Local Anesthetics

Drug
pK (% base at pH 7.4)
Onset (min)
Protein binding (%)
Durationa (h)
T ½ (min)
Dose (mg/kg)
Relative potency
Lidocaine
7.9 (24 %)
1–3
65
1–2
96
4.5
1.0
Prilocaine
7.9 (24 %)
1–3
55
1–2
93
6
0.8
Mepivacaine
7.6 (36 %)
1–3
75
1.5–3
114
4.5
2.6
Articaine
7.8 (35 %)
1–3
~85
2.4–4
30
5
1.5
Bupivacaine
8.1 (17 %)
2–10
95
4–8
162
1.3
3.6
Adapted from Malamed [2] and Moore and Hersh [6]
Duration – infiltration versus block; volume and concentration injected, vasoconstrictor presence, and tissues assessed

Potency

The intrinsic potency of a local anesthetic is associated with lipid solubility and the concentration required to achieve the desired effect of nerve blockade. Procaine has the lowest intrinsic potency; lidocaine, prilocaine, and mepivacaine have intermediate potency; tetracaine, bupivacaine, and etidocaine are of high potency; and articaine is slightly more potent than lidocaine but is cleared three times faster from the body. It is important to note that these types of local anesthetics do not necessarily come in the same percent concentration; hence, caution is needed to prevent exceeding toxic doses of local anesthesia, especially when used in combination with other agents affecting the cardiovascular and CNS (e.g., sedatives).

Onset Time

Onset time is the time required for the local anesthetic solution to penetrate the nerve fiber and cause complete conduction blockade. Clinically, it must be understood that conduction blockade requires time for onset; otherwise, unnecessary pain may result from beginning a procedure too soon.

Duration

Duration of anesthesia is one of the most important clinical properties considered when choosing an appropriate local anesthetic agent for a given procedure. A local anesthetic with increased protein-binding capacity and a vasoconstrictor will have a longer duration than an agent with decreased protein binding and no vasoconstrictor. Lidocaine, mepivacaine, articaine and prilocaine have an intermediate duration, whereas bupivacaine and etidocaine have a long duration.

Onset

Local anesthesia of the soft tissues by the infiltration technique occurs almost immediately with all of the local anesthetics. As more tissue penetration becomes necessary, the intrinsic latency of onset previously discussed plays a greater role. Generally, in dentistry, for any given drug, the onset time required is shortest with an infiltration block, longer with a peripheral (minor) nerve block, and longest for topical anesthesia. Onset of action is also affected by the dissociation constant (pKa) and the pH at which two forms of the molecule, charged and uncharged, exist in equivalent amounts. In other words when pKa equals pH, half of the anesthetic molecules present will be charged and half uncharged. A lower pKa, closer to a physiologic pH of 7.4, will result in faster diffusion through tissues and into nerve fibers. This is especially important when dealing with an infected tooth where the pH of the surrounding tissues may be lower than the physiologic pH. In these cases, mepivacaine may be the agent of choice given its pKa of 7.6 compared to that of lidocaine at 7.9.

Duration

The duration of anesthesia varies greatly with the regional technique performed. This profile may differ for different agents, depending on their intrinsic pharmacologic properties. For example, lidocaine (1 %) with epinephrine (1:200,000) has a duration of 416 min with infiltration, 178 min with ulnar nerve block, 156 min with epidural anesthesia, and 94 min with spinal block.

Dose

The quality, onset time, and duration of a local anesthetic block may be improved by increasing the dose of the agent by using a higher concentration or greater volume. Increases in dosage must be limited by anesthetic toxicity; however, for consistently effective local anesthetic block, an adequate concentration and volume must be administered as close to the target nerve(s) as possible.
In a survey of local anesthetic usage in pediatric patients by Florida dentists, Cheatham and Primosch found that younger children received much higher dosages of local anesthetics than older children. Frequently, the amount of local anesthetic administered to young children far exceeded the manufacturers’ maximum recommended dose [7, 8].
During any dental treatment for children but especially during pediatric sedation, the maximum dose of local anesthetic to be administered to the child must be carefully calculated and recorded prior to its administration. Table 5.1 shows the recommended dosages for each local anesthetic commonly used in pediatric dentistry. Note that the dosages shown are lower than those recommended by the manufacturers. The rationale for these differences will be discussed in a subsequent section of this chapter.

Vasoconstrictors

Onset time, duration, and quality of block are also affected by the addition of vasoconstrictor agents to the local anesthetic solution. Vasoconstrictor agents such as epinephrine decrease the rate of drug absorption by decreasing blood flow to the tissues, prolonging the duration of the anesthesia produced, and increasing the frequency with which adequate anesthesia is attained and maintained. Toxic effects of local anesthetics are reduced as a result of delay in absorption into the circulation. Onset time of anesthesia is sometimes shortened as well.
Only gold members can continue reading. Log In or Register to continue

Oct 18, 2015 | Posted by in General Dentistry | Comments Off on Local Anesthetics
Premium Wordpress Themes by UFO Themes