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Local Anesthetic
Prepared By :- Miss Anamika Singh
A N E S T H E S I A I S A RE VE R S I B L E CO N D I T I O N O F C O M F O RT A N D
Q U I E S C EN CE F O R A PAT I E NT W I T H I N T H E P H Y S I O L O G I C AL
L I M I T B E FO R E , D U R I N G A N D AF T E R P E R F O R M A N C E O F A
P R O C E D U R E .
WHAT IS ANAESTHESIA ?
Local anesthetic are drugs that produce a reversible
conduction blockade of impulse along central and
peripheral nerve pathways .
 in addition to blockade of impulse ,local anesthetics can
inhibit various receptor enhance release of glutamate ,and
depress the activity of certain intracellular signaling
pathways .
When local anesthetic are given systemically ,the function
of cardiac,skeletal,and smooth muscle ,as well as
transmission of impulse in the central and peripheral
nervous system and within the specialized conducting
system of heart ,can all be altered
INTRODUCTION
C O C A I N E - F I R ST L O C A L AN E S T H E T I C A G E NT I S O L AT E D B Y
N I E M A N - 1 8 6 0 F R O M T H E L E AV E S O F T H E C O C A T R E E .
I T ’ S A N E ST H E T I C A CT I O N WA S D E M O N S T RAT E D B Y K A R L
K O L L E R I N 1 8 8 4 .
F I R ST E F FE CT I VE A ND W I D E LY U S E D SYN T H E T I C L O C A L
A N E S T H E T I C P R O C A I N E - P R O D U C E D B Y
I T S A NE ST H E T I C PR O P E RT I E S W E R E I D E NT I F I E D B Y
B I B E R F I E L D A ND T H E A G E N T WA S I N T R O D U CE D I NTO C L I NI CAL
P R A C T I C E B Y B R A U N .
L I D O C A I N E – L O F G R E N I N 1 9 4 8 .
T H E D I S CO V E RY O F I T S A N E S T H E T I C P R O P E RT I E S WA S
F O L L O W E D I N 1 9 4 9 B Y I T S C L I N I C A L U S E B Y T. G O R D H
HISTORY
L O C A L A NES T H E T I C S AR E DR U G , W H E N A P P LI E D D I RE CTLY TO
P E R I P H E R AL N E RVO U S T I S S UE , B L O CK T H E N E RVE
C O N D U C T I O N A N D AB O L I S H A L L S E N S AT I O N S I N T H E PA RT
S U P P L I E D B Y T H E N E RV E W I T H O U T L O S S O F C O N S C I O U S N E S S .
DEFINITION
S H O U L D H AV E Q U I C K O N S E T O F A C T I O N
S H O U L D N O T B E I R R I TAT I N G TO S K I N & M U C O U S M E M B R A N E S
D U R A T I O N O F A C T I O N M U S T B E L O N G E N O U G H T O A L L O W
D E S I R E D S U R G E R Y T O B E C O M P L E T E D .
S H O U L D B E E F F E C T I V E O N B O T H I N J E C T I O N & L O C A L
A P P L I C A T I O N .
S H O U L D H A V E L O W S Y S T E M I C T O X I C I T Y .
FEATURE OF LOCAL
ANESTHETIC
S H O U L D N O T C A U S E A N Y P E R M A N E N T D A M A G E O N A N Y
T I S S U E
 S H O U L D R E L A T I V E L Y F R E E F R O M P R O D U C I N G A L L E R G I C
R E A C T I O N .
 S H O U L D B E S T A B L E I N S O L U T I O N A N D R E A D I L Y U N D E R G O
B I O T R A N S F O R M A T I O N .
 N O L A I N U S E T O D A Y S A T I S F Y A L L O F T H E S E C R I T E R I A
H O W E V E R A L L A N E S T H E T I C D O M E E T A M A J O R I T Y O F T H E M .
FEATURES OF LOCAL
ANESTHETIC
 R E V E R S I B L E A C T I O N
N O N - I R R I T A N T
N O A L L E R G I C R E A C T I O N
N O S Y S T E M I C T O X I C I T Y
R A P I D O N S E T O F A C T I O N
S U F F I C I E N T D U R A T I O N O F A C T I O N
P O T E N T
S T A B L E I N S O L U T I O N
N O T I N T E R F E R E W I T H H E A L I N G O F T I S S U E
H A V E A V A S O C O N S T R I C T O R A C T I O N O R C O M P A T I B L E W I T H
V C
N O T E X P E N S I V E
PROPERTIES OF IDEAL LOCAL
ANESTHEISA
 E L D E R L Y O R C H I L D P A T I E N T
H E P A T I C D Y S F U N C T I O N O R A L T E R E D H E P A T I C P E R F U S I O N
L O W C A R D I A C O U T P U T
H I G H C A R D I A C O U T P U T
C A R D I A C P A T H O L O G Y
R E D U C T I O N I N P L A S M A P R O T E I N
P R E G N A N C Y
RISK FACTOR
 N E E D L E B R E A K A G E
P A R E S T H E S I A
 F A C I A L N E R V E P A R A L Y S I S
T R I S M U S
S O F T – T I S S U E I N J U R Y
H E M A T O M A
P A I N O N I N J E C T I O N
B U R N I N G O N I N J E C T I O N
I N F E C T I O N
E D E M A
S L O U G H I N G O F T I S S U E
P O S T A N E S T H E T I C I N T R A O C U L A R L E S S I O N
COMPLICATION
 T A L K A T I V E N E S S
 S L U R R E D S P E E C H
D I Z Z I N E S S
N A U S E A
D E P R E S S I O N
E U P H O R I A
E X C I T E M E N T
C O N V U L S I O N
SIGN AND SYMPTOMS –TOXIC
REACTION TO LOCAL
ANESTHESIA
SAR OF LOCAL ANESTHETIC
A L L L O C A L A N E S T H E T I C H AV E A N A M I N E O N O N E E N D TO A N
A R O M AT I C R I N G O N T H E O T H E R
T H E A M I N E E N D I S H Y D R O P H I L I C A N D T H E A R O M AT I C E N D I S
L I P O P H I L L I C .
 T H E T W O G R O U P A R E C O N N E C T E D B Y M O S T LY A N E S T E R O R
A N A M I D E G R O U P A N D L E S S C O M M O N LY B Y E T H E R O R
K E TO N E S
T H U S T W O M A I N C L A S S E S O F L O C A L A N E S T H E T I C E XI S T : -
A M I D E S A N D E S T E R .
E S T E R S H AV E A N E S T E R L I N K B E T W E E N T H E A M I N E C H A I N
A N D A R O M AT I C E N D .
A M I D E S H AV E A N A M I D E L I N K B E T W E E N T H E A M I N E C H A I N
T H E A R O M AT I C E N D .
T H E Y H AV E P K A I N R A N G E O F 7 . 5 TO 9 . 5 .
E S T E R S A N D A M I N O A M I D E S D I F F E R I N M E TA B O L I S M
S TA B I L I T Y A N D A D V E R S E E F F E C T S .
 E S T E R S A R E M E TA B O L I ZE D I N T H E P L A S M A B U T A M I D E S A R E
M E TA B O L I ZE D I N T H E L I V E R .
E S T E R A R E U N S TA B L E I N S O L U T I O N , B U T A M I D E S A R E V E RY
S TA B L E I N S O L U T I O N .
E S T E R S A R E M U C H M O R E L I K E LY T H A N A M I D E S TO C A U S E
A L L E R G I C R E A C T I O N .
L I P H O P H I L I C I T Y I S I M P O RTA N T TO P E N E T R AT E T H E L I P I D
L AY E R A N D R E A C H T H E B I N D I N G S I T E O N T H E I N S I D E T H E
C E L L .
P R E S E N C E O F E L E C T R O N W I T H D R AW I N G G R O U P I N O RT H O O R
PA R A ( N O T M E TA ) P O S I T I O N D E C R E A S E L I P H O P H I L L I C I T Y B U T
S T I L L I N C R E A S E A C T I V I T Y F O R O N LY E S T E R G R O U P
LIPOPHILIC GROUP
P R O C A I N E I S M O R E P O T E N T I F I T H A S E - D O N A T I N G A M I N E
G R O U P I N T H E A R O M A T I C R I N G
T H I S I N C R E A S E I N A C T I V I T Y ( V A L I D F O R E S T E R O N L Y ) I S
D U E T O P O S S I B I L I T Y O F Z W I T T E R I O N I C F R O M W H I C H
E N H A N C E A C T I V I T Y D U E T O F O R M A T I O N O F Q U A N T E R N A R Y
A M I N E W H I C H I S I M P O R T A N T F O R B I N D I N G .
WHAT N WHEN IS ORTHO ,PARA
,META ?
P R E S E N C E O F E - W I T H D R AW I N G H A L O G E N I N O RT H O
P O S I T I O N O N LY C A N D E C R E A S E D U R AT I O N O F A C T I O N B Y
M A K I N G T H E E S T E R M O R E L I K E LY F O R A N U C L E O P H I L I C
AT TA C K
C H L O R I N E I N O RT H O G R O U P M AK E S T H E CA R B O N YL CA R B O N
M O R E P O S I T I VE A ND M O R E L I K ELY TO B E ATTAC K E D B Y
N U CL E O P H I L E S T H AT C A U S E S B RE A K D O W N O F C O M P O U N D
. N U C L E O P H I L E S C O N TA I N A L O N E PA I R O F E L E CT R O N . T H E Y
AT TA C K ATO M S W I T H P O S I T I V E CH A R G E S M O R E P O S I T I VE T HE
ATO M T H E B E T T E R T H E T H E B E T T E R T H E AT TA C K .
 P R E SE N CE O F E - W I T H D R AW I NG H A L O G E N I N O RT H O
P O S I T I O N O N LY C A N D E CR EA S E D U R AT I O N O F A C T I O N B Y
M A K I N G T H E E S T E R M O R E L I K E LY F O R A N U CL E O P H I L I C A
T TA C K
F O R A M I D E O N LY PR E SE N CE O F D I - O RT H O S U B S T I T UT ED
G R O U P P R E V E NT B RE AK D O W N O F A M I DE A N D T H U S I N C RE A SE
I T ’ S S TAB I L I T Y I N B O T H L I Q U I D F O R M U L AT I O N A N D T H E
B O D Y E N ZY M E S .
 L I N K E R G R O U P H A S S H O RT A L K Y N E N E ( - C H 2 ) C H A I N
C O N TA I N I NG F E W C A R B O N ATO M S A N D VA R I O U S F U N C T I O N A L
G R O U P S U C H A S A M I D E S , E S T E R S , E T H E R O R K E TO N E S
I N C RE A S I NG T H E L E N G T H O F A L K Y L E NE C H A I N I NC R E A S E
T H E P K A W H I C H R E D UC E P O T E N CY B E C AU SE M O R E P K A W H I C H
R E DU CE P O T E N C Y B E C A U S E M O R E D R U G G E T I O N I ZE D O U T S I DE
T H E M E M B R A NE A ND T H U S C A N ’ T PE NE T R AT E I NTO T H E
B I N D I N G S I T E .
LINKER GROUP
U S E F U L L A H AV E A S E C O N D A RY O R T E RT I A RY A M I N E G R O U P.
 T H I S I S I M P O RTA N T B E C A U S E I T I S B E L I E V E D T H AT W H E N
T H E Y E N T E R T H E C E L L , T H E Y W I L L A C C E P T A P R O TO N A N D
F R O M P O S I T I V E LY C H A R G E D Q U AT E R N A RY F R O M W H I C H I S
N E E D E D F O R B I N D I N G TO VO LTA G E G AT E D I O N C H A N N E L S .
 P R O C A I N E B E L I E V E D TO B I N D TO I T ’ S R E C E P TO R W H E N
A M I N E G R O U P I S P O S I T I V E LY C H A R G E Q U AT E R N A RY F R O M .
HYDROPHILLIC GROUP
 H O W E V E R , B E N ZO C A I N H A S N O A M I N E P O RT I O N B U T I S S T I L L
A N E F F E C T I V E TO P I C A L L A
T H U S T H E U S E O F A M I N E PA RT C O U L D O N LY B E F O R P R O P E R
WAT E R S O L U B I L I T Y A N D N O T D I R E C T LY R E L E AT E D TO P R O P E R
B I N D I N G
B E N Z O I C A C I D A N D A W I D E R A N G E O F D E R I VAT I VE S A ND
R E L AT E D B EN Z E N I C C O M P O U N D S , SU C H A S S A LT S , A L K Y L ES T E R S ,
PA R A B EN S , B E N Z Y L A L C O HO L , B EN Z A L D E H YDE , A N D B EN Z O Y L
P E R O X I D E , A R E C O M M O N LY U SE D A S A NT I B A C T E R I AL A N D
A N T I F U N GAL P R E S E RVAT I V E S A ND A S F L AVO R I N G A G EN T S I N
F O O D , C O S M E T I C , H Y G I E N E , A N D P H A R M A C E U T I C A L P R O D U C T S .
C O C A I N E
H E XY L C A I N E
M E P RY L A C I N E
C Y C L O M E T H Y C A I N E
 P I P E R O C A I N
BENZOIC ACID DERIVATIVES
F O R M U L A  C 7 H 2 1 N O 4
R O U T E O F A D M I N I S T R A T I O N  T O P I C A L , I N T R A V E N O U S
B I O A V A I L A B I L I T Y  M O U T H ( 3 3 % )
M E T A B O L I S M  L I V E R ( C Y P 3 A 4 )
O N S E T O F A C T I O N  S E C O N D T O M I N U T E S
D U R A T I O N O F A C T I O N  5 T O 9 0 M I N U T E S
E X C R E T I O N  K I D N E Y
U S E S : -
C O C A I N E I S N O W P R E D O M I N A N T L Y U S E D F O R N A S A L A N D L A C R I M A L
D U C T S U R G E R Y . T H E M A J O R D I S A D V A N T A G E S O F T H I S U S E A R E
C O C A I N E ' S P O T E N T I A L F O R C A R D I O V A S C U L A R T O X I C I T Y , G L A U C O M A ,
A N D P U P I L D I L A T I O N . [ 2 4 ] M E D I C I N A L U S E O F C O C A I N E H A S D E C R E A S E D A S
O T H E R S Y N T H E T I C L O C A L A N E S T H E T I C S S U C H
A S B E N Z O C A I N E , P R O P A R A C A I N E , L I D O C A I N E , A N D T E T R A C A I N E A R E N O W
U S E D M O R E O F T E N . [ 2 4 ] I F V A S O C O N S T R I C T I O N I S D E S I R E D F O R A
P R O C E D U R E ( A S I T R E D U C E S B L E E D I N G ) , T H E A N E S T H E T I C I S C O M B I N E D
W I T H A V A S O C O N S T R I C T O R S U C H A S P H E N Y L E P H R I N E O R E P I N E P H R I N E
COCAINE
F O R M U L A : - C 1 6 H 2 3 N O 2
M O L A R M A S S : - 2 6 1 . 3 6 5
U S E S : - H E XY L C A I N E H Y D R O C H L O R I D E , A B E N Z O I C A C I D
E S T E R , I S A L O C AL ANA E ST H E T I C T H AT H A S B E E N U SE D F O R
S U R FA CE A N AE S T H E SI A O F M U C O U S M E M B R AN E S . L O C A L
A N E S T H E T I C S P R O D UC E A T RAN S I E NT B L O C K O F N E RVE
C O N D U C T I O N B Y I N T E R F E R I NG W I T H S O D I U M C H A N N E L S .
HEXYLCAINE
F O R M U L A : - C 1 4 H 2 1 N O 2
M O L A R M A S S : - 2 3 5 . 3 2 7
U S E S : - M E P RYL C A I NE ( A L S O K N O W N A S E P I R O C A I NE A ND
O R A C A I N E ) I S A L O C AL AN E ST H E T I C W I T H S T I M U L A N T
P R O P E RT I E S T H AT I S ST RU C T U R AL LY R E L AT E D TO
D I M E T H O C A I N E . M E PRY L CA I NE H A S A R E L AT I VE LY PO T E NT
I N H I B I TO RY A CT I O N O N T H E M O N O A M I N E T R A N S P O RT E R A ND
I N H I B I T S T H E R E U P TAK E O F D O PA M I NE , N O R E P I NE P H R I NE
A N D S E R O TO N I N .
Meprylcaine
F O R M U L A : - C 2 2 H 2 3 N O 3
M O L A R M A S S : - 3 5 9 . 5 0 2 3 2
CYCLOMETHYCAINE
Uses:- CYCLOMETHYCAINE IS ALSO USED IN TOPICAL ANESTHESIA ON THE
SKIN OR MUCOUS MEMBRANES FOR CUTS, BITES, AND ALSO FOR
UROLOGICAL EXAMINATIONS. A COMMON SYNONYM OF THIS DRUG IS
SURFACAINE.
A M I N O B E N ZI O C A C I D I S A N E S SE NT I AL G R O W T H FA C TO R O F
B A CT E R I A R E Q U I R E D F O R T H E B I O S Y N T H E S I S O F F O L I C A C I D .
F O L I C A C I D A C T S A S T H E C O FA C TO R I N T H E T R A N S FE R O F
O N E - C A R B O N U N I T S I N A L L L I V I NG O R G A N I S M . I N M A M M A L S
, I T H A S TO B E S U P P L I E D I N T H E F O O D .
AMINO BENZOIC ACID
DERIVATIVES
F O R M U L A  C 9 H 11 N O 2
R O U T E O F  TO P I C A L , O R A L
M O L A R M A S S  1 6 5 . 1 9 2
U S E S : - B E N ZO C A I N E I S U S E D SH O RT T E R M TO
R E L I E V E PA I N FR O M M I N O R M O U T H PR OB L E M S ( S U C H A S
TO O T HA C H E , C A N K ER SO R E S , S OR E G U M S / T H R O AT, M O U T H / G U M
I N J U RY ) . I T I S A L O C A L A N E S T H E T I C T H AT W OR K S B Y N UM B I N G
T H E PA I N F U L A R E A .
Benzocain
Synthesis of benzocaine
R O U T E O F A D M I N I S T R AT I O N  TO P I C A L
F O R M U L A  C 11 H 1 5 N O 2
U S E S : - B U TA M B E N WA S I N D I C AT E D F O R
T H E T R E AT M E NT O F CH R O N I C PA I N D U E TO I T S L O N G - D UR AT I O N
E F F E C T. I T I S A L S O I N D I C AT E D A S A S UR FAC E AN E S T H E T IC
F O R S K I N A M U C OU S M E M B R A N E A N D F O R T H E R E L I E F
O F PA I N A N D P R U R I T U S A S S O C I AT E D W I T H A N O R EC TA L
D I S O R D E R S .
BUTAMBEN
R O U T E O F A D M I N I S T R AT I O N : - PA R E N T E R A L
B I O AVA I L A B I L I T Y : - N A
M E TA B O L I S M : - H Y D R O LY S I S
E XC R E T I O N : - R E N A L
F O R M U L A : - C 1 3 H 2 0 N 2 O 2
M O L A R M A S S : - 2 3 6 . 6 1 5
U S E S : - P R O C A I N E I S A N A N E S T H E T I C A G E N T I N D I C A T E D F O R
P R O D U C T I O N O F L O C A L O R R E G I O N A L A N E S T H E S I A ,
P A R T I C U L A R L Y F O R O R A L S U R G E R Y . P R O C A I N E ( L I K E C O C A I N E )
H A S T H E A D V A N T A G E O F C O N S T R I C T I N G B L O O D V E S S E LS W H I C H
R E D U C E S B L E E D I N G , U N L I K E O T H E R L O C A L A N E S T H E T I C S L I K E
L I D O C A I N E . P R O C A I N E I S A N E S T E R A N E S T H E T I C .
.
PROCAINE
PROCAINE SYNTHESIS
C H E M I C A L F O R M U L A : - C 1 8 H 1 3 N 2 O 2
M O L A R M A S S : - 3 0 6 . 4 4 3 G / M O L
U S E S : - B U TA C A I N E I S A W H I T E C RY S TA L L I N E E S T E R U S E D A S
A L O C A L A N E S T H E T I C .
BUTACAINE
C H E M I C A L F O R M U L A : - C 1 6 H 2 6 N 2 O 3
M O L A R M A S S : - 2 9 4 . 3 8 4 G / M O L
U S E S : - P R OPO X YC A I N E I S A L O C A L A N E S T H E T I C M E DI C AT I O N . I T
WA S U S E D B E G I N N I N G I N T H E 1 9 5 0 S D U R I N G D EN TA L P R O C ED U R E S
[ L 1 5 9 1 ] . I T H A S B E E N C O M B I N E D W I T H P R O C A I N E TO AC C EL E R AT E
I T S O N S E T O F A C TI O N A N D P R O V I D E L O N G E R - L A S T I N G
A N E S T H E T I C E F F E C T [ L 1 5 9 2 ] .
Propoxycain
R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L
P R O T E I N B I N D I N G : - 7 5 . 6
F O R M U L A : - C 1 5 H 2 4 N 2 O 2
M O L A R M A S S : - 2 6 4 . 3 6 9
U S E S : - T E T R A C A I N E E Y E D R O P S A R E U S E D T O N U M B
T H E E Y E B E F O R E S U R G E R Y , C E R T A I N T E S T S , O R P R O C E D U R E S .
T H E E Y E D R O P S A R E U S E D T O P R E V E N T P A I N D U R I N G T H E
P R O C E D U R E . T E T R A C A I N E B E L O N G S T O T H E G R O U P
O F M E D I C I N E S C A L L E D L O C A L A N E S T H E T I C S . I T W O R K S B Y
B L O C K I N G T H E P A I N S I G N A L S A T T H E N E R V E E N D I N G S I N
T H E E Y E .
Tetracain
R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L
F O R M U L A : - C 1 7 H 2 8 N 2 O 3
M O L A R M A S S : - 3 0 8 . 4 2 2
M E TA B O L I S M : - B L O O D P L A S M A I N L I V E R
U S E S : - O X YB U PR OC A I NE ( A L S O KN O W N A S B E N O XI N AT E ) I S A
L O C A L AN E S T H E T I C , W H I C H I S U S E D E S P E C I A L LY I N
O P H T H A L M OL O G Y A N D O TO L ARYN G O L OG Y. O X Y B U P R O C A I NE
B I N D S TO SO D I U M C H AN N E L S A ND R E V E R S I B LY S TA B I L I Z E S T H E
N E U R O N A L M E M B R A N E W H I C H D E C R E A S E S I T S P E R M E A B I LI T Y TO
S O D I U M I O N S .
Benoxinate
L I D O C A I NE , A L S O K NO W N A S L I G N O C A I N E , I S A L O C A L
A N E S T H E T I C O F T H E A M I N O A M I D E T Y P E . I T I S A L S O U S E D TO
T R E AT V E NT R I C U L AR TA C H YC AR DI A . W H E N U S E D F OR L O C A L
A N A E S T H ESI A O R I N N E RV E B L OC K S , L I D O CA I N E T Y P I C A L LY
B E G I N S W O R K I N G W I T H I N S E V E R A L M I N U T E S A N D L A ST S F OR
H A L F A N HO U R TO T H R E E H O UR S . L I D O C A I N E M I X T U R E S M AY
A L S O B E A P P L I E D DI R E C T LY TO T H E S KI N O R MU C OU S
M E M B R A N ES TO N U MB T H E A R E A . IT I S O F T E N U S E D M I X E D W I T H
A S M A L L AM O U N T O F A D R EN A L I NE ( E P I N E P H R I N E ) TO PR O L ON G
I T S L O C A L E F F E C T S A N D TO D E C R E A S E B L E E D I N G .
Lidocain Derivatives
R O U T E O F A D M I N I S T R AT I O N : - I N T R AV E N O U S , S U B C U TA N E O U S
B I O AVA I L A B I L I T Y : - 3 5 % ( M O U T H ) 3 % ( TO P I C A L )
M E TA B O L I S M : - L I V E R
E XC R E T I O N : - K I D N E Y
M E LT I N G P O I N T : - 6 8
F O R M U L A : - C 1 4 H 2 2 N 2 O
M O L A R M A S S : - 2 3 4 . 3 4 3
U S E S : - L I G N OC A I N E I N J E C T I O N B E L O N GS TO T W O G R O U P S O F
M E D I C I N E S K N O W N A S L O C A L ANA E S T H E T I C S A N D
A N T I A RR H YT H M I C D R UG S . L O C A L A N A E S T H E TI C S S TO P PA I N A ND
F E E L I N G I N T H E A R EA A R OU N D W H E R E I T I S I N J E C T E D ; A N D
A N T I A R R H YT H M I C D R U G S W O R K B Y R E S TO R I N G I R R E G U L AR
A N D / O R R A P I D H E A RT B E AT S TO N O R M A L .
Lignocaine
Lignocaine Synthesis
F O R M U L A : - C 1 5 H 2 2 N 2 O
M O L A R M A S S : - 2 4 6 . 3 5 4
U S E S : - M E P I VA C A I N E I S I N D I C AT E D F O R P R O D U C T I O N O F L O C A L
O R R E G I O N A L A N A L G E S I A A N D A N E S T H E S I A B Y L O C A L
I N F I LT R AT I O N , P E R I P H E R A L N E RV E B L O C K T E C H N I Q U E S , A N D
C E N T R A L N E U R A L T E C H N I Q U E S I N C L U D I N G E P I D U R A L A N D C A U D A L
B L O C K S .
MEPIVACCINE
R O U T E O F A D M I N I S T R AT I O N : - S U B C U TA N E O U S
P R O T E I N B I N D I N G : - 5 5 %
M E TA B O L I S M : - L I V E R A N D K I D N E Y
F O R M U L A : - C 1 3 H 2 0 N 2 O
M O L A R M A S S : - 2 2 0 . 3 1 6
U S E S : - T H I S M E D I C AT I O N C O NTA I N S 2 A M I D E - T Y P E L O C A L
A N E S T H E T I C S , L I D O C A I N E A N D P R I L O C A I N E . I T I S U S E D
O N N O R M A L, U N B R OK EN S K I N O R O N T H E O UT E R G E N I TAL A R EA TO
P R E V E NT PAI N B E F O R E C E RTA I N P RO C E DU R E S S U CH A S I N S E RT I N G A
N E E D L E , S KI N G R A F T S , O R S K I N L A S E R SU R G E RY. I T W O R KS B Y
T E M P O R A R I LY N U M B I N G T H E S K I N A N D S U R R O U N DI N G A R E A .
PRILOCAINE
R O U T E O F A D M I N I S T R AT I O N : - PA R E N T E R A L
M E TA B O L I S M : - H E PAT I C
E XC R E T I O N : - R E N A L
F O R M U L A : - C 1 7 H 2 8 N 2 O
M O L A R M A S S : - 2 7 6 . 4 2 4
U S E S : - U S E D A S A L O C A L A N E S T H E T I C ( A M I D E C A I N E ) , I T H A S
R A P I D O N S E T A N D L O N G A C T I O N P R O P E RT I E S , S I M I L A R TO
B U P I VA C A I N E , A N D I S G I V E N B Y I N J E C T I O N D U R I N G S U R G I C A L
P R O C E D U R E S A N D D U R I N G L A B O U R A N D D E L I V E RY. I T H A S A R O L E
A S A L O C A L A N A E S T H E T I C . E T I D O C A I N E I S M A R K E T E D U N D E R T H E
N A M E D U R A N E S T.
ETIDOCAINE
C H E M I C A L F O R M U L A : - C 1 8 H 2 2 N 2 O 2
M O L A R M A S S : - 2 9 8 . 3 8 6
U S E S : - P H E N A C A I N E I S A L S O K N O W N A S H O L O C A I N E I S A L O C A L
A N E S T H E T I C U S E D I N O P H T H A L M I C M E D I C I N E .
Phenacaine
U S E S : - D I P E R O D O N I S O N E O F S E V E R A L PH E N Y L UR ET H A NE
D E R I VAT I V E S O F D I A L K Y L A M I N O A L C O HO L S W H I C H H AVE
D E M O N S T R AT E D S I G N I F I C A N T L O C A L A N A E S T H E T I C A C T I V I T Y .
Diperodone
F O R M U L A : - C 2 0 H 2 9 N 3 O 2
M O L A R M A S S : - 3 4 3 . 4 7 1 G M O L - 1
R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L , I N T R AV E NO U S
U S E S : - C I N C H O C A I N E I S T H E A C T I V E I N G R E D I E N T I N S O M E
T O P I C A L H E M O R R H O I D C R E A M S S U C H A S P R O C T O S E D Y L . [ 3 ] I T I S
A L S O A C O M P O N E N T O F T H E V E T E R I N A R Y D R U G S O M U L O S E , U S E D
F O R E U T H A N A S I A O F H O R S E S A N D C A T T L E .
Dibucaine
Local anesthetic

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Local anesthetic

  • 1. Local Anesthetic Prepared By :- Miss Anamika Singh
  • 2. A N E S T H E S I A I S A RE VE R S I B L E CO N D I T I O N O F C O M F O RT A N D Q U I E S C EN CE F O R A PAT I E NT W I T H I N T H E P H Y S I O L O G I C AL L I M I T B E FO R E , D U R I N G A N D AF T E R P E R F O R M A N C E O F A P R O C E D U R E . WHAT IS ANAESTHESIA ?
  • 3. Local anesthetic are drugs that produce a reversible conduction blockade of impulse along central and peripheral nerve pathways .  in addition to blockade of impulse ,local anesthetics can inhibit various receptor enhance release of glutamate ,and depress the activity of certain intracellular signaling pathways . When local anesthetic are given systemically ,the function of cardiac,skeletal,and smooth muscle ,as well as transmission of impulse in the central and peripheral nervous system and within the specialized conducting system of heart ,can all be altered INTRODUCTION
  • 4. C O C A I N E - F I R ST L O C A L AN E S T H E T I C A G E NT I S O L AT E D B Y N I E M A N - 1 8 6 0 F R O M T H E L E AV E S O F T H E C O C A T R E E . I T ’ S A N E ST H E T I C A CT I O N WA S D E M O N S T RAT E D B Y K A R L K O L L E R I N 1 8 8 4 . F I R ST E F FE CT I VE A ND W I D E LY U S E D SYN T H E T I C L O C A L A N E S T H E T I C P R O C A I N E - P R O D U C E D B Y I T S A NE ST H E T I C PR O P E RT I E S W E R E I D E NT I F I E D B Y B I B E R F I E L D A ND T H E A G E N T WA S I N T R O D U CE D I NTO C L I NI CAL P R A C T I C E B Y B R A U N . L I D O C A I N E – L O F G R E N I N 1 9 4 8 . T H E D I S CO V E RY O F I T S A N E S T H E T I C P R O P E RT I E S WA S F O L L O W E D I N 1 9 4 9 B Y I T S C L I N I C A L U S E B Y T. G O R D H HISTORY
  • 5. L O C A L A NES T H E T I C S AR E DR U G , W H E N A P P LI E D D I RE CTLY TO P E R I P H E R AL N E RVO U S T I S S UE , B L O CK T H E N E RVE C O N D U C T I O N A N D AB O L I S H A L L S E N S AT I O N S I N T H E PA RT S U P P L I E D B Y T H E N E RV E W I T H O U T L O S S O F C O N S C I O U S N E S S . DEFINITION
  • 6. S H O U L D H AV E Q U I C K O N S E T O F A C T I O N S H O U L D N O T B E I R R I TAT I N G TO S K I N & M U C O U S M E M B R A N E S D U R A T I O N O F A C T I O N M U S T B E L O N G E N O U G H T O A L L O W D E S I R E D S U R G E R Y T O B E C O M P L E T E D . S H O U L D B E E F F E C T I V E O N B O T H I N J E C T I O N & L O C A L A P P L I C A T I O N . S H O U L D H A V E L O W S Y S T E M I C T O X I C I T Y . FEATURE OF LOCAL ANESTHETIC
  • 7. S H O U L D N O T C A U S E A N Y P E R M A N E N T D A M A G E O N A N Y T I S S U E  S H O U L D R E L A T I V E L Y F R E E F R O M P R O D U C I N G A L L E R G I C R E A C T I O N .  S H O U L D B E S T A B L E I N S O L U T I O N A N D R E A D I L Y U N D E R G O B I O T R A N S F O R M A T I O N .  N O L A I N U S E T O D A Y S A T I S F Y A L L O F T H E S E C R I T E R I A H O W E V E R A L L A N E S T H E T I C D O M E E T A M A J O R I T Y O F T H E M . FEATURES OF LOCAL ANESTHETIC
  • 8.  R E V E R S I B L E A C T I O N N O N - I R R I T A N T N O A L L E R G I C R E A C T I O N N O S Y S T E M I C T O X I C I T Y R A P I D O N S E T O F A C T I O N S U F F I C I E N T D U R A T I O N O F A C T I O N P O T E N T S T A B L E I N S O L U T I O N N O T I N T E R F E R E W I T H H E A L I N G O F T I S S U E H A V E A V A S O C O N S T R I C T O R A C T I O N O R C O M P A T I B L E W I T H V C N O T E X P E N S I V E PROPERTIES OF IDEAL LOCAL ANESTHEISA
  • 9.  E L D E R L Y O R C H I L D P A T I E N T H E P A T I C D Y S F U N C T I O N O R A L T E R E D H E P A T I C P E R F U S I O N L O W C A R D I A C O U T P U T H I G H C A R D I A C O U T P U T C A R D I A C P A T H O L O G Y R E D U C T I O N I N P L A S M A P R O T E I N P R E G N A N C Y RISK FACTOR
  • 10.  N E E D L E B R E A K A G E P A R E S T H E S I A  F A C I A L N E R V E P A R A L Y S I S T R I S M U S S O F T – T I S S U E I N J U R Y H E M A T O M A P A I N O N I N J E C T I O N B U R N I N G O N I N J E C T I O N I N F E C T I O N E D E M A S L O U G H I N G O F T I S S U E P O S T A N E S T H E T I C I N T R A O C U L A R L E S S I O N COMPLICATION
  • 11.  T A L K A T I V E N E S S  S L U R R E D S P E E C H D I Z Z I N E S S N A U S E A D E P R E S S I O N E U P H O R I A E X C I T E M E N T C O N V U L S I O N SIGN AND SYMPTOMS –TOXIC REACTION TO LOCAL ANESTHESIA
  • 12. SAR OF LOCAL ANESTHETIC
  • 13. A L L L O C A L A N E S T H E T I C H AV E A N A M I N E O N O N E E N D TO A N A R O M AT I C R I N G O N T H E O T H E R T H E A M I N E E N D I S H Y D R O P H I L I C A N D T H E A R O M AT I C E N D I S L I P O P H I L L I C .  T H E T W O G R O U P A R E C O N N E C T E D B Y M O S T LY A N E S T E R O R A N A M I D E G R O U P A N D L E S S C O M M O N LY B Y E T H E R O R K E TO N E S T H U S T W O M A I N C L A S S E S O F L O C A L A N E S T H E T I C E XI S T : - A M I D E S A N D E S T E R . E S T E R S H AV E A N E S T E R L I N K B E T W E E N T H E A M I N E C H A I N A N D A R O M AT I C E N D . A M I D E S H AV E A N A M I D E L I N K B E T W E E N T H E A M I N E C H A I N T H E A R O M AT I C E N D . T H E Y H AV E P K A I N R A N G E O F 7 . 5 TO 9 . 5 . E S T E R S A N D A M I N O A M I D E S D I F F E R I N M E TA B O L I S M S TA B I L I T Y A N D A D V E R S E E F F E C T S .  E S T E R S A R E M E TA B O L I ZE D I N T H E P L A S M A B U T A M I D E S A R E M E TA B O L I ZE D I N T H E L I V E R . E S T E R A R E U N S TA B L E I N S O L U T I O N , B U T A M I D E S A R E V E RY S TA B L E I N S O L U T I O N . E S T E R S A R E M U C H M O R E L I K E LY T H A N A M I D E S TO C A U S E A L L E R G I C R E A C T I O N .
  • 14. L I P H O P H I L I C I T Y I S I M P O RTA N T TO P E N E T R AT E T H E L I P I D L AY E R A N D R E A C H T H E B I N D I N G S I T E O N T H E I N S I D E T H E C E L L . P R E S E N C E O F E L E C T R O N W I T H D R AW I N G G R O U P I N O RT H O O R PA R A ( N O T M E TA ) P O S I T I O N D E C R E A S E L I P H O P H I L L I C I T Y B U T S T I L L I N C R E A S E A C T I V I T Y F O R O N LY E S T E R G R O U P LIPOPHILIC GROUP
  • 15. P R O C A I N E I S M O R E P O T E N T I F I T H A S E - D O N A T I N G A M I N E G R O U P I N T H E A R O M A T I C R I N G T H I S I N C R E A S E I N A C T I V I T Y ( V A L I D F O R E S T E R O N L Y ) I S D U E T O P O S S I B I L I T Y O F Z W I T T E R I O N I C F R O M W H I C H E N H A N C E A C T I V I T Y D U E T O F O R M A T I O N O F Q U A N T E R N A R Y A M I N E W H I C H I S I M P O R T A N T F O R B I N D I N G .
  • 16. WHAT N WHEN IS ORTHO ,PARA ,META ?
  • 17. P R E S E N C E O F E - W I T H D R AW I N G H A L O G E N I N O RT H O P O S I T I O N O N LY C A N D E C R E A S E D U R AT I O N O F A C T I O N B Y M A K I N G T H E E S T E R M O R E L I K E LY F O R A N U C L E O P H I L I C AT TA C K C H L O R I N E I N O RT H O G R O U P M AK E S T H E CA R B O N YL CA R B O N M O R E P O S I T I VE A ND M O R E L I K ELY TO B E ATTAC K E D B Y N U CL E O P H I L E S T H AT C A U S E S B RE A K D O W N O F C O M P O U N D . N U C L E O P H I L E S C O N TA I N A L O N E PA I R O F E L E CT R O N . T H E Y AT TA C K ATO M S W I T H P O S I T I V E CH A R G E S M O R E P O S I T I VE T HE ATO M T H E B E T T E R T H E T H E B E T T E R T H E AT TA C K .  P R E SE N CE O F E - W I T H D R AW I NG H A L O G E N I N O RT H O P O S I T I O N O N LY C A N D E CR EA S E D U R AT I O N O F A C T I O N B Y M A K I N G T H E E S T E R M O R E L I K E LY F O R A N U CL E O P H I L I C A T TA C K
  • 18. F O R A M I D E O N LY PR E SE N CE O F D I - O RT H O S U B S T I T UT ED G R O U P P R E V E NT B RE AK D O W N O F A M I DE A N D T H U S I N C RE A SE I T ’ S S TAB I L I T Y I N B O T H L I Q U I D F O R M U L AT I O N A N D T H E B O D Y E N ZY M E S .
  • 19.  L I N K E R G R O U P H A S S H O RT A L K Y N E N E ( - C H 2 ) C H A I N C O N TA I N I NG F E W C A R B O N ATO M S A N D VA R I O U S F U N C T I O N A L G R O U P S U C H A S A M I D E S , E S T E R S , E T H E R O R K E TO N E S I N C RE A S I NG T H E L E N G T H O F A L K Y L E NE C H A I N I NC R E A S E T H E P K A W H I C H R E D UC E P O T E N CY B E C AU SE M O R E P K A W H I C H R E DU CE P O T E N C Y B E C A U S E M O R E D R U G G E T I O N I ZE D O U T S I DE T H E M E M B R A NE A ND T H U S C A N ’ T PE NE T R AT E I NTO T H E B I N D I N G S I T E . LINKER GROUP
  • 20. U S E F U L L A H AV E A S E C O N D A RY O R T E RT I A RY A M I N E G R O U P.  T H I S I S I M P O RTA N T B E C A U S E I T I S B E L I E V E D T H AT W H E N T H E Y E N T E R T H E C E L L , T H E Y W I L L A C C E P T A P R O TO N A N D F R O M P O S I T I V E LY C H A R G E D Q U AT E R N A RY F R O M W H I C H I S N E E D E D F O R B I N D I N G TO VO LTA G E G AT E D I O N C H A N N E L S .  P R O C A I N E B E L I E V E D TO B I N D TO I T ’ S R E C E P TO R W H E N A M I N E G R O U P I S P O S I T I V E LY C H A R G E Q U AT E R N A RY F R O M . HYDROPHILLIC GROUP
  • 21.  H O W E V E R , B E N ZO C A I N H A S N O A M I N E P O RT I O N B U T I S S T I L L A N E F F E C T I V E TO P I C A L L A T H U S T H E U S E O F A M I N E PA RT C O U L D O N LY B E F O R P R O P E R WAT E R S O L U B I L I T Y A N D N O T D I R E C T LY R E L E AT E D TO P R O P E R B I N D I N G
  • 22. B E N Z O I C A C I D A N D A W I D E R A N G E O F D E R I VAT I VE S A ND R E L AT E D B EN Z E N I C C O M P O U N D S , SU C H A S S A LT S , A L K Y L ES T E R S , PA R A B EN S , B E N Z Y L A L C O HO L , B EN Z A L D E H YDE , A N D B EN Z O Y L P E R O X I D E , A R E C O M M O N LY U SE D A S A NT I B A C T E R I AL A N D A N T I F U N GAL P R E S E RVAT I V E S A ND A S F L AVO R I N G A G EN T S I N F O O D , C O S M E T I C , H Y G I E N E , A N D P H A R M A C E U T I C A L P R O D U C T S . C O C A I N E H E XY L C A I N E M E P RY L A C I N E C Y C L O M E T H Y C A I N E  P I P E R O C A I N BENZOIC ACID DERIVATIVES
  • 23. F O R M U L A  C 7 H 2 1 N O 4 R O U T E O F A D M I N I S T R A T I O N  T O P I C A L , I N T R A V E N O U S B I O A V A I L A B I L I T Y  M O U T H ( 3 3 % ) M E T A B O L I S M  L I V E R ( C Y P 3 A 4 ) O N S E T O F A C T I O N  S E C O N D T O M I N U T E S D U R A T I O N O F A C T I O N  5 T O 9 0 M I N U T E S E X C R E T I O N  K I D N E Y U S E S : - C O C A I N E I S N O W P R E D O M I N A N T L Y U S E D F O R N A S A L A N D L A C R I M A L D U C T S U R G E R Y . T H E M A J O R D I S A D V A N T A G E S O F T H I S U S E A R E C O C A I N E ' S P O T E N T I A L F O R C A R D I O V A S C U L A R T O X I C I T Y , G L A U C O M A , A N D P U P I L D I L A T I O N . [ 2 4 ] M E D I C I N A L U S E O F C O C A I N E H A S D E C R E A S E D A S O T H E R S Y N T H E T I C L O C A L A N E S T H E T I C S S U C H A S B E N Z O C A I N E , P R O P A R A C A I N E , L I D O C A I N E , A N D T E T R A C A I N E A R E N O W U S E D M O R E O F T E N . [ 2 4 ] I F V A S O C O N S T R I C T I O N I S D E S I R E D F O R A P R O C E D U R E ( A S I T R E D U C E S B L E E D I N G ) , T H E A N E S T H E T I C I S C O M B I N E D W I T H A V A S O C O N S T R I C T O R S U C H A S P H E N Y L E P H R I N E O R E P I N E P H R I N E COCAINE
  • 24. F O R M U L A : - C 1 6 H 2 3 N O 2 M O L A R M A S S : - 2 6 1 . 3 6 5 U S E S : - H E XY L C A I N E H Y D R O C H L O R I D E , A B E N Z O I C A C I D E S T E R , I S A L O C AL ANA E ST H E T I C T H AT H A S B E E N U SE D F O R S U R FA CE A N AE S T H E SI A O F M U C O U S M E M B R AN E S . L O C A L A N E S T H E T I C S P R O D UC E A T RAN S I E NT B L O C K O F N E RVE C O N D U C T I O N B Y I N T E R F E R I NG W I T H S O D I U M C H A N N E L S . HEXYLCAINE
  • 25. F O R M U L A : - C 1 4 H 2 1 N O 2 M O L A R M A S S : - 2 3 5 . 3 2 7 U S E S : - M E P RYL C A I NE ( A L S O K N O W N A S E P I R O C A I NE A ND O R A C A I N E ) I S A L O C AL AN E ST H E T I C W I T H S T I M U L A N T P R O P E RT I E S T H AT I S ST RU C T U R AL LY R E L AT E D TO D I M E T H O C A I N E . M E PRY L CA I NE H A S A R E L AT I VE LY PO T E NT I N H I B I TO RY A CT I O N O N T H E M O N O A M I N E T R A N S P O RT E R A ND I N H I B I T S T H E R E U P TAK E O F D O PA M I NE , N O R E P I NE P H R I NE A N D S E R O TO N I N . Meprylcaine
  • 26. F O R M U L A : - C 2 2 H 2 3 N O 3 M O L A R M A S S : - 3 5 9 . 5 0 2 3 2 CYCLOMETHYCAINE Uses:- CYCLOMETHYCAINE IS ALSO USED IN TOPICAL ANESTHESIA ON THE SKIN OR MUCOUS MEMBRANES FOR CUTS, BITES, AND ALSO FOR UROLOGICAL EXAMINATIONS. A COMMON SYNONYM OF THIS DRUG IS SURFACAINE.
  • 27. A M I N O B E N ZI O C A C I D I S A N E S SE NT I AL G R O W T H FA C TO R O F B A CT E R I A R E Q U I R E D F O R T H E B I O S Y N T H E S I S O F F O L I C A C I D . F O L I C A C I D A C T S A S T H E C O FA C TO R I N T H E T R A N S FE R O F O N E - C A R B O N U N I T S I N A L L L I V I NG O R G A N I S M . I N M A M M A L S , I T H A S TO B E S U P P L I E D I N T H E F O O D . AMINO BENZOIC ACID DERIVATIVES
  • 28. F O R M U L A  C 9 H 11 N O 2 R O U T E O F  TO P I C A L , O R A L M O L A R M A S S  1 6 5 . 1 9 2 U S E S : - B E N ZO C A I N E I S U S E D SH O RT T E R M TO R E L I E V E PA I N FR O M M I N O R M O U T H PR OB L E M S ( S U C H A S TO O T HA C H E , C A N K ER SO R E S , S OR E G U M S / T H R O AT, M O U T H / G U M I N J U RY ) . I T I S A L O C A L A N E S T H E T I C T H AT W OR K S B Y N UM B I N G T H E PA I N F U L A R E A . Benzocain
  • 30. R O U T E O F A D M I N I S T R AT I O N  TO P I C A L F O R M U L A  C 11 H 1 5 N O 2 U S E S : - B U TA M B E N WA S I N D I C AT E D F O R T H E T R E AT M E NT O F CH R O N I C PA I N D U E TO I T S L O N G - D UR AT I O N E F F E C T. I T I S A L S O I N D I C AT E D A S A S UR FAC E AN E S T H E T IC F O R S K I N A M U C OU S M E M B R A N E A N D F O R T H E R E L I E F O F PA I N A N D P R U R I T U S A S S O C I AT E D W I T H A N O R EC TA L D I S O R D E R S . BUTAMBEN
  • 31. R O U T E O F A D M I N I S T R AT I O N : - PA R E N T E R A L B I O AVA I L A B I L I T Y : - N A M E TA B O L I S M : - H Y D R O LY S I S E XC R E T I O N : - R E N A L F O R M U L A : - C 1 3 H 2 0 N 2 O 2 M O L A R M A S S : - 2 3 6 . 6 1 5 U S E S : - P R O C A I N E I S A N A N E S T H E T I C A G E N T I N D I C A T E D F O R P R O D U C T I O N O F L O C A L O R R E G I O N A L A N E S T H E S I A , P A R T I C U L A R L Y F O R O R A L S U R G E R Y . P R O C A I N E ( L I K E C O C A I N E ) H A S T H E A D V A N T A G E O F C O N S T R I C T I N G B L O O D V E S S E LS W H I C H R E D U C E S B L E E D I N G , U N L I K E O T H E R L O C A L A N E S T H E T I C S L I K E L I D O C A I N E . P R O C A I N E I S A N E S T E R A N E S T H E T I C . . PROCAINE
  • 33. C H E M I C A L F O R M U L A : - C 1 8 H 1 3 N 2 O 2 M O L A R M A S S : - 3 0 6 . 4 4 3 G / M O L U S E S : - B U TA C A I N E I S A W H I T E C RY S TA L L I N E E S T E R U S E D A S A L O C A L A N E S T H E T I C . BUTACAINE
  • 34. C H E M I C A L F O R M U L A : - C 1 6 H 2 6 N 2 O 3 M O L A R M A S S : - 2 9 4 . 3 8 4 G / M O L U S E S : - P R OPO X YC A I N E I S A L O C A L A N E S T H E T I C M E DI C AT I O N . I T WA S U S E D B E G I N N I N G I N T H E 1 9 5 0 S D U R I N G D EN TA L P R O C ED U R E S [ L 1 5 9 1 ] . I T H A S B E E N C O M B I N E D W I T H P R O C A I N E TO AC C EL E R AT E I T S O N S E T O F A C TI O N A N D P R O V I D E L O N G E R - L A S T I N G A N E S T H E T I C E F F E C T [ L 1 5 9 2 ] . Propoxycain
  • 35. R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L P R O T E I N B I N D I N G : - 7 5 . 6 F O R M U L A : - C 1 5 H 2 4 N 2 O 2 M O L A R M A S S : - 2 6 4 . 3 6 9 U S E S : - T E T R A C A I N E E Y E D R O P S A R E U S E D T O N U M B T H E E Y E B E F O R E S U R G E R Y , C E R T A I N T E S T S , O R P R O C E D U R E S . T H E E Y E D R O P S A R E U S E D T O P R E V E N T P A I N D U R I N G T H E P R O C E D U R E . T E T R A C A I N E B E L O N G S T O T H E G R O U P O F M E D I C I N E S C A L L E D L O C A L A N E S T H E T I C S . I T W O R K S B Y B L O C K I N G T H E P A I N S I G N A L S A T T H E N E R V E E N D I N G S I N T H E E Y E . Tetracain
  • 36. R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L F O R M U L A : - C 1 7 H 2 8 N 2 O 3 M O L A R M A S S : - 3 0 8 . 4 2 2 M E TA B O L I S M : - B L O O D P L A S M A I N L I V E R U S E S : - O X YB U PR OC A I NE ( A L S O KN O W N A S B E N O XI N AT E ) I S A L O C A L AN E S T H E T I C , W H I C H I S U S E D E S P E C I A L LY I N O P H T H A L M OL O G Y A N D O TO L ARYN G O L OG Y. O X Y B U P R O C A I NE B I N D S TO SO D I U M C H AN N E L S A ND R E V E R S I B LY S TA B I L I Z E S T H E N E U R O N A L M E M B R A N E W H I C H D E C R E A S E S I T S P E R M E A B I LI T Y TO S O D I U M I O N S . Benoxinate
  • 37. L I D O C A I NE , A L S O K NO W N A S L I G N O C A I N E , I S A L O C A L A N E S T H E T I C O F T H E A M I N O A M I D E T Y P E . I T I S A L S O U S E D TO T R E AT V E NT R I C U L AR TA C H YC AR DI A . W H E N U S E D F OR L O C A L A N A E S T H ESI A O R I N N E RV E B L OC K S , L I D O CA I N E T Y P I C A L LY B E G I N S W O R K I N G W I T H I N S E V E R A L M I N U T E S A N D L A ST S F OR H A L F A N HO U R TO T H R E E H O UR S . L I D O C A I N E M I X T U R E S M AY A L S O B E A P P L I E D DI R E C T LY TO T H E S KI N O R MU C OU S M E M B R A N ES TO N U MB T H E A R E A . IT I S O F T E N U S E D M I X E D W I T H A S M A L L AM O U N T O F A D R EN A L I NE ( E P I N E P H R I N E ) TO PR O L ON G I T S L O C A L E F F E C T S A N D TO D E C R E A S E B L E E D I N G . Lidocain Derivatives
  • 38. R O U T E O F A D M I N I S T R AT I O N : - I N T R AV E N O U S , S U B C U TA N E O U S B I O AVA I L A B I L I T Y : - 3 5 % ( M O U T H ) 3 % ( TO P I C A L ) M E TA B O L I S M : - L I V E R E XC R E T I O N : - K I D N E Y M E LT I N G P O I N T : - 6 8 F O R M U L A : - C 1 4 H 2 2 N 2 O M O L A R M A S S : - 2 3 4 . 3 4 3 U S E S : - L I G N OC A I N E I N J E C T I O N B E L O N GS TO T W O G R O U P S O F M E D I C I N E S K N O W N A S L O C A L ANA E S T H E T I C S A N D A N T I A RR H YT H M I C D R UG S . L O C A L A N A E S T H E TI C S S TO P PA I N A ND F E E L I N G I N T H E A R EA A R OU N D W H E R E I T I S I N J E C T E D ; A N D A N T I A R R H YT H M I C D R U G S W O R K B Y R E S TO R I N G I R R E G U L AR A N D / O R R A P I D H E A RT B E AT S TO N O R M A L . Lignocaine
  • 40. F O R M U L A : - C 1 5 H 2 2 N 2 O M O L A R M A S S : - 2 4 6 . 3 5 4 U S E S : - M E P I VA C A I N E I S I N D I C AT E D F O R P R O D U C T I O N O F L O C A L O R R E G I O N A L A N A L G E S I A A N D A N E S T H E S I A B Y L O C A L I N F I LT R AT I O N , P E R I P H E R A L N E RV E B L O C K T E C H N I Q U E S , A N D C E N T R A L N E U R A L T E C H N I Q U E S I N C L U D I N G E P I D U R A L A N D C A U D A L B L O C K S . MEPIVACCINE
  • 41. R O U T E O F A D M I N I S T R AT I O N : - S U B C U TA N E O U S P R O T E I N B I N D I N G : - 5 5 % M E TA B O L I S M : - L I V E R A N D K I D N E Y F O R M U L A : - C 1 3 H 2 0 N 2 O M O L A R M A S S : - 2 2 0 . 3 1 6 U S E S : - T H I S M E D I C AT I O N C O NTA I N S 2 A M I D E - T Y P E L O C A L A N E S T H E T I C S , L I D O C A I N E A N D P R I L O C A I N E . I T I S U S E D O N N O R M A L, U N B R OK EN S K I N O R O N T H E O UT E R G E N I TAL A R EA TO P R E V E NT PAI N B E F O R E C E RTA I N P RO C E DU R E S S U CH A S I N S E RT I N G A N E E D L E , S KI N G R A F T S , O R S K I N L A S E R SU R G E RY. I T W O R KS B Y T E M P O R A R I LY N U M B I N G T H E S K I N A N D S U R R O U N DI N G A R E A . PRILOCAINE
  • 42. R O U T E O F A D M I N I S T R AT I O N : - PA R E N T E R A L M E TA B O L I S M : - H E PAT I C E XC R E T I O N : - R E N A L F O R M U L A : - C 1 7 H 2 8 N 2 O M O L A R M A S S : - 2 7 6 . 4 2 4 U S E S : - U S E D A S A L O C A L A N E S T H E T I C ( A M I D E C A I N E ) , I T H A S R A P I D O N S E T A N D L O N G A C T I O N P R O P E RT I E S , S I M I L A R TO B U P I VA C A I N E , A N D I S G I V E N B Y I N J E C T I O N D U R I N G S U R G I C A L P R O C E D U R E S A N D D U R I N G L A B O U R A N D D E L I V E RY. I T H A S A R O L E A S A L O C A L A N A E S T H E T I C . E T I D O C A I N E I S M A R K E T E D U N D E R T H E N A M E D U R A N E S T. ETIDOCAINE
  • 43. C H E M I C A L F O R M U L A : - C 1 8 H 2 2 N 2 O 2 M O L A R M A S S : - 2 9 8 . 3 8 6 U S E S : - P H E N A C A I N E I S A L S O K N O W N A S H O L O C A I N E I S A L O C A L A N E S T H E T I C U S E D I N O P H T H A L M I C M E D I C I N E . Phenacaine
  • 44. U S E S : - D I P E R O D O N I S O N E O F S E V E R A L PH E N Y L UR ET H A NE D E R I VAT I V E S O F D I A L K Y L A M I N O A L C O HO L S W H I C H H AVE D E M O N S T R AT E D S I G N I F I C A N T L O C A L A N A E S T H E T I C A C T I V I T Y . Diperodone
  • 45. F O R M U L A : - C 2 0 H 2 9 N 3 O 2 M O L A R M A S S : - 3 4 3 . 4 7 1 G M O L - 1 R O U T E O F A D M I N I S T R AT I O N : - TO P I C A L , I N T R AV E NO U S U S E S : - C I N C H O C A I N E I S T H E A C T I V E I N G R E D I E N T I N S O M E T O P I C A L H E M O R R H O I D C R E A M S S U C H A S P R O C T O S E D Y L . [ 3 ] I T I S A L S O A C O M P O N E N T O F T H E V E T E R I N A R Y D R U G S O M U L O S E , U S E D F O R E U T H A N A S I A O F H O R S E S A N D C A T T L E . Dibucaine