Temozolomide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Temodal; Belgium: Temodal; Bulgaria: Temodal; Cyprus: Temodal; Czech Republic: Temodal; Denmark: Temodal; Estonia: Temodal; Finland: Temodal; France: Temodal; Germany: Temodal; Greece: Temodal; Hungary: Temodal; Ireland: Temodal; Italy: Temodal; Latvia: Temodal; Lithuania: Temodal; Luxembourg: Temodal; Malta: Temodal; Netherlands: Temodal; Poland: Temodal; Portugal: Temodal; Romania: Temodal; Slovakia: Temodal; Slovenia: Temodal; Spain: Temodal; Sweden: Temodal; UK: Temodal.

North America

Canada: Temodal; USA: Temodar.

Latin America

Argentina: Dralitem, Temodal, Tocitrap, Zolom; Brazil: Temodal; Mexico: Temodal.

Asia

Japan: Temodal.

Drug combinations

Chemistry

Temozolomide: C~6~H~6~N~6~O~2~. Mw: 194.15. (1) Imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide, 3,4-dihydro-3-methyl-4-oxo-; (2) 3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide. CAS-85622-93-1 (1999).

Pharmacologic Category

Antineoplastic Agents; Alkylating Agents. Triazene. (ATC-Code: L01AX03).

Mechanism of action

Converted to active alkylating metabolite MTIC ((methyl-triazene-1-yl)-imidazole-4-carboxamide)(like dacarbazine). Unlike dacarbazine, however, this conversion is spontaneous, nonenzymatic, and occurs under physiologic conditions in all tissues to which the drug distributes.

Therapeutic use

Treatment of adult patients with refractory anaplastic astrocytoma. Newly-diagnosed glioblastoma multiforme.

Pregnancy and lactiation implications

May cause fetal harm when administered to pregnant women. Pregnancy should be avoided while receiving drug. Not recommended in nursing women.

Unlabeled use

Metastatic melanoma.

Contraindications

Hypersensitivity to temozolomide or any component of the formulation. Hypersensitivity to dacarbazine (both drugs are metabolized to MTIC). Pregnancy.

Warnings and precautions

Myelosuppression may occur with use (increased incidence reported in geriatric and female patients). Pneumocystis jiroveci pneumonia may occur (increased risk in patients receiving steroids or longer dosing regimens). Rare cases of myelodysplastic syndrome and secondary malignancies, including acute myeloid leukemia reported. Use with caution in severe hepatic and renal impairment.

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