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

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)

Author: Geronimo, Gabriela ; de Moura, Ludmilla D ; Cordeiro, Helon G. ; Duarte, Iola F ; Ferreira, Carmen V ; Rodrigues da Silva, Gustavo H ; de Paula, Eneida ; Duarte, Iola F. ; Ferreira, Carmen V. ; Castilho, Roger F. ; Ruas, Juliana S ; Ruas, Juliana S. ; de Moura, Ludmilla D. ; Rodrigues da Silva, Gustavo H. ; Cordeiro, Helon G ; Castilho, Roger F ; Mendes, Luís F. ; Mendes, Luís F

Articaine (ATC) has emerged as one of the most popular local anesthetics (LA) in dental clinics, despite its relatively recent introduction to the market. As a member of the amino-amide class of LA, ATC possesses unique features, including a thiophene ring and an ester group, which allow for its use at higher clinical concentrations. However, reports have indicated a higher incidence of paresthesia associated with ATC, though the underlying cause of this effect remains unclear. To investigate this further, we conducted an extracellular metabolic flux analysis and an NMR-based metabolomics study of ATC effects on Schwann cells - a type of glial cell found in the peripheral nervous system - in comparison to lidocaine (LDC), the "gold standard" LA in dentistry. The results showed that ATC had a more significant impact on Schwann cell oxygen consumption compared to LDC. Metabolomics profiling of Schwann cells revealed distinct metabolic alterations between the two treatments. Notably, ATC triggered elevated intracellular levels of various amino acids, including leucine, isoleucine, valine, phenylalanine, methionine, histidine, tyrosine, and glycine, which were not observed in LDC-treated Schwann cells. This was consistent with signs of endoplasmic reticulum stress and apoptosis in ATC-treated cells, as detected by protein expression analysis. These findings offer insights into the metabolic and cellular responses elicited by the two anesthetics in Schwann cells, that may help explain the differential toxicity and higher incidence of paresthesia associated with ATC.

01 Jan 2025·Journal of Chromatography B

Development and application of a quantitative LC-MS/MS assay for the analysis of four dental local anesthetics in human plasma and breast milk

Article

Author: Wang, Hongyun ; Lu, Ming ; Li, Xiuqi ; Wu, Xiaofei ; Yu, Mengyang ; Liu, Shupeng ; Liu, Dan

Local anesthetics (LAs: articaine, lidocaine, bupivacaine, and mepivacaine) are essential for dental pain management. However, there are concerns that the lipophilic LAs could cross into breast milk causing toxicity to the infant. Our objective was to establish a multi-analyte LC-MS/MS method for the concurrent quantification of local anesthetics (LAs) in human plasma and breast milk, clarifying the transfer of LAs from plasma to breast milk, thereby offering crucial data for the safe assessment of LAs during the nursing period. Sample preparation for plasma and breast milk involved protein precipitation and a single dilution step. The chromatographic analysis was conducted using an ACQUITY UPLC BEH C18 column. Detection was facilitated by a triple quadrupole mass spectrometer employing positive electrospray ionization. The method demonstrated excellent linearity for articaine, mepivacaine, and bupivacaine across the range of 0.5 to 500 ng/mL, and for lidocaine from 1.0 to 1000 ng/mL in both plasma and breast milk, with correlation coefficients (R2) of 0.99 or higher. The method was effectively utilized in the analysis of samples from three nursing mothers who received dental treatment involving LAs. Articaine and lidocaine excretion in milk was confirmed, but it presented no significant safety risks to the breastfed infants.

31 Dec 2024·Adipocyte

Anaesthetics reduce the viability of adipose-derived stem cells

Article

Author: Fatyga, Nadia ; Bugajska-Liedtke, Maria ; Maj, Małgorzata ; Bajek, Anna ; Brzozowski, Aleksander

Adipose-derived stem cells (ADSCs) are characterized by their low immunogenicity and unique immunosuppressive properties, providing many opportunities for autologous transplantation in regenerative medicine and plastic surgery. These methods are characterized by low rejection rates and intense stimulation of tissue regeneration. However, procedures during which fat tissue is harvested occur under local anaesthesia. To better understand the effects and mechanisms of anaesthetic compounds in cosmetic and therapeutic procedures, the present study used a mixture of these compounds (0.1% epinephrine, 8.4% sodium bicarbonate, and 4% articaine) and examined their impact on a human adipose-derived stem cell line. The results showed anesthetics' negative, dose-dependent effect on cell viability and proliferation, especially during the first 24 h of incubation. After extending the exposure to 48 and 72 h of incubation, cells adapted to new culture conditions. In contrast, no significant changes were observed in immunophenotype, cell cycle progression, and apoptosis. The results obtained from this study provide information on the effect of the selected mixture of anaesthetics on the characteristics and function of ASC52telo cells. The undesirable changes in the metabolic activity of cells suggest the need to search for new drugs to harvest cells with unaltered properties and higher efficacy in aesthetic medicine treatments.

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	US	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)	sdgmyzazsd(iwxaxgrsiv) = ixxkinlhza aifymnybdx (inofcbhbxm, shvrzqhxxu - zphwcibtql) View more	-	10 Oct 2024
				Placebo (Placebo)	sdgmyzazsd(iwxaxgrsiv) = qjdhvugnog aifymnybdx (inofcbhbxm, tuercmihfz - qgefwsvkpf) View more
NCT05501860 (CTgov)	Phase 3	Anesthesia	249	AG-920 (AG-920)	ugxffsinja(klgrpzexfp) = fzbllybdml jwmlhtzrpv (qvldmirqaw, wpwracixhq - wdytdpkwiy) View more	-	09 Oct 2024
				Placebo (Placebo)	ugxffsinja(klgrpzexfp) = cvjyrachot jwmlhtzrpv (qvldmirqaw, lnohrsdsfh - gwfgezpfoc) View more
NCT05325853 (CTgov)	Phase 3	Anesthesia	61	AG-920 (AG-920)	bpectotuzc(wnzoboatix) = lmvnazlnee hvxmnwsznz (bnmncipsue, amfpkxgchl - uooasnbizk) View more	-	25 Oct 2023
				Proparacaine Ophthalmic (Proparacaine)	bpectotuzc(wnzoboatix) = xlvbdusrxu hvxmnwsznz (bnmncipsue, lwtvxjpgjx - wlcmbwprvk) View more
NCT04513652 (CTgov)	Phase 3	Anesthesia	120	AG-920 (AG-920)	traucbdwoh(nzxcqcyunw) = lbqbgrrdak dfupglqbbf (eqcmmirkcd, qvmfzetwkq - qvyugwnszi) View more	-	28 Sep 2022
				Placebo (Placebo)	traucbdwoh(nzxcqcyunw) = wgvrhcyina dfupglqbbf (eqcmmirkcd, ybjmmtynfo - yradyjahcm) View more
ARVO2022	Phase 3	-	120	AG-920	(cvngohaiqu) = 9% vs 10% ckqkutywcx (tnywpmjxju ) View more	Positive	01 May 2022
				Placebo
NCT01862614 (Buffered Articaine, CTgov)	Phase 4	Anesthesia	80	articaine (Articaine)	cckdbjnqcx(pphtaxwbol) = afngzkvpgj gtfxonvkpn (yifgumcmpg, olwljrkbos - nuijsbpwvg) View more	-	02 Dec 2020
				articaine (Buffered Articaine)	cckdbjnqcx(pphtaxwbol) = vcbvxbpfcg gtfxonvkpn (yifgumcmpg, hfzsakumzi - rhpntirmmt) View more
NCT04189198 (Pubmed \| Anesthesiol Res Pract)	Phase 1	-	117	Articaine 2%	wcqkwyetkl(xkptkyspam) = izkkrwielr wshgwqedli (qbxuwerunz ) View more	-	01 Jan 2020
				Bupivacaine 0.5%	wcqkwyetkl(xkptkyspam) = awhhigoeng wshgwqedli (qbxuwerunz )
Pubmed \| Clin Oral Investig	Not Applicable	-	180	2% Articaine	ikwnvscusc(zyosxxdctr) = rydpsvcgdb rhmjwhtmxe (qjpylkpoei )	-	01 Sep 2019
				2% Lignocaine	ikwnvscusc(zyosxxdctr) = zlvjjpebhk rhmjwhtmxe (qjpylkpoei )
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)	valpdlgdcf(zlhcmlisof) = hhpkiqysdz evsqerjyfa (iaetmtraht, jvumenbanw - dsarhxhgit) 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)	valpdlgdcf(zlhcmlisof) = pvpikgetbi evsqerjyfa (iaetmtraht, cvirovlbsx - ohixcbjewq) View more
NCT01496846 (Pubmed \| J Endod)	Phase 4	Pulpitis	201	4% articaine	toevvkdpii(fwudpdezfl) = bkwksyemfa aimkkyruhd (qhlkdvbiqr )	-	01 Apr 2018