Drug reference

Bupivacaine

Local Anesthetic · Anaesthesia

Also known as bupivacaine hydrochloride

Local AnestheticAnaesthesia

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

1 major

SEVERE in our sources

PREGNANCY

Crosses the placenta but not known to be

FDA category + note

Top interactions

PrilocaineSevereDatabaseDDInter

Mechanism

Bupivacaine is an amide-type local anesthetic employed to induce analgesia, exemplified by its use in epidural blocks for pain relief. Administered via epidural routes, its action results in clinical consequences such as motor blockade.

Indications

Local anesthetic of long duration for various applicationsProlonged analgesia during labor or the postoperative periodSurgical proceduresinfiltration and retrobulbar block anesthesiaInfiltrationNerve blockEpidural anaesthesia (long duration)Spinal anaesthesia (long duration)Obstetrics (analgesia during vaginal delivery)Postoperative pain relief (continuous epidural infusion)

Dosing

Adult: When used as a local anaesthetic, large doses can cause fetal bradycardia; if given during delivery can also cause neonatal respiratory depression, hypotonia, or bradycardia after paracervical or epidural block. l BREAST FEEDING Present in milk but amount too small to be harmful. l HEPATIC IMPAIRMENT Manufacturer advises caution (risk of increased exposure).…

Pharmacokinetics

Onset

Intermediate

Duration

120–360 min

Protein binding

Bound to α1 acid glycoprotein in plasma.

Metabolism

Primarily metabolized in the liver by CYP3A4 to pipecolylxylidine, which is then glucuronidated and excreted.

Contraindications

Should not be used for intravenous regional analgesia (due to cardiotoxicity).
0.75% concentration for epidural anaesthesia during labour is contraindicated (due to risk of cardiac arrest).

Side effects

Common

Sensory block at much lower concentration than needed for motor blockMore vasodilatory than lidocaineHighest local tissue irritancy

Serious

More cardiotoxic than equieffective doses of lidocaine
Severe ventricular arrhythmias and myocardial depression after inadvertent intravascular administration
Cardiac toxicity enhanced by coexisting acidosis, hypercarbia, and hypoxemia
allergic reactions
globe perforation
hemorrhage
inadvertent vascular and subdural injections
Relatively more cardiotoxic
Prolongs QTc interval
Induces ventricular tachycardia
Induces fibrillation
Cardiac depression