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Description:

White to greenish-gray or brown powder.

Composition:

Active substance: temozolomid – 100 mg;

Auxiliary substance: dextran phosphate sodium salt up to 1000 mg.

Release form:

Powder for gel preparation for topical use.

Pharmacotherapeutic group:

Antitumor agent of alkylating action.

ATX index:

L01AX03.

Clinical pharmacology:

Mechanism of action

Temodex is an antitumor agent of prolonged action for topical use, which is the temozolomide immobilized on a polymer carrier - dextran phosphate sodium salt. Temozolomide is an imidazotetrazine agent with antitumor activity. Upon entering the systemic circulation (at physiological pH values), it undergoes a rapid chemical transformation with the formation of an active compound - monomethyltriazenoimidazolcarboxamide (MTIC). It is believed that the cytotoxicity of the latter is mainly because of the alkylation of guanine at position O 6 and additional alkylation at position N7. Cytotoxic damage, which develops subsequently, most likely triggers the mechanism of aberrant recovery of the methyl residue.

Pharmacokinetics

The pharmacokinetics of temozolomide, immobilized on a polymer carrier (dextran phosphate sodium salt), with the local use of the medicine Temodex, is not currently studied. It is known that when taken orally, temozolomide is rapidly absorbed in the gastrointestinal tract. The time to reach the maximum concentration in the blood (Cmax) is 0.5-1.5 hours (at the earliest–20 minutes). Penetrates through the blood-brain barrier and enters the cerebrospinal fluid. The half-life (T1 / 2) is 1.8 h. The bond with plasma proteins is 10-20%. Renal excretion: 5-10% unchanged and as 4-amino-5-imidazolcarboxamide hydrochloride or unidentified polar metabolites. Eating causes a decrease in Cmax by 33% and a decrease in the area under the pharmacokinetic curve (AUC) by 9%. In children, the AUC index is higher, but the maximum tolerated dose in children and adults is the same - 1 g / m2.

Indications and usage:

Intraoperative chemotherapy of malignant brain tumors that are not subject to radical removal because of the peculiarities of biological growth, in order to have a local cytotoxic effect on the residual tumor tissue and prevent relapse and continued tumor growth. Indications for use are (i) newly identified glioblastoma multiforme (as part of combined treatment with radiation therapy), (ii) malignant glioma (glioblastoma multiforme or anaplastic astrocytoma).

Dosage and administration:

The medicine is used intraoperatively. 13-14 ml of water for injection is admitted into the vial of the medicine Temodex and kept for 20-30 minutes at room temperature with periodic shaking until swelling and gel formation. After the maximum available surgical removal of the brain tumor tissue, the porencephalic passage into the ventricle of the brain is isolated (if it has opened), thorough hemostasis is provided. After visualization of hemostasis, the resulting gel mass, preheated to a temperature of 37 ° C, is placed on the walls of the tumor bed.

Adverse reactions:

The most likely side effects are nausea, vomiting, fatigue, constipation, headache, decreased appetite, diarrhea, skin rashes, fever, drowsiness, asthenia, abdominal pain, dizziness, weight loss, malaise, shortness of breath, dyspepsia, alopecia, chills, itching, taste disorders, paresthesia; suppression of bone marrow hematopoiesis (thrombocytopenia, neutropenia).

Contraindications:

Hypersensitivity (including to dacarbazine), severe myelosuppression, childhood (up to 3 years - to treat recurrent or progressive malignant glioma and up to 18 years - to treat newly diagnosed glioblastoma multiforme or malignant melanoma). With caution: renal or hepatic insufficiency, old age.

Use in pregnancy and nursing mothers:

Use during pregnancy and lactation is contraindicated. Breastfeeding should be stopped for the duration of treatment.

Overdose:

With the local use of Demodex in the recommended doses, overdose phenomena are rare.

Symptoms: neuro- and thrombocytopenia.

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

Drug interactions:

Valproic acid reduces the clearance of temozolomide. Medications that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

Special instructions:

Men and women should use effective contraceptives during treatment and within 6 months after its end. A prerequisite for starting use is the absolute number of neutrophils - at least 1.5 thousand / ml, platelets - at least 100 thousand / ml. Patients with severe vomiting (over 5 attacks within 24 hours) are prescribed antiemetic therapy before and after treatment. During the treatment period, refrain from driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. There have been reports of cases of liver damage, including fatal liver failure, in patients taking temozolomide orally. Liver function indicators should be evaluated before neurosurgical surgery and intraoperative chemotherapy with Temodex. If laboratory parameters deviate from the norm, it is necessary to carefully assess the benefit-risk ratio during intraoperative chemotherapy with Temodex, including the possibility of developing liver failure with a fatal outcome.

Storage:

In a place protected from moisture and light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

1.5 years. Do not use it after the expiration date shown on the package.

Release conditions:

On medical prescription.

Package:

100 mg in glass vials № 1 in a pack of cardboard together with instructions for use.

Edited by:

UE «UNITEHPROM BSU»

220045, Republic of Belarus,

Minsk, Kurchatov str. 1

Phone/fax: +375 (17) 272-09-26

e-mail: unitehprombgu@gmail.com