About
Temozolomide is an oral alkylating chemotherapeutic agent primarily indicated for the treatment of specific brain cancers, including newly diagnosed glioblastoma multiforme and refractory anaplastic astrocytoma. As a prodrug, it undergoes non-enzymatic hydrolysis to its active metabolite, MTIC (5-(3-methyl-1-triazen-1-yl)imidazole-4-carboxamide), which then exerts its cytotoxic effects by methylating DNA. This methylation primarily occurs at the O6 position of guanine, leading to DNA repair pathway activation, subsequent DNA strand breaks, and ultimately programmed cell death (apoptosis) in tumor cells.
Its lipophilic nature allows it to readily cross the blood-brain barrier, making it a valuable therapeutic option for central nervous system malignancies where many other chemotherapeutic agents are ineffective. Temozolomide is often integrated into treatment protocols for glioblastoma, typically administered concurrently with radiation therapy followed by adjuvant cycles. Regular monitoring of complete blood counts is crucial throughout the treatment period due to the risk of myelosuppression.
Uses
- Treatment of newly diagnosed glioblastoma multiforme in adults.
- Treatment of refractory anaplastic astrocytoma in adults.
- Adjuvant therapy for glioblastoma after concurrent chemoradiation.
- Management of other high-grade gliomas that have progressed.
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 against aggressive brain tumors.
- Penetrates the blood-brain barrier efficiently.
- Convenient oral administration.
- Enhances the effect of radiation therapy in glioblastoma.
- Contributes to improved survival outcomes in glioblastoma patients.
- Targets DNA in cancer cells, leading to cell death.
Side Effects
- Nausea
- Vomiting
- Fatigue
- Headache
- Constipation
- Anorexia
- Hair loss (alopecia)
- Myelosuppression (low blood counts)
- Rash
- Dizziness
- Risk of opportunistic infections (e.g., PJP)
- Elevated liver enzymes
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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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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