Table 1:

Selected drugs that interact with grapefruit, associated oral bioavailability, adverse event(s), predicted risk and possible alternative agents

Interacting drugsInnate oral bioavailability*Dose-related adverse event(s)Predicted interaction riskPotential alternative agent(s)
Anticancer agents
CrizotinibIntermediateTorsade de pointes, myelotoxicityHigh
DasatinibNot knownTorsade de pointes, myelotoxicityHighImatinib
ErlotinibIntermediateMyelotoxicityHigh
EverolimusLowMyelotoxicity, nephrotoxicityHigh
LapatinibIncompleteTorsade de pointes, myelotoxicityHigh
NilotinibIntermediateTorsade de pointes, myelotoxicityHighImatinib
PazopanibIncompleteTorsade de pointes, myelotoxicityHighSorafenib
SunitinibNot knownTorsade de pointes, myelotoxicityHighSorafenib
VandetanibNot knownTorsade de pointes, myelotoxicityHigh
VenurafenibNot knownTorsade de pointes, myelotoxicityHigh
Anti-infective agents
ErythromycinIntermediateTorsade de pointesHighClarithromycin
HalofantrineLowTorsade de pointesVery highDoxycycline
MaravirocLowPostural hypotension, syncopeVery highEnfuvirtide
PrimaquineIntermediateMyelotoxicityHighDoxycycline
QuinineIntermediateTorsade de pointesHighDoxycycline
RilpivirineNot knownTorsade de pointesHighNevirapine
Antilipemic agents
AtorvastatinLowRhabdomyolysisHighPravastatin, rosuvastatin, fluvastatin
LovastatinVery lowRhabdomyolysisVery highPravastatin, rosuvastatin, fluvastatin
SimvastatinVery lowRhabdomyolysisVery highPravastatin, rosuvastatin, fluvastatin
Cardiovascular agents
AmiodaroneIntermediateTorsade de pointesHighSotalol
ApixabanIntermediateGI bleedingHighWarfarin
ClopidogrelVery lowLoss of efficacyHighAcetylsalicylic acid
DronedaroneLowTorsade de pointesVery highSotalol
EplerenoneIntermediateHyperkalemia, serious arrhythmiasHighSpironolactone
FelodipineLowHypotension, peripheral edemaIntermediateAmlodipine
NifedipineIntermediateHypotension, peripheral edemaIntermediateAmlodipine
QuinidineHighTorsade de pointesIntermediate
RivaroxabanHighGI bleedingIntermediateWarfarin
TicagrelorIntermediateGI or kidney bleedingHighAcetylsalicyclic acid
CNS agents
Alfentanil (oral)IntermediateRespiratory depressionHighHydromorphone, morphine
BuspironeVery lowDizziness, sedationHighOxazepam, tamazepam
DextromethorphanVery lowHallucinations, somnolenceHigh
Fentanyl (oral)IntermediateRespiratory depressionHighHydromorphone, morphine
Ketamine (oral)LowRespiratory depressionVery highHydromorphone, morphine
LurasidoneLowTorsade de pointes, orthostatic hypotension, syncopeVery highHaloperidol, risperidone olanzapine
OxycodoneIntermediateRespiratory depressionHighHydromorphone, morphine
PimozideIntermediateTorsade de pointesHighHaloperidol, risperidone, olanzapine
QuetiapineVery lowDizziness, somnolenceHighHaloperidol, risperidone, olanzapine
TriazolamIntermediateSedationIntermediateAlprazolam, lorazepam
ZiprasidoneIntermediateTorsade de pointesHighHaloperidol, risperidone olanzapine
Gastrointestinal agents
DomperidoneLowTorsade de pointesVery highMetoclopramide
Immunosuppressants
CyclosporineLowNephrotoxicityHigh
EverolimusLowMyelotoxicity, nephrotoxicityHigh
SirolimusLowMyelotoxicity, nephrotoxicityHigh
TacrolimusLowNephrotoxicityHigh
Urinary tract agents
DarifenacinLowUrinary retention, constipationIntermediate
FesoterodineIntermediateUrinary retention, constipationIntermediate
SolifenacinHighTorsade de pointesIntermediate
SilodosinIntermediatePostural hypotension, dizzinessIntermediate
TamsulosinIntermediatePostural hypotension, dizzinessIntermediate
  • Note: CNS = central nervous system, GI = gastrointestinal.

  • * Population average: very low < 10%, low >10%–30%, intermediate >30%–70%, high > 70%.

  • Based on the seriousness of the adverse effect and adjusted for the innate oral bioavailability of the drug, which is used to determine the potential increase in systemic drug concentration. For older patients, particularly the elderly, it is recommended that grapefruit or other citrus fruits be contraindicated for drugs in the very high or high category, or that a suggested alternative noninteracting drug be employed when available.

  • Commonly prescribed drugs (Top 100 prescribed in 2011 in Canada) with the same therapeutic indication that have no or minor pharmacokinetic interaction with grapefruit or other citrus fruits.