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paliperidone + olanzapine
- Development stage
- Unknown
- Lead developer
- Janssen Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Paliperidone + olanzapine is a combination of two atypical (second-generation) antipsychotic drugs. Both agents are used primarily in the treatment of schizophrenia and related psychotic disorders. Paliperidone, the active metabolite of risperidone, acts mainly as an antagonist at central dopamine D2 and serotonin 5HT2A receptors, with additional antagonism at alpha-1/alpha-2 adrenergic and H1 histaminergic receptors[2][6][8]. Olanzapine also exerts its effects through antagonism of multiple neuronal receptors including dopamine D1-D4, serotonin 5HT2A/5HT2C/5HT3/5HT6, alpha-1 adrenergic, H1 histamine, and muscarinic receptors[4][5]. The combination may be considered for patients who have not responded adequately to monotherapy or require broader receptor coverage; however, co-administration increases the risk of additive side effects such as sedation, anticholinergic effects (dry mouth, constipation), cardiovascular changes (irregular heartbeat), confusion, and memory problems[1].
- Other names
- paliperidone + olanzapine
02
Targets
DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)CHRM5 (M5)HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)ADRA2A (α2A)CHRM2 (M2)ADRA1A (α1A)CHRM4 (M4)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)CHRM3 (M3)
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