Drug intelligence / Profile preview

bupivacaine + ropivacaine + levobupivacaine + lidocaine

Development stage
Unknown
Lead developer
Plastic Surgery Hospital of Chinese Academy of Medical Sciences
Modality
Small Molecules
Administration
Percutaneous, Subcutaneous, Epidural, Intrathecal
01

Overview

This entry refers to a combination of four common amide-type local anesthetics: bupivacaine, ropivacaine, levobupivacaine, and lidocaine. These agents are primarily used in regional anesthesia and analgesia to manage acute pain, particularly in the postoperative setting. They function by reversibly binding to and inactivating voltage-gated sodium channels on the internal surface of nerve cell membranes, which prevents the generation and conduction of nerve impulses. Lidocaine is typically characterized by a rapid onset and intermediate duration of action, whereas bupivacaine, ropivacaine, and levobupivacaine offer a slower onset but a significantly longer duration of effect. In clinical practice, these drugs are often utilized for specialized regional techniques such as transversus abdominis plane (TAP) blocks and rectus sheath blocks. For instance, in the clinical trial ChiCTR2200066824, local anesthetics like ropivacaine are evaluated for their ability to improve the quality of recovery in patients undergoing major procedures such as DIEP flap breast reconstruction.

02

Targets

SCN11A (NaV1.9)SCN10A (Sodium channel protein type X alpha subunit)SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN5A (Sodium channel protein type 5 subunit alpha)SCN3A (Sodium channel protein type 3 subunit alpha)SCN9A (Sodium channel protein type 9 subunit alpha)

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