Levobupivacaine Hydrochloride

For the production of local or regional anesthesia for surgery and obstetrics, and for post-operative pain management.

Levobupivacaine is a long acting local anaesthetic of the amide type. It is the S-enantiomer of bupivacaine. It blocks nerve conduction in sensory and motor nerves mainly by interacting with voltage sensitive sodium channels on the cell membrane. It also interferes with impulse transmission and conduction in other tissues. Levobupivacaine is given as the hydrochloride for infiltration anaesthesia and regional nerve blocks including epidural block. It is contraindicated in obstetric paracervical block and IV regional anaesthesia (Bier's block). The 0.75% solution is also contraindicated for epidural blocks in obstetrics.

Acute pain: Pain relief during labour: 15-50 mg (6-20 ml) of a 0.25% solution, to be given as a bolus dose; alternatively, dose may be given via continuous infusion at 5-12.5 mg (4-10 ml) per hr using 0.125% solution or 5-12.5 mg (8-20 ml) per hr using 0.0625% solution.

Postoperative pain: 10-25 mg (4-10 ml) per hr of a 0.25% solution, 12.5-18.75 mg (10-15 ml) per hr of a 0.125% solution or 12.5-18.75 mg (20-30 ml) per hr of a 0.0625% solution; dose may be given as an epidural infusion. Max: 150 mg/dose; 400 mg/day.

Peripheral nerve block: 2.5-150 mg or 1-2 mg/kg (0.4 ml/kg) of a 0.25 or 0.5% solution. Not to exceed 40 ml. Max: 150 mg/dose; 400 mg/day.

Surgical anaesthesia: Epidural block: 50-100 mg (10-20 ml) of a 0.5% solution or 75-150 mg (10-20 ml) of a 0.75% solution. Caesarean section: 75-150 mg (15-30 ml) of a 0.5% solution. Spinal block: 15 mg (3 ml) of a 0.5% solution. Max: 150 mg/dose; 400 mg/day.

Infiltration anaesthesia:

• Adult: Up to 150 mg (60 ml) of a 0.25% solution. For peribulbar block in ophth procedures: 37.5-112.5 mg (5-15 ml) of a 0.75% solution. Max: 150 mg/dose; 400 mg/day.
• Child: For ilioinguinal or iliohypogastric blocks in children <12 yr: 0.625-2.5 mg/kg (0.25-0.5 ml/kg) of a 0.25 or 0.5% solution.

Plasma levels may be reduced when used with enzyme-inducing drugs such as rifampicin. Substrates for or inhibitors of CYP3A4 and CYP1A2 may affect the plasma levels of levobupivacaine.

Not to be used in IV regional anesth (Bier's block) and paracervical block in obstetrics. Do not use 0.75% solution for epidural block in obstetrics. Hypovolaemia, complete heart block.

CNS effects such as restlessness, anxiety, dizziness, confusion, respiratory depression and convulsions. Neuromuscular and skeletal weakness, blurred vision, pupillary constriction, tinnitus. Hypotension, bradycardia and CV collapse which may lead to cardiac arrest. Rarely, hypersensitivity reactions.

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Epilepsy, respiratory impairment, impaired cardiac conduction, bradycardia, severe shock, acute porphyria, myasthenia gravis, renal or hepatic impairment. Pregnancy, lactation. Reduce dose in elderly or debilitated patients. Resuscitative equipment should be available. Do not use solutions containing adrenaline for anesth in appendages. Do not use solutions containing preservatives for caudal or epidural block.

Regional anesthesia.

To be used immediately after opening. After dilution in normal saline: Chemical and physical in-use stability at 20-22°C for 7 days.