Articaine and epinephrine

Name: Articaine and epinephrine

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of methemoglobinemia like a blue or gray color of the lips, nails, or skin; a heartbeat that does not feel normal; seizures; very bad dizziness or passing out; very bad headache; feeling very sleepy; feeling tired or weak; or shortness of breath.
  • Feeling confused.
  • Chest pain.
  • Restlessness.
  • Anxiety.
  • Ringing in ears.
  • Dizziness.
  • Blurred eyesight.
  • Shakiness.
  • Low mood (depression).
  • Feeling sleepy.

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Injection, solution [for dental use]:

Articadent: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:100,000 (1.7 mL) [contains sodium metabisulfite]

Articadent: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:200,000 (1.7 mL) [contains sodium metabisulfite]

Orabloc: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:100,000 (1.8 mL) [contains sodium metabisulfite]

Orabloc: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:200,000 (1.8 mL) [contains sodium metabisulfite]

Septocaine with epinephrine 1:100,000: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:100,000 (1.7 mL) [contains sodium metabisulfite]

Septocaine with epinephrine 1:200,000: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:200,000 (1.7 mL) [contains sodium metabisulfite]

Zorcaine: Articaine hydrochloride 4% [40 mg/mL] and epinephrine 1:100,000 (1.7 mL) [contains sodium metabisulfite]

Pharmacologic Category

  • Local Anesthetic

Pharmacology

Articaine: Blocks both the initiation and conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.

Epinephrine: Increases the duration of action of articaine by causing vasoconstriction (via alpha effects) which slows the vascular absorption of articaine.

Distribution

Articaine: ~60% to 80%, bound to albumin and gamma globulins.

Metabolism

Articaine: Hepatic via plasma carboxyesterase to articainic acid (inactive)

Excretion

Urine (primarily as metabolites)

Onset of Action

1 to 9 minutes

Time to Peak

Articaine: ~25 minutes (single dose); 48 minutes (3 doses)

Contraindications

Sulfite hypersensitivity.

Documentation of allergenic cross-reactivity for local anesthetics is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosing Pediatric

Dental anesthesia: Submucosal infiltration and/or nerve block: Articaine 4%/epinephrine: Children and Adolescents 4 to 16 years: Note: These dosages are guides only; other dosages may be used; however, do not exceed maximum recommended dose. The actual volumes to be used depend upon a number of factors, such as type and extent of surgical procedure, depth of anesthesia, degree of muscular relaxation, and condition of the patient. In all cases, the smallest dose that will produce the desired result should be given. For most routine dental procedures, epinephrine 1:200,000 is preferred; when more pronounced hemostasis or improved visualization of the surgical field are required, epinephrine 1:100,000 may be used. Dosages should be reduced for patients with cardiac disease and acutely ill and/or debilitated patients:

Simple procedures: 0.76 to 5.65 mg/kg of articaine; maximum dose of articaine: 7 mg/kg (0.175 mL/kg).

Complex procedures: 0.37 to 7 mg/kg of articaine; maximum dose of articaine: 7 mg/kg (0.175 mL/kg).

Dosing Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

For the Consumer

Applies to articaine / epinephrine: parenteral injection

Side effects include:

Pain, headache, facial edema, gingivitis, paresthesia, infection.

Dose Adjustments

Dosages should be reduced for patients with cardiac disease.

Dosages in pediatric patients should be reduced, commensurate with age, body weight, and physical condition.

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