L01AX03 - Temozolomide |
Not porphyrinogenic |
NP |
Rationale
Non-hepatic metabolism. Temozolomide lacks CYP-affinity. Side effects as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Triazene derivative.
Therapeutic characteristics
Temozolomide is an alkylating antineoplastic agent used to treat newly diagnosed glioblastoma multiforme, recidivating or therapy resistent malignant glioma and refractory anaplastic astrocytoma. Given orally in combination with radiation therapy.
Common adverse reactions of temozolomide that can be confused with an acute porphyric attack are nausea, vomiting, obstipation, myopathy, paraesthesia.
Hepatic exposure
Not significant
Metabolism and pharmacokinetics
Rapid nonenzymatic hydrolysis hydrolysis at physiological pH to metabolites that undergo renal excretion. Distributed to brain giving rise to cytotoxic metabolites via spontaneous hydrolysis, where metabolites undergo renal clearence.
IPNet drug reports
No.
References
- Scientific articles
- Rendic, S. Summary of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448. PMID 11996015. #4559
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Busulfan. Pharmaceutical Press 2009. #3315
- Other sources
- Swedish National Formulary. FASS. Temodal. www.fass.se (product leaflet). #3316
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