Mekanisme Kerja Obat Anestesi Lokal

Ratno Samodro, Doso Sutiyono, Hari Hendriarto Satoto

Abstract
Regional anesthesia is growing and expanding its use, given the variety of benefits offered, such as
relatively cheap, minimal systemic effects, produce adequate analgesia and the ability to prevent the
stress response is more perfect. Local anesthetic drug is chemically divided into two major categories,
namely the class of Amide and ester groups. These chemical differences are reflected in differences in
the metabolism of the place, where the ester group is mainly metabolized by the enzyme pseudo-
cholinesterase in the plasma while the Amide groups mainly through enzymatic degradation in the
liver. This difference is also related to the magnitude of the possibility of allergies, in which the ester
group derived from p-amino-benzoic acid has a greater frequency of allergic tendencies. Local
anesthetic commonly used in our country for the class of esters are procaine, whereas the Amide
groups are lidocaine and bupivacaine. Mechanism of action of local anesthetic drugs to prevent
transmission of nerve impulses (conduction blockade) by inhibiting the delivery of sodium ions
through selective sodium ion gates in neuronal membranes. Failure of the sodium ion permeability of
the gate to increase the speed of depolarization of the slowdown as a potential threshold was not
reached so that action potentials are not propagated. Local anesthetic did not alter the resting potential
or transmembrane potential threshold. Pharmacokinetics of the drug include absorption, distribution,
metabolism and excretion. Complications of local anesthetic is a local side effects can occur at the
injection site hematoma and abscess while systemic side effects such as neurological in the central
nervous, respiratory, cardiovascular, immunological, musculoskeletal, and hematologic Some local
anesthetic drug interactions include coadministration may increase the potency of each drug.
decreased metabolism of local anesthetics as well as increase the potential for intoxication.

ABSTRAK

Anestesi regional semakin berkembang dan meluas pemakaiannya, mengingat berbagai keuntungan
yang ditawarkan, diantaranya relatif lebih murah, pengaruh sistemik yang minimal, menghasilkan
analgesi yang adekuat dan kemampuan mencegah respon stress secara lebih sempurna. Secara
kimiawi obat anestesi lokal dibagi dalam dua golongan besar, yaitu golongan ester dan golongan
amide. Perbedaan kimia ini direfleksikan dalam perbedaan tempat metabolisme, dimana golongan
ester terutama dimetabolisme oleh enzim pseudo-kolinesterase di plasma sedangkan golongan amide
terutama melalui degradasi enzimatis di hati. Perbedaan ini juga berkaitan dengan besarnya
kemungkinan terjadinya alergi, dimana golongan ester turunan dari p-amino-benzoic acid memiliki
frekwensi kecenderungan alergi lebih besar. Obat anestesi lokal yang lazim dipakai di negara kita
untuk golongan ester adalah prokain, sedangkan golongan amide adalah lidokain dan bupivakain.
Mekanisme kerja obat anestesi local mencegah transmisi impuls saraf (blokade konduksi) dengan
menghambat pengiriman ion natrium melalui gerbang ion natrium selektif pada membrane saraf.
Kegagalan permeabilitas gerbang ion natrium untuk meningkatkan perlambatan kecepatan
depolarisasi seperti ambang batas potensial tidak tercapai sehingga potensial aksi tidak disebarkan.
Obat anestesi lokal tidak mengubah potensial istirahat transmembran atau ambang batas potensial.
Farmakokinetik obat meliputi absorpsi, distribusi, metabolisme dan ekskresi. Komplikasi obat
anestesi lokal yaitu efek samping lokal pada tempat suntikan dapat timbul hematom dan abses
sedangkan efek samping sistemik antara lain neurologis pada Susunan Saraf Pusat, respirasi,
kardiovaskuler, imunologi ,muskuloskeletal dan hematologi Beberapa interaksi obat anestesi lokal
antara lain pemberian bersamaan dapat meningkatkan potensi masing-masing obat. penurunan
metabolisme dari anestesi lokal serta meningkatkan potensi intoksikasi.