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42
-DENTAL PHARMACOLOGY-
1.
Elimination
Local Anesthetic
(Beta)
Half-life
1,rnn J
Half-Life
6
hl f-life m in (hrs )
Procaine
Articaine
27
162
Cocaine
42
252 (4:52)
Lidocaine
-90
-540 (9:00)
Prilocaine
-90
-540 (9:00)
Mepivacaine
-120
Bupivacaine
36
-720 (12:00)
1260
Ester,_ Red
mide>=Blue
(2:42)
I
j
(2 1 00)
------------------ _______________ J
43
-DENTAL PHARMACOLOGYI
pKa*
(pH)
ONSET
LIPID
SOLUBILITYt
USUAL
PERCENTAGE
OF DRUG
USED IN
ANESTHETIC
PROTEIN
BINDING(%)
DURATION
Articaine
7.8
Fast
1.5
95
Moderate
Bupivacaine
8.1
Moderate
30 .0
0.5 to0.75
95
Long
Etidocaine
7.9
Fast
140.0
1.5
94
Long
Lidocaine
7.8
Fast
4.0
65
Moderate
Mepivacaine
7.7
Fast
1.0
2 to 3
75
Moderate
Prilocaine
7.9
Fast
1.5
55
Moderate
Procaine
9.1
Slow
1.0
2 to 4
Short
3.
Drug
Onset
Soft Tissue
3 - 5 min
60 min
3 - 5 hours
2 - 3 min
60 min
3 - 5 hours
Lidocaine
2/o
Epi
1:50k, 1:100k
Articaine 4/o
Epi
1 :100k
1 :200k
Mepivacaine
2/o
Epi 1 :100k
3 - 5 min
60 min
3 - 5 hours
Prilocaine
4/o
Epi
1 :200k
3 - 5 min
60 min
3 - 8 hours
44
Pulpal
(textbook)
-DENTAL PHARMACOLOGY-
II
'-"'
R
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a1se
TM
s1Nus un
SYSTEM
I
II
I
The iRaise features a channel, used to inject fluids beneath the Schneiderian
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-DENTAL PHARMACOLOGY-
assertion is not supported by clinical research.10,16 In studies including a combined 1554 patients there was no clinical
difference noted in the onset of pulpal anesthesia following
inferior alveolar nerve block between 2% lidocaine, epinephrine 1:100,000 and 4% articaine epinephrine 1:100,000.
However, the administration of articaine by mandibular infiltration in adults has been shown to be significantly more effective
in providing pulpal anesthesia than lidocaine infiltration when
used as a sole injection for mandibular anesthesia.17 Successful
pulpal anesthesia was assessed (using electric pulp tester [EPT])
following articaine or lidocaine infiltration ofl.8 mL in the
buccal fold adjacent to the mandibular 1" molar. Table 4 shows
the percentages of successful pulpal anesthesia (Table 4). Onset
time for pulpal anesthesia was also considerably more rapid with
articaine than lidocaine ( Table 5). The result was attributed to
articaine's thiophene ring, which is more lipid-soluble than the
benzene ring found in other local anesthetics.
Meechan and Ledvinka compared the infiltration of 4%
Tooth
Articaine onset
(min)
2nd molar
l" premolar
+/-
Standard
Deviation
4.6+/-4.0
4.2 +/-3.1
4.3 +/-2.3
4.7+/-2.4
Udocaine
onset (min)
+/-Standard
Deviation
11.1 +/-9.5
7.7 +/- 4.3
6.9 +[ -6.6
6.3 +/ - 3 .1
P value
.0001
.0002
.0014
.0137
..........................................................................................................................
.//./././/././././/./././/././././
articaine with epinephrine 1:100,000 and 2% lidocaine with
epinephrine 1:100,000 on mandibular incisors, both for
success and duration of pulpal anesthesia.18 Infiltrating 0.5
mL in the buccal fold produced a 94% success rate for artic-
'
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-DENTAL PHARMACOLOGY-
by the mandibular 1" molar. The 1" molar and 1" premolar
were pulp tested every three minutes for 45 minutes. Results
are shown in Figures 2 and 3. In both teeth the additional
articaine infiltration significantly increased the success rate
of pulpal anesthesia (55.6% to 91.7% for 1" molar; 66.7% to
88.9% for 1" premolar). Though the study concluded at 45
minu'tes there was no indication that pulpal anesthesia was
waning at that time.19
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48
-DENTAL PHARMACOLOGY-
Mandibular Incisors
I!:
~~
11
80
10
11 :
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Im :
~
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49
-DENTAL PHARMACOLOGY-
I st Molar
h
u
i~
l st Premolar
100
90
80
gt~ 70
1:1a
cc 00
~'ii 50
Ii
e:::_8 _ii
..
:ii 20
~E
- - - Troatment 1
Troatment 2
Og
I/.
10
15
20
25
30
Timo after lnjoction (min)
35
40
40
30
10
0
45
10
15
20
25
30
Tlmo alter lnjoction (min)
35
40
45
Figure 2 & 3 : Successful pulpal anesthesia. Blue= IANB - Lidocaine 2 % + epi 1:80,000 + " dummy" infiltration.
Purp le= IANB - Lidocaine 2 % + epi 1:80,000 + " articaine" infiltration. Reference #18
52
6. ~
Year
Haas,
Lennon . Canada
1995
70.6
22
2006
77
23
Author
Country
'
! Kingon, '
j
Sambrook ! Australia
G~~~~o, ,
Reference #
--+-----------+-
2011
USA
2010
L.__._J____ -----'~- ........
j
Lingual
80
25
92.7
24
L----.L.--_J
-DENTAL PHARMACOLOGY-
Drug
Articaine
HCI
Bupivacaine
Lidocaine
HCI
Mepivacaine
Prilocaine
HCI
HCI
HCI
54
-DENTAL PHARMACOLOGY-
~)
l ,800,000
Hiller
~o
1,600,000
3S
l ,-400,000
l ,200 ,000
2S
1,000,000
800,000 _
600,000
10
-400,000
I l _I
s
0
r!''
r',,
'\'
'\'
. .<f'
.
r'~
'\'
'\'
Adverst reacbcos
Use
200,000
f:l'~
'\'
'
:I
Figure 4 : Articaine sales (red line) and adverse event reports (blue bars) in Denmark, 2001-2010, refe rence #42
___,,,,,,,,,,,,,,,,,,///////////././
is assumed that, the nerve is in the area - if the patient's
anatomy is 'normal.'
2. Injections: Once a needle penetrates skin or mucou s
membrane, every injection is blind. In most intramuscular (IM) injections when therapeutic drugs are being
administered, the site selected for IM administration is
one that it is considered anatomically 'safe'. The vastus
lateralis muscle (located in the anterior lateral portion
of the thigh) is considered the safest place in the human
body to administer an IM injection with minimal risk
of damaging important structures (e.g. nerves, arteries,
veins). Local anesthetic administration in dentistry is
different. Consider that with a local anesthetic injection
we are 'aiming' to deposit a volume oflocal anesthetic
55
:I
I
11
-DENTAL PHARMACOLOGY-
q"//////////////////////.////////////////.///////
57
-DENTAL PHARMACOLOGY-
II
58
8.
USA
Table 8.
Ontario - 1993
Mepivacaine
1:623,112,900
1:1,125,000
Lidocaine
1 :181,076,673
1:1,125,000
Bupivacaine
1 :124.286,050
References 23. 44
OVERALL
1 : 13,800,970
Artlcalne
1:
4,159,848
Prilocaine
1:
2.070.678
1:
785,000
(2.27:1.000.000)
1:
440,529
(1 7 1.000,000)
1:
588.235
----------------------------~----------------------~----~
-DENTAL PHARMACOLOGY-
~
R
a1se
TM
31
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2
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- DENTAL PHARMACOLOGY-
Thamby estimated the risk of permanent nerve damage following IANB at 1in26,762 injections.52 They stated that "it
is reasonable to suggest that during a career, each dentist may
encounter at least one patient with an inferior alveolar nerve
block resulting in permanent nerve involvement. The mechanisms are unknown and there is no known prevention or
treatment."52 In the course of a twenty- to thirty-year dental
career, it is estimated that more than 30,000 IANBs will be
administered. 52
Why is it that the lingual nerve is primarily involved in
cases of paresthesia? Considering that when administering the
IANB the vast majority of local anesthetic volume is deposited
close to the IAN (e.g. 1.3 to 1.5 mL), not the lingual nerve
(e.g. 0.2 to 0.3 mL), if paresthesia was a local anesthetic neurotoxic phenomenon, we would expect the IAN to be affected
much more often than the lingual nerve.
The fact that the lingual nerve is stretched when the patient
~-
Dougl
1b1
1DS
Bad Bounces and Broken Teeth:
The Sports Dentistry Side of Your Practice
M
DDS
Update on Local Anesthesia
le
DDS
Applied Esthetic Principles for Treatment Success
Follow on
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61
lI
- DENTAL PHARMACOLOGY-
9.
% Cases of aresthesia
0
o Market share
2007
Lidocaine
(_~} ~ (_~~:. /
1.19
Articaine
= Exoectecl
Mepivacaine
2012
('. s
0.97
,~--~
L.
t)
L
Prilocaine
References #35,36
Market sh ar e and obser ved incidence of paraesthesia
62
~---~----
-DENTAL PHARMACOLOGY-
~
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-DENTAL PHARMACOLOGY-
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PACIFIC
TRAINING
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11
www.oralhealthgro up.com 65
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-DENTAL PHARMACOLOGY~
4.
Editors Note:
6.
7.
Dr. Stan ley Ma lamed on articaine. In his review, Dr. Malamed dis-
10g, 2012
8.
ular blocks has been an active ly debated topic for years. With re-
Germany
9.
Vree TB; Gielen MJ. Clinical pharmacology and the use of articaine for local and regional anaesthesia. Best Pract Res Clin
Anaesthesiol. lg(2):2g3-308, 2005
its faster metabol ism. What is not clear is why exposing a fetus
to a potent ia ll y more harmfu l drug, even for a shorter time is
advantageous.
18 . Meechan JG, Ledvinka JI. Pulpal anaesthesia for mandibular central incisor teeth: a comparison of infiltration and intraligamentary
References
1.
2.
Lopez-Valverde A; De Vicente J; Cutando A. The surgeons Halsted and Hal l, cocaine and the discovery of dental anaesthesia by
3.
Lofgren N. Studies on local anesthetics: Xylocaine , a new synthetic drug. Stockholm: Hoegstroems, lg43
I
ii
I'
www.oralhealthgroup.com
11
'"
67
111
111
-DENTAL PHARMACOLOGY-
various sources, 2012. Dr. J Mel Hawkins, Anes th esia Services for
Dentistry, Inc. Toronto, ON, Canada
~anish
Octobe r 2011
25. Garisto GA; Gaffen AS; Lawrence HP; Tenenbaum HC; Haas DA. Oc-
44 . Garisto GA, Gaffen AS, Lawrence HP, Tenenbaum HC, Haas DA.
26. Kingen A; Sambrook P; Goss A. Hi gher concentration loca l anaesthet ics causing pro longed anaesthes ia. Do th ey? A li terature
review and case reports Aust Dent J. S6(4):348-3Sl, 2011
27. Practice alert: Paraesthesia follow in g loca l anaesthetic injection.
Dispatch. Royal College of Dental Surgeons of Ontario. 19(3) 26,
200S
28. Oral and Dental Expert Group. Therapeutic guidelines: oral and
45. U.S. Food and Drug Administration Center for Drug Evaluation
'
S0(6):S63-S72, 1972
68
56. Baroni DB; Franz-Montan M; Cogo K; Berto LA; Volpato MC; Novaes PD ; Groppo FC. Effect of articaine on mental nerve anterior
portion: histological analysis in rats. Acta Odontol Scand. 71(1):8287, 2013
57. Malet A; Faure MO; Deletage N ; Pereira B; Haas J; Lambert G. The
comparative cytotoxic effects of different local anesthetics on a
human neuroblastoma cell lin e. Anesth Analg. 120(3):S89-S96,
201S