Iloperidone, sold under the brand name Fanapt among others, is an atypical antipsychotic for the treatment of schizophrenia and bipolar I disorder. It is an orally administered piperidinyl-based compound with a pharmacological profile characterized by antagonism at serotonin 5-HT2A and dopamine D2 receptors, with additional affinity for D3, 5-HT6 and alpha1-adrenergic receptors; the alpha1 blockade contributes to orthostatic hypotension risk. Iloperidone is primarily metabolized hepatically via cytochrome P450 enzymes CYP2D6 and CYP3A4, resulting in inactive and minor active metabolites, and elimination kinetics vary by CYP2D6 phenotype. Clinical pharmacokinetic properties include oral absorption with Tmax in the range of a few hours and an effective elimination half-life that is longer in poor CYP2D6 metabolizers compared with extensive metabolizers. Dose titration is recommended to reduce cardiovascular and CNS adverse effects, and clinical monitoring for QT prolongation, blood pressure changes, and metabolic parameters is standard practice.
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Parent: Iloperidone
Typical quality specifications for iloperidone active pharmaceutical ingredient define and control related substances arising from synthesis and degradation such as N-dealkylated derivatives, desmethyl-iloperidone, N-oxide and oxidation products, ring-opened impurities and trace residual solvents. In many industry specifications individual identified related compounds are limited to no more than 0.10 percent weight by weight, unspecified single impurities are commonly controlled at 0.05 percent w/w or below, and the total amount of impurities is often set at or below 0.50 percent w/w. Genotoxic impurity risk is assessed per ICH M7 and any identified mutagenic degradant is limited to levels below the appropriate control threshold. Residual solvent limits follow ICH Q3C with Class 2 solvents minimized and Class 1 solvents avoided.
Iloperidone is used to treat symptoms of schizophrenia in adults and for the management of bipolar I disorder when indicated; it targets positive and some negative symptoms through modulation of dopamine and serotonin receptors, and is prescribed with monitoring for cardiovascular and metabolic side effects.
Iloperidone and risperidone are both atypical antipsychotics and share antagonism at D2 and 5-HT2A receptors, but they differ in receptor affinity profiles, clinical adverse effect patterns and metabolism; iloperidone has relatively higher alpha1-adrenergic blockade and is metabolized predominantly by CYP2D6 and CYP3A4, which influences dosing and drug interaction considerations.
Iloperidone can cause weight gain as part of its metabolic adverse effect profile, though the magnitude varies by individual; baseline and periodic monitoring of weight, glucose and lipids is recommended during treatment.
Iloperidone exerts antipsychotic effects primarily through antagonism of dopamine D2 receptors and serotonin 5-HT2A receptors, with additional binding to D3, 5-HT6 and alpha1-adrenergic receptors; this combination of receptor interactions is thought to reduce psychotic symptoms while contributing to its side effect profile.
