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Bupivacaine + nalbuphine

Alzahraa Ahmed Abbas · FDA-approved active Small molecule

Bupivacaine provides local anesthesia by blocking sodium channels in nerve fibers, while nalbuphine provides opioid analgesia by acting as a mixed kappa agonist and mu antagonist.

Bupivacaine provides local anesthesia by blocking sodium channels in nerve fibers, while nalbuphine provides opioid analgesia by acting as a mixed kappa agonist and mu antagonist. Used for Local anesthesia with analgesia for surgical and regional anesthetic procedures.

At a glance

Generic nameBupivacaine + nalbuphine
SponsorAlzahraa Ahmed Abbas
Drug classLocal anesthetic + mixed opioid agonist-antagonist
TargetVoltage-gated sodium channels (bupivacaine); kappa and mu opioid receptors (nalbuphine)
ModalitySmall molecule
Therapeutic areaPain management, Anesthesia
PhaseFDA-approved

Mechanism of action

Bupivacaine is a long-acting amide local anesthetic that reversibly inhibits sodium influx into nerve cells, preventing depolarization and conduction of nerve impulses. Nalbuphine is an opioid analgesic that binds to kappa opioid receptors as an agonist and mu opioid receptors as an antagonist, providing pain relief with a lower abuse potential than pure mu agonists. The combination provides both local anesthetic and systemic analgesic effects for enhanced pain management.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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