Pronunciation:
kan-a-bi-dye-ol
Trade Name(s)
Ther. Class.
Pharm. Class.
cannabinoids
Controlled Substance Schedule: V
Seizures associated with Lennox-Gastaut syndrome, Dravet syndrome, or tuberous sclerosis complex.
Cannabidiol is a cannabinoid that naturally occurs in the Cannabis sativa plant. Mechanism of anticonvulsant effect unknown; does not work by interacting with cannabinoid receptors.
Therapeutic Effect(s):
Reduction in frequency of atonic, tonic, clonic, and tonic-clonic seizures.
Absorption: Extent of absorption unknown. High fat/high calorie meals increase extent of absorption.
Distribution: Extensively distributed to tissues.
Protein Binding: >94%.
Metabolism and Excretion: Primarily metabolized in the liver by the CYP2C9 and CYP3A4 isoenzymes to an active metabolite (7-OH-CBD). Primarily excreted in feces.
Half-life: 56–61 hr.
TIME/ACTION PROFILE (plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | unknown | 2.5–5 hr | unknown |
Contraindicated in:
Use Cautiously in:
Derm: rash
EENT: dry mouth
GI: ↓ appetite, ↑ liver enzymes, diarrhea, ↓ weight, abdominal pain, hepatotoxicity
GU: ↑ serum creatinine
Hemat: anemia
Neuro: fatigue, insomnia, sedation, aggressive behavior, agitation, ataxia, SUICIDAL THOUGHTS/BEHAVIORS
Misc: HYPERSENSITIVITY REACTIONS (including angioedema), infection, physical dependence, psychological dependence (high doses or prolonged therapy)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Drug-Drug
Seizures Associated with Lennox-Gastaut Syndrome or Dravet Syndrome
PO (Adults and Children ≥1 yr): 2.5 mg/kg twice daily; can ↑ dose to 5 mg/kg twice daily in 1 wk. If further reduction in seizure frequency needed, may continue to ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 2.5 mg/kg twice daily (max dose = 10 mg/kg twice daily).
Hepatic Impairment
PO (Adults and Children ≥1 yr): Moderate hepatic impairment (Child–Pugh B): 1.25 mg/kg twice daily; can ↑ dose to 2.5 mg/kg twice daily in 1 wk. If further reduction in seizure frequency needed, may continue to ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 1.25 mg/kg twice daily (max dose = 5 mg/kg twice daily); Severe hepatic impairment (Child–Pugh C): 0.5 mg/kg twice daily; can ↑ dose to 1 mg/kg twice daily in 1 wk. If further reduction in seizure frequency needed, may continue to ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 0.5 mg/kg twice daily (max dose = 2 mg/kg twice daily).
Seizures Associated with Tuberous Sclerosis Complex
PO (Adults and Children ≥1 yr): 2.5 mg/kg twice daily; can ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 2.5 mg/kg twice daily to recommended maintenance dosage of 12.5 mg/kg twice daily.
Hepatic Impairment
PO (Adults and Children ≥1 yr): Moderate hepatic impairment (Child–Pugh B): 1.25 mg/kg twice daily; can ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 1.25 mg/kg twice daily to recommended maintenance dosage of 6.25 mg/kg twice daily; Severe hepatic impairment (Child–Pugh C): 0.5 mg/kg twice daily; can ↑ dose on weekly basis (every other day if more rapid titration warranted) in increments of 0.5 mg/kg twice daily to recommended maintenance dosage of 2.5 mg/kg twice daily.
Oral solution (strawberry flavor): 100 mg/mL
Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts, behavior, or depression.
Monitor for signs and symptoms of hepatotoxicity (unexplained nausea, vomiting, right upper quadrant abdominal pain, fatigue, anorexia, jaundice and/or dark urine). If signs and symptoms occur, promptly measure serum transaminases and total bilirubin and interrupt or discontinue treatment with cannabidiol.
Lab Test Considerations:
Obtain serum transaminases (ALT, AST) and total bilirubin levels before starting therapy. Elevations usually respond to decreased dose or discontinuation of therapy. Monitor levels at 1, 3, and 6 mo after starting therapy, within 1 mo following dose changes, and as needed thereafter. Discontinue cannabidiol if transaminase levels >3 times upper limit of normal (ULN) and bilirubin levels >2 times ULN. Also discontinue therapy if transaminase persistently >5 times ULN.
Advise patient to notify health care professional promptly if signs and symptoms of hepatotoxicity occur.
Inform patients and families of risk of suicidal thoughts and behavior and advise that behavioral changes, emergency or worsening signs and symptoms of depression, unusual changes in mood, or emergence of suicidal thoughts, behavior, or thoughts of self-harm should be reported to health care professional immediately.
Decreased frequency and intensity of seizure activity.