Drug & supplement interaction

Grapefruit + Theophylline

Theophylline brand names: T-Phyl, Duraphyl, Aerolate JR, Aerolate SR, Theo-Dur, and others.

Moderate Interaction
Medically reviewed by · Updated October 2026
The bottom line Moderate

Theophylline falls into 2 drug categories that Grapefruit can interact with; the most serious is rated moderate. Theoretically, grapefruit juice might increase levels of drugs metabolized by CYP1A2.

Read the full interaction report
SeverityModerate
LikelihoodPossible
Interactions2
EvidenceD
What do Severity, Likelihood & Evidence mean?
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Interaction report

Grapefruit and Theophylline

These two interact in 2 distinct ways. Each one is explained separately below.

Why Are There 2 Interactions?

Grapefruit interacts with whole categories of medication. Theophylline falls into 2 of those categories, so it can interact with Grapefruit in 2 different ways. We’ve listed each one below — your overall risk is driven by the most serious of them (Moderate).

Moderate

CYTOCHROME P450 1A2 (CYP1A2) SUBSTRATES

1 of 2

Why this applies to Theophylline

Theophylline falls under CYTOCHROME P450 1A2 (CYP1A2) SUBSTRATES — the group Grapefruit interacts with.

Theoretically, grapefruit juice might increase levels of drugs metabolized by CYP1A2.
In vitro research suggests that grapefruit juice might inhibit CYP1A2 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 short version for theophylline: your body clears this medicine mainly through a liver enzyme called CYP1A2. In test-tube studies, compounds in grapefruit seem to slow that enzyme down a bit. In theory, that could let theophylline build up a little higher than expected, which matters because theophylline has a narrow safe range. Too much can cause nausea, a racing or pounding heartbeat, jitteriness, trouble sleeping, or in larger excesses, tremors.

The reassuring part is that this is only lab-based so far, and it has not actually been reported in people. So I wouldn't panic over an occasional half grapefruit. Still, because theophylline is a touchy drug, it's worth a quick chat with your pharmacist or doctor before making grapefruit a daily habit.

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

THEOPHYLLINE

2 of 2
Grapefruit juice can decrease blood levels of theophylline, potentially decreasing the effectiveness of theophylline.
Clinical research shows that grapefruit juice seems to modestly decrease theophylline levels when given concurrently with sustained-release theophylline. The mechanism of this interaction is unknown.
Severity Moderate Likelihood Probable Evidence B

Interaction 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..

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

Here's the gist for theophylline. Some studies suggest that drinking grapefruit juice can nudge your theophylline blood levels down a bit. Theophylline isn't a prodrug, so this isn't about activating it. Lower levels simply mean there may be less drug doing its job, which could let asthma or COPD symptoms like wheezing, coughing, or chest tightness creep back in.

Now, theophylline is a tricky medicine with a narrow safety window, so even modest changes are worth taking seriously. The evidence here is moderate and the effect seems small, so don't panic. Just be consistent, and chat with your pharmacist or doctor before adding regular grapefruit so they can keep an eye on your levels.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Gupta MC, Garg SK, Badyal D, et al. Effect of grapefruit juice on the pharmacokinetics of theophylline in healthy male volunteers. Methods Find Exp Clin Pharmacol 1999;21:679-82. PubMed

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 778 major, 150 moderate, 62 minor known drug interactions in our database — the Theophylline one above is among them. If you take anything else, check it against the full list below.

Major 778 Moderate 150 Minor 62 No known interaction 1,840 (incl. Theophylline)
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 Theophylline

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 Theophylline, 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 Theophylline

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

The most serious there right now: Activated Charcoal (major), Ephedra (major), Sida Cordifolia (major), Adrafinil (moderate) and African Wild Potato (moderate).

By severity: 3 major · 89 moderate · 34 minor.

From our pharmacist’s overview on the Theophylline page

“Stop ephedra before anything else if you take theophylline (Theo-Dur, Slo-Bid, and others) for asthma or COPD. Both are stimulants, and together they raise the risk of serious heart and nervous system effects; Sida cordifolia, an herb that contains ephedrine, carries the same major rating.”

Reviewed by 2 · Jul 18, 2026

Open the Theophylline 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 Theophylline 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 Theophylline 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 Theophylline
Steady interest

#1,980 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 Theophylline

What Is Theophylline Used For?

Brand names: T-Phyl, Duraphyl, Aerolate JR, Aerolate SR, Theo-Dur, Slo-Bid, Theo-24, Uniphyl, Slo-phyllin Gyrocaps, Theolair, Theolair SR, Quibron-T/SR, Quibron-T, Aerolate III, Theo-X, Bronkodyl, Theoclear LA-130, Constant-T, Theoclear LA-260, Elixophyllin, Theovent, Theobid Jr Duracap, Respbid, Theobid Duracap

Theophylline — available as extended-release capsules (Theo-24), extended-release tablets, and oral solution (Elixophyllin) — is used to treat symptoms and reversible airflow obstruction caused by chronic asthma, emphysema, and chronic bronchitis.

All supported formulations share these indications. Theophylline is intended for patients with ongoing or recurring symptoms, not for sudden (acute) breathing attacks, which need faster-acting treatments.

See full Theophylline 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.

778Major
150Moderate
62Minor
1,839No known interaction
778 Major 150 Moderate 62 Minor 1,839 No interaction
Major

778 interactions

Showing 60 of 778 major interactions — see all 778 on the Grapefruit page.

Moderate

150 interactions

Showing 60 of 150 moderate interactions — see all 150 on the Grapefruit page.

Minor

62 interactions

Showing 60 of 62 minor interactions — see all 62 on the Grapefruit page.

No interaction 1,839 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 1,839 medications checked with no known interaction — see the full Grapefruit list.

See the full Grapefruit interactions page
See every supplement checked against Theophylline, 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 Theophylline supplement interactions › Every supplement checked against Theophylline, ranked by severity Theophylline 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 Theophylline Together: Common Questions

Can you take Grapefruit with Theophylline?
There is a moderate interaction, so it may be acceptable with monitoring or timing changes — but check with your pharmacist first. Read the full details on this page and confirm with your pharmacist before combining them.
Why are there 2 interactions listed for Grapefruit and Theophylline?
Theophylline 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 Theophylline interaction?
We rate it Moderate. This combination may require monitoring, a dose adjustment, or separating the times you take each one. Consult your pharmacist before using them together.

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

Still Have a Question About Theophylline 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.