Last reviewed 2026-05-13 · How we verify

Bupivacaine Hydrochloride

Bupivacaine blocks nerve impulse generation and conduction by increasing electrical excitation threshold and slowing action potential rise.

Bupivacaine is an amide-type local anesthetic that blocks nerve impulses by increasing electrical excitation threshold and slowing action potential propagation, with a half-life of 2.7 hours and high protein binding of 95%. It is indicated for local or regional anesthesia in adults for surgery, dental procedures, and obstetrical procedures, but is contraindicated for obstetrical paracervical block and intravenous regional anesthesia due to serious fetal and cardiac risks. Major drug interactions exist with monoamine oxidase inhibitors, tricyclic antidepressants, ergot-type oxytocic drugs, nonselective beta-blockers, and potent inhalation anesthetics, requiring careful patient monitoring and avoidance of concurrent use. The drug's clinical utility is balanced against significant risks of systemic toxicity, cardiac arrest, and methemoglobinemia, necessitating careful dose selection and administration technique.

At a glance

Mechanism of action

Bupivacaine blocks the generation and conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. The progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers, with the clinical order of loss of nerve function being: pain, temperature, touch, proprioception, and skeletal muscle tone. Epinephrine is a vasoconstrictor added to bupivacaine to slow absorption into the general circulation and thus prolong maintenance of an active tissue concentration.

Approved indications

• Anesthesia for cesarean section
• Itching of skin
• Local Anesthesia for Ophthalmologic Procedure
• Local anesthesia
• Local anesthetic intrathecal block
• Major Nerve Block for Surgery
• Minor Skin Wound Pain
• Regional Anesthesia for Labor Pain
• Regional Anesthesia for Ophthalmologic Surgery
• Regional Anesthesia for Postoperative Pain
• Regional Anesthesia for Surgery
• Skin irritation

Boxed warnings

• WARNING: RISK OF CARDIAC ARREST WITH USE OF BUPIVACAINE HYDROCHLORIDE INJECTION IN OBSTETRICAL ANESTHESIA There have been reports of cardiac arrest with difficult resuscitation or death during use of Bupivacaine Hydrochloride Injection for epidural anesthesia in obstetrical patients. In most cases, this has followed use of the 0.75% (7.5 mg/mL) concentration. Resuscitation has been difficult or impossible despite apparently adequate preparation and appropriate management. Cardiac arrest has occu

Common side effects

• Local burning or blistering
• Any potential or definitive local anesthetic systemic toxicity or symptoms (LAST)
• Nausea and vomiting
• Dizziness
• Arrythmias
• Confusion or tremors
• Mental clouding
• Edema, erythema, pruritis, or irritation at site of injection
• Pruritis

Drug interactions

• Local Anesthetics
• Monoamine Oxidase Inhibitors and Tricyclic Antidepressants
• Ergot-Type Oxytocic Drugs
• Nonselective Beta-Adrenergic Antagonists
• Drugs Associated with Methemoglobinemia
• Potent Inhalation Anesthetics

Patents

Primary sources

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Competitive intelligence

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