Drug intelligence / Profile preview

diazepam + haloperidol

Development stage
Unknown
Lead developer
Roche
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Diazepam + haloperidol is a combination of two pharmaceutical drugs, diazepam and haloperidol. Diazepam is a benzodiazepine that acts as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA(A)) receptor, enhancing the inhibitory effects of GABA in the central nervous system. It is primarily used for anxiety, muscle spasms, alcohol withdrawal symptoms, and as an adjunct in certain types of seizures[5][8]. Haloperidol is a first-generation (typical) antipsychotic that exerts its primary effect by antagonizing dopamine D2 receptors in the brain, particularly within mesolimbic and mesocortical pathways. It is mainly indicated for schizophrenia and other psychotic disorders but also used for agitation and severe behavioral problems[3][6][9]. The combination may be used acutely to manage agitation or psychosis with comorbid anxiety or severe behavioral disturbance; however, it increases risks such as CNS depression (drowsiness, confusion), dizziness, and impaired concentration due to additive sedative effects[2][7]. Studies indicate complex changes in GABA(A) receptor binding when both drugs are administered together[1].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)ADRA1A (α1A)GABRR (GABA-A receptor subunit rho)DRD2 (Dopamine D2 Receptor)

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