Drug intelligence / Profile preview

pethidine + haloperidol

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Intravenous (based On Individual Drug Routes; Combinations May Be Administered Parenterally Especially In Hospital/palliative Settings)[3][6]
01

Overview

Pethidine + haloperidol is a combination of two pharmaceutical drugs, pethidine (also known as meperidine) and haloperidol. Pethidine is an opioid analgesic primarily used for the relief of moderate to severe pain, acting mainly as a mu-opioid receptor agonist to inhibit pain signaling in the central nervous system. Haloperidol is a first-generation (typical) antipsychotic that acts predominantly as an antagonist at dopamine D2 receptors in the brain, reducing dopaminergic neurotransmission and thereby exerting antipsychotic and antiemetic effects[1][3][5]. The combination has been used off-label for its sedative properties, particularly in settings such as palliative care or during childbirth to manage agitation, anxiety, or nausea alongside pain control. The sedative effects of both drugs are potentiated when combined, which can increase both efficacy and risk[9].

02

Targets

DRD4 (Dopamine D4 Receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)SIGMAR1 (Sigma non-opioid intracellular receptor 1)DRD1 (Dopamine D1 Receptor)MOR (Mu opioid receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)

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