Mohammad Shariful Alam (Shohan)

LOCAL ANAESTHESIA
Local anesthetics: These are the drugs that produce local lack of sensation without loss of consciousness whereby surgical procedures can be carried out painlessly. Or, Local loss of sensation after applying the drugs in a particular area. Structure:

Most local anesthetic agents consists of a lipophilic group (frequently an aromatic benzene ring) connected by an intermediate chain (commonly including an ester or amide) to an ionizable i.e. hydrophilic group (usually tertiary amine). Classification: According to chemical structure or based on interbridged chain: I. Ester group: Cocaine Procaine Tetracaine Benzocaine II. Amide group: Lidocaine/Lignocaine Prilocaine Bupivacaine Mepivacaine Ropivacaine According to duration of action: I. Short acting (30 to 60 minutes): Procaine (30 min) Amethocaine (1 hr) II. Intermediate acting (1 to 2 hours): Lidocaine (lignocaine, xylocaine 1-1.5hr) Articaine Prilocaine (2 hr) Mepivacaine Long acting (>2hours): Tetracaine Bupivacaine (3 hr) Levobupivacaine Etidocaine Ropivacaine

III.

Mohammad Shariful Alam (Shohan)

[Lidocaine is most widely used local anesthetic also known as lignocaine. Usually used in surgery requiring 60-120 minutes]

Criteria of a local anesthetic: Should produce affective analgesia without loss of consciousness and any systemic adverse effect. ii) It should be rapidly acting, non-irritating to tissue, not causing permanent damage to the nerve and the effect should be continued after completion of surgery. i) Pharmacokinetics: Routes of administration: Injection into the area of the nerve fiber to be blocked, topical. Onset of action: Slow onsetAmethocaine Moderate onset- Procaine, Prilocaine, and Dibucaine Rapid onsetLignocaine Duration of action: *** Tissue penetration: SlowProcaine ModerateBupivacaine, Prilocaine RapidLignocane (lidocaine) Metabolism: Ester groupby plasma butyrylcholinesterase (pseudo cholinesterase) Amide group- hydrolyzed by liver microsomal cytochrome P450. Mechanism of action: Local anesthetic Binds with the protein of the Na+ channels at inactivated stage (at the interior site) Blocks the voltage dependent Na+ conductance (i.e. prevent Na+ influx) Block the depolarization, so fails to initiation and propagation of action potential Afferent impulse (nociceptive) cannot go the higher center No pain sensation
[Pain is transmitted by lateral spinothalamic tract through type C (dorsal root) & type A (delta) nerve fibers]

Indication: i) As local anaesthesia in Surface anaesthesia Infiltrative anaesthesia Nerve block anaesthesia Spinal anaesthesia & Epidural anaesthesia. ii) Status epilepticus iii) Cardiac arrhythmia.

Mohammad Shariful Alam (Shohan)

Site of action: Surface anaesthesia: Local anesthetic solution is directly applied to the mucous membrane of nose, mouth, bronchial tree, oesophagus or genito-urinary tract. e.g., Lidocaine, tetracaine, benzocaine. Infiltrating anaesthesia: Injected into subcutaneous tissue. Site of action is sensory nerve endings in subcutaneous tissue. e.g., Lidocaine. Nerve block anaesthesia: Injected close to the sensory nerves to produce a loss of sensation peripherally. e.g., Lidocaine. Spinal anaesthesia: Injected into the sub-arachnoid space which contains CSF. e.g., Lidocaine. Epidural anaesthesia: Injected just outside the dura, into a narrow space; between the dura and the bony spinal canal, containing fat & connective tissue. e.g., Lidocaine, bupivacaine. Q. How can we prolong the action of a local anesthetic? Ans. 1. By altering the site of injection: Highly vascular area (tracheal mucosa) rapid absorption. Low vascular area delayed absorption. 2. By adding a vasoconstrictor agent with local anesthetic e.g., Adrenaline (retards the removal of local anesthetic from the injection site). 3. By giving large dose. 4. By giving repeated dose. 5. By slowing injection.
[The onset of local anesthesia can be accelerated by use of solutions saturated with carbon dioxide (carbonated)]

Adverse effects:

1. CNS:

Euphoria (cocaine) Sleepiness Light headedness Visual and auditory disturbances Restlessness Nystagmus, muscular twitching Shivering Convulsions

(at low dose)

(at high dose)

2. PNS: 3. CVS:

Neurotoxicity producing transient radicular irritation Sensory & motor deficit Myocardial depression Vasodilatation may be due to release of histamine Hypotension Hypertension and arrhythmia-cocaine (blocks nor-epinephrine reuptake
vasoconstriction hypertension)

[Bupivacaine is more cardio toxic than other local anesthetics]

4. Hematological:

Methaemoglobinaemia (prilocaine >10mg/kg)

5. Allergic reactions.