EPIDIOLEX Dosage & Rx Info | Uses, Side Effects

Epidiolex Generic Name & Formulations

Legal Class

General Description

Cannabidiol 100mg/mL; oral soln; strawberry-flavored; contains dehydrated alcohol, sesame seed oil.

Pharmacological Class

Cannabinoid.

How Supplied

Oral soln (w. dosing syringes + adapter)—60mL, 100mL

Manufacturer

Jazz Pharmaceuticals plc

Generic Availability

Mechanism of Action

The precise mechanisms by which cannabidiol exerts its anticonvulsant effect in humans are unknown. Cannabidiol does not appear to exert its anticonvulsant effects through interaction with cannabinoid receptors.

Epidiolex Indications

Indications

Treatment of seizures associated with Lennox-Gastaut syndrome (LGS), Dravet syndrome (DS), or tuberous sclerosis complex (TSC).

Epidiolex Dosage and Administration

Adults and Children

<1yr: not established. Use calibrated measuring device. May be given via nasogastric or gastrotomy tubes, if needed. ≥1yr: LGS or DS: initially 2.5mg/kg twice daily; may increase to 5mg/kg twice daily after 1 week. May further increase in weekly increments of 2.5mg/kg twice daily (or no sooner than every other day) as tolerated; max 10mg/kg twice daily. TSC: initially 2.5mg/kg twice daily; increase in weekly increments of 2.5mg/kg twice daily (or no sooner than every other day) as tolerated, to maintenance dose of 12.5mg/kg twice daily. Moderate to severe hepatic impairment: see full labeling.

Administration

Discard unused medication 12 weeks after first opening the bottle.

Nursing Considerations

Discard unused medication 12 weeks after first opening the bottle.

Epidiolex Contraindications

Not Applicable

Epidiolex Boxed Warnings

Not Applicable

Epidiolex Warnings/Precautions

Warnings/Precautions

Risk of hepatocellular injury. Obtain ALT/AST and total bilirubin prior to, at 1 month, 3 months, and 6 months after initiation, and periodically thereafter; also obtain levels within 1 month after dose adjustments or concomitant drugs known to impact the liver. Evaluate and consider more frequent monitoring if elevated liver enzymes at baseline. Interrupt or discontinue if hepatic dysfunction occurs; discontinue if ALT/AST elevations >3×ULN and bilirubin >2×ULN, or sustained ALT/AST elevations >5×ULN. Monitor for somnolence and sedation. Monitor for emergence or worsening of depression, suicidal thoughts/behavior or any unusual changes in mood/behavior. Discontinue if hypersensitivity reactions occur. Withdraw gradually. Avoid abrupt cessation. Moderate or severe hepatic impairment. Elderly. Pregnancy. Nursing mothers.

Epidiolex Pharmacokinetics

Absorption

Time to maximum plasma concentration: 2.5 to 5 hours.

Distribution

Apparent volume of distribution: 20963 to 42849 L. >94% plasma protein bound.

Metabolism

Hepatic (CYP2C19, CYP3A4, UGT1A7, UGT1A9, UGT2B7).

Elimination

Fecal, renal (minor). Half-life: 56–61 hours.

Epidiolex Interactions

Interactions

Antagonized by strong CYP3A4 or CYP2C19 inducers: consider increasing Epidiolex dose. May potentiate CYP1A2 (eg, theophylline, caffeine, tizanidine), UGT1A9 (eg, diflunisal, propofol, fenofibrate), UGT2B7 (eg, gemfibrozil, lamotrigine, morphine, lorazepam), CYP2C8 or CYP2C9 (eg, phenytoin) substrates: consider reducing dose of these. May affect CYP2B6 (eg, bupropion, efavirenz) substrates: consider adjusting dose of these. Potentiates sensitive CYP2C19 substrates (eg, diazepam, clobazam), P-gp/CYP3A4 substrates (eg, everolimus), or other orally administered P-gp substrates (eg, sirolimus, tacrolimus, digoxin): monitor and consider reducing dose of substrates. Monitor with stiripentol. Increased transaminase or ammonia level elevations with concomitant valproate and/or clobazam; monitor more frequently, consider discontinuation or dose adjustment of these drugs. May increase risk of somnolence and sedation with concomitant clobazam, CNS depressants, alcohol; monitor.

Epidiolex Adverse Reactions

Adverse Reactions

Somnolence, decreased appetite, diarrhea, transaminase elevations, fatigue, malaise, asthenia, rash, insomnia, sleep disorders, poor quality sleep, infections, pyrexia, vomiting; hypersensitivity reactions.

Epidiolex Clinical Trials

See Literature

Epidiolex Note

Notes

Enroll pregnant patients exposed to Epidiolex in the North American Antiepileptic Drug pregnancy registry by calling (888) 233-2334.

Epidiolex Patient Counseling