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This crossover study aimed to compare the anesthetic effects of buffered 2% articaine with 1:200,000 epinephrine with that of non-buffered 4% articaine with 1:200,000 epinephrine. Forty-seven volunteers were administered two doses of anesthesia in the buccal region of the second mandibular molars in two sessions using 1.8 mL of different local anesthetic solutions. The onset time and duration of pulp anesthesia, soft tissue pressure pain threshold, and the score of pain on puncture and burning during injection were evaluated. The operator, volunteers, and statistician were blinded. There were no significant differences in the parameters: onset of soft tissue anesthesia (p = 0.80), duration of soft tissue anesthesia (p = 0.10), onset of pulpal anesthesia in the second (p = 0.28) and first molars (p = 0.45), duration of pulp anesthesia of the second (p = 0.60) and first molars (p = 0.30), pain during puncture (p = 0.82) and injection (p = 0.80). No significant adverse events were observed. Buffered 2% articaine with 1:200,000 epinephrine did not differ from non-buffered 4% articaine with 1:200,000 epinephrine considering anesthetic success, safety, onset, duration of anesthesia, and pain on injection.

Background: The aim of this study is to compare the effects of %4 articaine and %2 lidocaine on inferior alveolar nerve block (IANB) for implant surgery in the posterior mandible., Material and Methods: The patients who have inserted implants in the posterior mandible were divided into 2 groups for IANB: lidocaine and articaine. VAS = visual analog scale, pain during surgery and injection, lip numbness time, mandibular canal-implant apex distance, age, gender, bone density, implant number, release incision, adjacent teeth, and duration of surgery were analyzed using t-test, Mann-Whitney U test, Spearman's coefficient, and, Pearson's chi-squared test. This trial followed the recommendations of the Consort Statement for reporting randomized controlled trials., Results: 577 patients were included and 1185 dental implants were analyzed. There was no significant difference between the two groups in terms of injection and surgery VAS values (p>0.05). The lip numbness time of lidocaine was 3.06±3.22min while articaine was found to be 2.96±3.09min (p>0.05). Mandibular canal-implant apex distance was found to be 2.28±0.75mm in the articaine and 2.45±0.86mm in the lidocaine group (p<0.05). Release incision was made more in the articaine group (51/252) than in the lidocaine group (40/325) (p<0.05)., Conclusions: There was no difference between the %4 articaine and %2 lidocaine in terms of pain perception in posterior mandible implant applications. Both anesthetics provided adequate anesthesia for implant application.

As a new drug for local dental anesthesia, articaine has become popular in the clinic in recent years. In this review, we describe the development of articaine, explain its mechanism of action, compare its efficacy with that of other commonly used local anesthetics in dental treatment, and summarize the application of articaine in special populations. In conclusion, the anesthetic efficacy of articaine in clinical dental treatment is better than that of lidocaine, and its safety is not statistically different from that of lidocaine. In particular, articaine has several advantages and can be selected flexibly for clinical use. Atecaine has great potential for wide application in dental clinics in the near future., Competing Interests: The authors have no conflicts of interest to disclose., (Copyright © 2022 the Author(s). Published by Wolters Kluwer Health, Inc.)

Background: Inferior Alveolar Nerve Block (IANB) with Buccal Infiltration (BI) anaesthesia is required to completely anesthetize the mandibular molars with symptomatic irreversible pulpitis. 4% Articaine and 2% Lidocaine provide local anaesthesia during the nonsurgical endodontic treatment of mandibular molars with symptomatic irreversible pulpitis. Objective of the study was to compare the effect of Articaine and Lidocaine in the combination of Inferior alveolar nerve block with buccal infiltration anaesthesia during the nonsurgical endodontic treatment of mandibular molars with symptomatic Irreversible Pulpitis., Methods: One hundred and sixty participants with Symptomatic Irreversible Pulpitis of permanent mandibular molars were divided randomly in two groups. Group A was given Articaine 4% IANB along with BI whereas group B was given Lidocaine 2%. Pain was assessed after 15 minutes of administration of local anaesthesia. Anaesthetic success of the agents is defined as, absence of pain or mild pain first during the access cavity preparation then instrumentation of the canals of tooth. Chi-square test was applied to analyse data for statistical significance., Results: Anaesthetic success of Articaine was 96.2% during access cavity preparation compared to Lidocaine (86.2%). Success during instrumentation of canals was also found to be high in Articaine (90.2%) compared to Lidocaine (76.2%). This difference of anaesthetic efficacy between Articaine and Lidocaine was found statistically significant. (p=0.02)., Conclusions: Articaine is found to be better than Lidocaine regarding anaesthetic efficacy and hence, it can be a safer alternative to Lidocaine.

Anesthetic failure is common in dental inflammation processes, even when modern agents, such as articaine, are used. Nanostructured lipid carriers (NLC) are systems with the potential to improve anesthetic efficacy, in which active excipients can provide desirable properties, such as anti-inflammatory. Coupling factorial design (FD) for in vitro formulation development with in vivo zebrafish tests, six different NLC formulations, composed of synthetic (cetyl palmitate/triglycerides) or natural (avocado butter/olive oil/copaiba oil) lipids were evaluated for loading articaine. The formulations selected by FD were physicochemically characterized, tested for shelf stability and in vitro release kinetics and had their in vivo effect (anti-inflammatory and anesthetic effect) screened in zebrafish. The optimized NLC formulation composed of avocado butter, copaiba oil, Tween 80 and 2% articaine showed adequate physicochemical properties (size = 217.7 ± 0.8 nm, PDI = 0.174 ± 0.004, zeta potential = - 40.2 ± 1.1 mV, %EE = 70.6 ± 1.8) and exhibited anti-inflammatory activity. The anesthetic effect on touch reaction and heart rate of zebrafish was improved to 100 and 60%, respectively, in comparison to free articaine. The combined FD/zebrafish approach was very effective to reveal the best articaine-in-NLC formulation, aiming the control of pain at inflamed tissues.

The present study was conducted to determine the protective effect of articaine (ART) in an lipopolysaccharide (LPS)-induced acute kidney injury (AKI) animal model. The results suggest ART causes a significant decrease in serum blood urea nitrogen, creatinine, and serum cystatin C level, showing a protective effect against LPS-induced AKI. This has been further supported by histopathological findings of kidney tissues. The level of tumor necrosis factor-α, interleukin (IL)-6, and IL-1β in serum and kidney tissues was remarkably inhibited by ART in a dose-dependent manner. ART causes a significant reduction of malondialdehyde and increases the activities of glutathione and superoxide dismutase with an increase in dose as compared to the LPS-treated group. Moreover, the ART-treated group showed dose-dependent inhibition of LPS-induced nuclear factor-κB activation and TLR4 expression as confirmed by Western blot analysis. The level of Bcl-2 family genes (Bcl-2 and Bax) was restored near to normal by ART. Collectively, all the above results indicated that ART had protective effects against LPS-induced AKI by blocking inflammatory and oxidative responses., (© 2020 Wiley Periodicals LLC.)

The local anesthetics lidocaine and articaine are among the most widely used drugs in the dentist's arsenal, relieving pain by blocking voltage-dependent Na + channels and thus preventing transmission of the pain signal. Given reports of infrequent but prolonged paresthesias with 4% articaine, we compared its neurotoxicity and functional impairment by screening cultured neural SH-SY5Y cells with formulations used in patients (2% lidocaine + 1:100,000 epinephrine or 4% articaine + 1:100,000 epinephrine) and with pure formulations of the drugs. Voltage-dependent sodium channels Na(v)1.2 and Na(v)1.7 were expressed in SH-SY5Y cells. To test the effects on viability, cells were exposed to drugs for 5 minutes, and after washing, cells were treated with the ratiometric Live/Dead assay. Articaine had no effect on the survival of SH-SY5Y cells, while lidocaine produced a significant reduction only when used as pure powder. To determine reversibility of blockage, wells were exposed to drugs for 5 minutes and returned for medium for 30 minutes, and the calcium elevation induced by depolarizing cells with a high-potassium solution was measured using the calcium indicator Fura-2. High potassium raised calcium in control SH-SY5Y cells and those treated with articaine, but lidocaine treatment significantly reduced the response. In conclusion, articaine does not damage neural cells more than lidocaine in this in vitro model. While this does not question the safety of lidocaine used clinically, it does suggest that articaine is no more neurotoxic, at least in the in vitro setting.

The selection of local anaesthetic in dental practice is essential to the patient's comfort and the success of the treatment. Many patients prefer anaesthesia even for short treatments. Articaine is a local anaesthetic commonly used for dental practice. The duration of the effect of articaine on the nerve fibres is not yet precisely reported. This study was aimed to evaluate the clinical efficacy of 4% articaine with and without epinephrine in treatment of occlusal caries. Thirty healthy patients were included in this randomised double-blind study. Each subject received 4% articaine with and without epinephrine (1:100 000). Maxillary infiltration was used for occlusal caries of the maxillary premolars on right and left sides. Quantitative sensory testing (QST) was performed in the innervation area of the infraorbital nerve, and pulp vitality test was performed on restoration-free canines. Duration of anaesthesia was longer when articaine with epinephrine was used. Articaine without epinephrine showed faster recovery of sensory blockade compared to articaine with epinephrine. The epinephrine-containing agent, when compared to the plain articaine solution, showed significantly stronger and longer anaesthetic efficacy on the soft tissue by all parameters of QST. Articaine with epinephrine caused a more reliable pulpal analgesia. A pain-free treatment of the soft tissue up to 15 minutes can be performed under the vasoconstrictor-free anaesthetic without causing long-lasting numbness. Epinephrine-containing articaine delivers a longer, more effective anaesthesia and is preferable for caries treatments and longer invasive treatments of the soft tissue., (© 2018 John Wiley & Sons Ltd.)

Objective: Chronic stress can alter nociceptive sensitivity. However, the effect of stress exposure on dental nociception has been less addressed. Therefore, the present study investigated the effects of chronic exposures to some social and psychological stresses on pulpal nociceptive responses., Design: The stress groups were constructed as follows: forced swimming (n=6), restraint (n=6), and mild (n=10) and severe (n=15) crowding stresses. Rats were subjected to stress for 1h per day for a week. At the end of the stress session, pulp irritation was induced by intradental application of capsaicin (100μg). There were another capsaicin or capsaicin plus stress training groups that received articaine 5min before the administration of capsaicin. Nociceptive responses were recorded for 40min. The time (ins) of continuous shaking of the lower jaw and excessive grooming and rubbing of the mouth near the procedure site was measured as nociceptive behaviors. Data was analyzed using one-way analysis of variance (ANOVA) followed by post hoc Tukey's test., Results: Significant nociceptive responses were evoked by the administration of capsaicin. Exposures to forced swimming (p<0.01), restraint (p<0.001), and both mild and severe crowding stresses (p<0.05) exaggerated capsaicin-induced nociceptive reaction. There was, however, no significant difference in nociceptive reaction time between the different stress groups. Articaine buccal infiltration attenuated nociceptive time in capsaicin and capsaicin plus stress training groups (p<0.001)., Conclusions: The current data support the association between chronic stress exposures and nociceptive behavior following intradental capsaicin administration., (Copyright © 2017 Elsevier Ltd. All rights reserved.)

Since a significant proportion of diabetic patients have clinical or subclinical neuropathy, there may be concerns about the use of local anaesthetics. The present study was designed to determine and compare the effects of articaine, a widely used anaesthetic in dental practice, and lidocaine on the resting and axonal stimulation-evoked release of [ 3 H]noradrenaline ([ 3 H]NA) in prefrontal cortex slices and the release of [ 3 H]NA in spinal cord slices prepared from non-diabetic and streptozocin (STZ)-induced diabetic (glucose level=22.03±2.31mmol/l) rats. The peak of allodynia was achieved 9 weeks after STZ-treatment. Articaine and lidocaine inhibited the stimulation-evoked release in a concentration-dependent manner and increased the resting release by two to six times. These effects indicate an inhibitory action of these anaesthetics on Na + - and K + -channels. There was no difference in clinically important nerve conduction between non-diabetic and diabetic rats, as measured by the release of transmitter in response to axonal stimulation. The uptake and resting release of NA was significantly higher in the brain slices prepared from diabetic rats, but there were no differences in the spinal cord. For the adverse effects, the effects of articaine on K + channels (resting release) are more pronounced compared to lidocaine. In this respect, articaine has a thiophene ring with high lipid solubility, which may present potential risks for some patients., (Copyright © 2017 The Authors. Published by Elsevier Inc. All rights reserved.)

Aim: The aim of this study is to assess the efficacy of 4% articaine with 1:100,000 adrenaline given as buccal and lingual infiltration in adult patients undergoing erupted mandibular first and second molar teeth extraction versus inferior alveolar nerve block technique using 2% lignocaine with 1:80,000 adrenaline., Materials and Methods: A total of 100 patients undergoing extraction of mandibular posterior teeth were divided into two equally matched groups for the study, out of which 50 patients were given 4% articaine with 1:100,000 adrenaline as buccal and lingual infiltration and 50 patients were given 2% lignocaine with 1:80,000 adrenaline using classic direct inferior alveolar nerve block with lingual and buccal nerve block. Efficacy of anesthesia was determined using a numeric analog scale (NAS) ranging from 0 indicating no pain to 10 indicating the worst pain imaginable. The NAS was taken by a different operator to avoid bias., Results: The pain scores in both groups were analyzed using the Mann-Whitney U test, and a p value of 0.338 was obtained which is not statistically significant. Hence, no significant difference in the pain score was established between both groups. The adverse effects of both the local anesthetics if any were noted., Conclusion: From this study, we concluded that the use of 4% articaine with 1:100,000 adrenaline is as effective as inferior alveolar nerve block with lignocaine but without the risk of attendant adverse effects of inferior alveolar nerve block technique.

Aims: To determine the effect of articaine on sarcoendoplasmic reticulum calcium adenosine triphosphatase (SERCA) isoforms of the medial pterygoid muscle., Methods: Native SERCA from the medial pterygoid muscles of 24 rabbits was isolated by ultracentrifugation, and its isoforms were purified by chromatography and assessed by enzyme-linked immunosorbent assay (ELISA). SERCA activity and calcium transport capability were determined by using colorimetric and radioisotopic methods. The mean ± standard deviation (SD) half maximal inhibitory concentration (IC50) of articaine was determined for each isoform, and these values were compared by using analysis of variance (ANOVA) (P < .05)., Results: The native SERCA preparation consisted of 34% SERCA1a, 53% SERCA2a, 10% SERCA2b, and 3% combined SERCA3 and SERCA1b. Articaine caused inhibition of activity and calcium uptake in the native SERCA preparation and in each of the purified isoforms. The IC50 (mM) values for enzymatic activity were: SERCA1a 22.0 ± 2.3 > SERCA2a 16.4 ± 2.4 > SERCA2b 11.3 ± 1.9, and 15.1 ± 2.1 for native SERCA. For calcium transport, IC50 values were: SERCA1a 31.1 ± 3.3 > SERCA2a 24.8 ± 1.8 > SERCA2b 21.5 ± 1.5, and 25.2 ± 3.2 for native SERCA. IC50 values for inhibition of enzymatic activity were significantly different among the purified isoforms, but only the value obtained for SERCA1a was significantly different compared to native SERCA. For inhibition of calcium transport, IC50 values for both SERCA2a and SERCA2b differed significantly compared to SERCA1a, and the value for SERCA1a was significantly different compared to native SERCA. The most articaine-sensitive isoform was SERCA2b, and the native preparation showed sensitivity similar to SERCA2a., Conclusion: The differential inhibition of articaine on medial pterygoid SERCA isoforms is evident at concentrations lower than used in current dental practice (125 mM) and accounts for anesthetic myotoxicity. Muscle relaxation likely becomes impaired as a result of increased calcium levels in the myoplasm due to the decreased activity and calcium transport caused by the inhibition of SERCA.

Objective: To determine if full crown preparation causes an increase in pulpal blood flow (PBF), indicating inflammation, in human subjects., Design: The experiments were carried out on 35 intact, mandibular posterior teeth in 13 subjects: 32 were abutments for 16 fixed bridges that replaced first molars; the other 3 were first premolars adjacent to abutment teeth that served as un-operated controls. Crown preparations were made using an air-rotor with water-spray under regional block anaesthesia (4% articaine with epinephrine 1:100,000). PBF was recorded with a laser Doppler flow meter (LDF) before and after administering the anaesthetic, with the LDF probe on the buccal enamel. PBF was then recorded from the abutment teeth with the probe on buccal dentine after preparing the buccal surfaces of both teeth, after completing the crown preparations, and after 1 and 7days. PBF was also recorded from the buccal enamel of the control teeth on each occasion., Results: The mean±S.D. PBF values before and after anaesthesia were 2.63±2.13 and 2.42±2.38P.U. respectively, which were not significantly different (Paired t-test). The mean values for the abutment teeth after buccal preparation, after complete crown preparation, and after 1 and 7days were 5.20±2.49, 4.53±2.52, 4.92±2.98 and 5.48±2.65P.U. respectively. The 4 values for each tooth were not significantly different (two-way RM ANOVA). In the control group, the values under all six conditions were not significantly different., Conclusions: Regional block anaesthesia produced no change in PBF, nor did full-crown preparation, neither immediately after the procedure nor 1 and 7days later., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Drug effects of loco-regional anesthetics are commonly measured by unidimensional pain rating scales. These scales require subjects to transform their perceptual correlates of stimulus intensities onto a visual, verbal, or numerical construct that uses a unitless cognitive reference frame. The conceptual understanding and execution of this magnitude estimation task may vary among individuals and populations. To circumvent inherent shortcomings of conventional experimental pain scales, this study used a novel perceptual reference approach to track subjective sensory perceptions during onset of an analgesic nerve block. In 34 male subjects, nociceptive electric stimuli of 1-ms duration were repetitively applied to left (target) and right (reference) mandibular canines every 5 s for 600 s, with a side latency of 1 ms. Stimulus strength to the target canine was programmed to evoke a tolerable pain intensity perception and remained constant at this level throughout the experiment. A dose of 0.6 ml of articaine 4% was submucosally injected at the left mental foramen. Subjects then reported drug effects by adjusting the stimulus strength (in milliamperes) to the reference tooth, so that the perceived intensity in the reference tooth was equi-intense to the target tooth. Pain and stimulus perception offsets were indicated by subjects. Thus, the current approach for matching the sensory experience in one anatomic location after regional anesthesia allows detailed tracking of evolving perceptual changes in another location. This novel perceptual reference approach facilitates direct and accurate quantification of analgesic effects with high temporal resolution. We propose using this method for future experimental investigations of analgesic/anesthetic drug efficacy., (Copyright © 2016 the American Physiological Society.)

Objective: To evaluate success of pulpal anaesthesia of mandibular 1st molar by using 4% articaine in buccal infiltration versus 2% lidocaine in inferior alveolar nerve block., Study Design: Randomized control trial., Place and Duration of Study: Department of Operative Dentistry, Sardar Begum Dental College, Gandhara University, Peshawar, from March to August 2014., Methodology: One hundred and fifty-six emergency patients, who had 1st molar diagnosed with irreversible pulpitis, participated in the study. Subjects were divided into two groups by random allocation. One group received 4% articaine buccal infiltration and the other group received inferior alveolar nerve block of 2% lidocaine. Subjects&rsquo;self-reported pain response was recorded on Heft Parker Visual Analogue Scale after local anaesthetic administration during access cavity preparation and pulp extirpation., Results: Mean age of subjects was 31.46 &plusmn;10.994 years. The success rate of 4% buccal infiltration was 76.9%; whereas the success rate of 2% lidocaine inferior alveolar nerve block was 62.8%. There was no statistically significant difference between the two groups., Conclusion: 4% articaine buccal infiltration can be considered a viable alternative to 2% lidocaine inferior alveolar nerve block in securing successful pulpal anaesthesia for endodontic therapy.

Aim: To compare the anaesthetic efficacy of different volumes (1.8 mL vs. 3.6 mL) of 4% articaine with 1 : 100 000 epinephrine injected as buccal infiltrations after a failed inferior alveolar nerve block (IANB) in patients with symptomatic irreversible pulpitis., Methodology: Two hundred and thirty-four adult patients, diagnosed with irreversible pulpitis in a mandibular tooth, participated in this multicentre, randomized double-blinded trial. Patients received IANB with 1.8 mL of 4% articaine with 1 : 100 000 epinephrine. Pain during treatment was recorded using the Heft-Parker visual analogue scale (HP VAS). The primary outcome measure, and the definition of 'success', was the ability to undertake pulp chamber access and canal instrumentation with no or mild pain (HP VAS score <55 mm). Patients who experienced 'moderate-to-severe' pain (HP VAS score ≥ 55 mm) were randomly allocated into two groups and received buccal infiltrations with either 1.8 mL or 3.6 mL of 4% articaine with 1 : 100 000 epinephrine. Root canal treatment was re-initiated after 10 min. Success was again defined as no pain or weak/mild pain during endodontic access preparation and instrumentation. Statistical analysis was performed using Mann-Whitney U and chi-square tests., Results: The initial IANB of 4% articaine gave an overall success rate of 37%. The success rate of supplementary buccal infiltration with 1.8 and 3.6 mL volumes was 62% and 64%, respectively. The difference between the success rates of the two volumes was not statistically significant., Conclusions: Increasing the volume of 4% articaine with 1 : 100 000 epinephrine from 1.8 to 3.6 mL, given as supplementary buccal infiltrations after a failed primary IANB with 1.8 mL of 4% articaine with 1 : 100 000, did not improve the anaesthetic success rates in patients with symptomatic irreversible pulpitis., (© 2014 International Endodontic Journal. Published by John Wiley & Sons Ltd.)

One of the current challenges in drug encapsulation concerns the development of carrier systems for hydrophilic compounds. Potential carriers include nanocapsules prepared with amphiphilic polymers, which consist of a polymeric coating surrounding an aqueous nucleus, or dense matrices such as nanospheres of alginate/chitosan, where the drug may be dispersed in the matrix or adsorbed on the surface. The development of new formulations of nanocarriers, for example the poly(ethylene glycol)-poly(ɛ-caprolactone) (PEG-PCL) nanocapsules and alginate/chitosan (AG/CS) nanospheres described in this work, is needed in the case of ionized drugs such as articaine. This amino amide local anesthetic is the drug of choice in dentistry for regional anesthesia as well as the relief of acute and chronic pain. Here, the physico-chemical properties of suspensions of the nanoparticles (considering diameter, polydispersion, and zeta potential) were determined as a function of time, in order to establish the stability of the systems. The formulations did not show any substantial changes in these parameters, and were stable for up to 120 days of storage at ambient temperature. Satisfactory encapsulation efficiencies were obtained for the PEG-PCL nanocapsules (60%) and the AG/CS nanospheres (45%). Cytotoxicity assays confirmed that the encapsulation of articaine reduced its toxicity, relative to the free drug. The most promising results were obtained using the vesicular system (PEG-PCL nanocapsules), which not only altered the release profile of the drug, but also resulted in the lowest toxicity. This carrier system therefore holds promise for use in future practical applications., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Purpose of Review: Spinal anesthesia (SPA) has not been popular for day-case surgery because of prolonged neurologic blockade with long-acting local anesthetics such as bupivacaine, thereby delaying discharge. Although the intermediate duration of action of lidocaine and mepivacaine appears to be more suitable for day-case surgery, their use is not deemed appropriate by many because of a high incidence of transient neurologic symptoms (TNSs). The present review summarizes recent clinical data on the intrathecal use of alternative local anesthetics and adjuvants that may offer valuable alternatives to general anesthesia in day-case surgery., Recent Findings: Prilocaine has a similar intrathecal pharmacokinetic profile as lidocaine but with a significantly lower risk of TNSs. Onset of spinal after 2-chloroprocaine is comparable with lidocaine or prilocaine, but with a considerably shorter duration of action. Also, TNS is clearly less frequent compared with lidocaine. Although its intrathecal use has recently been approved in Europe, this is still considered to be off-label in the USA. Articaine provides an extraordinary fast onset and a short duration of spinal block, the latter being approximately intermediate between chloroprocaine and prilocaine. However, articaine is associated with a high risk for intraoperative hypotension and a small risk for TNS, albeit but less frequent than after lidocaine. Concerns regarding possible neurotoxicity of articaine remain to be resolved., Summary: SPA for day cases might become a most valuable method for ambulatory surgery when using short acting local anesthetics. This, however, not only depends on drugs being used but also on infrastructure (post anaesthesia care unit) and organizational issues.

Objective: To evaluate hemodynamic changes with the use of 4% articaine and 2 different concentrations of epinephrine (1:100,000 and 1:200,000) in the surgical removal of symmetrically positioned lower third molars., Study Design: A prospective, randomized, double-blind clinical trial was carried out involving 42 patients each undergoing 2 surgeries on separate occasions under local anesthesia with 4% articaine and either epinephrine 1:100,000 or 1:200,000. The following parameters were assessed at 4 different moments: systolic, diastolic, and mean blood pressure; heart rate; oxygen saturation; rate pressure product (RPP); and pressure rate quotient (PRQ)., Results: The concentration of epinephrine did not affect diastolic blood pressure or oxygen saturation during the surgeries. Significant differences between were detected for heart rate, RPP, and PRQ (P < .05)., Conclusions: The epinephrine concentration (1:100,000 or 1:200,000) in a 4% articaine solution influences hemodynamic parameters without perceptible clinical changes in healthy patients undergoing lower third molar removal., (Copyright © 2013 Elsevier Inc. All rights reserved.)

Introduction: The aim of this study was to compare the efficacies of buccal local anesthetic infiltrations at various sites of the mandible in order to elucidate the mechanism of action of articaine mandibular infiltrations., Methods: After a power calculation and ethical approval, 22 volunteers received 1.8 mL 4% articaine hydrochloride with 1:100,000 adrenaline as a buccal infiltration at the canine, first, or second molar in a randomized, double-blind, crossover design. The injections at the canine and first molar were considered equidistant from the mental foramen. Responses of the first and second molars, first premolar, and lateral and central incisors were assessed using an electronic pulp tester over a 47-minute period. Volunteers were asked to rate the discomfort of each injection using a visual analog scale. Data were analyzed using repeated measures analysis, McNemar, and Mann-Whitney U testing., Results: Injections at the canine and first molar teeth produced anesthesia in all teeth tested in some volunteers. There was no significant difference between anesthetic success of the first premolar after infiltration at the canine or the first molar. Injection at the second molar failed to produce anesthesia of the incisor teeth. Anesthesia was significantly more likely after injections at an adjacent site. There was no difference in discomfort associated with injections at different sites of the mandible., Conclusions: Articaine first mandibular molar infiltrations achieve an effect via a combination of modified mental and incisive nerve block and local infiltration. Infiltration at the second molar produces anesthesia of both molar and premolar teeth, primarily via infiltration., (Copyright © 2013 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.)

Background: The aim of the present study was to analyze hemodynamic changes after the administration of either 2% lidocaine with epinephrine 1:100,000 (L100) or 4% articaine with epinephrine 1:200,000 (A200) in the surgical removal of symmetrically positioned lower third molars., Methods: A prospective, randomized, double-blind, clinical trial was carried out involving 43 patients. Each patient underwent 2 surgeries on different occasions-one under local anesthesia with L100 and the other with A200. The following parameters were assessed at 4 different times: systolic, diastolic, and mean blood pressure; heart rate; oxygen saturation; rate pressure product (RPP); and pressure rate quotient (PRQ)., Results: No hypertensive peak was observed in systolic, diastolic, and mean blood pressure at any evaluation time. Moreover, the type of anesthetic solution did not affect diastolic blood pressure, oxygen saturation or PRQ during the surgeries. Statistically significant differences between groups were detected with regard to heart rate and RPP (P < 0.05)., Conclusions: The epinephrine concentration (1:100,000 or 1:200,000) and local anesthetic solutions used (2% lidocaine or 4% articaine) influenced hemodynamic parameters without perceptible clinical changes in healthy patients undergoing lower third molar removal.

Objectives: The aim of the present study is to compare cardiovascular safety profiles of two dental anesthetics: articaine versus two standard mepivacaine solutions used during etiological periodontal treatment in cardiovascular patients., Study Design: Using a cross-over study design, ten cardiovascular patients were randomly assigned to dental treatment with 1.8 mL of a local anesthetic injected on each quadrant of the mouth: Articaine (40 mg with Epinephrine 0.5 mg % and 40 mg with Epinephrine 1mg %) or Mepivacaine (30 mg and 20 mg with Epinephrine 1mg %). A computer programme enabled continuous longitudinal data collection: O2 saturation, blood pressure (BP) and heart rate (HR)., Results: No severe clinical side effects were observed. During the treatment period, we observed statistically significant differences as regards HR between injections with and without adrenalin (p< 0.039) and as regards systolic (p< 0.046) and diastolic (p < 0.046) blood pressure during the stabilization period. In both cases, the parameters under study increase. Age, gender, jaw treated, treatment duration and the rest of cardiovascular variables did not affect the results. None of the patients underwent ischemic alterations or any other complication derived from the treatment or the anesthesia., Conclusions: According to the results of our study, dental anesthetics with standard concentrations of Epinephrine seem to alter HR and BP. Although no cardiac ischemic alterations or any other cardiovascular complications have been observed, we must be cautious with the administration of anesthetics containing vasoconstrictors in patients with cardiovascular diseases.

Background: An increase in blood pressure during dental treatment has been investigated with regard to potential medical risks since previous studies suggest that dental procedures may cause stress to the patient and, consequently, the cardiovascular system. The aim of the present study was to analyze hemodynamic changes following the administration of either 2% lidocaine (L100) or 4% articaine (A100) (both with epinephrine 1:100,000) in the surgical removal of symmetrically positioned lower third molars., Methods: A prospective, randomized, double-blind, clinical trial was carried out involving 47 patients. Each patient underwent 1 surgery at each of 2 appointments--one under local anesthesia with L100 and the other with A100. The following parameters were assessed at 4 different times: systolic, diastolic, and mean blood pressure; heart rate; oxygen saturation; rate pressure product; and pressure rate quotient., Results: No hypertensive peak was observed in systolic, diastolic, and mean blood pressure at any evaluation time. Moreover, the type of anesthetic solution did not affect diastolic blood pressure, heart rate, or oxygen saturation during the surgeries. The pressure rate quotient was the only parameter to exhibit statistically significant differences between groups at different evaluation times (P < 0.05)., Conclusions: The hemodynamic parameters evaluated in third molar surgery with 2% lidocaine and 4% articaine (both with epinephrine 1:100,000) did not show significant differences.

Local anesthetics have an impressive history of efficacy and safety in medical and dental practice. Their use is so routine, and adverse effects are so infrequent, that providers may understandably overlook many of their pharmacotherapeutic principles. The purpose of this continuing education article is to provide a review and update of essential pharmacology for the various local anesthetic formulations in current use. Technical considerations will be addressed in a subsequent article.

Objectives: To compare the clinical anesthetic efficacy of 0.5% bupivacaine and 4% articaine (both with 1:200.000 adrenaline) for anterior maxillary infiltration in healthy volunteers., Material and Methods: A triple-blind split-mouth randomized clinical trial was carried out in 20 volunteers. A supraperiosteal buccal injection of 0.9 ml of either solution at the apex of the lateral incisor was done in 2 appointments separated 2 weeks apart. The following outcome variables were measured: latency time, anesthetic efficacy (dental pulp, keratinized gingiva, alveolar mucosa and upper lip mucosa and tissue) and the duration of anesthetic effect. Hemodynamic parameters were monitored during the procedure., Results: Latency time recorded was similar for both anesthetic solutions (p>0.05). No statistically significant differences were found in terms of anesthetic efficacy for dental pulp, keratinized gingiva or alveolar mucosa. Articaine had a significant higher proportion of successful anesthesia at 10 minutes after infiltration in lip mucosa and lip skin (p=0.039). The duration of anesthesia was 336 minutes for bupivacaine and 167 minutes for articaine. (p<0.001). No significant hemodynamic alterations were noted during the procedure., Conclusions: Articaine and bupivacaine exhibited similar anesthetic efficacy for maxillary infiltrations. The duration of anesthesia was longer with the bupivacaine solution, but lip anesthesia was better with articaine.

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.

Aim: To compare the efficacy, onset time and duration of maxillary infiltration anaesthesia with 0.5% plain ropivacaine or 4% articaine with epinephrine 1 : 100 000 and to determine their possible influence on cardiovascular parameters., Methodology: Sixty volunteers received 1.8 mL of the anaesthetic for buccal infiltration anaesthesia of maxillary central and lateral incisors and canine teeth without caries, restorations or signs of pulpitis. The efficacy, onset time and duration of pulp anaesthesia were assessed with an electric pulp tester. The duration of numbness of the upper lip was also monitored. Blood pressure and heart rate were measured before and after administration of the solutions., Results: The efficacy of anaesthesia of lateral and central incisors was 100% for both anaesthetics. There were insignificant differences in effectiveness of canine pulp anaesthesia. The mean onset time was significantly (P < 0.05) shorter for ropivacaine (2.22 min) when compared with articaine (4.08 min). The duration of action and soft tissue anaesthesia were also significantly (P < 0.05) longer for ropivacaine (79.2 and 264 min) when compared with articaine (63.7 and 195.2 min, respectively). Ropivacaine caused significant (P < 0.05) increases in blood pressure and heart rate., Conclusions: Ropivacaine (0.5%) achieved effective and long duration of uninflamed pulp and soft tissue anaesthesia. Ropivacaine could be useful for long-lasting operative procedures without the need for a vasoconstrictor., (© 2011 International Endodontic Journal.)

Background: We performed this study to quantify the detrimental effect of intraneural injection of 50 μL of saline, articaine 2%, or articaine 4% in the rat sciatic nerve., Methods: Lumbar-evoked electrospinograms from stimulation of the sciatic nerve were recorded before and immediately after injection and again after 3 weeks. Test substance was injected into the right sciatic nerve, and the untreated left sciatic nerve served as control. The animals were killed after the 3-week follow-up, and cross-sections of the sciatic nerve were examined stereologically., Results: The evoked spinal cord field potential in the articaine groups faded away immediately after injection and was concentration-dependently, significantly more reduced at the 3-week follow-up in comparison with the saline group. The response from the control sides was unaffected in all groups. The number of myelinated axons was unaffected by the treatment. The mean cross-sectional axon area and the mean myelin sheath thickness were significantly reduced in animals injected with articaine 4%., Conclusions: These observations indicate concentration-dependent neurotoxic injuries after injection of articaine with a significant difference between 2% and 4% formulations. The mechanical injury of needle penetration with saline injection had no significant effect on nerve conduction or histomorphology.

Articaine is one of the most recent local anaesthetic drugs made available to dentists worldwide. Anecdotal reports advocate its superiority over other common local anaesthetic agents and controversy exists concerning its clinical safety. This article reviews the current literature on articaine use in dentistry specifically addressing the issues of efficacy and safety.

Background: Chloroprocaine and articaine have recently gained interest as short-acting spinal anaesthetics. They have not, however, previously been compared in an ambulatory surgery setting., Methods: In this double-blind, randomised, controlled trial, adult patients (≤65 years, ASA I-II, body mass index<36 kg/m2) underwent day-case knee arthroscopy under spinal anaesthesia with either 40 mg of plain chloroprocaine (20 mg/ml) (group C40; n=39) or 60 mg of plain articaine (40 mg/ml) (group A60; n=39). Study parameters included the onset, degree, and regression of both sensory and motor block. Standardised telephone interviews on the first and seventh post-operative day were aimed at detecting any untoward sequelae, e.g., transient neurologic symptoms (TNSs)., Results: The groups were comparable regarding demographic data, onset and maximal spread of spinal anaesthesia, and duration of surgery. All arthroscopies were performed successfully under spinal anaesthesia, except for one patient (C40, unforeseen delay in the start of surgery). The duration of sensory block≥dermatome L1 was significantly shorter in C40 vs. A60. Correspondingly, complete recovery was significantly faster (P<0.0001, Mann-Whitney U-test) in C40 vs. A60 for both motor [75 (60/90) vs. 135 (105/150) min] and sensory [105 (105/135) vs. 165 (135/180) min] block, respectively [data are median (25th/75th percentiles)]. No TNSs were noted., Conclusions: Both anaesthetics used provided a rapid onset of spinal anaesthesia of about 1 h and were satisfactory for day-case knee arthroscopy. Recovery, however, was significantly faster in group C40. The data add to earlier results that TNSs seem to be uncommon after spinal chloroprocaine and articaine., (© 2010 The Authors. Journal compilation © 2010 The Acta Anaesthesiologica Scandinavica Foundation.)

Background: Autologous fat transplantation is a well-established technique in surgery. Moreover, the use of preadipocytes in soft-tissue engineering is currently being intensely investigated. Current efforts focus on identifying maneuvers that may minimize resorption and provide predictable late results. The aim of this study was to investigate the influence of different local anesthetics frequently used in clinical practice on the viability of preadipocytes and their ability to differentiate into adipocytes., Methods: Human preadipocytes were isolated from subcutaneous adipose tissue of 15 patients and treated with bupivacaine, mepivacaine, ropivacaine, articaine/epinephrine, and lidocaine for 30 minutes. Viability was determined directly after treatment and during the ensuing cultivation. Differentiation of preadipocytes was determined by expression of the adipocyte marker adiponectin., Results: Although the immediate effects of mepivacaine and ropivacaine were only moderate, treatment with articaine/epinephrine and lidocaine strongly impaired preadipocyte viability. Cells normally attached to the culture dishes and proliferated irrespective of the previous treatment. During long-term cultivation, articaine/epinephrine-treated cell viability decreased markedly, whereas other local anesthetics had no impact. Despite normal phenotypic appearance of cells treated with bupivacaine, mepivacaine, ropivacaine, and lidocaine, all local anesthetics markedly impaired adipocyte differentiation as determined by adiponectin expression., Conclusions: The authors' results show that there is a marked influence of local anesthetics not only on the quantity but also on the quality of viable preadipocytes as determined by their ability to differentiate into mature adipocytes. Therefore, these results should be considered in the context of autologous fat transfer and soft-tissue engineering.

The aim of our study was to find the most effective xylidine derivative, which reduced mortality, reduced incidence and duration of severe arrhythmias and had a beneficial influence on hemodynamic parameters in an in vivo setting. We compared the action of lidocaine, articaine, ropivacaine and mepivacaine in a dose 2.5 or 5mg/kg/ml/h infused from 10min before left anterior descending coronary artery occlusion until the end of the experiment. In the rat ischemia- and re-perfusion-induced arrhythmia models, the following parameters were measured or calculated: mortality index, ventricular fibrillation and tachycardia incidence and duration, systolic, diastolic and mean arterial blood pressure, heart rate and pressure rate product. Lidocaine produced the most significant reduction in mortality index (P<0.05) after both doses. At the higher dose, lidocaine and articaine shortened ventricular fibrillation and tachycardia duration (P<0.05-P<0.001), while ropivacaine prolonged them. A hypertensive effect was observed after a lower dose of lidocaine during occlusion and early re-perfusion as compared to others (P<0.05). Beneficial effects were mainly observed with lidocaine, which protected against sudden cardiac death. The novelty was lidocaine's dose independent protection against blood pressure drop in early re-perfusion, which could be linked to the effects observed on the other end-points. Articaine showed beneficial effects but they weren't as pronounced as that of lidocaine. Nevertheless, in the light of our results, articaine could supposedly be used as a substitute for lidocaine in patients with hypertension., (Copyright 2010 Elsevier B.V. All rights reserved.)

Infiltration is preferred to regional block techniques in the maxilla as the former offers a number of advantages. This paper considers the evidence for the efficacy of infiltration anesthesia in the mandible in the adult dentition, both as a primary and as a supplemental method., (Copyright © 2010 Elsevier Inc. All rights reserved.)

In 2000, the US Food and Drug Administration (FDA) approved the use of 4% articaine with epinephrine 1:100,000, and with epinephrine 1:200,000 in 2006. Articaine has been commonly compared with its predecessor, lidocaine hydrochloride. Since its introduction in 1948, lidocaine has maintained a status as the most widely used local dental anesthetic in most countries. Proven efficacy with low allergenicity and toxicity over long-term clinical use and research have confirmed the value and safety of this drug. Thus, it became the gold standard to which all new local anesthetics are compared. Despite the gold standard status of lidocaine, numerous reports and editorials have supported and recognized the use of articaine., (Copyright © 2010 Elsevier Inc. All rights reserved.)

The development of safe and effective local anesthetic agents has possibly been the most important advancement in dental science to occur in the last century. The agents currently available in dentistry are extremely safe and fulfill most of the characteristics of an ideal local anesthetic. These local anesthetic agents can be administered with minimal tissue irritation and with little likelihood of inducing allergic reactions. A variety of agents are available that provide rapid onset and adequate duration of surgical anesthesia. This introductory article provides a brief update of the clinical pharmacology of local anesthetic agents and formulations used in dentistry at present., (Copyright © 2010 Elsevier Inc. All rights reserved.)

Background: Only a few studies have so far compared the use of different local anesthetic agents in septoplasty procedure with regard to reduction in pain, effectiveness, and related complications. The aim of this study was to compare articaine and lidocaine as local anesthetics for septoplasty surgery, in terms of their efficacy and safety., Methods: Seventy patients randomized into two groups were included in this study. For local anesthesia, 35 patients received articaine and 35 received lidocaine. All patients were asked to rate their pain levels on a visual analog scale (VAS) at the 1st, 2nd, 4th, 6th, 8th, 12th, 18th, and 24th postoperative hours. In addition, analgesic consumption of each patient as well as postoperative complications was recorded in both groups., Results: VAS scores for pain were significantly lower in the articaine group than in the lidocaine group at the 2nd, 6th, 8th, 12th, and 24th postoperative hours (p< 0.05). Comparison of the patients' usage of analgesics during the first 24 hours postoperatively showed that in the articaine group, the percentage of patients that had not used analgesics was 58.5%, and in the lidocaine group the corresponding figure was 41.5%., Conclusion: Articaine is a safe local anesthetic agent with rapid onset of action. When compared with lidocaine, it is associated with improved tissue diffusion, rare postoperative complications, and less postoperative pain, thus, representing a safe and effective local anesthetic agent for septoplasty procedure.

Background and Objective: In spite of the widespread clinical use of articaine and ropivacaine there is little information available on the effects of these drugs on myocardial Ca handling. In the present study, therefore, the concentration-dependent effects of articaine and ropivacaine on the components of intracellular Ca handling were studied and compared in canine ventricular myocardium., Methods: Contractility was measured in ventricular trabeculae, [Ca]i transients were recorded from electrically stimulated isolated ventricular myocytes loaded with the calcium-sensitive dye fura-2, L-type Ca current was recorded under whole cell patch clamp conditions, and the release and reuptake of Ca was monitored in sarcoplasmic reticulum vesicles., Results: Articaine and ropivacaine caused a reversible and concentration-dependent decrease in amplitude of the [Ca]i transient (EC50 = 87.4 +/- 12 and 99.3 +/- 17 micromol l, respectively), which was congruent with the reduction obtained for contractility (EC50 = 73.7 +/- 10 and 72.8 +/- 14 micromol l, respectively). No significant change in diastolic [Ca]i was found. L-type Ca current was significantly reduced by articaine and ropivacaine with EC50 values of 327 +/- 56 and 263 +/- 67 micromol l, respectively. Neither Ca release and Ca uptake nor the ATPase activity of the sarcoplasmic reticulum vesicles was altered by articaine or ropivacaine at concentrations less than 200 micromol l. In summary, articaine and ropivacaine caused no significant changes at the therapeutically relevant concentrations of the micromolar range. No significant differences between the effects of articaine and ropivacaine on contractility, [Ca]i transients, L-type Ca current, and sarcoplasmic reticulum Ca release and uptake were observed., Conclusions: Under conditions of normal application both articaine and ropivacaine are free of cardiodepressant effects; however, a negative inotropic action can be anticipated in cases of accidental intravenous injection or overdose. The observed negative inotropic actions of articaine and ropivacaine are similar in magnitude, and can be mainly attributed to a reduction in net trans-sarcolemmal Ca influx.

By their mechanism of action local anaesthesia methods were divided into diffused and vascular. Intraosseous, intraseptal and intraligamental anesthaesias are vascular ones at capillary-venous system level. Circulatory mechanism besides effectiveness increased more than 2-fold and also promotes enhancement of cardiovascular system responses.

Background: Autogenous fat transfer with lipoinjection for soft tissue augmentation is a commonly used surgical technique. Abundant donor tissue availability and relative ease of harvesting have made autologous fat an attractive soft tissue filler. The overall reliability of this technique is often disputed, and different authors describe different results after autologous fat transplantation despite using similar techniques. In this study, we examined the influence of different local anesthetics commonly used in fat harvest and the pH of the anesthetic solution on the viability of harvested preadipocytes., Methods and Materials: Preadipocytes were incubated with 1% lidocaine, 1% articaine plus epinephrine 1:200,000, 0.75% ropivacaine, and 1% prilocaine or our standardized tumescent solution (1 L of 0.9% sodium chloride solution plus 25 mL of 1% articaine plus epinephrine 1:200,000 plus 25 mL of bicarbonate) for 30 minutes. Additionally, we incubated cells with the local anesthetics as described above but diluted 1:2 with phosphate buffered saline (pH 7.4). Viability was measured using trypan blue dying as well as propidium iodine staining and fluorescence-activated cell sorting analysis., Results: There are significant differences in the viability of preadipocytes under the influence of various local anesthetics., Discussion: Our data could partially explain the varying results after autogenous fat transfer.

5 articaine preparations including besides 4% articaine with epinephrine 1:100 000 and 1:200 000, 4% articaine with epinephrine 1:400 000, 2% articaine 1:200 000 and articaine without a vasoconstrictor were investigated on 52 volunteers, dental students. It was established that new combinations of articaine with epinephrine had relatively high activity to anesthetize dental pulp which was comparable with classic agents but slightly inferior to them in all the criteria studied. Articaine without adrenaline had not practically induced pulpal analgesia.

Background: A local anaesthetic with fast onset and short reliable duration of anaesthesia may be preferable for out-patient lower limb surgery. Articaine is believed to act faster and to have a shorter duration of action than bupivacaine, but there are no conclusive data available. The purpose of this study was to compare articaine and bupivacaine for day-case lower limb surgery., Methods: Eighty patients planned for day-case lower limb surgery enrolled in this study. Patients were randomized to receive hyperbaric articaine 80 mg or plain bupivacaine 15 mg intrathecally. Primary outcome variable was recovery time from motor block. Secondary outcomes were: onset of sensory and motor block, maximum spread of sensory block, time to micturition, discharge from the hospital, and complications., Results: The groups were comparable for the medians and the range of the maximum blocks after 30 min. Median time to complete regression of motor block was 101 min (range 80-129) for articaine compared with 307 min (range 225-350) for bupivacaine (P<0.0005). First spontaneous micturition occurred after 257 min (210-293) in the articaine group and after 350 min (304-370) in the bupivacaine group (P<0.0005). In the articaine and bupivacaine groups, patients were discharged after 300 min (273-347) and 380 min (332-431), respectively (P<0.0005). There was no significant difference in the occurrence of complications between the groups., Conclusions: Spinal anaesthesia with 80 mg of hyperbaric articaine has a shorter duration than a spinal anaesthesia with 15 mg of plain bupivacaine in lower limb surgery of approximately 1 h duration.

Seven local anaesthetics and their active anaesthetic components [Ultracaine D-S (articaine hydrochloride), Carbostesin (bupivacaine hydrochloride), Scandicaine (mepivacaine hydrochloride), Xylonest (prilocaine hydrochloride), Xylocaine (lidocaine hydrochloride), Hostacaine (butanilicaine phosphate) and Novocaine (procaine hydrochloride)] were tested for their antimicrobial activity against 311 bacterial strains from 52 different species and 14 Candida albicans strains. The tested pathogens were members of the oral flora, and partly members of the skin and intestinal flora. Additionally, the antimicrobial activity of methyl-4-hydroxybenzoate, sodium disulfite, adrenaline hydrogen tartrate and adrenaline (the preservative and vasoconstrictive components of the anaesthetics) was tested. For determination of MIC and minimal bactericidal concentration (MBC), the agar dilution method using Wilkins-Chalgren agar was applied. The trade preparation Ultracaine D-S showed the most prominent antimicrobial activity with regard to both MIC and MBC. Ultracaine D-S and its active substance, articaine hydrochloride, showed similar MIC values, suggesting that the antimicrobial activity is mainly caused by the anaesthetic component. Novocaine showed the lowest antimicrobial activity and did not inhibit 35 of the species tested. The MIC values of all local anaesthetics were between 0.25 and 16 mg ml(-1). The routinely applied concentration of Ultracaine D-S was roughly four times higher, and of Hostacaine was two times higher, than the MBC values for the tested bacteria, whereas for the other anaesthetics, the MBC values were not reached or exceeded with the concentrations used. The MIC range of the preservatives was 0.5-1.0 mg ml(-1) for methyl-4-hydroxybenzoate and 0.2-0.5 mg ml(-1) for sodium disulfite. The articaine MIC values were two to three serial dilution steps lower, and the butanilicaine MIC values one to two serial dilution steps lower, than the MIC of the preservatives. The mepivacaine mean MIC values were slightly lower for Fusobacterium nucleatum, Prevotella intermedia, Porphyromonas gingivalis and Staphylococcus aureus, but higher for Streptococcus intermedius, compared with the preservative methyl-4-hydroxybenzoate. The same result was found with Streptococcus intermedius and lidocaine. Screening of 20 MIC values of 4 pure anaesthetic substances and the corresponding preservative found 2/20 instances where the MICs of the preservatives against 5 representative species (67 strains) were lower, indicating that the antimicrobial effect was mainly due to the preservative, but 18/20 results where the pure anaesthetic component showed greater antimicrobial effects compared with the preservative. The in vitro results for Carbostesin, Scandicaine and especially for Novocaine indicate that a local disinfection should be done prior to injection of the anaesthetics. Due to the results obtained with nosocomial strains (Escherichia coli, S. aureus and Pseudomonas), disinfection of the mucous membranes should be performed routinely in immunocompromised patients, regardless of the anaesthetic used.

The biocompatibility of innovative tetrasilicate cements proposed for root-end filling restorations was tested. White ProRoot-MTA and AH Plus were used as control. The new cements were mixed with a local anesthetic solution (4% articaine) to form a paste. Human osteoblast-like cells Saos-2 were challenged in short-term cultures (72 hours) with solid materials and with material extracts prepared in culture medium. Cell growth and viability, cellular attachment, and morphologic features were assessed to verify cell/material interactions. No acute toxicity was exerted by the experimental cements in the assay systems. On solid samples Saos-2 adhered and proliferated on all the experimental cements and on MTA. The ultrastructural findings revealed that Saos-2 were able to adhere and to spread. The maintenance of the osteoblastic phenotype on the innovative cements was confirmed by the alkaline phosphatase assay. All experimental cements prepared with articaine supported the growth of bone-like cells, showing suitable properties to be used as canal sealers and root-end filling materials.

Background: In spite of its widespread clinical application, there is little information on the cellular cardiac effects of articaine. In the present study, the concentration-dependent effects of articaine on action potential morphology and the underlying ion currents were studied in isolated canine ventricular cardiomyocytes., Methods: Action potentials were recorded from the enzymatically dispersed myocytes using sharp microelectrodes (16 cells from 3 dogs). Conventional patch clamp and action potential voltage clamp arrangements were used to study the effects of articaine on transmembrane ion currents (37 cells from 14 dogs)., Results: Articaine-induced concentration-dependent changes in action potential configuration including shortening of the action potentials, reduction of their amplitude and maximum velocity of depolarization (V(max)), suppression of early repolarization and depression of plateau. The EC50 value obtained for the V(max) block was 162 (sd 30) microM. Both the reduction of V(max) and action potential shortening were frequency dependent: the former was more prominent at shorter, while the latter at longer pacing cycle lengths. A rate dependent V(max) block, having rapid offset kinetics [tau = 91 (20) ms], was observed in addition to tonic block. Under voltage clamp conditions, a variety of ion currents were blocked by articaine: I(Ca) [EC50 = 471 (75) microM], I(to) [EC50 = 365 (62) microM], I(K1) [EC50 = 372 (46) microM], I(Kr) [EC50 = 278 (79) microM], and I(Ks) [EC50 = 326 (65) microM]. Hill coefficients were close to unity indicating a single binding site for articaine, except for I(K1)., Conclusions: Articaine can modify cardiac action potentials and ion currents at concentrations higher than the therapeutic range which can be achieved only by accidental venous injection. Since its suppressive effects on the inward and outward currents are relatively well balanced, the articaine-induced changes in action potential morphology may be moderate even in the case of overdose.

Background: Autogenous fat transfer with lipoinjection for soft-tissue augmentation is a commonly used technique in plastic surgery. The efficiency of this technique has often been discussed and authors still describe very different results after autologous fat transplantation. The purpose of our investigations was to evaluate the effect of the various local anaesthetics, used in the region of harvesting, on the viability of preadipocytes., Material and Method: Preadipocytes were isolated from human subcutaneous adipose tissue samples and incubated with lidocaine, prilocaine, articaine + epinephrine, ropivacaine or our standardised tumescent solution for 30 minutes. NaCl solution (0.9 %) served as a control. Vitality was measured with FACS analysis., Results: There are significant differences in the viability of the preadipocytes after incubation with the different substances. Viability ranged from > 90 % to less then 20 %., Conclusion: For the first time the influence of local anaesthesia on the viability of preadipocytes has been investigated. The significant differences between the substances could explain the varying results in autologous fat transplantation. Our results should help by choosing the right local anaesthesia for infiltrating the donor site.