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8.3:

Anestésicos Locais: Farmacocinética

JoVE Core
Pharmacology
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JoVE Core Pharmacology
Local Anesthetics: Pharmacokinetics

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Pharmacokinetics describes how rapidly local anesthetics or LAs are absorbed, distributed, metabolized, and eliminated from the body, which affects their potency and duration of action. When LAs are administered in vascular tissues, they escape into the systemic circulation leading to unwanted effects. So, LAs are often administered with vasoconstrictors that reduce the local blood flow and limit the anesthesia to the target area. The distribution of LAs depends on the type of target tissue. For example, if an LA injected into the subarachnoid space has the same density as the cerebrospinal fluid, it will remain static, allowing localized anesthesia as long as the patient remains upright. The effects of LA are reversed when ester-linked LAs like procaine are metabolized by serum cholinesterases, while most amide-linked LAs are metabolized in the liver by cytochrome P450 enzymes. The resulting metabolites are water-soluble and can be eliminated by the kidneys.

8.3:

Anestésicos Locais: Farmacocinética

The potency and duration of action of local anesthetics (LAs) are determined by their pharmacokinetics. Pharmacokinetics describes how LAs are absorbed, distributed, metabolized, and eliminated from the body. When administered to the vascular tissues, LAs are quickly absorbed and enter the systemic circulation, reducing their localized effects. Adding vasoconstrictors such as epinephrine to LAs reduces their absorption into the systemic circulation, making them clinically effective. The vasoconstrictors localize the anesthetics at the desired site and enhance neuronal uptake to produce a more prolonged blockade. Vasoconstrictors also promote LA metabolism and elimination to reduce their systemic toxicity. Furthermore, vasoconstrictors reduce the total anesthetic requirement and extend anesthesia duration, making them suitable for lengthy surgical procedures and postoperative pain control.

However, the inclusion of vasoconstrictors can also have unwanted effects. It increases the probability of necrosis and edema in local tissues. It may reduce the local oxygen supply, which results in delayed wound healing. In susceptible individuals, LAs may increase blood pressure and cause arrhythmia.