Lignocaine

Registered South African indications:

• Ventricular arrhythmias
• Local anaesthesia

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to anaesthetics of the amide type

Ventricular arrhythmia (inj)

• Sino-atrial disorders
• All grades of atrioventricular block
• Severe myocardial depression
• Porphyria 

Local anaesthesia (inj)

• Complete heart block
• Hypovolaemia

Cautions 

• Pregnancy
• Breastfeeding
• Renal impairment (cat)
• Severe renal impairment (spo, inj)
• Severe hepatic impairment (gel)
• Hepatic impairment (spo, inj, cat)
• Elderly
• Epilepsy
• Myasthenia gravis
• Cardiac conduction disturbances
• Congestive cardiac failure
• Bradycardia
• Severe shock
• Impaired respiratory function
• Following cardiac surgery
• Hypokalaemia
• Hypoxia
• Disorders of acid-base balance
• Administration into inflamed or infected area
• Intra-articular administration
• Impaired cardiovascular function (epidural anaesthesia)
• Neonates
• Injections in the head and neck regions
• Retro- and peribulbar injections
• Intramuscular administration
• Wounds or traumatised mucosa in application region (spo)
• Paralysed patients (spo)
• Porphyric patients (spo, gel)
• Oropharyngeal use (spo)
• Contact with eyes (gel)
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: inj, cat, spo, gel

Ventricular arrhythmias
- Suppression of ventricular extrasystoles and ventricular tachycardia, especially after an acute myocardial infarction

• IV: 50-100mg, bolus given at a rate of 25-50mg/min; May be repeated after 5min; Max: 200-300mg/1hr; Maintenance: 20-50μg/kg/min, as an infusion (0.2 or 0.4% solution in 5% glucose)

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Elderly patients and those with congestive heart failure or cardiogenic shock may require smaller bolus doses

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Slower infusion rates should be used in patients with congestive heart failure or liver disease

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When arrhythmias reappear during a constant infusion of lignocaine, a small bolus may be given rapidly; the infusion rate is increased simultaneously. The infusion should be terminated as soon as the patient's basic cardiac rhythm appears to be stable or at the earliest sign of toxicity

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Constant ECG monitoring is recommended during lignocaine therapy, however, if not available and a ventricular arrhythmia is suspected, a single IM dose may be administered into the deltoid muscle if bradycardia is not present

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Local anaesthesia (additional agent may be required)

- Epidural anaesthesia

• IV: 20-30mg for each dermatome; Max: 100mg/dose

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For continuous epidural anaesthesia, Max dose should not be repeated at intervals of less than 1.5 hours

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A test dose of 2-5mls should be injected at least 5 minutes prior to administering the total dose

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- Caudal block for production of obstetric analgesia
- Epidural thoracic block

• IV: 200-300mg

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For continuous caudal anaesthesia, Max dose should not be repeated at intervals of less than 1.5 hours

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A test dose of 2-5mls should be injected at least 5 minutes prior to administering the total dose

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- Epidural lumbar anaesthesia

• IV: 250-300mg

- Intercostal nerve block

• IV: 30mg; Max: 200mg/dose

- Paraverterbral nerve block

• IV: 30-50mg; Max: 200mg/dose

- Pudendal nerve block

• IV: 100mg on each side; Max: 200mg/dose

- Paracervical nerve block for obstetric analgesia

• IV: 100mg on each side; Max: 200mg/dose

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Max recommended dosage of 200mg should not be repeated at intervals of less than 1.5 hours

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- Sympathetic nerve blocks
- Cervical (stellate ganglion) nerve block

• IV: 50mg; Max: 200mg/dose

- Lumbar nerve block

• IV: 50-100mg; Max: 200mg/dose

- Percutaneous infiltration anaesthesia

• IV: 5-300mg

- IV regional anaesthesia

• IV: 50-300mg; Max: 4mg/kg

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For field infiltration, 2% solution does not have significant advantages over 1%; It lasts slightly longer but burns considerably more with injection

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Nerve blocks: Dose varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient

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Anaesthesia of male urethra

• Urethral (gel): 10-15ml

Anaesthesia of female urethra

• Urethral (gel): 5-7ml

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To broken skin and mucous membranes do not apply more than 10ml at any one time

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Anaesthesia prior to minor non-invasive procedures of the nasal cavity, pharynx and epipharynx including rhinoscopy and laryngoscopy 
Insertion of instruments and catheters into the respiratory and digestive tract
- Provides surface anaesthesia for the oropharyngeal and tracheal areas to reduce reflex activity, attenuate haemodynamic response and to facilitate insertion of the catheter or the passage of instruments during endotracheal intubation, laryngoscopy, bronchoscopy, oesophagoscopy and gastroscopy
Obstetrics
- As supplementary pain control for procedures not requiring aseptic technique

Each actuation delivers 10mg lignocaine

• Topical (spo): Max: 200mg

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Should not be used on cuffs or endotracheal tubes made of plastic (polypropylene)

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The number of sprays depend on the extent of the area to be anaesthetised

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As with any local anaesthetic, reactions and complications are best averted by employing the minimal effective dosage. Debilitated or elderly patients should be given doses commensurate with their age and physical condition

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Dental practice
- Before minor dental procedures where local anaesthesia is desired (spo)

• Topical (spo): 10-50mg to the mucous membranes

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May interfere with swallowing and thus enhance the danger of aspiration. Numbness of the tongue or buccal mucosa may increase the danger of biting trauma

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- Local anaesthesia or dental extractions and operations (cat) (additional agent may be required)

• Local infiltration (cat): 36-200mg, as needed; Max: 240mg

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Dose depends on nature, magnitude, duration and locality of the operation

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Caution must be used to avoid intravenous injection to avoid systemic side effects

Paed. forms avail. in SA and covered in this monograph: inj, cat, spo, gel

Ventricular arrhythmias

• IV: Initial: 0.5-1mg/kg bolus; Repeat if needed according to response of patient; Max bolus dose: 3-5mg/kg; Maintenance: 10-50μg/kg/min, as an infusion

Advanced cardiac life support

• IV: Initial: 1mg/kg bolus; Maintenance if ventricular tachycardia or ventricular fibrillation is not corrected: 20-50μg/kg/min

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Infusion may be started if arrhythmia not corrected following initial bolus

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Local or regional anaesthesia
- Single doses for anaesthesia other than spinal

<12 years

• No information available

12-18 years

• IV: Max: 200mg

Local infiltration

<12 years

• IV: Max: 3mg/kg, 4hrly

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Use of a more dilute solution of 0.5% or 1% is advised in paediatrics

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Anaesthesia prior to minor non-invasive procedures of the nasal cavity, pharynx and epipharynx including rhinoscopy and laryngoscopy 

Insertion of instruments and catheters into the respiratory and digestive tract
- Provides surface anaesthesia for the oropharyngeal and tracheal areas to reduce reflex activity, attenuate haemodynamic response and to facilitate insertion of the catheter or the passage of instruments during endotracheal intubation, laryngoscopy, bronchoscopy, oesophagoscopy and gastroscopy

Obstetrics
- As supplementary pain control for procedures not requiring aseptic technique

Each actuation delivers 10mg lignocaine

• Topical (spo): Max: 200mg

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Children should be given doses commensurate with their age and weight

---

Should not be used on cuffs or endotracheal tubes made of plastic (polypropylene)

---

The number of sprays depend on the extent of the area to be anaesthetised

---

As with any local anaesthetic, reactions and complications are best averted by employing the minimal effective dosage. Debilitated patients or children should be given doses commensurate with their age and physical condition

---

Dental practice
- Before minor dental procedures where local anaesthesia is desired (spo)

• Topical (spo): 10-50mg to the mucous membranes

---

Children should be given doses commensurate with their age and weight

---

May interfere with swallowing and thus enhance the danger of aspiration. Numbness of the tongue or buccal mucosa may increase the danger of biting trauma

---

- Local anaesthesia or dental extractions and operations (additional agent may be required)

• Local infiltration (cat): 36-200mg, as needed; Max: 240mg

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Dose depends on nature, magnitude, duration and locality of the operation

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Caution must be used to avoid intravenous injection to avoid systemic side effects

Pregnancy 

• Caution
• Although animal studies have revealed no evidence of harm to the foetus, lidocaine crosses the placenta and should not be administered during early pregnancy unless the benefits are considered to outweigh the risks
• Lidocaine given by epidural or paracervical block, especially in large doses, or by local perineal infiltration prior to delivery crosses rapidly into the foetal circulation
• Elevated lidocaine levels may persist in the newborn for at least 48 hours after deliver. Foetal bradycardia or neonatal bradycardia, hypotonia or respiratory depression may occur
• Topical spray: There is no or inadequate evidence of safety of the drug in human pregnancy but it has been in wide use for many years without apparent ill consequence and animal studies have shown no hazard. If drug therapy is needed in pregnancy, lidocaine spray can be used if there is no safer alternative
• Cartridge: No information available 

Breastfeeding 

• Caution
• Small amounts of lignocaine are secreted into breast milk and the possibility of an allergic reaction in the infant, albeit remote, should be borne in mind when using lignocaine in breastfeeding mothers

Renal Impairment 

• No dose adjustment recommended (gel)
• Mild to moderate: No dose adjustment recommended (spo, inj)
• Severe: Caution; no dose adjustment recommended (spo, inj)
  Inj: eGFR<30ml/min/1.73m²: Slower infusion rates recommended and close monitoring for lignocaine toxicity is advised
• Caution; no information available (cat) 

Hepatic Impairment 

• Mild to moderate: No dose adjustment recommended (gel)
  Severe: Caution; no dose adjustment recommended (gel)
• Caution; no dose adjustment recommended (spo, cat)
• Caution; dose adjustment recommended (inj)
  Slower infusion rates recommended and close monitoring for lignocaine toxicity is advised

Elderly

• Caution; no dose adjustment recommended
  Lower doses are recommended, proportionate to age and physical status

Porphyria Information

• Probably not porphyrinogenic (PNP)
  Lidocaine has been shown to be porphyrinogenic in animals and should be avoided in persons suffering from porphyria
  Adverse reactions of lidocaine that can be confused with an acute porphyric attack are nausea, vomiting, confusion, paresthesia, tremors, seizures, numbness and respiratory depression

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders 

• Dizziness
• Nervousness
• Tremor
• Circumoral paraesthesia
• Drowsiness
• Seizures
• Coma
• Nervous system reactions
  - Excitatory
  - Depressant
• Transient neurological symptoms
  - Pain of the lower back, buttock and legs
• Arachnoiditis
• Cauda equina syndrome
  - Persistent paraesthesia
  - Bowel and urinary dysfunction
  - Lower limb paralysis

Cardiovascular Disorders

• Hypotension
• Bradycardia
• Myocardial depression
• Cardiac arrhythmias
• Cardiac arrest
• Circulatory collapse

Respiratory Disorders

• Dyspnoea
• Bronchospasm
• Respiratory depression
• Respiratory arrest
• Sore throat (spo)
• Hoarseness (spo)
• Loss of voice (spo)

Gastrointestinal Disorders

• Nausea and vomiting

Musculoskeletal Disorders

• Pain
  - Lower back
  - Buttock
  - Legs

Skin and Subcutaneous Tissue Disorders

• Rash
• Urticaria
• Oedema
  - Angioedema
  - Face oedema
• Application site irritation (spo)

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
  - Allergic or anaphylactoid reactions
  - Anaphylactic shock
• Methaemoglobinaemia

Sensory Disorders

• Tinnitus
• Hyperacusis
• Blurred vision
• Diplopia
• Amaurosis
• Numbness of the tongue
• Orbital inflammation

• Amide-type local anaesthetics
• Agents structurally related to amide-type local anaesthetics
• Antiarrhythmics (Class III)
• Amiodarone
• Mexiletine
• Muscle relaxants
• Suxamethonium
• Beta-blockers
• Propranolol
• Cimetidine
• Antivirals
• Amprenavir
• Atazanavir
• Darunavir
• Lopinavir
• Antipsychotics which may prolong the QT interval
• Pimozide
• Sertindole
• Olanzapine
• Quetiapine
• Zotepine
• Serotonin antagonists
• Tropisetron
• Dolasetron
• Adrenaline (epinephrine)
• Verapamil
• Timolol
• Quniupristin
• Dalfopristin
• Loop diuretics
• Thiazide diuretics
• Acetazolamide
• CYP1A2 inhibitors
• Fluvoxamine
• Erythromycin
• Phenytoin
• Oral hormone replacement therapy
• Narcotics
• Fentanyl
• Opioid-antiemetics
• Oestrogens

Other interactions

• Plastic
• PVC and non-PVC cuffs of endotracheal tubes

• Liver function
• Electrocardiogram

None routine. Specific cases may require

• Lidocaine concentrations

Gel 2g/100g, Injection - EML (Primary) 

Pump spray 10mg/ml - EML (Hospital)

Lidocaine is a local anaesthetic of the amide type. It is used to provide local anaesthesia by nerve blockade at various sites in the body and in the ionic control of dysrhythmias. It acts by inhibiting the ionic refluxes required for the initiation and conduction of impulses, thereby stabilising the neuronal membrane. In addition to blocking conduction in nerve axons in the peripheral nervous system, Lidocaine has important effects on the central nervous system and cardiovascular system. After absorption Lidocaine may cause stimulation of the CNS followed by depression and in the cardiovascular system, it acts primarily on the myocardium where it may produce decreases in electrical excitability, conduction rate and force of contraction.

Gel (per 100g) 2g

• Remicaine jelly (Adcock Ingram) originator

Pump spray (per ml) 10mg

• Xylocaine (AstraZeneca) originator

Injection (per ml) 10mg 

• Lignocaine HCl Fresenius 1% (Bodene)
• Lignocaine-HCl B Braun 1% (B Braun)

Injection (per ml) 20mg 

• Lignocaine HCl Fresenius 2% (Bodene)
• Lignocaine-HCl B Braun 2% (B Braun)
• Remicaine 2% (Adcock Ingram) originator
• Xylotox S.E Plain (Adcock Ingram) originator

Injection (per ml) 100mg

• Remicard (Adcock Ingram) originator

Injection  (per 5ml) 100mg

• Lignocaine HCI Fresenius 2% (Bodene)

Injection  (per 5ml) 500mg

• Lignocaine HCI Fresenius 10% (Bodene)

COMBINATION PREPARATIONS

Lignocaine/ Adrenaline

Injection (per ml) 20mg/12,5μg

• Xylotox E80-A (Adcock Ingram) originator

Lignocaine/Noradrenaline

Injection (per ml) 20mg/12,5μg

• Xylotox L (Adcock Ingram) originator