ARTICAINE

1. Articaine
S.Yazhini

2. Synopsis
• Introduction
• LA classification
• Metabolism
• Mechanism of action
• Maximum dosage
• Usage in dentistry
• Conclusion
• References

3. Introduction
• Local anesthetics block peripheral nerves and are used to prevent
pain, to provide motor blockade during surgical or dental
procedures.
• Originally synthesized as ‘Carticaine HCl’ by H. Rusching et al in
1969, entered dentistry practice in 1976.

4. Classification of LA
Esters Amides
Esters of benzoic
acid
Esters of para
aminobenzoic acid
Quinolones
Centbucridine
Butacaine
Cocaine
Ethyl
aminobenzoate
(benzocaine)
Hexylcaine
Piperocaine
Tetracaine
Chloroprocaine
Procaine
Propoxycaine
Articaine
Bupivacaine
Dibucaine
Etidocaine
Lidocaine
Mepivacaine
Prilocaine
Ropivacaine
Malamed SF. Handbook of Local Anesthesia, 7th edition, Mosby. 2019.

5. Articaine
• 4-methyl-3-[2-(propylamino)-propionamido]-2-thiophene-
carboxylic acid, methyl ester hydrochloride
• Thiophene ring allows greater lipid solubility - facilitates diffusion
across the lipid rich nerve membrane - helps in the entry of a greater
amount of the administered anaesthetic solution into the neurons
Intermediate-potency,
short-acting
amide local anesthetic
with a fast metabolism
Ananthu H. Articaine: Opening up a New Vista For Pediatric Dentists. Indian Journal of Forensic Medicine and
Toxicology.2021;15(4):82-89.

6. Metabolism
• Biotransformation of articaine HCl occur in
serum - plasmacholinestrase
hydrolysis into articainic acid (inactive)
liver - hepatic microsomal enzymes (cytochrome P-450 and
NADPH-cytochrome C reductase, phosphatidylcholine)
kidney - articainic acid glucuronide (inactive)
• Articainic acid , articainic acid glucuronide and the parent drug are
excreted via urine.
Vasodilatory effect- increasing its systemic
absorption
Snoeck. Articaine: a review of its use for local and regional anesthesia. Local and regional anesthesia.2012; 5 : 23-33

7. Mechanism of action
• Articaine blocks nerve conduction by reversibly binding to the α-
subunit of the voltage-gated sodium channels within the inner cavity
of the nerve

8. Elimination:
half-life of app.
27 minutes.
It is eliminated
from the blood in
162 minutes
(2 hours 42
minutes)
Malamed SF. Articaine 30 Years Later. Available at: https://www.oralhealthgroup.com/features/1003919408/. Accessed May 8, 2023

9. Allergic reactions
• Edema, urticaria, erythema and anaphylactic shock –
Vasoconstrictor preservative.
• 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-
not contra indicated in sulpha allergy.
• Has a high affinity for plasma protein binding and it is the only
amide analgesia to contain an ester group; this allows it to be
rapidly broken down into its inactive state, thus decreasing systemic
toxicity
Ananthu H. Articaine: Opening up a New Vista For Pediatric Dentists. Indian Journal of Forensic
Medicine & Toxicology, October-December 2021;15(4):82-89.

10. Articaine in pediatric dentistry
• The potency of articaine is 1.5 times that of lidocaine, which enables
the administration of a smaller volume of the drug.
• It is also 0.6 times less toxic as compared to lidocaine.
• Articaine can be given via buccal infiltration to children requiring
pulp therapy and extractions and can thereby be used to replace
inferior alveolar nerve block (IANB).
Thaminee. Articaine in Dentistry. J Pharm Sci Res. 2015; 7(9):792-794

11. • Buccal and palatal infiltration with other local anaesthetic agents
was replaced by a single buccal infiltration using articaine.
• Extent of soft tissue analgesia experienced by the patient can be
reduced and therefore the incidence of complications like lip biting
can be minimized.
• Wright et al in 1989- 21% of 373 American dentists satisfactorily use
articaine in younger children-2–3 years of age.
• Elheeny et al in 2020 - Efficient and safe use to use for children
between age 3 to 4.
• Wright GZ, Weinberger SJ, Friedman CS, Plotzke OB. Use of articaine local anesthesia in children
under 4 years of age – a retrospective report. Anesth Prog. 1989;36:268–271.
• Elheeny AAH. Articaine efficacy and safety in young children below the age of four years : An
equivalent parallel randomized control trial. Int J Paediatr Dent. 2020;30(5):547–55.

12. Conclusion
• Pain management plays a crucial role in the success of any dental
treatment in a pediatric patient. Minimising the fear and anxiety, a
proper management protocol can help develop a positive attitude.
• Evidence of superiority over other LA drugs, use of articaine - the
choice will be based on the personal preference and experiences of
individual clinicians.

13. References
• Malamed SF. Handbook of Local Anesthesia, 7th edition, Mosby. 2019.
• Wright GZ, Weinberger SJ, Friedman CS, Plotzke OB. Use of articaine local anesthesia in children
under 4 years of age – a retrospective report. Anesth Prog. 1989;36:268–271.
• Elheeny AAH. Articaine efficacy and safety in young children below the age of four years : An
equivalent parallel randomized control trial. Int J Paediatr Dent. 2020;30(5):547–55.
• Thaminee. Articaine in Dentistry. J Pharm Sci Res. 2015; 7(9):792-794.
• Snoeck. Articaine: a review of its use for local and regional anesthesia. Local and regional
anesthesia.2012; 5 : 23-33
• Ananthu H. Articaine: Opening up a New Vista For Pediatric Dentists. Indian Journal of Forensic
Medicine and Toxicology.2021;15(4):82-89.
• Malamed SF. Articaine 30 Years Later. Available at:
https://www.oralhealthgroup.com/features/1003919408/. Accessed May 8, 2023