least 6 weeks after taking the drug), an extensive clinical blood test should be performed.

    When appointing lomustine therapy and determining the dose should be guided mainly by the values ​​of the concentration of hemoglobin, leukocytes and platelets in the blood serum. Myelosuppression caused by lomustine is cumulative, so the next dose should be selected taking into account the minimum value of the concentration of the formed blood elements observed after the last drug intake. The use of lomustine can potentially lead to impaired liver function, bycheck. It is necessary to periodically monitor the function of the liver and kidneys.

    The pulmonary toxicity of lomustine is dose-dependent. Before and during the treatment it is necessary to regularly monitor lung function. Patients with a baseline reduction of less than 70% of the forced vital capacity of the lungs, as well as diffusion ability of the lungs for the absorption of carbon monoxide (DLco), are included in the group of special risk.

    It was reported that a possible interrelation between the development of secondary malignant neoplasms and long-term use of nitrosoureas preparations.

    Fertility

    Men and women of childbearing age during treatment and, at least, within 6 months after its termination, it is necessary to apply reliable methods of contraception.

    Male patients should be informed of the risk of irreversible infertility as a result of lomustine treatment.

    Care should be taken when handling lomustine, as with any other antitumor drugs. Do not open capsules. Avoid contact of the contents of the capsules with the skin and mucous membranes. When in contact with the powder of the preparation, it is necessary to use specially materials used for this purpose, use gloves, after contact, dispose of used materials and wash hands with soap and water.

    Effect on the ability to drive transp. cf. and fur:The drug may affect the ability to drive and use mechanisms due to the risk of developing nausea and vomiting.When these undesirable phenomena appear, one should refrain from performing these activities.
    Form release / dosage:Capsules 40 mg.
    Packaging:

    For 20 capsules in a plastic jar with the control of the first autopsy. 1 bank together with instructions for use in a cardboard bundle.

    Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N016023 / 01
    Date of registration:25.11.2009 / 19.01.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:medac GmbHmedac GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspKorPharma, Open CompanyKorPharma, Open CompanyRussia
    Information update date: & nbsp02.04.2018
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