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Leukeran

Leukeran
Leukeran is used for lymphogranulomatosis, malignant lymphomas, chronic lymphocytic leukemia, Waldenstrom's macroglobulinemia.

Brand: Chlorambucil

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: April 2024
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Leukeran 5 mg
90 pills - 5 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$930.95 $10.34 $196.36 Add to cart
60 pills - 5 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$682.05 $11.37 $69.49 Add to cart
30 pills - 5 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$375.77 $12.53 No Add to cart
Leukeran 2 mg
90 pills - 2 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$661.15 $7.35 $118.28 Add to cart
60 pills - 2 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$483.92 $8.07 $35.70 Add to cart
30 pills - 2 mg
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$259.81 $8.66 No Add to cart

Product description

Pharmacological action of the Leukeran 

Buy Leukeran in Canada

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

Pharmacokinetics

The drug is well absorbed from the gastrointestinal tract. Cmax (492 ± 160 ng / ml) are reached within 0.25-2 hours after administration. T1/2 averages 1.3 ± 0.5 hours. The connection with plasma proteins is 99%.

After oral administration of chlorambucil labeled with 14C, the maximum plasma radioactivity is observed after 40-70 minutes. Chlorambucil is excreted from the blood plasma after an average of 1.5 hours.

It is rapidly and completely metabolized in the liver (metabolism is associated with S-oxidation of the side chain of butyric acid) to a pharmacologically active metabolite of phenylacetic mustard (bis-2-chloroethyl-2 (4-aminophenyl) -acetylic acid). It is excreted by the kidneys - 15-60%. T1/2 averages 1.8 ± 0.4 hours. The AUC of bis-2-chloroethyl-2 (4-aminophenyl) -acetylic acid is approximately 1.33 times higher than the AUC of chlorambucil, which confirms the alkylating activity of the metabolite.

Does not penetrate the BBB. Passes through the placental barrier.

Indications of the drug Leukeran

Leukeran for the treatment of non-Hodgkin's lymphoma

  • lymphogranulomatosis (Hodgkin's disease);

  • malignant lymphomas (including lymphosarcoma);

  • chronic lymphocytic leukemia;

  • Waldenstrom's macroglobulinemia.

Dosage regimen of the Leukeran 

Leukeran is usually one of the components of combination therapy, and therefore, when choosing doses and a regimen of drug administration, refer to the special literature. Leikeran is taken orally. The tablets should not be divided into parts.

Hodgkin's disease

As monotherapy, Leikeran is usually used at a dose of 0.2 mg / kg of body weight / day for 4-8 weeks.

Non-Hodgkin's lymphomas

As monotherapy, Leikeran is usually used initially at a dose of 0.1-0.2 mg / kg bw / day for 4-8 weeks; then maintenance therapy is carried out either at a lower daily dose, or in intermittent courses.

Chronic lymphocytic leukemia

The initial dose of Leukeran is 0.15 mg / kg of body weight / day until the total number of blood leukocytes drops to 10,000 / μl. 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.

Macroglobulinemia of Waldenstrom

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 in adults.

In case of lymphocytic infiltration of the bone marrow or in case of bone marrow hypoplasia, the daily dose of Leukeran should not exceed 0.1 mg / kg of body weight.

Contraindications

  • pregnancy;

  • lactation period;

  • hypersensitivity to any component of this drug.

With care (it is necessary to compare the risk and benefit) - inhibition of bone marrow function (severe leukopenia, thrombocytopenia and anemia); chickenpox (currently or recently transferred), herpes zoster, acute infectious diseases of a viral, fungal and bacterial nature, infiltration of bone marrow with tumor cells, gout (history), urate nephrourolithiasis, head trauma (history), epilepsy (history ), severe liver and kidney disease.

Application during pregnancy and lactation

Contraindicated: pregnancy, lactation period.

Application for violations of liver function

With caution (risk and benefit must be weighed) Severe liver disease.

Application for impaired renal function

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

Use in Children

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

Special instructions

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

If the outer shell is intact, contact of Leukeran tablets with the skin is harmless. Dividing tablets is prohibited. When using Leukeran tablets, the recommendations for the use of cytotoxic drugs should be followed.

Since Leukeran can cause irreversible inhibition of bone marrow function, during treatment it is necessary to systematically (at least 2-3 times a week) perform a complete blood count with the counting of peripheral blood cells.

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 Leukeran at the first sign of a decrease in the neutrophil count, but it should be remembered that the decrease in the neutrophil count may continue for 10 days or more after the last dose.

Patients who have previously been treated with cytostatic drugs or have undergone radiation therapy, Leykerai is prescribed no earlier than 1.5-2 months after the end of the previous treatment, provided that there is no severe leukopenia, thrombocytopenia and anemia.

Children with nephritic syndrome, patients receiving high-dose pulse therapy with Leukeran, and patients with a history of seizures should be closely monitored by a physician during the course of treatment with Leukeran, as they may have an increased risk of developing seizures.

Patients with impaired renal excretory function should be closely monitored. they may develop more severe myelosuppression associated with azotemia.

With an increase in the concentration of uric acid in the blood serum, it is recommended to use urine alkalizing agents. Nephropathy can be prevented with adequate fluid intake or allopurinol as needed.

Patients with severely impaired liver function should be given lower doses.

Since the use of alkylating agents is associated with a significant increase in the incidence of acute leukemia, when prescribing chlorambucil, 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, hyperexcitability, ataxia, repeated epileptoid seizures of the grand mal type. No specific antidote is known.

Treatment: immediate gastric lavage, monitoring and maintenance of vital body functions, careful monitoring of blood tests and general supportive measures, including transfusion of blood or blood components as indicated. Dialysis is not effective.

Drug interaction

With simultaneous use with drugs that inhibit hematopoiesis, myelotoxicity may increase.

With simultaneous use with anti-gout drugs, an adjustment of the doses of the latter is required (chlorambucil can increase the concentration of uric acid in the blood).

Tricyclic antidepressants, as well as haloperidol, maprotiline, monoamine oxidase inhibitors, phenothiazines, thioxanthenes, can lower the threshold of seizure activity and increase the risk of seizures.

Drugs that strongly bind to plasma proteins increase the toxicity of chlorambucil (competition at the level of protein binding).

With inactivated viral vaccines - a decrease in the production of antibodies in response to the vaccine; with live viral vaccines - an intensification of the replication of the vaccine virus, an increase in its side / adverse effects and / or a decrease in the production of antibodies.


Side effects

Myelosuppression, gastrointestinal disorders, liver dysfunction, jaundice, skin rash, fever, peripheral neuropathy, pneumonia, aseptic cystitis, seizures (in children with nephrotoxic syndrome), amenorrhea, azoospermia; rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, pulmonary fibrosis (with prolonged use), acute leukemia (after treatment).