Asparaginase is an antitumor agent. This is the only currently available enzyme preparation that can be used to treat acute leukemia.
The active ingredient is found in nature. To isolate it, serum of guinea pig and bacteria are used. The use of the first option is difficult. Therefore, an E. coli from various strains of bacteria is more often used.
Composition, form and packaging
The active ingredient is L-Asparagine amidohydrolase. This substance is available in the form of a white powder. It easily dissolves in water, but is not subject to structural changes in methanol, acetone, chloroform.
Manufacturer
This medicine is produced in many countries. On an industrial scale, they are produced from various sources.
Powder for the preparation of solution for intravenous or intramuscular injection is produced in Russia, Germany, Japan, Ukraine, India.
Indications for use
It is prescribed for adults and children with blood cancer.
Together with other medications it is used to prolong remission with lymphoblastic leukemia, lymphoblastic non-Hodgkin's lymphomas.
However, it is not recommended to use the drug as part of maintenance therapy schemes, as resistance to the drug develops rapidly. The cells cease to synthesize asparagine on their own.
Contraindications
One of the main contraindications is
- pancreatitis at the time of treatment initiation or its presence in the medical history,
- allergic reactions to the active substance,
- disorders of the kidney and liver,
- pregnancy or the period of breastfeeding,
- CNS disease.
Pharmacological action of
Asparaginase leads to the cleavage of the amino acid asparagine. It is needed to maintain the vital functions of the cell.
The effect of this active substance leads to a decrease in the level of amino acid in tumors that are unable to produce asparagine on their own. The result is a violation of the synthesis of protein, DNA and RNA.
The maximum amount in plasma is achieved with intravenous administration almost immediately. If the drug is administered intramuscularly, then the greatest amount of action appears after 14-24 hours.
The active substance passes into the reticulo-endothelial system, where it slowly decomposes to inactive substances. The half-life is 8-30 hours.
Instructions for use Asparaginase: dosage
The first administration is carried out in a hospital. First, a test is made to study the sensitivity of the individual organism to the drug.
For manipulation, 10 IU is dissolved in 0.1 ml of water for injection and injected subcutaneously. The reaction is monitored for an hour. To obtain a control reaction, the same amount of isotonic solution is administered. If there is no negative reaction, then treatment begins.
A single dose of 200-300 IU per kilogram of body. Depending on the treatment regimen and the age of the patient, the dosage is reduced by the doctor.
Side effects of
Allergic manifestations are possible in 20-35% of cases. It is expressed by the appearance of a rash or blisters. In some cases, anaphylactic shock with a fatal outcome is possible.
The risk of negative drug manifestations increases with repeated administration of the drug.
In the first hours, body temperature can rise. Sometimes there is a chill. These manifests cease on their own.
Other adverse reactions are noted:
- From the side of the digestive system: pancreatitis, pseudocyst formation. Therefore, within four months after the end of treatment, the patient should be observed by the doctor. There may be nausea and vomiting.
- Metabolic side: decreased glucose uptake, lowered insulin levels. Sometimes ketoacidosis develops.
- From the side of the urinary system: a violation of kidney function.
- From the nervous system: drowsiness, confusion, convulsions.
Overdose
If the dose is incorrect, nausea, vomiting, fever, coagulation, anaphylactic shock are noted. For treatment, antihistamines and calcium chloride are used.
Special instructions
A tolerance test is carried out before the start. With intramuscular injection, the volume should not exceed 2 ml. If more is required, the dose is divided.
To reduce the risk of allergic reactions, a fractional administration is important. When they occur, treatment stops, and antihistamines are prescribed.
During treatment, monitoring of liver and kidney function, other organs is assigned.
In case of accidental skin contact, wash the area with water for 15 minutes. Toxic manifestations are most pronounced in adults than in children.
Drug Interactions
Asparaginase reduces the activity of methotrexate and other drugs that affect the papules of tumor cells.
Simultaneously, there is a mutual increase in the action of immunosuppressants. Prednisolone increases toxicity. With simultaneous reception with uricosuric drugs, the risk of developing nephropathy increases.
Price Asparaginase
The cost of the drug starts at 2300 rubles. This is the cost of one bottle of 10 thousand IU.If the same amount of active substance is bought in a pack of 5 bottles, the cost is from 17450 rubles.
Analogs and synonyms for
- Asparaginase Medak,
- Vero-Asparaginase,
- Leynase,
- PEG-L-asparaginase.
- Krasnitin,
- Crasnitinum,
- Leunase.
Conditions for dispensing from pharmacies
The drug is on the list B. It is available on prescription.
Storage Conditions and Shelf Life
Shelf life 24 months. After the end of the drug is prohibited. Store in a dry place, away from exposure to sunlight at temperatures not exceeding 10 degrees.