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ANESTESI LOKAL
(AL)

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Anestesi lokal
 Blok transmisi sensoris dr area
tubuh lokal ke SSP
 struktur kimia =
 blok kanal sodium membran
excitable
 sec. lokal, topikal, inj di area ttt

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 Kimia
Derivat Benzene
- ester
- amida

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Farmakokinetik
 AL short-acting perinj  cepat abs.
 efek sebentar
 Agar efek lebih lama :
 aliran darah ke area
+ vasokonstriksi
(simpatomimetik agonis)

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Cocain :
 efek simpatomimetik intrinsik
(hambat reuptake NE ke ujung saraf)

 tidak perlu vasokonstriktor

 Senyawa longer-acting
tetracaine & bupivacaine
tidak perlu vasokonstriktor

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AL Ester :

 cepat dimetab. o/ plasma

cholinesterase

 t ½ procaine & chloroprocaine

 1-2 menit

AL Amida
 dihidrolisa di liver
 t ½ 1.8-6 jam
 Bupivacaine & ropivacaine : sangat
larut lemak & long-acting
 Disfungsi liver   t ½ eliminasi

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Mekanisme Kerja
 blok voltage-dependent sodium
channel
 influx ion sodium
 cegah depolarisasi membran
 blok konduksi potensial aksi

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Interaksi

 Kadar K+ ekstraseluler >>   aktifitas AL

  Ca2+ ekstraseluler  mengantagonisnya

Efek
 Saraf
 Jar lain

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saraf
Perbedaan sensitifitas thd AL tgt :

 diameter serat
 myelinasi
 kec. firing fisiologis
 lokasi anatomis

Jaringan lain
 efek pada jantung (+)  anti-aritmia
klas I
 blok transmisi neuromuskular otot
skeletal
  emosi (cocaine)

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Penggunaan Klinis AL
 u/ bedah minor
 anestesi spinal
 u/ blokade otonomik pada iskemi
 Infus epidural, pelan, kadar rendah 
analgesi postoperasi (= infus opioid
epidural)
 Pemberian berulang inj epidural 
takifilaksis

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Toksisitas
 SSP
 Kardiovaskuler
 Lain

SSP
 Semua AL  efek sentral
 Sedasi, lelah, nistagmus & konvulsi
tonic-clonic
 Konvulsi berat  koma  depresi
pernapasan & kardiovaskuler

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Kardiovaskuler

 semua AL : vasodilator (kec cocaine)

 blok jantung & gg fungsi elektrik

jantung

 Bupivacaine iv  toksisitas
kardiovaskuler  aritmia & hipotensi

Cocaine
 blok reuptake NE pd junction
neuroeffector simpatetik
 efek vasokonstriksi
  toksisitas kardiovaskuler :
. hipertensi berat
. perdarahan serebral
. aritmia jantung
. infark miokard

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Efek toksik lain

 Prilocaine  metabolisme 
methemoglobinemia
 AL ester  metabolisme 
pembentukan antibodi pada px ttt
 AL amida : r/ alergi <<
 AL kadar >> : efek neurotoksik lokal

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Terapi toksisitas
 Simptomatis
 Konvulsi :
. diazepam iv
. barbiturat short-acting (thiopental)
. neuromuscular-bloker
 Hiperventilasi : oksigen

Subklas Prot ot ip Senyawa Senyawa

ut ama lain

Est er Procaine Cocaine, Benzocaine

t et racaine

Amida Lidocaine Bupivacaine Et idocaine,

prilocaine

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Thank You

Properties of local anesthetics

include all of the following EXCEPT

A. Blockade of voltage-dependent sodium

channels
B. Preferential binding to resting channels
C. Slowing of axonal impulse conduction
D. An increase in membrane refractory
period
E. Effects on vascular tone

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 Which of the following statements about

nerve blockade with local anesthetics is
most correct?

A. Block is faster in onset in infected tissues

B. Block is faster in onset in myelinated fibers
C. Block is faster in onset in hypocalcemia
D. Block is slower in onset in hyperkalemia
E. Block is slower in onset in the periphery of a
nerve bundle than in the center of a bundle

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