Temozolomyd | Temodal capsules 140 mg, 5 pcs.
Special Price
$260.93
Regular Price
$277.00
In stock
SKU
BID608906
Release form
Capsules.
Packaging
In a dark glass bottle 5 capsules. In a cardboard box 1 bottle.
Pharmacological action
Pharmacodynamics
Antitumor agent with an alkylating effect, has an imidazotetrazine structure.
In the systemic circulation, at physiological pH values, it undergoes a rapid chemical transformation to form the active compound, monomethyltriazenoimidazolecarboxamide (MTIC). It is believed that the cytotoxicity of MTIC is primarily due to the alkylation of guanine at position O6 and additional alkylation at position N7. Apparently, the cytotoxic damage resulting from this triggers the mechanism of aberrant recovery of the methyl residue.
Pharmacokinetics
After oral administration, it is rapidly absorbed from the digestive tract.
Cmax of temozolomide in plasma is achieved on average after 0.5-1.5 hours (at least 20 minutes) after taking a single dose. When taken with food, there was a decrease in Cmax by 33% and a decrease in AUC by 9%.
Temozolomide quickly penetrates the BBB and enters the cerebrospinal fluid.
Plasma protein binding is 10-20%.
T1 / 2 from plasma is approximately 1.8 hours. It is rapidly excreted mainly by the kidneys.
24 hours after ingestion, about 5-10% of the dose is determined unchanged in the urine, the rest 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 is common metastatic malignant melanoma (as a first-line therapeutic agent).
Contraindications
Severe myeloid depression
pregnancy
lactation (breastfeeding)
hypersensitivity to temozolomide or dacarbazine.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation (breastfeeding).
Men and women of childbearing age should use effective contraceptives during treatment and for at least 6 months after treatment ends.
Composition
1 capsule contains:
Active substances: temozolomide 140 mg.
Excipients: lactose, sodium carboxymethyl starch, colloidal silicon dioxide, tartaric acid, stearic acid.
Capsule shell composition: titanium dioxide, indigo carmine, sodium lauryl sulfate, gelatin.
Ink composition for inscription on the capsule shell: black dye (shellac, ethanol, isopropanol, butanol, propylene glycol, purified water, aqueous ammonia, potassium hydroxide, black iron dye).
Dosage and administration
Individual, depending on age and previous chemotherapy.
Side effects of the
From the digestive system: nausea, vomiting, constipation, anorexia, diarrhea, abdominal pain, dyspepsia, taste disturbance.
From the side of the central nervous system: fatigue, headache, drowsiness, dizziness, paresthesia.
Dermatological reactions: skin rashes, alopecia, skin itching.
From the respiratory system: shortness of breath.
From the hemopoietic system: thrombocytopenia and neutropenia of 3 or 4 degrees, pancytopenia, leukopenia and anemia.
Other: fever, asthenia, weight loss, malaise, chills.
Drug Interaction
When concomitantly administered temozolomide with valproic acid, a slight but statistically significant decrease in the clearance of temozolomide is observed.
About the simultaneous use of temozolomide with other drugs that have a depressing effect on the bone marrow may increase the risk of myelosuppression.
Overdose
When using the drug at doses of 500, 750, 1000, and 1250 mg / m2 (total dose received over a 5-day treatment cycle), the dose-limiting toxicity was hematologic, which was observed at any dose, but more pronounced - at higher doses. A case of overdose (taking a dose of 2000 mg per day for 5 days) has been described, resulting 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, there was a depression of hematopoiesis, complicated or not complicated by infection, in some cases - prolonged and pronounced, with a fatal outcome.
Treatment: Antidote to Temodal is unknown. Hematologic control and symptomatic therapy are recommended.
Storage conditions
Store at 2–30 РC.
Expiration
2 years.
Deystvuyuschee substances
Temozolomyd
pharmacy terms for prescription
Dosage Form Drug
form
capsules
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