Gemcitabine

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Monitor 7 Adverse-effects 8 Mechanism-of-action 9 More General Terms 10 Internet Database 11 References

Introduction

• Tradename: Gemzar.

Indications

• adenocarcinoma of the pancreas
• non-small cell lung cancer
• bladder cancer, transitional cell carcinoma
• small cell lung cancer (trials in progress 1999)
• cholangiocarcinoma
• gallbladder cancer

Contraindications

• Caution:
• use with caution in patients with renal insufficiency
  

• pregnancy category = d

Dosage

• 1000 mg/m2 IV weekly for 7 weeks, 1 week of rest, then a 3-week-on & 1-week-off schedule
• given over 30 minutes

• Powder for injection: ( lyophilized) 20 mg/mL (10 mL, 50 mL)

Pharmacokinetics

• metabolized in liver & blood
• most is eliminated in the urine
• 1/2life is 10-15 minutes
• metabolite 1/2life is 10 hours
  

• elimination via liver
• elimination via kidney
• 1/2life = 10 hours

Monitor

• complete blood count ( CBC) prior to each dose
• liver function tests prior to initiation of therapy & periodically
• serum creatinine & BUN prior to initiation of therapy & periodically

Adverse-effects

• common (> 10%)
• myelosuppression

• leukopenia, thrombocytopenia, anemia
• dose-limiting toxicity

• fever (41%) occurs in the absence of infection
• rash (30%)

• macular or finely granular maculopapular
• mild to moderately pruritic
• involves the trunk & extremities

• peripheral edema
• alopecia
• mild nausea
• constipation or diarrhea
• stomatitis
• headache
• flu-like syndrome
• elevated liver function tests
• pain
• proteinuria
• hematuria
• elevated urea nitrogen
• dyspnea
• infection
• thromboembolism

Mechanism-of-action

• nucleoside analog
• S-phase specific
• metabolized intracellularly to its active triphosphate form which inhibits DNA replication & repair by blocking DNA synthesis

More General Terms

• antineoplastic agent (chemotherapeutic agent)

Internet Database

PubChem: 60750
PubChem: 356653
PubChem: 3461
PubChem: 60749

References

1. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
3. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
4. Hahn MH et al A multicenter phase II study of cisplatin (C), gemcitabine (G), and bevacizumab (B) as first-line chemotherapy for metastatic urothelial carcinoma (UC): Hoosier Oncology Group GU-0475. J Clin Oncol 27:15s, 2009 (suppl; abstr 5018) [1]
5. National Guideline Clearinghouse
   - Use of gemcitabine in the treatment of advanced pancreatic adenocarcinoma (Program in Evidence-based Care) ngc-guideline: [2]
   - The role of gemcitabine in the management of metastatic breast cancer: a clinical practice guideline. (Program in Evidence-based Care) ngc-guideline: [3]
   - The role of gemcitabine in the treatment of cholangiocarcinoma and gallbladder cancer. (Program in Evidence-based Care) ngc-guideline: [4]

gemcitabine (Gemzar)