Articaine Hydrochloride

Intermediate-acting local anesthetic (amide type).1 2 3 4

Absorption

Bioavailability

Peak plasma concentrations achieved approximately 25 minutes following single dose and 48 minutes following 3 doses.1

Onset

1–6 minutes following submucosal injection.1 Average onset of anesthesia following articaine administration appears to be similar to that of prilocaine5 6 8 but slightly faster than that of other local anesthetics (e.g., lidocaine).3 5 8

Duration

Complete anesthesia lasts approximately 1 hour.1

Distribution

Plasma Protein Binding

Approximately 60–80% (albumin and γ-globulins).1

Elimination

Metabolism

Systemically absorbed articaine is rapidly metabolized by plasma carboxyesterase to articainic acid (inactive);1 approximately 5–10% of available articaine is metabolized to articainic acid by CYP enzymes.1 3

Elimination Route

Excreted principally in urine as inactive metabolites and small amounts (2%) of unchanged drug;1 4 approximately 53–57% of administered dose excreted within 24 hours following submucosal administration.1

Half-life

Approximately 1.8 hours.1

Storage

Parenteral

25°C (may be exposed to 15–30°C).1 Protect from light.1

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

May be incompatible with strong oxidizing agents.a

• Local anesthetics block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.1

• Formulated with epinephrine to decrease articaine’s rate and extent of systemic absorption and to prolong its duration of action.1 4

• Has intermediate duration of action (approximately 1 hour).1 2 3 4

• Prior to administration, advise patients of the possibility of temporary loss of sensation and muscle function following infiltration and nerve block injections.1

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease).1

• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1

• Importance of informing patients of other important precautionary information. (See Cautions.)