PHARMACOLOGICAL ACTION: Regibloc (Bupivacaine) is a long acting local anaesthetic with an intermediate, to slow onset of action. Regibloc (Bupivacaine) blocks conduction by decreasing or preventing the large transient increase in the permeability of the membrane to sodium ions, by means of a slight depolarization of the membrane. The permeability of a resting nerve to both potassium and sodium ions is reduced. Regibloc (Bupivacaine) penetrates the tissues as an unprotonated amine. Regibloc (Bupivacaine) is not detoxified by plasma esterases; detoxification takes place in liver via conjugation with glucoronic acid. It is extensively bound to plasma proteins and foetal concentrations are lower than maternal concentrations because of the lower circulation distribution and rapid removal.
INDICATIONS: Regional nerve block including conduction anaesthesia when a prolonged effect is required.
CONTRA-INDICATIONS: Patients with known sensitivity to Regibloc (Bupivacaine). It should not be used extensively in patients with severe hepatic damage. Exercise caution in cases of myasthenia gravis or epilepsy. Regibloc (Bupivacaine) is not indicated for intravenous regional anaesthesia. Techniques such as epidural anaesthesia should not be used in patients with cerebrospinal diseases.
WARNINGS: Using Regibloc (Bupivacaine) to produce paracervical block during labour, especially continuous block, is not recommended as serious foetal bradycardia may be produced.
Always have resuscitation equipment and medication at hand when Regibloc (Bupivacaine) is used. The inadvertent intravenous injection or infiltration of Regibloc (Bupivacaine) may cause cardiac arrest and convulsions. It is not recommended for children under 12 years of age.
DOSAGE AND DIRECTIONS FOR USE: Dose depends on the site to be anaesthetised, the area thereof and the technique employed. Normally single doses are sufficient. The total dose administered over a period of 4 hours should not exceed 2 mg per kg body-mass, i.e. 20 to 30 mL of the 0,5% m/v Injection or 150 mg Regibloc (Bupivacaine) for adults.
Regional never block: 5 to 30 mL
Surgical procedures lumbar epidural block: 15 to 20 mL
Doses should be reduced in elderly or debilitated patients.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS: Caution should be exercised in the presence of cardiac conduction disorders, heart block and hepatic insufficiency. Regibloc (Bupivacaine) should also be used with caution in patients with epilepsy and impaired respiratory function. Allergic reactions, idiosyncratic and vasovagal attacks may occur with Regibloc (Bupivacaine).
The main systemic toxic effects are excitation of the central nervous system manifested by yawning, restlessness, excitement, nervousness, dizziness, blurred vision, nausea, vomiting, muscle twitching, spinal headache and convulsions. Excitation might be transient and followed by depression, drowsiness, respiratory failure and coma. There is simultaneous depression of the cardiovascular system with pallor, vasodilation, sweating and hypotension. Arrhythmia and cardiac arrest may be precipitated by overdosage.
Any unused portion should be discarded. If the solution contains a precipitate or is discoloured it should not be used.
Severe systemic side-effects may occur when Regibloc (Bupivacaine) is accidentally injected intravascularly. Spinal anaesthetics should be used with caution in patients with impaired cardiovascular function such as severe disturbances of cardiac rhythm, shock, heart block or congestive heart failure. Careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness is advised. Convulsions and cardiovascular collapse, that may be dose-related, may result from diminished tolerance and/or rapid absorption from the injection site.
Adverse neurologic effects following spinal anaesthesia may include impaired perineal sensation and sexual function, persistent anaesthesia, paraesthesia, weakness and paralysis of the lower extremities, and loss of sphincter control, (all of which may have slow, incomplete, or no recovery) hypotension, high or total spinal block, urinary retention, headache, backache, septic meningitis, meningismus, arachnoiditis. Slowing of labour, increased incidence of forceps delivery; shivering; cranial nerve palsies due to traction on nerves (from loss of cerebrospinal fluid), and faecal and urinary incontinence. Allergic type reactions may occur as a result of sensitivity to local anaesthetics.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: See Side-effects and Special Precautions. Numbness of the tongue and perioral region is an early sign of toxicity. Serious foetal bradycardia may occur. Overdosage should be treated symptomatically and supportive. However, resuscitation equipment and medication should always be at hand for emergencies.
IDENTIFICATION: A clear colourless solution in a clear 10 mL ampoule.
PRESENTATION: 10 mL clear ampoules containing a 0,5% m/v solution of Bupivacaine hydrochloride in packs of 10.
STORAGE INSTRUCTIONS: Store below 25°C
KEEP OUT OF REACH OF CHILDREN.
REGISTRATION NUMBER: W/4/335
NAME AND BUSINESS ADDRESS OF APPLICANT: INTRAMED (PTY) LTD
6 Gibaud Road
Port Elizabeth, 6001