Bupivacaine is indicated for producing local or regional anesthesia or analgesia in surgical procedures, oral surgery, diagnostic and therapeutic procedures, and obstetrical procedures.

Routes of administration and concentrations:

• Local infiltration: 0.25%
• Peripheral nerve block: 0.25%, 0.5%
• Sympathetic block: 0.25%
• Lumbar epidural: 0.25%, 0.5% and 0.75% (non-obstetrical use)
• Caudal block: 0.25%, 0.5%

Bupivacaine Hydrochloride is an amide-type local anesthetic with a relatively slow onset but a prolonged duration of action (approximately 8 hours). It produces effective sensory anesthesia along with motor blockade. It works by blocking the generation and transmission of nerve impulses by inhibiting depolarization and ion exchange in nerve fibers. These effects are reversible. Bupivacaine is highly protein-bound (about 95%). The elimination half-life ranges from 1.5 to 5.5 hours in adults and approximately 8 hours in neonates.

Each 30 ml contains 150 mg Bupivacaine Hydrochloride (anhydrous) USP.

The dose of any local anaesthetic administered varies with the anaesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked. In recommended doses, Bupivacaine produces complete sensory block, but the effect on motor function differs among the three concentrations.

0.25% when used for caudal, epidural, or peripheral nerve block, produces incomplete motor block. Should be used for operations in which muscle relaxation is not important, or when another means of providing muscle relaxation is used concurrently. Onset of action may be slower than with the 0.5% or 0.75% solutions.

0.5% provides motor blockade for caudal, epidural, or nerve block, but muscle relaxation may be inadequate for operations in which complete muscle relaxation is essential.

Maximum dosage limit must be individualized in each case after evaluating the size and physical status of the patient, as well as the usual rate of systemic absorption from a particular injection site. Most experience to date is with single doses of Bupivacaine up to 175 mg. These doses may be repeated up to once every three hours. In clinical studies to date, total daily doses up to 400 mg have been reported. Until further experience is gained, this dose should not be exceeded in 24 hours.

The following dosages have generally proved satisfactory and are recommended as a guide for use in the average adult. These dosages should be reduced for young, elderly or debilitated patients.

• Local Infiltration: 0.25%: up to max (mg)
• Epidural: 0.5%: 50–100 mg
• Epidural: 0.25%: 25–50 mg
• Caudal: 0.5%: 75–150 mg
• Caudal: 0.25%: 37.5–75 mg
• Peripheral Nerves: 0.5%: 25 mg to max.
• Peripheral Nerves: 0.25%: 12.5 mg to max.
• Sympathetic 0.25%: 50–125 mg

Bupivacaine should be used cautiously in patients receiving other local anesthetics or drugs structurally similar to amide-type anesthetics (e.g., antiarrhythmic agents like lidocaine and mexiletine), as their systemic toxic effects may be additive. Specific interaction studies with class III antiarrhythmic drugs (e.g., amiodarone) have not been conducted; therefore, caution is advised when used together.

Known hypersensitivity to Bupivacaine, other amide-type local anesthetics, or any component of these formulations is a contraindication. Its use in intravenous regional anesthesia is contraindicated, and it should not be used for obstetrical paracervical block anesthesia.

Central Nervous System: Restlessness, anxiety, nervousness, dizziness, tinnitus, blurred vision, pupil constriction (miosis), nausea, vomiting, numbness around the mouth, chills, tremors, muscle twitching, and seizures.

Cardiovascular System: Myocardial depression, peripheral vasodilation leading to hypotension, bradycardia, ventricular arrhythmias, and cardiac arrest.

Hypersensitivity Reactions: Urticaria, itching, redness, angioedema, tachycardia, sneezing, nausea, vomiting, dizziness, fainting, excessive sweating, fever, and in rare cases, anaphylactoid reactions.

Bupivacaine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised when administering to breastfeeding mothers.

Local anaesthetics should be administered only by clinicians who are experienced in diagnosing and managing dose-related toxicity and other acute emergencies that may arise from the intended block. This should be done only after ensuring the immediate availability of oxygen, resuscitative medications, cardiopulmonary resuscitation equipment, and trained personnel required to manage toxic reactions and related emergencies.

Caution should be exercised when administering to elderly patients, debilitated individuals, and children, as well as to patients with epilepsy, impaired cardiac conduction, shock, liver impairment, and myasthenia gravis.

The minimum effective dose of local anaesthetic should be used to achieve adequate anaesthesia in order to prevent high plasma concentrations and serious adverse effects. Rapid injection of large volumes should be avoided; instead, incremental (fractional) dosing is recommended whenever possible.

Continuous and careful monitoring of cardiovascular and respiratory functions (including adequacy of ventilation), along with the patient’s level of consciousness, should be maintained after each administration of local anaesthetic. Due to the risk of systemic adverse effects from rapid absorption, local anaesthetics should not be injected into inflamed or infected tissues and should not be applied to damaged mucosal surfaces.

Children: Use in children under 12 years is not recommended until sufficient clinical experience is available.

Regional anesthesia

Store in a cool and dry place, protected from light. Keep out of reach of children.