Drug intelligence / Profile preview

fentanyl + nefopam

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Intravenous
01

Overview

Fentanyl + nefopam is a combination of two analgesic drugs used primarily for postoperative pain management, often administered via intravenous patient-controlled analgesia (IV-PCA). Fentanyl is a potent synthetic opioid agonist that acts primarily on the mu-opioid receptor to provide strong analgesia. Nefopam is a non-opioid, non-steroidal, centrally acting analgesic that inhibits the reuptake of serotonin, norepinephrine, and dopamine and also exhibits NMDA receptor antagonism. The combination aims to achieve effective pain control while reducing the required dose of fentanyl, thereby minimizing opioid-related adverse effects such as respiratory depression and sedation. Clinical studies have shown that co-administration allows for significant reduction in total fentanyl consumption without compromising analgesic efficacy[1][2][3][4][5]. Nefopam may also offer advantages over NSAIDs due to its lack of effect on platelet aggregation or renal function[1][4].

02

Targets

DAT (Dopamine plasma membrane transport protein)MOR (Mu opioid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)

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