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ARTICAINE 30 Years Later O"//////////////////////////////////////////////////////////////////////////////////////////////////////////////////////h
Stanley F. Malamed, DDS Introduction
ocal anesthesia forms the backbone of pain control techniques in dentistry. Local anesthetics represent the safest (when used properly) and most effective drugs for the prevention and management of perioperative and post-operative pain. • • • • The first known injection of a local anesthetic (1885) was an inferior alveolar nerve block administered by the famed medical surgeon Dr. William Stewart Halsted (1852-1922).1 The drugs injected were the combination of cocaine and epinephrine. The dental profession quickly adopted local anesthesia as its primary means of controlling pain eschewing general anesthesia that had been, along with no anesthesia, the techniques of choice prior to 1885. The introduction, in 1905, of procaine (2% with epinephrine 1:50,000), led to a rapid increase in the use oflocal anesthesia by dentists and to the burgeoning of access to dentistry for millions of people worldwide.2 Known everywhere by its primary proprietary name 'Novocain,' procaine is synonymous, to most people, as the 'shot' you receive when you visit the dentist. The amino-ester local anesthetics (LAs), primarily procaine, propoxycaine and tetracaine, were the drugs used from 1906 until the mid-1940's when Astra Pharmaceuticals, in Sweden, synthesized and introduced the first amino-amide local anesthetic, lidocaine (Xylocaine) in 19483 (Fig . 1). The demonstrably superior clinical characteristics oflidocaine compared to the most commonly used esters in dentistry led to its rapid adoption and to the development of other drugs in this same category. The amide local anesthetics mepivacaine (1960), prilocaine (1965), bupivacaine (1972), and etidocaine (1976), were 'borrowed' from medicine for use in the dental
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oralhealth FEBRUARY 2016
Figure 1. Ch e mical form ula of procaine (ester), lidocai ne (amide) and a rt icaine.
profession. The ester local anesthetics are rarely employed today for pain control in the dental profession, worldwide. Carticaine, first prepared by Rusching and colleagues in 1969, had its generic name changed to articaine when it entered clinical practice in Germany in 1976.4 Its use gradually spread, entering North America in Canada in 1983.5 The United Kingdom launched the drug in 1998, the United States in 2000, and Australia in 2005. Articaine represents the first, and still only, local anesthetic developed specifically for use in dentistry. Though articaine is classified as an amide LA, articaine possesses chemical characteristics of both the amide and ester groups ( Fig . 1) . It has become an extremely popular local anesthetic wherever it has been made available . In 2014, articaine was the second most used local anesthetic in the United States with a 34.86% market share
-DENTAL PHARMACOLOGY-
(lidocaine was first at 49.35%).6 In Australia 70% of dentists use articaine.7 In 2012, in Germany, where the drug was introduced in 1976, 97% oflocal anesthetic use by dentists was articaine. 8 Articaine is being used increasingly by the medical profession. 9
Articaine - Chemistry and Pharmacokinetics Articaine is 4-methyl-3(2-[propylamino]propionamido) -2-thiophenecarboxylic acid, methyl ester hydrochloride with a molecular weight of 320.84. It is the only amide local anesthetic that contains a thiophene ring. In addition, articaine is the only widely used amide local anesthetic that also contains an ester linkage ( Fig. 1). Ester LAs undergo metabolism (biotransformation, detoxification) as soon as the drug diffuses into capillaries and veins (hydrolysis by plasma esterase) . Amide LAs enter the blood as still active drugs, circulating throughout the body until they enter the liver where they undergo metabolism by hepatic microsomal enzymes. Unlike the other amide local anesthetics that undergo metabolism in the liver, the biotransformation of articaine occurs in both the liver a~d in plasma. The elimination (beta) half-life of a drug is the time required to decrease its blood (plasma) level or concentration by 50%. It is commonly stated that a drug is 'gone' (eliminated) from the body in six half-lives (The blood level has actually decreased by 98.25%at six-halflives). The elimination half-lives of esters and amides are found in Table 1. Elimination half-lives of esters is comparatively short to those of the amides. Procaine has a half-life of 6 minutes, lidocaine approximately 90 minutes. It is important to remember that the half-life of a drug has absolutely no relevance to the clinical duration of action of that drug. A drug is clinically effective as long as it remains in its target organ (e.g. inferior alveolar nerve) in a high enough (therapeutic) concentration. The clinical action (e.g. 'anesthesia') of the drug ceases when it diffuses out of the target organ into capillaries and veins. It is then that the elimination half-life starts. Articaine, possessing both ester and amide characteristics, has an elimination half-life of approximately 27 minutes. It is eliminated from the blood in 162 minutes (2 hours 42 minutes). This becomes clinically significant when treating (1) pregnant patients, (2) nursing mothers, and (3) lighter weight patients (persons weighing less than 30 kg). Articaine has many of the physicochemical properties of the most commonly used local anesthetics (lidocaine, mepivacaine and prilocaine) with the exception of the aromatic ring and its degree of protein binding (Table 2) . Articaine effectively penetrates tissue and is highly diffusible . Its plasma protein binding of approximately 95 percent is higher than that observed with many local anesthetics. Additionally, the thiophene ring of articaine increases its liposolubility.
1.
Elimination Local Anesthetic
(Beta)
Half-life
1,rnn J
Half-Life 6·
h•l f-life m in (hrs )
Procaine
6
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
i
(2 1 00)
------------------ _______________ J
Elimination half-l ives of local a nesthetics /////./././/././././././././././././././././././././././././././././././././././././h
Articaine and Allergy The incidence of true, documented and reproducible allergy to amide LAs is exceptionally low, though alleged 'allergy' is reported occasionally. True allergy to the ester LAs is - though still quite rare - more common . The immunogenic potential of articaine is very low. Historical experiences indicate that allergic reactions resulting from sensitivity to articaine are rare. However, all LA solutions with a vasoconstrictor (e.g. epinephrine) contain the antioxidant, sodium bisulfite, which can cause allergic reactions . Allergic reactions that have been reported with articaine include edema, urticaria, erythema and anaphylactic shock. In three studies (number of subjects = 1332) comparing articaine 4% with epinephrine 1:100,000 to lidocaine 2% with epinephrine 1:100,000, reports of rash or pruritis were no more frequent with articaine (n = 2) than with lidocaine (n = 4), and no serious allergic reactions were seen in either treatment group. Patients allergic to articaine likely would be allergic to lidocaine and the other amide local anesthetics.10-12 Furthermore, the allergen paraminobenzoic acid (PABA), a frequent metabolite of ester metabolism, is not a byproduct of the hydrolysis phase of articaine.13 As articaine possesses a sulfur-containing thiophene ring (Figure 1) this author is frequently asked if a patient having a sulfa, sulfite or sulfur allergy represents a contraindication to its administration. The answer is 'no'. The 'S' in articaine is an integral part of the thiophene ring and as such cannot be 'seen' or recognized by the patient's immune system . Methemoglobinemia has been shown to develop with some types oflocal anesthetics . Clinical tests of articaine, wwworalhealthgroup.com
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-DENTAL PHARMACOLOGYI
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2
· PHARMACOKINETIC PROPERTIES OF COMMON DENTAL LOCAL ANESTHETICS. LOCAL ANESTHETIC
pKa* (pH)
ONSET
LIPID SOLUBILITYt
USUAL PERCENTAGE OF DRUG USED IN ANESTHETIC
PROTEIN BINDING(%)
DURATION
Articaine
7.8
Fast
1.5
4
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
2
65
Moderate
Mepivacaine
7.7
Fast
1.0
2 to 3
75
Moderate
Prilocaine
7.9
Fast
1.5
4
55
Moderate
Procaine
9.1
Slow
1.0
2 to 4
5
Short
• pKa is a dissociation constant.
t Lipid solubility is a ratio , using procaine as I . Physicochemical characteristics of common LAs
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
Intermediate duration LAs north america
44
Pulpal
(textbook)
oralhealth FEBRUARY 2016
-DENTAL PHARMACOLOGY-
bupivacaine and etidocaine administered as central nerve block anesthetic for urological procedures (n = 103) indicated no elevation of methemoglobin with articaine.14
I
II
Art ica ine - Cli nical Characteristics The clinical preparations of articaine in North America - 4% with 1:100,000 and 1:200,000 epinephrine - are classified as intermediate duration local anesthetics ( Table 3) . Patients responding normally to the drug (normo-responders on a 'bell-shaped curve') should experience pulpal anesthesia of approximately 60 minutes duration and soft tissue anesthesia of between three to five hours duration. Duration of pulpal anesthesia is of slightly longer duration following nerve block compared with infiltration.15 The depth and duration of anesthesia are the same with both epinephrine concentrations. Many doctors report that 'in their opinion' the onset of anesthesia following both infiltration and nerve block with articaine is more rapid than with other local anesthetics. This
Articain e, lidoca ine pulpal anesthesia success rat es - Robert son, Nusstein etal, reference #16
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oralhealth FEBRUARY 2016
-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
Art ica ine, lidocai ne onset o f p ulpal anesthes ia - Robertso n, Nusstein etal , reference #16
.......................................................................................................................... .//./././/././././/./././/././././ 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-
aine compared with 70% for lidocaine. Infiltrating 0.5 mL on both the buccal and lingual of the lateral incisor increased the success rate to 97% for articaine and 88% for lidocaine. The duration of pulpal anesthesia was also significantly longer with both articaine infiltrations. ( Table 6). The increased success rate for infiltration in the adult mandible was thought to be due to the fact that the cortical plate of bone, both buccal and lingual, is quite thin and might provide little resistance to infiltration.18 Given articaine's ability to diffuse through the thick cortical plate of bone following infiltration in the adult mandible, Kanaa et al looked at the ability of articaine infiltration to increase the success rate of pulpal anesthesia following an inferior alveolar nerve block (IANB) with 2% lidocaine with epinephrine 1:80,000.19Patients received IANBs at each of two occasions (2.0 mL lidocaine with epinephrine). Then they received either a buccal infiltration of 4% articaine with epinephrine 1:100,000 or a 'dummy' injection in the buccal fold
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
Articaine in Special Patient Populations: Pregnancy, Nursing and Pediatrics. In the United States the Food and Drug Administration classifies drugs by their safety during pregnancy and nursing.20 The author is unaware of similar listings by Health Canada (www.hc-sc.gc.ca). Pregnancy: All injectable local anesthetics, including articaine, and epinephrine, are classified as 'B' [Caution advised - no evidence of 2"" or 3"1 trimester risk; fetal harm
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oralhealth FEBRUARY 2016
.
-DENTAL PHARMACOLOGY-
possible but unlikely] or 'C' [Weigh risk/benefit - weigh possible fetal risk vs. maternal benefit; see package insert for drug-specific recommendations]. Lidocaine and prilocaine are 'B' rated, all other local anesthetics (including articaine), and epinephrine are 'C'. To minimize exposure of the fetus to the effects of the local anesthetic drug, a drug with a shorter elimination half-life is preferred. The 27-minute half-life of articaine is preferable to the 90-minute or greater half-life of the other available local anesthetics . Nursing : FDA categories for nursing infants are 'S' (Safe for nursing infant); ' S?' (Safety in nursing infants unknown); 'S*' (Potential for significant effects on nursing infants) and 'NS' (Not safe for nursing infants). 20 Lidocaine is the only 'S' local anesthetic. All others are 'S?' including epinephrine (in dental concentrations). As nurs-
Mandibular Incisors
I
I!: ~~
11
80
10
11 :
1! :
+
Uoleb
**'
Attll Att b•I
u.i. ....
Im : ~
O ....._O- S- 1 0-415-:zo-ZS-JO- .- 4 0___.45
. ......_.............
TIM• (MlllVTES)
Duration of pulpal anesthesia following mandibular infiltration . Meechan, Ledvinka , reference #17
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-DENTAL PHARMACOLOGY-
a
I st Molar
h u
•
i~
l st Premolar
100 90
80
gt~ 70 1:1a cc 00
~'ii 50
h
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
4
e
e
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
ing mothers are normally reluctant to expose their infant to any drug that child does not need, it is not uncommon in the dental environment to have a nursing mother in need of dental care ask their dentist, 'Will the drug (e.g. lidocaine) be in the milk?" The answer will always be 'Yes.' The mother immediately states that they do not want the drug. This becomes problematic when the dental procedure is potentially painful. The concept of"pump and discard ' successfully handles this situation. Following exposure to a drug the nursing mother should pump and discard the milk for a period covering six elimination half-lives of the drug administered. For all local anesthetics except articaine this is a period of nine hours. The FDA states 'When using articaine, nursing mothers may choose to pump and discard breast milk for approximately four hours (based on plasma halflife) following an injection of articaine (to minimize infant ingestion) and then resume breastfeeding." Ped iatrics: All local anesthetics can produce seizures (a classic local anesthetic overdose manifests as a generalized tonic-clonic convulsion) if their blood level becomes elevated above the seizure threshold for that drug. One cartridge of any local anesthetic administered rapidly (0
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www.oralhealthgro up.com 65
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-DENTAL PHARMACOLOGY~
4.
Dr. Stanley Ma lamed is a dentist anesthesio logist and emeritus professor of dentistry a t the Herman Ostrow Sc h oo l of Dent istry of U.S.C, in L os A n geles, Ca lifornia.
Muschaweck R, Rippel R. Ein neues Lokalanasthetikum (Carticain) aus der Thiophenre ihe [A new local anaesthetic (carticaine) in the thiophene ser ies]. Prakt Anaesth g(3):135-146, lg74
5 . Lemay H; Albert G; Helie P; Dufour L; Gagnon P; Payant L; Laliberte R. Ultracaine en dentisterie operatoire conventionnelle.
Oral Health welcomes this original article.
[Ultracaine in conventional operative dentistry]. J Can Dent As soc. 50(g):703-708, lg34
Editors Note:
6.
Dental local anesthetic market share , United States, Calendar year-2014, 23 April 2015. Septodont Inc. Lancaster, PA
Ora l Health welcomes this original article from the well-respected
7.
Yapp KE; Hopcraft MS; Parashos P. Dentists' perceptions of a new
Dr. Stan ley Ma lamed on articaine. In his review, Dr. Malamed dis-
loca l anaesthetic drug-articaine. Aust Dent J. 57(1):18-22; quiz
cusses artica in e and paraesthesias. It is worth noting that the use
10g, 2012
of articaine and other 4% loca l anaesthetic so lutions for mandib-
8.
Deutcher Denta lmarkt Jahresbericht (DOM) 2010 (German
ular blocks has been an active ly debated topic for years. With re-
Dental Market Annua l Report 2010). GfK HealthCare, Nuremberg,
gard to paraesthesias currently, the bulk of the literature suggests
Germany
a higher-than-expected incidence when higher concentrat ion (4%) local anaesthetic preparations are used. In the interest of presenting topics in a balanced way, and acknow ledging Dr. Malc;imed 's ,enthusiastic support for t h e cont inued use of articaine for inferior alveo lar nerve b locks in this artic le, our readers may wish to also review articles by Dr. Dan Haas and Dr. S0ren H il lerup. Drs. Haas and H ill e r up are two of the more notable addi t ion al au tho rs on the incidence of paraesthesias and some assoc iat ed factors.
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
10. Malamed SF, Gagnon S, Leblanc D: Efficacy of articaine: a new
amide local anesthetic. J Amer Dent Assoc 131(5):635-642, 2000 11 . Malamed SF, Gagnon S, Leblanc D: Safety of articaine: a new am-
ide local anesthet ic. J Amer Dent Assoc, 132(2):177-185, 2001 12. Malamed SF, Gagnon S, Leblanc D: Articaine hydrochloride in
Their viewpoint represents a more guarded approach in t h e use
pediatric dentistry: safety and efficacy of a new am ide-type local
of 4% solutions for mandibu lar b locks.
anesthetic. Pediatr Dent 22(4):307-311, 2000 13. Hawkins, JM, Moore, PA. Local anesthesia: advances in agents
Also at issue in this article is the use of articaine in pregnant women. Dr. Ma lamed suggests that articaine, an F DA C-rated
and techniques. Dent Clin N Amer 46:719-732,2002. 14. Rupieper N; Stocker L. Haemiglobinspiegel unter Lokalanaesth-
agent should be used instead of B - rated lidocaine. T he reason
esie mit Bupivacain, Carticain und Etidocain. [Met-Hb formation
given is the shorter fetal exposure time to articaine because of
and local anesthesia using bupivacaine, carticaine and etido-
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.
caine]. Anaesthesist. 30(5):23-25, 1981 15. Ultracaine DS Forte 1:100,000, Drug package insert. HANSAmed,
Mississauga, Ontario, Canada, September 2015 16. Malamed SF, Tavana S, Falke l M. Faster onset and more com-
As always, h ow you choose to treat your patients is ultimately
fortab le injection with alka linized 2% lidocaine with epinephrine
your decision . A t Oral Health , we would like these decisions to
1:100,000. Compendium 34(Spec issue #1):1-11, 2013
be based on the best information avai lable. We hope that you enjoyed Dr. Malamed's article.
17. Robertson D, Nusstein J, Reader A , Beck M, McCartney M. The
anesthetic efficacy of articaine in buccal infiltration of mandibular posterior teeth. J Am Dent Assoc 138:1104-lll2, 2007
Dr. Peter Nkansah
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
buccal infil t rat ion enhances the effectiveness of lidocaine inferior
nerve blocking. Br Dent J. 211(10):485-487, 2011
alveolar nerve b lock. Int Endod J 42:238-246, 2009
Ruetsch YA; Boni T; Borgeat A . From cocaine to ropivacaine: the history of local anesthetic drugs. Curr Top Med Chem. 1(3):175182, 2001
3.
injections. Int Endod J 35:629-634, 2002 19. Kanaa JM, Whitworth JM, Corbett IP, Meechan JG. Articaine
Lofgren N. Studies on local anesthetics: Xylocaine , a new synthetic drug. Stockholm: Hoegstroems, lg43
20 . United States FDA Pregnancy Categories. http://www.drugs.
com/pregnancy-categories.html. Accessed 17 September 2015 21 . Malamed SF. Systemic complications, in Handbook of Local Anes-
I ii
thesia, 6 1h ed. 2013 , Mosby Elsevier, St. Louis , pages 313-314
I'
22. Hawkins JM. Local anesthetic maximum doses. Adapted from
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various sources, 2012. Dr. J Mel Hawkins, Anes th esia Services for Dentistry, Inc. Toronto, ON, Canada
alveolar nerves. Anesth Prog. 37(1):42-4S, 1990 42. Stenver D I, Case number: 3200-1367, Adverse effects from an -
23 . Haas DA, Lennon D : A 21 year retrospective study of reports o f
aesthet ics used in relation with dental ca re with a special focus
paresthesia following local anesthetic administration , J Can Dent
on anaesthetics containing articaine. Pharmacovigilance Working
Assoc 61:319 - 320, 323 - 326, 329 - 330, 199S. 24. Hillerup S, Jensen R. Nerve injur y caused by mandibular block
analgesia. Int J Oral Maxillofac Surg. 3S:437-443, 2006
Party of the European Union. 20 October, 2006 43.
~anish
Medicines Agency ( Laegemidde l Styrelsen), Report 2S
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.
currence of paresthesia afte r dental local anesthetic administration
Occurrence of paresthesia aftert dental local anesthetic admin-
in the United States. J Am Dent Assoc. 141(7):836-844, 2010
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
dental 2012 , Version 2, Australian Dental Association , Melbourne, pag e 116 29. Stedman 's Online Medical Dictionary. Paresthesia (definition).
Available at: www.stedmans.com. Accessed 16 September 201S
30 . Haas DA. Articaine and paresthesia: epidemio log ica l studies. J Am Coll Dent 73(3):S - 10, 2006
31 . Pogrel MA , Thamby S: Permanent nerve involvement resulting from inferior alveolar nerve blocks . J Am Dent Assoc 131:901-907, 2000
32 . Pogrel MA , Thamby S : The etiology of altered sensation in the inferior alveo lar, lin gual , and mental nerves as a result of denta l treatment , J Calif Dent Assoc 27:S31-S38, 1999.
33. Pogrel MA , Thamby S: The etiology of altered sensation in the inferior alveolar, lingual , and mental nerves as a result of dental treatment , J Calif Dent Assoc 27:S31-S38 , 1999 34. Dower JS Jr: A review of paresthesia in assoc iation with admin is-
tration of local anesthesia, Dent Today 22:64-69, 2003 35 . Berde CB , Strichartz GR. Local Anesthetics , in Miller 's Anesthesia, Miller RD editor. 8 1h ed. 201S. Saunders Elsevier, pages 1028-10S4 36. Pogrel MA. Permanent nerve damage from inferior alveo lar
nerve blocks - an update to include articaine. J Calif Dent Assoc 36(4):271-273, 2007 37. Pogrel MA. Permanent nerve damage from inferior alveo lar nerve blocks : a current update. J Calif Dent Assoc 40(10):79S-797, 2012 38. McDowell AJ. Effective practica l steps to avoid comp li cations in
45. U.S. Food and Drug Administration Center for Drug Evaluation
and Research, Office of Post-Marketing Drug Risk Assessment. Revised 9 January 2009. http://www.fda.gov/Drugs/ Guidance ComplianceRegulatorylnformation/ Surveillance/ AdverseDrugEffects/defau lt.htm 46. Weber JCP. Epidemiology of adverse reactions to nonsteroidal
antiinflammatory drugs. In Rainsford KD , Velo GP eds. Advances in Inflammation Research. Vol. 6. New York, Raven Press, 1984, pages 1-7 47. Hartnell NR; Wilson JP. Replication of the Weber effect using
postmarketing adverse event reports volu ntaril y submitted to the United States Food and Drug Administration. Pharmacotherapy. 24(6):743-749, 2004
48. Alling CC 3rd. Dysesthesia of the lingual and inferior alveolar nerves following third molar surgery. J Ora l Maxillofac Surg. 44(6):4S4-4S7, 1986
'
49. Ellies LG. A ltered sensation following mandibular implant surgery:
a retrospective study. J Prosthet Dent. 68(4):664-71 , 1992 50 . Medline search. Years 1946-201S key words: paresthesia , dentistry.
Search 16 September 201S 51. Snoeck M. Articaine: a review of its use for local and regional
anesthes ia. Local Regional Anesth S:23-33, 2012 52 . Pogrel MA , Thamby S. Permanent nerve involvement resulting from
inferior alveolar nerve blocks. J Am Dent Assoc 131:901-907, 2000 53 . Pogrel MA; Schmidt BL; Sambajon V; Jordan RC. Lingual nerve damage due to inferior alveolar nerve blocks: a possible exp lana tion. J Am Dent Assoc. 134(2):19S-199, 2003 54. Katya l V. The efficacy and safety of articaine versus lignocaine in
dental treatments : a meta-analysis. J Dent. 38(4):307-317, 2010 55 . Brandt RG; Anderson PF; McDonald NJ; Sohn W ; Peters MC. The
face-lifting. Review of lOS consecutive cases. Plast Reconstr Surg.
pu lpal anesthetic efficacy of articaine versus lidocaine in dentistry:
S0(6):S63-S72, 1972
a meta-ana lysis. J Am Dent Assoc. 142(S):493-S04, 2011
39. Lagarde P. Paresthesies du territoire mentonnier, secondaires a
un traitement endodontique. [Paresthesia in the area of the chin, secondary to endodontic treatment]. Inf Dent. 60(19):17-23, 1978 40. Hickel R, Spitzer WJ , Petschelt A, Voss A. Zur Problematik von
Sensibilitatsstorungen nach Leitungsanasthesie im Unterkiefer. [Sensitivity problems following mandibular conduction anesthesia]. Dtsch Zahnarztl Z. 43(11):11S9-1161 , 1988 41 . Nickel AA Jr. A retrospective study of paresthesia of the dental
68
istration in the United States. J Am Dent Assoc 141(7):836- 844, 2010
oralhealth FEBRUARY 2016
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
