OBJECTIVES: Tenofovir and emtricitabine are very effective and well-tolerated antiretrovirals representing current backbone of the antiretroviral combination regimens for the prevention of perinatal HIV transmission. The aim of our study was to determine whether tenofovir or emtricitabine administered in long-term fashion affect expression of two widely described pharmacokinetic determinants, P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), in maternal or fetal biological tissues. METHODS: For this purpose, pregnant Wistar rats were administered tenofovir (2.25 mg/kg/day), emtricitabine (3.5 mg/kg/day) or saline i.m. for 10 days (from the 12th to 21st gestation day). On the 22nd day, the placenta and maternal/fetal intestine, brain, kidneys and liver were sampled and analysed for Abcb1a, Abcb1b and Abcg2 expression; placental and newborns' weights were also monitored. KEY FINDINGS: We found that long-term application of tenofovir or emtricitabine did not significantly affect expression of Abcb1a, Abcb1b and Abcg2 in either maternal or fetal organs. However, tenofovir administration significantly increased placenta-to-birthweight ratio, a strong indicator of various diseases occurring later in life. CONCLUSIONS: Our data broaden current knowledge on safety profile of tenofovir and emtricitabine use in pregnancy. Nevertheless, further research in other mammal species, including humans, is important to fully elucidate this issue.
- Klíčová slova
- ABC transporters, drug interactions, emtricitabine, pregnancy, tenofovir,
- MeSH
- ABC transportér z rodiny G, člen 2 MeSH
- ABC transportéry metabolismus MeSH
- emtricitabin aplikace a dávkování MeSH
- krysa rodu Rattus MeSH
- P-glykoproteiny metabolismus MeSH
- placenta účinky léků metabolismus MeSH
- plod účinky léků metabolismus MeSH
- potkani Wistar MeSH
- těhotenství MeSH
- tenofovir aplikace a dávkování MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- ABC transportér z rodiny G, člen 2 MeSH
- ABC transportéry MeSH
- Abcg2 protein, rat MeSH Prohlížeč
- emtricitabin MeSH
- multidrug resistance protein 3 MeSH Prohlížeč
- P-glykoproteiny MeSH
- tenofovir MeSH
