Comparative Pharmacology
Head-to-head clinical analysis: DACARBAZINE versus GLEOSTINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DACARBAZINE versus GLEOSTINE.
DACARBAZINE vs GLEOSTINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Alkylating agent; inhibits DNA and RNA synthesis by forming covalent bonds with DNA, leading to cross-linking and strand breaks. Also inhibits purine synthesis and has some activity as a methylating agent.
GLEOSTINE (lomustine) is a nitrosourea alkylating agent that crosslinks DNA and RNA, inhibiting DNA synthesis and repair. It is cell cycle phase-nonspecific.
2.4-4.5 mg/kg IV daily for 10 days every 28 days; or 250 mg/m2 IV daily for 5 days every 21 days; or 375-450 mg/m2 IV single dose every 21-28 days.
130 mg/m2 orally every 6 weeks as a single dose; alternatively, 75 mg/m2 orally every 3 weeks.
None Documented
None Documented
Terminal half-life: 5 hours (range 3-8 h) after IV administration; biphasic decay with initial half-life ~19 min.
Clinical Note
moderateDacarbazine + Digoxin
"Dacarbazine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateDacarbazine + Digitoxin
"Dacarbazine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateDacarbazine + Deslanoside
"Dacarbazine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateDacarbazine + Acetyldigitoxin
"Dacarbazine may decrease the cardiotoxic activities of Acetyldigitoxin."
16-48 hours (terminal), with an active metabolite half-life of up to 5 days, requiring dose adjustment for renal impairment
Renal: 40-50% unchanged; hepatic: 30-50% as metabolites (primarily 5-aminoimidazole-4-carboxamide); <10% fecal.
Renal: 60% (as metabolites), Fecal: <5% (unchanged and metabolites), Biliary: minimal
Category D/X
Category C
Alkylating Agent
Alkylating Agent