Local and general anaesthetics

• LAs
– block conduction of pain impulses to spinal cord
• GAs
– block conduction of pain impulses to the sensory
cortex
 Classification
Ester type
• Cocaine, procaine, chloroprocaine, benzocaine,
tetracaine
Amide type
• Lidocaine, etidocaine
– Infiltration
• Bupivacaine, mepivacaine, ropivacaine
– Obstetrical anaesthesia
• Prilocaine
– Topical/infiltration
– A/E - methemoglobinemia
 Local anaesthetics
MOA
– Cause reversible inhibition of axonal nerve conduction
by blocking Na+ channels in nerve membranes, thus
prolonging the inactivation stage of the channels
P/kinetics
• Duration of action varies
– Short, medium or long
– Epinephrine, phenylephrine & dextran may be used to
prolong action
– Esters generally have shorter duration of action
compared to local anesthetics with amides
A/Effects
– CNS stimulation(restlessness/tremors/euphoria)
followed by inhibition(drowsiness/sedation)
– At high concs.-seizures/resp. failure, coma
– CVS - Hypotension, cardiac depression,
tachyarrhythmias
– hypersensitivity rxns. (ester type)
Interactions
– Potentiate NMJ drugs e.g. tubocuratine
Indications
– Topical/Infiltration/regional/spinal/epidural
anaesthesia
 LA A/Effects /Toxicities & Neurotoxicity

 Allergic reactions
– High risk in ester type (those metabolized to PABA)
– Also due to added preservatives ( e.g. methylparaben –
metabolized to PABA)
 Systemic toxicity
• Secondary to high plasma/tissue local anesthetic concs.
 Systemic toxicities
CNS
• Tongue and circumoral (areas around the mouth) numbness (at
low conc.)
• Tinnitus, vertigo, restlessness
• Seizures
 Neurotoxicity
• Results from of LA inj. into subarachnoid or epidural spaces
– Groin numbness, muscle weakness
–  Cauda equina syndrome
• Acute loss of lumbar plexus function leading to sensory
anesthesia
•  Bowel & bladder sphincter dysfunction
• Paraplegia, urinary / fecal incontinence
Transient Radicular Irritation
– Moderate/severe lower back, buttocks, posterior thigh pain
 Clinical applications
Regional anaesthesia (commonest use)
• Lidocaine
Topical/Surface anaesthesia
• Cocaine, lidocaine, tetracaine
– Application of LA to mucous membranes of nose, mouth,
esophagus, tracheobronchial tree, genitourinary tract
inorder to relieve pain for Dx or surgery
Local infiltration
• Lidocaine, bupivacaine, ropivacaine
• LA injected into subcutaneus or other superficial tissue
primarily for minor surgical procedures e.g. dental surgery
or support of intravascular cannula placement
Peripheral Nerve / Field Block
• Lidocaine, bupivacaine, ropivacaine, prilocaine
• LA injection into tissues around individual nerves or nerve
plexuses - to block sensory nerves from that area or around
the operative field
Epidural Anesthesia
• Bupivacaine, lidocaine , ropivacaine, ropivacaine
• Anesthesia caused by local anesthetic solutions injected into
epidural or sacral caudal space
• MOA:
–  Direct action on nerve roots and spinal cord following local
anesthetic diffusion across the dura
–  Diffusion of local anesthetic into paravertebral region through
the intervertebral foramina causing paravertebral nerve blocks  
Spinal Anesthesia
• Tetracaine, lidocaine, bupivacaine
– Anesthesia following local anesthetic injection
into lumbar subarachnoid space
– Sites of action:
–  Primary: preganglionic fibers leading the spinal
cord in the anterior rami
–  Secondary: superficial spinal cord layers
 Agents added to LAs
 Vasoconstrictors e.g. epinephrine, phenylephrine
 Dextran (low-mol-wt)
Vasoconstrictors
Rationale
– Prolongation of conduction blockade (inc duration of action)
– Reduced systemic absorption
– Higher anesthetic concentration near nerve fibers
– Reduced bleeding
MOA - prolongation
– Decreased systemic absorption
– Increased local anesthetic concentration in the vicinity of sensory
nerves
– Increased uptake of the local anesthetic
A/E: Increased risk of cardiac arrhythmias; Increased risk of hypertension
in susceptible patients
Dextran
• Inc. peripheral nerve block anesthesia duration (probably due to a
reduction in local anesthetic systemic absorption)