Pharmacokinetics, efficacy and convulsive dose of articaine hydrochloride in goat kids.

OBJECTIVE: To investigate the pharmacokinetics, efficacy and convulsive dose of articaine hydrochloride in goat kids. STUDY DESIGN: Experimental prospective study. ANIMALS: A total of 18 (n = 6 animals per experiment) male Saanen goat kids (2-4 weeks old). METHODS: The study consisted of three experiments. The first determined the pharmacokinetics of articaine following intravenous administration of articaine hydrochloride (8 mg kg-1). The second experiment investigated the anaesthetic efficacy and pharmacokinetics following cornual nerve block using 1.5% articaine hydrochloride. Anaesthesia of horn buds was evaluated using the response to pinprick test. Non-compartmental analysis was used. The final experiment determined the convulsive dose of articaine and its corresponding plasma concentration following intravenous infusion of articaine hydrochloride (4 mg kg-1 minute-1). Data are shown as mean ± standard deviation. RESULTS: The mean terminal half-life (t1/2λz), mean volume of distribution at steady state (Vdss) and mean plasma clearance (CL) of articaine following intravenous administration were 0.66 hour, 3.81 L kg-1 and 5.33 L hour-1 kg-1, respectively. After cornual nerve block, the mean maximum plasma concentration of articaine was 587 ng mL-1 at 0.22 hour and its mean t1/2λz was 1.26 hours. Anaesthesia of horn buds was observed within 4 minutes following cornual nerve block. The mean dose required to produce convulsions was 16.24 mg kg-1 and mean convulsive plasma concentrations of articaine and articainic acid were 9905 and 1517 ng mL-1, respectively. CONCLUSIONS: Intravenous administration of 8 mg kg-1 of articaine hydrochloride did not cause any adverse effects. Pharmacokinetic data suggest that articaine was rapidly eliminated and cleared. Cornual nerve block using 1.5% articaine hydrochloride alleviated the response to the acute nociceptive stimulus during disbudding. CLINICAL RELEVANCE: Articaine hydrochloride appears to be a safe and effective local anaesthetic for disbudding in goat kids.

Analgesic efficacy of articaine hydrochloride for velvet antler removal in red deer (Cervus elaphus) and analysis of drug residues in the harvested velvet antlers.

AIMS: To investigate the analgesic efficacy of articaine hydrochloride for antler removal in red deer (Cervus elaphus) following S/C administration as a ring block, and to quantify the residue concentrations of articaine compared to lignocaine in the harvested antlers. METHODS: Articaine hydrochloride (40 mg/mL) was administered to 10 male red deer as a ring block around the base of each antler at 1 mL/cm of pedicle circumference. Analgesia was evaluated by determining the response to a saw cut test every 1-minute, until no response was observed. Behaviour during and following removal of antlers was also recorded. Twenty commercially harvested velvet antlers were also collected following S/C administration of 2% lignocaine hydrochloride. A liquid chromatography-mass spectrometry (LC-MS) method for quantification of residues of articaine and lignocaine in velvet antlers was developed and validated. RESULTS: In red deer administered 4% articaine hydrochloride as a ring block, the median interval to analgesia was 4 (min 3, max 5) minutes and no deer showed withdrawal responses during antler removal. There were no signs of toxicity or adverse effects up to 2 hours after administration. The sample preparation method developed for the LC-MS was simple and had acceptable extraction recoveries of articaine and lignocaine from the velvet antlers. The lower limits of quantification of lignocaine and articaine were 5 and 50 ng/g, respectively. Mean concentrations of articaine in antlers following ring block with 4% articaine hydrochloride were 1.50 (SD 1.09) mg/kg, and of lignocaine following ring block with 2% lignocaine hydrochloride were 0.66 (SD 0.71) mg/kg. CONCLUSIONS AND CLINICAL RELEVANCE: A ring block with 4% articaine hydrochloride at a dose of 1 mL/cm of pedicle circumference provided effective analgesia for velvet antler removal in red deer. The LC-MS method developed and validated to quantify articaine and lignocaine was simple and sensitive. Based on these results, articaine hydrochloride appears to be an effective alternative to lignocaine hydrochloride for velvet antler removal. However, further studies to evaluate the safety and residue concentrations of articaine and articainic acid are required before it can be recommended for use in deer.Abbreviations: DMA: 2,6-dimethylaniline; LC-MS: Liquid chromatography-mass spectrometry; MEGX: Monoethylglycinexylidide; MRL: Maximum residue level.

Pharmacokinetics of articaine hydrochloride and its metabolite articainic acid after subcutaneous administration in red deer (Cervus elaphus).

AIM: To develop and validate a simple and sensitive method using liquid chromatography-mass spectrometry (LC-MS) for quantification of articaine, and its major metabolite articainic acid, in plasma of red deer (Cervus elaphus), and to investigate the pharmacokinetics of articaine hydrochloride and articainic acid in red deer following S/C administration of articaine hydrochloride as a complete ring block around the antler pedicle. METHODS: The LC-MS method was validated by determining linearity, sensitivity, recovery, carry-over and repeatability. Articaine hydrochloride (40 mg/mL) was administered S/C to six healthy male red deer, at a dose of 1 mL/cm of pedicle circumference, as a complete ring block around the base of each antler. Blood samples were collected at various times over the following 12 hours. Concentrations in plasma of articaine and articainic acid were quantified using the validated LC-MS method. Pharmacokinetic parameters of articaine and articainic acid were estimated using non-compartmental analysis. RESULTS: Calibration curves were linear for both articaine and articainic acid. The limits of quantifications for articaine and articainic acid were 5 and 10 ng/mL, respectively. Extraction recoveries were >72% for articaine and >68% for articainic acid. After S/C administration as a ring block around the base of each antler, mean maximum concentrations in plasma (Cmax) of articaine were 1,013.9 (SD 510.1) ng/mL, detected at 0.17 (SD 0.00) hours, and the Cmax for articainic acid was 762.6 (SD 95.4) ng/mL at 0.50 (SD 0.00) hours. The elimination half-lives of articaine hydrochloride and articainic acid were 1.12 (SD 0.17) and 0.90 (SD 0.07) hours, respectively. CONCLUSIONS AND CLINICAL RELEVANCE: The LC-MS method used for the quantification of articaine and its metabolite articainic acid in the plasma of red deer was simple, accurate and sensitive. Articaine hydrochloride was rapidly absorbed, hydrolysed to its inactive metabolite articainic acid, and eliminated following S/C administration as a ring block in red deer. These favourable pharmacokinetic properties suggest that articaine hydrochloride should be tested for efficacy as a local anaesthetic in red deer for removal of velvet antlers. Further studies to evaluate the safety and residues of articaine hydrochloride and articainic acid are required before articaine can be recommended for use as a local anaesthetic for this purpose.

Comparison of the Efficacy Between Articaine and Lignocaine in Simultaneous Bilateral Orthodontic Maxillary Premolar Extractions: A Split-Mouth Comparative Study.

Introduction Local anesthesia plays a crucial role in ensuring patient comfort during orthodontic extractions. Among the various local anesthetic agents commonly used in the field of oral surgery are articaine and lidocaine, which differ in their duration of action and pain effectiveness (pain control) during surgical procedures. This article aimed to analyze the characteristics of 2% lignocaine with 1:80000 adrenaline and 4% articaine with 1:100000 adrenaline regarding duration of action and pain control in patients undergoing bilateral orthodontic maxillary premolar extractions. Materials and methods A split-mouth comparative study was conducted at Saveetha Dental College and Hospitals, Chennai, for which 50 patients of age less than 30 years and who required bilateral orthodontic premolar extractions were selected. Approximately 4% articaine hydrochloride solution was administered on one side, and 2% lignocaine hydrochloride was administered on the contralateral side. Palatal infiltration was not given in the articaine group. The degree of extraction difficulty was similar in both groups, with no discernible variation. In each patient, the duration of anesthesia and pain control were assessed. The IBM Statistical Package for Social Sciences (SPSS version 24.0, IBM SPSS Statistics for Windows, Armonk, NY) was used to perform the student's paired t-test for detecting the difference in outcome parameters between the two groups. Results Upon comparing both groups, it was concluded that the articaine group had a longer mean anesthetic duration of action of 217 minutes, whereas for the lignocaine group, it was 169 minutes, and greater pain reduction was present with the articaine group. The articaine group exhibited less pain (superior pain control) with a mean visual analogue scale (VAS) score of 1.07 compared to that of the lignocaine group with a mean VAS score of 1.53 during orthodontic premolar extractions. Both the results were statistically significant (P=0.001). Conclusion This split-mouth comparative study concludes that articaine is a more effective local anesthetic in terms of duration of action and pain reduction than that of lignocaine, and it can be used as a local anesthetic of choice for orthodontic maxillary premolar extractions.

Pressure Algometry Validation and Determination of Efficacy of Articaine Hydrochloride Ring Block in Antler Removal in Red Deer (Cervus elaphus).

New Zealand deer farming centres on the production of meat and velvet antler. Velvet antler removal is a painful procedure and currently, New Zealand Animal Welfare regulations dictate surgical removal of velvet antlers under lignocaine anaesthesia. To improve our knowledge on the efficacy and duration of other local anaesthetics to mitigate pain after antler removal, it is important to accurately assess and quantify pain arising from antler removal. Therefore, the current study was designed to validate mechanical nociceptive threshold (MNT) testing using a Wagner hand-held algometer, and to apply this methodology to assess the efficacy and duration of action of articaine for antler removal in deer. Baseline force (N) required to elicit the nociceptive response was recorded in 40 yearling male red deer on three alternate days. Ten of the 40 animals were selected for antler removal after administration of 4% articaine hydrochloride as a ring block. The duration of analgesic efficacy of articaine was assessed by algometry across 5 time points. There was a significant difference in MNTs among the three days (day 3 versus day 1 (p < 0.0001), day 2 versus day 1 (p < 0.0001), and day 1 versus day 2 (p < 0.01)). Positive correlations were observed between weight, antler length and thresholds. The MNT values remained above 20N for 6 h after removal of velvet antlers under the articaine ring block. This study provides valuable information about the use of MNT in red deer. These findings lay a foundation for future studies in the topics of peri-operative and postoperative pain management in deer antler removal, and a possible alternative use for articaine.

4% Articaine and 2% Lignocaine for Surgical Removal of Third Molar by Mandibular Nerve Block: A Randomized Clinical Trial for Efficacy and Safety.

OBJECTIVE: Articaine entered clinical use in 1976; however, evidence basis for articaine's reputation is not entirely clear. The aim of the study is to compare and analyze 4% articaine with 1:100,000 epinephrine and 2% lignocaine with 1:100,000 epinephrine in patients operated for mandibular third molar impaction with respect to efficacy and safety, time of onset and duration of anesthesia and duration of postoperative analgesia. METHODS: The study was done on fifty patients requiring surgical extraction of mandibular third molar; randomly divided into two groups of 25 each, receiving 4% articaine hydrochloride with 1:100,000 epinephrine and 2% lignocaine hydrochloride with 1:100,000 epinephrine. Difficulty index for extraction, volume, onset and duration of anesthesia and duration of postoperative analgesia were recorded. Pain was assessed using Heft-Parker VAS. The data were analyzed using appropriate statistical analysis. RESULTS: The mean onset time for articaine and lignocaine is 3.16 ± 0.55 and 3.2 ± 0.48 min, respectively. Articaine group experienced statistically significant longer period of analgesia and duration of action 289.04 ± 40 and 361.88 ± 40 min, respectively, as compared to lignocaine which is 144.2 ± 12 and 197.44 ± 25 min, respectively. No statistical difference between the two groups with regard to pain experience. CONCLUSION: 4% Articaine is more potent and has longer duration of action with better postoperative analgesia and could be considered as an alternative to lignocaine in clinical practice. With management of postoperative pain being the critical component of patient care, clinical trials are required to develop long acting local anesthetic with increased postoperative analgesia effect.

Anesthetic efficacy of 4% articaine versus 2% lignocaine during the surgical removal of the third molar: A comparative prospective study.

AIM: The study aimed at evaluating the clinical efficacy of articaine over lidocaine in the surgical removal of impacted mandibular third molars. OBJECTIVE: The objectives were to compare the onset of anesthesia, pain during injection, during the procedure and after the procedure, compare the duration of anesthesia, and need for re-anesthesia. MATERIALS AND METHODS: A prospective study was conducted on 70 subjects planned for surgical removal of mandibular third molars. Subjects were randomly administered one of two local anesthetics. The anesthetic agent used was unknown for the patient and the observer who performed the measurements. RESULTS: The differences in latency with 4% articaine (56.57 ± 9.8 s) and with 2% lignocaine (88.26 ± 12.87 s), pain during procedure for articaine 1.31 ± 0.87 and for lignocaine 2.60 ± 1.06, pain after procedure was 0.89 ± 0.58 for articaine and 1.31 ± 1.05 for lignocaine, and mean duration of anesthetic effect for articaine was 231 ± 57.15 min and 174.80 ± 37.02 min for lignocaine, which was statistically significant. For re-anesthesia, 6 out of 35 patients needed re-anesthesia at the frequency of 8.57% for articaine and 13 out of 35 patients needed re-anesthesia at a frequency of 18.57% for lignocaine. CONCLUSION: The results proved that articaine had a significant faster onset of action and longer duration of action when compared to lignocaine. Hence, the pain experienced by the patients during and after the surgical procedure was significantly less. The study was concluded that articaine is a safe alternative to lignocaine, which is potent and effective in minor surgical procedures such as removal of mandibular third molars.

Anesthetic effects of articaine hydrochloride and epinephrine tartrate injection in oral treatment of elder patient / 中国基层医药

Objective To observe the anesthetic effects of articaine hydrochloride and epinephrine tartrate injection in oral treatment of elder patients.Methods 66 teeth of 56 elder patients were treated.Pain intensity was scaled by VAS.Pulse and blood pressure were observed before and after drugs administration for 0,5 minutes.ResuIts Pain during injection of articaine hydrochloride and epinephrine tartrate injection and surgery subsequently was rare.The total respouse rate was 95%～100%.No significent toxic effects were found.Pulse and blood pressure remained after injection.Conclusion Articaine hydrochloride and epinephrine tartrate injection was one of local anesthetics with good infiltration,safety and anesehetic effect.It would be more widely used in elder patients oral treatment field in the future.