. Author manuscript; available in PMC: 2010 Jun 26.

Published in final edited form as: Adv Ther. 2009 Jun 26;26(6):588–599. doi: 10.1007/s12325-009-0039-0

Table 1.

Properties of long-acting risperidone(LAR).

Pharmacodynamics⁹
	Serotonin 5-HT2A, dopamine D2, histaminergic H1, and adrenergic alpha-1 and alpha-2 antagonist Increasing degrees of D₂-receptor occupation with increasing doses of LAR injection Little or no affinity for cholinergic muscarinic or beta-1 and beta-2 adrenergic receptors.
Pharmacokinetics¹⁰
	Repeated administration every 2 weeks achieves steady-state plasma levels after the fourth injection Linearpharmacokinetics Intramuscular and oral preperations are bioequvelant but LAR is associated with lower steady-state peak concentrations and less fluctiations in plasma levels compared with oral treatment.
Metabolism and elimination¹¹
	Metabolized by cytochrome P-450 (CYP) isoenzyme 2D6 to 9-hydroxyrisperidone The half-life of LAR is 3–6 days because of the extended-release profile rather than the metabolic half-life (N-dealkylation is an alternative pathway) LAR is completely eliminated from the body after 6–7 weeks.