Drug intelligence / Profile preview

hyperbaric bupivacaine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intrathecal, Spinal
01

Overview

Hyperbaric bupivacaine is a formulation of the local anesthetic bupivacaine that is made hyperbaric (denser than cerebrospinal fluid) by the addition of dextrose. It is an amide-type local anesthetic used primarily for spinal (subarachnoid) anesthesia. The addition of dextrose increases the solution's density, allowing it to spread predictably under gravity within the intrathecal space. Hyperbaric bupivacaine acts by blocking voltage-gated sodium channels on neuronal membranes, inhibiting nerve impulse generation and conduction and thus producing loss of sensation and motor function in targeted regions. It is commonly used for surgical anesthesia in procedures such as cesarean section, lower limb surgery, abdominal surgery, and urological procedures[4][5][7]. Its onset is rapid with a long duration of action.

Brand names
Marcaine SpinalBupivacaine Spinal
Other names
hyperbaric bupivacainebupivacaine hydrochloride in dextrose injectionhyperbaric bupivacaine hydrochloride
02

Targets

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

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