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NERVOUS SYSTEM › ANESTHETICS › ANESTHETICS, LOCAL › Amides
combinations
N01BB20
Forms & Strengths
- Injectable solution: Lidocaine HCl + Epinephrine (various concentrations, e.g., 1% + 1:100,000)
- Topical preparations: Lidocaine + Prilocaine cream (2.5% / 2.5%)
- Dental cartridges: Articaine HCl 4% + Epinephrine 1:100,000 or 1:200,000
- Topical sprays/gels: Benzocaine + Tetracaine combinations
Adult Dosing
- Infiltration/Local Anesthesia (Lidocaine/Epinephrine): Max 7 mg/kg with epinephrine, not to exceed 500 mg total dose
- Topical Anesthesia (Lidocaine/Prilocaine): Apply 1 to 2 g of cream per 10 cm2 of skin for at least 60 minutes
- Dental Anesthesia (Articaine/Epinephrine): 1.7 to 3.4 mL (68 to 136 mg articaine) for routine procedures; max 7 mg/kg
Pediatric Dosing
- Local Infiltration (Lidocaine/Epinephrine): Do not exceed 4.5 to 7 mg/kg based on formulation and patient weight
- Topical Anesthesia (Lidocaine/Prilocaine): Dosing varies by age and weight; neonates 0-3 months max 1 g / 10 cm2 applied for 1 hour
- Dental Anesthesia (Articaine/Epinephrine): Children >4 years, 1.7 mg/kg to max 5 mg/kg depending on age and weight
Indications
- Local, regional, or spinal anesthesia for surgical procedures
- Dental anesthesia for routine and complex procedures
- Surface anesthesia of intact skin or mucous membranes prior to minor dermal procedures
- Symptomatic relief of local pruritus or pain
Mechanism of Action
- Local anesthetics block fast voltage-gated sodium channels in the neuronal cell membrane, inhibiting depolarization and nerve impulse propagation
- Vasoconstrictors (e.g., epinephrine) constrict local blood vessels, reducing systemic absorption, prolonging local anesthetic duration, and minimizing bleeding
Contraindications
- Hypersensitivity to amide- or ester-type local anesthetics or any component of the formulation
- Presence of severe inflammation or sepsis at the injection site
- Idiopathic or congenital methemoglobinemia (for prilocaine-containing combinations)
- Severe conduction disturbances or cardiogenic shock (when systemic absorption is significant)
Adverse Reactions
- Central nervous system effects: Tinnitus, dizziness, apprehension, lightheadedness, tremors, seizures
- Cardiovascular effects: Hypotension, bradycardia, myocardial depression, arrhythmias
- Local reactions: Edema, burning sensation, tenderness, prolonged numbness
- Hematological: Methemoglobinemia associated with high doses of prilocaine or benzocaine
Drug Interactions
- Class I antiarrhythmic drugs (e.g., mexiletine): Additive toxic effects on cardiac conduction
- Non-selective beta-blockers: Risk of severe hypertension and bradycardia due to unopposed alpha-adrenergic vasoconstriction from epinephrine
- Monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants: Enhanced pressor response to vasopressors, precipitating severe hypertension
- Drugs associated with methemoglobinemia (e.g., sulfonamides, acetaminophen): Increased risk of methemoglobin formation when combined with prilocaine or benzocaine
Curated Content: Needs Vetting Before Put to Clinical Use