Drug intelligence / Profile preview

aripiprazole + cocaine

Development stage
Unknown
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral, Intramuscular, Intranasal, Inhalation, Intravenous
01

Overview

Aripiprazole + cocaine refers to the concurrent use or co-administration of aripiprazole, an atypical antipsychotic, and cocaine, a powerful central nervous system stimulant. Aripiprazole acts primarily as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors. Cocaine blocks the reuptake of dopamine, norepinephrine, and serotonin in the brain, leading to increased concentrations of these neurotransmitters and pronounced stimulant effects. Research on their combination has focused on whether aripiprazole can modulate the reinforcing or subjective effects of cocaine. Acute administration of aripiprazole may attenuate some subjective effects (such as craving or perceived drug quality) but can also increase self-administration behavior in some settings[1][3][5]. The interaction is complex; while some studies suggest reduced discriminative stimulus and cardiovascular effects when combined acutely[5], others indicate that chronic use may lead to compensatory increases in cocaine intake[1][3]. There are also case reports suggesting that combining these drugs (especially with other serotonergic agents) could increase risk for adverse events such as serotonin syndrome[4].

02

Targets

SERT (Sodium-dependent serotonin transporter)HTR2A (Serotonin receptor 5-HT2A)DAT (Dopamine plasma membrane transport protein)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)NET (Norepinephrine Transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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