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Pharmacology Chemotherapy 8c40eda4

Which group of anticancer drugs temozolomide belong to:

A
Oral alkylating agent
B
Antitumor Antibiotic
C
Antimetabolite
D
Mitotic Spindle Inhibitor
High-Yield Explanation
Temozolomide is used to treat specific types of brain cancer (eg, glioblastoma multiforme, anaplastic astrocytoma) in patients whose tumors have returned or whose tumors have just been diagnosed. It belongs to the group of medicines known as antineoplastics (cancer medicines). Mechanism of Action Imidazotetrazine derivative prodrug; active metabolite MTIC methylates guanine-rich areas of DNA that initiate transcription, which lead to DNA double strand breaks and apoptosis Absorption Rapidly and completely absorbed after oral administration Peak Plasma Time: 1 hr (empty stomach); 2.25 hr (high-fat meal) Bioequivalence: 100%; IV infusion (when administered over 90 min) is bioequivalent to same dose of oral capsule Mean peak plasma concentration and AUC decreased by 32% and 9%, respectively when administered after a high-fat breakfast Distribution Protein Bound: 15% Vd: 0.4 L/kg Metabolism Metabolite: Hydrolyzed at physiologic pH to 3-methyl-(triazen-1-yl) imidazole-4-carboxamide (MTIC); MTIC fuher hydrolyzed to to 5-amino-imidazole-4-carboxamide (AIC), which is known to be an intermediate in purine and nucleic acid biosynthesis, and to methylhydrazine, which is believed to be the active alkylating species Elimination Half-life: 1.8 hr Clearance: 5.5 L/hr/m2 Excretion: primarily urine (~38%) REFERENCE: www.medscape.com, www.mayoclinic.org

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