Adult: In newly diagnosed patients: Concomitant phase: 75 mg/m2 via infusion over 90 minutes once daily for 42 days, with focal radiotherapy. Dosing interruption or discontinuation may be required during the concomitant phase based on toxicity (refer to product guideline). Maintenance phase (starting 4 weeks after completion of concomitant phase): Cycle 1: 150 mg/m2 once daily on Days 1-5 of a 28-day cycle. Cycles 2-6: May increase to 200 mg/m2 once daily on Days 1-5 of each 28-day cycle; if the dose was not escalated at the onset of Cycle 2, do not increase the dose in succeeding cycles. Dose reduction, interruption or discontinuation may be required during the maintenance phase according to individual safety or tolerability (refer to detailed product guideline).
Intravenous Refractory anaplastic astrocytoma
Adult: In patients who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine: 150 mg/m2 via infusion over 90 minutes once daily on Days 1-5 of a 28-day cycle; dose for succeeding cycles may be increased to 200 mg/m2 once daily on Days 1-5 of a 28-day cycle if there is no toxicity. Continue until disease progression or unacceptable toxicity. Dose modifications may be needed according to individual safety or tolerability (refer to detailed product guideline).
Adult: Patients who are not previously treated with chemotherapy: 200 mg/m2 once daily for Days 1-5 of a 28-day cycle. Patients previously treated with chemotherapy: 150 mg/m2 once daily on Days 1-5 of a 28-day cycle; dose for succeeding cycles may be increased to 200 mg/m2 daily on Days 1-5 of a 28-day cycle if there is no toxicity. Continue until disease progression or unacceptable toxicity. Dose modifications may be needed according to individual safety or tolerability (refer to detailed product guideline). Child: ≥3 years Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.
Oral Metastatic malignant melanoma
Adult: 200 mg/m2 once daily on Days 1-5 of a 28-day cycle.
Oral Glioblastoma multiforme
Adult: In newly diagnosed patients: Concomitant phase: 75 mg/m2 once daily for 42 days, with focal radiotherapy. Dosing interruption or discontinuation may be required during the concomitant phase based on toxicity. Maintenance phase (starting 4 weeks after completion of concomitant phase): Cycle 1: 150 mg/m2 once daily on Days 1-5 of a 28-day cycle. Cycles 2-6: May increase to 200 mg/m2 once daily on Days 1-5 of a 28-day cycle; if the dose was not escalated at the onset of Cycle 2, do not increase the dose in succeeding cycles. Dose reduction, interruption or discontinuation may be required during the maintenance phase according to individual safety or tolerability (refer to detailed product guideline).
What are the brands available for Temozolomide in Philippines?
Temozolomide May be taken with or without food. Take on empty stomach to reduce nausea & vomiting.
Reconstitution
IV: Bring the vial to room temperature prior to reconstitution. Add 41 mL of sterile water for inj to the vial labelled as containing 100 mg to a final concentration of 2.5 mg/mL. Swirl gently; do not shake. Transfer reconstituted solution from each vial into an empty 250 mL infusion bag.
Contraindications
Hypersensitivity to temozolomide or dacarbazine. Severe myelosuppression. Pregnancy and lactation.
Special Precautions
Patient with Pneumocystis jirovecii pneumonia. Severe hepatic and renal impairment. Children.
Adverse Reactions
Significant: Hypersensitivity (e.g. anaphylaxis), Pneumocystis jirovecii pneumonia, nausea, vomiting. Rarely, myelodysplastic syndrome and secondary malignancies (e.g. myeloid leukaemia). Ear and labyrinth disorders: Deafness, earache, tinnitus, vertigo. Endocrine disorders: Cushingoid. Eye disorders: Blurred vision, diplopia, eye pain, hemianopia, vision disorder, visual field defect. Gastrointestinal disorders: Constipation, diarrhoea, dyspepsia, dysphagia, abdominal pain, stomatitis, taste perversion, oral candidiasis. General disorders and administration site conditions: Fatigue, asthenia, fever, influenza-like symptoms, malaise, pain, oedema; petechiae, haematoma, pain, irritation, pruritus, warmth, swelling, erythema at the inj site (IV). Infections and infestations: Herpes zoster. Investigations: Increased liver enzymes, increased or decreased weight. Metabolism and nutrition disorders: Anorexia, hyperglycaemia. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, back pain, myopathy, musculoskeletal pain. Nervous system disorders: Headache, convulsion, tremors, dizziness, hemiparesis, hypoaesthesia, aphasia or dysphasia, ataxia, neuropathy, paraesthesia, reduced consciousness, speech disorder; impaired balance, cognition, concentration or memory. Psychiatric disorders: Agitation, amnesia, anxiety, confusion, depression, insomnia, somnolence. Renal and urinary disorders: Urinary incontinence, micturition frequency. Respiratory, thoracic and mediastinal disorders: Dyspnoea, sinusitis, bronchitis, pharyngitis, cough, upper respiratory infection. Skin and subcutaneous tissue disorders: Alopecia, dry skin, erythema, rash, pruritus. Vascular disorders: Haemorrhage, DVT, embolism, hypertension. Potentially Fatal: Myelosuppression (e.g. anaemia, leucopenia, pancytopenia), hepatotoxicity (e.g. hepatic failure). Rarely, reactivation of infections (e.g. hepatitis B virus), herpes simplex encephalitis.
IV/PO: Z (Spontaneous abortions and congenital malformations have been described in postmarketing reports. Temozolomide use during pregnancy is generally not recommended.)
Patient Counseling Information
This drug may cause fatigue and somnolence; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor CBC with differential and platelets (prior to treatment initiation, weekly during the concomitant phase with radiation therapy, and on days 1 and 22 of each 28-day cycle; may require more frequent monitoring if myelosuppression occur); LFT (at baseline, halfway through the 1st cycle, before each subsequent cycle, and at approx 2-4 weeks after the last dose). Evaluate pregnancy status prior to use in females of reproductive potential. Monitor for lymphopenia and for signs/symptoms of Pneumocystis jirovecii pneumonia, hypersensitivity, and secondary malignancies.
Decreased clearance with valproic acid. Increased risk of myelosuppression with other myelosuppressive agents.
Food Interaction
Food reduces the rate and extent of absorption of temozolomide.
Action
Description: Mechanism of Action: Temozolomide, a triazene, is a prodrug which is rapidly hydrolysed to 5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is believed to be due to alkylation of DNA, mainly at the O6 and N7 positions of guanine, leading to DNA double strand breaks and apoptosis. Pharmacokinetics: Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 100%. Reduced rate and extent of absorption with food. Time to peak plasma concentration: 0.5-1.5 hours. Distribution: Crosses the blood-brain barrier and detected in the CSF. Volume of distribution: 0.4 L/kg. Plasma protein binding: Approx 10-20%. Metabolism: Undergoes spontaneous hydrolysis to its active metabolite 5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide (MTIC), which is further hydrolysed to 5-amino-imidazole-4-carboxamide (AIC) and methylhydrazine. Excretion: Mainly via urine (approx 38%; 5-10% as unchanged drug and 12% as AIC); faeces (<1%). Elimination half-life: Approx 1.8 hours.
Chemical Structure
Temozolomide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5394, Temozolomide. https://pubchem.ncbi.nlm.nih.gov/compound/Temozolomide. Accessed Sept. 27, 2021.
Storage
Cap: Store at or below 25°C. Protect from light and moisture. Powder for inj: Store between 2-8°C.
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