Eab Clobazam Mechanism of action- benzodiazepine oA: activates GABA receptor a. Adjunctive treatment of Lennox-Gastaut seizures for patients >2 years o000oc0= Pharmacokinetics V=100L Active metabolite N-desmethylclobazam Metabolized by CyP2C19 decrease dose in poor metabolizers 1/2=36-42 hours(metabolite 71-82 hours) KENTUCKY College of Pharmacy
Clobazam • Mechanism of action – benzodiazepine; activates GABA receptor • Adjunctive treatment of Lennox-Gastaut seizures for patients ≥ 2 years • Pharmacokinetics – Vd=100 L – Active metabolite N-desmethylclobazam – Metabolized by CYP2C19; decrease dose in poor metabolizers – t1/2=36-42 hours (metabolite 71-82 hours)
Eab Clobazam Drug-drug interactions 00 Weak cyp3A4 inducer- hormonal contraceptives CYP2D5 inhibitor o000oc0= CYP2C19 inhibitors may increase clobazam (fluconazole, fluvoxamine, ticlopide omeprazole Development of tolerance KENTUCKY College of Pharmacy
Clobazam • Drug-drug interactions – Weak CYP3A4 inducer – hormonal contraceptives – CYP2D5 inhibitor – CYP2C19 inhibitors may increase clobazam (fluconazole, fluvoxamine, ticlopide, omeprazole) • Development of tolerance
Eab Clobazam Adverse effects- sedation 00 Rare- Stevens-Johnson syndrome and toxic epidermal necrolysIs Controlled substance o0000=0×0oo Dosing If 5 mg/day, can give as one dose; if >5 mg/day, should divide twice daily Dose ≤30k >30kg Initial 5 mg 10 mg Day 7 10 mg 20 mg Dav 14 20 mg 40 mg NTUCKY ollege of Pharmacy
Clobazam • Adverse effects – sedation – Rare – Stevens-Johnson syndrome and toxic epidermal necrolysis • Controlled substance • Dosing – If 5 mg/day, can give as one dose; if >5 mg/day, should divide twice daily Dose ≤30 kg >30 kg Initial 5 mg 10 mg Day 7 10 mg 20 mg Day 14 20 mg 40 mg
Perampane 右F.° Mechanism of action Non-competitive aMpa glutamate receptor 00 antagonist Anti-seizure effects should still be maintained even when glutamate concentrations are high · Pharmacokinetics 95% protein bound to albumin and al-acid glycoprotein Metabolized by cyP3A4 and CYP3A5 Half-life= 105 hours ¨·| interactions Decreases levonorgestrel KENTUCKY College of Pharmacy
Perampanel • Mechanism of action – Non-competitive AMPA glutamate receptor antagonist • Anti-seizure effects should still be maintained even when glutamate concentrations are high • Pharmacokinetics – 95% protein bound to albumin and α1-acid glycoprotein – Metabolized by CYP3A4 and CYP3A5 – Half-life = 105 hours • Interactions – Decreases levonorgestrel
Perampane oF. Controlled substance- awaiting DEA of. classification 00 Adverse effects Dizziness Gait disturbance/falls o000oc0= Somnolence Weight gain Psychiatric and behavioral effects (aggression hostility irritability anger, homicidal ideation)can occur with or without psychiatric history(2-20%) KENTUCKY College of Pharmacy
Perampanel • Controlled substance – awaiting DEA classification • Adverse effects – Dizziness – Gait disturbance/falls – Somnolence – Weight gain – Psychiatric and behavioral effects (aggression, hostility, irritability, anger, homicidal ideation) can occur with or without psychiatric history (2-20%)