Drug intelligence / Profile preview

fentanyl + nefopam + ramosetron

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

Overview

This is a combination drug consisting of three active pharmaceutical ingredients: - **Fentanyl**: A potent synthetic opioid analgesic that acts primarily as a mu-opioid receptor agonist, providing strong pain relief. - **Nefopam**: A centrally acting, non-opioid, non-steroidal analgesic. Its mechanism involves inhibition of the synaptosomal reuptake of serotonin, norepinephrine, and dopamine in the central nervous system, contributing to its antinociceptive effects. - **Ramosetron**: A selective serotonin 5-HT3 receptor antagonist used as an antiemetic for the prevention and treatment of postoperative nausea and vomiting (PONV). It blocks 5-HT3 receptors in both the central nervous system and gastrointestinal tract. This combination is typically used in intravenous patient-controlled analgesia (IV PCA) settings for postoperative pain management. Fentanyl provides opioid-based analgesia; nefopam offers additional non-opioid pain control with possible opioid-sparing effects; ramosetron reduces the risk of opioid-induced nausea and vomiting[1][4][9]. The mixture has been shown to be physically stable when combined for IV administration[4]. There is no evidence suggesting significant pharmacodynamic antagonism between nefopam’s serotonergic activity and ramosetron’s 5-HT3 antagonism[1][5].

02

Targets

SERT (Sodium-dependent serotonin transporter)HTR3A (5-hydroxytryptamine receptor 3A)DAT (Dopamine plasma membrane transport protein)MOR (Mu opioid receptor)NET (Norepinephrine Transporter)

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