Expert consensus of the Chinese Association for the Study of Pain on ion channel drugs for neuropathic pain

Table 1 Pharmacodynamics of ion channel drugs

	Sodium channel blockers				Calcium channel modulators
	Carbamazepine	Oxcarbazepine	Lidocaine, by iv	BLA	Pregabalin	Gabapentin
T max	Within 12 h	4.5 h	5 min		1 h	3 h
C max	0.5-25 μg/mL	31.5 μmol/L	2-5 mg/lanalgesic use		3.83-9.46 μg/mL	2.7-2.99 mg/L
t1/2	25-65 h (single dose); 12-17 h (long-term oral)	2 h; 9 h (MHD)	10 min (single dose); 1.5-2 h (continuous infusion)	4 h	5-6.5 h	6.5 h
Bioavailability	58%-85%	> 95%	100%		90%	47%-60%
Effect-onset time	8-72 h	1-3 h	5 min (onset); 1 h (maintain)		Within 30 min (acute toothache); 5 h (maintain); 1 wk (diabetic neuropathy)	24-28 h (repeated administration); no capping effect
Metabolism	Liver	Liver	Liver (mainly)		Liver (less)	No metabolism in the body
Excretion	Kidney (72%); Feces (28%)	Kidney (> 95%)		Kidney (mainly)	Kidney (92-99%) excreted as drug prototype	Kidney (mainly) excreted as drug prototype

BLA: Bulleyaconitine A; C max: Maximum concentration; iv: Intravenous; MHD: Monohydroxycarbazepine; t_1/2: Half life time; T max: Peak time.