Iloperidone (hydrochloride)

Iloperidone hydrochloride (HP 873 hydrochloride) is a D₂/5-HT₂ receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms^[1][2]. In Vitro: Iloperidone hydrochloride displays higher affinity for the dopamine D₃ receptor (K_i=7.1 nM) than for the dopamine D₄ receptor (K_i=25 nM). Iloperidone displays high affinity for the 5-HT₆ and 5-HT₇ receptors (K_i=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT_2A (Ki=5.6 nM) than for the 5-HT_2C receptor (K_i=42.8 nM)^[1].
In Vivo: Iloperidone hydrochloride is eliminated slowly, with a mean t_1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t_max, or C_max. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events^[2].