Drug intelligence / Profile preview

fentanyl + lidocaine + midazolam

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

Overview

This is a combination of three pharmaceutical agents—fentanyl, lidocaine, and midazolam—used together primarily for procedural sedation and analgesia (PSA) in emergency and perioperative settings. \n- **Fentanyl** is a potent synthetic opioid analgesic that acts as an agonist at the mu-opioid receptor, providing rapid-onset pain relief. \n- **Lidocaine** is a local anesthetic and antiarrhythmic agent that blocks voltage-gated sodium channels in neuronal cell membranes, inhibiting nerve impulse conduction to provide local or regional anesthesia. \n- **Midazolam** is a short-acting benzodiazepine with sedative, anxiolytic, amnestic, and muscle relaxant properties; it acts as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor.\n\nThe combination aims to achieve effective sedation (midazolam), potent analgesia (fentanyl), and additional local anesthesia or reduction of injection pain (lidocaine). This regimen has been studied for use in procedures such as anterior shoulder dislocation reduction[1], endoscopy[2][5], and other interventions requiring deep sedation[4]. The addition of lidocaine may not always confer extra benefit over fentanyl plus midazolam alone for some indications but can be used to reduce injection pain or enhance patient comfort.

02

Targets

SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)MOR (Mu opioid receptor)

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