ABSTRACT
Purpose: To evaluate the preclinical effects, and preclinical and clinical ocular and systemic pharmacokinetics of a new topical, non-preserved ocular anesthetic, AG-920 (articaine ophthalmic solution). Methods: Five studies: one in vitro melanin binding study; three studies in rabbits receiving an ocular dose of AG-920 evaluating corneal sensitivity, ocular tolerability, and systemic exposure to articaine and its inactive metabolite, articainic acid; and one clinical study in 14 healthy adult volunteers receiving an ocular dose of AG-920, with blood samples over 24 h. A liquid chromatography with tandem mass spectrometry (LC-MS-MS) method was used to detect both parent and metabolite with a lower limit of quantitation (LLOQ) of 0.1 and 0.2 ng/mL, respectively. Results: Melanin binding of articaine was up to 7.4%. A decrease in corneal sensitivity was noted for 20 min post-treatment in all active groups, and returned to baseline by 60 min post-dose. No dose-response relationship was observed. Concentrations of articaine in ocular matrices generally peaked early and then decreased over time. Both parent and metabolite were observed in blood at early time points. There were no ocular safety issues with AG-920. Conclusions: These early stage development studies showed that AG-920 was well tolerated in the standard preclinical models and did not cause any toxicity. AG-920 ophthalmic solution elicited a rapid onset and potentially clinically useful duration of corneal anesthesia. The studies supported the clinical evaluation of the 8% strength. Registered with clinicaltrials.gov as NCT04759339.
Subject(s)
Carticaine , Melanins , Adult , Anesthetics, Local/pharmacology , Animals , Carticaine/chemistry , Carticaine/pharmacokinetics , Chromatography, Liquid , Clinical Studies as Topic , Humans , Ophthalmic Solutions/pharmacology , RabbitsABSTRACT
Local anaesthetics (LAs) are commonly used in surgery, especially in dentistry. They cause a transitory inhibition of nerve signal due to the blockade of the voltage-gated sodium channels. LAs are administrated alone or with vasoconstriction agents, such as adrenaline. Toxicity of LAs is associated to neurological and cardiovascular alterations. Tachycardia, arrhythmia, tremors, tonic-clonic seizure and respiratory depression (at high doses) are the main symptoms of intoxication by LAs. Lidocaine, articaine and mepivacaine are among the most used anaesthetics. This study aimed to fully validated a new method for the simultaneous detection of articaine and mepivacaine in whole blood. Sample treatment consisted in a liquid-liquid extraction with phosphate buffer (pH 8, 0.1 M) and ethyl-acetate. Analysis was performed by liquid chromatography-tandem mass spectrometry in multiple reaction monitoring mode (transitions: articaine, 285â8658 m/z; mepivacaine, 247â9870 m/z; lidocaine - internal standard -, 235â8658 m/z). The method proved to be highly sensitive with limit of quantifications for articaine and mepivacaine of 0.8 and 0.1 ng/mL, respectively. Accuracy and precision were always within the acceptance criteria. The new procedure was also successfully applied to a preliminary pharmacokinetics study.
Subject(s)
Anesthetics, Local/analysis , Carticaine/analysis , Chromatography, Liquid/methods , Mepivacaine/analysis , Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Female , Humans , Liquid-Liquid Extraction , Male , Mepivacaine/pharmacokinetics , Reproducibility of Results , Tandem Mass Spectrometry/methodsABSTRACT
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 (40â mg/mL) was administered to 10 male red deer as a ring block around the base of each antler at 1â 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 50â 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 1â 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.
Subject(s)
Anesthetics, Local/administration & dosage , Anesthetics, Local/pharmacokinetics , Antlers , Carticaine/administration & dosage , Carticaine/pharmacokinetics , Deer , Analgesics , Animals , Antlers/chemistry , Behavior, Animal , Male , Mass Spectrometry/methods , Mass Spectrometry/veterinary , Nerve Block/methods , Nerve Block/veterinaryABSTRACT
BACKGROUND AND OBJECTIVES: Articaine is more and more used in third molar surgery under local anesthesia (LA). The objectives of this analysis were to characterize the pharmacokinetics of articaine for this type of surgery and to simulate dosing regimens. METHODS: Non-linear mixed-effects modeling conducted in Monolix 4.4.0 was used to describe articaine plasma concentration-time data from 20 patients. Monte Carlo simulations were then performed to evaluate the probability of cardiotoxic target attainment (PCTA) of various dosage regimens. RESULTS: Articaine concentration data were best described by a linear one-compartment model, with an additional depot compartment for submucosal route with a zero-order transfer to central compartment. Age and gender were found to influence duration transfer (Tk0) and elimination rate constant (Ke), respectively. Simulated maximum recommended dose regimen (7mg/kg) had a PCTA of 0%. Simulated higher doses of 10mg/kg and 15mg/kg had a PCTA of 0% and about 1-4%, respectively. CONCLUSIONS: The model adequately described the articaine pharmacokinetics. This is the first PK model qualified for articaine administered by submucosal route. The simulations suggest that maximum recommended dose regimen is safe concerning the cardiotoxicity in healthy patients.
Subject(s)
Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Epinephrine/pharmacokinetics , Molar, Third/metabolism , Molar, Third/surgery , Nonlinear Dynamics , Adolescent , Adult , Anesthetics, Local/administration & dosage , Carticaine/administration & dosage , Dose-Response Relationship, Drug , Epinephrine/administration & dosage , Female , Humans , Male , Molar, Third/drug effects , Retrospective Studies , Young AdultABSTRACT
PURPOSE: Palatal local anesthetic injection is a painful procedure. Previous studies have reported successful extraction of maxillary teeth using only buccal infiltration of 4% articaine without palatal anesthesia. The aim of the present study was to determine levels of 4% articaine solution in palatal bone and mucosal tissues after buccal injection and compare those levels with 2% lidocaine solution in New Zealand white rabbits. MATERIALS AND METHODS: Eight rabbits received 2 different injections of 0.6 mL of 4% articaine with 1:100,000 epinephrine and 0.6 mL of 2% lidocaine with 1:100,000 epinephrine buccal to the right and left maxillary first molar, respectively, in a split-mouth study design using quantitative syringes. All injections were administered using the buccal infiltration technique without any palatal injection. Ten minutes later, palatal bone and mucosa specimens were collected for analysis. Levels of the 2 local anesthetic agents were measured in palatal tissues using high-performance liquid chromatography (HPLC). RESULTS: HPLC analysis showed markedly higher 4% articaine solution values (0.319 ± 0.037) in palatal mucosal tissues compared with palatal mucosal concentrations of 2% lidocaine solution (0.0839 ± 0.017). In palatal bone, the mean concentration of 2% lidocaine solution was markedly lower than the mean concentration of 4% articaine solution (0.085 ± 0.012 vs 0.155 ± 0.012, respectively). There was no relevant difference between levels of 2% lidocaine in the palatal bone and mucosal tissues. However, the mean concentration of 4% articaine in the palatal mucosa was markedly higher than its concentration in palatal bone. CONCLUSIONS: The buccal vestibule-palatal diffusion of 4% articaine solution with 1:100,000 epinephrine is greater than 2% lidocaine solution with 1:100,000 epinephrine in a rabbit model.
Subject(s)
Anesthesia, Local/methods , Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Lidocaine/pharmacokinetics , Palate, Hard/metabolism , Administration, Buccal , Anesthetics, Local/administration & dosage , Animals , Carticaine/administration & dosage , Chromatography, High Pressure Liquid , Lidocaine/administration & dosage , Male , RabbitsABSTRACT
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 (40â mg/mL) was administered S/C to six healthy male red deer, at a dose of 1â 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 10â 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.
Subject(s)
Anesthetics, Local/pharmacokinetics , Carticaine/analogs & derivatives , Carticaine/pharmacokinetics , Chromatography, Liquid/veterinary , Deer/metabolism , Mass Spectrometry/veterinary , Anesthetics, Local/administration & dosage , Animals , Carticaine/administration & dosage , Chromatography, Liquid/standards , Deer/blood , Linear Models , Male , Mass Spectrometry/standards , Reproducibility of Results , Subcutaneous AbsorptionABSTRACT
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 1.8mL of a local anesthetic injected on each quadrant of the mouth: Articaine (40mg with Epinephrine 0.5mg % and 40mg with Epinephrine 1mg %) or Mepivacaine (30mg and 20mg 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 (AU)
Subject(s)
Humans , Carticaine/pharmacokinetics , Anesthesia, Dental/methods , Epinephrine/pharmacokinetics , Mepivacaine/pharmacokinetics , Cardiovascular Diseases , Cross-Sectional Studies , Periodontitis/surgery , Risk FactorsABSTRACT
Objectives: To compare the clinical anesthetic efficacy of 0.5% bupivacaine and 4% articaine (both with 1:200.000adrenaline) 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 (AU)
Subject(s)
Humans , Bupivacaine/pharmacokinetics , Carticaine/pharmacokinetics , Infusions, Intraosseous/methods , Anesthesia, Dental/methods , Prospective Studies , Anesthesia, Local/methodsABSTRACT
Objectives: To evaluate the anaesthetic properties and tolerance of articaine versus lidocaine at equal vasoconstrictor concentration. Study Design: A total of 96 male and female patients who underwent surgical treatment of the lower third molar participated. Patients were randomly assigned to articaine hydrochloride with epinephrine 1:100,000 and lidocaine hydrochloride with epinephrine 1:100,000. The variables analysed were latency period, duration of anaesthetic effect, tolerance and adverse reactions. Results: Both the latency period and the duration of anaesthetic effect were greater for articaine, although the differences were not statistically significant. Latency: mean difference of 2.70 ± 2.12 minutes (95%CI of -1.51minutes - 6.92 minutes). Duration: mean difference of -33 minutes 5 seconds ± 31 minutes (95% CI -1 hour 35minutes - 29 minutes).There were 4 adverse events that did not require the patients to be withdrawn from the study. Conclusions: The anaesthetics in this study have very similar properties for use in surgery and have demonstrated a good safety and tolerability profile (AU)
Subject(s)
Humans , Anesthesia, Dental/methods , Carticaine/pharmacokinetics , Lidocaine/pharmacokinetics , Oral Surgical Procedures/methods , Drug Tolerance , Molar, Third/surgeryABSTRACT
Objective: Pain reduction has been the subject of continuous research in the field of oral and maxillofacial surgery since postoperative pain with ranging of intensity and duration may affects the patient submitted in an oral surgical procedure. The aim of present study was to compare the analgesic effectiveness between two different anesthetic solutions (articaine and lidocaine) in third molar surgery. Study Design: A prospective, randomized and clinical study with patients submitted to third molar surgery at two distinct times. The visual analogue scale, the McGill Pain Questionnaire and the analgesic consumption record were used to measure the pain after each surgical time. Results: Duration of surgery, latency, the amount of anesthetic used and analgesic consumption showed clinical differences with highlights of articaine, though statistical significance was not observed (P<0.05). The pain scores indicated similar anesthetic efficacy with both solutions. Conclusion: In the present study no significant differences were observed between lidocaine and articaine in the control of postoperative pain (AU)
Subject(s)
Humans , Carticaine/pharmacokinetics , Lidocaine/pharmacokinetics , Molar, Third/surgery , Oral Surgical Procedures/methods , Pain, Postoperative/drug therapy , Tooth Extraction/methods , Prospective StudiesABSTRACT
PURPOSE: The aim of this study was to evaluate the distribution and absorption of local anesthetic solutions in inferior alveolar nerve block using magnetic resonance imaging. MATERIALS AND METHODS: Forty healthy volunteers were divided into 4 groups and injected with 1.5 mL for inferior alveolar nerve block and 0.3 mL for lingual nerve block. The solutions used for the different groups were 2% lidocaine, 2% lidocaine with 0.125 mg/mL epinephrine, 4% articaine with 0.006 mg/mL epinephrine, and 4% articaine with 0.012 mg/mL epinephrine. All subjects had axial T2-weighted and fat-suppressed images at 0, 60, and 120 minutes after injection. The localization, area, and intensity (signal characteristics) of the solutions were analyzed and onset and duration times of the anesthesia were recorded. RESULTS: There were no significant differences between groups with regard to the intensity and area of the solutions at 0, 60, and 120 minutes after injection, but differences were found within each group. CONCLUSIONS: No between-group differences were found on magnetic resonance imaging in the distribution and absorption of lidocaine with or without epinephrine and articaine with 0.006 and 0.012 mg/mL epinephrine. All solutions were noticeably absorbed at 120 minutes after injection.
Subject(s)
Anesthetics, Local/pharmacokinetics , Magnetic Resonance Imaging/methods , Mandibular Nerve , Nerve Block , Absorption , Anesthesia, Local , Anesthetics, Local/administration & dosage , Carticaine/administration & dosage , Carticaine/pharmacokinetics , Epinephrine/administration & dosage , Epinephrine/pharmacokinetics , Female , Humans , Image Enhancement/methods , Image Processing, Computer-Assisted/methods , Injections/methods , Lidocaine/administration & dosage , Lidocaine/pharmacokinetics , Lingual Nerve/drug effects , Lip/drug effects , Male , Mandibular Nerve/drug effects , Time Factors , Tissue Distribution , Tongue/drug effects , Vasoconstrictor Agents/administration & dosage , Vasoconstrictor Agents/pharmacokinetics , Young AdultABSTRACT
Objective: The third molar extraction is one of the most common surgical procedures in oral surgery and is usuallyaccompanied by postoperative discomfort. It has been suggested that the longer duration of action of bupivacaineassociated with the residual analgesia and the gradual onset of pain, could decrease the need for analgesics duringthe postoperative period. This study aims to compare the efficacy and safety of bupivacaine and articaine as localanesthetics for the extraction of mandibular third molars and to check whether bupivacaine produced residualanalgesia.Study design: We compared bupivacaine 0.5% and articaine 4% with an epinephrine concentration of 1:200 000in a crossover design model of extraction of bilaterally symmetrical mandibular third molars.Results: Regarding efficacy, patients experienced less postoperative pain at 6 and 12 hours and shorter durationof soft tissue anesthesia with articaine. With respect to safety, no differences were found between the anestheticscompared, showing a similar local and systemic toxicity. With regard to the preference of patients, it was higherfor articaine, the main reasons being the greater postoperative pain and swelling with bupivacaine.Conclusion: It can be concluded that articaine seems to be a more appropriate anesthetic for the extraction of mandibularthird molars due to the shorter duration of the anesthetic effect in the soft tissues, lower pain reported bypatients during the immediate postoperative period and the personal preference of patients for this drug (AU)
No disponible
Subject(s)
Humans , Molar, Third/surgery , Tooth Extraction/methods , Anesthetics, Local/administration & dosage , Anesthesia, Dental/methods , Bupivacaine/pharmacokinetics , Carticaine/pharmacokineticsABSTRACT
In 56 laboratory blind investigations in 26 volunteers effects of intraligamentary anesthesia with 4% articaine solutions with different adrenaline concentrations and without it on arterial pressure and heart rate changes by means of automatic monitor were evaluated. Period of intraligamentary injection of anesthetic solutions (1-2 min) was chacterized by the most manifestation of these reactions which might be due to vascular distribution of the anesthetic solution within tissues as well as adrenaline content in it.
Subject(s)
Anesthesia, Dental/adverse effects , Anesthetics, Local/adverse effects , Blood Pressure/drug effects , Carticaine/adverse effects , Heart Rate/drug effects , Anesthetics, Local/administration & dosage , Anesthetics, Local/pharmacokinetics , Carticaine/administration & dosage , Carticaine/pharmacokinetics , Double-Blind Method , Epinephrine/administration & dosage , Epinephrine/adverse effects , Female , Humans , Male , Young AdultABSTRACT
Local anesthetics (LAs) are drugs that cause reversible loss of nociception during surgical procedures. Articaine is a commonly used LA in dentistry that has proven to be exceptionally effective in penetrating bone tissue and induce anesthesia on posterior teeth in maxilla and mandibula. In the present study, our aim was to gain a deeper understanding of the penetration of articaine through biological membranes by studying the interactions of articaine with a phospholipid membrane. Our approach involves Langmuir monolayer experiments combined with molecular dynamics simulations. Membrane permeability of LAs can be modulated by pH due to a titratable amine group with a pKa value close to physiological pH. A change in protonation state is thus known to act as a lipophilicity switch in LAs. Our study shows that articaine has an additional unique lipophilicity switch in its ability to form an intramolecular hydrogen bond. We suggest this intramolecular hydrogen bond as a novel and additional solvent-dependent mechanism for modulation of lipophilicity of articaine which may enhance its diffusion through membranes and connective tissue.
Subject(s)
Anesthetics, Local/chemistry , Anesthetics, Local/pharmacokinetics , Bone and Bones/metabolism , Carticaine/chemistry , Carticaine/pharmacokinetics , Molecular Dynamics Simulation , Diffusion , Hydrogen Bonding , Phosphatidylcholines/analysisABSTRACT
Aims: The aim of this study was to evaluate the vestibular-palatal diffusion of 4% articaine with epinephrine 1:100,000 and 1:200,000, in impacted maxillary third molar extractions, without palatal injection. Materials and Method: Two hundred teeth were selected from patients age 15 to 46. Patients were divided into 4 groups: 1A, were anesthetized with 4% articaine 1:100,000 and the surgery was initiated 5 minutes following anesthesia. 1B, used 4% articaine 1:100,000 but the surgery was started 10 minutes after anesthesia. 2A, used 4% articaine 1:200,000 the surgery was started 5 minutes after. 2B, used 4% articaine 1:200,000 but 10 minutes was allowed for anesthetic diffusion before the initiation of in groups (50 extractions each) only buccal vestibule anesthesia was initially administered (i.e. no palatal injections were used). Results: The rate of sufficient vestibule-palatal diffusion, as determined by the lack of necessity of supplemental palatal anesthesia, was: 1A(84%), 1B(98%), 2A(78%), 2B(82%). Chi-square (X2) and residual analyses showed that a higher vestibule-palatal diffusion was obtained using 4% articaine 1:100,000 with a period of 10 minutes (p<0.05). Conclusions: Most of the extractions could be performed only with vestibule anesthesia. However, vasoconstrictor concentration and the time interval between administration of the anesthetic and initiation of surgery did influence buccal vestibule-palatal diffusion of 4% articaine in the extraction models used (AU)
Subject(s)
Humans , Adolescent , Young Adult , Adult , Middle Aged , Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Molar, Third/surgery , Mouth/metabolism , Palate/metabolism , Tooth Extraction , Tooth, Impacted/surgery , Diffusion , Maxilla , Tissue DistributionABSTRACT
AIMS: The aim of this study was to evaluate the vestibular-palatal diffusion of 4% Articaine with epinephrine 1:100,000 and 1:200,000, in impacted maxillary third molar extractions, without palatal injection. MATERIALS AND METHOD: Two hundred teeth were selected from patients age 15 to 46. Patients were divided into 4 groups: 1A, were anesthetized with 4% articaine 1:100,000 and the surgery was initiated 5 minutes following anesthesia. 1B, used 4% articaine 1:100,000 but the surgery was started 10 minutes after anesthesia. 2A, used 4% articaine 1:200,000 the surgery was started 5 minutes after. 2B, used 4% articaine 1:200,000 but 10 minutes was allowed for anesthetic diffusion before the initiation of in groups (50 extractions each) only buccal vestibule anesthesia was initially administered (i.e. no palatal injections were used). RESULTS: The rate of sufficient vestibule-palatal diffusion, as determined by the lack of necessity of supplemental palatal anesthesia, was: 1A(84%), 1B(98%), 2A(78%), 2B(82%). Chi-square (Chi2) and residual analyses showed that a higher vestibule-palatal diffusion was obtained using 4% articaine 1:100,000 with a period of 10 minutes (p<0.05). CONCLUSIONS: Most of the extractions could be performed only with vestibule anesthesia. However, vasoconstrictor concentration and the time interval between administration of the anesthetic and initiation of surgery did influence buccal vestibule-palatal diffusion of 4% articaine in the extraction models used.
Subject(s)
Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Molar, Third/surgery , Mouth/metabolism , Palate/metabolism , Tooth Extraction , Tooth, Impacted/surgery , Adolescent , Adult , Diffusion , Humans , Maxilla , Middle Aged , Tissue Distribution , Young AdultABSTRACT
A specific liquid chromatography-mass spectrometric (LC-MS) method using an ion trap spectrometer was developed for the quantitation of articaine in human plasma. Articaine and the internal standard (trazodone) were extracted in a single step with diethyl-ether from 0.5 mL of alkalinized plasma. The mobile phase consisted of acetonitrile with 0.1% formic acid (40:60, v/v). It was delivered at a flow rate of 0.3 mL/min. The effluent was monitored by MS in positive-ion mode. Ionisation was performed using an electrospray ion source operating at 200 degrees C. Articaine was identified and quantified in SIM mode at m/z 185. Calibration curves were linear over the concentration range of 78.1-5000 ng/mL with determination coefficients>0.996. This method was fast (total run-time<3 min), accurate (bias<16%), and reproducible (intra-assay and inter-assay precision<14%) with a quantitation limit of 78.1 ng/mL. The good specificity and sensitivity achieved by this method allowed the determination of articaine plasma levels in patients following a submucosal infiltration injection of articaine in the patients undergoing a third molar surgery.
Subject(s)
Anesthetics, Local/blood , Carticaine/blood , Anesthetics, Local/pharmacokinetics , Anesthetics, Local/therapeutic use , Antidepressive Agents, Second-Generation/analysis , Calibration , Carticaine/pharmacokinetics , Carticaine/therapeutic use , Chromatography, High Pressure Liquid , Humans , Indicators and Reagents , Molar, Third , Pain, Postoperative/drug therapy , Quality Control , Reference Standards , Reproducibility of Results , Spectrometry, Mass, Electrospray Ionization , Tooth Extraction , Trazodone/analysisABSTRACT
No disponible
Objective: The objective of the present study was to investigate the pain on injection of articaine with adrenaline, prilocaine with phenylpressin , and lidocaine with adrenaline. Study Design: The study sample was comprised of 497consecutively seen patients received 497 maxillary buccal infiltration injections or inferior alveolar block injections of 4% articaine with 1:200.000 adrenaline, 3% prilocaine with 1.08mcg phenylpressin, or 2% lidocaine with 1:100.000 adrenaline. Immediately after the injection, patients were asked to rate their injection pain on a six-point scale. Results: There were no significant differences among the anesthetic solutions for injection pain. Patients usually reported mild or no injection pain for all of anesthetic administrations.Conclusion: Under the conditions of this study that lidocaine with adrenaline, articaine with adrenaline and prilocaine with phenylpressin seemed to be similar for pain on injection and they could be quite painless
Subject(s)
Humans , Anesthesia, Dental/methods , Toothache , Carticaine/pharmacokinetics , Lidocaine/pharmacokinetics , Prilocaine/pharmacokinetics , Epinephrine/pharmacokinetics , Injections/methods , Mandibular Nerve , Nerve Block/methodsSubject(s)
Anesthesia, Dental/methods , Anesthesia, Local/methods , Anesthetics, Local/pharmacokinetics , Carticaine/pharmacokinetics , Lidocaine/pharmacokinetics , Anesthetics, Local/administration & dosage , Carticaine/administration & dosage , Dose-Response Relationship, Drug , Humans , Lidocaine/administration & dosage , Mandible , Therapeutic Equivalency , Tooth/drug effectsABSTRACT
PURPOSE: Local anesthesia administration is integral to pain control in dental hygiene. As of 2006, 40 licensing jurisdictions in the United States include local anesthesia administration in the scope of dental hygiene practice. While the risks associated with use of intraoral local anesthesia are not great, careful attention to recommended practices helps foster patient safety. As new products are introduced, it is important to study their advantages and limitations to see where they fit into dental hygiene practice. An amide local anesthetic agent, articaine, that has been available in Europe for over 20 years, was approved for US distribution in 2000. METHODS: The purpose of this article is to review the current peer reviewed literature on the characteristics of articaine so it can be incorporated into dental hygiene practice when indicated. RESULTS: Rather than simply using one agent for all procedures, patient care is enhanced when local anesthetics are selected based on the unique needs of the procedure, the patient and with safety and effectiveness in mind.