gemcitabine (Gemzar)
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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
- breast cancer[5]
- ovarian cancer
- head & neck cancer
- testicular cancer
- osteosarcoma
- Ewing sarcoma[5]
Contraindications
Caution:
- use with caution in patients with renal insufficiency
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
- thrombotic thrombocytopenic purpura (TTP)[6]
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
- pyrimidine antimetabolite; antimetabolite; pyrimidine analog
- antineoplastic agent (chemotherapeutic agent)
References
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
- ↑ 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) http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=65&abstractID=33576
- ↑ 5.0 5.1 5.2 Deprecated Reference
- ↑ 6.0 6.1 Lim MY Non-Small Cell Lung Cancer: 5 Management Challenges. Medscape. Nov 30, 2016 http://reference.medscape.com/features/slideshow/non-small-cell-lung-cancer