About
Temozolomide is an oral alkylating agent used in the treatment of certain brain tumors, including newly diagnosed glioblastoma multiforme and refractory anaplastic astrocytoma. It is a prodrug that undergoes rapid chemical conversion at physiological pH to its active metabolite, MTIC (5-(3-methyl-1-triazen-1-yl)imidazole-4-carboxamide). MTIC then methylates DNA at various sites, primarily at the O6 and N7 positions of guanine.
This DNA methylation leads to DNA damage and subsequent cell cycle arrest and apoptosis, particularly in rapidly dividing cancer cells. Its ability to cross the blood-brain barrier makes it an effective agent for central nervous system malignancies. Temozolomide is often used in combination with radiation therapy for newly diagnosed glioblastoma. Close monitoring of hematological parameters is essential due to its myelosuppressive effects.
Uses
- Newly diagnosed glioblastoma multiforme concurrently with radiotherapy and as adjuvant therapy.
- Refractory anaplastic astrocytoma.
- Other malignant gliomas that are recurrent or progressive.
- Off-label use in certain neuroendocrine tumors.
Directions For Use
Take orally on an empty stomach, at least one hour before food, usually once daily for a specified number of days per cycle, as directed by your oncologist.
Benefits
- Effective in treating aggressive brain tumors.
- Can cross the blood-brain barrier.
- Available in oral form, offering convenience.
- Often used in combination with radiation therapy for enhanced efficacy.
- Improves progression-free and overall survival in glioblastoma.
- Provides a targeted approach to DNA damage in cancer cells.
Side Effects
- Nausea
- Vomiting
- Fatigue
- Headache
- Constipation
- Anorexia
- Alopecia
- Myelosuppression (neutropenia, thrombocytopenia)
- Rash
- Dizziness
- Pneumocystis jirovecii pneumonia (PJP) risk
- Liver enzyme elevation
Safety Measures
- Alcohol - Avoid or limit alcohol consumption as it may exacerbate gastrointestinal side effects like nausea and vomiting.
- Pregnancy - Temozolomide can cause fetal harm. It is contraindicated in pregnancy, and effective contraception must be used by both male and female patients.
- Breastfeeding - It is unknown if temozolomide is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is contraindicated.
- Liver - Use with caution in patients with severe hepatic impairment. Liver function tests should be monitored, and dose adjustments may be necessary.
- Kidney - Use with caution in patients with severe renal impairment. No specific dose recommendations exist, but close monitoring is advised.
- Lung - Rare but serious pulmonary adverse events, including interstitial pneumonitis, have been reported. Monitor for new or worsening respiratory symptoms.
Disclaimer
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