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Articaine Hydrochloride

/

Epinephrine

Pronunciation: AR-ti-kane HYE-droe-KLOR-ide/EP-i-NEF-rin
Class: Local anesthetic, Vasoconstrictor

Trade Names

Orabloc
- Injection, solution articaine 4% with epinephrine 1:100,000 (0.018 mg/mL)
- Injection, solution articaine 4% with epinephrine 1:200,000 (0.009 mg/mL)

Pharmacology

Articaine

Stabilizes neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

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Epinephrine

Stimulates both alpha- and beta-receptors within sympathetic nervous system; relaxes smooth muscle of bronchi and iris and is an antagonist of histamine.

Indications and Usage

For local, infiltrative, or conductive anesthesia in both simple and complex dental procedures.

Contraindications

Hypersensitivity to products containing sulfites.

Dosage and Administration

Dental anesthesia
Adults

Submucosal infiltration/nerve block For infiltration, 0.5 to 2.5 mL (20 to 100 mg of articaine); for nerve block, 0.5 to 3.4 mL (20 to 136 mg of articaine); for oral surgery, 1 to 5.1 mL (40 to 204 mg of articaine). Max, 7 mg/kg (0.175 mL/kg) of articaine.

Children 4 y and older

Submucosal infiltration/nerve block / The quantity of articaine should be determined by the age and weight of the child and the magnitude of the operation. For simple procedures, 0.76 to 5.65 mg/kg (0.9 to 5.1 mL) of articaine was administered safely to 51 patients. For complex procedures, 0.37 to 7.48 mg/kg (0.7 to 3.9 mL) of articaine was administered safely to 10 patients. Max, 7 mg/kg (0.175 mL/kg) of articaine.

Elderly

Dose reduction may be required.

General Advice

  • For submucosal infiltration or nerve block.
  • The smallest dose that will produce the desired result should be given.
  • Caution should be exercised when employing large volumes because the incidence of adverse effects may be dose-related.
  • For most routine dental procedures, articaine containing epinephrine 1:200,000 is preferred. However, when more pronounced hemostasis or improved visualization of the surgical field is required, articaine containing epinephrine 1:100,000 may be used.
  • For chemical disinfection of the carpule, either isopropyl alcohol (91%) or ethyl alcohol (70%) is recommended. Many commercially available brands of isopropyl (rubbing) alcohol, as well as solutions of ethyl alcohol not of USP grade, contain denaturants that are injurious to rubber and therefore are not to be used.
  • Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Storage/Stability

Store at 77°F, with brief excursions permitted between 59° and 86°F. Protect from light. Do not freeze.

Drug Interactions

Butyrophenones (eg, haloperidol) and phenothiazines (eg, thioridazine)

The pressor effects of epinephrine, which is present in articaine intraoral injection, may be reduced or reversed. Concomitant use should generally be avoided. If concurrent use cannot be avoided, carefully monitor the patient.

Monoamine oxidase inhibitors (eg, phenelzine), nonselective beta-adrenergic blockers (eg, propranolol), or tricyclic antidepressants (eg, amitriptyline)

Because articaine intraoral injection contains epinephrine, the risk of severe, prolonged hypertension may be increased. Concomitant use should generally be avoided. If concurrent use cannot be avoided, carefully monitor the patient.

Adverse Reactions

CNS

Headache (5%); numbness and tingling, paresthesia, sleepiness (1%); hypoesthesia, persistent paresthesia of the lips, tongue, and oral tissues (postmarketing).

EENT

Ear symptoms (eg, earache, otitis media) (1%); paralysis of ocular muscles (eg, diplopia, mydriasis, ptosis, difficulty in abduction of the affected eyes) (postmarketing).

GI

Nausea and emesis (2%); gingivitis (1%).

Local

Ischemic injury and necrosis (postmarketing).

Miscellaneous

Pain (13%); swelling (3%); trismus (2%); cough, face edema, infection, palpitation (1%).

Precautions

Monitor

Constant and careful monitoring of CV and respiratory (adequacy of ventilation) vital signs and the patient's state of consciousness should be performed after each injection.


Pregnancy

Category C .

Lactation

Undetermined. Breast-feeding women may choose to pump and discard breast milk for approximately 4 hours following an injection of articaine and then resume breast-feeding.

Children

Safety and effectiveness in pediatric patients younger than 4 years have not been established.

Elderly

Give reduced doses to commensurate with their age and physical condition.

Hepatic Function

Use with caution in patients with severe hepatic disease.

Special Risk Patients

Use with caution in patients with heart block, impaired CV function, peripheral vascular disease, hypertensive vascular disease, or acute illness, and in debilitated patients.

Sulfite Sensitivity

Use caution in sulfite-sensitive patients.

Intravascular injection

Accidental intravascular injection may be associated with convulsions, followed by CNS or cardiorespiratory depression and coma, progressing to respiratory arrest. To avoid accidental intravascular administration, preform aspiration before injection.

Methemoglobinemia

May cause methemoglobinemia; do not use in patients with congenital or idiopathic methemoglobinemia or in patients who are receiving treatment with methemoglobin-inducing agents.

Systemic toxicity

Small doses of local anesthetics injected in dental blocks may produce adverse reactions similar to systemic toxicity (eg, confusion, convulsions, respiratory depression, and/or respiratory arrest) seen with unintentional intravascular injections of larger doses.

Toxic reactions

Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.

Vasoconstrictor toxicity

May exhibit exaggerated vasoconstrictor response and ischemic injury or necrosis may result.

Overdosage

Symptoms

Convulsions, CV depression (eg, hypoxia, acidosis, bradycardia, arrhythmias, and/or cardiac arrest).

Patient Information

  • Inform patients in advance of the possibility of temporary loss of sensation and muscle function.
  • Instruct patients not to eat or drink until normal sensation returns.

Copyright © 2009 Wolters Kluwer Health.

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