Drug intelligence / Profile preview

chlordiazepoxide + zolpidem + trazodone + tramadol + tapentadol + buprenorphine

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Transdermal, Intravenous, Intramuscular, Sublingual
01

Overview

This is a **combination drug** composed of six active pharmaceutical ingredients: **chlordiazepoxide** (a benzodiazepine anxiolytic), **zolpidem** (a non-benzodiazepine hypnotic), **trazodone** (a serotonin modulator and antidepressant), **tramadol** (an opioid analgesic with serotonergic and noradrenergic effects), **tapentadol** (an opioid analgesic with norepinephrine reuptake inhibition), and **buprenorphine** (a mixed opioid agonist-antagonist). - Chlordiazepoxide acts primarily as a positive allosteric modulator at the GABA-A receptor, producing anxiolytic and sedative effects[1]. - Zolpidem selectively binds to the GABA-A receptor alpha1 subunit, inducing sedation. - Trazodone inhibits serotonin reuptake and antagonizes various serotonin receptors, used primarily for depression and insomnia. - Tramadol is a weak mu-opioid receptor agonist and inhibits reuptake of norepinephrine and serotonin, used for moderate pain[2][3][6][8]. - Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor, indicated for moderate to severe pain[2][3][5][6]. - Buprenorphine is a partial agonist at the mu-opioid receptor, antagonist at kappa- and delta-opioid receptors, used in pain management and opioid dependence[5]. This combination has no known approved medicinal use and would present a high risk of synergistic central nervous system depression, serotonin syndrome, respiratory depression, and other potentially fatal interactions.

02

Targets

ADRA1A (α1A)GABRR (GABA-A receptor subunit rho)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)SERT (Sodium-dependent serotonin transporter)DOR (Opioid Receptor Delta 1)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)NOP (Nociceptin/orphanin FQ peptide receptor)NET (Norepinephrine Transporter)

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