Drug intelligence / Profile preview

bupivacaine + epinephrine + saline

Development stage
Unknown
Lead developer
Pfizer
Modality
Implantable Devices → Device-based Delivery → Drug Delivery Systems, Small Molecules, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Infiltration, Peripheral Nerve Block, Epidural
01

Overview

Bupivacaine + epinephrine + saline is a combination injectable solution used primarily for local or regional anesthesia. Bupivacaine is an amide-type local anesthetic that blocks nerve impulse transmission by inhibiting voltage-gated sodium channels, resulting in loss of sensation and pain relief. Epinephrine (adrenaline) acts as a vasoconstrictor, prolonging the duration of anesthesia by reducing systemic absorption of bupivacaine and minimizing bleeding at the injection site. Saline serves as the diluent to achieve appropriate volume and concentration for clinical use. This combination is commonly administered via infiltration, peripheral nerve block, or epidural routes during surgical procedures, dental work, obstetric interventions (excluding paracervical block), and acute pain management[1][4][5][6][7]. The addition of epinephrine allows for higher doses of bupivacaine with reduced risk of systemic toxicity due to slower absorption[1][5].

02

Targets

ADRB1 (β1)ADRA1A (α1A)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)PTGER1 (Prostaglandin E Receptor 1)

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