Temozolomide

Indications
 Oral
Glioblastoma multiforme
Adult: 75 mg/m2 once daily for 42 days with focal radiotherapy (concomitant phase). Do not reduce dose during concomitant phrase but interrupt or discontinue therapy depending on toxicity. Continue if absolute neutrophil count (ANC)≥ 1.5x109/L, thrombocyte count ≥100x109/L and Common Toxicity Criteria (CTC) non-haematological toxicity ≤ Grade 1 (except for alopecia, nausea and vomiting). Initiate monotherapy 4 wk after completing concomitant phase: 150 mg/m2 once daily for 5 days followed by a 23 day break (1 cycle). In cycle 2, increase dose to 200 mg/m2 once daily for 5 days, if ANC ≥1.5x109/L, thrombocyte count ≥100x109/L and CTC non-haematological toxicity for cycle 1 is ≤ Grade 2 (except for alopecia, nausea and vomiting). If dose cannot be increased in cycle 2, do not increase dose in subsequent cycles. Dose used in cycle 2 is given for the rest of the cycles, toxicity allowing, up to 6 cycles.
Oral
Recurrent or progressive malignant gliomas
Adult: Previously untreated with chemotherapy: 200 mg/m2 once daily for 5 days, followed by a 23 day break (1 cycle). Previously treated with chemotherapy: 150 mg/m2 daily for 5 days followed by 23 day break (1 cycle) increased to 200 mg/m2 daily for the 2nd cycle if there is no haematological toxicity.
Child: >3 yr: Previously untreated with chemotherapy: 200 mg/m2 once daily for 5 days, followed by a 23 day break (1 cycle). Previously treated with chemotherapy: 150 mg/m2 daily for 5 days followed by 23 day break (1 cycle) increased to 200 mg/m2 for the 2nd cycle if there is no haematological toxicity.
Oral
Metastatic melanoma
Adult: 200 mg/m2 daily for 5 days every 28 days.
Contraindications
 Hypersensitivity to dacarbazine. Severe myelosupression. Pregnancy.
Warnings / Precautions
 Severe hepatic and renal impairment. Elderly >70 yr, children. Women of child bearing potential should avoid becoming pregnant during therapy. Males should be advised not to father a child up to 6 mth after treatment and to consider cryoconservation of sperms due to possibility of irreversible infertility. Unknown if distributed into breastmilk, discontinue nursing due to potential risk. May impair ability to drive or operate machinery. Swallow capsules whole with a full glass of water on an empty stomach or at bedtime. Do not take a 2nd dose if capsules are vomited. Monitor CBC wkly during concomitant therapy and on day 22 of each 28 day treatment cycle, followed by wkly blood count until recovery. Hepatitis screening and prophylactic therapy with antiviral agents as clinically indicated to be considered. Prophylaxis for Pneumocystis jiroveci (or Pneumocystis carinii) pneumonia (PCP) needed for all patients receiving concomitant temozolomide and radiation therapy for the 42-day regimen; if patients experience lymphocytopenia during the concomitant phase of therapy, PCP prophylaxis should be continued until recovery from lymphocytopenia. Monitor closely for PCP development in all patients. Anti-emetic prophylaxis recommended.
Adverse Reactions
 Nausea, vomiting, taste perversion, constipation, diarrhoea, abdominal pain, stomatitis, anorexia, headache, fatigue, convulsions, dizziness, memory impairment, impaired concentration, tremors, blurred vision, hearing impairment, speech disorder, rash, infection, oral candidiasis, dyspnoea, coughing, neutropenia, thrombocytopenia, leucopenia, anaemia, hyperglycemia, decreased wt, insomnia, anxiety, alopecia, muscle weakness, urinary incontinence, increased alanine aminotransferase. Rarely, myelodysplastic syndrome and secondary malignancies.
Drug Interactions
 Reduced effectiveness of vaccines and generalised infection may occur in patients immunised with live vaccines. Decreased temozolomide clearance with valproic acid.
Potentially Fatal: Increased risk of myelosupression with other myelosuppressive agents. Increased risk of myelosuppression with colony stimulating factors (e.g. filgrastim, molgramostim and lenograstim) if given at the same time, colony stimulating factors to be used 24 hr before or until 24 hr after chemotherapy.
See Below for More temozolomide Drug Interactions
Mechanism of Actions
 Temozolomide, a triazene, is an inactive prodrug. It is chemically hydrolysed to 3-methyl-(triazen-1-yl) imidazole-4-carboxamide (MTIC), the active metabolite of dacarbazine. The cytotoxicity of MTIC is believed to be due alkylation of DNA, mainly at the O6 and N7 positions of guanine.
Absorption: Rapidly and completely absorbed from GI tract. Peak plasma concentration: 0.5-1.5 hr. Rate and extent of absorption decreased by food.
Distribution: Protein binding: 15%. Cross blood-brain barrier.
Metabolism: Undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound MTIC and to temozolomide acid metabolite. MTIC is further hydrolysed to 5-amino-imidazole-4-carboxamide (AIC) and methylhydrazine.
Excretion: Excreted mainly in urine as unchanged drug, AIC, temozolomide acid metabolite and unidentified polar metabolites. Plasma half life: 1.8 hr.
Administration
 Should be taken on an empty stomach. (Take on an empty stomach at least 1 hr before meals.)
Storage Conditions
 Oral: Store at 15-30°C.
ATC Classification
 L01AX03 - temozolomide ; Belongs to the class of other alkylating agents. Used in the treatment of cancer.
Storage
 Oral: Store at 15-30°C.
Available As
  • Temozolomide 100 mg
  • Temozolomide 20 mg
  • Temozolomide 250 mg
  • Temozolomide 5 mg

    • Subscribe for latest updates

    Subscribe to our e-mail newsletter to receive updates.

    No comments yet.

    Post Review about Temozolomide


    Temozolomide Containing Brands

    We are Developing Our database, More results coming soon.

    Temozolomide is used in following diseases

    We are Developing Our database, More results coming soon.

    Drug - Drug Interactions of Temozolomide

    We are Developing Our database, More results coming soon.