ALPHACAINE HYDROCHLORIDE W/ EPINEPHRINE
Clinical safety rating
safeBeta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
Beta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
Local anesthesia for infiltration, nerve block, and epidural anesthesiaDental anesthesiaSurgical procedures requiring local anesthesia
cardiac arrest
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. |
| Molecular Weight | Lidocaine HCl: 270.8 Da; Epinephrine bitartrate: 333.3 Da (epinephrine free base: 183.2 Da) |
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 | Use only if clearly needed; epinephrine may cause maternal vasoconstriction and potential fetal hypoxia. Lidocaine is generally considered safe, but epinephrine use in first trimester has theoretical risks of reduced uterine blood flow. |
| 2nd trimester | Considered relatively safe; epinephrine dosing should be minimized to avoid uterine artery vasoconstriction. |
| 3rd trimester | Peripartum: Avoid high doses of epinephrine as it may reduce placental perfusion and cause fetal acidosis. Lidocaine crosses placenta but is not known to cause major malformations. |
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 |
| Placental transfer | Lidocaine crosses placenta via passive diffusion; fetal/maternal ratio approximately 0.5-0.7. Epinephrine placental transfer is limited due to rapid enzymatic degradation. |
| Breastfeeding | Minimal excretion into breast milk; lidocaine and epinephrine are considered compatible with breastfeeding. Epinephrine has poor oral bioavailability and short half-life. Observe infant for signs of local anesthetic toxicity (unlikely at maternal dental doses). |
| Lactation Rating | L2 - Safer |
| Teratogenic Risk | 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. |
■ 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 anesthetics or epinephrineSevere hypotensionCyanotic shockCardiac conduction defects (e.g., complete heart block, Stokes-Adams syndrome)Concurrent MAO inhibitor therapy or tricyclic antidepressants (risk of hypertensive crisis with epinephrine)Cocaine use (additive vasoconstrictive effects)Sulfite allergy (formulations may contain metabisulfite)
| 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. |
| 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. |
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