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. Author manuscript; available in PMC: 2022 Apr 5.
Published in final edited form as: Neuropharmacology. 2020 Feb 14;168:108009. doi: 10.1016/j.neuropharm.2020.108009

Table 2.

Pharmacokinetic parameters of pimavanserin or lorcaserin following a single dose of each medication alone or in combination (mean ± SEM).

CMAX (ng/ml) TMAX (hr) AUC0-t(ng-hr/ml) AUC0-inf(ng-hr/ml) AUCExtrap(%) λ(1/hr) Half-life, t1/2(hr) Cl/F(L/hr/kg)

Pimavanserin
Pimavanserin(mg/kg; s.c.)
0.5 12.17 ± 0.38 0.29 ± 0.04 14.40 ± 0.31 15.02 ± 0.32 3.89 ± 1.42 0.76 ± 0.14 1.29 ± 0.45 33.40 ± 0.73
1 30.13 ± 2.17 0.25 ± 0.00 41.27 ± 2.64 41.72 ± 2.7 1.09 ± 0.28 0.79 ± 0.04 0.89 ± 0.05 24.55 ± 1.81
3 79.52 ± 3.76 0.38 ± 0.06 189.33 ± 7.75 197.5 ± 8.33 4.26 ± 0.68 0.59 ± 0.03 1.18 ± 0.05 15.28 ± 0.65
10 213.17 ± 15.86 0.96 ± 0.25 857.50 ± 54.72 1290.17 ± 112.09 32.22 ± 4.18 0.21 ± 0.02 3.63 ± 0.54 8.10 ± 0.83
Pim + Lora(mg/kg; s.c.)
0.5 + 0.5 12.03 ± 1.97 0.25 ± 0.00 13.88 ± 3.32 14.34 ± 3.47 2.90 ± 0.69 0.80 ± 0.09 0.93 ± 0.12 41.15 ± 5.30
1 + 1 26.87 ± 5.04 0.25 ± 0.00 38.18 ± 11.19 39.05 ± 11.56 1.90 ± 0.44 0.68 ± 0.05 1.05 ± 0.08 28.00 ± 7.26
Lorcaserin
Lorcaserin(mg/kg; s.c.)
0.5 15.63 ± 0.74 0.29 ± 0.04 29.03 ± 0.53 33.43 ± 1.31 12.68 ± 2.45 0.31 ± 0.03 2.39 ± 0.33 15.07 ± 0.56
1 34.35 ± 3.19 0.25 ± 0.00 58.52 ± 3.41 63.70 ± 3.91 8.06 ± 0.47 0.39 ± 0.02 1.80 ± 0.09 15.97 ± 0.85
3 106.33 ± 14.74 0.42 ± 0.05 183.50 ± 7.71 199.17 ± 8.24 7.97 ± 0.50 0.38 ± 0.01 1.83 ± 0.07 15.18 ± 0.66
Pim + Lora(mg/kg; s.c.)
0.5 + 0.5 14.74 ± 0.71 0.30 ± 0.05 26.46 ± 1.80 28.48 ± 1.88 7.14 ± 0.75 0.40 ± 0.02 1.74 ± 0.11 17.9 ± 1.29
1 + 1 26.62 ± 1.69 0.35 ± 0.06 48.88 ± 2.71 52.82 ± 2.84 7.55 ± 0.52 0.41 ± 0.02 1.71 ± 0.07 19.12 ± 0.99
a

Pimavanserin administered 15 min prior to lorcaserin; CMAX, maximum serum concentration; TMAX, time to reach CMAX; AUC0-t, area under plasma drug concentration-time curve (AUC) up to time ‘t’; AUC0-inf, extrapolated AUC to infinity; AUCExtrap, effect of extrapolated AUC on AUC0-inf estimation; λ, individual estimate of terminal elimination rate constant; t1/2, elimination half-life; Cl/F, apparent total body clearance.