Comparative Pharmacology
Head-to-head clinical analysis: LURASIDONE HYDROCHLORIDE versus RISPERDAL CONSTA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LURASIDONE HYDROCHLORIDE versus RISPERDAL CONSTA.
LURASIDONE HYDROCHLORIDE vs RISPERDAL CONSTA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lurasidone is an atypical antipsychotic that acts as a full antagonist at D2 and 5-HT2A receptors, with high affinity for 5-HT7 and 5-HT1A receptors, moderate affinity for alpha2C and alpha2A adrenergic receptors, and no appreciable affinity for H1, M1, or alpha1 receptors.
Risperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also binds to alpha1-adrenergic, alpha2-adrenergic, and histamine H1 receptors, with low affinity for muscarinic receptors. The combination of 5-HT2A and D2 antagonism is thought to improve negative symptoms and reduce extrapyramidal side effects.
40 mg orally once daily initially, titrated to 80 mg once daily; maximum 80 mg per day.
25 mg intramuscular every 2 weeks; may increase to 37.5 mg or 50 mg after 4 weeks if needed.
None Documented
None Documented
Terminal elimination half-life is approximately 18 hours (range 14–24 hours), supporting once-daily dosing.
The terminal elimination half-life of risperidone is approximately 20 hours for CYP2D6 extensive metabolizers and 24 hours for poor metabolizers (accounting for both risperidone and 9-hydroxyrisperidone). The half-life of the active moiety is about 20 hours, allowing for biweekly dosing of the long-acting injection.
Approximately 80% of total radioactivity recovered in feces (67% as metabolites, 9% as unchanged drug) and 19% in urine (mostly metabolites); less than 1% excreted as unchanged parent in urine.
Risperidone and its active metabolite 9-hydroxyrisperidone are primarily excreted renally (70%), with 14% excreted in feces. The remainder is eliminated via biliary and metabolic pathways.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic