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Benzocaine 20% | Lidocaine 6% | Tetracaine 4%

Benzocaine 20% | Lidocaine 6% | Tetracaine 4% is a prescriber-directed topical or oral numbing/pain preparation. It should be matched to location, surface area, intact vs. non-intact tissue, duration of use, and total anesthetic exposure.

CreamTopicalRx Only503A Compounded

This is a triple-anesthetic topical preparation combining three local anesthetics—benzocaine 20%, lidocaine 6%, and tetracaine 4%—in a single compounded cream or gel. Each agent independently blocks voltage-gated sodium channels to inhibit nerve impulse conduction, providing rapid-onset, synergistic topical anesthesia. Genesis Compounding prepares this as a prescription-only 503A compounded preparation, not FDA-approved as a compounded product, for patient-specific procedural anesthesia under prescriber direction.

Active IngredientPharmacologic Role
Benzocaine 20%Ester-type local anesthetic that rapidly blocks voltage-gated sodium channels in nerve membranes, producing short-duration surface anesthesia with quick onset.
Lidocaine 6%Amide-type class IB local anesthetic that reversibly binds sodium channels from the intracellular surface, offering intermediate duration and rapid onset with predictable tissue penetration.
Tetracaine 4%Ester-type local anesthetic with high lipid solubility providing longer duration of action, extending and deepening the anesthetic effect of the combination.

Route: Topical application to intact skin or mucous membranes prior to procedures (e.g., laser resurfacing, dermal filler injection, venipuncture, cosmetic procedures).

  • Apply a thin, uniform layer to the target area and cover with occlusive dressing or leave open per prescriber protocol.
  • Allow 20–45 minutes of contact time for full anesthetic effect before initiating the procedure.
  • Remove excess cream prior to procedure; avoid application to broken, inflamed, or highly vascular skin where systemic absorption may be increased.
  • Do not apply near eyes, ears, or mucous membranes unless specifically directed by the prescriber.

Dosing is prescriber-determined based on the area to be anesthetized, the procedure type, and the patient's weight and clinical status. General principles:

  • Apply the minimum effective quantity to achieve anesthesia; avoid large surface area application to limit systemic absorption.
  • Contact time is typically 20–45 minutes under occlusion; longer contact may increase depth of anesthesia but also systemic absorption risk.
  • This formulation is not intended for injection. Final dosing instructions are established by the treating prescriber.
  • Benzocaine: Ester-type local anesthetic; diffuses across the nerve membrane and blocks voltage-gated sodium channels, preventing depolarization and propagation of the action potential. Rapid onset due to high unionized fraction at tissue pH.
  • Lidocaine: Amide-type local anesthetic; the uncharged form penetrates the axonal membrane and the ionized form binds sodium channels from the intracellular side, locking them in an inactive state. Acts selectively on frequently depolarizing channels (use-dependent block).
  • Tetracaine: Ester-type local anesthetic with high lipid solubility; penetrates neural membranes effectively and blocks sodium channel conductance, producing prolonged anesthetic duration compared to benzocaine.

This triple-anesthetic combination is used prescriber-directed for topical anesthesia prior to minimally invasive procedures including laser treatments, microneedling, dermal filler injections, vascular access, and minor dermatologic procedures. The complementary pharmacokinetic profiles of the three agents (rapid-onset benzocaine, intermediate lidocaine, long-duration tetracaine) are intended to provide layered anesthetic coverage.

Monitoring considerations:

  • Limit application area, particularly in pediatric or low-body-weight patients, to reduce systemic absorption risk.
  • Monitor for signs of local anesthetic systemic toxicity (LAST): perioral numbness, metallic taste, tinnitus, visual changes, seizure, cardiac arrhythmia—especially if applied over large surface areas or compromised skin.
  • Ester anesthetics (benzocaine, tetracaine) are metabolized to PABA derivatives; use with caution in patients with PABA hypersensitivity or sulfonamide allergy.
  • Benzocaine is associated with methemoglobinemia; use with caution in patients with G6PD deficiency, hemoglobinopathy, or concomitant oxidant drug use.

Contraindications:

  • Known hypersensitivity to any component (benzocaine, lidocaine, tetracaine, or formulation excipients)
  • PABA hypersensitivity (relevant to ester anesthetics benzocaine and tetracaine)
  • Application over large open wounds or highly vascular surfaces without prescriber supervision

Warnings & Precautions:

  • Methemoglobinemia: Benzocaine carries a known risk of methemoglobinemia, particularly with large-area application, prolonged contact, or use in patients with G6PD deficiency or hemoglobinopathy.
  • Systemic toxicity (LAST): Excessive absorption of any local anesthetic may cause CNS excitation progressing to seizure, and cardiovascular depression; use lowest effective amount.
  • Cholinesterase deficiency: Ester anesthetics (benzocaine, tetracaine) may have prolonged effect in patients with pseudocholinesterase deficiency.
  • Hepatic impairment: Lidocaine (amide) metabolism may be prolonged with significant hepatic dysfunction.
  • Avoid use near eyes without explicit prescriber direction.

Drug Interactions:

  • Concurrent use of other local anesthetics may increase systemic toxicity risk.
  • Agents that cause methemoglobinemia (nitrates, dapsone, sulfonamides, hydroxyurea, chloroquine) may be additive with benzocaine.
  • Propranolol increases lidocaine plasma concentrations.

Common Side Effects: Local erythema, blanching, pruritus, and edema at the application site; transient burning or stinging upon application; rarely, allergic contact dermatitis.

Store at controlled room temperature (20–25°C / 68–77°F). Protect from excessive heat, freezing, and direct light. Keep container tightly closed. Do not apply if product shows visible signs of separation or discoloration. As a 503A compounded preparation, this product carries a beyond-use date assigned by Genesis Compounding; do not use after the labeled expiration date. Keep out of reach of children.

What is the purpose of combining three anesthetics?

Each agent works through a similar sodium-channel mechanism but has a different onset and duration profile. Benzocaine provides very rapid onset, lidocaine offers reliable intermediate duration, and tetracaine extends the anesthetic effect. Together they provide layered, synergistic topical anesthesia for procedural use.

How long should this cream be left on before a procedure?

Typically 20–45 minutes under occlusion, depending on the procedure and prescriber protocol. Your prescriber will specify the optimal contact time for your intended procedure.

Is this product FDA-approved?

This is a 503A compounded preparation prepared by Genesis Compounding for a specific patient based on a prescriber's order. It is not an FDA-approved drug product. Each ingredient (benzocaine, lidocaine, tetracaine) is an established local anesthetic with well-characterized pharmacology.

What is methemoglobinemia, and how does benzocaine cause it?

Methemoglobinemia is a condition in which hemoglobin is oxidized to a form that cannot carry oxygen effectively. Benzocaine can oxidize hemoglobin, particularly at high doses or over large areas. Patients with G6PD deficiency or certain blood disorders are at higher risk. Signs include cyanosis, shortness of breath, and dizziness.

How should unused product be stored?

Keep tightly sealed at room temperature, away from heat and light. Do not use after the beyond-use date printed on the label. Return unused product to the pharmacy or dispose of per local guidelines.

Clinical References

Authoritative sources reviewed in preparing this clinical summary. Provided for prescriber reference; not a substitute for the prescriber’s clinical judgment.

Topical, Local, and Regional Anesthesia and Anesthetics — StatPearls
NCBI Bookshelf / StatPearls, 2025
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Lidocaine — StatPearls
NCBI Bookshelf / StatPearls, 2024
Source →
Benzocaine Topical — DailyMed (FDA)
FDA DailyMed, NLM
Source →
Methemoglobinemia Risk with Topical Benzocaine
FDA Drug Safety Communication
Source →