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| __NOTOC__
| | #REDIRECT [[Felodipine#Drug Interactions]] |
| {{Felodipine}}
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| {{CMG}}; {{AE}} {{SS}}
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| ==Drug Interactions==
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| '''CYP3A4 Inhibitors''' – Felodipine is metabolized by CYP3A4. Co-administration of CYP3A4 inhibitors (eg, [[ketoconazole]], [[itraconazole]], [[erythromycin]], grapefruit juice, [[cimetidine]]) with felodipine may lead to several-fold increases in the plasma levels of felodipine, either due to an increase in bioavailability or due to a decrease in metabolism. These increases in concentration may lead to increased effects, (lower blood pressure and increased heart rate). These effects have been observed with co-administration of itraconazole (a potent CYP3A4 inhibitor). Caution should be used when CYP3A4 inhibitors are co-administered with felodipine. A conservative approach to dosing felodipine should be taken. The following specific interactions have been reported:
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| '''Itraconazole''' – Co-administration of another extended release formulation of felodipine with [[itraconazole]] resulted in approximately 8-fold increase in the AUC, more than 6-fold increase in the Cmax, and 2-fold prolongation in the half-life of felodipine.
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| '''Erythromycin''' – Co-administration of felodipine (PLENDIL) with [[erythromycin]] resulted in approximately 2.5-fold increase in the AUC and Cmax, and about 2-fold prolongation in the half-life of felodipine.
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| '''Grapefruit juice''' – Co-administration of felodipine with grapefruit juice resulted in more than 2-fold increase in the AUC and Cmax, but no prolongation in the half-life of felodipine.
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| '''Cimetidine '''– Co-administration of felodipine with [[cimetidine]] (a non-specific CYP-450 inhibitor) resulted in an increase of approximately 50% in the AUC and the Cmax, of felodipine.
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| '''Beta-Blocking Agents''' – A pharmacokinetic study of felodipine in conjunction with metoprolol demonstrated no significant effects on the pharmacokinetics of felodipine. The AUC and Cmax of metoprolol, however, were increased approximately 31 and 38%, respectively. In controlled clinical trials, however, [[beta blockers]] including metoprolol were concurrently administered with felodipine and were well tolerated.
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| '''Digoxin '''– When given concomitantly with PLENDIL the pharmacokinetics of [[digoxin]] in patients with heart failure were not significantly altered.
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| '''Anticonvulsants''' – In a pharmacokinetic study, maximum plasma concentrations of felodipine were considerably lower in epileptic patients on long-term anticonvulsant therapy (eg, [[phenytoin]], [[carbamazepine]], or [[phenobarbital]]) than in healthy volunteers. In such patients, the mean area under the felodipine plasma concentration-time curve was also reduced to approximately 6% of that observed in healthy volunteers. Since a clinically significant interaction may be anticipated, alternative antihypertensive therapy should be considered in these patients.
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| '''Tacrolimus''' – Felodipine may increase the blood concentration of [[tacrolimus]]. When given concomitantly with felodipine, the tacrolimus blood concentration should be followed and the tacrolimus dose may need to be adjusted.
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| '''Other Concomitant Therapy''' – In healthy subjects there were no clinically significant interactions when felodipine was given concomitantly with [[indomethacin]] or [[spironolactone]].
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| Interaction with Food – See CLINICAL PHARMACOLOGY, Pharmacokinetics and Metabolism.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = PLENDIL (FELODIPINE) TABLET, EXTENDED RELEASE [ASTRAZENECA LP] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=2aad9cdf-6431-4661-5cb4-f69e735f47e4 | publisher = | date = | accessdate = 28 February 2014 }}</ref>
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| ==References ==
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| {{Reflist|2}}
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| {{Calcium channel blockers}}
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| [[Category:Calcium channel blockers]]
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| [[Category:Dihydropyridines]]
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| [[Category:Carboxylate esters]]
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| [[Category:Organochlorides]]
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| [[Category:Cardiovascular Drugs]]
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| [[Category:Drugs]]
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