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
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.

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

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

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.

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)

Connections

← Back to the class: 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 (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.