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Bupivacaine 0.5% (hyperbaric)

Nazmy Edward Seif · FDA-approved active Small molecule

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

Bupivacaine is a local anesthetic that blocks sodium channels in nerve cell membranes, preventing the initiation and propagation of action potentials. Used for Spinal anesthesia for surgical procedures, Local and regional anesthesia for pain management.

At a glance

Generic nameBupivacaine 0.5% (hyperbaric)
Also known asHeavy Marcaine
SponsorNazmy Edward Seif
Drug classLocal anesthetic (amide class)
TargetVoltage-gated sodium channels
ModalitySmall molecule
Therapeutic areaAnesthesia
PhaseFDA-approved

Mechanism of action

Bupivacaine reversibly binds to and inactivates voltage-gated sodium channels on the inner surface of nerve cell membranes, thereby preventing depolarization and conduction of nerve impulses. The hyperbaric formulation (containing dextrose) increases the specific gravity of the solution, allowing it to settle dependently in the cerebrospinal fluid when used for spinal anesthesia. This property enables more predictable and localized anesthetic distribution in the subarachnoid space.

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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