Drug intelligence / Profile preview

ropivacaine

Development stage
Approved
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Epidural, Intrathecal, Peripheral Nerve Block, Field Block, Local Infiltration, Fascial Plane Block, Intraperitoneal, Intramuscular
01

Overview

Ropivacaine is a long-acting amide-type local anesthetic, primarily available as the pure S-enantiomer. It acts by reversibly blocking sodium ion influx through voltage-gated sodium channels in nerve cell membranes, thereby inhibiting nerve impulse conduction and producing local anesthesia and analgesia. Compared to bupivacaine, ropivacaine has lower lipid solubility and reduced cardiotoxicity, making it safer for use in regional anesthesia including epidural, spinal (subarachnoid), peripheral nerve blocks, and infiltration anesthesia. It is widely used for surgical anesthesia as well as acute pain management such as postoperative or labor analgesia[1][2][4][5]. The drug was developed to provide a safer alternative to bupivacaine after reports of cardiac arrest associated with the latter[1][2]. Ropivacaine’s clinical advantages include sensory-motor separation at low concentrations (providing analgesia with minimal motor block) and frequency-dependent blockade favoring C-fibers over A-fibers[2].

Brand names
Naropin
Other names
罗哌卡因Ropivacaine hydrochloride盐酸罗哌卡因
02

Targets

SCN10A (Sodium channel protein type X alpha subunit)NaV alpha (Voltage-gated sodium channel alpha subunit family)

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