Document Detail


Pharmacokinetic profiling of efavirenz-emtricitabine-tenofovir fixed dose combination in pregnant and non-pregnant rats.
MedLine Citation:
PMID:  22610784     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
During pregnancy, disposition of various drugs is altered due to changes in physiological condition, maternal gastrointestinal absorption, gastric secretion and motility. Fixed dose combination of antiretrovirals is commonly prescribed for the treatment of HIV infection. There is a need to understand the pharmacokinetics and placental transfer of efavirenz-emtricitabine-tenofovir in fixed dose combination during pregnancy. The pharmacokinetics and placental transfer of efavirenz-emtricitabine-tenofovir fixed dose combination was evaluated in the timed pregnant and non-pregnant Sprague Dawley rats at 30, 10, 15 mg/kg, p.o. respectively. The plasma, placental tissue, amniotic fluid and fetal tissue concentrations were measured using high performance liquid chromatography combined with tandem mass spectrometric detector (LC-MS/MS). To summarize, pharmacokinetic profile of efavirenz remained similar in the pregnant and non-pregnant rats. However, considerable difference in pharmacokinetics of emtricitabine and tenofovir was observed between pregnant and non-pregnant rats. Efavirenz and emtricitabine showed appreciable placental, amniotic fluid and fetal exposure compared to tenofovir. The present study suggests that a profound impact on antiretroviral pharmacokinetics was observed during pregnancy and there is a need to monitor exposure levels of each drug when administered as a fixed dose combination during pregnancy. Further studies to explore pharmacokinetic parameters of fixed dose antiretrovirals during preclinical stage in timed-pregnancy rat model are required. Such studies can help in development of safe and effective medications with reduced risk of perinatal transmission of HIV-1 infection. Copyright © 2012 John Wiley & Sons, Ltd.
Authors:
Ramakrishna Nirogi; Gopinadh Bhyrapuneni; Vishwottam Kandikere; Nageswararao Muddana; Ramanatha Saralaya; Prashanth Komarneni; Koteshwara Mudigonda; K Mukkanti
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-5-18
Journal Detail:
Title:  Biopharmaceutics & drug disposition     Volume:  -     ISSN:  1099-081X     ISO Abbreviation:  -     Publication Date:  2012 May 
Date Detail:
Created Date:  2012-5-21     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7911226     Medline TA:  Biopharm Drug Dispos     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 John Wiley & Sons, Ltd.
Affiliation:
Pharmacokinetics and Drug Metabolism, Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad, 500034, India. ramakrishna_nirogi@yahoo.co.in, nvsrk@suven.com.
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