articaine
Trade name: Septocaine
Approved
Apr 3, 2000
Articaine is a dental local anesthetic, which is the most widely used in a number of European countries and is available in many countries around the world. Articaine in combination with epinephrine under the brand name Septocaine is indicated for local, infiltrative, or conductive anesthesia in both simple and complex dental procedures. Local anesthetics block the generation and conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rising of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of the affected nerve fibers. Articaine blocks the actions on Na+ channels. Epinephrine is a vasoconstrictor added to articaine HCl to slow absorption into the general circulation and thus prolong maintenance of an active tissue concentration. — NCATS
Clinical trial activity
77 trials · 56 clinical orgs · 6 marketing orgs
Earliest trial started Nov 1, 2005 (NCT00247741)
Timeline
2000s
2010s
- Feb 26, 2010
Pierrel Research — NDA Secondary Org
- Jun 18, 2010
Hospira — Marketing Organization
- Jan 1, 2012
Earliest Phase 1 Sponsor(trial)
- Jul 11, 2017
HansaBioMed — Marketing Organization
- Jul 11, 2017
Lonza — Marketing Organization
- Jan 1, 2018
Earliest Phase 2 Sponsor(trial)
2020s
- Aug 15, 2025
Thea Pharma — Marketing Organization
Indications
Approved for
Studied for
- Abdominal Pain · Phase 4
- Anesthesia · Phase 4
- Anesthesia, Dental · Phase 4
- Anesthesia, Local · Phase 4
- Anesthesia, Spinal · Phase 3
- Anesthetics · Phase 4
- Aortic Valve Disease · Phase 4
- Behavior · Phase 1/Phase 2
- Child Behavior · Phase 3
- Cicatrix · Phase 4
- Contraception · Phase 4
- Dental Caries · Phase 3
- Dental Implantation · Phase 4
- Dental Pulp Diseases · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 4
- Dyspepsia · Phase 4
- Gastroscopy · Phase 4
- General Surgery · Phase 1
- Healthy Volunteers · Phase 1
- Heartburn · Phase 4
- Heart Septal Defects, Atrial · Phase 4
- Hematemesis · Phase 4
- Intrauterine Devices · Phase 4
- Mandibular Nerve Injuries · Phase 1
- Mitral Valve · Phase 4
- Myxoma · Phase 4
- Opioid-Related Disorders · Phase 4
- Pain · Phase 4
- Periapical Periodontitis · Phase 2
- Periodontitis · Phase 4
- Pharmacokinetics · Phase 4
- Postoperative Pain · Phase 4
- Pulpitis · Phase 4
- Renal Insufficiency · Early Phase 1
- Stomatognathic Diseases · Phase 3
- Tooth · Phase 4
- Tooth Abnormalities · Phase 4
- Tooth Extraction · Phase 4
Mechanism of action
- Sodium channel alpha subunitBLOCKER
Sodium channel alpha subunit blocker
- Sodium channel protein type 1 subunit alpha (SCN1A) ↗
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗
- Sodium channel protein type 7 subunit alpha (SCN7A) ↗
- Sodium channel protein type 2 subunit alpha (SCN2A) ↗
- Sodium channel protein type 9 subunit alpha (SCN9A) ↗
- Sodium channel protein type 3 subunit alpha (SCN3A) ↗
- Sodium channel protein type 11 subunit alpha (SCN11A) ↗
- Sodium channel protein type 8 subunit alpha (SCN8A) ↗
- Sodium channel protein type 10 subunit alpha (SCN10A) ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type VII alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
Combination products
septocaine
with epinephrine
Also known as orabloc, ultacan, ultacan forte
Approval history
- approvedApr 3, 2000
Chemistry & pharmacology
SMILES
CCCNC(C)C(=O)Nc1c(C)csc1C(=O)OC- Mol. weight
- 284.38 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL1093 ↗
- WikipediaArticaine ↗
- NCATSD3SQ406G9X ↗
- ChEMBLCHEMBL203266 ↗
- ChEMBLCHEMBL1200819 ↗
Also known as
- 40045
- 40 045
- articaine
- articaine
- articaine
- articaine
- articaine
- articaine
- articaine
- articaine
- articaine
- articaine hcl
- articaine hcl
- articaine hcl
- articaine hydrochloride
- articaine hydrochloride
- articaine hydrochloride
- carticaine
- carticaine
- carticaine
- hoe-045
- hoe-045
- septanest
- septanest
- septocaine
- septocaine
- septocaine
- ultracaine
- ultracaine
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07231614 | Phase 4 | Dec 20, 2025 | Universidad Austral de Chile |
| NCT07066306 | N/A | Jun 21, 2025 | Bezmialem University |
| NCT06980363 | Phase 1 | Jun 1, 2025 | Fayoum University |
| NCT06927726 | N/A | Jan 10, 2025 | Tanta University |
| NCT07145879 | N/A | Jan 1, 2025 | Pamukkale University |
| NCT06630819 | N/A | Nov 3, 2024 | Qassim University |
| NCT06461143 | N/A | Aug 21, 2024 | Istanbul University |
| NCT06423859 | N/A | Feb 1, 2024 | Benha University |
| NCT06538233 | Phase 2 | Jan 1, 2024 | Cleveland Dental Institute |
| NCT06564987 | Phase 1 | Jan 1, 2024 | Cleveland Dental Institute |
| NCT06119139 | N/A | Dec 31, 2023 | Cairo University |
| NCT06047366 | Phase 4 | Dec 5, 2023 | Indiana University, United States Army |
| NCT06161714 | Phase 4 | Nov 30, 2023 | Riyadh Elm University |
| NCT05908305 | Phase 4 | Jun 10, 2023 | University of Algiers |
| NCT05839548 | Phase 3 | Jun 1, 2023 | Qassim Health Cluster, Qassim University |
| NCT05944341 | N/A | Jun 1, 2023 | Minia University |
| NCT05840913 | Phase 2 | Apr 30, 2023 | Government of Pakistan |
| NCT06679660 | N/A | Feb 20, 2023 | Cukurova University |
| NCT05728151 | N/A | Feb 12, 2023 | Research Institute of Ophthalmology, Egypt |
| NCT06862570 | Phase 2 | Dec 19, 2022 | Pakistan Army |
Organizations
Research & Development (56)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cairo University | Academic/Hospital | 10 | 10 | 3 | 2014 |
| American Genomics, LLC | Academic/Hospital | 5 | 5 | 2 | 2020 |
| Minia University | Academic/Hospital | 3 | 3 | 2 | 2019 |
| Netherlands Institute for Pigment Disorders | Academic/Hospital | 3 | 3 | 1 | 2014 |
| University of Amsterdam | Academic/Hospital | 3 | 0 | 1 | 2014 |
| University of Helsinki | Academic/Hospital | 3 | 3 | 1 | 2009 |
| University of Sao Paulo | Academic/Hospital | 3 | 3 | 2 | 2010 |
| Virginia Commonwealth University | Academic/Hospital | 3 | 3 | 1 | 2019 |
| Ain Shams University | Academic/Hospital | 2 | 2 | 1 | 2019 |
| Cleveland Dental Institute | Academic/Hospital | 2 | 2 | 2 | 2024 |
| Fayoum University | Academic/Hospital | 2 | 2 | 2 | 2022 |
| Fundação de Amparo à Pesquisa do Estado de São Paulo | Academic/Hospital | 2 | 0 | 1 | 2010 |
| Qassim University | Academic/Hospital | 2 | 1 | 2 | 2023 |
| Taibah University | Academic/Hospital | 2 | 2 | 2 | 2017 |
| Tishreen University | Academic/Hospital | 2 | 2 | 1 | 2022 |
| University of Michigan | Academic/Hospital | 2 | 2 | 1 | 2011 |
| Ahl al-Bayt University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Altinbas University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| American Association of Endodontists | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Anfomed GmbH | For profit | 1 | 0 | 1 | 2017 |
Marketing (7)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Deproco | For profit | NDA2 | Apr 3, 2000 |
| Deproco | For profit | NDA | Apr 3, 2000 |
| HansaBioMed | For profit | MKTG | Jul 11, 2017 |
| Hospira | For profit | MKTG | Jun 18, 2010 |
| Lonza | For profit | MKTG | Jul 11, 2017 |
| Pierrel Research | For profit | NDA2 | Feb 26, 2010 |
| Thea Pharma | For profit | MKTG | Aug 15, 2025 |