Pharmacokinetics and pharmacodynamics of lignocaine: A review

Table 1 Immuno-modulating and anti-inflammatory effects of lignocaine

Effects	Immuno-modulating and inflammatory actions
Anti-nociceptive and analgesic effects[12,16,17,34,101]	Interaction with nociceptive pathways
	Blockade of neuronal sodium channels
	Blockade of potassium currents
	Muscarinic receptor antagonist
	Blockade of dopamine receptors
	Glycine inhibitor
	Reduction in excitatory amino acids
	Reduction in thromboxane
	Release of endogenous opioid peptides
	Reduction in neurokinins
	Release of ATP-adenosine triphosphate
Wound healing effects[19,38,39,102-104]	Retardation by reduction of mucopolysaccharide and collagen synthesis
	Reduction in recruitment and metabolic response of
	Inhibition of thrombus formation
	Antithrombotic activity
	Inhibition of platelet aggregation via blockade of calcium influx
	Mobilization of intracellular calcium stores
	Inhibition of oxygen free radical production
	Inhibition of inflammatory cytokines
	Inhibition of vascular permeability
	Inhibition of edema formation
Inhibition of immune cell mediators from monocytes[18,105]	Inhibition of interleukin 1α
	Inhibition of interleukin β
	Inhibition of interleukin 8
	Inhibition of tumor necrosis factor
Inhibition of immune cell mediators from neutrophils[18,24-26,28,33,102,106]	Inhibition of prostaglandins
	Inhibition of thromboxanes
	Inhibition of leukotrienes
	Inhibition of lysosomal enzymes
	Inhibition of free radicals
Inhibition of immune cell mediators from mast cells[36]	Inhibition of histamine release
Anti-bactericidal effects[16-18,43-46,107]	Inhibitory actions on Pseudomonas aeruginosa
	Inhibitory actions on Escherichia coli
	Inhibitory actions on Staphylococcus aureus
	Inhibitory actions on Haemophilus influenza
	Inhibitory actions on Mycobacterium tuberculosis
Anti-viral and anti-fungal effects[16,17,108]	Inhibitory actions on Herpes simplex virus
	Inhibitory actions on Candida albicans
Clinical effects in inflammation-related disease[109-117]	Protective effects in acute lung injury
	Protective effects in septic shock
	Protective effects in cardiac ischemia
	Beneficial effects in ischemia-reperfusion injuries
	Protective effects in interstitial cystitis
	Protective effects in ulcerative colitis
	Protective effects in ulcerative proctitis
	Protective effects in burn injuries
	Accelerated return of bowel function in major surgery
	Blockade of airway hyperactivity in asthma
	Treatment of intractable hiccups
	Beneficial effects in traumatic brain injury

Table 2 Adverse effects of lignocaine toxicity

System	Effects
CNS	Biphasic effects
	Early: CNS excitation with seizures
	Late: CNS depression, termination of convulsions, reduced level of consciousness, leading to respiratory depression and/or arrest
	Mechanism: Local inhibition of inhibitory CNS pathways (CNS stimulation), then inhibition of inhibitory and excitatory pathways (CNS inhibition)
	Symptoms and signs
	Anxiety
	Dizziness or light headed
	Confusion
	Euphoria
	Tinnitus
	Blurring of vision or diplopia
	Nausea and vomiting
	Twitching and tremors
	Seizures with reduced consciousness
Cardiovascular	General effects
	Conduction block of neural impulses
	Prevention of passage of sodium through sodium channels
	Stabilization of excitable membranes
	Prevention of the initiation and transmission of nerve impulses
	Attenuation of phase 4 diastolic depolarization
	Reduction in automaticity
	Reduction in absolute refractory period
	Increase in the ratio of effective refractory period: action potential duration
	Decrease in action potential duration
	Ventricular fibrillation threshold: raised
	Higher serum concentrations
	Blockage of sodium channels
	Depression of rate of depolarization during phase 0 of the cardiac action potential
	Re-entrant arrhythmias
	Suppression of conduction through the sinus and atrioventricular nodes
	Symptoms and signs
	Bradycardia
	Hypotension
	Cardiovascular depression
	Cardiac arrest
Respiratory	Symptoms and signs
	Tachypnea
	Respiratory depression
	Respiratory arrest
Allergic reactions	Extremely rare
	Symptoms and signs
	Cutaneous lesions: urticaria, edema
	Anaphylaxis

CNS: Central nervous system.