Drug intelligence / Profile preview

propofol + bupivacaine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous, Intrathecal, Epidural
01

Overview

The combination of propofol and bupivacaine represents an anesthetic pairing used in clinical practice. This combination leverages synergistic effects that enhance anesthetic efficacy while potentially allowing for reduced dosing of individual components. Propofol is a sedative-hypnotic agent used for induction and maintenance of anesthesia or sedation. It works by positively modulating the inhibitory function of gamma-aminobutyric acid (GABA) through GABA-A receptors[4]. When administered intravenously, propofol produces rapid hypnosis with minimal excitation, usually within 40 seconds from injection[4]. Bupivacaine is an amide local anesthetic that provides anesthesia through blockade of nerve impulse generation and conduction. It crosses the neuronal membrane and blocks voltage-gated sodium channels at the intracellular portion of their pore-forming transmembrane segments[5]. This prevents sodium ions from passing through the channel's pore, stabilizing the membrane at rest and preventing neurotransmission[5]. Studies have shown that bupivacaine significantly enhances the hypnotic effect of propofol in a dose-dependent manner[2]. Bupivacaine-induced spinal block has been found to reduce the ED50 (median effective dose) of propofol by approximately 39%[1][2]. This enhancement is primarily attributed to reduced afferent input, though differences in potency between drugs suggest additional factors may be involved[1]. The combination allows for lower total doses of propofol compared to propofol alone, which may be beneficial in certain clinical scenarios[7]. However, research has shown variable results regarding whether this combination provides superior hemodynamic stability compared to propofol alone[7]. ## Clinical Applications This combination is used during: - Spinal anesthesia procedures - Regional anesthesia - Surgical procedures requiring both sedation and local/regional anesthesia - Procedures where reduced doses of individual agents may be beneficial ## Considerations When using this combination, clinicians should be aware that: - The dose of propofol should be modified accordingly when used with bupivacaine[2] - Recovery time may be slightly longer with the combination compared to propofol alone[7] - Both drugs can cause cardiovascular depression, though some research suggests propofol may attenuate bupivacaine-induced cardiovascular toxicity[3]

Other names
Local anesthesiaIV sedationBupivacainePropofollocal anesthesia-Memorial Sloan Kettering Cancer Center-procedural pain
02

Targets

SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)

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