Temobel

General characteristics. Structure:

Active ingredient: 20 mg, 100 mg or 250 mg of a temozolomid.

Antineoplastic means of the alkylating action.

Pharmacological properties:

Pharmacodynamics. Temozolamid represents imidazotetrazinovy means with antineoplastic activity. At receipt in system circulation (at physiological values рН) is exposed to bystry chemical transformation with formation of active connection — a monometiltriazenoimidazolkarboksamid (MTIK). Believe that cytotoxicity of the last is caused mainly by alkylation of guanine in situation O6 and additional alkylation in situation N7.

Cytotoxic damage which develops afterwards most likely starts the mechanism of aberrant recovery of the methyl rest.

Pharmacokinetics. At oral administration it is quickly soaked up in digestive tract. Time of achievement of the maximum concentration in blood (Cmax) makes 0.5-1.5 h (the earliest - 20 min.). Gets through a blood-brain barrier and gets to cerebrospinal fluid. An elimination half-life (T 1/2) - 1.8 h. Communication with proteins of plasma - 10-20%.

Removal by kidneys: 5-10% in not changed look and in a look a 4-amino-5-imidazole-karboksamida of a hydrochloride or not identified polar metabolites. Meal causes decrease in Cmax by 33% and reduction of AUC by 9%. At children the indicator of AUC is higher, however the maximum tolerable dose at children and at adults is identical.

Indications to use:

For the first time the revealed multiformny glioblastoma: the combined treatment with radiation therapy with the subsequent adjuvant monotherapy. A malignant glioma (a multiformny glioblastoma or an anaplastic astrocytoma) in the presence of a recurrence or progressing of a disease after standard therapy. The widespread metastasizing melanoma (row drug I).

Route of administration and doses:

Inside, on an empty stomach. To adults and children 3 years, not being exposed to chemotherapy, - 200 mg / кв.м once a day within 5 days within a 28-day cycle are more senior; undergone chemotherapy - 150 mg / кв.м once a day; in the second cycle - 200 mg / кв.м, provided that in 1 day of the following cycle absolute number of neutrophils not less than 1.5 thousand / мкл, thrombocytes not less than 100 thousand / мкл. The minimum dose - 100 mg/sq.m. The maximum duration of treatment - 2 years. Capsules should be swallowed entirely, washing down with a glass of water.

Features of use:

The appointed dose has to be accepted with use of minimum possible number of capsules. Men and women have to use effective contraceptive remedies during treatment and within 6 months after its termination. A necessary condition to start use is: absolute number of neutrophils - not less than 1.5 thousand / мкл, thrombocytes - not less than 100 thousand / мкл. For 21 days after reception of the first dose carrying out an integrated analysis of blood, further weekly until the absolute number of neutrophils exceeds 1.5 thousand / мкл, thrombocytes - 100 thousand / мкл is necessary.

If the absolute number of neutrophils are lower than 1 thousand / мкл or the number of thrombocytes are lower than 50 thousand / мкл during any cycle of treatment, the dose in the following cycle has to be lowered on one step. The patient with severe vomiting (more than 5 attacks during 24 h) - antiemetic therapy before treatment.

During treatment to abstain from control of vehicles and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. To avoid hit of contents of the capsule (at its damage) on skin and mucous membranes. At hit on skin or mucous to wash out water.

Side effects:

Nausea, vomiting, increased fatigue, locks, headache, loss of appetite, diarrhea, skin rashes, fever, drowsiness, adynamy, abdominal pain, dizziness, decrease in body weight, indisposition, short wind, dyspepsia, alopecia, fever, itch, disturbance of taste, paresthesia; oppression of a marrowy hemopoiesis (thrombocytopenia, neutropenia).

Interaction with other medicines:

Valproic acid reduces clearance of a temozolomid.

The medicines oppressing a marrowy hemopoiesis increase risk of a miyelosupressiya.

Contraindications:

Hypersensitivity (including to a dakarbazin), the expressed miyelosupressiya, children's age (up to 3 years - for treatment of the recuring or progressing malignant glioma and up to 18 years - for treatment for the first time the revealed multiformny glioblastoma or a malignant melanoma), pregnancy, the lactation period.

With care: Renal or liver failure, advanced age.

Overdose:

Symptoms: neytro-and thrombocytopenia.

Treatment: there is no specific antidote, symptomatic therapy is carried out

Issue conditions:

According to the recipe

Packaging:

Capsules of 20 mg, 100 mg, 250 mg on 6 capsules in a blister strip packaging.