Temodal lyophilizate solution for infusion 100mg vials, 1pc

Composition

1 bottle contains:

Active ingredients:

temozolomide 100 mg.

Auxiliary substances:

mannitol 600 mg,

threonine 160 mg,

polysorbate 80 120 mg,

sodium citrate dihydrate 235.2 mg,

concentrated hydrochloric acid 160 mg.

In a bottle of colorless glass 100 mg of lyophilizate.

In a cardboard box 1 bottle.

Pharmacological action

Pharmacodynamics

Antitumor agent of alkylating action, has an imidazotetrazine structure.

In the systemic circulation, at physiological pH values, it undergoes a rapid chemical transformation with the formation of the active compound – monomethyltriazenoimidazolecarboxamide (MTIC). It is believed that the cytotoxicity of MTIC is primarily due to the alkylation of guanine at the O6 position and additional alkylation at the N7 position. Apparently, cytotoxic damage resulting from this triggers the mechanism of aberrant reduction of the methyl residue.

Pharmacokinetics

After oral use, it is rapidly absorbed from the gastrointestinal tract.

Cmax of temozolomide in plasma is reached on average in 0.5-1.5 hours (at least 20 minutes) after taking a single dose. When taken with food, there was a 33% decrease in Cmax and a 9% decrease in AUC.

Temozolomide quickly penetrates the BBB and enters the cerebrospinal fluid.

Binding to plasma proteins is 10-20%.

T1 / 2 from plasma is approximately 1.8 h. It is rapidly excreted from the body mainly by the kidneys.

24 hours after oral use, about 5-10% of the dose is detected unchanged in the urine; the remainder is excreted as 4-amino-5-imidazole-carboxamide hydrochloride or unidentified polar metabolites.

Indications

• Malignant gliomas (including glioblastoma multiforme, anaplastic astrocytoma) in the presence of relapse or progression of the disease after standard therapy;
• common metastatic malignant melanoma (as a first-line therapeutic agent).

Contraindications

• Severe myelodepression;
• pregnancy;
• lactation (breastfeeding);
• hypersensitivity to temozolomide or dacarbazine.

Side effects

From the digestive system: nausea, vomiting, constipation, anorexia, diarrhea, abdominal pain, dyspepsia, taste disorders.

From the central nervous system: fatigue, headache, drowsiness, dizziness, paresthesia.

Dermatological reactions: skin rashes, alopecia, pruritus.

Respiratory system disorders: shortness of breath.

From the hematopoietic system: thrombocytopenia and neutropenia of 3 or 4 degrees, pancytopenia, leukopenia and anemia.

Others: fever, asthenia, weight loss, malaise, chills.

Interaction

When temozolomide is co-administered with valproic acid, there is a mild but statistically significant decrease in the clearance of temozolomide.

Concomitant use of temozolomide with other drugs that have a depressing effect on the bone marrow may increase the risk of developing myelosuppression.

How to take, course of use and dosage

Individual, depending on age and previous chemotherapy.

Overdose

When using the drug in doses of 500,750,1000 and 1250 mg/m2 (the total dose received during the 5-day treatment cycle), the dose — limiting toxicity was hematological, which was noted at any dose, but more pronounced at higher doses. A case of overdose (taking a dose of 2000 mg per day for 5 days) was described, which resulted in pancytopenia, pyrexia, multiple organ failure and death. When taking the drug for more than 5 days (up to 64 days), among other side effects, hematopoiesis suppression was noted, complicated or not complicated by infection, in some cases-long and pronounced, with a fatal outcome.

Treatment: The antidote to Temodal is unknown. Hematological monitoring and, if necessary, symptomatic therapy are recommended.

Special instructions

Use with caution in patients with severe hepatic or renal impairment, elderly patients (since people over 70 years of age have a higher risk of developing neutropenia and thrombocytopenia than younger ones).

There is no clinical experience with glioblastoma multiforme in children under 3 years of age and malignant melanoma in children and adolescents under 18 years of age. Clinical experience with glioma in children over 3 years of age is limited.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Temozolomide can cause drowsiness and fatigue and therefore negatively affect the ability to drive vehicles and manage complex mechanisms.

Form of production

Lyophilizate for preparation of solution for infusions.

Storage conditions

At a temperature of 2-30 °C

Shelf life

2 years

Active ingredient

Temozolomide

Conditions of release from pharmacies

By prescription

Dosage form

lyophilizate for solution preparation

Description

For adults as directed by your doctor

Indications

Cancer