Leykeran - pharmacological agents from the group of anti-tumor agents used to treat cancer lymphoproliferative disorders.
Structure and Composition
Leykeran produced in the form of coated tablets. Tablets are brown, round biconvex. The active ingredient - chlorambucil. Also in the tablets include auxiliary components: anhydrous lactose, microcrystalline cellulose, colloidal silicon anhydrous, stearic acid.
Leykeran produced tablets of 2 mg. During dark glass bottles at 25, 50 and 100 tablets. In a cardboard box of one vial with the instruction.
Pharmacological action Leykerana
Leykeran relates to alkylating compounds which have antitumor effect. In the alkylation process is a process of formation of highly active free radicals. The exact mechanism of antitumor action is unknown, allegedly carried out cross-linking radicals to DNA and its replication process violation (division).
According to the instructions it Leykeran well absorbed from the digestive tract. Its maximum concentration in serum observed at 0, 5-2 hours after ingestion. The drug is excreted from the body after an average of 1.5 hours (0, 5:00). Leykeran almost completely metabolized in the liver. This drug does not pass through the blood-brain barrier, but penetrates the placental blood.
Leykeran indicated for such diseases:
- Hodgkin's disease (Hodgkin's disease);
- chronic lymphocytic leukemia;
- malignant lymphoma (e.g., lymphosarcoma);
- Waldenstrom's macroglobulinemia.
According to the instructions Leykeran contraindicated in patients who have recently had radiotherapy, chemotherapy or other drugs. Hypersensitivity to the drug and pregnancy are also contraindications to its use.
Precautions Leykeran prescribed for symptoms of depression of bone marrow function, varicella or herpes zoster, acute infectious diseases, viral or fungal origin. It is also necessary to compare the benefits and risks of the use of the drug if the patient is marked infiltration of bone marrow tumor cells, or he suffers from gout, epilepsy and suffered head injuries in history.
Instructions Leykerana: Dosage and administration
According to the instructions Leykeran can be used in combination with other drugs. The dosage and mode of administration selected individually chemotherapist doctor. Tablets Leykerana taken orally, their division is inadmissible.
Hodgkin's disease Leykeran on instructions may be designated as monotherapy in a daily dose of 0, 2 mg / kg body weight, duration of treatment is 4-8 weeks.
In treating non-Hodgkin's lymphomas Leykeran recommended daily starting dose of 0, 1 - 0, 2 mg / kg of body weight for 4-8 weeks. Then the patient is transferred to the maintenance dose (reducing it or assigning intermittent).
In chronic lymphocytic leukemia Leykeran used at a dose of 0, 15 mg / kg of body weight per day. The duration of therapy is determined based on laboratory parameters. A month after the end of the first course of treatment was resumed at a maintenance dose (0, 1 mg / kg).
In the treatment of Waldenstrom's macroglobulinemia Leykeran is the drug of choice. The starting daily dose of 6-12 mg / kg per day, and after reducing the number of blood leukocytes recommended move to a maintenance dose (2-8 mg / kg).
Leykeran used in children for the treatment of Hodgkin's disease and malignant lymphomas, patterns of use are similar to adults.
Side effects Leykerana
From the hematopoietic system in 10% of cases may decrease the number of white blood cells, platelets, hemoglobin decrease. At 0, 01% of cases there may be a suppression of bone marrow function.
From the digestive system in 1% of cases may develop nausea, vomiting, diarrhea, ulceration of the mucous membranes. At 0, 1% of the cases there Leykerana hepatotoxicity (cirrhosis, gepatonekroz, cholestasis with jaundice).
The respiratory system is extremely rare (less than 0, 01%) may cause the development of interstitial pneumonia or interstitial pulmonary fibrosis (with prolonged use Leykerana).
From the nervous system may develop seizures (in children) - to 0, 1-1% of the dose, also noted the uncertainty in walking, tremors, muscle twitching, sensory disturbances, paresis, weakness, anxiety (less than 0.01% of the cases).
Allergic reactions are rare. Sometimes there is a skin rash, rarely generalized allergic reaction (Stevens - Johnson syndrome, toxic epidermal necrolysis).
With the genitourinary system rarely develops aseptic cystitis (less than 0, 01%).
In case of overdose can occur leukeran: reversible pancytopenia (reduction in the number of cells), ataxia, irritability, recurrent epileptic seizures. There is no specific antidote. Treatment of overdoses is gastric lavage, appointment symptomatic therapy (including transfusions of blood components) under careful monitoring of vital body functions.
Interaction Leykerana with other drugs
When used with other Leykerana myelotoxicity drugs may experience increased adverse effects on the bone marrow.
Using simultaneously protivopodagricakih drugs require dose adjustments of the latter, since Leykeran can increase the content of uric acid in serum.
Using Leykerana with tricyclic antidepressants, MAO inhibitors, fenotiazenami increases the risk of seizures.
According to the instructions Leykeran refers to cytotoxic drugs, its use is possible only under the supervision of a specialist.
Dividing the tablets of this drug is prohibited. During therapy leukeran recommended 2-3 times a week to monitor the status of peripheral blood. There is no need to stop treatment leukeran at the first sign of neutropenia. But it must be remembered that reducing the number of neutrophils can grow in 10 days after the last dose.
Women of childbearing age in the treatment must be observed leukeran reliable methods of contraception.
Children with symptoms of nephrotic syndrome, and patients with a history of seizures should be under close medical supervision during the entire course of therapy leukeran, as they have an increased risk of seizures.