Professional Documents
Culture Documents
Anastesia 4 - 5935955432286717286
Anastesia 4 - 5935955432286717286
Anastesia 4 - 5935955432286717286
DR. KWEYAMBA
LOCAL ANAESTHETICS
Local anesthetics: are drugs which cause reversible
loss of sensory perception, especially of pain, in a
restricted area of the body where they are applied.
Apnea
Apnea and convulsions result in hypoxia, hypercapnia
and metabolic acidosis.
The acidosis increases the proportion of ionized local
anesthetic agent.
Toxicity results from the presence of ionised drug
within the cell blocking the ion channel.
Acidosis effectively reduces the proportion of
diffusible drug within the cells, and slows clearance
SYSTEMIC EFFECTS
Cardiovascular system
Most local anesthetic agents (except cocaine) relax
vascular smooth muscle, causing vasodilatation.
Direct cardiovascular toxicity is caused by the
membrane-stabilizing activity of the drugs on
myocardial muscle, which is a feature of blockade of
voltage-gated fast sodium channels.
Cardiac toxicity may result in any of the following
effects:
Prolongation of PR interval
Supra ventricular tachycardia
Decreased automaticity
Widening of QRS complex
Ventricular ectopic beats
Prolongation of ST interval
T-wave changes
Respiratory system
The respiratory effects of local anesthetic agents are due
combination of peripheral neuronal blockade and
systemic toxicity.
Apnea with systemic toxicity affecting the respiratory centre
Broncho dilatation secondary to relaxation of bronchial
smooth muscle
Other effects
Local anesthetic drugs have a weak neuromuscular
blocking action.
Amides block plasma cholinesterase
They may cause anaphylactic reaction due to
preservatives
METABOLISM
Ester local anesthetics are rapidly metabolized by
plasma cholinesterase, and systemic toxicity is rarely
a problem.
Amide local anesthetics are metabolized by the liver,
Hepatic failure must be very severe for their metabolism
to be affected.
THE ISSUES
Glucose
OF ADDITIVES
Standard solutions of local anesthetic agents are slightly
hypobaric at body temperature and ph.
Tend to move upwards in the cerebrospinal fluid away
from the gravitational pull.
Glucose is added to these local anesthetics to make
hyperbaric
E.g hyperbaric lignocaine and bupivacaine
Epinephrine
Epinephrine is added to local anesthetic solutions to
reduce vascularity of the area by direct vasoconstriction.
This in turn reduces the systemic uptake of the drug
pH manipulation
Alkali nation of solutions by addition of bicarbonate
increases tissue ph. This results in a higher proportion of
non-ionized drug, which diffuses into the neurons more
rapidly.
Amide-linked agents
Bupivacaine
Bupivacaine is a long-acting local anesthetic agent with
a slow onset of action.
Blockade of a large peripheral nerve such as the sciatic
nerve may take 60 minutes, depending on the approach
Intrathecal injection in contrast produces an acceptable
block within a few minutes
prone to causing myocardial depression.
Reversal may be slow due to high Pk and high affinity to
cardiac proteins
To avoid systemic effect, this drug should be avoided
in
Avoid bupivacaine in IVRA
Avoid 0.75% bupivacaine in obstetric practices
Limit dose to 2mg/kg .
Metabolism
N-dealkylation to pipecolylxylidine (N-
desbutylbupivacaine).Hydroxybupivacaine is also
produced.
The metabolites are excreted in the urine.
Lidocaine (lignocaine)
Lidocaine is primarily classified as a local anesthetic
agent but is also a Class IB antiarrhythmic
Has rapid onset of action and intermediate effect up to
45 min.
May be combined with bupivacaine to balance the onset
of action and duration of action between these two
drugs
Metabolism
N-dealykalation followed by hydrolysis to form
ethylgylcine and xylidide which are excreted by the
kidneys.
Prilocaine
This is more related to lidocaine in terms of
pharmacological effects
They have the same Pka- 7.9
Can lead to Methaemoglobinaemia which can lead to
cyanosis.
Ester-linked agents
Cocaine
Cocaine is a naturally occurring ester derived from
benzoic acid.
Can be extracted from the leaves of Erythroxylumcoca.
Available in solution and paste formulation in conc
of 1% and 10%
It is mainly used for topical anesthesia and to reduce
bleeding during nasal surgery
Indication-The only indication for cocaine is in ocular
anesthesia
Effects in the CNS
Cocaine initially blocks the inhibitory pathways
resulting.
euphoria
hyperthermia
altered vision and hearing, nausea
eventually convulsions.
Higher levels of cocaine also block the excitatory
pathways, resulting in central nervous depression
leading to sedation and unconsciousness, with
respiratory depression.
Amethocaine
Amethocaine (tetra Caine) is an ester local anesthetic
agent used for topical anesthesia.
It is available as a gel (4%) for local anesthesia of the
skin before intravascular cannulation.
INDICATIONS OF LOCAL ANAESTHETICS
1. Surface anesthesia
It is produced by topical application of a surface
anesthetic to mucous membranes and abraded skin.
2. Infiltration anesthesia
Dilute solution of LA is infiltrated under the skin in
the area of operation
blocks sensory nerve endings
. Onset of action is almost immediate and duration is
shorter than that after nerve block,
3. Conduction block
The LA is injected around nerve trunks so that the area
distal to injection is anaesthetized and paralyzed.
This can be
Nerve block- -a specific nerve is blocked
Field block--all nerves coming to a particular field are
blocked.
4. Spinal anesthesia
5. epidural anesthesia
6. intravenous regional anesthesia
References