Back to Search
Start Over
Role of human placental apical membrane transporters in the efflux of glyburide, rosiglitazone, and metformin.
- Source :
-
American journal of obstetrics and gynecology [Am J Obstet Gynecol] 2010 Apr; Vol. 202 (4), pp. 383.e1-7. - Publication Year :
- 2010
-
Abstract
- Objective: Substrates of placental efflux transporters could compete for a single transporter, which could result in an increase in the transfer of each substrate to the fetal circulation. Our aim was to determine the role of placental transporters in the biodisposition of oral hypoglycemic drugs that could be used as monotherapy or in combination therapy for gestational diabetes.<br />Study Design: Inside-out brush border membrane vesicles from term placentas were used to determine the efflux of glyburide, rosiglitazone, and metformin by P-glycoprotein, breast cancer resistance protein, and multidrug resistance protein.<br />Results: Glyburide was transported by multidrug resistance protein (43 +/- 4%); breast cancer resistance protein (25 +/- 5%); and P-glycoprotein (9 +/- 5%). Rosiglitazone was transported predominantly by P-glycoprotein (71 +/- 26%). Metformin was transported by P-glycoprotein (58 +/- 20%) and breast cancer resistance protein (25 +/- 14%).<br />Conclusion: Multiple placental transporters contribute to efflux of glyburide, rosiglitazone, and metformin. Administration of drug combinations could lead to their competition for efflux transporters.<br /> (Copyright 2010 Mosby, Inc. All rights reserved.)
- Subjects :
- Adenosine Triphosphate metabolism
Biological Transport physiology
Carbon Radioisotopes
Carrier Proteins metabolism
Cell Polarity physiology
Diabetes, Gestational drug therapy
Diabetes, Gestational metabolism
Drug Interactions
Female
Humans
Maternal-Fetal Exchange
Microvilli metabolism
Pregnancy
Rosiglitazone
Tritium
Glyburide pharmacokinetics
Hypoglycemic Agents pharmacokinetics
Metformin pharmacokinetics
Placenta metabolism
Thiazolidinediones pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1097-6868
- Volume :
- 202
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- American journal of obstetrics and gynecology
- Publication Type :
- Academic Journal
- Accession number :
- 20350646
- Full Text :
- https://doi.org/10.1016/j.ajog.2010.01.035