Drug intelligence / Profile preview

Hydromorphone + naloxone

Development stage
Unknown
Lead developer
Knoll
Modality
Small Molecules
Administration
Oral, Intravenous, Intranasal
01

Overview

Hydromorphone + naloxone is a fixed-dose combination of two drugs used primarily for pain management and to reduce the risk of opioid-induced side effects. Hydromorphone is a potent opioid analgesic that acts as an agonist at mu-opioid receptors, providing strong pain relief but also carrying risks such as respiratory depression, sedation, and dependence[1][6][8]. Naloxone is an opioid antagonist that binds to opioid receptors without activating them, thereby blocking or reversing the effects of opioids like hydromorphone[2][5]. When combined in a single formulation (often in oral tablets), naloxone has minimal systemic effect when taken as directed (due to low oral bioavailability), but if the combination is misused by injection or other non-oral routes, naloxone can precipitate withdrawal and block euphoric effects. This discourages abuse while allowing effective pain control when used properly. The primary indication for this combination is severe pain requiring long-term opioid treatment with reduced risk of misuse.

Other names
hydromorphone/naloxonehydromorphone hydrochloride + naloxone hydrochloride
02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)FLNA (Filamin A)

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