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Local anesthetics (LA) can cause undesired effects such as sustained contraction of skeletal muscles as a result of structural and functional changes. Proper skeletal muscle function is controlled by intracellular Ca2+ concentration and efficient energy (ATP) production, which is closely related to cell ultrastructure. Aim: The aim of this study was to identify the structural and functional changes caused by LAs. Materials and Method: Male Wistar rats weighing 200 to 250g were used (n:49). They were divided into seven groups. One group was not anesthetized or treated (Control). The other six groups underwent intramuscular (IM) anesthesia with xylazine 2% (0.05 ml) and ketamine 50 mg/ml (0.1 ml/100g rat weight), and one of the following was applied to the masseter muscle (MM): no further treatment (Anesthetic Control group, CA); 0.1ml physiological saline solution (group SF); Carrageenin (group Carr) 1% as positive control group; prilocaine (group Pri), mepivacaine (group Mepi); or articaine (group Arti) 0.3M, IM. The animals were euthanized by cervical dislocation one hour after treatment. The effects of the different anesthetics on the MM were evaluated histologically and by electronic microscopy (EM). Ca-ATPase and membrane lipid peroxidation (LPX) were evaluated in muscle homogenates under the same conditions as those used to prepare the histological sections. Results: In general, structural damage and increased muscle contraction were observed in tissues treated with anesthetics. The most extreme values of Ca-ATPase activity and LPX were observed in the positive control group (carrageenin). Results were analyzed by one-way ANOVA for multiple comparisons and Tukey's test (p < 0.05). Conclusions: The results suggest that in the short term, local anesthetics affect the muscle function and are associated to structural changes., Competing Interests: The authors declare no conflicts of interest concerning the publication of this article., (SAIO.)

Local anesthetics used in dentistry have myotoxic effects. Articaine, also known as carticaine, is one of the local anesthetics most widely used in clinical dentistry. The aim of this work was to describe its effect on the sarcoplasmic reticulum Ca-ATPase isolated from medial pterygoid muscle. Ca-ATPase enzymatic activity was determined by a colorimetric method and ATP-dependent calcium uptake with a radioisotopic technique. Articaine inhibited both Ca-ATPase activity and calcium uptake in a concentration-dependent manner. Both inhibitory effects became evident at articaine concentrations lower than those employed in clinical dentistry. Half-maximal inhibitory concentrations (K) were 15.1 +/- 1.8 mM (n = 6) and 25.2 +/- 1.6 mM (n = 6) for enzymatic activity and calcium uptake, respectively. Preincubation of sarcoplasmic reticulum membranes with articaine enhanced Ca-ATPase activity in the absence of calcium ionophore, suggesting an ionophoric-like effect of the local anesthetic. We conclude that the inhibitory effect of articaine on the sarcoplasmic reticulum Ca-ATPase isolated from medial pterygoid muscle is due to a direct interaction of the anesthetic with the enzyme and to the increased membrane permeability to calcium induced by this drug.