[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/) › Articaine # Articaine ## Local anesthetics? Local anesthetics Dental amide local anaesthetic with an ester side chain, so plasma esterases end its action quickly. Given with epinephrine. Updated Nov 1, 2026 Also called: Articaine hydrochloride, Carticaine ## Quick facts **Group** [Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/) **Target** Voltage-gated sodium channels (Nav) **Used for** Local **Key effects** Pain at the injection site and headache · Palpitations **Monitor** Heart rate · Early signs of toxicity **ATC** N01BB08 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ⇅**Voltage-gated sodium channels (Nav)**Articaine ⓘ There is no structure with articaine. The figure shows levobupivacaine, another amide local anaesthetic, in the inner pore of the human Nav1.7 sodium channel. **Target in 3D:** Voltage-gated sodium channels (Nav). PDB structure 8I5B (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8I5B) · Drag to rotate · pinch to zoom Articaine blocks voltage-gated sodium channels from inside the nerve, like other local anaesthetics, so the pain signal is not conducted. It is classed as an amide, but it has a thiophene ring and also carries an ester group: plasma carboxylesterases hydrolyse that ester to inactive articainic acid, so its action and systemic exposure end relatively fast. It is marketed with epinephrine, which keeps it at the injection site and reduces bleeding. - Injected next to the dental nerve with epinephrine - Blocks the sodium channel: no pain signal - Plasma esterases hydrolyse its ester group - Inactive articainic acid: short systemic action ## Indications - Local, infiltrative or conductive anaesthesia for simple and complex dental procedures in adults and children from four years of age ## Adverse effects ### Common - Pain at the injection site and headache - Persistent numbness or tingling of lips, tongue or mouth - Palpitations - Symptoms of systemic toxicity with high levels ### Serious (rare, important) - Accidental intravascular injection: seizures, coma and respiratory arrest - Persistent paraesthesia after mandibular nerve block, with slow or incomplete recovery - Methaemoglobinaemia - Allergic-type reactions to the sulfite in the epinephrine solution, including asthma attacks ## Contraindications - Hypersensitivity to sulfites (the epinephrine solution contains a sulfite) - Hypersensitivity to amide-type local anaesthetics ## Key interactions **MAO inhibitors, non-selective beta-blockers and tricyclic antidepressants** The epinephrine in the solution may cause severe, prolonged hypertension. **Phenothiazines and butyrophenones** May reduce or reverse the pressor effect of epinephrine. **Drugs that cause methaemoglobinaemia** Higher risk of methaemoglobinaemia. ## What is monitored - Heart rate, blood pressure, breathing and consciousness after each injection - Early signs of toxicity: restlessness, tinnitus, metallic taste, perioral numbness - Colour of skin and lips (methaemoglobinaemia) ## Administration and safety - Intraoral submucosal infiltration or nerve block only; aspirate before injecting and inject slowly. - Oxygen, resuscitation drugs and equipment are kept available. - Two epinephrine strengths exist: the weaker one is preferred for routine procedures. - Cartridges with cloudy or discoloured solution are discarded. ## Pregnancy and breastfeeding Animal studies suggest possible fetal harm. Caution is advised in breastfeeding. ## Nursing care - Ask about sulfite or local anaesthetic allergy, asthma, heart disease and MAO inhibitors, beta-blockers or tricyclics. - Warn about biting the lips, tongue or cheek until sensation returns. - Report numbness that lasts beyond the expected time. - In children, check the planned amount against weight before the injection. ## Pharmacokinetics **Metabolism** Mainly by plasma carboxylesterase to inactive articainic acid; a small share by liver CYP enzymes. **Elimination** Kidney, mostly as articainic acid. **Half-life** Less than an hour. **Onset and duration** Rapid. ## Memory aid ARTIcaine: «Amide + esteR, Thiophene Inside»: an amide that plasma esterases switch off fast. ## Test yourself Think of the answer, then tap the question to see it. ## Why does articaine have a short systemic action although it is an amide? It also contains an ester group that plasma carboxylesterases hydrolyse to inactive articainic acid. ## Which allergy contraindicates articaine with epinephrine? Sulfite hypersensitivity, because the epinephrine solution contains a sulfite. ## Which nerve complication has been reported after mandibular blocks with articaine? Persistent paraesthesia of lips, tongue and oral tissues, with slow, incomplete or no recovery. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/articaine/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## Connections ## Related drugs 3 - [Lidocaine](https://durgical.com/en/pharmacology/lidocaine/) - [Prilocaine](https://durgical.com/en/pharmacology/prilocaine/) - [Mepivacaine](https://durgical.com/en/pharmacology/mepivacaine/) [← Back to the class: Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [DailyMed - ARTICAINE HYDROCHLORIDE AND EPINEPHRINE injection, solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=636cbf11-819c-48f8-915d-ac5fb38bd352) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N01BB08) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/articaine/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/articaine/