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gemcitabine (Gemzar)

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: 1) 1000 mg/m2 IV weekly for 7 weeks, 1 week of rest, then a 3-week-on & 1-week-off schedule 2) given over 30 minutes Powder for injection: (lyophilized) 20 mg/mL (10 mL, 50 mL) Pharmacokinetics: 1) metabolized in liver & blood 2) most is eliminated in the urine 3) 1/2life is 10-15 minutes 4) metabolite 1/2life is 10 hours Monitor: 1) complete blood count (CBC) prior to each dose 2) liver function tests prior to initiation of therapy & periodically 3) serum creatinine & BUN prior to initiation of therapy & periodically Adverse effects: - common (> 10%) 1) myelosuppression a) leukopenia, thrombocytopenia, anemia b) dose-limiting toxicity 2) fever (41%) occurs in the absence of infection 3) rash (30%) a) macular or finely granular maculopapular b) mild to moderately pruritic c) involves the trunk & extremities 4) peripheral edema 5) alopecia 6) mild nausea 7) constipation or diarrhea 8) stomatitis 9) headache 10) flu-like syndrome 11) elevated liver function tests 12) pain 13) proteinuria 14) hematuria 15) elevated urea nitrogen 16) dyspnea 17) infection 18) thromboembolism 19) thrombotic thrombocytopenic purpura (TTP) [6] Mechanism of action: 1) nucleoside analog 2) S-phase specific 3) metabolized intracellularly to its active triphosphate form which inhibits DNA replication & repair by blocking DNA synthesis

General

antineoplastic agent (chemotherapeutic agent) pyrimidine antimetabolite; antimetabolite; pyrimidine analog

Properties

MISC-INFO: elimination route LIVER KIDNEY pregnancy-category D 1/2life 10 HOURS

Database Correlations

PUBCHEM correlations

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) http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=65&abstractID=33576
  5. Deprecated Reference
  6. 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