Pharmacy Division Ramathibodi Hospital


News 12/07/2544

What's the latest in articaine hydrochloride? Articaine is a member of the amide class of local anesthetics.

Articaine Hydrochloride

Articaine Hydrochloride: A Study of the Safety of a New Amide Local Anesthetic

Malamed SF, Gagnon S, Leblanc D
J Am Dent Assoc. 2001;132:177-85

Background: Articaine is an amide local anesthetic introduced clinically in Germany in 1976 and subsequently throughout Europe, Canada and, in 2000, the United States.
Methods: The authors report on three identical single-dose, randomized, double-blind, parallel-group, active-controlled multicenter studies that were conducted to compare the safety and efficacy of articaine (4 percent with epinephrine 1:100,000) with that of lidocaine (2 percent with epinephrine 1:100,000).
Results: A total of 1,325 subjects participated in these studies, 882 of whom received articaine 4 percent with epinephrine 1:100,000 and 443 of whom received lidocaine 2 percent with epinephrine 1:100,000. The overall incidence of adverse events in the combined studies was 22 percent for the articaine group and 20 percent for the lidocaine group. The most frequently reported adverse events in the articaine group, excluding postprocedural dental pain, were headache (4 percent), facial edema, infection, gingivitis and paresthesia (1 percent each). The incidence of these events was similar to that reported for subjects who received lidocaine. The adverse events most frequently reported as related to articaine use were paresthesia (0.9 percent), hypesthesia (0.7 percent), headache (0.55 percent), infection (0.45 percent), and rash and pain (0.3 percent each).
Conclusions: Articaine is a well-tolerated, safe and effective local anesthetic for use in clinical dentistry.

Efficacy of Articaine: A New Amide Local Anesthetic

Malamed SF, Gagnon S, Leblanc D
J Am Dent Assoc. 2000;131:635-42

Background: The authors compared the safety and efficacy of 4 percent articaine with epinephrine 1:100,000 with 2 percent lidocaine with epinephrine 1:100,000.
Methods: In three identical randomized, double-blind, multicenter trials, subjects 4 to 80 years of age received either 4 percent articaine with epinephrine 1:100,000 or 2 percent lidocaine with epinephrine 1:100,000 for simple or complex dental procedures. In each trial, the authors randomized the subjects in a 2:1 ratio to receive articaine or lidocaine. Efficacy was determined by both subject and investigator using a visual analog scale, or VAS. The authors used the Kruskal-Wallis test to analyze the data.
Results: A total of 882 subjects received articaine, and 443 received lidocaine. The authors found no statistical differences between the groups (P = .05). They also compared drug volumes for both articaine and lidocaine groups (2.5 milliliters +/- 0.07 standard error of mean, or SEM, vs. 2.6 mL +/- 0.09 SEM for simple procedures and 4.2 mL +/- 0.15 SEM vs. 4.5 mL +/- 0.21 SEM for complex procedures). The procedures' durations were comparable for both the articaine and lidocaine groups. The authors found no statistical difference between the two treatment groups (P = .05) with respect to subject or investigator pain ratings using the VAS; the mean pain scores determined by both patients and investigators for all groups tested were less than 1.0.
Conclusions: The authors found that 4 percent articaine with epinephrine 1:100,000 was well-tolerated in 882 subjects. It also provided clinically effective pain relief during most dental procedures and had a time to onset and duration of anesthesia appropriate for clinical use and comparable to those observed for other commercially available local anesthetics.
Clinical Implications: Pain control is a major component of patient comfort and safety. Local anesthetics form the backbone of pain control techniques in dentistry. Four percent articaine with epinephrine is an amide local anesthetic that will meet the clinical requirements for pain control of most dental procedures in most patients.

Similar Motor Block Effects With Different Disposition Kinetics Between Lidocaine and (+ or -) Articaine in Patients Undergoing Axillary Brachial Plexus Block During Day Case Surgery

Simon MA, Vree TB, Gielen MJ, et al
Int J Clin Pharmacol Ther. 1999;37:598-607

Aim: The aim of this investigation was to compare the clinical effects and pharmacokinetics of lidocaine and articaine in two groups of 15 patients undergoing axillary brachial plexus anesthesia.
Method: The study had a randomized design. Thirty patients were allocated to one of the two groups. Each patient received either lidocaine (600 mg = 2.561 mMol + 5 microg/ml adrenaline) or articaine (600 mg = 2.113 mMol + 5 microg/ml adrenaline), injected via the axilla of the brachial plexus over a period of 30 seconds. Onset of surgical analgesia was defined as the period from the end of the injection of the local anesthetic to the loss of pinprick sensation in the distribution of all three nerves.
Results: The mean onset time of sensory block of the median nerve of both lidocaine and articaine were approximately 10 min. Lidocaine is biexponentially eliminated with a t1/2alpha of 9.95 +/- 14.3 min and a t1/2beta of 2.86 +/- 1.55 h. Lidocaine is metabolized into MEGX (mono-ethyl-glycyl-xilidide) (t(max) 2.31 +/- 0.84 h; C(max) 0.32 +/- 0.13 mg/l; t1/2beta 2.36 +/- 2.35 h). Lidocaine total body clearance was 67.9 +/- 28.9 l/h. Articaine is rapidly and monoexponentially eliminated with a t1/2beta of 0.95 +/- 0.39 h. The total body clearance of articaine is higher than that of lidocaine, 1,133 +/- 582 l/h vs 67.9 +/- 28.9 l/h, respectively (p < 0.0001). The volume of distribution (V(d)), of articaine is a factor 16 higher times than that of lidocaine (p < 0.0001).
Conclusion: For the axillary administration, lidocaine and articaine show similar pharmacodynamics with a different pharmacokinetic behavior and can therefore be used to the clinical preference for this regional anesthetic technique.

The Effect of Age on Pharmacokinetics of the Local Anesthetic Drug Articaine

Oertel R, Ebert U, Rahn R, et al
Reg Anesth Pain Med. 1999;24:524-8

Background and Objectives: With increasing age, there are physiologic changes that could affect pharmacokinetics of drugs. More elderly patients are undergoing routine dental procedures for which local anesthesia could be required. The goal of the present study was to evaluate the effect of age on pharmacokinetics of the local anesthetic agent articaine.
Methods: The submucosal infiltration anesthesia from two different dosages of 4% articaine without epinephrine was compared in healthy elderly and young volunteers. High performance liquid chromatography has been used to determine concentrations of articaine in serum. Basic pharmacokinetic parameters were calculated according to standard procedures using a two-exponent equation.
Results: The clearance and volume of distribution (Vdss) of articaine after infiltration anesthesia were significantly lower in elderly volunteers compared with young volunteers. The area under the serum concentration-time curve and maximum drug concentration (Cmax) values did not differ significantly with age; however, both parameters tended to be higher in elderly volunteers. No changes in terminal half-life and time to reach maximum serum concentration (t(max)) were observed. The Cmax and tmax values of the metabolite articainic acid were similar in young and elderly volunteers.
Conclusions: The results show that the metabolism of articaine is age-independent in healthy male volunteers. The smaller Vdss in the elderly results in a trend to higher serum levels after a given dose of articaine. No change of dosage of articaine in elderly patients should be necessary.

Comparison of 0.5% Articaine and 0.5% Prilocaine in Intravenous Regional Anesthesia of the Arm: A Cross-Over Study in Volunteers

Pitkanen MT, Xu M, Haasio J, et al
Reg Anesth Pain Med. 1999;24:131-5

Background and Objectives: Earlier studies of the use of articaine in intravenous regional anesthesia (IVRA) are conflicting. In fact, despite similar physicochemical properties and regional anesthetic action, significant differences between articaine and prilocaine in IVRA have been reported. Articaine, being a potent local anesthetic with low degree of toxicity and being rapidly metabolized by esterases, could be a useful local anesthetic particularly in IVRA and, perhaps, could challenge prilocaine, the present local anesthetic of choice for this technique.
Methods: A double-blind, cross-over study of IVRA of the upper extremity in 10 healthy volunteers was performed. There was at least a 1-week interval between the use of the two anesthetics in each volunteer. After exsanguination with an Esmarch bandage, IVRA was induced either with preservative-free 0.5% articaine (5% Ultracaine, Hoechst, Germany, diluted with 0.9% NaCl) or 0.5% prilocaine (Citanest, Astra, Sodertalje, Sweden) (35-50 mL, according to weight), injected in 2 minutes. Sensation at defined skin spots that were innervated by the median, musculocutaneous, radial, and ulnar nerves was tested by pinprick; motor function was tested by the movements of the wrist. After 20 minutes, the tourniquet cuff was deflated in one step. Circulatory, toxic, and skin reactions were registered. At least 1 week after the second IVRA intracutaneous allergy testing with 0.5% articaine, 0.5% prilocaine, histamine, and saline was performed.
Results: There were no significant differences between the two local anesthetics in the onset of analgesia or anesthesia, degree of motor block, and recovery of IVRA. Onset of analgesia occurred 4.2-5.6 minutes, on average, after the injection. One volunteer had short-lasting tinnitus after tourniquet cuff deflation when prilocaine was used. Erythematous nonitching skin rashes developed in 8 of 10 volunteers when articaine was used, and two volunteers had rashes when prilocaine was used. These rashes disappeared within an hour, and negative intracutaneous test results confirmed their nonallergic origin.
Conclusion: Both 0.5% articaine and 0.5% prilocaine, in a median dose of 40 mL in adults, injected in 2 minutes, are effective and equipotent local anesthetics in IVRA of the arm. An earlier reported four-time faster onset time of the block by articaine in comparison with prilocaine may be caused by a very rapid injection rate (40 mL/30 sec) by the investigators of that study. The erythematous skin rashes after IVRA, in particular when articaine was used, may be a sign of venous endothelial irritation.

A Comparison Between Articaine HCl and Lidocaine HCl in Pediatric Dental Patients

Malamed SF, Gagnon S, Leblanc D
Pediatr Dent. 2000;22:307-11

Purpose: Three identical single-dose, randomized, double-blind, parallel-group, active-controlled multicenter studies were conducted to compare the safety and efficacy of articaine HCl (4% with epinephrine 1:100,000) to that of lidocaine HCl (2% with epinephrine 1:100,000) in patients aged 4 years to 79 years, with subgroup analysis on subjects 4 to < 13 years.
Methods: Fifty subjects under the age of 13 years were treated in the articaine group and 20 subjects under the age of 13 were treated with lidocaine. Subjects were randomized in a 2:1 ratio to receive articaine or lidocaine. Efficacy was determined on a gross scale immediately following the procedure by having both the subject and investigator rate the pain experienced by the subject during the procedure using a visual analog scale (VAS). Safety was evaluated by measuring vital signs before and after administration of anesthetic (1 and 5 minutes post-medication and at the end of the procedure) and by assessing adverse events throughout the study. Adverse events were elicited during telephone follow-up at 24 hours and 7 days after the procedure.
Results: Pediatric patients received equal volumes, but higher mg/kg doses, of articaine than lidocaine during both simple and complex dental procedures. Pain ratings: Articaine: VAS (Visual Analogue Scale) scores (from 0 to 10 cm) by patients 4 to < 13 years of age were 0.5 for simple procedures and 1.1 for complex procedures, and average investigator scores were 0.4 and 0.6 for simple and complex procedures, respectively. Lidocaine: patients 0.7 (simple) and 2.3 (complex); investigators 0.3 (simple) and 2.8 (complex). Adverse events: No serious adverse events related to the articaine occurred. The only adverse event considered related to articaine was accidental lip injury in one patient.
Conclusions: VAS scores indicate that articaine is an effective local anesthetic in children and that articaine is as effective as lidocaine when measured on this gross scale. Articaine 4% with epinephrine 1:100,000 is a safe and effective local anesthetic for use in pediatric dentistry. Time to onset and duration of anesthesia are appropriate for clinical use and are comparable to those observed for other commercially available local anesthetics.

Back To Top © 2001-2009 RxRama ---- All rights reserved.