Arocaine-A DC4%+0.001%

Arocaine-A DC is an amide-type local anesthetic combined with a vasoconstrictor, indicated for producing local, infiltrative, or conductive (nerve block) anesthesia in dental and periodontal procedures.

Established / Approved Uses

• Local infiltration anesthesia for routine and complex dental procedures (e.g. restorative work, extractions) in adults and children aged 4 years and older.
• Conductive (nerve block) anesthesia for dental and periodontal surgical procedures.

Use Not Established

Arocaine-A DC is intended strictly for dental/oral procedures. It is not indicated for use outside this dental/oral clinical context (e.g. general surgical or obstetric regional anesthesia), and safety and effectiveness for such uses have not been established.

Each mL of the injectable dental anesthetic solution typically contains:

• Articaine Hydrochloride 40 mg (4% w/v)
• Epinephrine (as epinephrine bitartrate), commonly available in strengths of 1:100,000 or 1:200,000

Articaine Hydrochloride + Epinephrine is supplied as a sterile injectable solution, usually in single-use dental cartridges, for submucosal or nerve-block injection by a dental professional.

Arocaine-A DC is a fixed-dose combination of articaine, an amide-type local anesthetic, and epinephrine, a vasoconstrictor. Articaine reversibly blocks nerve conduction to produce loss of sensation in a localized area, while epinephrine constricts local blood vessels, which slows systemic absorption of articaine, prolongs the duration of anesthesia, and helps reduce bleeding at the treatment site.

Arocaine-A DC is used exclusively by dental and oral healthcare professionals to provide anesthesia during dental and periodontal procedures.

Amide-type local anesthetic in fixed-dose combination with a vasoconstrictor (adrenergic agonist); Arocaine-A DC belongs to the dental local anesthetic drug class.

Mechanism of Action

The articaine component of Articaine Hydrochloride + Epinephrine reversibly blocks voltage-gated sodium channels in neuronal membranes, raising the electrical excitation threshold and slowing impulse propagation, which progressively prevents generation and conduction of nerve impulses in the area of administration.

The epinephrine component acts on vascular alpha-adrenergic receptors, producing local vasoconstriction. This reduces the rate of vascular absorption of articaine, prolongs contact of the anesthetic with nerve fibers, increases the depth and duration of anesthesia, and reduces local bleeding.

Onset and Duration

Following submucosal infiltration, anesthesia with Articaine Hydrochloride + Epinephrine typically has an onset of approximately 1 to 6 minutes, with a duration of pulpal anesthesia of around 45 to 60 minutes and soft-tissue anesthesia lasting longer.

Pharmacokinetics

Articaine is unique among amide anesthetics in containing an additional ester side chain, allowing it to be metabolized primarily by plasma esterases to articainic acid (an inactive metabolite), with only a minor pathway via hepatic microsomal enzymes. Elimination is mainly renal.

Arocaine-A DC is administered only by, or under the direct supervision of, a qualified dental or oral healthcare professional, by submucosal infiltration or regional nerve block injection in the oral cavity.

• Aspirate carefully before injection to reduce the risk of inadvertent intravascular injection.
• Inject slowly to reduce the risk of high systemic (plasma) levels and associated systemic toxicity.
• Resuscitative equipment, oxygen, and other emergency medications/personnel should be immediately available whenever Arocaine-A DC is administered.
• Not intended for intravenous administration.

Clinically significant interactions with Arocaine-A DC relate mainly to its epinephrine component:

• Monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants: Concomitant use with the epinephrine in Arocaine-A DC may result in severe, prolonged hypertension due to potentiated pressor response.
• Non-selective beta-blockers (e.g. propranolol): May lead to unopposed alpha-adrenergic effects of epinephrine, causing significant hypertension and reflex bradycardia.
• Other sympathomimetic agents and vasopressors: Additive cardiovascular (pressor) effects are possible when combined with the epinephrine component.
• Other agents capable of inducing methemoglobinemia (e.g. certain sulfonamides, nitrates, phenytoin): may increase the risk of methemoglobinemia when combined with articaine (see Precautions and Warnings).

Side effects reported with Arocaine-A DC include:

Common

• Injection-site pain
• Headache
• Facial/perioral edema
• Paresthesia (transient numbness/tingling)

Less Common

• Dizziness, nausea
• Syncope (vasovagal episode)
• Transient facial nerve palsy (e.g. eyelid drooping, due to spread of anesthetic near the facial nerve)
• Palpitations, tachycardia, or elevated blood pressure related to the epinephrine component

Rare but Serious

• Methemoglobinemia (see Precautions and Warnings)
• Prolonged paresthesia or nerve injury, reported numerically more often with articaine-containing inferior alveolar nerve blocks in some studies
• Systemic toxicity (central nervous system and cardiovascular) from inadvertent intravascular injection or excessive dose
• Allergic/anaphylactic reactions, particularly in sulfite-sensitive individuals

Pregnancy: Arocaine-A DC has been assigned to Pregnancy Category C. Animal reproduction studies have not shown evidence of embryofetal harm at recommended doses, but adequate and well-controlled studies in pregnant women are lacking. Arocaine-A DC should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, and only after consultation with a physician.

Lactation: It is not known whether articaine or epinephrine is excreted in human breast milk. Caution should be exercised, and Arocaine-A DC should be used in nursing mothers only if clearly needed, in consultation with a physician.

The following precautions apply to the use of Arocaine-A DC:

• Cardiovascular effects: The epinephrine component can cause tachycardia, palpitations, and elevated blood pressure. Use with caution in patients with cardiovascular disease, hypertension, hyperthyroidism, or significant uncontrolled cardiac arrhythmias, and in those taking interacting drugs such as non-selective beta-blockers or MAOIs (see Interactions).
• Methemoglobinemia: Articaine carries a recognized, dose-related risk of methemoglobinemia, particularly with higher doses or in patients with predisposing conditions such as G6PD deficiency or congenital methemoglobinemia. Seek prompt medical attention if signs such as cyanosis (bluish discoloration of skin/lips) or unusual fatigue/shortness of breath occur.
• Intravascular injection: Aspirate before injecting, per standard dental anesthetic technique, to reduce the risk of inadvertent intravascular injection and systemic (local anesthetic) toxicity.
• Maximum dose limits: Weight-based maximum dose limits should always be observed to avoid local anesthetic systemic toxicity (LAST) (see Dosage).
• Injection into inflamed or infected tissue: Should generally be avoided, as anesthetic efficacy may be reduced and there is added injection-site risk.
• Nerve injury/paresthesia: A numerically higher rate of paresthesia has been reported with articaine in some studies of inferior alveolar nerve blocks specifically, compared with some other local anesthetics; this remains an area of ongoing clinical discussion, and technique-appropriate use is advised.
• Scope of use: Arocaine-A DC is intended for dental/oral procedures only and should not be used outside this clinical context without appropriate justification.
• Resuscitative equipment and trained personnel should be readily available whenever Arocaine-A DC is administered.

Overdose or inadvertent intravascular injection of Arocaine-A DC can produce systemic toxicity, with early signs such as circumoral numbness, tinnitus, dizziness, and restlessness, potentially progressing to seizures/convulsions, followed by central nervous system or cardiorespiratory depression, hypotension, cardiac arrhythmias, and, rarely, cardiac arrest. Excess epinephrine absorption can additionally cause marked tachycardia, palpitations, and hypertension.

If overdose or systemic toxicity is suspected, seek immediate medical attention or contact emergency services/poison control right away. Management is supportive and should be provided by trained medical personnel, and may include airway maintenance, assisted ventilation with oxygen, circulatory support, and anticonvulsant therapy; cardiopulmonary resuscitation should be instituted if needed. Do not attempt to manage a suspected overdose at home.

Arocaine-A DC should be stored at controlled room temperature (approximately 15°C to 30°C, ideally around 25°C), protected from light, and should not be frozen. Keep out of reach of children. Do not use if the solution is discolored or contains particulate matter.

• Pediatric: Not recommended in children below 4 years of age; safety and effectiveness have not been established in this age group. In children 4 years and older, weight-based dosing with reduced volumes should be used (see Dosage).
• Geriatric: Reduced doses are recommended, commensurate with age and physical status; clinical experience has not shown major differences in overall safety between elderly and younger adult patients, though close monitoring is prudent.
• Hepatic impairment: Articaine is primarily metabolized by plasma esterases rather than hepatic enzymes, but caution is still advised in significant hepatic impairment; use the lowest effective dose.
• Renal impairment: Since elimination is mainly renal, caution and dose reduction should be considered in patients with significant renal impairment.
• Cardiovascular disease: Use with caution due to the epinephrine component (see Precautions and Warnings).
• Pregnancy and lactation: See Pregnancy and Lactation section.

Arocaine-A DC is intended for single-procedure (single-visit) dental use, not for ongoing or repeated daily treatment. The amount and number of injections given during one dental appointment should not exceed the maximum weight-based dose (see Dosage), regardless of the length of the procedure. Re-administration during a later, separate dental visit should again follow the same weight-based dosing limits.

Articaine Hydrochloride + Epinephrine belongs to the amide local anesthetic class combined with a vasoconstrictor (sympathomimetic/adrenergic agonist); it is classified as a dental local anesthetic combination product.

Articaine Hydrochloride + Epinephrine combines two complementary mechanisms: articaine reversibly binds to and blocks voltage-gated sodium channels along nerve fiber membranes, preventing the influx of sodium ions required to generate and propagate action potentials, thereby producing localized, reversible loss of sensation. Epinephrine, acting on local vascular alpha-adrenergic receptors, produces vasoconstriction that slows systemic absorption of articaine from the injection site, extends the duration of anesthesia, deepens the anesthetic effect, and reduces local surgical-site bleeding.

C

Arocaine-A DC is not recommended for use in children below 4 years of age, as safety and effectiveness have not been established in this population. In children aged 4 years and older, Arocaine-A DC may be used for dental local/infiltration or nerve-block anesthesia, with the dose calculated on a weight basis and not exceeding 7 mg/kg (0.175 mL/kg) of body weight; smaller volumes and reduced concentrations should be used for younger or lighter children, and administration should be limited to trained dental professionals experienced in pediatric dosing.