Pharmacokinetic parameters of nalmefene following intranasal and intramuscular administration

Parameter (U)a3 mg IN (N = 14)3 mg IN/0.25% DDM (N = 13)1.5 mg IN (N = 11)1.5 mg i.m. (N = 13)
Cmax (ng/ml)1.99(51.3)4.45(65.7)0.961(43.8)1.53(43.5)
Cmax/D (ng/ml/mg)0.662(51.3)1.48(65.7)0.641(43.8)1.02(43.5)
Tmax (h)2.00(0.33–3.00)0.25(0.17–1.00)2.00(1.00–2.07)0.33(0.25–8.00)
AUC0–t (ng·h/ml)12.7(68.1)15.2(71.8)5.58b(57.9)10.6(45.7)
AUC0–2.5 min0.00(0.00)0.004(0.006)0.00(0.00)0.00(0.00)
AUC0–5 min0.00(0.00)0.029(0.037)0.00(0.00)0.008(0.013)
AUC0–10 min0.005(0.010)0.257(0.239)0.00(0.00)0.072(0.053)
AUC0–15 min0.026(0.036)0.596(0.506)0.006(0.006)0.168(0.106)
AUC0–20 min0.226(0.202)0.924(0.708)0.023(0.019)0.278(0.170)
AUC0–t/D (ng·h/ml/mg)4.24(68.1)5.06(71.8)3.72(57.9)7.07(45.7)
t1/2 (h)7.87c(40.8)7.11(45.5)6.59d(53.3)8.01b(39.2)
  • AUC0–t/D, AUC0–t divided by the dose; AUC0–x, AUC from time zero to x minutes; Cmax/D, Cmax divided by the dose; %CV, percentage coefficient of variation.

  • a Geometric mean values (%CV) for all except Tmax, which is median (minimum, maximum).

  • b N = 12.

  • c N = 13.

  • d N = 10.