Limited P-glycoprotein mediated efflux for anti-epileptic drugs.
A variety of anti-epileptic drugs (AEDs) were tested for their ability to be transported by P-glycoprotein (P-gp) through Caco-2 monolayers using bi-directional (apical (Ap) to basolateral (Bas), and Bas to Ap) studies. Transport rates were equivalent in both directions for vigabatrin, gabapentin, p...
| Main Authors: | , |
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| Format: | Journal Article |
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informa UK Ltd
2006
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| Online Access: | http://hdl.handle.net/20.500.11937/8478 |
| _version_ | 1848745670267109376 |
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| author | Crowe, Andrew Teoh, Y. |
| author_facet | Crowe, Andrew Teoh, Y. |
| author_sort | Crowe, Andrew |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | A variety of anti-epileptic drugs (AEDs) were tested for their ability to be transported by P-glycoprotein (P-gp) through Caco-2 monolayers using bi-directional (apical (Ap) to basolateral (Bas), and Bas to Ap) studies. Transport rates were equivalent in both directions for vigabatrin, gabapentin, phenobarbitone, lamotrigine and carbamazepine, being 0.7 × 10− 6, 0.1 × 10− 6, 34 × 10− 6, 36 × 10− 6 and 55 × 10− 6 cm/s, respectively. Phenytoin displayed a 20% increase in Ap to Bas transport, while topiramate and ethosuximide each had greater transport in the uptake direction, with both drugs showing no efflux. None of the transport rates for these drugs were affected by P-gp inhibitors. However, the efflux rate for acetazolamide was 3-fold higher than its uptake and this was significantly reduced by P-gp inhibitors. Thus, only one anti-epileptic, acetazolamide, was shown to be weak P-gp substrate, suggesting that P-gp efflux may not be a factor in relation to the development of resistance of epilepsy therapy. |
| first_indexed | 2025-11-14T06:21:03Z |
| format | Journal Article |
| id | curtin-20.500.11937-8478 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T06:21:03Z |
| publishDate | 2006 |
| publisher | informa UK Ltd |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-84782017-09-13T15:54:28Z Limited P-glycoprotein mediated efflux for anti-epileptic drugs. Crowe, Andrew Teoh, Y. A variety of anti-epileptic drugs (AEDs) were tested for their ability to be transported by P-glycoprotein (P-gp) through Caco-2 monolayers using bi-directional (apical (Ap) to basolateral (Bas), and Bas to Ap) studies. Transport rates were equivalent in both directions for vigabatrin, gabapentin, phenobarbitone, lamotrigine and carbamazepine, being 0.7 × 10− 6, 0.1 × 10− 6, 34 × 10− 6, 36 × 10− 6 and 55 × 10− 6 cm/s, respectively. Phenytoin displayed a 20% increase in Ap to Bas transport, while topiramate and ethosuximide each had greater transport in the uptake direction, with both drugs showing no efflux. None of the transport rates for these drugs were affected by P-gp inhibitors. However, the efflux rate for acetazolamide was 3-fold higher than its uptake and this was significantly reduced by P-gp inhibitors. Thus, only one anti-epileptic, acetazolamide, was shown to be weak P-gp substrate, suggesting that P-gp efflux may not be a factor in relation to the development of resistance of epilepsy therapy. 2006 Journal Article http://hdl.handle.net/20.500.11937/8478 10.1080/10611860600720814 informa UK Ltd restricted |
| spellingShingle | Crowe, Andrew Teoh, Y. Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title | Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title_full | Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title_fullStr | Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title_full_unstemmed | Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title_short | Limited P-glycoprotein mediated efflux for anti-epileptic drugs. |
| title_sort | limited p-glycoprotein mediated efflux for anti-epileptic drugs. |
| url | http://hdl.handle.net/20.500.11937/8478 |