Chapter 10

Local Anesthetics

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Local Anesthetics

History of Local Anesthetics

Local anesthetics are derivatives of cocaine which is a derivative of the coca leaf

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Desirable Properties of Local Anesthetics

Potent Reversible Absence of local and systemic reactions Absence of allergic reactions Rapid onset and satisfactory duration Adequate tissue penetration Low cost Stability in solution

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Site and Mechanism of Action

Local anesthetics are divided into 2 chemical groups; esters and amides. Esters have a higher rate of allergic reaction. Local anesthetics slows or blocks depolarization by reducing Na permeability into the nerve cytoplasm, thus inhibiting the flow of K out of the cell. Nerve impulse travels from node to node. Local anesthetics effectively block nerve impulse travel.

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Ionization Factors

Local anesthetics are weak bases occurring equilibrated between their 2 forms, the fat soluble, free base and water-soluble hydrochloride salt. The portion of drug in each form is determined by the pKa of the local anesthetic and the pH of the environment. Once injected into local tissue, the amount of local anesthetic in the free base form increases and allows for greater tissue penetration. If there is an infection or inflammation, the free base form decreases and less drug penetrates the tissue. Other factors that can affect tissue penetration include inflammation, vasodilation, and dilution by fluid.
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Local Anesthetics

Absorption

Absorption of local anesthetics is dependent on the route of injection. Once injected, the rate of absorption is dependent on tissue vascularity. Tissue vascularity is a function of inflammation, vasodilating properties of the local anesthetic, presence of heat, or the use of massage. Systemic absorption of the local anesthetic is reduced with the addition of a vasoconstrictor.

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Local Anesthetics

Distribution The local anesthetic becomes partially bound to plasma and red blood cells. The unbound drug freely diffuses to other tissue including the CNS and across the placenta. Distribution allows absorption to occur in 3 phases.

The drug occurs at highly vascular tissues in the lungs and kidneys It appears in less vascular muscle and fat The drug is metabolized

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Local Anesthetics

Metabolism and Excretion

Primarily inactivated in the liver Excretion in urine 2-5% of active drug form Articaine is removed faster than the other amides

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Local Anesthetics

Pharmacologic Effects

The main pharmacologic effect of the local anesthetic is to reversibly block peripheral nerve conduction. Local anesthetics also have a direct effect on the cardiac muscle by blocking cardiac Na channels and depressing abnormal cardiac pacemaker activity, excitability, and conduction.

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Local Anesthetics

Adverse Reactions

Adverse reactions and toxicity of local anesthetics are directly related to drug plasma levels. The factors that influence toxicity include: Drug itself Concentration Route of administration Rate of injection Vascularity Patients weight Rate of metabolism and excretion
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Local Anesthetics

Adverse Effects

Both CNS stimulation and depression can occur. Local anesthetics can produce myocardial depression and cardiac arrest with peripheral vasodilation. Local effects include physical injury caused by poor injection technique. Malignant hyperthermia only occurs in those persons with the inherited autosomal dominant gene. It is not related to amide local anesthetic use. The incidence of allergic reactions to amide local anesthetics is very low.

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Composition of Local Anesthetics

Local anesthetic solutions are also made up of the following:

Vasoconstrictor that delays local anesthetic absorption, reduces systemic toxicity, and prolongs the duration of action. Antioxidant that delays the oxidation of epinephrine. Some are used to prolong shelf-life. Sodium hydroxide adjusts the pH of the solution to between 6 and 7. Sodium chloride makes the injectable solution isotonic.
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Local Anesthetic Agents

Several different amide local anesthetics are available for use. Choice of local anesthetic should be based upon onset of action, duration of local anesthesia required and side effects. Presence or absence of a vasoconstrictor. This is of particular importance if the patient has hypertension.

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Local Anesthetic Agents

Anesthetic Procaine pKa 9.1 Onset Slow Duration (with epi) (min) 45-90 Max Dose (with epi) (mg/kg) 8-10

Lidocaine
Bupivacaine Prilocaine Articaine

7.9
8.1 7.9 7.8

Rapid
Slow Medium Rapid

120-240
240-480 90-360 140-270

4.5-7
2.5-3 5-7.5 4-7

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Vasoconstrictors

Benefits of Local Anesthetics

Suppress systemic absorption of anesthetic agent Increase duration and intensify block Localize hemostasis Reduce toxicity Act on alpha and beta receptors in body tissues, causing the constriction of blood vessels

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Vasoconstrictors

Contraindications Heart attack in the last 6 months Uncontrolled high blood pressure Daily angina Tricyclic antidepressants Uncontrolled hyperthyroidism Uncontrolled arrhythmias

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Vasoconstrictors

Dental Concerns

Vasoconstrictors increase the length of anesthetic effect which increases the chance of accidental patient selfmutilation. In small quantities, epinephrine acts as a vasodilator thus having the potential to increase post-op bleeding. Patients with cardiovascular disease, who can receive a vasoconstrictor, should receive the lowest dose possible by means of the best injection technique. Ischemia Prolonged pain, numbness or paresthesia Feelings of nervousness or fast heart rate

Adverse Reactions

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Topical Anesthetics

Several different topical anesthetics are available for use. Choice should be based upon onset, duration of action, and allergenic potential. The patient should be instructed to avoid eating for 1 hour after application so that the gag reflex can become fully functional.

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Topical Anesthetics

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Topical Anesthetics

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