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Bupivacaine (Hyperbaric 0.5%)

Guy's and St Thomas' NHS Foundation Trust · FDA-approved active Small molecule

Bupivacaine is a local anesthetic that blocks sodium channels in nerve cell membranes, preventing the initiation and conduction of nerve impulses.

Bupivacaine is a local anesthetic that blocks sodium channels in nerve cell membranes, preventing the initiation and conduction of nerve impulses. Used for Spinal anesthesia for surgical procedures, Regional anesthesia for pain management.

At a glance

Generic nameBupivacaine (Hyperbaric 0.5%)
Also known asHeavy bupivacaine 0.5%, heavy marcaine 0.5%
SponsorGuy's and St Thomas' NHS Foundation Trust
Drug classLocal anesthetic
TargetVoltage-gated sodium channels
ModalitySmall molecule
Therapeutic areaAnesthesia
PhaseFDA-approved

Mechanism of action

Bupivacaine reversibly binds to and blocks voltage-gated sodium channels on the inner surface of nerve cell membranes, preventing depolarization and action potential propagation. The hyperbaric formulation (suspended in dextrose) is denser than cerebrospinal fluid, allowing it to settle dependently in the spinal canal for targeted regional anesthesia. This results in loss of sensation and motor function in the anesthetized region.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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