Drug & supplement interaction

Grapefruit + Guaifenesin, Theophylline

Guaifenesin, Theophylline brand names: Mudrane GG-2, Bronchial, Theolair-Plus, Quibron, Quibron-300.

Moderate Interaction
The bottom line Moderate

Guaifenesin, 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 Guaifenesin, 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. Guaifenesin, 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 Guaifenesin, Theophylline

Guaifenesin, 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

This combo product pairs guaifenesin (a simple expectorant that thins mucus) with theophylline, which is the one to watch here. Theophylline opens the airways but has a narrow safety window, meaning the gap between a helpful dose and a toxic one is small. Lab studies suggest grapefruit may block the CYP1A2 enzyme that breaks theophylline down, so in theory the drug could build up in your body.

If that happened, you might notice nausea, a racing or pounding heart, restlessness, shaking, or trouble sleeping. The good news: this has only been seen in test-tube research, not in real people. Still, because theophylline is finicky, it is worth mentioning grapefruit to your pharmacist or doctor before making it a daily habit.

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

Guaifenesin, Theophylline also falls under THEOPHYLLINE.

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

This combination product pairs guaifenesin (an expectorant that loosens mucus) with theophylline, a breathing medicine used for asthma and COPD. The interaction here is really about the theophylline part. Studies show that drinking grapefruit juice can modestly lower your theophylline blood levels, and lower levels can mean it simply doesn't work as well. The exact reason isn't fully understood.

Why does this matter? Theophylline is a tricky drug with a narrow safe range, so changes in its level can tip things either direction. If levels drop, you might notice more wheezing, coughing, or shortness of breath. Don't stop your grapefruit or your medicine on your own. Just mention your grapefruit habit to your pharmacist or doctor so they can keep an eye on things.

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 776 major, 150 moderate, 63 minor known drug interactions in our database — the Guaifenesin, Theophylline one above is among them. If you take anything else, check it against the full list below.

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 Guaifenesin, 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 Guaifenesin, 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 Guaifenesin, Theophylline

This page covers Grapefruit only. If you take other supplements — a multivitamin, a sleep aid, something for joints — the Guaifenesin, 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.

Open the Guaifenesin, 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 Guaifenesin, 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 Guaifenesin, 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%

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

29 days ago today
Medication Guaifenesin, Theophylline
Steady interest

#2,384 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
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.

776Major
150Moderate
63Minor
1,840No known interaction
Major

776 interactions

Showing 60 of 776 major interactions — see all 776 on the Grapefruit page.

Moderate

150 interactions

Showing 60 of 150 moderate interactions — see all 150 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
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

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Pharmacist Counseling Corner

Taking Grapefruit and Guaifenesin, Theophylline Together: Common Questions

Can you take Grapefruit with Guaifenesin, 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 Guaifenesin, Theophylline?
Guaifenesin, 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 Guaifenesin, 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

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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.