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Temozolomide (Temodal) 💊
💊 Temozolomide (TMZ) is an oral alkylating agent indicated for newly diagnosed high-grade glioma (GBM) in adults (with radiotherapy) and as monotherapycheck the BNF link here.
⚙️ Mode of Action
- Prodrug → converts to MTIC (monomethyl triazeno imidazole carboxamide).
- Alkylates/methylates DNA → triggers apoptosis in rapidly dividing cells.
- Depletes MGMT (DNA repair enzyme); tumour MGMT methylation predicts better response.
- Easily crosses the blood–brain barrier.
💊 Indications & Dose
- Glioblastoma multiforme (GBM): Standard of care (Stupp regimen: RT + TMZ, then maintenance).
- Other CNS tumours: Astrocytoma (second-line).
- Metastatic melanoma.
- Aggressive pituitary tumours: Prolactinomas, pituitary carcinoma (esp. MEN1).
- Typical dose: 150–200 mg/m² orally once daily for 5 days, repeated every 28 days.
🔗 Interactions
- May be used in combination with Carmustine (BCNU) implants after surgical resection of GBM.
⚠️ Cautions
- Risk of severe myelosuppression → monitor FBC regularly.
- Infection risk (esp. Pneumocystis jirovecii pneumonia during RT + TMZ → prophylaxis may be required).
- Monitor LFTs (hepatotoxicity possible).
🚫 Contraindications
- See BNF (e.g. severe myelosuppression, hypersensitivity).
❗ Side Effects
- Very common: Nausea, vomiting, fatigue.
- Haematological: Myelosuppression (neutropenia, thrombocytopenia), risk of infection.
- Hepatic: Abnormal LFTs, rarely severe liver injury.
- Other: Headache, constipation, rash, alopecia.
📚 References
- BNF – Temozolomide
- Stupp R et al. "Radiotherapy plus concomitant and adjuvant temozolomide for glioblastoma." NEJM, 2005.
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