Drug intelligence / Profile preview

ropivacaine + bupivacaine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Epidural, Intrathecal, Local Infiltration, Perineural
01

Overview

Ropivacaine + bupivacaine is a combination of two long-acting amide-type local anesthetics used primarily for regional anesthesia, including surgical anesthesia and pain management in procedures such as labor or postoperative care. Both drugs act by reversibly inhibiting sodium ion influx through voltage-gated sodium channels in neuronal membranes, thereby blocking nerve impulse conduction and producing loss of sensation. Ropivacaine is the S(-) enantiomer derived from propivacaine and is less lipophilic than bupivacaine, resulting in a greater degree of sensory-motor differentiation and reduced risk of cardiotoxicity. Bupivacaine provides potent local anesthesia with a higher tendency for motor blockade compared to ropivacaine. When combined, these agents may exhibit additive or synergistic effects on sensory and motor block duration while maintaining hemodynamic stability[1][4][5][8]. This combination is sometimes used to optimize the onset, duration, and quality of regional blocks.

Other names
ropivacaine hydrochloridebupivacaine hydrochloride
02

Targets

SCN10A (Sodium channel protein type X alpha subunit)SCN5A (Sodium channel protein type 5 subunit alpha)KCNA5 (Ultra-rapid delayed rectifier potassium channel)CaV (Voltage-gated calcium channel protein complex)

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