Document Detail

Acyclovir, ganciclovir, and zidovudine transfer into rat milk.
MedLine Citation:
PMID:  12019097     Owner:  NLM     Status:  MEDLINE    
Treatment with antiviral agents that accumulate in breast milk may offer a novel approach to reduce the rates of vertical transmission of important viruses and the risk of clinical illness in suckling neonates. The present study evaluated the extent and mechanism of transfer of three antiviral nucleoside analogues into milk in a lactating rat model system. Acyclovir (0.26 mg/h), ganciclovir (0.13 mg/h), and zidovudine (0.5 mg/h) were each infused to steady-state concentrations in six rats 15 to 16 days postpartum. The observed ratios of the concentrations in milk to the concentrations in serum (observed milk-to-serum ratio), calculated from the ratio of the steady-state concentration in serum to the steady-state concentration in milk, determined the extent of drug transfer into milk. To identify the mechanism of transfer into milk, the observed milk-to-serum ratio was compared to a predicted milk-to-serum ratio estimated from an in vitro passive diffusion model of transfer of each drug into milk. High-pressure liquid chromatography methods determined milk and serum drug concentrations. Mean +/- standard deviation observed milk-to-serum ratios for acyclovir, ganciclovir, and zidovudine were 5.1 +/- 1.4, 1.6 +/- 0.33, and 1.0 +/- 0.29, respectively, compared with their corresponding predicted ratios of 1.1, 0.85, and 0.71. These results suggest that acyclovir accumulates in milk due to active transport mechanisms, while passive diffusion processes govern the transfer of both ganciclovir and zidovudine into milk. The presence of all three antiviral drugs in milk and the potential for active drug transfer into milk warrants further investigation of the accumulation of other antiviral drugs in milk and their therapeutic benefits in reducing the vertical transmission of viruses and clinical sequelae in the breast-feeding infant.
Jane Alcorn; Patrick J McNamara
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Antimicrobial agents and chemotherapy     Volume:  46     ISSN:  0066-4804     ISO Abbreviation:  Antimicrob. Agents Chemother.     Publication Date:  2002 Jun 
Date Detail:
Created Date:  2002-05-20     Completed Date:  2002-10-22     Revised Date:  2013-04-18    
Medline Journal Info:
Nlm Unique ID:  0315061     Medline TA:  Antimicrob Agents Chemother     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1831-6     Citation Subset:  IM    
Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536-0082, USA.
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MeSH Terms
Acyclovir / blood,  pharmacokinetics*
Anti-HIV Agents / blood,  pharmacokinetics*
Antiviral Agents / blood,  pharmacokinetics*
Chromatography, High Pressure Liquid
Ganciclovir / blood,  pharmacokinetics*
Infusions, Intravenous
Lactation / physiology
Milk / metabolism*
Rats, Sprague-Dawley
Zidovudine / blood,  pharmacokinetics*
Reg. No./Substance:
0/Anti-HIV Agents; 0/Antiviral Agents; 30516-87-1/Zidovudine; 59277-89-3/Acyclovir; 82410-32-0/Ganciclovir

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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