Universal reference book for medicines
Product name: LEUKERAN (LEUKERAN)

Active substance: chlorambucil

Type: Antitumor drug.
Alkylating compound
Manufacturer: GlaxoSmithKleining Trading (Russia) manufactured by EXCELLA (Germany)
Composition, form of production and packaging
The tablets covered with a cover of
brown color, round, biconcave, on one side an engraving "L", on another - "GX EG3".

1 tab.

chlorambucil 2 mg

Excipients: lactose anhydrous, microcrystalline cellulose, silicic colloid anhydrous, stearic acid.

Composition of the shell: Opadry brown YS-1-16655A (hypromellose, titanium dioxide, macrogol, iron oxide, yellow, iron oxide red).

25 pcs.
- bottles of dark glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Chlorambucil refers to aromatic derivatives of nitrogen mustard gas and acts as a bifunctional alkylating drug.
Alkylation occurs through the formation of highly active radicals of ethylenimonium. Probably, there is a cross-linking of ethyleneimoyium radicals to a DNA spiral and a subsequent disruption of the DNA replication process.
PHARMACOKINETICS

The drug is well absorbed from the digestive tract.
C max (492 ± 160 ng / ml) are achieved after 0.25 -2 h after administration. T 1/2 is an average of 1.3 ± 0.5 h. The connection with plasma proteins is 99%.
After ingestion of chlorambucil, labeled 14 C, the maximum radioactivity of the plasma is observed after 40-70 minutes.
Chlorambucil is excreted from the blood plasma on average after 1.5 hours.
Rapidly and completely metabolized in the liver (metabolism is associated with S-oxidation of the side chain of butyric acid) to the pharmacologically active metabolite of phenylacetic mustard (bis-2-chloroethyl-2 (4-aminophenyl) -acetyl acid).
It is excreted by the kidneys - 15-60%. T 1/2 is an average of 1.8 ± 0.4 h. The AUC of bis-2-chloroethyl-2 (4-aminophenyl) -acetyl acid is approximately 1.33 times greater than the chlorambucil AUC, which confirms the alkylating activity of the metabolite.
Does not penetrate the BBB.
Passes through the placental barrier.
INDICATIONS

- lymphogranulomatosis (Hodgkin's disease);

- malignant lymphomas (including lymphosarcoma);

- chronic lymphocytic leukemia;

Waldenstrom macroglobulinemia.

DOSING MODE

Leukeran is usually one of the components of combination therapy, so when choosing the doses and the mode of administration of the drug should refer to the special literature.
Leukeran is taken internally. Tablets should not be divided into parts.
Hodgkin's disease

In the form of monotherapy, Leicheran is usually used at a dose of 0.2 mg / kg body weight / day for 4-8 weeks.

Non-Hodgkin's Lymphomas

In the form of monotherapy, Leicheran is usually used initially at a dose of 0.1-0.2 mg / kg body weight / day for 4-8 weeks;
then support therapy is provided either at a lower daily dose, or with intermittent courses.
Chronic lymphatic leukemia

The initial dose of Leykeran is 0.15 mg / kg body weight / day until the total number of blood leukocytes decreases to 10,000 / μl.
After 4 weeks after the end of the first course of therapy, treatment can be resumed at a maintenance dose of 0.1 mg / kg body weight / day.
Waldenstrom's macroglobulinemia

Leukeran is the drug of choice.
The initial dose is 6-12 mg / day daily, and after the development of leukopenia, it is recommended to switch to maintenance therapy at a dose of 2-8 mg / day daily for an indefinite period of time.
Children:
Leukeran can be used to treat Hodgkin's disease and non-Hodgkin's lymphomas in children using the same regimens as adults.
With lymphocyte infiltration of the bone marrow or in the case of bone marrow hypoplasia, the daily dose of Leykeran should not exceed 0.1 mg / kg of body weight.

SIDE EFFECT

Frequency determination: very often (> 1/10), often (> 1/100 to <1/10), sometimes (> 1/1000 to <1/100) rarely (> 1 / 10,000 to <1 / 1000), very rarely (<1/10000).

On the part of the hematopoiesis system: very often - leukopenia (reversible if the drug is stopped on time), thrombocytopenia, lymphopenia, neutropenia, decreased hemoglobin content;
extremely rare - irreversible oppression of bone marrow function.
From the gastrointestinal tract: often - nausea, vomiting, diarrhea, ulceration of the oral mucosa;
rarely - hepatotoxic effect of toxic-allergic genesis (hepatonecrosis or cirrhosis, cholestasis, jaundice).
On the part of the respiratory system: very rarely - interstitial lung fibrosis (with prolonged use of chlorambucil), interstitial pneumonia.

Allergic reactions: sometimes - skin rash;
rarely - urtikaropodobnaya rash, angioedema; extremely rarely - multiforme erythema exudative (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
From the nervous system: often - convulsions in children with nephrotic syndrome;
rarely - local and / or generalized convulsions in children and adults receiving chlorambucil in therapeutic doses daily or courses of high-dose pulse therapy; very rarely - uncertainty when walking, tremor, muscle twitching, peripheral neuropathy, paresis, agitation, confusion, marked weakness, anxiety, hallucinations.
From the urinary system: very rarely - aseptic cystitis.

Other: drug hyperthermia, hyperuricemia or nephropathy due to increased formation of uric acid (the result of rapid decay of cells), menstrual disorder, secondary amenorrhea, azoospermia, secondary malignancy.

CONTRAINDICATIONS

- Pregnancy;

- the period of breastfeeding;

- Hypersensitivity to any component of this drug.

With caution (it is necessary to compare the risk and benefit) - depression of bone marrow function (expressed leukopenia, thrombocytopenia and anemia);
chicken pox (currently or recently transferred), herpes zoster, acute infectious diseases of viral, fungal and bacterial nature, bone marrow infiltration by tumor cells, gout (history), nephrourolytiasis urate, head trauma (history), epilepsy (in anamnesis ), severe liver and kidney disease.
PREGNANCY AND LACTATION

Contraindicated: pregnancy, lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution (it is necessary to compare the risk and benefit) - severe kidney disease.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution (it is necessary to compare the risk and benefit) severe liver disease.

APPLICATION FOR CHILDREN

Children: Leukeran can be used to treat Hodgkin's disease and non-Hodgkin's lymphomas in children using the same regimens as adults.

SPECIAL INSTRUCTIONS

Leukeran is a cytotoxic agent that should be used only under the supervision of a physician with experience in the use of such drugs.

With an undamaged outer shell, the contact of Leukeran tablets with the skin is harmless.
The division of tablets is prohibited. When using Leukeran tablets, recommendations for the use of cytotoxic drugs should be followed.
Since Leukeran can cause irreversible suppression of bone marrow function, during the treatment it is necessary to perform a systematic blood test (at least 2-3 times per week) with counting the formed elements of peripheral blood.

When used in therapeutic doses, Leukeran inhibits the production of lymphocytes and to a lesser extent affects the number of neutrophils and platelets, as well as the level of hemoglobin.

It is not necessary to stop taking Leykeran at the first sign of a decrease in the number of neutrophils, but remember that a decrease in the number of neutrophils can continue for 10 or more days after the last dose.

Patients previously treated with cytostatic drugs or undergoing radiotherapy are given no earlier than 1.5-2 months after the end of the previous treatment, provided there is no pronounced leukopenia, thrombocytopenia and anemia.

Children with nephritic syndrome, patients receiving high-dose pulsed therapy with Leykeran, as well as patients with convulsive seizures in the anamnesis should be carefully monitored by the doctor during the course of treatment with Leykeran, since they may be at increased risk of developing seizures.

Patients with violations of the excretory function of the kidney should be carefully monitored, as.
they can develop more pronounced myelosuppression associated with azotemia.
When the concentration of uric acid in the blood serum increases, the use of funds that alkalinize urine is recommended.
The development of nephropathy can be prevented by adequate fluid intake or by the appointment of allopurinol, if necessary.
Patients with severe impairment of liver function should be given smaller doses.

Since the use of alkylating agents is associated with a significant increase in the incidence of acute leukemia, when chlorambucil is prescribed, it is necessary to compare the risk of acute leukemia with the potential therapeutic effect of this drug.

Patients of childbearing age should use reliable methods of contraception.

OVERDOSE

Symptoms: reversible pancytopenia, increased excitability, ataxia, repeated epileptoid seizures of the type grand mal.
The specific antidote is not known.
Treatment: immediate gastric lavage, monitoring and maintenance of vital body functions, careful monitoring of blood tests and general supportive activities, including transfusion of blood or its components according to indications.
Dialysis is not effective.
DRUG INTERACTION

When used simultaneously with drugs that oppress hemopoies, it is possible to increase myelotoxicity.

When used simultaneously with antidotal drugs, adjustment of the doses of the latter (chlorambucil may increase the concentration of uric acid in the blood) is required.

Tricyclic aide depressants, as well as haloperidol, maprotiline, monoamine oxidase inhibitors, phenothiazines, thioxantenes can reduce the threshold of convulsive activity and increase the risk of convulsions.

Preparations, intensely binding to plasma proteins, increase the toxicity of chlorambucil (competition at the level of communication with protein).

With inactivated viral vaccines, reduced antibody production in response to vaccine administration;
with live viral vaccines - intensification of the replication process of the vaccine virus, increased side effects / adverse effects and / or decreased production of antibodies.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List A. Store at 2-8 ° C in a place inaccessible to children.
Shelf life - 3 years. Do not use the drug after the expiry date printed on the package.
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