Table 1.
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.