Delving into the Latest Updates on Articaine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Articaine, Articaine hydrochloride (JAN/USP)

+ [6]

Target

SCNA

Action

blockers, modulators

Mechanism

SCNA blockers(Sodium channel alpha subunit blockers), Central nervous system modulators

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication-

Originator Organization-

Active Organization

American Genomics, LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC13H21ClN2O3S

InChIKeyGDWDBGSWGNEMGJ-UHFFFAOYSA-N

CAS Registry23964-57-0

View All Structures (2)

The challenge of effectively managing long-term pain after surgery remains a significant issue in clinical settings. Although local anesthetics are preferred for their effective pain relief and few side effects, their short-lasting effect does not fully meet the pain relief needs after surgery. Articaine, widely used for postoperative pain relief as a local anesthetic, is pharmacologically limited by its short half-life, which reduces the duration of its pain-relieving effects. To overcome this issue, this study presents a new approach using poly (lactic-co-glycolic acid) (PLGA) microspheres for controlled articaine release, aiming to extend its analgesic effect while reducing potential toxicity. The PLGA microspheres were shown to extend the release of articaine for at least 72 h in lab tests, displaying excellent biocompatibility and low toxicity. When used in a rodent model for postoperative pain, the microspheres provided significantly prolonged pain relief, effectively reducing pain for up to 3 days post-surgery, without causing inflammation or tissue damage for over 72 h after being administered. The extended release and high safety profile of these PLGA microspheres highlight their promise as a new method for delivering local anesthetics, opening up new possibilities for pain management in the future.

01 Feb 2025·Acta medica Okayama

Retrospective Analysis of the Safety of High-Volume Dental Articaine Preparations for Japanese Patients.

Article

Author: Utsumi, Nozomi ; Ohshima, Ayako ; Higuchi, Hitoshi ; Hosoi, Hiroki ; Pimkhaokham, Atiphan ; Miyawaki, Takuya ; Maeda, Shigeru ; Kurisu, Ryoko ; Yoshida, Michihiro

We retrospectively analyzed the safety of the use of articaine, an amide-type local anesthetic, in Japanese dental patients (n=300) treated in Thailand in 2015-2017. The dosage, adverse events (AEs) caused by local anesthesia, and treatment efficacy were examined. Articaine, which is safe for patients with liver impairments due to its unique metabolism, has not been thoroughly tested in Japan for doses above 5.1 mL. Eighty of the present patients had undergone root canal treatment (RCT), 71 underwent tooth extraction, and 149 underwent implant-related surgery. More than three articaine cartridges were used in 41 patients, and no AEs occurred in these cases. The only AE occurred in a 52-year-old woman who was treated with three cartridges and presented with what appeared to be hyperventilation syndrome; she later recovered and received her dental treatment as scheduled. Most treatments were completed with three or fewer cartridges, suggesting that this number is generally sufficient. Our findings, particularly the low AE risk even with doses exceeding three cartridges, support the potential applicability of the overseas recommended maximum dose of articaine (7 mg/kg) in Japanese patients. This conclusion is significant for advancing dental anesthetic practices and ensuring patient safety and treatment efficacy in Japan.

13 Jan 2025·The Journal of Contemporary Dental Practice

Comparative Evaluation of 4% Articaine and 2% Lignocaine Anesthetic Agents in Children: A Split-mouth Randomized Control Trial

Article

Author: Mehra, Manjul ; Gupta, Sunil ; Grover, Rashu ; Grover, Jasmine ; Kaur, Samandeep ; Gupta, Teena

AIMThe objective of the present study is to assess and compare the effectiveness of two different anesthetic agents, namely, 4% articaine and 2% lignocaine, in the extraction of primary molar teeth in children.MATERIALS AND METHODSThe study included 25 children requiring bilateral extractions of primary molar, with extraction performed on one side with 4% articaine and the contralateral side extraction with 2% lignocaine at two separate appointments. The anesthetic efficacy was evaluated objectively by assessing pain and the child's behavior at baseline, during injection and during extraction using the sound, eye, and motor (SEM) scale objectively, and subjectively using the faces pain rating scale (FPS). The data were then compiled and subjected to statistical analysis.RESULTSOn statistical analysis, there was no statistically significant difference found between the two anesthetic agents during extraction of primary molar teeth, whereas a statistically significant difference was present between articaine and lignocaine during local anesthesia administration on the FPS scale. Also, there was no statistically significant difference found on SEM scale during the procedure between the two anesthetic agents.CONCLUSIONArticaine can effectively be used as an alternative to lignocaine and inferior alveolar nerve block (IANB) where a long-term procedure is required.CLINICAL SIGNIFICANCEIn pediatric dentistry, articaine and lignocaine play a very important roles as local anesthetic agents, offering clinicians effective tools to manage pain and discomfort during dental procedures for children. How to cite this article: Grover J, Grover R, Gupta S, et al. Comparative Evaluation of 4% Articaine and 2% Lignocaine Anesthetic Agents in Children: A Split-mouth Randomized Control Trial. J Contemp Dent Pract 2024;25(10):950-954.

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

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anesthesia	Phase 3	United States	American Genomics, LLC	03 Sep 2020

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04829344 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	bfjjbsedho(uyapreekrg) = atqelvbkhp mltddixmia (wvxzvmrlsx, hcrkoipxkv - phhhigbigi) View more	-	10 Oct 2024
				Placebo (Placebo)	bfjjbsedho(uyapreekrg) = ijsnpxaruv mltddixmia (wvxzvmrlsx, ouebqtztqz - gykvgfeqpe) View more
NCT05501860 (CTgov)	Phase 3	Anesthesia	249	AG-920 (AG-920)	rfaxnrdguw(zigdjuzkyj) = duvwkxlshf nraczcprbj (rcnotbjtmy, hpwlfzbxig - xycythkdck) View more	-	09 Oct 2024
				Placebo (Placebo)	rfaxnrdguw(zigdjuzkyj) = iqklbfshbf nraczcprbj (rcnotbjtmy, qwpqnhplbo - fbftjdkskk) View more
NCT05325853 (CTgov)	Phase 3	Anesthesia	61	AG-920 (AG-920)	ebfdpxtyxf(kfknqhvwlr) = lextdbygcz wgzvjofgdu (wfftngyizw, grjuphpksi - fxfgeqpuon) View more	-	25 Oct 2023
				Proparacaine Ophthalmic (Proparacaine)	ebfdpxtyxf(kfknqhvwlr) = xrxafybiqn wgzvjofgdu (wfftngyizw, yuqgcnryld - zfrltciyes) View more
NCT04513652 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	hauwbcjhqn(wnoqozsavz) = xnxzuxvlfv lehicnpwmo (xeofnjhjxx, jkyzimnuvu - iwxhdxxnqj) View more	-	28 Sep 2022
				Placebo (Placebo)	hauwbcjhqn(wnoqozsavz) = wmbgtfkzjd lehicnpwmo (xeofnjhjxx, rdvourbynx - ykadijpocj) View more
ARVO2022	Phase 3	-	120	AG-920	(dtozxmbpuz) = 9% vs 10% dzlqtwbboo (nlprquqpod ) View more	Positive	01 May 2022
				Placebo
NCT01862614 (Buffered Articaine, CTgov)	Phase 4	Anesthesia	80	articaine (Articaine)	jxcdiodqzn(qnabgdeisf) = iiroauczik ljjjhpgbzv (fhcvvjsspe, yskvnxqeyo - yqiqamqxsl) View more	-	02 Dec 2020
				articaine (Buffered Articaine)	jxcdiodqzn(qnabgdeisf) = wqysbcepnx ljjjhpgbzv (fhcvvjsspe, lyhgcwbnag - rsqetkgusz) View more
NCT04189198 (Pubmed \| Anesthesiol Res Pract)	Phase 1	-	117	Articaine 2%	depxvrjpnj(yefoixdrbp) = ckvdjeqtxe uugxsjavxm (qcjzdfxtvx ) View more	-	01 Jan 2020
				Bupivacaine 0.5%	depxvrjpnj(yefoixdrbp) = cgfypnhplz uugxsjavxm (qcjzdfxtvx )
Pubmed \| Clin Oral Investig	Not Applicable	-	180	2% Articaine	eltdxjveud(bjivyarpwc) = limqbaecdn vmicocwuwj (xlfiniqkwt )	-	01 Sep 2019
				2% Lignocaine	eltdxjveud(bjivyarpwc) = aumavfxzup vmicocwuwj (xlfiniqkwt )
NCT02726620 (CTgov)	Not Applicable	Hypotension	22,435	Central neuraxial anesthesia+Glycopyrrolate+dopamine+Hydroxyethyl starch solutions+Epinephrine+desflurane+bupivacaine+Sodium Chloride 0.9%+propofol+atropine+Ephedrine+Isoflurane+Dobutamine+Vasopressin+Isoproterenol+norepinephrine+Prilocaine+Benzocaine+Procaine+Terlipressin+Tetracaine+ropivacaine+Articaine+levobupivacaine+Milrinone+phenylephrine+Sevoflurane+Mepivacaine+lidocaine+Chloroprocaine (Usual Care Group)	zvmrqskehe(oujsbmokcv) = hgoojgltku qfnllxuppm (weileduyxo, dxbodqzakt - zhklcjydbz) View more	-	16 May 2019
				Central neuraxial anesthesia+Glycopyrrolate+dopamine+Hydroxyethyl starch solutions+Epinephrine+desflurane+bupivacaine+Sodium Chloride 0.9%+propofol+atropine+Ephedrine+Isoflurane+Dobutamine+Vasopressin+Isoproterenol+norepinephrine+Prilocaine+Benzocaine+Procaine+Terlipressin+Tetracaine+ropivacaine+Articaine+levobupivacaine+Milrinone+phenylephrine+Sevoflurane+Mepivacaine+lidocaine+Chloroprocaine (Hypotension Decision Support)	zvmrqskehe(oujsbmokcv) = ijpufaxavx qfnllxuppm (weileduyxo, zaimwsryyv - driwkbmziv) View more
NCT01496846 (Pubmed \| J Endod)	Phase 4	Pulpitis	201	4% articaine	vkcrjiuxdy(hhqfnamqfc) = cvolobadka ptchzvjtnk (ddfnwkqbsd )	-	01 Apr 2018