Table 3.

Pharmacokinetic parameters of first- and second-generation NNRTIs [13–23]

	First-generation NNRTIs				Second-generation NNRTIs
	NVP	NVP (extended release)	DLV	EFV	ETR	RPV
Dosage (mg)	200, bid	400, opd	400, tid	600, opd	200, bid	25, opd
tmax (h)	4	24	1.2	3–5	4, 200 mg/12 h 3, 400 mg/24 h	4
Cmax (µg/mL)	2	2.1	3.3	4.1	0.40, 200 mg/12 h 0.70, 400 mg/24 h	0.15
CL (L/h)	1.5, SD 3.3, MD		60.3, SD 7.79, MD	9.4	43.7	11.8
Vd (L/kg)	1.2		0.8–1	3.8	6.0	–a
F	>90%	75%	85%, SDb	40–45%	–a	–a
t1/2 (h)	45, SD 25–30, MD		2.4	52–76, SD 40–55, MD	30–40	47.7
Protein binding	62%		98%	>99%	99.9%	99.7%

t_max: time to maximum plasma concentration (C_max); CL: apparent plasma clearance; Vd: apparent volume of distribution; F: bioavailability; t_1/2: half-life.

^aNot available

^bsingle-dose bioavailability of DLV tablets relative to an oral solution.

bid: twice daily; opd.: once daily; tid: three times daily.

SD: single dose; MD: multiple doses.