Arian Mechanism of Action

Pharmacology: Pharmacodynamics: Aripiprazole is a psychotropic drug intended for the treatment of schizophrenia and related manic disorders.
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5.HT1A and 5.HT2A receptors, moderate affinity for dopamine D4, serotonin 5.HT2C and 5.HT7, alpha 1.adrenergic and histamine HI receptors and moderate affinity for the serotonin reuptake site. Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors.
The exact mechanism of action of aripiprazole is unknown. However, it has been proposed that the efficacy of aripiprazole is medicated through a combination of partial agonist activity at D2 and 5.HT1A receptors and antagonist activity at 5-HT2A receptors.
Pharmacokinetics: Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within 3 hours to 5 hours; the absolute oral bioavailability of the tablet formulation is 87%. ARIAN tablets can be administered with or without food. At therapeutic concentrations, Aripiprazole and its major metabolite are greater than 99% bound to serum proteins, primarily to albumin. In healthy human volunteers administered 0.5 mg/day to 30 mg/day Aripiprazole for 14 days, there was dose-dependent D2 receptor occupancy indicating brain penetration of Aripiprazole in humans.
Aripiprazole is metabolized primarily by three biotrasformation pathways: dehydrogenation, hydroxylation, and N-dealkylation. Based on in vitro studies, CYP3A4 and CYP2D6 enzymes are responsible for dehydrogenation and hydroxylation of Aripiprazole, and N.dealkylation is catalyzed by CYP3A4. Aripiprazole is the predominant drug moiety in the systemic circulation. At steady-state, dehydroaripiprazole, the active metabolite, represents about 40% of aripiprazole AUC in plasma.