Pub. Date : 1998 Aug
PMID : 9694927
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | We previously showed that terfenadine blocked HERG (Human Ether-a-Gogo Related Gene), an important component of the repolarizing cardiac delayed rectifier IK with concentration needed to obtain 50% of the block (IC50) in the therapeutic range (300 nM). | Terfenadine | potassium voltage-gated channel subfamily H member 2 | Homo sapiens |
| 2 | We conclude that ketoconazole may potentiate the effects of terfenadine first by an indirect pharmacokinetic action to elevate plasma levels and second by a direct pharmacodynamic action on HERG currents. | Terfenadine | potassium voltage-gated channel subfamily H member 2 | Homo sapiens |
| 3 | These potential dual actions on HERG currents suggest that precautions should be taken in long-term ketoconazole treatment, particularly for patients who have decreased liver function or are on a drug regimen requiring simultaneous medications that use cytochrome-P450 for breakdown, such as terfenadine or erythromycin, or Class III antiarrhythmic drugs. | Terfenadine | potassium voltage-gated channel subfamily H member 2 | Homo sapiens |