Temozolomide
Cytostatic · Alkylating agent
Indications
Treatment of adult patients with refractory (first relapse) anaplastic astrocytoma who have experienced disease progression on nitrosourea and procarbazine. Treatment of newly-diagnosed glioblastoma multiforme (initially in combination with radiotherapy, then as maintenance treatment).
Dosage
Adults: Anaplastic astrocytoma: 150-200 mg/m²/day for 5 days, repeat every 28 days. Glioblastoma multiforme (newly diagnosed, high-grade glioma): Oral/IV: Concomitant phase: 75 mg/m² once daily for 42 days with focal radiotherapy (60 Gy administered in 30 fractions). Children: Not recommended.
Adverse Effects
Peripheral oedema, headache, convulsions, dizziness, GI upsets, neutropenia, thrombocytopenia, anaemia, paresthesia, infection, blood dyscrasias, anorexia, wt loss, hyperglycaemia, anxiety, emotional lability, insomnia, depression, CNS effects, tremor, visual disturbances, impaired hearing, tinnitus, haemorrhage, oedema, thrombosis, dyspnoea, cough, stomatitis, dysphagia, dry mouth, rash, alopecia, skin changes, pruritus, arthralgia, myalgia, muscle weakness and pain, urinary frequency and incontinence, fatigue, raised liver enzymes, fever, taste perversion. Second leukaemia, Stevens-Johnson syndrome, respiratory failure, hepatic injury and herpetic meningoencephalitis.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Positive evidence of risk: Use only when no safer alternative exists for a serious problem. Lactation: Contraindicated or not recommended. Precautions: Hepatic & renal impairment, elderly. Anti-emetic prophylaxis is recommended after the first dose of concomitant phase and during monotherapy phase. Risk of opportunistic infection. Co-infection with HBV. Risk of Pneumocystis jirovecii pneumonia; prophylaxis required in patients receiving concomitant radiotherapy. Risk of myelosuppression (sometimes fatal); monitor blood counts before and during treatment.
Interactions
Valproic acid, other myelosuppressive agents.
Advice to Patient
Take atleast 1 hour before meals or 2 hours after meals or at bedtime. Take each dose at the same time each day. Do not chew or crush or open capsules. Swallow whole with a full glass of water. Contact prescriber if there is acute headache, change in vision, unrelieved GI upset, chest pain, palpitations, acute joint, back pain, bone pain or muscle pain, vaginal discharge, itching or burning on urination, unusual cough, difficulty in breathing. Stay in cool dark room or apply cool compresses to reduce hot flushes.
Pharmacokinetics
Absorption: Oral: Rapid and complete. Metabolism: Prodrug, hydrolyzed to the active form, MTIC. Bioavailability: Oral: 100% ( on mg/mg basis, IV temozolomide, infused over 90 minutes, is bioequivalent to an oral dose). Half-life elimination: Mean: Parent drug: Children: 1.7 hours; Adults: 1.6-1.8 hours. Time to peak: Oral: Empty stomach: 1 hour, with food (high-fat meal): 2.25 hours. Excretion: Urine (approx. 38%; parent drug 6%); feces<1%.
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
Always consult a pharmacist or doctor.