Blok transmisi sensoris dr area tubuh lokal ke SSPstruktur kimia =blok kanal sodium membran excitablesec. lokal, topikal, inj di area ttt

Kimia Derivat Benzene - ester - amida

AL short-acting perinj cepat abs. efek sebentarAgar efek lebih lama : aliran darah ke area + vasokonstriksi (simpatomimetik agonis)

efek simpatomimetik intrinsik (hambat reuptake NE ke ujung saraf)

tidak perlu vasokonstriktor

Senyawa longer-acting tetracaine & bupivacaine tidak perlu vasokonstriktor

cepat dimetab. o/ plasma cholinesteraset procaine & chloroprocaine 1-2 menit

dihidrolisa di liver t 1.8-6 jamBupivacaine & ropivacaine : sangat larut lemak & long-actingDisfungsi liver t eliminasi

blok voltage-dependent sodium channel influx ion sodium cegah depolarisasi membran blok konduksi potensial aksi

Kadar K+ ekstraseluler >> aktifitas AL Ca2+ ekstraseluler mengantagonisnya

SarafJar lain

Perbedaan sensitifitas thd AL tgt : diameter seratmyelinasikec. firing fisiologis lokasi anatomis

efek pada jantung (+) anti-aritmia klas Iblok transmisi neuromuskular otot skeletal emosi (cocaine)

u/ bedah minoranestesi spinal u/ blokade otonomik pada iskemiInfus epidural, pelan, kadar rendah analgesi postoperasi (= infus opioid epidural)Pemberian berulang inj epidural takifilaksis

SSP

Kardiovaskuler

Lain

Semua AL efek sentralSedasi, lelah, nistagmus & konvulsi tonic-clonicKonvulsi berat koma depresi pernapasan & kardiovaskuler

semua AL : vasodilator (kec cocaine)blok jantung & gg fungsi elektrik jantung Bupivacaine iv toksisitas kardiovaskuler aritmia & hipotensi

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

Prilocaine metabolisme methemoglobinemiaAL ester metabolisme pembentukan antibodi pada px tttAL amida : r/ alergi > : efek neurotoksik lokal

SimptomatisKonvulsi : . diazepam iv . barbiturat short-acting (thiopental) . neuromuscular-blokerHiperventilasi : oksigen

Subklas

Prototip

Senyawa utama

Senyawa lain

Ester

Procaine

Cocaine, tetracaine

Benzocaine

Amida

Lidocaine

Bupivacaine

Etidocaine, prilocaine

Properties of local anesthetics include all of the following EXCEPT

Blockade of voltage-dependent sodium channelsPreferential binding to resting channels Slowing of axonal impulse conduction An increase in membrane refractory period Effects on vascular tone

Which of the following statements about nerve blockade with local anesthetics is most correct?

Block is faster in onset in infected tissues Block is faster in onset in myelinated fibers Block is faster in onset in hypocalcemia Block is slower in onset in hyperkalemiaBlock is slower in onset in the periphery of a nerve bundle than in the center of a bundle