Cladribine is a drug with antitumor activity and immunosuppressive action. The drug has found wide application for the therapy of hairy cell leukemia and multiple sclerosis.
Form release, formulation and packaging
Cladribine is released in the form of a colorless concentrate solution for the preparation of an infusion solution.
Cytostatic is produced in 10 ml vial No. 1, No. 40 or in 5 ml No. 5, No. 10 ampoules.
Manufacturer
The drug is produced in China, Zunan Kommers.
Indications for use
Cladribine is widely used for the therapy of the following conditions:
- Hairy cell leukemia;
- Follicular non-Hodgkin's lymphomas;
- Lymphocytic leukemia;
- Waldenstrom Macroglobulinemia;
- Multiple Sclerosis.
Contraindications
The drug is prohibited in the following cases:
- Hypersensitivity to any ingredient in the preparation;
- Child's age;
- Against the background of the use of other mielosupressive drugs;
- Chronic liver pathologies;
- Pregnancy and lactation;
- Moderate or severe renal pathology in which creatinine clearance does not exceed 50 mL / min.
Mechanism of action
Cladribine is an analogue of the purine glycoside, which acts like antimetabolite.
The chemical compound is resistant to the deamination process by replacing the hydrogen atom with chlorine in the second position.
Cladribine is a pro-drug that cells rapidly absorb after intravenous administration.
Next, intracellular phosphorylation occurs, converting the compound into the active nucleotide 2-chloro-oxy-adenosine-5 triphosphate.
The active form of Cladribine accumulates in lymphocytes and other hematopoietic cells.
The drug has a cytotoxic effect that involves inhibition of DNA synthesis, inhibition of ribonucleotide reductase, specific biochemical processes that destroy actively proliferating cells also develop.
Lymphoid cells are highly sensitive to the drug. Up to 25% Cladribine is able to penetrate into the cerebrospinal fluid. The elimination period is from 5 to 19 hours. The drug is excreted in the urine, in an insignificant amount with a caloric mass.
Instructions for use Cladribine
In hair follicular leukemia, the cytotoxic agent is administered parenterally, the dosage averages 0.09-0.1 mg / kg per day. The course of therapy is 7 days.
Multiple sclerosis shows oral administration of the drug at 10-20 mg / day. Scheme and duration of therapy should be selected by the doctor depending on the clinical picture and tolerability.
Side effects of
During the application of Cladribine, the following undesirable effects occur:
- On the part of the hematopoiesis , development of leukopenia, neutropenia, thrombocytopenia, anemia( hemolytic or aplastic), pancytopenia is possible. There is also a development of myelodysplastic syndrome;
- In some cases, the development of rash , skin flaking, itchy skin;
- From the side of the central nervous system: sleep disorders, dizziness, development of peripheral sensory neuropathy, headache;
- Possible development of puffiness and increased heart rate , as a violation of the cardiovascular system;
- On the part of the digestive system: nausea and vomiting, anorexia, diarrhea or constipation, stomach pain, increased bilirubin;
- Respiratory organs: cough, increased respiratory rate, violation of auscultatory characteristics;
- The appearance of erythema , soreness, swelling, thrombosis and phlebitis is possible at the site of cytostatic administration.
Also patients can note the following symptoms: increased fatigue, asthenia, hyperthermia, pain syndrome, development of purpura, nasal bleeding, decreased immunity, which is accompanied by the development of opportunistic infections.
Overdose
With increasing dose, the development of symptoms of acute nephrotoxicity and irreversible neurotoxicity( paresis, tetraparesis) is possible. The patient is marked myelosuppression.
This condition requires urgent symptomatic therapy.
Special instructions
Male patients should use contraceptives for 3 months after therapy. This is due to the negative effect of Cladribine on the process of spermatogenesis.
If the partner becomes pregnant, it is necessary to inform the gynecologist about the possible embryotoxic and teratogenic effects of the drug.
Caution is prescribed cytostatics in elderly patients due to the lack of clinical information.
If the patient has a history of renal or hepatic insufficiency, it is necessary during the therapy to constantly monitor the work of these organs. When developing signs of hepa- or nephrotoxicity, discontinue treatment.
If necessary, prescribe antibiotics, and cytostatics stop treatment. Cladribine therapy is contraindicated within 3 months after the administration of live or attenuated vaccines due to an increased risk of infection.
For neurotoxic therapy, therapy should be discontinued until well-being is restored. There are reports of the appearance of melanoma, ovarian cancer and pancreas on the background of treatment with cytostatics.
The decision to use Cladribine in cancer patients with multiple sclerosis must be made on an individual basis. If, during treatment, the patient is dizzy, it is better to give up driving.
Drug Interaction
When combined therapy with immunomodulating medications requires continuous clinical monitoring along with an assessment of the parameters of a general blood test.
Short-term treatment with glucocorticosteroids allows the co-administration of Cladribine with Interferon or Ibuprofen. But we need constant monitoring of hematological parameters.
The appointment of cytotoxic to patients who received immunosuppressants( Methotrexate, Mitoxantrone, Cyclosporine) or glucocorticosteroids for a long time, is contraindicated. This is associated with an increased risk of side effects of the cytostatic.
Drugs that inhibit the activity of proteins ABCG2( Atazanivir, Ritonavir, Lopinavir) in the organs of the digestive system are able to increase the bioavailability of Cladribine( up to 2.5 times) and its systemic effect.
Cladribine is sensitive to acidic conditions, so drugs that change the acidity of the stomach, can affect the bioavailability of the cytostatic. However, studies have shown that simultaneous administration of Cladribine and omeprazole is possible.
Reviews
Antonina, 37, Moscow:
They offered to take part in the Cladribine study, I have multiple sclerosis. Therapy involves taking the drug 2 times a year in a short course. I receive a drug for 4 years - I managed to completely exclude the development of exacerbations.
Maria, 47, Astrakhan:
The doctor appointed Cladribine for hairy cell leukemia. The drug was effective enough, but greatly reduced the number of lymphocytes, so after treatment I developed pneumonia.
Price for Cladribine in Russia
The cost of the drug in Russian pharmacies varies from 26.3 to 37.7 thousand rubles for 7 bottles of 10 ml.
Analogs
Among the group analogs, the following drugs are distinguished:
- Mercaptopurine;
- Methotrexate;
- Hydroxycarbamide;
- Fluoraffur;
- Cytarabine.
Synonyms for
The following are the synonyms: Leukladin, Vero-Cladribine, Movecctro.
Terms of dispensing from pharmacies
The cytotoxic belongs to list B, so it is prescription-dispensed.
Storage conditions and shelf life
Cladribine must be stored in a dark place where sunlight does not penetrate. Temperature regime: 2-8 ° С.Cytostatics should be used within 5 years.