Pharmacokinetics of gemcitabine and 2',2'- Difluorodeoxyuridine in a patient with ascites

Brian J. Delauter; Ramesh K. Ramanathan; Merrill J. Egorin; Lori L. Stover; Eleanor G. Zuhowski; William Plunkett; William C. Zamboni

doi:10.1592/phco.20.15.1204.34586

Pharmacokinetics of gemcitabine and 2',2'- Difluorodeoxyuridine in a patient with ascites

Brian J. Delauter, Ramesh K. Ramanathan, Merrill J. Egorin, Lori L. Stover, Eleanor G. Zuhowski, William Plunkett, William C. Zamboni

Hematology/Oncology

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

Abstract

Gemcitabine (dFdC) is a prodrug that undergoes metabolism by cytidine deaminase to form an inactive metabolite, 2',2'-difluorodeoxyuridine (dFdU). The pharmacokinetics of dFdC and dFdU have been studied; however, their disposition has never been evaluated in a patient with ascites. A patient with pancreatic cancer and malignant ascites was treated with dFdC 1500 mg/m² over 150 minutes weekly for 3 weeks, repeated every 4 weeks. Serial plasma and ascites samples were obtained on weeks 1 and 2 of cycle 2. High-pressure liquid chromatography was used to quantify dFdC and dFdU in plasma and ascites. The systemic dispositions of dFdC and dFdU were similar to those reported in patients without ascites. The concentration of dFdC in ascites approached 1 mg/ml. Ascitic fluid did not serve as a depot for dFdC, and the agent's concentration in ascites approached that at which its phosphorylation is saturated.

Original language	English (US)
Pages (from-to)	1204-1207
Number of pages	4
Journal	Pharmacotherapy
Volume	20
Issue number	10
DOIs	https://doi.org/10.1592/phco.20.15.1204.34586
State	Published - 2000

ASJC Scopus subject areas

Pharmacology (medical)

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title = "Pharmacokinetics of gemcitabine and 2',2'- Difluorodeoxyuridine in a patient with ascites",

abstract = "Gemcitabine (dFdC) is a prodrug that undergoes metabolism by cytidine deaminase to form an inactive metabolite, 2',2'-difluorodeoxyuridine (dFdU). The pharmacokinetics of dFdC and dFdU have been studied; however, their disposition has never been evaluated in a patient with ascites. A patient with pancreatic cancer and malignant ascites was treated with dFdC 1500 mg/m2 over 150 minutes weekly for 3 weeks, repeated every 4 weeks. Serial plasma and ascites samples were obtained on weeks 1 and 2 of cycle 2. High-pressure liquid chromatography was used to quantify dFdC and dFdU in plasma and ascites. The systemic dispositions of dFdC and dFdU were similar to those reported in patients without ascites. The concentration of dFdC in ascites approached 1 mg/ml. Ascitic fluid did not serve as a depot for dFdC, and the agent's concentration in ascites approached that at which its phosphorylation is saturated.",

author = "Delauter, {Brian J.} and Ramanathan, {Ramesh K.} and Egorin, {Merrill J.} and Stover, {Lori L.} and Zuhowski, {Eleanor G.} and William Plunkett and Zamboni, {William C.}",

year = "2000",

doi = "10.1592/phco.20.15.1204.34586",

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T1 - Pharmacokinetics of gemcitabine and 2',2'- Difluorodeoxyuridine in a patient with ascites

AU - Delauter, Brian J.

AU - Ramanathan, Ramesh K.

AU - Egorin, Merrill J.

AU - Stover, Lori L.

AU - Zuhowski, Eleanor G.

AU - Plunkett, William

AU - Zamboni, William C.

PY - 2000

Y1 - 2000

N2 - Gemcitabine (dFdC) is a prodrug that undergoes metabolism by cytidine deaminase to form an inactive metabolite, 2',2'-difluorodeoxyuridine (dFdU). The pharmacokinetics of dFdC and dFdU have been studied; however, their disposition has never been evaluated in a patient with ascites. A patient with pancreatic cancer and malignant ascites was treated with dFdC 1500 mg/m2 over 150 minutes weekly for 3 weeks, repeated every 4 weeks. Serial plasma and ascites samples were obtained on weeks 1 and 2 of cycle 2. High-pressure liquid chromatography was used to quantify dFdC and dFdU in plasma and ascites. The systemic dispositions of dFdC and dFdU were similar to those reported in patients without ascites. The concentration of dFdC in ascites approached 1 mg/ml. Ascitic fluid did not serve as a depot for dFdC, and the agent's concentration in ascites approached that at which its phosphorylation is saturated.

AB - Gemcitabine (dFdC) is a prodrug that undergoes metabolism by cytidine deaminase to form an inactive metabolite, 2',2'-difluorodeoxyuridine (dFdU). The pharmacokinetics of dFdC and dFdU have been studied; however, their disposition has never been evaluated in a patient with ascites. A patient with pancreatic cancer and malignant ascites was treated with dFdC 1500 mg/m2 over 150 minutes weekly for 3 weeks, repeated every 4 weeks. Serial plasma and ascites samples were obtained on weeks 1 and 2 of cycle 2. High-pressure liquid chromatography was used to quantify dFdC and dFdU in plasma and ascites. The systemic dispositions of dFdC and dFdU were similar to those reported in patients without ascites. The concentration of dFdC in ascites approached 1 mg/ml. Ascitic fluid did not serve as a depot for dFdC, and the agent's concentration in ascites approached that at which its phosphorylation is saturated.

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JO - Pharmacotherapy

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Pharmacokinetics of gemcitabine and 2',2'- Difluorodeoxyuridine in a patient with ascites

Abstract

ASJC Scopus subject areas

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