Drug intelligence / Profile preview

diphenhydramine + lorazepam

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Combination of diphenhydramine and lorazepam, two centrally acting small molecule drugs. Diphenhydramine is a first-generation antihistamine that acts as an inverse agonist at the histamine H1 receptor, also antagonizes muscarinic acetylcholine receptors, and inhibits sodium channels. It is widely used for allergies, insomnia, and as an antiemetic and antiparkinson agent[4][7]. Lorazepam is a benzodiazepine that acts as a positive allosteric modulator at the GABA-A receptor, producing anxiolytic, sedative, anticonvulsant, and muscle relaxant effects[2][6][8]. The combination is not marketed under a unique brand name but has been studied experimentally for short-term treatment of insomnia and acute agitation, with reported increased sedation and risk of additive central nervous system depression[1][3][5].

Other names
diphenhydramine and lorazepam
02

Targets

BZD site (GABA-A receptor benzodiazepine site)mAChR (Muscarinic acetylcholine receptors)NaV (Voltage-gated sodium channels)HRH1 (Histamine H1 Receptor)

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