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. 2015 Oct 11;3(4):245–260. doi: 10.1093/nop/npv038

Table 1.

Pharmacokinetic characteristics of antiepileptic drugsa

AED Usual Oral Dose (mg/day) Therapeutic Range (mg/L) Oral Bioavailability (%) Time to Steady State (days) T1/2 (h) without Enzyme Inducers T1/2 (h) with Enzyme Inducers Cl (mL/kg/h) without Enzyme Inducers Cl (mL/kg/h) with Enzyme Inducers Protein Binding (%)
Carbamazepine 400–1600 4–12 75–85 2–4 8–20 9–10 133 80 75
Clobazam 5–40 0.1–0.3 80–90 10–30 10–45 12–60 40–70 bfactor 2–3 85
Clonazepamc 0.5–4, max.20 0.02–0.08 90 17–56 1–4 1–3 90 factor 1.2–1.6 85
Eslicarbazepine 400–1200 3–35 90 3–4 20–24 9–20 35–50 40–65 40
Gabapentin 900–3600 12–20 <60 1–2 5–9 5–9 120–230 120–230 0
Lacosamide 200–400 10–20 >95 3 12–16 12–16 28–40 28–40 <15
Lamotrigine 200–600 2.5–15 >95 3–15 22–38 14–15 20–35 50–80 55
Levetiracetam 1000–3000 8–26 80–90 1–2 5–11 5–8 30–50 45–75 0
Midazolamd in 5–15 100–400 30–70 1–2 1–4 1–2 250–540 12–30 95–97
Oxcarbazepine 900–2400 12–35 80–100 2–3 5–30 6–19 40–50 50–70 40–60
Perampanel 4–12 0.2–1.0 100 10–19 66–105 ∼25 8–12 12–20 95%
Phenobarbital 30–180 10–40 95 15–30 70–140 80–100 6–9 12–18 45–60
Phenytoin 150–400 10–20 95 6–21 24–100 <24–72 7–42 factor ∼2 85–95
Pregabalin 150–600 2–8 90 1–2 5–7 5–7 45–75 45–75 0
Retigabine 600–1200 60 1–2 6–10 4–7 670 470 80
Topiramate 100–500 5–20 81%–95% 4–7 20–30 9–12 15–36 30–50 15
Valproic acid 500–2500 50–100 >95 2–4 13–18 2–11 6–15 4–10 85–95
Vigabatrin 200–300 0.8–36 80–90 1–2 6–8 4–6 130–150 130–150 0
Zonisamide 200–600 10–38 >90 5–12 50–70 25–37 15–20 20–30 40–60

Abbreviations: AED, antiepileptic drug; Cl, clearance; in, intranasal.

aData drawn from Johannessen SI, 200610; Bénit CP, 20127; Patsalos, 201311; De Leon, 201316; Italiano D, 2013.12

bDespite faster clearance, clinical activity of clobazam is 1.5 to 2 times higher due to increased conversion into the active metabolite N-desmethylclobazam.

cUse of clonazepam as oral or buccal (sublingual/sublabial) administration.

dMidazolam as intranasal administration on an as-needed basis.