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