Arocaine-A DC

• Local anesthesia for dental procedures:
• Used for infiltration and nerve block anesthesia in dental surgeries, including tooth extractions, restorations, root canal treatments, and periodontal procedures.
• Suitable for adult and pediatric patients requiring short to intermediate duration anesthesia.
• Soft tissue anesthesia:
• Provides profound analgesia of soft tissues (gingiva, mucosa) in dental interventions.
• Off-label uses:
• Occasionally used in minor oral maxillofacial surgeries requiring local anesthesia.
• Used in some ENT and dermatological procedures involving localized anesthesia.

• Adults:
• Typical concentration: Articaine 4% with Epinephrine 1:100,000 or 1:200,000.
• Dose range: Up to 7 mg/kg of articaine; maximum recommended dose approximately 500 mg per session.
• Volume per injection varies with procedure; usually 1.5–3.6 mL per nerve block or infiltration.
• Epinephrine limits depend on patient cardiovascular status; generally up to 0.2 mg per appointment.
• Pediatrics:
• Dose should be calculated based on body weight (maximum 7 mg/kg articaine).
• Careful dosing and monitoring essential.
• Elderly:
• May require dose reduction due to reduced metabolism and cardiovascular sensitivity.
• Administration:
• Injected via dental syringe as infiltration or nerve block (e.g., inferior alveolar nerve block).
• Aspirate prior to injection to avoid intravascular administration.
• Repeat dosing possible with careful cumulative dose monitoring.

Articaine hydrochloride is an amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, preventing the initiation and propagation of nerve impulses. This blockade inhibits depolarization and transmission of pain signals, producing local anesthesia. Epinephrine bitartrate acts as a vasoconstrictor, constricting blood vessels at the injection site. This prolongs the anesthetic effect by reducing systemic absorption of articaine, decreases bleeding during procedures, and limits systemic toxicity.

• Absorption:
• Rapidly absorbed after local injection; absorption rate is reduced by epinephrine-induced vasoconstriction.
• Distribution:
• Widely distributed; articaine has a large volume of distribution due to lipid solubility.
• Crosses the placenta and blood-brain barrier.
• Metabolism:
• Articaine is rapidly hydrolyzed by plasma esterases and liver enzymes to inactive metabolites.
• Has a unique thiophene ring and ester group, enhancing metabolism and reducing systemic toxicity.
• Elimination:
• Primarily renal excretion of metabolites.
• Half-life of articaine: approximately 20–40 minutes.
• Epinephrine:
• Metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO).
• Half-life: ~2 minutes.

• Pregnancy:
• Articaine is classified as FDA Pregnancy Category C. Use only if clearly needed and after risk-benefit assessment.
• Limited human data; animal studies show no clear teratogenicity but caution advised.
• Lactation:
• Unknown if articaine or epinephrine is excreted in human milk; likely minimal exposure.
• Use cautiously; avoid high doses or frequent administration in nursing mothers.

• Articaine: Local anesthetic (amide type)
• Epinephrine: Vasoconstrictor (adrenergic agonist)
• Combination: Local anesthetic with vasoconstrictor

• Known hypersensitivity to articaine, epinephrine, or other amide-type anesthetics
• Severe cardiovascular disease or uncontrolled hypertension (due to epinephrine)
• Patients taking non-selective beta-blockers, monoamine oxidase inhibitors (MAOIs), or tricyclic antidepressants without proper monitoring
• Local infection or inflammation at the injection site
• History of malignant hyperthermia (rare association)

• Use caution in patients with cardiovascular disease, hyperthyroidism, diabetes, or pheochromocytoma due to epinephrine effects.
• Monitor for signs of systemic toxicity (e.g., CNS excitation, seizures).
• Avoid intravascular injection by aspiration prior to administration.
• Epinephrine can cause increased heart rate, blood pressure, and arrhythmias; monitor vital signs in high-risk patients.
• Caution in elderly or debilitated patients due to slower metabolism.
• Rare risk of methemoglobinemia; consider if cyanosis develops without respiratory cause.

Common Adverse Effects:

• Localized pain or burning on injection
• Mild swelling or redness at injection site
• Temporary numbness or paresthesia lasting beyond expected duration

Serious/Rare Adverse Effects:

• Allergic reactions (rash, anaphylaxis)
• CNS toxicity: dizziness, tremors, seizures (rare)
• Cardiovascular reactions: tachycardia, hypertension, arrhythmia
• Prolonged anesthesia or nerve damage (rare)
• Methemoglobinemia (rare)

• MAO Inhibitors and Tricyclic Antidepressants: Increased risk of hypertensive crisis with epinephrine.
• Non-selective Beta-Blockers: Enhanced hypertensive and bradycardic effects due to epinephrine.
• Other Vasoconstrictors: Additive cardiovascular effects.
• CYP450 Metabolized Drugs: Articaine metabolism minimally affected; no significant interactions.
• Alcohol: No significant interaction.

• Recent dental guidelines recommend using articaine with epinephrine cautiously in patients with cardiovascular comorbidities.
• Emphasis on aspiration technique to avoid intravascular injection and systemic toxicity.
• Monitoring cumulative dose is crucial to prevent overdose, especially in lengthy procedures.

• Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C.
• Protect from light and freezing.
• Keep in original packaging until use.
• Use immediately after opening; discard any unused portion.
• No reconstitution needed; supplied as ready-to-use solution.