Comparative Pharmacology
Head-to-head clinical analysis: LATUDA versus RISPERDAL CONSTA.
Head-to-head clinical analysis: LATUDA versus RISPERDAL CONSTA.
LATUDA vs RISPERDAL CONSTA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lurasidone is an atypical antipsychotic with high affinity for dopamine D2, serotonin 5-HT2A, and serotonin 5-HT7 receptors, and moderate affinity for serotonin 5-HT1A receptors. It acts as an antagonist at D2 and 5-HT2A receptors, and as a partial agonist at 5-HT1A receptors. The exact mechanism of action in schizophrenia and bipolar depression is unknown but is thought to involve modulation of these 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 80-160 mg once daily; maximum 160 mg/day. Administer with food (at least 350 calories).
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 20–40 hours (mean about 29 hours) in adults, supporting once-daily dosing. Steady-state is reached within 7 days.
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 the dose is eliminated in feces (mostly as unchanged drug and metabolites) and about 10% in urine. Less than 2% is excreted as unchanged lurasidone 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 C
Category C
Atypical Antipsychotic
Atypical Antipsychotic