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Mechanism of local anaesthetic:

Local anesthetic prevents the transmission of nerve impulses (conduction blockade) by


inhibiting the delivery of sodium ions through selective sodium ion gates in the nerve membrane.
The sodium gate itself is a specific receptor of local anesthetic molecules. The blockage of ion
gates that are open with local anesthetic molecules contributes a little to almost overall the
inhibition of sodium permeability. Failure of permeability of sodium ion gates to increase
deceleration speed of depolarization such as potential threshold is not achieved so the action
potential is not spread. Local anesthetic drugs work by not changing the potential transmembrane
residual or potential threshold.

Local anesthetics also block calcium channels and potassium and N-methyl-D-aspartate
(NMDA) receptors with any different degrees. Several other classes of drugs, such as tricyclic
antidepressants (amytriptiline), meperidine, inhalation anesthetics, and ketamine also have the
effect of blocking sodium channels.

Not all nerve fibers are affected equally by local anesthetics. Sensitivity to blockade is
determined by:

1. axonal diameter
larger-diameter myelinated fibers have a greater internodal distance than smaller
myelinated fibers, there is a differential sensitivity to the effects of local anesthetics
based on the diameter of the nerve fiber.
2. the size of myelination,
because conduction along myelinated nerves occurs from one node of Ranvier to
another (ie, saltatory conduction), a longer critical length is required for exposure to
local anesthetics for a block to occur. This results in a differential sensitivity of nerve
fibers to the effects of local anesthetics based on their size. Smaller nerve fibers, either
myelinated or unmyelinated, typically transmit pain and proprioceptive impulses,
whereas larger myelinated fibers carry motor impulses.
3. various other anatomical and physiological factors.

 The small diameter and the amount of myelin can increase the sensitivity of local
anesthesia.
 Thus, when local anesthetics are applied to a nerve trunk, there is a sequence of
disappearance of sensations based on the differential sensitivity of the nerves involved.
Typically, pain fibers are blocked first, followed by temperature, touch, pressure, and
motor function.

*note: penjelasan yang no.1 sama 2 gausah ditaroh di ppt gapapa pin, nanti dippt point2
nya aja… aku yg jelasin aja nnti.. biar di ppt ga trlalu banyak.

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