Drug & supplement interaction

Valerian + Brexpiprazole

Brexpiprazole brand name: Rexulti.

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

Brexpiprazole falls into 2 drug categories that Valerian can interact with; the most serious is rated minor. Valerian does not seem to have a clinically relevant effect on levels of drugs metabolized by CYP2D6.

Read the full interaction report
SeverityMinor
LikelihoodUnlikely
Interactions2
EvidenceB
What do Severity, Likelihood & Evidence mean?
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Interaction report

Valerian and Brexpiprazole

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

Why Are There 2 Interactions?

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

Minor

CYTOCHROME P450 2D6 (CYP2D6) SUBSTRATES

1 of 2

Why this applies to Brexpiprazole

Brexpiprazole falls under CYTOCHROME P450 2D6 (CYP2D6) SUBSTRATES — the group Valerian interacts with.

Valerian does not seem to have a clinically relevant effect on levels of drugs metabolized by CYP2D6.
Although some in vitro evidence suggests that valerian affects CYP2D6, clinical pharmacokinetic (PK) studies show that valerian is unlikely to affect the CYP2D6 enzyme. In one PK study, taking valerian 1000 mg (providing about 11 mg valerenic acid) nightly for 14 days did not affect the metabolism of dextromethorphan, a CYP2D6 substrate. In another PK study, taking valerian 125 mg three times daily for 28 days did not affect metabolism of debrisoquine, an accepted CYP2D6 probe-substrate.
Severity Minor Likelihood Unlikely Evidence B

Interaction has been demonstrated in animal or in lab research but has been shown not to occur in humans..

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

Here's the good news if you're taking Rexulti (brexpiprazole) and thinking about valerian for sleep: the concern on paper is that valerian might slow down an enzyme called CYP2D6, which is one of the main routes your body uses to clear brexpiprazole. In theory, blocking that pathway could let the drug build up and increase side effects like drowsiness, dizziness, restlessness, or weight changes.

But the actual human studies don't back that up. When researchers gave people valerian and tracked CYP2D6 activity, they saw no meaningful change. So while a lab test once hinted at an effect, real-world data says it's unlikely to matter. Both products can make you sleepy, though, so go easy on the combo at first and check in with your pharmacist or doctor before starting valerian.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Donovan JL, DeVane CL, Chavin KD, et al. Multiple night-time doses of valerian (Valeriana officinalis) had minimal effects on CYP3A4 activity and no effect on CYP2D6 activity in healthy volunteers. Drug Metab Dispos 2004;32:1333-6. PubMed
  2. Gurley BJ, Gardner SF, Hubbard MA, et al. In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes. Clin Pharmacol Ther 2005;77:415-26. PubMed
  3. Hellum BH, Nilsen OG. The in vitro inhibitory potential of trade herbal products on human CYP2D6-mediated metabolism and the influence of ethanol. Basic Clin Pharmacol Toxicol. 2007 Nov;101:350-8.
  4. Hellum BH, Hu Z, Nilsen OG. The induction of CYP1A2, CYP2D6 and CYP3A4 by six trade herbal products in cultured primary human hepatocytes. Basic Clin Pharmacol Toxicol. 2007 Jan;100:23-30. PubMed
Minor

CYTOCHROME P450 3A4 (CYP3A4) SUBSTRATES

2 of 2

Brexpiprazole also falls under CYTOCHROME P450 3A4 (CYP3A4) SUBSTRATES.

Valerian does not seem to have a clinically relevant effect on levels of drugs metabolized by CYP3A4.
Although some in vitro evidence suggests that valerian extract might inhibit or induce CYP3A4, clinical pharmacokinetic (PK) studies show that valerian does not have a clinically significant effect on the CYP3A4 enzyme. In one PK study, taking valerian 125 mg three times daily for 28 days did not affect metabolism of midazolam, an accepted CYP3A4 probe-substrate. In another PK study, taking valerian 1000 mg (providing about 11 mg valerenic acid) nightly for 14 days modestly increases levels of alprazolam, a CYP3A4 substrate, suggesting mild inhibition of CYP3A4. However, this mild inhibition is unlikely to be clinically relevant.
Severity Minor Likelihood Possible Evidence B

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 on combining valerian with Rexulti (brexpiprazole): the metabolism side of this pairing looks pretty quiet. Brexpiprazole is partly cleared by an enzyme called CYP3A4, and while a few lab tests hinted that valerian might slow that enzyme down, real-world studies in people did not find a meaningful effect. So valerian is unlikely to cause brexpiprazole to build up to worrisome levels.

The more practical thing to keep in mind is that both can be calming. Valerian is a mild sedative, and brexpiprazole can already make some people drowsy. Together you might feel a bit more tired or foggy. That's not dangerous for most folks, but it's worth running past your pharmacist or doctor before you start, especially when you're driving.

Contact Dr. Brian directly if you have additional questions on this interaction
References
  1. Budzinski JW, Foster BC, Vandenhoek S, Arnason JT. An in vitro evaluation of human cytochrome P450 3A4 inhibition by selected commercial herbal extracts and tinctures. Phytomedicine 2000;7:273-82. PubMed
  2. Lefebvre T, Foster BC, Drouin CE, et al. In vitro activity of commercial valerian root extracts against human cytochrome P450 3A4. J Pharm Pharmaceut Sci 2004;7:265-73.
  3. Donovan JL, DeVane CL, Chavin KD, et al. Multiple night-time doses of valerian (Valeriana officinalis) had minimal effects on CYP3A4 activity and no effect on CYP2D6 activity in healthy volunteers. Drug Metab Dispos 2004;32:1333-6. PubMed
  4. Gurley BJ, Gardner SF, Hubbard MA, et al. In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes. Clin Pharmacol Ther 2005;77:415-26. PubMed
  5. Hellum BH, Hu Z, Nilsen OG. The induction of CYP1A2, CYP2D6 and CYP3A4 by six trade herbal products in cultured primary human hepatocytes. Basic Clin Pharmacol Toxicol. 2007 Jan;100:23-30. 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

Valerian Also Interacts With Other Medications

Valerian has 338 moderate, 563 minor known drug interactions in our database — the Brexpiprazole one above is among them. If you take anything else, check it against the full list below.

Moderate 338 Minor 563 No known interaction 1,929 (incl. Brexpiprazole)
Taking anything else?

Check Another of Your Medications Against Valerian

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

From our Q&A

Questions About Valerian or Brexpiprazole

These are real questions from readers, answered by the pharmacists at HelloPharmacist — written by a person, not generated from a database. Each one covers Valerian or Brexpiprazole, 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 Brexpiprazole

This page covers Valerian only. If you take other supplements — a multivitamin, a sleep aid, something for joints — the Brexpiprazole page lists 177 supplements it has a documented interaction with, worst first, each one explained.

The most serious there right now: Activated Charcoal (major), Grapefruit (major), Indian Snakeroot (major), Lithium (major) and Rauvolfia Vomitoria (major).

By severity: 6 major · 130 moderate · 41 minor.

From our pharmacist’s overview on the Brexpiprazole page

“Brexpiprazole (Rexulti) treats schizophrenia and is added to antidepressants for depression, and its supplement list warrants real care before you add anything to it. The bulk of the 177 entries change how your liver clears the drug, so grapefruit can push levels up while St.”

Reviewed by 2 · Jul 18, 2026

Open the Brexpiprazole interaction page

One more smart check

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

We hold 2,185 real supplement products containing Valerian, each one broken down to its full ingredient list — and combination products often carry several ingredients besides Valerian. Your product may carry other ingredients that interact with Brexpiprazole too, on top of Valerian — 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 Valerian and Brexpiprazole 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 Valerian
Top 10%

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

29 days ago today
Medication Brexpiprazole
Steady interest

#1,818 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 Valerian

What is Valerian?

Valerian
  • Insomnia and poor sleep
  • Anxiety and stress
  • Restlessness
  • Muscle tension or cramps
  • Menstrual discomfort

Valerian is an herb whose root is widely used as a natural sleep aid and for calming nerves. The evidence is mixed and often weak, so it may help some people sleep but does not work reliably for everyone. It is generally well tolerated for short-term use, but talk to your pharmacist or doctor before starting it.

Read the full Valerian monograph & all interactions
Medication

About Brexpiprazole

What Is Brexpiprazole Used For?

Brand name: Rexulti

Brexpiprazole tablets are approved for two uses in adults: as an add-on (adjunctive) treatment alongside antidepressants for major depressive disorder (MDD), and as a treatment for schizophrenia. These uses apply to both the generic brexpiprazole tablets and Rexulti.

Rexulti has one additional approved use: treating agitation associated with dementia due to Alzheimer's disease in adults. Rexulti is also approved for schizophrenia in adolescents ages 13 and older. Note that Rexulti is not approved for dementia-related psychosis without agitation from Alzheimer's disease, and it is not meant to be used on an as-needed basis for Alzheimer's-related agitation.

See full Brexpiprazole drug information
Keep checking

Other Drugs & Valerian

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

0Major
338Moderate
563Minor
1,928No known interaction
338 Moderate 563 Minor 1,928 No interaction
Moderate

338 interactions

Showing 60 of 338 moderate interactions — see all 338 on the Valerian page.

Minor

563 interactions

Showing 60 of 563 minor interactions — see all 563 on the Valerian page.

No interaction 1,928 drugs checked — show the list

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

Showing the 60 most looked-up of 1,928 medications checked with no known interaction — see the full Valerian list.

See the full Valerian interactions page
See every supplement checked against Brexpiprazole, 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
Valerian monograph › Uses, safety, and every drug interaction in one place Brexpiprazole supplement interactions › Every supplement checked against Brexpiprazole, ranked by severity Brexpiprazole 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 Valerian and Brexpiprazole Together: Common Questions

Can you take Valerian with Brexpiprazole?
There is only a minor interaction, which is usually not serious. Read the full details on this page and confirm with your pharmacist before combining them.
Why are there 2 interactions listed for Valerian and Brexpiprazole?
Brexpiprazole belongs to more than one drug category, and Valerian 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 Valerian and Brexpiprazole interaction?
We rate it Minor. This interaction is generally not clinically significant, but it remains worth noting and discussing with your pharmacist.

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

Still Have a Question About Brexpiprazole and Valerian?

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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.