ALPHACAINE HYDROCHLORIDE W/ EPINEPHRINE
Clinical safety rating: safe
Beta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
Lidocaine, an amide-type local anesthetic, stabilizes the neuronal membrane by inhibiting sodium ion influx, thereby blocking nerve impulse initiation and conduction. Epinephrine acts as a vasoconstrictor via alpha-1 adrenergic receptor agonism, reducing local blood flow and prolonging anesthetic effect.
| Metabolism | Lidocaine is primarily metabolized in the liver via CYP3A4 and CYP1A2 to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Epinephrine is metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). |
| Excretion | Primarily renal excretion of metabolites and unchanged drug; <5% excreted unchanged in urine. Biliary excretion accounts for a minor fraction. |
| Half-life | Alphacaine: 1.5-2 hours; epinephrine: 2-3 minutes. Clinical context: The duration of local anesthesia is prolonged by epinephrine-induced vasoconstriction, not by the half-life of alphacaine. |
| Protein binding | Alphacaine: 55-65% bound to alpha-1-acid glycoprotein; Epinephrine: minimal binding (15-20% to albumin). |
| Volume of Distribution | Alphacaine: 1.0-1.5 L/kg, indicating extensive tissue distribution; Epinephrine: 0.2-0.4 L/kg, reflecting rapid uptake into adrenergic tissues. |
| Bioavailability | Intravenous: 100%; Oral: negligible (high first-pass metabolism); Topical: variable (minimal systemic absorption); Local injection: essentially 100% at the site but systemic bioavailability is reduced by epinephrine. |
| Onset of Action | Infiltration: 2-5 minutes; Nerve block: 5-15 minutes; Epidural: 10-20 minutes. |
| Duration of Action | Infiltration without epinephrine: 0.5-1 hour; with epinephrine: 2-4 hours. Nerve block: 1-3 hours; Epidural: 1-2 hours. Note: Epinephrine prolongs duration by reducing vascular absorption. |
1-2 mL of 2% lidocaine (20-40 mg) with epinephrine 1:100,000 (0.01-0.02 mg epinephrine) injected locally; maximum single dose 7 mg/kg lidocaine (7 mL/kg of 0.1% solution equivalent).
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required; lidocaine clearance minimally affected by renal impairment. Epinephrine use with caution if severe renal impairment due to potential vasoconstrictor effects. |
| Liver impairment | Child-Pugh Class A: 60-80% of normal dose; Class B: 40-60% of normal dose; Class C: 20-40% of normal dose; reduce maximum single dose to 70% of standard in severe impairment. |
| Pediatric use | Weight-based: 1-2 mg/kg lidocaine with epinephrine 1:100,000 (0.009-0.018 mg/kg epinephrine) for local infiltration; maximum single dose 4.5 mg/kg lidocaine (0.045 mL/kg of 1% solution). |
| Geriatric use | Start with lowest effective dose (e.g., 0.5-1 mL of 2% lidocaine with epinephrine); reduce maximum single dose to 80% of adult maximum; monitor for cardiovascular effects of epinephrine. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Beta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
| FDA category | Animal |
| Breastfeeding | Lidocaine and epinephrine are excreted in breast milk in low amounts. Lidocaine M/P ratio ~0.5; epinephrine M/P ratio unknown. Infant dose via milk is ~1-2% of maternal weight-adjusted dose. Risk of neonatal bradycardia or irritability is low with standard doses. Use caution with high doses or repeated administration. |
| Teratogenic Risk |
■ FDA Black Box Warning
Not for use in obstetrical paracervical block anesthesia due to risk of fetal bradycardia and fetal death.
| Common Effects | cardiac arrest |
| Serious Effects |
["Hypersensitivity to amide-type anesthetics","Severe hypotension","Concurrent use of MAO inhibitors or tricyclic antidepressants (relative)","Shock","Avoid use in areas with poor blood supply"]
| Precautions | ["Risk of systemic toxicity including CNS and cardiac effects","Use with caution in patients with hepatic impairment or severe renal disease","Avoid inadvertent intravascular injection","Epinephrine may cause tachycardia, hypertension, and arrhythmias","Use minimum effective dose","Monitor for signs of methemoglobinemia"] |
| Food/Dietary | No significant food interactions. Avoid hot liquids or food until numbness resolves to prevent oral burns. |
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| Pregnancy category C. First trimester: Lidocaine crosses placenta; epinephrine may reduce uterine blood flow. No well-controlled human studies; animal studies show fetal harm at high doses. Second trimester: Similar risks; avoid near cervix to prevent systemic absorption. Third trimester: Placental transfer increases; risk of fetal acidosis, bradycardia, and neurobehavioral depression with high doses. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and signs of systemic toxicity (e.g., CNS depression, arrhythmias). Fetal heart rate monitoring recommended during labor to detect bradycardia or late decelerations. Assess for uterine hypertonus if epinephrine causes vasoconstriction. |
| Fertility Effects | No evidence indicates direct effects on fertility from lidocaine or epinephrine. Epinephrine may cause temporary uterine vasoconstriction, potentially affecting implantation. High doses could theoretically impair reproductive function, but clinical significance unknown. |
| Clinical Pearls | Alphacaine Hydrochloride w/ Epinephrine is a dental local anesthetic solution containing lidocaine HCl 2% with epinephrine 1:100,000 or 1:50,000. The epinephrine component provides vasoconstriction, prolonging anesthetic duration and reducing systemic absorption. Maximum dose of lidocaine with epinephrine is 7 mg/kg (not to exceed 500 mg). For dental infiltration, use smallest effective volume. Avoid intravascular injection; aspirate before injection. Use caution in patients with severe cardiovascular disease, hypertension, hyperthyroidism, or those on MAOIs or tricyclic antidepressants due to potential for hypertensive crisis. Epinephrine may cause tachycardia or hypertension. Do not use in patients with allergy to amide anesthetics or sulfites (present in some formulations). |
| Patient Advice | This medication is a local anesthetic used to numb a specific area in your mouth for dental procedures. · You may feel a burning sensation during injection, but numbness should set in quickly. · Avoid eating or drinking hot beverages for at least 1 hour after the procedure to prevent burns while numb. · Do not chew on the numb side until sensation returns fully. · If you experience chest pain, palpitations, severe headache, or difficulty breathing, seek emergency medical attention immediately. · Report any signs of allergic reaction such as rash, swelling, or difficulty breathing to your dentist or doctor. · Inform your dentist of all medications you take, especially MAOIs, tricyclic antidepressants, beta-blockers, or thyroid medications. · This medication contains epinephrine, which can raise heart rate and blood pressure. |