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

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication-

Originator Organization-

Active Organization

American Genomics, LLC

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC13H21ClN2O3S

InChIKeyGDWDBGSWGNEMGJ-UHFFFAOYSA-N

CAS Registry23964-57-0

View All Structures (2)

OBJECTIVELocal 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.METHODSWe 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.RESULTSWe 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).CONCLUSIONOur 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 RELEVANCEThe 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 May 2025·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Probing the articaine–human serum albumin interaction and influences of paracetamol and caffeine on the interaction by spectroscopy, voltammetry, and bioinformatics

Article

Author: Kabir, Md Zahirul ; Mohamad, Saharuddin B ; Rehman, Fazal ; Erkmen, Cem

Interaction between a local anesthetic drug, articaine (ART) and human serum albumin (HSA) was investigated in the absence and presence of paracetamol (PAR) and caffeine (CAF) using spectroscopic, voltammetric, and computational techniques for the first time. The results demonstrated that increasing concentrations of ART in HSA solution led to a decrease in HSA fluorescence signal, indicating the ART-HSA complex formation via the static quenching mechanism. The binding strength of the complex was moderate (binding constant, K_a = 5.87 × 10³ M^-1 in fluorescence and 6.31 × 10³ M^-1 in voltammetric at 298 K). Thermodynamic analysis (ΔS = +28.32 J mol^-1 K^-1; ΔH = -30.17 kJ/mol) of the binding reaction suggested involvement of hydrophobic interactions, van der Waal's forces and hydrogen bonding in stabilizing the ART-HSA complex. Significant microenvironmental alterations near the Trp and Tyr residues of HSA consequent to the ART-HSA complex formation. ART predominantly binds to Sudlow's site I of HSA with more negative binding energy and stronger hydrophobic interactions compared to Site II. The stability of the ART-HSA complex at Site I over a 100 ns timeframe, supported by stable hydrogen bonding and compact HSA structure throughout the molecular dynamics simulations. The effect of PAR and CAF on the binding strength between ART and HSA was also examined, and presence of PAR and CAF in the reaction mixture produced significant reduction in the binding affinity of ART to HSA. These findings underscore the competitive binding between ART, PAR, and CAF, which impacts their pharmacokinetics and efficacy. This study provides valuable insights into the complex interactions between anesthetic drugs and common pharmaceuticals, potentially guiding clinical practices and drug development.

01 Apr 2025·Journal of Endodontics

Anesthetic Effectiveness of Mental/Incisive Nerve Block versus Inferior Alveolar Nerve Block in Mandibular First and Second Premolars with Symptomatic Irreversible Pulpitis: A Randomized Clinical Trial

Article

Author: Yoldas, Oguz ; Küden, Cihan ; Dumani, Aysin ; Kussever, Helin ; Sülek, Tolga

INTRODUCTIONThis study aimed to compare the effectiveness of mental/incisive nerve block (MINB) and conventional inferior alveolar nerve block (IANB) anesthesia during endodontic treatment of mandibular first and second premolars with symptomatic irreversible pulpitis.METHODSIn this randomized, double-blind, clinical trial, 120 patients undergoing endodontic treatment of mandibular premolars were randomly assigned to IANB (n = 60) or MINB (n = 60) using 1.8 mL 4% articaine with 1:100,000 epinephrine hydrochloride. Pain levels were evaluated preoperatively and during cold tests, cavity preparation, and pulp extirpation using the Numerical Rating Scale. Statistical analyses included the independent t test, chi-square test, and Mann-Whitney U test (α = 0.05).RESULTSBoth groups showed a success rate of 70% for anesthesia (P = 1.000). While IANB demonstrated similar efficacy between first (71.4%) and second (68.8%) premolars (P > .05), MINB was significantly more effective for first premolars (76.9%) than second premolars (64.7%) (P < .05).CONCLUSIONSMINB and IANB provide comparable pain control for mandibular premolars during endodontic procedures. However, MINB was observed to be less effective for second premolars compared to first premolars. The study suggests that, despite the comparable success rates of both anesthesia techniques, supplemental anesthesia may still be required to achieve adequate pain management for mandibular premolars with symptomatic irreversible pulpitis.

100 Deals associated with Articaine Hydrochloride

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D02991	Articaine Hydrochloride	N01BB08	DB09009

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Anesthesia	-	-	-

Developing

10 top R&D records.

Login

to view more data

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

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04829344 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	ehzghstkfi(ktaqzvfoiz) = cqkkyvcewd jkyycdtzjk (jpgbqrqwhz, vtabbiaecu - ocboldfgew) View more	-	10 Oct 2024
				Placebo (Placebo)	ehzghstkfi(ktaqzvfoiz) = fguqhdrdjq jkyycdtzjk (jpgbqrqwhz, zwurwtxvpo - wfcjyggpum) View more
NCT05501860 (CTgov)	Phase 3	Anesthesia	249	AG-920 (AG-920)	vrjfddwxbj(mqheumqfhd) = kkpmrhiwnm vgtagbjdsn (jvuutknkup, ijyfkndoec - kkxepknpnw) View more	-	09 Oct 2024
				Placebo (Placebo)	vrjfddwxbj(mqheumqfhd) = rkjuysbevu vgtagbjdsn (jvuutknkup, ewxmyuernc - hdfeyzyunb) View more
NCT05325853 (CTgov)	Phase 3	Anesthesia	61	AG-920 (AG-920)	gvhfujvlwa(grngevdxcp) = xadfollybm zmbgkmmopg (tzgthhovbr, yfcaciozny - ptuejajwai) View more	-	25 Oct 2023
				Proparacaine Ophthalmic (Proparacaine)	gvhfujvlwa(grngevdxcp) = oqdfwpsgmv zmbgkmmopg (tzgthhovbr, cykfbvjrqu - fbujqidmax) View more
NCT04513652 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	avdhxcgrsl(ubawuuejff) = gmpkehkbng hlfsbknkep (ftvmertgor, oimptcjakq - pktmbjurpp) View more	-	28 Sep 2022
				Placebo (Placebo)	avdhxcgrsl(ubawuuejff) = shymnrqngq hlfsbknkep (ftvmertgor, deiftxcogm - kkrexmxlul) View more
ARVO2022	Phase 3	-	120	AG-920	(cdowspqztx) = 9% vs 10% amjlvdqfze (kdmhytsunr ) View more	Positive	01 May 2022
				Placebo
NCT01862614 (Buffered Articaine, CTgov)	Phase 4	Anesthesia	80	articaine (Articaine)	vbdaamlcze(kdrqskrilp) = sucfvfmzvh blbmgssgoi (dfvurlhlus, qiiiclnhds - nzesuruiac) View more	-	02 Dec 2020
				articaine (Buffered Articaine)	vbdaamlcze(kdrqskrilp) = askdtvwuue blbmgssgoi (dfvurlhlus, kitdjfcjep - pjvihiqgqv) View more
NCT04189198 (Pubmed \| Anesthesiol Res Pract)	Phase 1	-	117	Articaine 2%	fgnqllddnl(tmiwatzouf) = zozztytjne sjjvadfqdh (dghwomfafs ) View more	-	01 Jan 2020
				Bupivacaine 0.5%	fgnqllddnl(tmiwatzouf) = advhlqxkte sjjvadfqdh (dghwomfafs )
Pubmed \| Clin Oral Investig	Not Applicable	-	180	2% Articaine	uopilxvdcq(xnsatjiods) = igffjvdqut dlvxhrhghk (ivxbtjrqoh )	-	01 Sep 2019
				2% Lignocaine	uopilxvdcq(xnsatjiods) = rlcjqkiizj dlvxhrhghk (ivxbtjrqoh )
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)	aljfetqvxa(fmkjhsrmvu) = hlfiqfoiyt jdhcnlzesf (bmdczofypp, oyehpgjzjj - rspcnkbjxm) 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)	aljfetqvxa(fmkjhsrmvu) = jrpvucspqh jdhcnlzesf (bmdczofypp, hwhtcmqjfb - oyselfzvik) View more
NCT01496846 (Pubmed \| J Endod)	Phase 4	Pulpitis	201	4% articaine	twvppgolvs(xqvfuyaarf) = exdgtvgqgq gjpxupjkua (edwqrvnvqc )	-	01 Apr 2018