Drug intelligence / Profile preview

risperidone + haloperidol + olanzapine + quetiapine + aripiprazole + paliperidone + levomepromazine + perphenazine

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

This is a combination of eight antipsychotic drugs, each with distinct pharmacological profiles but all primarily used in the management of psychiatric disorders such as schizophrenia and bipolar disorder. The included agents are: - **Risperidone** (second-generation/atypical antipsychotic): Primarily acts as an antagonist at dopamine D2 and serotonin 5-HT2A receptors. - **Haloperidol** (first-generation/typical antipsychotic): Potent dopamine D2 receptor antagonist. - **Olanzapine** (second-generation/atypical antipsychotic): Antagonist at multiple receptors including dopamine D2, serotonin 5-HT2A, histamine H1, muscarinic, and adrenergic receptors. - **Quetiapine** (second-generation/atypical antipsychotic): Antagonist at serotonin 5-HT2A and dopamine D2 receptors; also affects histamine H1 and adrenergic alpha1 receptors. - **Aripiprazole** (second-generation/atypical antipsychotic): Partial agonist at dopamine D2 and serotonin 5-HT1A; antagonist at serotonin 5-HT2A receptor. - **Paliperidone** (second-generation/atypical antipsychotic; active metabolite of risperidone): Similar mechanism to risperidone—antagonism of dopamine D2 and serotonin 5-HT2A receptors[4]. - **Levomepromazine** (first-generation/typical phenothiazine derivative): Broad-spectrum antagonist affecting dopaminergic, serotonergic, histaminergic, cholinergic, and adrenergic systems[4]. - **Perphenazine** (first-generation/typical phenothiazine derivative): Dopamine D2 receptor antagonist with additional antagonism at other neurotransmitter sites. These drugs are not typically combined together in clinical practice due to overlapping mechanisms of action and increased risk for adverse effects. Each is individually approved for use in various psychoses or mood disorders[3][4][5].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HRH1 (Histamine H1 Receptor)ADRA1A (α1A)mAChR (Muscarinic acetylcholine receptors)DRD2 (Dopamine D2 Receptor)

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