Temozolomide is an antitumor drug that is distinguished by the ability to suppress immunity, refers to the second generation of imidazotetrazine derivatives.
Form release, formulation and packaging
Temozolomide is intended for oral use. Capsules are packaged in vials of dark glass, packed in packs of cardboard.
Manufacturer of Temozolomide
- Temozolomide capsules are manufactured by India, Russia.
- Temozolomide-Teva - Israel.
Indications for use
- Treatment of malignant gliomas in complex therapy in cases of relapse of the disease;
- Malignant melanoma with metastases.
Mechanism of action
Temozolomide is destroyed, instead of it is formed monomethyltriazenoimidazolecarboxamide( MTIK).
MTIC is an active metabolite, decomposing into aminoimidazolecarboxamide + diazonium ion. The diazonium ion is an active component that transfers methyl groups to DNA, reacts with the nitrogenous base of DNA.
The main reaction occurs in the position of guanine O6, the auxiliary reaction occurs in the position of guanine N7, the position of adenine O3.The most significant damage occurs when DNA guanine is methylated at position O6.
During this reaction, thymidine is inserted in the DNA chain instead of cytosine, which is perceived by the cell control system as a signal to stop the cycle.
The interruption occurs at the G2 / M point corresponding to the stage preceding mitosis-cell division. Cell division does not occur, stopping at the control point G2 / M triggers the process of apoptosis( programmed destruction) of the cancer cell. Temozolomide undergoes suction in the stomach. The medicine is excreted by the kidneys.
Instructions for use: dosage
Capsules are drunk once 60 minutes before meals. The capsule is ingested with water. The drug is taken cyclically, the duration of each cycle is 28 days.
The initial dosage is:
- in patients who did not take chemotherapy treatment - 200 mg / m2 for 5 days, after which a pause is made, which lasts 23 days;
- in patients treated with chemotherapy - 150 mg / m2 for 5 days, then a break for 23 days.
For patients who undergo re-chemotherapy, the dosage can be increased to 200 mg / m2 if, on the first day of the recurrence cycle:
- neutrophils will be 1.5 × 109 / L;
- platelets - not less than 100 × 109 / l.
Side effects of
Temozolomide suppresses immunity. This quality is manifested by the propensity to infectious viral, bacterial, fungal infections. Common infections in the treatment are herpetic, candidal, flu-like conditions.
Laboratory blood tests revealed in the treatment with Temozolomide:
- decrease in the number of platelets, neutrophils, lymphocytes;
- is less likely to have a shortage of all types of blood cells, leukopenia, anemia.
Side effects are manifested by changes in the system:
- of the nervous - drowsiness, asthenia, headaches, depression, confused consciousness, tremor, poor coordination, dizziness;
- cardiovascular - edema of the extremities, tachycardia, vein thrombosis;
- immune - urticaria, anaphylactic shock, angioedema, edema;
- of the skin of - rashes, alopecia, itching, erythroderma, pigmentation, facial swelling;
- respiratory organs - shortness of breath, infections;
- of the digestive tract - nausea, anorexia, a disorder of the stool, a taste disorder, a pain in the abdomen.
Overdose
There is no antidote to Temozolomide. When an overdose is symptomatic treatment under hematological control.
Special instructions
Temozolomide is prohibited during pregnancy.
The drug has a teratogenic effect, belongs to category D according to the FDA classification of action on the fetus. The agent is not used in lactation because of the lack of data on its ability to penetrate into the milk.
Due to the damaging effect of the drug on the DNA during treatment, contraceptive methods should be used. Because of the risk of irreversible infertility, men are recommended to cryopreserve sperm before treatment.
Temozolomide is prohibited for children;
- for less than 3 years for glioblastoma multiforme;
- is less than 18 years old for melanoma.
Caution is used Temozolomide for the elderly, in the case of renal, hepatic insufficiency, lactose intolerance, galactose.
With severe nausea before or after treatment with Temozolomide, antiemetics are used, drugs specially designed to eliminate nausea in the treatment with antineoplastic agents.
The drug causes drowsiness, the ability to control moving vehicles, vehicles deteriorates.
Drug Interaction
The use of Temozolomide with medicines:
- valproic acid - leads to a decrease in the rate of its removal from the blood plasma;
- worsening the activity of the bone marrow - increases the risk of myelosuppression.
Reviews
Chemistry of Temozolomide is recommended for relapses of malignant brain gliomas. The use of treatment is able to stabilize the condition, not always for a long time, but prolong the time of remission.
Price of medicine
Cost of Temozolomide( package 5 capsules, India) in rubles:
- 100 mg - 34144;
- 250 - 85361.
Temozolomide Packing, India, 20 capsules, price in rubles:
- 100 mg - 136578;
- 250 - 341445.
The cost of Temozolomide Teva( 5 capsules, Israel) in rubles:
- 20 mg - 2161;
- 100 - 9944.
Analogues of Temozolomide
Drugs used to treat malignant glioblastomas, melanomas with metastases that have a similar effect - Carmustine, Carboplatin, Cisplatinum, Avastin, PCV protocol, which includes lomustine, vincristine, procarbazine.
Synonyms
Drugs are synonyms for the active substance - Temozolomide-Teva, Temcital, Temodal, Astroglyph, Tezalom.
Conditions for dispensing from pharmacies
Withdraw by prescription.
Storage conditions, shelf life
The drug is suitable for 3 years, keep it in a dark place, at a temperature not exceeding 30 ° C.