Iloperidone

An atypical antipsychotic that exhibits high affinity to serotonin 5HT2A (Ki =5.6 nM), dopamine D2 (Ki=6.3 nM) and D3 (Ki=7.1 nM) and noradrenaline α1 receptors (Ki=0.36 nM), moderate affinity for D4 (25 nM), 5HT6 (43 nM), 5HT7 (22 nM), and low affinity for 5HT1A (168 nM), D1 and histamine H1 receptors; is used for the treatment of schizophrenia.Schizophrenia Approved (In Vitro) :Iloperidone displays higher affinity for the dopamine D3 receptor (Ki=7.1 nM) than for the dopamine D4 receptor (Ki=25 nM) . Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki=5.6 nM) than for the 5-HT2C receptor (Ki=42.8 nM) . (In Vivo) :Iloperidone is eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. 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.