Universal reference book for medicines
Product name: LEIKLADIN (LEICLADIN)

Active substance: cladribine

Type: Antitumor drug.
Antimetabolite
Manufacturer: BELMEDPREPARATY (Republic of Belarus)
A typical clinical and pharmacological article
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
An analogue of 2'-deoxyadenosine, which is part of the DNA molecule.
Cladribine exhibits cytotoxic effects (due to the active metabolite of 5'-triphosphate-2-chloro-2'-deoxyadenosine) against fissile and non-dividing cells, inhibiting DNA synthesis and repair (inhibits ribonucleotide reductase catalyzing deoxynucleoside triphosphate formation, DNA polymerase and activates a specific endonuclease, which leads to single-strand breaks of DNA), which ultimately leads to cell death.Lymphoid cells are more sensitive to the drug (because they have a higher level of deoxycytidine kinase and a lower level of 5'-nucleotidase activity) than non-lymphoid ones.
PHARMACOKINETICS
In the CSF penetrates 25% of the drug.
It is subject to intracellular metabolism. At the initial stage phosphorylation to 5'-monophosphate carries out deoxycytidine kinase. Since the level of deoxycytidine kinase activity is higher than that of 5'-nucleotidase, and also due to drug resistance to adenosine deaminase, all three phosphorylated forms of 2-chloro-2'-deoxyadenosine rapidly accumulate in the cell. With IV introduction, T 1/2 is 5.7-19.7 hours. It is excreted mainly with urine (35%), insignificant (1%) with feces.
INDICATIONS
- hairy cell leukemia.

DOSING MODE
In / in the drip, in the form of 2 or 24 hour infusion.
The dose and duration of treatment are determined depending on the characteristics of the course of the disease and the severity of the condition. The recommended dose is 0.09-0.1 mg / kg / day for 7 days. Data on the increase in the antitumor effect in the course of additional courses are not available.

Before the introduction, the necessary amount of concentrate is diluted in 0.5-1 L of 0.9% sodium chloride solution, for the 24 infusions a bacteriostatic 0.9% solution of sodium chloride is used (contains benzyl alcohol as a preservative).

SIDE EFFECT
On the part of the hematopoiesis : leukopenia, neutropenia, thrombocytopenia, anemia, pancytopenia, aplastic and hemolytic anemia;
very rarely - myelodysplastic syndrome.

On the part of the digestive system: nausea, vomiting, anorexia, diarrhea, constipation, gastralgia, increased bilirubin and / or transaminases.


From the nervous system: headache, dizziness, insomnia, peripheral sensory neuropathies.


From the cardiovascular system: tachycardia, edema.


On the part of the respiratory system: cough, rapid breathing, interstitial pneumonitis, changes in percussion sound and auscultatory characteristics of respiration.


Dermatological reactions: a rash, skin peeling, skin itching, hives.


Local reactions: erythema, pain, swelling, thrombosis, phlebitis.


Other: hyperthermia, weakness, asthenia, fatigue, pain of different localization, purpura, petechiae, nosebleeds, decreased immunity;
predisposition to opportunistic infections, infections caused by Herpes simplex, Herpes zoster, cytomegalovirus.
CONTRAINDICATIONS
hypersensitivity;

- Moderate or severe chronic renal failure (CC less than 50 ml / min);

- moderate or severe hepatic impairment (4 or more on the Child-Pugh scale);

- simultaneous use of myelosuppressive drugs;

- Children's age (up to 16 years);

- Pregnancy;

lactation period.

With caution: oppression of bone marrow function, infection.

PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated with moderate or severe chronic renal failure (CC less than 50 ml / min).

Treatment of patients with mild renal insufficiency should be carried out under the direct control of kidney function.
Treatment should be discontinued if nephrotoxicity develops.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in moderate or severe hepatic insufficiency (CC less than 50 ml / min).

Treatment of patients with mild hepatic insufficiency should be carried out under the direct control of liver function.
Treatment should be discontinued if hepatotoxicity develops.
APPLICATION FOR CHILDREN
Contraindicated: children under 16 years.

APPLICATION IN ELDERLY PATIENTS
Careful monitoring of elderly patients is necessary (due to the lack of data on pharmacokinetics).

SPECIAL INSTRUCTIONS
Treatment with the drug should be carried out under the supervision of a doctor who has experience in the use of antitumor therapy.


Myelosuppression caused by the drug, dose-dependent and usually reversible, manifests itself within a month from the moment of treatment.
During treatment and at least for 4-8 weeks after careful monitoring of blood hematologic parameters is necessary.

Particular care should be taken in patients with initial oppression of bone marrow function of any origin because of the risk of prolonged hypoplasia.


In some cases, treatment can lead to severe forms of immunosuppression with a decrease in the level of CD4 leukocytes.
If hyperthermia occurs against a background of neutropenia, it is necessary to monitor the general condition of the patient during the first month of treatment and, if necessary, administer antibiotic therapy.

In the case of neurotoxicity, treatment with the drug should be suspended until the resolution of neurological symptoms.


Treatment of patients with renal and / or liver failure should be carried out under the direct control of kidney and liver function.
Treatment should be discontinued if nephro- or hepatotoxicity develops.

Careful monitoring of elderly patients is necessary (due to the lack of data on pharmacokinetics).

OVERDOSE
Symptoms: irreversible neurotoxicity (paresis / tetraparesis), acute nephrotoxicity, severe inhibition of bone marrow hematopoiesis (neutropenia, anemia, thrombocytopenia).


Treatment: symptomatic, antidote is unknown.

DRUG INTERACTION
When administered simultaneously or immediately after other myelotoxic drugs, additive inhibition of bone marrow function is possible.


When prescribed in high doses in combination with cyclophosphamide and radiation therapy, neurotoxicity (irreversible para- and tetraparesis) and nephrotoxicity (acute renal failure) increase.


Allopurinol and antibiotics increase skin rash.


When mixed with a 5% solution of dextrose - increased degradation of cladribine.

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