Drug intelligence / Profile preview

bupivacaine + dexmedetomidine

Development stage
Unknown
Lead developer
Yonsei University
Modality
Small Molecules
Administration
Intrathecal
01

Overview

bupivacaine + dexmedetomidine is a combination drug regimen used for spinal anesthesia, specifically studied by Yonsei University for elderly patients undergoing transurethral resection of the prostate (TURP) due to benign prostatic hyperplasia. Bupivacaine is a long-acting amide-type local anesthetic that functions by binding to and blocking voltage-gated sodium channels on the internal surface of nerve cell membranes, thereby preventing the influx of sodium ions and the subsequent propagation of action potentials. Dexmedetomidine is a highly selective alpha-2 adrenergic receptor agonist that, when administered intrathecally as an adjuvant, acts on receptors in the dorsal horn of the spinal cord to inhibit the release of nociceptive neurotransmitters and hyperpolarize neurons. This combination is designed to provide high-quality sensory and motor blockade with a lower dose of bupivacaine, which helps maintain hemodynamic stability and reduces the incidence of opioid-related side effects such as pruritus and nausea in the geriatric population.

Other names
intrathecal dexmedetomidine and bupivacaineDXM-low-dose bupivacaine
02

Targets

ADRA2C (α2C)NeuraminidaseADRA2A (α2A)ADRA2B (α2B)NaV (Voltage-gated sodium channels)

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