Drug intelligence / Profile preview

bupivacaine + naloxone

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intrapleural, Intrathecal, Perineural
01

Overview

Bupivacaine + naloxone is a combination of two drugs used primarily as an adjuvant in regional anesthesia and analgesia. Bupivacaine is a long-acting amide local anesthetic that works by blocking voltage-gated sodium channels on neuronal membranes, thereby inhibiting nerve impulse conduction and producing local or regional anesthesia. Naloxone is an opioid receptor antagonist, traditionally used to reverse opioid overdose, but at ultra-low doses it has been shown to prolong the duration of neural blockade when added to local anesthetics like bupivacaine. The addition of low-dose naloxone to bupivacaine in peripheral nerve blocks (such as supraclavicular brachial plexus block) or intrapleural/intrathecal analgesia can significantly extend the duration of sensory and motor block without increasing adverse effects[1][8]. This combination is not marketed under a unique brand name but may be prepared for use in specific clinical settings.

02

Targets

SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)MOR (Mu opioid receptor)

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