Drug intelligence / Profile preview

levobupivacaine + clonidine

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Epidural, Perineural
01

Overview

Levobupivacaine + clonidine is a combination of two drugs used primarily as an adjunct for regional anesthesia and postoperative analgesia. Levobupivacaine is a long-acting amide-type local anesthetic, the S-enantiomer of bupivacaine, which blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse conduction and providing sensory and motor block. Clonidine is an alpha-2 adrenergic receptor agonist that enhances analgesia by inhibiting nociceptive neurotransmission in the dorsal horn of the spinal cord and reducing sympathetic outflow. When combined, clonidine potentiates the analgesic effects of levobupivacaine, prolongs duration of action, reduces opioid requirements postoperatively, and may improve overall pain control compared to either agent alone[1][2][6]. This combination has been studied for epidural infusions (e.g., after hip replacement), peripheral nerve blocks (e.g., brachial plexus or pudendal block), and paravertebral blocks for various surgical procedures[1][2][3][6]. The main indications are perioperative pain management in adults undergoing major surgery.

Other names
clonidine and levobupivacaineclonidine/levobupivacaine
02

Targets

ADRA2A (α2A)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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