EpilepsyRx

Cannabidiol

Epidiolex

DailyMed-verified antiseizure indications

Indication / use

Label / evidence summary
Epidiolex: seizures associated with Lennox-Gastaut syndrome, Dravet syndrome, or tuberous sclerosis syndrome from age 1 year.
Role
Maintenance
Class
Human antiseizure mechanism unresolved; proposed non-CB1/CB2 pathways

Indications checked 26 September 2026. Product, route, age, and treatment-role limits apply. A DailyMed listing alone does not establish FDA approval.

Formulations & strengths

U.S. products unless another country is named. Strengths are per unit or stated volume.

Brand & formulation labels

Each link names the product and formulation it covers. Archived labels do not establish current availability.

Dosing & administration

Adult / product-specific schedule
LGS/Dravet syndrome: 2.5 mg/kg twice daily for 1 week → 5 mg/kg twice daily; if needed, maximum 10 mg/kg twice daily. TSC: 2.5 mg/kg twice daily, increase weekly by 2.5 mg/kg twice daily to recommended 12.5 mg/kg twice daily (25 mg/kg/day).
Pediatric
Age ≥1 year: same syndrome-specific weight-based schedule. TSC maintenance differs from LGS/Dravet syndrome. Adjust for moderate/severe hepatic impairment.
Titration / repeat dosing
Use the syndrome-specific schedule above; measure the 100 mg/mL solution with a calibrated oral syringe.

Practical administration

Product instructions
EPIDIOLEX is 100 mg/mL. Give consistently with respect to meals because food substantially changes exposure. Measure with the supplied syringe. Use the product instructions for compatible feeding tubes and flushing.

Dose adjustment & concentrations

Renal impairment
No labeled dose adjustment.
Hepatic impairment
Reduced starting, titration, and maintenance doses in moderate/severe impairment.
Serum reference information
No established therapeutic range

Safety

Boxed warning
No boxed warning.
Contraindications
Hypersensitivity to cannabidiol or ingredients (including sesame seed oil).
Serious precautions & monitoring
ALT/AST/bilirubin before starting, at 1, 3 and 6 months and periodically thereafter; recheck within 1 month of dose changes or changes in hepatotoxic co-medications. More frequent monitoring with valproate or abnormal baseline tests. Sedation, appetite/weight loss and diarrhea.

Common / selected adverse effects

  • Somnolence
  • Decreased appetite
  • Diarrhea
  • Transaminase elevation
  • Fatigue/malaise
  • Insomnia/sleep disorder

Drug interactions: toxicity & clinical action

Partner / combinationClinical effectClinical action
ClobazamInhibits clearance of active N-desmethylclobazam; sedation and other benzodiazepine adverse effects increase.Consider reducing clobazam if adverse effects occur; use levels when clinically helpful.
Valproate (especially with clobazam)Greater transaminase/hepatic-injury risk; not simply an increase in valproate concentration.Obtain and follow ALT/AST/bilirubin per label; consider reducing/stopping the contributing drug if liver tests rise.
Everolimus / CYP and UGT substratesCan increase everolimus and selected substrate exposure, causing toxicity.Review the exact substrate and label; monitor everolimus troughs and adjust dose.
Strong CYP3A4/CYP2C19 inducers / other sedativesInducers lower cannabidiol exposure; sedatives add impairment.Review effectiveness and adjust within labeled limits; monitor sedation.

Pregnancy & contraception

Fetal / neonatal risk
Human data are inadequate to define cannabidiol pregnancy risk. Animal studies found developmental toxicity, including embryofetal loss and impaired growth, at exposures similar to or greater than therapeutic exposure.
Pregnancy / postpartum monitoring
Epidiolex has a product-specific pregnancy surveillance program in addition to the North American ASM pregnancy registry.

Clinical evidence

Research summaries describe studied populations and outcomes; they do not add indications or constitute treatment recommendations.

Direct pivotal trial

Trial summary

Study design / duration
Randomized, double-blind, placebo-controlled trials in Lennox-Gastaut syndrome, Dravet syndrome, and TSC; 4-week baseline followed by approximately 14–16 weeks of treatment; syndrome-specific countable-seizure frequency was primary.
Primary endpoint
No single pivotal endpoint is identified in the cited source.
Results
Lennox-Gastaut syndrome trials: median drop-seizure reductions were approximately 37–44% with cannabidiol versus 17–22% with placebo. Dravet syndrome trial: convulsive seizures fell 39% versus 13%. TSC trial: seizure reduction was 48% versus 24%.

Trial publications

Mechanism of action

  • The FDA label states that the human anticonvulsant mechanism is unknown and does not appear to be mediated through cannabinoid receptors; cannabidiol should not be portrayed as a THC-like CB1 agonist.
  • GPR55-related signaling is one proposed pathway supported by experiments in a Dravet syndrome mouse model. Its contribution to clinical benefit remains unproven; other proposed molecular targets likewise require clinical validation.

Pharmacology

Adult values unless specified. Vd/F denotes apparent oral distribution volume.

Pharmacokinetics

Bioavailability
Absolute oral bioavailability is not specified in the U.S. label. Food substantially increases exposure; give consistently in relation to meals.
Elimination half-life
56–61 hours terminal half-life after twice-daily dosing for 7 days in healthy adults. A primary study estimated an effective accumulation half-life of 10–17 hours; these are different measures.
Volume of distribution
Apparent oral Vz/F: 20,963–42,849 L in healthy subjects. This is an apparent oral parameter strongly influenced by bioavailability, not a physical body-fluid volume.
Active metabolite(s)
7-OH-CBD is active. The current U.S. label also reports anticonvulsant activity of 7-COOH-CBD in one of two mouse models; its contribution in human epilepsy is unknown.
Active-metabolite half-life
7-OH-CBD: mean terminal values 24.7 and 31.7 hours after 750 and 1,500 mg CBD twice daily for 7 days in healthy adults. 7-COOH-CBD: 21.3 and 22.0 hours in the same study; its human antiseizure contribution is unestablished.
Protein binding
>94%
Metabolism / elimination
CYP2C19/CYP3A4 and UGT1A7/1A9/2B7

Metabolite values are study-specific healthy-adult estimates, not established pediatric constants. Terminal half-life alone does not determine the dosing interval.

Molecular structure

Molecular structure of Cannabidiol
Principal compound; salt and product forms may differ.
NIH PubChem structure and record ↗

Product history

Initial U.S. approval
2018
Brands
Epidiolex
Manufacturer / marketer
Jazz Pharmaceuticals (Epidiolex)
Generic availability
No
Related drugs
Purified pharmaceutical cannabidiol; not equivalent to nonprescription cannabis/CBD products.

Sources & review status

Indications and DailyMed PDFs checked: 2026-09-26. Other profile sources reviewed: 2026-09-15 · label revision noted at that review: 5/2026. This is a draft reference; final review is pending.