Drug intelligence / Profile preview

levobupivacaine + epinephrine

Development stage
Phase 4
Lead developer
UCB
Modality
Small Molecules
Administration
Epidural, Infiltration, Perineural, Intrathecal, Subcutaneous
01

Overview

Levobupivacaine + epinephrine is a combination of two agents used for local or regional anesthesia. Levobupivacaine is the S(-)-enantiomer of bupivacaine, an amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, thereby inhibiting nerve impulse conduction and producing loss of sensation in the targeted area. Epinephrine (adrenaline) is a vasoconstrictor that acts on alpha- and beta-adrenergic receptors; when combined with local anesthetics like levobupivacaine, it constricts blood vessels at the injection site, reducing systemic absorption of the anesthetic, prolonging its effect, and decreasing peak plasma concentrations. This combination is commonly used to provide anesthesia for surgical procedures, labor analgesia, dental work, and other interventions requiring localized numbness[1][4][6]. The addition of epinephrine does not significantly alter block characteristics or duration but reduces systemic exposure to levobupivacaine[1].

Other names
levobupivacaine and epinephrinelevobupivacaine with epinephrinelevobupivacaine and adrenaline
02

Targets

ADRA1A (α1A)ADRA2A (α2A)β-AR (Beta-adrenergic receptor family)ADRB3 (β3)SCN5A (Sodium channel protein type 5 subunit alpha)ADRA1 (Alpha-1 adrenergic receptor family)ADRB1 (β1)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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