Delving into the Latest Updates on Articaine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Articaine, Articaine hydrochloride (JAN/USP), 40-045

+ [7]

Target

SCNA

Action

blockers, modulators

Mechanism

SCNA blockers(Sodium voltage-gated channel alpha subunits blockers), Central nervous system modulators

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication-

Originator Organization

North American Genomics LLC

Active Organization

North American Genomics LLC

Inactive Organization

American Genomics, LLC

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (15 Aug 2025),

Anesthesia

Regulation-

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Structure/Sequence

Molecular FormulaC13H21ClN2O3S

InChIKeyGDWDBGSWGNEMGJ-UHFFFAOYSA-N

CAS Registry23964-57-0

When using dental local anesthetics containing adrenaline as a vasoconstrictor, it is essential to exercise sufficient caution regarding hemodynamic fluctuations, particularly in patients with cardiovascular disease. In this report, we introduce a safe and simple method to halve the adrenaline concentration in anesthetic cartridges. The equipment used includes a syringe (1-3 mL), an IV catheter (22- or 24-G), and a metal needle, which are typically available in dental clinics for IV sedation or emergency use. By connecting the inner needle (24- or 27-G) of the IV catheter to the syringe and puncturing the edge of the rubber stopper at the head of the cartridge, 0.9 mL of anesthetic solution can be accurately aspirated while reducing the risk of coring. Furthermore, by injecting an equal volume of 2% lidocaine without adrenaline into the cartridge, the adrenaline concentration can be effectively halved. This method is quick, broadly applicable, and does not require any special equipment, making it feasible even for dentists who are not specialists in dental anesthesia. In Japan, four types of dental local anesthetics are commonly used. However, dental treatment cannot always be completed with a preparation that does not contain adrenaline, and there are many situations where the excellent anesthetic and hemostatic effects of adrenaline are required. Dentists must accurately assess these situations and confidently select and administer the appropriate anesthetic. It should be noted that articaine alone is not commercially available in Japan; therefore, this method can only be applied to cartridges containing 2% lidocaine with 1:80,000 adrenaline. Although local anesthetics containing 1:80,000 adrenaline are generally considered safe for patients with cardiovascular disease, the use of the lowest possible adrenaline concentration is desirable. Therefore, this method provides a practical approach to minimize cardiovascular risk while maintaining anesthetic efficacy and hemostasis, especially in procedures requiring large amounts of local anesthetic. Given the increasing number of patients with cardiovascular disease due to aging, this technique is considered a practical approach to ensuring safer dental treatment.

01 Jun 2025·INTERNATIONAL DENTAL JOURNAL

Analysis of Adverse Events Associated With Dental Local Anaesthetics Using Food and Drug Administration Adverse Event Reporting System Data

Article

Author: Aydin, Volkan ; Bayram, Ferit ; Apari, Asli Melda ; Akici, Ahmet

OBJECTIVE:

Local anaesthetics (LAs), almost indispensable aspect of dental practice for pain-free procedures, occasionally leads to worrisome adverse events (AEs). We aimed to compare serious and nonserious AEs of LAs for dental reasons in the US Food and Drug Administration AE Reporting System.

METHODS:

We retrospectively analysed dental AE reports associated with LAs in the Food and Drug Administration AE Reporting System database from its inception to April 2024. We described AEs by patients' demographic and clinical characteristics and compared ester and amide LA-associated AEs by their severity.

RESULTS:

We identified 1956 dental cases with a significant increase of AE reports after 2017. Lidocaine and articaine were the most commonly reported LAs (40.4% and 39.2%, respectively). Serious AEs constituted 46.2%, more commonly in females than males (56.6% vs 43.4%, P < .001) and in those on concomitant medications (70.2% vs 42.2, P < .001). These were also significantly higher in epinephrine-containing LAs (70.1%) than that without (34.2%, P < .01). Ester LAs had increased risk of serious AEs (odds ratios [OR]: 3.86; 95% confidence intervals [CI]: 2.77-5.39), particularly as hospitalization, life-threatening event, or death. The odds of serious AEs were lower with lidocaine (OR: 0.59; 95% CI: 0.48-0.71) and articaine (OR: 0.63; 95% CI: 0.52-0.76).

CONCLUSION:

Our study showed higher rate of serious AEs with ester LAs and those with vasoconstrictor-added practices. Besides, serious outcomes appear as more likely in females and those where additional drug use was reported.

CLINICAL RELEVANCE:

The integration of clinical evidence with pharmacovigilance data has the potential to influence clinicians' LA preferences in dental practice, enabling more informed and evidence-based decision-making.

01 Jun 2025·Evidence-based dentistry

Anaesthesia for mandibular premolars with symptomatic irreversible pulpitis – which nerve block is best?

Article

Author: Hayes, Ellis

A COMMENTARY ON:

Sülek T, Dumani A, Küden C, Kussever H, Yoldas O. Anaesthetic effectiveness of mental/incisive nerve block versus inferior alveolar nerve block in mandibular first and second premolars with symptomatic irreversible pulpitis: a randomised clinical trial. J Endod 2025; https://doi.org/10.1016/j.joen.2025.01.016 .

DESIGN:

This study is a randomised, double-blinded, parallel-group clinical trial investigating the efficacy of Mental Nerve Block (MNB) and Inferior Alveolar Nerve Block (IANB) techniques for anaesthesia of mandibular Premolars with Symptomatic Irreversible Pulpitis (SIP). The aim of the clinical trial is to establish if one anaesthetic technique is superior in facilitating Endodontic treatment in Mandibular Premolar Teeth with SIP and to explore if a difference is observed when comparing anaesthesia of First and Second Premolars with use of MNB and IANB techniques. Patients were enroled as per strict inclusion and exclusion criteria, then attended for Endodontic treatment of a Mandibular Premolar Tooth with SIP. Local anaesthetic block technique was determined by random assignment to MNB or IANB. To ensure blinding of the operator with regards to the anaesthesia method, one clinician administered anaesthesia and placed dental dam, and a second clinician completed the procedure.

CASE SELECTION:

In total, 120 patients with a diagnosis of SIP of a Mandibular Premolar Tooth were enroled in the clinical trial. Inclusion criteria required participants be aged 18 to 65 years old and ASA Class I/II. Clinical signs indicative of SIP were required, including: carious pulpal exposure, haemorrhage during cavity preparation and prolonged pain in response to and persisting after thermal stimuli. Participants were excluded from the trial if they experienced pain involving multiple teeth or if there was use of pharmacological agents, with the ability to influence pain perception, within 6 hours of treatment. Participants were excluded from the trial if there was radiographic evidence of Periapical pathology, symptoms indicative of Apical Periodontitis or lack of anaesthesia 15 minutes after IANB administration. The sample size was determined using G*Power software and 60 patients were allocated to each group: MNB and IANB respectively. The drug preparation administered in all cases was 1.8 ml Articaine 4% with 1:100,000 epinephrine hydrochloride and the aspirating technique was used.

DATA ANALYSIS:

Statistical analysis was completed using SPSS Statistics. Patients were verbally questioned prior to Endodontic treatment, with responses recorded on the Numerical Rating Scale (NRS). Pain scores were recorded relating to pre-operative assessments, cold tests, cavity preparation and pulp extirpation. Success rates for the MNB and IANB anaesthesia groups were explored using chi-squared and probability ratio tests. The Man-Whitney U test allowed for comparison of tooth type and gender. In this study, success was defined as patients completing treatment with no pain (NRS = 0) or mild pain (NRS < 3), without additional anaesthesia.

RESULTS:

120 patients were included in the clinical trial, 52 male and 68 female. The number of Premolar teeth that received Endodontic treatment was 120, this was comprised of 54 First Premolars and 66 Second Premolars. 60 patients were randomly allocated to each group: MNB and IANB, for each group data showed similar distributions of patient age, gender and tooth type. All patients reported lip numbness and both anaesthesia techniques achieved a success rate of approximately 70%. The percentage of patients that experienced pain during cavity preparation or pulp extirpation was 30% for both groups. These patients required supplementary injections and were given intraligamentary anaesthesia, 50% experienced adequate pain relief as a result. The IANB technique achieved sufficient anaesthesia for 71.4% of First Premolars and 68.8% of Second Premolars, with no statistically significant difference (P > 0.05). The MNB technique achieved sufficient anaesthesia for 76.9% of First Premolars and 64.7% of Second Premolars, with a statistically significant difference (P < 0.05) recorded comparing the Premolar tooth types.

CONCLUSIONS:

IANB and MNB techniques have comparable efficacy in achieving anaesthesia of First and Second Premolars with SIP. The anaesthesia efficacy achieved by the IANB technique was comparable for First and Second Premolars. It would be beneficial to use the MNB technique for anaesthesia of First Premolars, compared to Second Premolars, as a statistically significant difference was recorded, with higher success rates observed for anaesthesia of First Premolars by the MNB technique. Irrespective of Nerve Block technique and Premolar tooth type, it was identified that for 1 in 3 Premolars with SIP supplementary anaesthesia was required to ensure adequate anaesthesia and patient comfort.

100 Deals associated with Articaine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D02991	Articaine Hydrochloride	N01BB08	DB09009

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	United States	North American Genomics LLC	15 Aug 2025

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


FDA_CDER Manual	Phase 1	-	240	ARTICAINE	tdofdmzdqj(ugillvwcqa) = The treatment effect (difference from placebo) was 65% in both studies. tjrqnypmsi (pswsjbecij )	Positive	15 Aug 2025
				placebo
NCT06047366 (CTgov)	Phase 4	Pulpitis	40	Articaine w/ epi+Mepivacaine plain+Sodium bicarbonate+Lidocaine w/ epi (Buffered)	zwtsezhwwr(oojsmipbzi) = exfoetkmkn ecigqhdbrb (zggouehupy, wetmxoddwi - ncfutfvuqz) View more	-	13 May 2025
				Articaine w/ epi+Mepivacaine plain+Lidocaine w/ epi (Unbuffered)	zwtsezhwwr(oojsmipbzi) = dxawbniwob ecigqhdbrb (zggouehupy, numcqgvame - tbxoxrvobs) View more
NCT04829344 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	vkxrrxltas(otcfqbxqrh) = gkumdgwext lygmukztkf (njipcbnjkg, 0.61) View more	-	10 Oct 2024
				Placebo (Placebo)	vkxrrxltas(otcfqbxqrh) = hzgkldwilh lygmukztkf (njipcbnjkg, 1.67) View more
NCT05501860 (CTgov)	Phase 3	Anesthesia	249	AG-920 (AG-920)	rddqprqnle = erfeckwaah ymwidyvcjb (lkzbvvhthx, dvxvnzzlbz - gkalpsagpt) View more	-	09 Oct 2024
				Placebo (Placebo)	rddqprqnle = rfmzjsowjs ymwidyvcjb (lkzbvvhthx, ulfowqytlv - eaycxrwpje) View more
NCT05325853 (CTgov)	Phase 3	Anesthesia	61	AG-920 (AG-920)	gxqfjjcssk = jzyhoadffg ptkhnmraih (hkbdydwhuy, dscwgrlicl - fkliubscty) View more	-	25 Oct 2023
				Proparacaine Ophthalmic (Proparacaine)	gxqfjjcssk = otanitbszh ptkhnmraih (hkbdydwhuy, xdfernekxg - kqbfkdzbih) View more
NCT04513652 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	mbbstoliac = hhsvdrssam qsxmlfvnev (mxlkjdshsr, dymtibcydk - iohnnuzlwa) View more	-	28 Sep 2022
				Placebo (Placebo)	mbbstoliac = xknjkhrcky qsxmlfvnev (mxlkjdshsr, lrbqbehrxo - nlqttqacbb) View more
ARVO2022	Phase 3	-	120	AG-920	jnfyutrkyr(hcnesevrdb) = 9% vs 10% wcwpjhzzeu (oncmowcfol ) View more	Positive	01 May 2022
				Placebo
NCT01862614 (Buffered Articaine, CTgov)	Phase 4	Anesthesia	80	articaine (Articaine)	opzvpctfux = cpcgqgljzj njjrbajdki (pnkbpnopaj, blavxhhxvu - ypwshygaqv) View more	-	02 Dec 2020
				articaine (Buffered Articaine)	opzvpctfux = lxlaolbpah njjrbajdki (pnkbpnopaj, kamqtdukvv - ndmiyvgqyb) View more
NCT02457325 (CTgov)	Phase 4	Blood Loss, Surgical \| Drug-Related Side Effects and Adverse Reactions	50	articaíne (Surgery With 2%Articaine)	denmkqsfcz(ydcvrjpsqx) = sgeluzhder ednfcpteiw (grygmruqqr, 0.6) View more	-	24 Nov 2020
				articaíne (Surgery With 4%Articaine)	denmkqsfcz(ydcvrjpsqx) = qttzegqzba ednfcpteiw (grygmruqqr, 0.6) View more
NCT04189198 (Pubmed \| Anesthesiol Res Pract)	Phase 1	-	117	Articaine 2%	qfglkviogf(djukxgixcz) = rrtfbatvyk deprklmzli (llwnsudamm ) View more	-	01 Jan 2020
				Bupivacaine 0.5%	qfglkviogf(djukxgixcz) = gaxbwjmcvv deprklmzli (llwnsudamm )