Temodal® [Temozolomide]
Schering-Plough
525 Items
2019-09-19
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Clinical Pharmacology
The antitumor agent of the alkylating action has an imidazotetrazinovuyu structure.
In the systemic circulation, under physiological pH, it undergoes a rapid chemical transformation with the formation of the active compound, monomethyltriazenoimidazolecarboxamide (MTIC). It is believed that the cytotoxicity of MTIK is due primarily to the alkylation of guanine at the O6 position and the additional alkylation at the N7 position. Apparently, the cytotoxic damage resulting from this triggers the mechanism of aberrant reduction of the methyl residue.
Pharmacokinetics
After ingestion is rapidly absorbed from the gastrointestinal tract.
Cmax plasma temozolomide is achieved on average in 0.5-1.5 hours (minimum - in 20 minutes) after taking a single dose. When taken with food, a decrease in C was observed.max by 33% and a decrease in AUC by 9%.
Temozolomid quickly penetrates the BBB and enters the cerebrospinal fluid.
Plasma protein binding is 10-20%.
T1/2 from plasma is approximately 1.8 hours. Quickly excreted mainly by the kidneys.
24 hours after ingestion, about 5-10% of the dose is determined unchanged in the urine; the remainder is displayed as 4-amino-5-imidazole-carboxamide hydrochloride or unidentified polar metabolites.
Indications
- Malignant gliomas (including glioblastoma multiforme, anaplastic astrocytoma) in the presence of recurrence or progression of the disease after standard therapy;
- common metastatic malignant melanoma (as a first-line therapeutic agent).
Composition
1 capsule contains:
Active substances: Temozolomide 100 mg.
Excipients: anhydrous lactose, colloidal silicon dioxide, sodium carboxymethyl starch, tartaric acid, stearic acid.
The composition of the capsule shell: titanium dioxide, sodium lauryl sulfate, gelatin.
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Dosage and Administration
Individual, depending on age and previous chemotherapy.
Adverse reactions
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, paresthesias.
Dermatological reactions: skin rashes, alopecia, pruritus.
On the part of the respiratory system: dyspnea.
From the hemopoietic system: thrombocytopenia and grade 3 or 4 neutropenia, pancytopenia, leukopenia and anemia.
Other: fever, asthenia, weight loss, malaise, chills.
Contraindications
- Severe myelopepression;
- pregnancy;
- lactation (breastfeeding);
- hypersensitivity to temozolomide or dacarbazine.
Drug interactions
With simultaneous use of temozolomide with valproic acid, a mild, but statistically significant decrease in temozolomide clearance is observed.
About the simultaneous use of temozolomide with other drugs that have a depressant effect on the bone marrow, you may increase the risk of developing myelosuppression.
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 the end of treatment.
Special instructions
Use with caution in patients with severely impaired liver or kidney function in elderly patients (as in those older than 70, the risk of developing neutropenia and thrombocytopenia is higher than in younger patients).
Clinical experience with glioblastoma multiforme in children under 3 years of age and with malignant melanoma in children and adolescents under 18 is absent. Clinical experience with glioma in children older than 3 years is limited.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
Temozolomid can cause drowsiness and fatigue and therefore adversely affect the ability to drive vehicles and manage complex mechanisms.
Overdosage
When using the drug in doses of 500, 750, 1000 and 1250 mg / m2 (the total dose received for the 5-day cycle of treatment) was hematologic dose-limiting toxicity, which was observed when taking any dose, but more pronounced with higher doses. A case of overdose has been described (a dose of 2000 mg per day for 5 days), which resulted in pancytopenia, pyrexia, multiple organ dysfunction and death. When taking the drug for more than 5 days (up to 64 days), among other side effects, blood formation was inhibited, complicated or not complicated by infection, in some cases - prolonged and severe, with a fatal outcome.
Treatment: antidote to Temodal unknown. Hematological control and, if necessary, symptomatic therapy are recommended.
- Brand name: Temodal
- Active ingredient: Temozolomide
- Dosage form: Capsules
- Manufacturer: Schering-Plough
- Country of Origin: USA
Studies and clinical trials of Temozolomide (Click to expand)
- Tailored temozolomide therapy according to MGMT methylation status for elderly patients with acute myeloid leukemia
- Dynamic history of low-grade gliomas before and after temozolomide treatment
- ChemInform Abstract: A New Route to the Antitumor Drug Temozolomide, But Not Thiotemozolomide.
- ChemInform Abstract: Antitumor Imidazotetrazines. Part 35. New Synthetic Routes to the Antitumor Drug Temozolomide.
- ChemInform Abstract: Antitumor Imidazotetrazines. Part 36. Conversion of 5-Aminoimidazole-4-carboxamide to Imidazo[5,1-d][1,2,3,5]tetrazin-4(3H)-ones and Imidazo[1,5-a][1,3,5]triazin-4(3H)-ones Related in Structure to the Antitumor Agents Temozolomide and Mitozolomide.
- ChemInform Abstract: Pyrrolo[2,1-d][1,2,3,5]tetrazines, a New Class of Azolotetrazines Related to the Antitumor Drug Temozolomide.
- ChemInform Abstract: Synthesis and Antibacterial Activity of Dual-Action Agents of a β-Lactam Antibiotic with Cytotoxic Agent Mitozolomide or Temozolomide.
- A New Synthesis of Temozolomide.
- Temozolomide in combination with interferon α-2b in patients with metastatic melanoma : A Phase I dose-escalation study
- Phase I study of temozolomide and escalating doses of oral etoposide for adults with recurrent malignant glioma
- Temozolomide as an alternative to irradiation for elderly patients with newly diagnosed malignant gliomas
- A phase II trial of temozolomide in patients with unresectable or metastatic soft tissue sarcoma
- A two-arm phase II study of temozolomide in patients with advanced gastrointestinal stromal tumors and other soft tissue sarcomas
- Temozolomide in the treatment of recurrent malignant glioma
- Salvage chemotherapy with cyclophosphamide for recurrent, temozolomide-refractory glioblastoma multiforme
- Phase II study of neoadjuvant 1, 3-bis (2-chloroethyl)-1-nitrosourea and temozolomide for newly diagnosed anaplastic glioma : A North American Brain Tumor Consortium trial
- Phase II study of temozolomide without radiotherapy in newly diagnosed glioblastoma multiforme in an elderly populations
- Immunochemotherapy with rituximab and temozolomide for central nervous system lymphomas
- Can we afford to add chemotherapy to radiotherapy for glioblastoma multiforme? Cost-identification analysis of concomitant and adjuvant treatment with temozolomide until patient death
- Immunochemotherapy with rituximab and temozolomide for central nervous system lymphomas
- Phase II study of temozolomide without radiotherapy in newly diagnosed glioblastoma multiforme in an elderly population
- Role of temozolomide after radiotherapy for newly diagnosed diffuse brainstem glioma in children : Results of a multiinstitutional study (SJHG-98)
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