Temozolomide

When ATH:
L01AX03

Pharmacological action.
Antitumor, alkylating, immunosuppressive.

Application.

Malignant glioma (glioblastoma multiforme, anaplastic astrocytoma) if recurrence or progression after standard therapy; widespread metastatic malignant melanoma (1 line therapy).

Contraindications.

Hypersensitivity, incl. to dacarbazine, severe myelosuppression, pregnancy, lactation.

Restrictions apply.

Age to 3 years with glioblastoma multiforme and up 18 years with malignant melanoma (efficacy and safety have not been determined).

Pregnancy and breast-feeding.

Contraindicated in pregnancy (there is no clinical experience), The appointment should notify the patient of the possible risks to the fetus.

Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)

At the time of treatment should stop breastfeeding (information on the penetration of breast milk is not available).

Side effects.

From the nervous system and sensory organs: fatigue (22%), headache (14%), drowsiness (6%), 2–5% — астения, malaise, dizziness, paraesthesia, taste disturbance.

Cardio-vascular system and blood (hematopoiesis, hemostasis): thrombocytopenia (19%) and neutropenia (17%) 3 or 4 degree in patients with glioma (hospitalization and / or cancellation of therapy 8% and 4% cases), у пациентов с меланомой — 20% and 22%, respectively (hospitalization and / or cancellation of therapy 3% and 1,3% cases), reversible myelosuppression (during the first cycle of treatment, with a maximum between 21 and 28 recently).

From the digestive tract: nausea (43%) and vomiting (36%) medium or low severity (no more 5 emetic episodes per day), severe nausea and vomiting (4%), constipation (17%,), anorexia (11%), diarrhea (8%), 2–5% — диспепсия.

Allergic reactions: rash (6%), 2–5% — зуд.

Other: fever (6%), 2–5% — болевой синдром, incl. abdominal pain, breathlessness, chills, alopecia, weight loss.

Cooperation.

Simultaneous reception of, oppressing bone marrow, It increases the likelihood of myelosuppression. Valproic acid decreases the clearance of temozolomide.

Overdose.

Symptoms: neutropenia, thrombocytopenia (при разовом приеме в дозах 1000 mg / m² and more).

Treatment: maintenance therapy.

Dosing and Administration.

Inside, fasting, at least 1 hours before the meal; capsules swallowed whole, with a glass of water. Adults and children over 3 years, previously subjected to chemotherapy: the initial dose - 200 mg / m² 1 once a day for 5 consecutive days in a 28-day treatment cycle. Patient, before undergoing chemotherapy, the initial dose - 150 mg / m² с последующим ее повышением во втором цикле до 200 mg / m² (если в 1-й день следующего цикла число нейтрофилов не ниже 1,5·10⁹/l, а число тромбоцитов — не ниже 100·10⁹/l). The course continues until disease progression (maximally 2 year).

Precautions.

Use only under medical supervision, with experience chemotherapy. Treatment starts, если число нейтрофилов не менее 1,5·10⁹/l, тромбоцитов — не менее 100·10⁹/l. Required clinical blood before and during therapy: 22 day, ie. 21 days after the first dose (but no later than 48 hours after this day) and further 1 once a week, пока число нейтрофилов не достигнет 1,5·10⁹/l, а число тромбоцитов — 100·10⁹/l. При числе нейтрофилов менее 1,0·10⁹/л или тромбоцитов менее 50·10⁹/l during any cycle of treatment to reduce the dose in the next cycle (минимальная рекомендованная доза — 100 mg / m²).

Women of childbearing age, as well as men during treatment and during 6 months after it is necessary to use effective contraception. Men are encouraged to seek advice on the cryopreservation of sperm prior to treatment because of the possible risk of irreversible infertility.

To apply caution in patients over 70 years (increased risk of neutrons- thrombocytopenia and) and in patients with severe liver and kidney function. After contact with the powder of the capsule on the damaged skin or mucous membranes, it should be immediately and thoroughly rinse with water. Experience in the use of glioma in children older 3 years limited.

Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

Antiemetics taken before or after administration of temozolomide. If you have severe vomiting (more 5 attacks during 1 d) necessary to conduct a preliminary antiemetic therapy.

Cooperation