Local Anesthesia Flashcards
Classification - Chemical Properties
Esters
- Procaine
- Chlorprocaine
- Cocaine
- Benzocaine
- Tetracaine
Amides
- Lignocaine
- Bupivacaine
- Ropivacaine
- Prilocaine
- Mepivacaine
- Etidocaine
Classification - Duration of Action and Potency
Short DOA, low potency
- Procaine
- Chlorprocaine
Intermediate DOA and potency
- Lignocaine
- Mepivicaine
- Prilocaine
- Cocaine
Long DOA, high potency
- Bupivacaine
- Tetracaine
- Etidocaine
Factors affecting onset of action
- pKa
- pH
- Concentration
- Lipid solubility
- CT surrounding nerve
- Temperature
- Vasoconstrictors
Shortening onset of action
- Warm local anaesthetic
- Add sodium bicarbonate 1ml/ 10ml LA
- Add adrenaline separately
Factors affecting duration of action
- Lipid solubility
- Protein binding
- Dose
- Site of Injection
- Additives
Additives prolonging duration of action
- Alpha-adrenergic agonists (e.g. adrenaline, clonidine or dexmetetomidine)
- Opioids (neuraxial blocks)
- NaHCO3 (epidural blocks)
- Hyluronidase (ophthalmic blocks)
- Ketamine (caudal and epidural blocks)
- Magnesium (peripheral nerve - controversial)
- Dextrose (increase baricity for intrathecal injection)
Factors affecting absorption
- Site of injection (IVI > tracheal > intercostal > caudal > paracervical > epidural > brachial plexus > subcutaneous)
- Vasoconstrictors
- Protein bindings
Mechanism of action
Primarily: block conduction via Na+ channels by binding to the α subunit
Secondarily: block K+ and Ca2+ channels, and NMDA glutamate receptors
Metabolism and Excretion
Esters: plasma pseudocholinesterase (butyrylcholinesterase) breaks LA down to PABA (may trigger allergic reaction) - excreted unchanged in urine
Cocaine: partially metabolised by the liver, partially excreted unchanged by the kidney
Amides: microsomal P450 system (lignocaine > ropivacaine > bupivacaine)
Potency
Bupivacaine > levobupivacaine > ropivacaine > lignocaine > procaine
Toxicity - CNS
Initial Phase
- Circumoral paraesthesia
- Tinnitus
- Confusion
Excitatory Phase
- Convulsions
Depressive Phase
- Loss of consciousness
- Coma
- Respiratory depression
Management
- Stop injection
- Apply oxygen
- Secure airway
- Avoid hypoventilation and acidosis
- Treat seizures
- Midazolam 0.05-0.1mg/kg
- Propofol 0.5-1mg/kg
- Thiopentone 1-2mg/kg
Toxicity - CVS
Initial phase
- Hypertension
- Tachycardia
Intermediary phase
- Myocardial depression
- Decreased CO
- Hypotension
Terminal phase
- Peripheral vasodilation
- Severe hypotension
- Sinus bradycardia
- Conduction defects
- Dysrhythmias
Management
- Resuscitate according to ACLS
- Intravenous fluids, vasopressors
- Amiodarone and vasopressors instead of lignocaine and adrenaline
- Intralipid infusion
- CPR
- Insulin, 50% glucose, and potassium infusion (2IU/kg/hr, 2ml/kg/hr, 2mmol/kg/hr respectively)
Intralipid (Dosage)
- 20% solution
- 1.5ml/kg bolus IVI over 1 minute
- Followed by 0.25ml/kg/min infusion
- Bolus can be repeated twice at 5 minute intervals
- Infusion can be increased to 0.5ml/kg/min
Side Effects
- Direct neuronal toxicity
- Cauda equina syndrome (persistent neurological injury)
- Transient neurological syndrome (marked dysaesthesia)
- Allergy
- PABA from ester metabolism
- Methylparaben preservative in amide formulations
- Myotoxicity (hyper contraction, vacuole formation, edema, and necrosis)
- Hematological
- Reduced coagulation, enhanced fibrinolysis (lignocaine)
- Prilocaine (metabolised to orthotoline which oxidises Hb to metHb - treated with methylene blue 1-2mg/kg IVI over 5 minutes)
Contraindications to adrenaline
- CVS
- Unstable angine
- Arrhythmia
- Uncontrolled hypertension
- Uteroplacental insufficiency
- Drugs
- MAOI
- TCA
- Poor collateral flow (digits, penis)
- IV regional anesthesia