Pharmacological Effects of Common Medications with
| PHARMACOLOGICAL EFFECTS OF GRAPEFRUIT JUICE WITH MEDICATIONS | ||
|---|---|---|
| Grapefruit or grapefruit juice has been shown to affect the metabolism of many medications, increasing the risk of toxicity and adverse events. Characteristics of oral medications that may interact with grapefruit include extensive metabolism through the intestinal cytochrome P450 3A4 (CYP3A4) system, low bioavailability, and a narrow therapeutic index. Grapefruit juice interacts through the intestinal CYP3A4 system and can inhibit the concentration for 24−72hrs. Not an exclusive list of medications that may interact with grapefruit. Caution should be taken by both patient and physician and monitor adverse reactions when taking medications that may interact with grapefruit or juice. | ||
| Generic | Brand | Clinical Implications of Co‑administration with Grapefruit or Grapefruit Juice |
| ALKALOID | ||
| colchicine | Colcrys | Increases the risk of colchicine-induced toxic effects; significant increase in colchicine plasma concentration is anticipated. Grapefruit and grapefruit juice should not be consumed during colchicine treatment. |
| ANTIARRHYTHMICS | ||
| amiodarone | — | Inhibits CYP3A4-mediated metabolism of oral amiodarone resulting in increase plasma levels of amiodarone. Avoid co‑administration. |
| dofetilide | Tikosyn | Inhibitor of the CYP3A4 isoenzyme, thus could increase systemic dofetilide exposure. If co‑administration is necessary, use with caution. |
| dronedarone | Multaq | Moderate inhibitor of CYP3A, results in a 3‑fold increase in dronedarone exposure and a 2.5‑fold increase in Cmax. Avoid co‑administration. |
| ANTIHELMINTHIC | ||
| praziquantel | Biltricide | 1.6-fold increase in the Cmax and a 1.9‑fold increase in the AUC of praziquantel. |
| ANTIPSYCHOTIC | ||
| pimozide | Orap | Inhibits CYP3A4-mediated metabolism of pimozide. Avoid co‑administration. |
| CALCIUM CHANNEL BLOCKERS | ||
| felodipine | — | 2-fold increase in felodipine AUC and Cmax. Avoid co‑administration prior to and during treatment. |
| nifedipine | Procardia | 2-fold increase in nifedipine AUC and Cmax with no change in half‑life. Avoid co‑administration. |
| nisoldipine | Sular | 3-fold increase in nisoldipine Cmax and 2‑fold increase in nisoldipine AUC. Avoid co‑administration. |
| verapamil | Verelan | May significantly increase concentrations of verapamil. Increased S- and R‑verapamil AUC0−12 by 36% and 28%, respectively. Steady state Cmax and Cmin of S‑verapamil increased by 57% and 16.7%, respectively compared to control. Cmax and Cmin of R‑verapamil increased by 40% and 13%, respectively. No clinical consequences expected. |
| CHOLESTEROL-LOWERING MEDICATIONS | ||
| atorvastatin | Lipitor | Inhibits CYP3A4 and can increase plasma concentrations of atorvastatin, especially with excessive grapefruit juice consumption (>1.2L/day). |
| lovastatin | — | Inhibits CYP3A4 and can increase plasma concentrations of lovastatin. Avoid co-administration. |
| simvastatin | Zocor | Inhibits CYP3A4 and can increase plasma concentrations of simvastatin and may increase risk of myopathy. Avoid co-administration. |
| CYSTIC FIBROSIS THERAPY | ||
| ivacaftor | Kalydeco | Co-administration may increase exposure of ivacaftor. Grapefruit or Seville oranges should be avoided during treatment. |
| ERGOT ALKALOIDS | ||
| dihydroergo– tamine mesylate |
D.H.E. 45 | A potential risk for serious toxicity (including vasospasm) exists. |
| ergotamine tartrate + caffeine |
— | A potential risk for serious toxicity (including vasospasm) exists. |
| H1-RECEPTOR ANTAGONIST | ||
| fexofenadine | Allegra | May reduce bioavailability and exposure of fexofenadine. In a bioequivalence study, the bioavailability of fexofenadine was reduced by 36%. Take with water. |
| HYPONATREMIA THERAPY | ||
| tolvaptan | Samsca | Co-administration results in a 1.8‑fold increase in exposure to tolvaptan. |
| IMMUNOSUPPRESSANTS | ||
| cyclosporine | Neoral | Affects metabolism and increases blood concentrations of cyclosporine. Avoid co‑administration. |
| everolimus | Zortress | Inhibits CYP3A4 and P‑gp activity and should therefore be avoided with concomitant use of everolimus and cyclosporine. |
| sirolimus | Rapamune | Reduces CYP3A4-mediated drug metabolism and must not be taken with or used for dilution of sirolimus. |
| tacrolimus | Prograf | Affects CYP3A-mediated metabolism and should be avoided. |
| temsirolimus | Torisel | May increase plasma concentrations of sirolimus, a major metabolite of temsirolimus, and should be avoided. |
| INTERMITTENT CLAUDICATION THERAPY | ||
| cilostazol | — | Increase in the Cmax of cilostazol by ∼50%, but has no effect on AUC. Reduce dose to 50mg with co-administration. |
| MYELOFIBROSIS THERAPY | ||
| ruxolitinib | Jakafi | The recommended starting dose of ruloxitinib is 10mg twice daily for patients with a platelet count ≥100 × 109/L. Concurrent administration of should be avoided in patients with platelet counts <100 × 109/L. |
| ONCOLOGY AGENTS | ||
| axitinib | Inlyta | May increase plasma concentrations of axitinib and should be avoided. |
| crizotinib | Xalkori | May increase plasma concentrations of crizotinib and should be avoided. |
| dasatinib | Sprycel | May increase plasma concentrations of dasatinib and should be avoided. |
| everolimus | Afinitor | May increase exposures of everolimus and should be avoided. |
| ixabepilone | Ixempra | May increase plasma concentrations of ixabepilone and should be avoided. |
| lapatanib | Tykerb | May increase plasma concentrations of lapatinib and should be avoided. |
| nilotinib | Tasigna | May increase plasma concentrations of nilotinib and should be avoided. |
| pazopanib | Votrient | May increase plasma concentrations of pazopanib and should be avoided. |
| sunitinib | Sutent | May increase plasma concentrations of sunitinib and should be avoided. |
| OPIOID | ||
| fentanyl | Fentora | May result in a potentially dangerous increase in fentanyl plasma concentrations, which could increase or prolong adverse drug effects and may cause potentially fatal respiratory depression. |
| PHOSPHODIESTERASE TYPE 5 INHIBITORS | ||
| tadalafil | Cialis | Likely increase of tadalafil exposure. |
| vardenafil | Staxyn | Do not use, as the systemic concentration of vardenafil is increased. |
| PSYCHOTROPIC AGENTS | ||
| buspirone | — | 4.3 fold increase in Cmax; 9.2 fold increase in AUC. Avoid drinking large amounts (200mL double-strength three times daily) of grapefruit juice. |
| triazolam | Halcion | Increases the Cmax of triazolam by 25%, increases AUC by 48%, and increases half-life by 18%. Use with caution. |
| STEROID | ||
| budesonide | Entocort EC |
After extensive intake of grapefruit juice, the systemic exposure for oral budesonide increased about two times. Ingestion of grapefruit or grapefruit juice should be avoided. |
| REFERENCES | ||
|
Stump AL, Mayo T, Blum A. Management of Grapefruit-Drug Interactions. Am Fam Physician. 2006 Aug 15;74(4):605–608. (Rev. 6/2018) |
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This article originally appeared on MPR
