LOCAL ANAESTHESIA (LA): AN OVERVIEW

 

 

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ABOUT AUTHORS:
Mayure Vijay Kumar*, V. Sravanthi
Maheshwara College of Pharmacy (B-Pharm Scholar)
Department of pharmacology,
Maheshwara College of Pharmacy, Chitkul (V), Isnapur “X” Road, Patancheru, Hyderabad, A.P.
mayurevijaykumar@gmail.com

ABSTRACT:
The anaesthetic agents are the drugs which causes anaesthesia-reversible loss sensation. It deals with the property of relieving the pain without eliminating sensation. These drugs are generally administered to facilitate surgery. It can be described by two main classes. General anaesthetic, which causes a reversible loss of consciousness, and local anaesthetics, which causes a reversible loss of sensation for a limited region of the body while maintaining consciousness. Here I explain about the Local anaesthetics agents that prevent transmission of nerve impulses without causing unconsciousness. They act by binding to fast sodium channels from within in an open state.
BACKGROUND: The purpose of this Review article is to summarize the Local anaesthetics agents, general mechanism, structures, therapeutic uses, adverse effects and also explains their properties.

REFERENCE ID: PHARMATUTOR-ART-2250

PharmaTutor (ISSN: 2347 - 7881)

Volume 2, Issue 10

Received On: 07/07/2014; Accepted On: 22/07/2014; Published On: 01/10/2014

How to cite this article: VK Mayure, V Sravanthi; Local Anaesthesia (LA): An Overview; PharmaTutor; 2014; 2(10); 68-79

INTRODUCTION:(General)
Cocaine is a naturally occurring compound indigenous to the Andes Mountains, West Indies, and Java. It was the first anaesthetic to be discovered and is the only naturally occurring Local anaesthetic; all others are synthetically derived. Cocaine was introduced in to Europe in the 1800s following its isolation from Coca beans. Sigmund Freud, the noted Austrian psychoanalyst, used cocaine on his patients and became addicted through self-experimentation.

In the latter half of the 1800s, interest in the drug became widespread, and many of cocaine’s pharmacologic actions and adverse effects were elucidated during this time. In the 1880s, Koller introduced cocaine to the field of ophthalmology, and Hall introduced it to dentistry. Halsted was the first to report the use of cocaine for nerve blocks in the US in 1885 and also became addicted to the drug through self-experimentation.

Procaine, the first synthetic derivative of cocaine, was developed in 1904. Lofgren later developed lidocaine, the most widely used cocaine derivative, during World War II in 1943. 

GENERAL MECHANISM OF ACTION OF LOCAL ANAESTHETIC:

Table 1: Properties of local anaesthetics:

Drug

Onset

Duration

Tissue penetration

Plasma half-life(h)

Main unwanted effects

notes

Cocaine

Medium

Medium

Good

-1

CVS and CNS effects owing to block of amine uptake

Rarely used, only as spray for upper respiratory tract

Procaine

Medium

Short

Poor

<1

CNS:

anxiety,

Restlessness, shivering, depression.

CVS: Bradycardia,

and decrease cardiac output, vasodilatation,

The first synthetic agent  No longer used

Lidocaine

Rapid

Medium

Good

-2

Less tendency to cause CNS effects

Used intra venously fortreating ventricular dysrythmias .

Tetracaine

Very slow

Long

Moderate

-1 as lidocaine

As lidocaine

Used mainly for spinal andcorneal anaesthesia.

Bupivacaine

Slow

Long

Moderate

-2

As lidocaine, but greater cardiotoxicity

Widely used causes less cardio toxicity(levobupivacaine)

Prilocaine

Medium

Medium

Moderate

-2

No vasodilator activity can cause methaemoglobinaemia

Widely used

Table 2: local anaesthetics:

The below list/table are the drugs belonging to local anaesthetics their therapeutic use, adverse effects and structures in pharmaceutical field:






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