Table 1.
Pharmacokinetic parameters of current antiepileptic medications
| Drug | Oral bioavailability (%) | Reference concentration range (mg/l) | t max (h) | Time to steady state (days) | t ½ (h) | Protein binding (%) | Volume of distribution (l/kg) | Active metabolite | Need for TDM | References |
|---|---|---|---|---|---|---|---|---|---|---|
| Rufinamide | ≥85 | 5–30 | 5–6 | 2 | 8–12 | 30 | 07–1.1 | No | Intermediate to frequent | [11, 12] |
| Stiripentol | ≥90 | 4–22 | 1–2 | 1–2 | 4.5–13 | 99 | Variable | No | Frequent | [15, 16, 21] |
| Perampanel | 100 | a | 05–1.5 | 14–21 | 70–110 | 96 | 77 | No | a | [23, 24] |
| Retigabine | 60 | a | 0.5–2 | 1–2 | 8 | 80 | 6.2 | No | a | [12, 35] |
| Eslicarbazepine acetate | ≥80 | 10–35 | 1–4 | 4–5 | 20–40 | 35 | 2.7 | Yes | Intermediate | [38, 43] |
| Vigabatrin | ≥60 | 0.8–36 | 1–2 | 1–2 | 5–8 | 0 | 0.8 | No | Intermediate | [55] |
| Lacosamide | ≥95 | 5–10 | 05–4 | 2–4 | 12–13 | 15 | 0.6 | No | Uncommon | [60] |
| Pregabalin | ≥90 | 2–5 | 1–2 | 1–2 | 5–7 | 0 | 0.5 | No | Intermediate | [73, 82] |
| Zonisamide | ≥65 | 10–40 | 2–5 | 9–12 | 50–70 | 50 | 1.45 | No | Frequent | [96] |
| Levetiracetam | ≥95 | 12–46 | 1 | 1–2 | 6–8 | 0 | 0.5–0.7 | No | Intermediate | [100, 104] |
| Tiagabine | ≥90 | 0.02–0.2 | 0.5–2 | 1–2 | 5–9 | 96 | 1–1.3 | No | Frequent | [109, 112] |
| Topiramate | ≥80 | 5–20 | 2–4 | 4–5 | 20–30 | 15 | 0.6–0.8 | No | Intermediate | [121, 130] |
| Lamotrigine | ≥95 | 2.5–15 | 1–3 | 3–6 | 15–35 | 55 | 1–1.4 | No | Frequent | [143, 144] |
| Felbamate | >90 | 30–60 | 2–6 | 3–4 | 16–22 | 25 | 0.8 | No | Intermediate | [157, 159] |
| Gabapentin | <60 | 2–20 | 2–3 | 1–2 | 5–9 | 0 | 0.6–0.8 | No | Uncommon | [170] |
T ½ elimination half-life, TDM therapeutic drug monitoring, t max time to reach maximum plasma concentration following drug administration
aNot yet established