OncoPharm

Gemcitabine

23 snips
Jul 30, 2020
Dive into the world of gemcitabine, a pivotal chemotherapy drug effectively targeting solid tumors such as pancreatic and breast cancer. Explore its intricate pharmacology and recommended dosing, alongside vital safety considerations for patients with liver issues. The conversation also delves into comparisons with cytarabine, highlighting gemcitabine's unique role in oncology. Tune in for a comprehensive look at this essential treatment in cancer care.
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INSIGHT

Gemcitabine Activation Mechanism

  • Gemcitabine requires phosphorylation mostly by deoxycytidine kinase to an active triphosphate metabolite that inhibits DNA polymerization.
  • It acts as a false base pair in DNA, primarily targeting S-phase cells and possibly inhibiting topoisomerase 1 and ribonucleotide reductase.
INSIGHT

Key Differences from Cytarabine

  • Gemcitabine has faster intracellular uptake and phosphorylation to its active form than cytarabine, allowing shorter infusion times.
  • This pharmacokinetic difference enables gemcitabine to be effective against solid tumors where cytarabine is not.
ADVICE

Gemcitabine Infusion Duration Advice

  • Avoid giving gemcitabine infusion longer than 30 minutes to reduce increased hematologic toxicity.
  • Longer infusions increase intracellular active metabolites but do not improve clinical outcomes.
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