Articaine anesthetic raw powder anesthetic raw powder is an intermediate-potency, short-acting amide local anesthetic with a fast metabolism due to an ester group in its structure. It is effective with local infiltration or peripheral nerve block in dentistry, when administered as a spinal, epidural, ocular, or regional nerve block, or when injected intravenously for regional anesthesia. In comparative trials, its clinical effects were not generally significantly different from those of other short-acting local anesthetics like lidocaine, prilocaine, and chloroprocaine, and there is no conclusive evidence demonstrating above-average neurotoxicity. Articaine proved to be suitable and safe for procedures requiring a short duration of action in which a fast onset of anesthesia is desired, eg, dental procedures and ambulatory spinal anesthesia, in normal and in special populations.
Patients with hepatic or renal impairment
Metabolism and elimination of exogenous substances in general depend significantly on normal function of the liver and kidney(s). Metabolism of local anesthetics produces metabolites that are more water soluble and ready to excrete than the parent compounds. Articaine is metabolized in the serum by plasma cholinesterase; although synthesis of cholinesterase is decreased in patients with liver diseases, fast hydrolysis is presumably preserved in their erythrocytes. Seventy-five percent of articainic acid is excreted unchanged; the rest is glucuronidated by the kidneys before excretion. In patients with severe renal failure, both metabolites can accumulate, which in theory can cause local anesthetic systemic toxicity (LAST). The pharmacokinetics of lidocaine have been studied in renal-failure patients receiving hemodialysis. Case reports describing other local anesthetics associate LAST with underlying cardiac, neurologic, pulmonary, renal, hepatic, or metabolic disease. The American Society of Regional Anesthesia and Pain Medicine advises that heightened vigilance may be warranted in these patients, particularly if they are at the extremes of age.
Pharmacodynamics of local anesthetics in children are comparable to those in adults; pharmacokinetics, on the other hand, differ significantly. Special caution should be observed when using the amide local anesthetics because a lower intrinsic clearance or a decreased serum protein binding can easily lead to an increased risk of toxic reactions in younger patients. The route of administration is one of the main determinants of safety in the use of local anesthetics in neonates and children; the application of articaine in children is mainly for those undergoing dental procedures for which local anesthesia is required or as an addition to general anesthesia. The absorption of local anesthetics from mucous membrane after topical anesthesia is increased in children due to a greater local blood flow and cardiac output than in adults. In a study investigating 27 children 3–12 years of age, the authors advised the use of 2% articaine in pediatric dentistry because of the lower Cmax and the shorter half-life. They showed a shorter time to maximum concentration and increased clearance compared to investigations in adults. Based on their findings, they concluded there is no need to lower the articaine dose administered to adults in mg/kg for children. Vasoactive agents like epinephrine are very effective in reducing systemic uptake of local anesthetics, resulting in a longer duration and a lower Cmax. Articaine 4% with epinephrine 1:100,000 was also shown to be effective and safe for use in pediatric dentistry. Among patients 4–13 years of age, the only adverse event directly related to articaine was accidental lip injury; no pharmacokinetic investigation was performed.
Prolonged numbness appears to be the most frequent adverse event after articaine for dental intervention, occurring primarily in children younger than 7 years old. Notwithstanding manufacturers’ recommendations that articaine not be used in children under 7 years of age, 21% of 373 American dentists satisfactorily use articaine in younger children-2–3 years of age. The available literature on articaine use in children shows that it is safe and effective for clinical procedures in children of all ages.
With advancing age, peripheral nerve conduction changes: there is a decrease in the number and density of nerve fibers, a degeneration of axons as a result of a reduction in the expression and axonal transport of cytoskeletal proteins, and an increase in motor unit action potentials. Peripheral motor and sensory conduction velocities slow progressively, and the onset latencies of F-waves and somatosensory evoked potentials increase gradually with advancing age. These and other age-related physiologic changes concerning the peripheral nervous system most probably have a direct effect on the clinical duration of peripheral nerve blocks and might be the cause of direct local anesthetic neurotoxicity. All local anesthetics are neurotoxic in a concentration-dependent manner due to neuroapoptosis, but articaine had the lowest apoptotic potency in a study investigating amide-type local anesthetics and ester-type local anesthetics in a human neuronal cell culture model.
Furthermore, aging is associated with loss of reserve capacity, and renal, hepatic, and cardiac diseases cause reduced clearance of local anesthetics, which requires reduction of the dose for repeated or continuous administration. The magnitude of the reduction of all local anesthetics should be related to the expected influence of the pharmacodynamic or pharmacokinetic change. In healthy elderly and young volunteers, it has been shown that the metabolism of articaine is age independent.
Pain management in the parturient requires knowledge of maternal and fetal physiology; the challenge is to provide fast analgesia and minimize physiologic perturbations. Epidural anesthesia with a variety of local anesthetics is by far the most used technique for this purpose. Articaine is rarely used for this indication. Two Russian investigators claimed that epidural anesthesia using a single dose of 1% articaine (Ultracaine) of 1.0–1.2 mg/kg in over 1000 healthy and high-risk parturients proved to be highly effective and safe for the mother and exerted no depressive effect on the newborn. Two German groups compared articaine (carticaine 1.5%) with bupivacaine for epidural anesthesia in cesarean sections (n = 25 and n = 15). Onset, quality of the analgesia, hemodynamic stability, and newborn Apgar scores were good. Pharmacokinetic investigation showed an articaine plasma concentration of 0.48 μg/mL at delivery, proving its rapid metabolism. The ratio of the unmetabolized drug to that of the metabolite found in maternal serum at that moment was 0.75. The umbilical venous-maternal arterial serum concentration ratio was 0.32. The latter is equal to early investigation after placental transfer of carticaine where the mean neonatal carticaine plasma concentration of nine newborns was found to be 32% (±7%) of the maternal after epidural anesthesia. Referenced in the literature for other local anesthetics are lidocaine (0.52–0.58), mepivacaine (0.64), and bupivacaine (0.23–0.26).
A special aspect that should be taken in account when articaine is used during pregnancy is its metabolism by plasma cholinesterases and the reduced hydrolysis rates in newborns and infants up to 6 months. Plasma cholinesterase activity or better butyrylcholinesterase (BChE) activity of healthy, normal infants has been found to be reduced by 50% compared to normal adults. This reduction seemed not of clinical importance.18 It can be of clinical importance if the newborn (and/or the mother) possesses one or more of the 58 possible known mutations in the butyrylcholinesterase gene (BCHE). BChE serves as the primary articaine hydrolase producing articainic acid; reduction or inactivity of BChE may contribute to increased toxicity after articaine use. However, articaine has an important second metabolism that prevents increasing plasma concentrations similar to cocaine toxicity in people with mutations in the BCHE gene that reduce BChE activity.
Articaine blocks nerve conduction by reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, similar to other local anesthetics. Binding of articaine to the sodium channel reduces sodium influx so that the threshold potential will not be reached and impulse conduction stops. The blocking action of articaine on the sodium channel is state dependent: it has the highest affinity for the open state, an intermediate affinity for the inactivated state, and the lowest affinity for the resting state.
The degree of neuronal block is affected by the diameter of the nerve. Larger-diameter fibers (touch/pressure/ motor) require higher concentrations of local anesthetic compared with small myelinated fibers (pain afferents). Articaine is lipid soluble, highly protein-bound (94%), and has a dissociation constant (pKa) of 7.8. Articaine is an intermediate-potency, short-acting local anesthetic with a fast onset of action.
Ascribing local anesthetic potency is an attempt to define the sensitivity of nerves to different local anesthetics and to estimate anesthetic requirements during regional anesthesia. The potency of local anesthetics increases parallel with increasing lipid solubility. The binding ability of local anesthetics to the phospholipid membrane as a result of physicochemical features and in vivo interaction has also been found to be directly in parallel with the potency. In clinical practice, other factors affect the potency of a local anesthetic, including:
hydrogen ion balance
fiber size, type, and myelination
vasodilator/vasoconstrictor properties (affects rate of vascular uptake)
frequency of nerve stimulation
ambient pH (lower pH results in greater ionisation and a reduction in efficacy)
electrolyte concentrations (hypokalemia and hypercalcemia antagonizes blockade)
For assessing the potency of different local anesthetics, dose-finding, single-dose nerve blocks are studied to determine the median effective dose or the minimum local analgesic dose. The relative analgesic potency for articaine, based on early investigations and specified of its equieffective anesthetic concentration, often compared to lidocaine, is intermediate.
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