Drug intelligence / Profile preview

cocaine + N-acetylcysteine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Intranasal, Inhalation
01

Overview

This is a combination of two substances, cocaine and N-acetylcysteine. Cocaine is a central nervous system stimulant and local anesthetic with high abuse potential, acting primarily by blocking the reuptake of dopamine, norepinephrine, and serotonin in the brain. N-acetylcysteine (NAC) is an antioxidant and cysteine prodrug that restores glutamate homeostasis in the brain by modulating the cystine-glutamate exchanger (system xc−). While there are no approved pharmaceutical products combining these agents for clinical use, research has investigated NAC as a pharmacological intervention to mitigate cocaine-induced neurotoxicity or reduce relapse risk in individuals with cocaine dependence. Preclinical studies show that NAC can prevent or reverse some of the neurochemical changes induced by repeated cocaine exposure—such as disruption of glutamate signaling—and may reduce drug-seeking behavior[2][3][4][5]. In vitro studies also suggest NAC can protect astrocytes from acute cocaine toxicity via its antioxidant properties[5]. Clinical trials indicate that NAC may decrease cue-induced craving or desire for cocaine among abstinent users but does not directly antagonize acute effects of administered cocaine[2][3].

Other names
cocaine + N-acetylcysteineacetylcysteine + cocaineNAC for cocaine use disorder
02

Targets

DAT (Dopamine plasma membrane transport protein)SLC7A11 (Cystine-Glutamate Antiporter)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)GSH (Glutathione synthesis / redox)

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