Temozolomide - instructions for use, dose, side effects, contraindications

In the body it turns into monomethyltriazene imidazolecarboxamide, which penetrates into the nuclei of tumor cells and exerts an alkylating effect on DNA molecules, disconnecting the nucleotide chains.As a result, DNA synthesis in tumor cells ceases.

Pharmacokinetics:

After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 0.5-1.5 hours. The connection with plasma proteins is 10-20%.

Penetrates through the blood-brain and placental barrier. It is not metabolized in the liver.

The elimination half-life is 1.8 hours. Elimination by the kidneys.

Indications:

It is used for the treatment of malignant glioma (anaplastic astrocytoma, multimorphic glioblastoma). Used in a common metastatic melanoma.

ICD-10

II.C69-C72.C72 Malignant neoplasm of the spinal cord, cranial nerves and other parts of the central nervous system

II.D10-D36.D33 Benign neoplasm of the brain and other parts of the central nervous system

II.C43-C44.C43.9 Malignant melanoma of skin, unspecified

II.C69-C72.C71 Malignant neoplasm of brain

Contraindications:

Hepatic and renal failure, expressed myelosuppression, individual intolerance, children under 12 months.

Carefully:

With multimorphic glioblastoma - age up to 3 years and with malignant melanoma - up to 18 years.

Pregnancy and lactation:

Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside on an empty stomach (1 hour before meals), 200 mg / m². The treatment schedule is determined individually.

Side effects:

Central and peripheral nervous system: asthenia, hallucinations, cerebral circulation disorders, paresthesia.

Hemopoietic system: anemia, reversible myelosuppression.

Digestive system: anorexia, weight loss, nausea, vomiting, diarrhea.

Dermatological reactions: toxic epidermal necrosis, rash, erythema multiforme, alopecia.

Reproductive system: teratogenic effect, azoospermia, amenorrhea.

Allergic reactions.

Overdose:

Thrombocytopenia, neutropenia.

Treatment is symptomatic.

Interaction:

Simultaneous use with drugs that depress hemopoiesis increases the risk of myelosuppression.

Valproic acid increases the clearance of temozolomide.

Special instructions:

People of childbearing age are recommended to use effective methods of contraception during treatment and six months after taking the drug.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Temozolomide (Temozolomidum)