Drug intelligence / Profile preview

prilocaine + fentanyl

Development stage
Unknown
Lead developer
Cairo University
Modality
Small Molecules
Administration
Intrathecal
01

Overview

The combination of prilocaine and fentanyl is an investigational anesthetic regimen being studied for spinal anesthesia in geriatric patients. Prilocaine is a small molecule local anesthetic of the amide type that functions by binding to and inhibiting voltage-gated sodium channels on the internal surface of nerve cell membranes. This action prevents the influx of sodium ions, thereby blocking the initiation and conduction of nerve impulses and resulting in local anesthesia. Fentanyl is a potent synthetic opioid analgesic that acts primarily as an agonist at the mu-opioid receptor (MOR). When administered intrathecally alongside a local anesthetic, fentanyl provides synergistic analgesia, potentially improving the quality of the sensory block and allowing for a reduction in the dose of the local anesthetic, which is particularly beneficial in elderly populations to minimize hemodynamic instability. This specific combination, utilizing hyperbaric prilocaine 2% (Takipril), is being evaluated by Cairo University in various dosing cohorts (30 mg, 40 mg, and 50 mg of prilocaine with 25 µg of fentanyl) for day-case lower abdominal and urologic surgeries.

Other names
pilocaine + fentanylintrathecal prilocaine and fentanylprilocaine hydrochloride + fentanyl
02

Targets

MOR (Mu opioid receptor)NaV (Voltage-gated sodium channels)

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