Buy Alexan solution 50 mg/ml 20 ml bottle 1 pc.
  • Buy Alexan solution 50 mg/ml 20 ml bottle 1 pc.

Citarabine

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Clinical Pharmacology

The active ingredient of Alexan® is cytarabine.

Cytarabine belongs to the group of pyrimidine antimetabolites, inhibits DNA synthesis in the cell, mainly in the S-phase of the cell cycle. Antileukemic activity of the drug acquires as a result of phosphorylation to arabinosyl cytosine triphosphate (Ara-CTP), which competitively inhibits DNA polymerase.

Also, DNA synthesis is inhibited by embedding cytarabine in DNA. The cytostatic effect is dose dependent.

Several mechanisms for the development of cytarabine resistance are known: inhibition of membrane transport, deficiency of phosphorylating enzymes, increased activity of inactivating enzymes, reduced affinity of DNA polymerase.

Maintaining a high intracellular concentration of Ara-CTP is crucial for the development of a cytotoxic effect.

Indications

High-dose cytarabine therapy:

  • refractory to non-Hodgkin lymphoma therapy;
  • acute non-lymphoblastic and / or lymphoblastic leukemia, refractory to therapy, as well as variants with an unfavorable prognosis; recurrence of acute leukemia;
  • secondary leukemias after previous chemotherapy and / or radiation therapy;
  • manifest leukemia after transformation of prelecoses;
  • acute non-lymphoblastic leukemia in patients younger than 60 years of age (for consolidation of remission);
  • blast crises in chronic myeloid leukemia.

Composition

1 ml of 50 mg / ml solution contains:

Active substances: cytarabine 50.00 mg;

Excipients: sodium lactate 60% solution 10.40 mg, lactic acid (pH regulator) 0.045 mg, water for injection to 1 ml.

Citarabine is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Alexan solution
Cytosar Pfizer USA lyophilisate

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Citarabine

Dosage and Administration

The scheme and method of application vary with the use of different chemotherapy regimens.

Use of the drug Alexan® is possible only in specialized clinics under the supervision of doctors. Oral administration of the drug Alexan® is not active.

The drug Alexan® can be used both in monotherapy, and in combination with cytostatics and, in some cases, glucocorticosteroids.

The drug Alexan® can be administered intravenously (bolus or drip), subcutaneously, intramuscularly (usually used only during therapy aimed at maintaining remission), as well as intrathecal.

The average daily dose is 100-200 mg / m2. For elderly patients or those with reduced blood formation reserves, the daily dose should not exceed 50-70 mg / m2.

Induction of remission in acute leukemia: in combination with other anticancer drugs - 100 mg / m2 / day in the form of a continuous fast or slow intravenous infusion for 5-10 days or intravenously every 12 hours for 7 consecutive days. Total spend 4-7 treatment courses. Intervals between courses - at least 14 days.

High-dose therapy: high-dose therapy in the treatment of leukemias with a poor prognosis, as well as refractory leukemias and relapses, is carried out with the use of the drug Alexan® at a dose of 2-3 g / m2 of the body surface as an intravenous infusion of 1-3 hours, with a 12-hour interval, for 4-6 days as monotherapy or in combination with other anticancer drugs.

Intrathecal therapy (treatment of leukemia of the central nervous system): in acute leukemia, the dose of Alexan® is 5-75 mg / m2. The frequency of administration can vary from once a day for 4 days to 1 time in 4 days. Cytarabine is most often used on a 30 mg / m2 body surface every 4 days until normalization of indicators, followed by another additional administration. However, the dose and intervals between injections depend on the clinical situation. Due to the fact that the dose and mode of administration of the drug Alexan® depend on specially developed schemes of polychemotherapy, in each individual case, refer to the special literature.

In case of renal and hepatic insufficiency, it is necessary to use Alexan® with caution and, if necessary, reduce the dose, especially in patients with severe impaired liver and kidney function.

Cytarabine is eliminated during hemodialysis. It is not recommended to use the drug immediately before and immediately after the dialysis session.

In elderly patients (over 60 years), the use of high-dose therapy is possible only after a thorough assessment of the benefit / risk ratio.

Preparation of solution for infusion

Alexan® is diluted in the required dose in 0.9% sodium chloride solution or in 5% dextrose solution. The concentration of cytarabine should not exceed 100 mg / ml.

With intrathecal administration of Alexan®, you can use 0.9% sodium chloride solution or 5% dextrose solution. Do not use solvents containing preservatives.

It is recommended that you first take 5-8 ml of cerebrospinal fluid, mix it with an injection solution in a syringe, and then slowly inject the resulting solution back.

It is necessary to collect solution from a bottle just before use.

Use only freshly prepared clear solutions and only once!

Adverse reactions

Side effects depend on the dose, route of administration and duration of therapy.

On the part of the hematopoietic system: leukopenia, thrombocytopenia, anemia, megaloblastosis, reticulocytopenia. The decrease in the number of leukocytes is biphasic, with the first maximum decrease being reached by 7-9 days Then follows a short rise with a maximum on the 12th day. At the second and deeper decrease, the minimum number of leukocytes is noted in 15-24 days.In the next 10 days, the number of leukocytes increases rapidly. The decrease in the number of platelets is noted by 5 days, the minimum is noted between 12-15 days. In the next 10 days, there is a rapid increase in platelet count to baseline. The severity of these reactions depends on the dose and regimen of administration.

On the part of the digestive system: nausea, vomiting, loss of appetite, abdominal pain, diarrhea, inflammation or ulceration of the gastrointestinal mucosa (including the oral cavity, rectum, less often - the esophagus). Nausea and vomiting occur most frequently following rapid IV administration. With high-dose therapy (2-3 g / m2), ulceration of the gastrointestinal tract can be severe, may develop necrotic colitis, necrosis of the small intestine, cystic pneumatosis of the intestine, leading to peritonitis.

Liver and pancreas: impaired liver function, jaundice. In high-dose therapy, liver dysfunction with hyperbilirubinemia, sepsis, and liver abscess. It was also reported on individual cases of development of hepatic vein thrombosis (Budd-Chiari syndrome), as well as pancreatitis during high-dose therapy in combination with other antineoplastic drugs.

The nervous system: neuritis, neurotoxicity, headache, dizziness. Violations of the central nervous system are mainly observed during high-dose therapy (mainly disorders of the brain and cerebellum are detected) - nystagmus, dysarthria, ataxia, confusion, personality changes, drowsiness, coma. Violations by the central nervous system are reversible. Cases of peripheral motor and sensory neuropathy and late progressive ascending paralysis have also been reported. In some cases, nausea, vomiting, dizziness, fever, possibly associated with lumbar puncture, were observed after intrathecal administration. Cumulative neurotoxicity may also occur, especially with short intervals between doses. With intrathecal administration of the drug, individual cases of necrotizing leukoencephalopathy, paraplegia and blindness have been described.

From the senses: conjunctivitis (photophobia, burning in the eyes, pronounced tearing), keratitis; with high-dose therapy - reversible ulcerative keratitis, hemorrhagic conjunctivitis, visual disturbances.

On the part of the musculoskeletal system: for high-dose therapy, myalgia and / or arthralgia in the neck and lower extremities. An isolated case of rhabdomyolysis is described.

On the part of the respiratory system: sore throat, shortness of breath, pneumonia, diffuse interstitial pneumonitis (when used in medium doses of 1 g / m2), progressive respiratory distress syndrome leading to pulmonary edema and cardiomegaly with possible fatal outcome (when using high-dose therapy) .

Since the cardiovascular system: cardiomyopathy (including fatal when using cytarabine in high doses in combination with cyclophosphamide), pericarditis, transient arrhythmia.

On the part of the urinary system: renal dysfunction, urinary retention, hyperuricemia or urate nephropathy.

Dermatological reactions: itching, maculo-papular or urticarial rash, the appearance of pigment spots on the skin, skin ulceration, alopecia; rarely, severe skin rash leading to desquamation.

Allergic reactions: urticaria, anaphylaxis, edema.

Local reactions: inflammation of the subcutaneous fat at the injection site.

Infectious complications: viral, bacterial, fungal, parasitic or saprophytic flora-induced infections of any localization (including sepsis), usually mild or moderate in severity, but can be severe and sometimes fatal (their development is due to reduced immunity).

Other: fever, thrombophlebitis; in some cases - the syndrome of inadequate production of ADH.

6-12 hours after Alexan's drug administration, cytarabine syndrome can develop: fever, muscle pain, bone pain, sometimes chest pain, maculopapular rash, conjunctivitis, malaise (the effectiveness of GCS has been established).

Carefully

should be used in patients with hepatic and / or renal failure (due to an increased risk of side effects, especially during high-dose therapy), with drug-induced hematopoietic suppression, bone marrow infiltration with tumor cells, and acute viral infectious diseases ( chickenpox, herpes zoster, of a fungal or bacterial nature (the risk of severe complications and generalization of the process), diseases in which there is an increased risk of developing and ithia hyperuricemia (gout or urate nephrolithiasis). In the treatment of cytarabine, as well as the use of other drugs that suppress the immune system, vaccination with live vaccines should be avoided. In patients older than 60 years, the use of high doses of cytarabine is possible after a thorough assessment of the benefit / risk ratio.

Drug interactions

Do not mix in the same syringe or dropper with other drugs: pharmaceutically incompatible with heparin, insulin, methotrexate, fluorouracil, oxacillin, benzylpenicillin, methylprednisolone.

Combined use with other anti-tumor myelosuppressive drugs or radiation therapy enhances the cytotoxic and immunosuppressive activity of these drugs.

Patients receiving chemotherapy, including vincristine, prednisone, and cyclophosphamide with cytarabine or procarbazine, reversibly decrease the equilibrium concentration of digoxin in the blood plasma (impaired absorption due to toxic effects on the intestinal mucosa), and also reduces renal excretion of glycoside. An alternative for such patients is the use of digitoxin, the equilibrium plasma concentration of which does not change. In vitro studies of the interaction between gentamicin and cytarabine revealed the existence of antagonism, as a result of which it is possible to reduce the sensitivity of Klebsiella pneumoniae strains to gentamicin. Perhaps a decrease in the effectiveness of fluorocytosine with simultaneous use with cytarabine.

Immunosuppressants (azathioprine, chlorambucil, glucocorticosteroids, cyclophosphamide, cyclosporine, mercaptopurine, tacrolimus) increase the risk of developing infectious complications.

Killed viral vaccines - due to the suppression of the normal defense mechanisms of cytarabine, it is possible to reduce the formation of antibodies.

Live virus vaccines - due to the suppression of the normal defense mechanisms of cytarabine, potentiation of viral replication is possible, increased side effects, reduced antibody formation.

Pregnancy and Lactation

Preclinical studies have shown that cytarabine has embryotoxic and teratogenic effects. Therefore, during pregnancy, the use of the drug Alexan® is contraindicated.

It is not known whether cytarabine is excreted in breast milk, therefore, in order to avoid the toxic effect of the drug on the child, breastfeeding should be stopped for the period of treatment.

Special instructions

Use of the drug Alexan® should be carried out under the supervision of a qualified physician with experience in working with anticancer chemotherapeutic drugs and only in the hospital. Alexan® can be used both as a monotherapy, and in combination with other anticancer drugs. Dose and regimen of the drug is selected individually. In the case of combination therapy, the cumulative myelosuppressive effect of all drugs included in the treatment regimen should be considered.

Care must be taken when working with Alexan®.Dilute the drug should be in aseptic conditions in a specially designated room. This should be done by trained personnel. It is necessary to take all measures to prevent cytarabine solution on the skin and mucous membranes, in particular, to use protective clothing (gown, cap, mask, goggles and disposable gloves). If cytarabine comes in contact with skin or mucous membranes, rinse thoroughly with soap and water or (eyes) with plenty of water. Cytarabine strongly inhibits bone marrow function. Alexan® therapy should be started with caution in patients with already existing myelosuppression. It is necessary to regularly monitor the clinical analysis of blood (daily with induction therapy), plasma uric acid concentration, function of the bone marrow, liver, kidneys, central nervous system, lungs. If platelet decreases below 50,000 / mm3 or polymorphonuclear granulocytes below 1000 / mm3, the treatment regimen should be suspended or changed. The number of formed elements in the peripheral blood can continue to fall after discontinuation of the drug and reach a minimum level in 12-24 days. If there is evidence, therapy can be resumed when clear signs of recovery of hematopoiesis appear on the results of a bone marrow study.

It should be borne in mind that the development of such complications as bleeding (secondary to thrombocytopenia) and severe infection (secondary to granulocytopenia) is possible.

There are reports of the development of severe toxicity from the central nervous system, gastrointestinal tract and lungs (other than that developed with standard cytarabine therapy), sometimes with the development of a fatal outcome. Perhaps a reversible lesion of the cornea; dysfunction of the brain, especially the cerebellum, which are usually reversible, drowsiness, seizures; severe gastrointestinal ulcers, including cystic pneumatosis of the intestine, which can lead to the development of peritonitis; sepsis, liver abscess, pulmonary edema.

The occurrence of peripheral motor and sensory neuropathy was reported after the combined use of high doses of cytarabine, daunorubicin and asparaginase in adult patients with acute non-lymphoblastic leukemia. Therefore, care must be taken when using high doses of cytarabine and adjust doses in time to avoid irreversible neurological disorders. There are reports of the development of delayed progressive ascending paralysis, which led to the death of children with acute myeloid leukemia after intrathecal and intravenous administration of cytarabine in usual doses in combination with other drugs.

In patients who have previously been treated with a damaging effect on the central nervous system, such as intrathecal chemotherapy or radiation therapy, the use of high doses of cytarabine increases the risk of neurotoxicity. With the rapid intravenous administration of cytarabine, nausea and vomiting often occur within a few hours after application. It is possible to reduce the frequency of occurrence and severity of these side effects when using the drug infusion. The literature describes cases of development of peritonitis and colitis with a positive sample for hidden blood in combination with neutropenia and thrombocytopenia in patients using conventional doses of cytarabine in combination with other drugs. Patients were successfully treated without surgery. There are reports of the occurrence of cardiomyopathy (including fatal) with the use of high doses of cytarabine in combination with cyclophosphamide. If cytarabine syndrome occurs, the use of Alexan® should be stopped and treatment with glucocorticosteroids should begin. With the effectiveness of steroid therapy, treatment with cytarabine can be continued.

For the prevention of hemorrhagic conjunctivitis, topical glucocorticosteroids are recommended.

Care must be taken when using the drug in patients with impaired liver and kidney function.

When conducting high-dose therapy and intrathecal therapy, solutions containing benzyl alcohol cannot be used.

Like other antitumor agents, Alexan® can lead to the development of hyperuricemia due to the rapid breakdown of tumor cells. It is recommended to prevent hyperuricemia in patients with a high content of blast cells or with large tumor masses (for example, in non-Hodgkin's lymphomas): to receive allopurinol and a sufficient amount of fluid.

Vaccination of patients who are treated with Alexan® therapy should be carried out with extreme caution, after a thorough assessment of the hematological status and with the consent of the doctor conducting cytarabine therapy. The interval between the end of immunosuppressive therapy and vaccination depends on the type of immunosuppressant, the underlying disease and other factors, and varies from 3 months to 1 year. Cytarabine is excreted by hemodialysis. Therefore, patients on dialysis should not administer Alexan® directly before and during dialysis.

Women and men, as well as their sexual partners during treatment and for 6 months after its completion should use reliable contraception.

Influence on ability to steer the car and mechanisms

Patients receiving chemotherapy may have a reduced ability to drive a vehicle and work with mechanisms, so whenever possible you should refrain from practicing potentially hazardous activities that require increased concentration and psychomotor speed.

Overdosage

Symptoms: vomiting, diarrhea, pronounced suppression of bone marrow function, bleeding, development of infection, symptoms of neurotoxicity (impaired consciousness, movement disorders, convulsions, cognitive disorders).

Treatment: there is no specific antidote. If an overdose occurs, then symptomatic therapy (blood transfusion) should be carried out. In the case of a severe overdose, after intrathecal administration, the cerebrospinal fluid should be replaced with isotonic saline immediately. Cytarabine is eliminated during hemodialysis. However, there is no information on the effectiveness of hemodialysis in overdose of cytarabine.

  • Brand name: Alexan
  • Active ingredient: Citarabine
  • Dosage form: Injection.
  • Manufacturer: Meda Pharma GmbH & Co. KG

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