Drug intelligence / Profile preview

mepivacaine + bupivacaine

Development stage
Phase 4
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Epidural, Perineural, Local Infiltration
01

Overview

Mepivacaine + bupivacaine is a combination of two amide-type local anesthetics used to achieve regional or local anesthesia, particularly in procedures requiring both rapid onset and prolonged duration of nerve block. Mepivacaine provides a relatively fast onset and intermediate duration, while bupivacaine offers a slower onset but longer-lasting effect. When mixed, the combination aims to provide the rapid onset characteristic of mepivacaine with an extended duration closer to that of bupivacaine alone. Both drugs act by reversibly blocking voltage-gated sodium channels on neuronal membranes, thereby inhibiting nerve impulse propagation and producing loss of sensation in the targeted area[1][2][3][4][6]. This mixture is commonly used for peripheral nerve blocks (e.g., interscalene brachial plexus block) and caudal blocks in pediatric patients[1][2]. The combination has been shown to result in an intermediate duration of analgesia compared to either drug alone[1].

Other names
mepivacaine/bupivacaine mixture
02

Targets

ORM1 (Alpha-1-acid glycoprotein 1)Kir (Inward-rectifier potassium channels)NaV alpha (Voltage-gated sodium channel alpha subunit family)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)

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