Bupivacaine/ Adrenaline

Registered South African indications:

• Regional anaesthesia

Contraindications

• Hypersensitivity to the active ingredients or any of the excipients in this combination product
• Intravenous regional anaesthesia
• Thyrotoxicosis
• Severe heart disease
• Digital, nasal, external ear or genital administration

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Administration in areas with high vascularity
• Heart block
• Fixed cardiac output
• Respiratory distress
• Hyperthyroidism
• Diabetes mellitus
• Phaeochromocytoma
• Narrow angle glaucoma
• Hypokalaemia
• Hypercalcaemia
• Prostatic adenoma
• Cerebrovascular disease
• Arteriosclerosis
• Shock
• Cardiac dilatation
• Arrhythmias
• Angina
• Prolonged use
• Paediatric use

Forms avail. in SA and covered in this monograph: inj

Peripheral nerve block

• Local infiltration: Dosage dependant on nature, magnitude and duration of procedure involved; Max: 150mg/dose

Epidural block
Caudal block

• Intrathecal: Dosage dependant on nature, magnitude and duration of procedure involved; Max: 150mg/dose

Not established for use in children younger than 12 years

Pregnancy

• Caution
• There is no evidence of untoward effects in human pregnancy. In large doses, there is evidence of decreased pup survival in rats and an embryological effect in rabbits if bupivacaine is administered in pregnancy. Bupivacaine should not, therefore, be given in early pregnancy unless the benefits are considered to outweigh the risks
• The addition of adrenaline may potentially decrease uterine blood flow and contractility, especially after inadvertent injection into maternal blood vessels. Foetal bradycardia may occur following paracervical nerve block
• Labour may be prolonged leading to the need for caesarean section

Breastfeeding

• Caution
• Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended
  Dose reduction may be required

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Paraesthesia
• Dizziness
• Seizures
• Circumoral paraesthesia
• Loss of consciousness
• Tremor
• Light headedness
• Dysarthria
• Muscle twitching

Cardiovascular Disorders

• Bradycardia
• Cardiac arrest
• Cardiac arrhythmias
• Hypotension
• Hypertension

Respiratory Disorders

• Respiratory depression

Gastrointestinal Disorders

• Nausea and vomiting

Genitourinary Disorders

• Urinary retention

Immune, Blood and Lymphatic Disorders

• Allergic reactions
• Anaphylactic shock

Sensory Disorders

• Diplopia
• Tinnitus
• Visual disturbances
• Numbness of the tongue
• Hyperacusis

• Sympathomimetics 
• Alpha blockers
• Beta blockers 
• General anaesthetics
• Antihypertensives
• Antidepressants
• Phenothiazines
• Digoxin
• Antihistamines
• Thyroid hormones
• Dopaminergic agents
• Insulin
• Oral hypoglycaemic agents
• Agents that decrease serum potassium

ECG

Bupivacaine
Bupivacaine is a long acting local anaesthetic with both anaesthetic and analgesic effects. At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block with less pronounced motor block. It causes reversible blockade of impulse propagation along nerve fibres by binding to sodium channels and preventing the inward movement of sodium ions through the cell membrane of the nerve fibres.

Adrenaline
Adrenaline is a sympathomimetic amine which is a potent stimulant of alpha- and beta- adrenergic receptors.  It has strong vasoconstrictor action through alpha- adrenergic stimulation, which counteracts the vasodilatation and increases vascular permeability leading to loss of intravascular fluid and subsequent hypotension in anaphylactic shock. Adrenaline stimulates bronchial beta-adrenergic receptors, causing bronchial smooth muscle relaxation.

COMBINATION PREPARATIONS

Bupivacaine/ Epinephrine

Injection (per ml) 5mg/5µg

• Macaine HCl 0.5% Injection with Adrenaline (Adcock)