About
Temozolomide is an oral alkylating agent specifically designed for the treatment of certain aggressive brain tumors, notably glioblastoma multiforme and anaplastic astrocytoma. It functions as a prodrug, meaning it is inactive until it undergoes spontaneous chemical conversion within the body to its active metabolite, 5-(3-methyl-1-triazen-1-yl)imidazole-4-carboxamide (MTIC). MTIC then exerts its therapeutic effect by methylating DNA at specific guanine residues. This methylation leads to DNA damage and mispairing during replication, triggering cell cycle arrest and ultimately inducing apoptosis in rapidly proliferating cancer cells. A key advantage of temozolomide is its lipophilic nature, which allows it to efficiently cross the blood-brain barrier, making it particularly effective against central nervous system malignancies where many other chemotherapeutic agents struggle to penetrate. It is often used in combination with radiation therapy to enhance its anti-tumor activity.
Uses
- Treatment of newly diagnosed glioblastoma multiforme.
- Management of refractory anaplastic astrocytoma.
- Therapy for other malignant gliomas.
- Used in combination with radiation therapy.
Directions For Use
Take orally on an empty stomach, preferably at bedtime, to minimize nausea and vomiting. Swallow capsules whole with a glass of water.
Benefits
- Effective against specific brain tumors.
- Crosses the blood-brain barrier efficiently.
- Available in oral formulation, improving convenience.
- Can be used concurrently with radiation therapy.
- Improves progression-free and overall survival in glioblastoma.
- Well-established treatment for certain CNS malignancies.
Side Effects
- Nausea
- Vomiting
- Fatigue
- Headache
- Constipation
- Hair loss (alopecia)
- Myelosuppression (low blood counts)
- Anorexia
- Rash
- Dizziness
- Opportunistic infections (e.g., PCP)
- Liver enzyme elevation
Safety Measures
- Alcohol - Avoid or limit alcohol consumption as it may exacerbate gastrointestinal side effects and potentially increase liver strain.
- Pregnancy - Contraindicated due to potential for severe fetal harm. Effective contraception is mandatory for both male and female patients.
- Breastfeeding - Contraindicated. Temozolomide is likely excreted in breast milk and can cause serious adverse effects in the infant.
- Liver - Use with caution in patients with severe liver impairment; monitor liver function tests closely.
- Kidney - Use with caution in patients with severe kidney impairment; monitor renal function.
- Lung - Monitor for pulmonary toxicity, though rare, and for increased susceptibility to lung infections, especially Pneumocystis pneumonia (PCP).
Disclaimer
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Always consult your doctor for any medical concerns, and discuss your questions about health conditions or medications with a qualified healthcare professional. Do not ignore or delay seeking professional medical advice based on information found on Med E Hub.
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