Fluorescence polarization immunoassay for zidovudine

Granich, G G; Eveland, Michael; Krogstad, Donald J.

doi:10.1128/aac.33.8.1275

Cited by 23 publications

(8 citation statements)

References 17 publications

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“…The development of a fluorescence polarisation assay and a radioimmunoassay (RIA) method to measure plasma zidovudine concentrations has provided more sensitive tools for investigating the pharmacokinetics of the drug (Granich et al 1989). A study conducted in HIV-infected patients with haemophilia (with CD4+ counts ranging from 200 to 500 cells/mm 3 ) employed a 12 to 24h sampling period and RIA to evaluate zidovudine disposition (intravenous and oral) every 6 weeks while patients were enrolled in a 12-week modified phase I study .…”

Section: Endogenous Nucleosidesmentioning

confidence: 99%

Comparative Pharmacokinetics of Antiviral Nucleoside Analogues

Morse

Shelton

O’Donnell

1993

Clinical Pharmacokinetics

119

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The recent development of nucleoside analogues with antiviral activity has expanded the small but useful armamentarium for the treatment of certain viral diseases such as the human immunodeficiency virus, cytomegalovirus and others. Their intracellular site of action and need for sequential phosphorylation require that traditional pharmacokinetic parameters be used in conjunction with an understanding of intracellular metabolism when designing dosage regimens. This review summarises the available pharmacokinetic literature for zidovudine, didanosine, zalcitabine, aciclovir, ganciclovir, vidarabine and ribavirin. After oral administration, didanosine, aciclovir and ribavirin are < 50% bioavailable and ganciclovir is < 6% absorbed. In contrast, zidovudine and zalcitabine are > 60% bioavailable, although zidovudine undergoes considerable and variable first-pass hepatic glucuronidation while zalcitabine has no first-pass effect. Zidovudine, zalcitabine and didanosine are absorbed rapidly in the fasted state, with peak plasma concentrations exceeding their respective in vitro antiretroviral inhibitory concentrations. All reviewed agents except ribavirin have a relatively short plasma half-life (approximately 0.5 to 4h), with each agent demonstrating a different intracellular enzymatic activation scheme. For example, the rate-limiting step for formation of zidovudine triphosphate is the conversion of the monophosphate to the diphosphate, while didanosine is ultimately converted to dideoxyadenosine triphosphate which has the longest intracellular half-life (approximately 12 to 24h) among these agents. These drugs are not highly protein bound and they distribute into tissues with an apparent volume of distribution at steady-state ranging from 0.3 to 1.2 L/kg. They vary in the extent to which they enter cerebrospinal fluid, ranging from a low of < 25% for didanosine to a high of > 70% of a concurrent plasma concentration for ribavirin and vidarabine. These agents also vary with regard to degree of renal excretion of the parent drug, with the lowest noted for vidarabine (1 to 3%) and the highest for zalcitabine (approximately 75%) and ganciclovir (> 90%). With the increasing number of clinically useful nucleoside analogues, it is essential for the clinician to appreciate the subtle differences among these agents to ensure that optimal therapeutic outcomes may be attained with minimal toxicity.

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Section: Endogenous Nucleosidesmentioning

confidence: 99%

Comparative Pharmacokinetics of Antiviral Nucleoside Analogues

Morse

Shelton

O’Donnell

1993

Clinical Pharmacokinetics

119

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“…Several methods have been discovered for the quantitative determination of zidovudine including chromatog- raphy [9][10][11][12][13][14][15], fluorescence polarization immunoassay [16], using diamond paste based immunosensor [17], fluorescence spectroscopy [18] and voltammetry [19][20][21][22][23][24].…”

Section: Introductionmentioning

confidence: 99%

Determination of the Antiretroviral Drug Zidovudine in Diluted Alkaline Electrolyte by Adsorptive Stripping Voltammetry at the Mercury Film Electrode

Castro¹,

Aucélio²,

Rey³

et al. 2011

AJAC

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This paper describes a stripping method for the determination of zidovudine at the submicromolar concentration levels. This method is based on the controlled adsorptive accumulation of zidovudine at the thin-film mercury electrode, followed by a linear-sweep stripping voltammetry measurement of the surface species. Optimal experimental conditions include a NaOH solution of 2.0 × 10 -3 mol·L -1 (supporting electrolyte), an accumulation potential of -0.30 V and a scan rate of 100 mV·s -1 . The response of zidovudine is linear over the concentration range 0.01 -0.08 ppm. After an accumulation time of 5 minutes, the detection limit was found to be 0.67 ppb (2.5 × 10 -9 mol·L -1 ). More convenient methods to measure zidovudine concentration in the presence of the didanosine, acyclovir, nevirapine, lamivudine, and efavirenz, were also investigated. The presence of zidovudine together with ATP or ssDNA demonstrates the utility of this method.

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“…The antibodies used in both immunoassays have extremely small cross-reactivities with GZDV. Therefore, enzymatic hydrolysis of GZDV to ZDV by (3-glucuronidase can be performed prior to immunoassay (33,34). In these procedures, serum samples are split, and one portion is treated with enzyme prior to assay.…”

Section: Fpiamentioning

confidence: 99%

“…Good correlation with HPLC has been observed in both immunoassays. The ZDV-Trac RIA kit instructions include the GZDV procedure, while the FPIA GZDV procedure can be found in reference (34).…”

Section: Fpiamentioning

confidence: 99%

State‐Of‐The‐Art of zidovudine monitoring

Stretcher

1991

Clinical Laboratory Analysis

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Zidovudine, the only drug approved by the FDA for the treatment of AIDS, has well-documented efficacy, but numerous toxic side effects. Despite considerable knowledge of the pharmacology of the drug, however, a therapeutic concentration range has not been established. This article reviews methodologies used for measurement of zidovudine in serum. Procedures for several methods are described and comparisons offered. In addition to methodologies, other issues of concern in establishing or maintaining a zidovudine monitoring service are also discussed, including the clinical relevance of routine zidovudine monitoring, method-related quality control, and laboratory safety. Methodologies currently being developed to measure the active intracellular metabolites of zidovudine are also described. These methods are believed to be the key to fully understanding the relationships between zidovudine pharmacology, toxicity, and efficacy.

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Fluorescence polarization immunoassay for zidovudine

Cited by 23 publications

References 17 publications

Comparative Pharmacokinetics of Antiviral Nucleoside Analogues

Comparative Pharmacokinetics of Antiviral Nucleoside Analogues

Determination of the Antiretroviral Drug Zidovudine in Diluted Alkaline Electrolyte by Adsorptive Stripping Voltammetry at the Mercury Film Electrode

State‐Of‐The‐Art of zidovudine monitoring

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