Drug & supplement interaction

Grapefruit + Pitavastatin

Pitavastatin brand names: Zypitamag, Nikita.

Major Interaction
Medically reviewed by · Updated September 2026
The bottom line Major

Pitavastatin falls into 3 drug categories that Grapefruit can interact with; the most serious is rated major. Grapefruit juice can increase blood levels of statins that are metabolized by cytochrome P450 3A4 (CYP3A4), potentially increasing the effects and adverse effects of these statins.

Read the full interaction report
SeverityMajor
LikelihoodLikely
Interactions3
EvidenceB
What do Severity, Likelihood & Evidence mean?
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Interaction report

Grapefruit and Pitavastatin

These two interact in 3 distinct ways. Each one is explained separately below.

Why Are There 3 Interactions?

Grapefruit interacts with whole categories of medication. Pitavastatin falls into 3 of those categories, so it can interact with Grapefruit in 3 different ways. We’ve listed each one below — your overall risk is driven by the most serious of them (Major).

Major

HMG-CoA REDUCTASE INHIBITORS ("Statins")

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Why this applies to Pitavastatin

Pitavastatin falls under HMG-CoA REDUCTASE INHIBITORS ("Statins") — the group Grapefruit interacts with.

Grapefruit juice can increase blood levels of statins that are metabolized by cytochrome P450 3A4 (CYP3A4), potentially increasing the effects and adverse effects of these statins. Additionally, grapefruit juice might interfere with the bioavailability of statins that are substrates of organic anion transporting polypeptides (OATP).
Clinical research shows that grapefruit juice inhibits metabolism and increases absorption and plasma concentrations of statins that are metabolized by CYP3A4. These include lovastatin, simvastatin, and atorvastatin. Keep in mind that there is considerable variability in the effect of grapefruit juice on drug metabolism, so individual patient response is difficult to predict.
Some statins, including pravastatin, fluvastatin, pitavastatin, and rosuvastatin, are not metabolized by CYP3A4. However, grapefruit juice might still affect the bioavailability of these statins. These statins are substrates of OATP. Grapefruit juice can inhibit OATP. Therefore, grapefruit juice may reduce the bioavailability or increase drug levels of these statins depending on the type of OATP. However, grapefruit juice affects OATP for only a short time. Therefore, separating drug administration by at least 4 hours is likely to avoid this interaction.
Severity Major Likelihood Likely Evidence B

Well-controlled human studies have demonstrated the likely existence of this interaction.

Dr. Brian Staiger, PharmD, BCPS
Dr. Brian Staiger explains PharmD, Clinical Pharmacist

Here's some good news if you enjoy grapefruit: pitavastatin (Zypitamag, Nikita) is one of the statins that does not rely much on the CYP3A4 enzyme that grapefruit famously blocks. So you won't see the big buildup that happens with simvastatin or atorvastatin.

That said, grapefruit can briefly affect a transporter called OATP that helps move pitavastatin into your system. This may nudge your drug levels up or down for a short while, though the effect is usually mild and short-lived. A simple fix is to space your grapefruit and your pitavastatin by at least 4 hours. If you eat grapefruit regularly, just mention it to your pharmacist or doctor so they can keep an eye on muscle aches or other statin side effects.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Kantola T, Kivisto KT, Neuvonen PJ, et al. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998 63:397-402. PubMed
  2. Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. Clin Pharmacol Ther 1999;66:118-27. DOI
  3. Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. Clin Pharmacol Ther 1998;64:477-83. PubMed
  4. Erlund I, Meririnne E, Alfthan G, Aro A. Plasma kinetics and urinary excretion of the flavanones naringenin and hesperetin in humans after ingestion of orange juice and grapefruit juice. J Nutr 2001;131:235-41. PubMed
  5. Bailey DG, Dresser GK. Grapefruit juice-lovastatin interaction. Clin Pharmacol Ther 2000;67:690.
  6. Lilja JJ, Kivisto KT, Neuvonen PJ. Duration of effect of grapefruit juice on the pharmacokinetics of the CYP3A4 substrate simvastatin. Clin Pharmacol Ther 2000;68:384-90. PubMed
  7. Rogers JD, Zhao J, Liu L, et al. Grapefruit juice has minimal effects on plasma concentrations of lovastatin-derived 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Clin Pharmacol Ther 1999;66:358-66. PubMed
  8. Fukazawa I, Uchida N, Uchida E, Yasuhara H. Effects of grapefruit juice on the pharmacokinetics of atorvastatin and pravastatin in Japanese. Br J Clin Pharmacol 2003;57:448-55.
  9. Potential drug interactions with grapefruit. Pharmacist's Letter / Prescriber's Letter 2007;23(2):230204.
  10. Ando, H., Tsuruoka, S., Yanagihara, H., Sugimoto, K., Miyata, M., Yamazoe, Y., Takamura, T., Kaneko, S., and Fujimura, A. Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin. Br J Clin Pharmacol 2005;60(5):494-497. DOI
  11. Lilja, J. J., Neuvonen, M., and Neuvonen, P. J. Effects of regular consumption of grapefruit juice on the pharmacokinetics of simvastatin. Br J Clin Pharmacol 2004;58(1):56-60. PubMed
  12. Hu M, Mak VW, Yin OQ, Chu TT, Tomlinson B. Effects of grapefruit juice and SLCO1B1 388A>G polymorphism on the pharmacokinetics of pitavastatin. Drug Metab Pharmacokinet. 2013;28(2):104-8.
Moderate

CYTOCHROME P450 2C9 (CYP2C9) SUBSTRATES

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Pitavastatin also falls under CYTOCHROME P450 2C9 (CYP2C9) SUBSTRATES.

Theoretically, grapefruit juice might increase levels of drugs metabolized by CYP2C9.
In vitro research suggests that grapefruit juice might inhibit CYP2C9 enzymes. So far, this interaction has not been reported in humans.
Severity Moderate Likelihood Possible Evidence D

Interaction has been documented in animal or in lab research, or the interaction has been documented in humans but is limited to case reports or conflicting clinical research exists.

Dr. Brian Staiger, PharmD, BCPS
Dr. Brian Staiger explains PharmD, Clinical Pharmacist

Here's the good news with pitavastatin (Zypitamag, Nikita): it's actually one of the few statins that mostly sidesteps the grapefruit problem. Unlike simvastatin or atorvastatin, pitavastatin isn't heavily processed by the enzyme grapefruit famously blocks, so it doesn't build up the same way most statins can.

The note on file here is theoretical. In test-tube studies, grapefruit juice may slow down a liver enzyme called CYP2C9, which could in theory nudge pitavastatin levels up a bit. But this has never actually been seen in real people. If it did happen, you might notice more typical statin side effects like muscle aches or soreness. I wouldn't lose sleep over an occasional grapefruit, but since you're on a statin, it's worth a quick mention to your pharmacist or doctor.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Unger M, Frank A. Simultaneous determination of the inhibitory potency of herbal extracts on the activity of six major cytochrome P450 enzymes using liquid chromatography/mass spectrometry and automated online extraction. Rapid Commun Mass Spectrom 2004;1 PubMed
Moderate

PITAVASTATIN (Livalo)

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Grapefruit juice can increase blood levels of pitavastatin, potentially increasing the effects and adverse effects of pitavastatin.
Pharmacokinetic research shows that taking grapefruit juice with pitavastatin 2-4 mg can increase blood levels of pitavastatin by 13% to 14%. Unlike simvastatin and atorvastatin, pitavastatin is not significantly metabolized by cytochrome P450 3A4 (CYP3A4) enzymes. Grapefruit juice appears to increase levels of pitavastatin by inhibiting its uptake by organic anion transporting polypeptide 1B1 (OATP1B1) into hepatocytes for metabolism and clearance from the body. Grapefruit juice seems to increase levels of pitavastatin to a greater degree in patients homozygous for a specific polymorphism (388A>G) in the OATP1B1 gene compared to those heterozygous for this polymorphism.
Severity Moderate Likelihood Likely Evidence B

Well-controlled human studies have demonstrated the likely existence of this interaction.

Dr. Brian Staiger, PharmD, BCPS
Dr. Brian Staiger explains PharmD, Clinical Pharmacist

Here's something nice about pitavastatin: it's one of the few statins that doesn't lean heavily on the CYP3A4 pathway, so grapefruit doesn't hit it nearly as hard as it does drugs like simvastatin or atorvastatin. What grapefruit does do is gently slow a liver transporter (OATP1B1) that helps move pitavastatin into the liver, so a little more stays in your bloodstream.

In studies, this bumped pitavastatin levels by roughly 13 to 14 percent, which is fairly modest. In theory, higher levels could mean a bit more muscle aching or soreness, but for most people this small change isn't a big deal. If you genuinely love your grapefruit, just mention it to your pharmacist or doctor so they can keep an eye on things rather than you stopping anything on your own.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Ando, H., Tsuruoka, S., Yanagihara, H., Sugimoto, K., Miyata, M., Yamazoe, Y., Takamura, T., Kaneko, S., and Fujimura, A. Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin. Br J Clin Pharmacol 2005;60(5):494-497. DOI
  2. Hu M, Mak VW, Yin OQ, Chu TT, Tomlinson B. Effects of grapefruit juice and SLCO1B1 388A>G polymorphism on the pharmacokinetics of pitavastatin. Drug Metab Pharmacokinet. 2013;28(2):104-8.

What These Ratings Mean

Every interaction above is graded three ways — here’s the key to each label.

Severity how clinically significant the interaction is
Major

Clinically significant. Avoid the combination, or use only under close professional supervision.

Moderate

Usually worth avoiding or managing — may need monitoring, a dose change, or timing apart.

Minor

Generally not serious. Be aware of it and mention it to your pharmacist.

Likelihood how strong the evidence is that the interaction actually happens in people
  • LikelyWell-controlled human studies have demonstrated the likely existence of this interaction.
  • ProbableInteraction has not been documented in well-controlled studies, however, the interaction has been demonstrated in some small human studies or in controlled animal studies in conjunction with multiple case reports.
  • PossibleInteraction has been documented in animal or in lab research, or the interaction has been documented in humans but is limited to case reports or conflicting clinical research exists.
  • UnlikelyInteraction has been demonstrated in animal or in lab research but has been shown not to occur in humans.
Evidence the quality of the studies behind the rating (graded A–D)
  • AHigh-quality meta-analysis (quantitative systematic review).
  • BCase-control study.
  • CConsensus.
  • DAnecdotal evidence.

These ratings are for information only. Never start, stop, or otherwise change your therapy before speaking with your provider.

Keep it in perspective

Grapefruit Also Interacts With Other Medications

Grapefruit has 775 major, 151 moderate, 63 minor known drug interactions in our database — the Pitavastatin one above is among them. If you take anything else, check it against the full list below.

Major 775 Moderate 151 Minor 63 No known interaction 1,841 (incl. Pitavastatin)
Taking anything else?

Check Another of Your Medications Against Grapefruit

Covers the 2,830 medications we’ve checked against Grapefruit. Pick one to open its full report.

From our Q&A

Questions About Grapefruit or Pitavastatin

These are real questions from readers, answered by the pharmacists at HelloPharmacist — written by a person, not generated from a database. Each one covers Grapefruit or Pitavastatin, not necessarily both, but if one is close to what you were about to ask it will usually go further than a database entry can:

Not quite your question? Ask our pharmacists directly — it is free, there is no account required, and answers usually come back within 24 hours.

Everything else you take

See Every Supplement That Interacts With Pitavastatin

This page covers Grapefruit only. If you take other supplements — a multivitamin, a sleep aid, something for joints — the Pitavastatin page lists 126 supplements it has a documented interaction with, worst first, each one explained.

The most serious there right now: Activated Charcoal (major), Beer (major), Siberian Cocklebur (major), Wine (major) and Adrafinil (moderate).

By severity: 5 major · 98 moderate · 23 minor.

From our pharmacist’s overview on the Pitavastatin page

“Liver strain runs through the serious end of pitavastatin's (Zypitamag, Nikita) supplement interactions, and this list deserves real care rather than a quick skim. The biggest cluster of worrisome entries is herbs and ingredients with their own record of liver injury, and alcohol belongs to that group too, with beer and wine both carry…”

Reviewed by 2 · Jul 18, 2026

Open the Pitavastatin interaction page

One more smart check

Taking Grapefruit as Part of a Dietary Supplement Product? Check It for Interactions

We hold 1,144 real supplement products containing Grapefruit, each one broken down to its full ingredient list — and combination products often carry several ingredients besides Grapefruit. Your product may carry other ingredients that interact with Pitavastatin too, on top of Grapefruit — and those would not show on this page. Find your product and we’ll check every ingredient on its label:

How much people look this up

Where Grapefruit and Pitavastatin Sit Against Everything Else

Out of every supplement and medication people look up on HelloPharmacist, here is where these two land this week — and which way each has been moving.

Supplement Grapefruit
Top 10%

#108 of 1,452 supplements looked up here in the last 7 days

29 days ago today
Medication Pitavastatin
Steady interest

#2,181 of 2,830 medications looked up here in the last 7 days

29 days ago today

Position among everything looked up on this site, not a measure of how commonly either one is used or how important it is. A supplement can climb this list because of a news story. It counts every request to the page, automated ones included, and nothing here identifies anyone.

Supplement

About Grapefruit

What is Grapefruit?

Grapefruit
  • Source of vitamin C
  • Digestive complaints
  • Antimicrobial (seed extract)
  • Weight management
  • Skin and cosmetic uses

Grapefruit is a nutritious citrus fruit rich in vitamin C and other nutrients, and it is generally safe to eat. However, grapefruit is famous for serious interactions with many prescription medicines, so anyone taking medication should check with a pharmacist or doctor before consuming it regularly.

Read the full Grapefruit monograph & all interactions
Medication

About Pitavastatin

What Is Pitavastatin Used For?

Brand names: Zypitamag, Nikita

Pitavastatin tablets are used alongside a cholesterol-lowering diet to reduce LDL-C (low-density lipoprotein, or "bad" cholesterol) in adults with primary hyperlipidemia (high cholesterol not caused by another disease).

Livalo, Pitavastatin Calcium (tablet), and some other pitavastatin tablet products are also approved for adults and children aged 8 years and older with heterozygous familial hypercholesterolemia (HeFH) — an inherited condition that causes very high LDL-C from birth. Zypitamag is labeled only for adults with primary hyperlipidemia; its labeling does not include the pediatric HeFH indication.

See full Pitavastatin drug information
Keep checking

Other Drugs & Grapefruit

Browse every other medication we’ve checked against Grapefruit — both the ones with a known interaction and the ones without. Select any drug for the full detail.

775Major
151Moderate
63Minor
1,840No known interaction
775 Major 151 Moderate 63 Minor 1,840 No interaction
Major

775 interactions

Showing 60 of 775 major interactions — see all 775 on the Grapefruit page.

Moderate

151 interactions

Showing 60 of 151 moderate interactions — see all 151 on the Grapefruit page.

Minor

63 interactions

Showing 60 of 63 minor interactions — see all 63 on the Grapefruit page.

No interaction 1,840 drugs checked — show the list

We also checked Grapefruit against these medications and found no known interaction in our sources. Open any page to confirm.

Showing the 60 most looked-up of 1,840 medications checked with no known interaction — see the full Grapefruit list.

See the full Grapefruit interactions page
See every supplement checked against Pitavastatin, ranked by severity
Sources

Sources & How We Checked

Interaction details are evidence-graded and sourced from the Natural Medicines database. The medication overview comes from MedlinePlus.

Content is written and reviewed by licensed HelloPharmacist pharmacists. See our data sources and editorial standards for how this information is built and checked.

Parts of this content are provided by the Therapeutic Research Center, LLC.

DISCLAIMER: Currently this does not check for drug-drug interactions. This is not an all-inclusive comprehensive list of potential interactions and is for informational purposes only. Not all interactions are known or well-reported in the scientific literature, and new interactions are continually being reported. Input is needed from a qualified healthcare provider including a pharmacist before starting any therapy. Application of clinical judgment is necessary.

© 2021 Therapeutic Research Center, LLC

Keep exploring
Grapefruit monograph › Uses, safety, and every drug interaction in one place Pitavastatin supplement interactions › Every supplement checked against Pitavastatin, ranked by severity Pitavastatin drug information › The full plain-English guide to this medication Supplement interaction checker › Check any supplement or product against your medications Browse medications A–Z › Every drug we've checked against herbs & supplements Ask a pharmacist › Free, personal answer from our licensed team
Pharmacist Counseling Corner

Taking Grapefruit and Pitavastatin Together: Common Questions

Can you take Grapefruit with Pitavastatin?
This is rated a major interaction, so the combination is best avoided unless your doctor or pharmacist has specifically told you otherwise. Read the full details on this page and confirm with your pharmacist before combining them.
Why are there 3 interactions listed for Grapefruit and Pitavastatin?
Pitavastatin belongs to more than one drug category, and Grapefruit interacts with each of those categories a little differently. We list every one so nothing is missed — your overall risk is driven by the most serious of them.
How serious is the Grapefruit and Pitavastatin interaction?
We rate it Major. This is a clinically significant combination that is generally best avoided, or used only under the direct supervision of your physician or pharmacist.

Written and reviewed by the HelloPharmacist editorial staff. Our editorial policy

Still Have a Question About Pitavastatin and Grapefruit?

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This information is for education only and is not a substitute for professional medical advice. Always check with your pharmacist or doctor before starting, stopping, or combining supplements and medications.