ADVANCED

PHARMACOLOGY - I
LOCAL ANAESTHETICS
PRESENTED BY
LOGESH P
M.PHARM 1 SEMESTER
DEFINITION OF LOCAL
ANAESTHETICS:
• Local anaesthetics are drugs which, when applied directly to the
peripheral nerves, block nerve conduction and abolish the sensations
in the part supplied by the nerve.
• They are applied to somatic nerves and act on axons, cell body,
dendrites and synapses.
• These drugs preferred for performing minor surgery.
PROPERTIES:
• Non irritant
• Non local tissue damage
• Minimal systemic toxicity
• Rapid on set of action
• Prolonged action
• Water soluble
ORDER TO BLOCK:
Pain followed by temperature, touch, pressure, skeletal muscle power
CLASSIFICATION:
• BASED ON DURATION OF ACTION
3.MISCELLANEOUS DRUGS WITH LOCAL
ACTION:
Clove oil, phenol, chlorpromazine,
diphenhydramine, propranolol.
Local anesthetics can be produced by
cooling
CHEMISTRY OF LA:
MECHANISM OF ACION:
PROLONGATION OF ACTION BY
VASOCONSTRICTOR:
• Adrenaline like vasoconstrictors delays its absorption, produce
prolong action and reduce systemic toxicity.
• Adrenaline(1:100000 to 1:200000; in dentistry 1:50000 to 1:100000).
• norepinephrine- not preferred.
• Not used for nerve block of extremity and end organ
• Felypressin used as an vasoconstrictor, it not affected heart rate ,BP
and maybe preferable in patients with CVD
PHARMACOLOGICAL ACTIONS:
CNS
• Initial CNS stimulation later depression action
• They cross BBB- excitation ,tremor, restlessness, convulsion, euphoria,
twitching of muscle
• Higher dose – respiratory depressant, coma, death.
CVS
• LAs are cardiac depressants
• Higher doses decrease heart rate, excitability, contractility, cardiac output,
conductivity.
• Lignocaine is used as an antiarrhythmic drug
• At higher concentration LAs can induce arrhythmias
• Bupivacaine is more cardiotoxic produced
SMOOTH MUSCLE:
• Relaxation of vascular and bronchial smooth muscle.
PHARMACOKINETICS:
• Soluble surface anaesthetics are rapidly absorbed from mucous membranes but
minimal absorption in intact skin.
• It is distributed throughout all body tissues.
• Ester linked LAs rapidly metabolized by plasma cholinesterase
• Amide linked LAs degraded in the liver microsomes by dealkylation and
hydrolysis.
• The kidneys are the primary excretory organ for local anaesthetics and its
metabolites. Ester appear in only very small concentration in the urine.
ADVERSE EFFECTS:
• CNS:
restlessness, tremor, headache, drowsiness, confusion and convulsions followed by
respiratory depression, coma, death.
• CVS:
Bradycardia, hypotension, cardiac arrhythmias, rarely cardiovascular collapse and death.
• ALLERGIC REACTONS:
These are skin rashes, itching, erythema urticaria, wheezing, bronchospasm and rarely
anaphylactic reaction. The incidence of allergic reactions is more with ester linked LAs than
with amide linked Las.
• BLOOD:
large dose of prilocaine lead to accumulation of metabolite orthotoluidine.it forms
methemoglobin higher level of the latter leads cyanosis. To reducing agent like methylene blue
or ascorbic acid convert of methemoglobin.
TECHNIQUES OF LAs:
SURFACE ANESTHESIA:
• This type of anesthesia is accomplished by the application of a local
anesthetic to skin or mucous membranes.
• Surface anesthesia is used to relieve surface pain, itching, burning.
• This technique is often used during examination procedures involving
the respiratory tract.
• The topical block easily anesthetizes the surface of the cornea and the
oral mucosa.
INFILTRATION ANESTHESIA:
• Local infiltration occurs when the nerve endings in the skin and
subcutaneous tissues are blocked by direct contact with a local
anesthetic, which is injected into the tissue.
• It is used primarily for surgical procedures involving a small area of
tissue
ex, suturing a cut
• CONDUCTION BLOCK ANAESTHESIA:
1.FIELD BLOCK
LAs is injected s.c in the surrounding area of the nerves. So the all
other nerves coming to a particular field are blocked. e.g scalp and
anterior abdominal walls
2.NERVE BLOCK
LAs injected around the anatomically localized nerve trunk. The
block is usually described by adding the nerve name. e.g radial nerve
block.
SPINAL BLOCK ANESTHESIA:
• In spinal anesthesia, the local anesthetic is injected into the
subarachnoid space of the spinal cord
• Also called subarachnoid or intrathecal block or spinal anesthesia.
• Site- subarachnoid space between L2-L3 or L3-L4
• Used to anesthetize lower abdomen, hind limbs.
EPIDURAL ANESTHESIA:
• This type of anesthesia is accomplished by injecting a local anesthetic
into the epidural space.
• Widely used to provide analgesia or anesthesia in surgical and
obstetric practice.
INTRAVENOUS REGIONAL ANESTHESIA:
Also referred as bier’s block
used for upper limb and orthopedic procedures.
LIGNOCAINE:
• Most commonly used
• Stable, stored at room temperature
• Can be autoclave repeatedly
• Has quick onset of action and high degree of penetration
• Excellent surface anesthesia
• Toxicities similar to other LA
• Recommended for topical, nerve block, epidural, dental analgesia
• Can be used subjects allergic to procaine and other type of ester LAs
BUPIVACAINE:
• It is about four times as potent as lignocaine and more prolonged
action up to 8 hours.
• Toxicity similar to lignocaine
• It is used for spinal and epidural anesthesia.
THANK YOU