Phase 1 trial maps CBD drug interactions with three common epilepsy medications

CBD had little effect on clobazam itself but tripled its active metabolite levels, slightly increased stiripentol exposure, and had no clinically relevant effect on valproate.

Morrison, Gilmour et al.·Clinical pharmacology in drug development·2019·Strong EvidenceRandomized Controlled Trial
RTHC-02195Randomized Controlled TrialStrong Evidence2019RETHINKTHC RESEARCH DATABASErethinkthc.com/research

Quick Facts

Study Type
Randomized Controlled Trial
Evidence
Strong Evidence
Sample
Not reported

What This Study Found

CBD increased N-desmethylclobazam (active clobazam metabolite) 3.4-fold for both Cmax and AUC. Stiripentol exposure increased modestly (Cmax 1.3-fold, AUC 1.6-fold). No clinically relevant effect on valproate. Clobazam increased 7-OH-CBD levels 1.5-1.7-fold. Stiripentol slightly decreased CBD metabolite levels. CBD was moderately well tolerated with all three AEDs.

Key Numbers

N-desmethylclobazam: Cmax and AUC 3.4-fold increase. Clobazam: 1.2-fold increase. Stiripentol: Cmax 1.3-fold, AUC 1.6-fold. Valproate: no relevant change. 7-OH-CBD with clobazam: Cmax 1.7-fold, AUC 1.5-fold.

How They Did This

Phase 1, open-label, fixed-sequence drug-drug interaction study in healthy volunteers, examining bidirectional pharmacokinetic interactions between pharmaceutical CBD (Epidiolex) and clobazam, stiripentol, and valproate at steady state.

Why This Research Matters

These three AEDs are among the most commonly co-prescribed with CBD for Lennox-Gastaut and Dravet syndromes. Knowing that CBD triples the active clobazam metabolite is clinically actionable: clobazam doses may need reduction when adding CBD.

The Bigger Picture

The somnolence commonly attributed to CBD in epilepsy may partly be caused by the 3.4-fold increase in the active clobazam metabolite. Understanding these interactions allows dose adjustments that could improve tolerability.

What This Study Doesn't Tell Us

Healthy volunteers, not epilepsy patients. Single-dose escalation design. Cannot assess whether interactions change with chronic dosing or in patients with hepatic impairment.

Questions This Raises

  • ?Should clobazam doses be routinely reduced when CBD is added?
  • ?Do these pharmacokinetic interactions translate to meaningful clinical differences in seizure control?

Trust & Context

Key Stat:
3.4-fold clobazam metabolite increase
Evidence Grade:
Strong: well-designed Phase 1 PK study from the Epidiolex manufacturer with bidirectional interaction data.
Study Age:
Published in 2019.
Original Title:
A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate Possible Drug-Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects.
Published In:
Clinical pharmacology in drug development, 8(8), 1009-1031 (2019)
Database ID:
RTHC-02195

Evidence Hierarchy

Meta-Analysis / Systematic Review
Randomized Controlled TrialGold standard for testing treatments
This study
Cohort / Case-Control
Cross-Sectional / Observational
Case Report / Animal Study

Participants are randomly assigned to treatment or placebo groups to test cause and effect.

What do these levels mean? →

Frequently Asked Questions

Does CBD interact with clobazam?

Yes, CBD tripled blood levels of clobazam's active metabolite (N-desmethylclobazam), which may increase side effects like sedation. Clobazam dose reduction may be needed when adding CBD.

Is it safe to take CBD with valproate?

This study found no clinically relevant pharmacokinetic interaction between CBD and valproate, suggesting the combination is likely safe from an interaction standpoint.

Read More on RethinkTHC

Cite This Study

RTHC-02195·https://rethinkthc.com/research/RTHC-02195

APA

Morrison, Gilmour; Crockett, Julie; Blakey, Graham; Sommerville, Kenneth. (2019). A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate Possible Drug-Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects.. Clinical pharmacology in drug development, 8(8), 1009-1031. https://doi.org/10.1002/cpdd.665

MLA

Morrison, Gilmour, et al. "A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate Possible Drug-Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects.." Clinical pharmacology in drug development, 2019. https://doi.org/10.1002/cpdd.665

RethinkTHC

RethinkTHC Research Database. "A Phase 1, Open-Label, Pharmacokinetic Trial to Investigate ..." RTHC-02195. Retrieved from https://rethinkthc.com/research/morrison-2019-a-phase-1-openlabel

Access the Original Study

Study data sourced from PubMed, a service of the U.S. National Library of Medicine, National Institutes of Health.

This study breakdown was produced by the RethinkTHC research team. We analyze and report published research findings without making health recommendations. All interpretations are based solely on the published abstract and study data.