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Benzocaine

D04A - Antipruritics, incl. antihistamines, anesthetics ATC D04AB04 Small molecule Natural product

JFDA label: Neosol Aerosol 150gm

Mechanism of Action

— Unknown

Indications

Approved

  • Dermal irritation
  • Gel 10% and 20%, lozenge, spray 5%, liquid 10% and 20%
  • Mouth and gum irritation
  • Ointment 20%
  • Poison ivy/sumac
  • Sore throat/mouth, gag reflex suppression
  • Topical anesthetic
  • Topical, external
  • Topical, oral

Contraindications

Source: Lexicomp

  • Hypersensitivity to benzocaine, para-aminobenzoic acid (PABA), or any component of the formulation OTC labeling: When used for self-medication, do not use if you have allergy to local anesthetics (procaine, butacaine, benzocaine, or other "caine" anesthetics). Do not use over deep or puncture wounds, infections, serious burns, or lacerations Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (2)

Not Known Localized burning · stinging sensation

Blood and lymphatic system disorders (1)

Not Known Methemoglobinemia

Immune system disorders (1)

Not Known Hypersensitivity

Skin and subcutaneous tissue disorders (4)

Not Known Contact dermatitis · localized erythema · localized rash · urticaria

General disorders and administration site conditions (3)

Not Known Local pruritus · localized edema · localized tenderness

Dosing

Source: Lexicomp

Note: General dosing guidelines provided; refer to specific product labeling for dosing instructions. Dermal irritation: Topical (external): Spray 5% and 20%, ointment 5%: Apply to affected area or use 1 spray up to 4 times daily as needed. In cases of bee stings, remove stinger before treatment. Mouth and gum irritation: Topical (oral): Gel 10% or 20%, liquid 10% or 20%, ointment 20%, spray 5%: Apply thin layer to affected area or use 1 spray up to 4 times daily as needed. Poison ivy/sumac: Topical (external): Spray 5% (Ivy-Rid only): Spray affected area until wet. Sore throat/mouth, gag reflex suppression: Topical (oral): Lozenge: Allow 1 lozenge to dissolve slowly in mouth; may repeat every 2 hours as needed. Spray 20%: Benz-O-Sthetic: Spray 2 to 3 times or as needed. Repeat if needed for larger areas. Hurricaine: Spray on affected area or throat up to 4 times daily. Topical anesthetic: Topical (oral): Gel or liquid 20% (Topex only): Apply a small amount to mucosa to achieve topical anesthesia.
(For additional information see "Benzocaine: Pediatric drug information") Note: General dosing guidelines provided; refer to specific product labeling for dosing instructions. Dermal irritation: Topical (external): Spray 5% and 20%, ointment 5%: Children ≥2 years and Adolescents: Refer to adult dosing. Mouth and gum irritation: Topical (oral): Gel 10% or 20%, liquid 10% or 20%, ointment 20%: Children ≥2 years and Adolescents: Refer to adult dosing. Spray 5%: Children ≥6 years and Adolescents: Refer to adult dosing. Sore throat/mouth, gag reflex suppression: Topical (oral): Lozenge: Children ≥5 years and Adolescents: Refer to adult dosing. Spray 20%: Benz-O-Sthetic: Children ≥6 years and Adolescents: Refer to adult dosing. Hurricaine: Children ≥2 years and Adolescents: Refer to adult dosing. Teething pain: Note: Use not recommended by AAP, FDA, and the American Academy of Pediatric Dentistry (AAP 2011; AAPD 2012): Manufacturer's labeling: Infants ≥4 months and Children: Topical (oral): Gel 7.5%: Apply pea-size amount to affected gum area up to 4 times daily. Topical anesthetic: Topical (oral): Gel or liquid 20% (Topex only): Refer to adult dosing.
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer's labeling.
There are no dosage adjustments provided in the manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Methemoglobinemia

Has been reported following topical use, particularly with higher concentration (14% to 20%) spray formulations applied to the mouth or mucous membranes. When applied as a spray to the mouth or throat, multiple sprays (or sprays of longer than indicated duration) are not recommended. Use caution with breathing problems (asthma, bronchitis, emphysema, in smokers), inflamed/damaged mucosa, heart disease, children Special populations:

Pediatric

Due to the heightened risk of methemoglobinemia, not recommended for use in patients Dosage form specific issues:

Benzyl alcohol and derivatives

Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

Propylene glycol

Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures and respiratory depression; use caution (AAP 1997; Zar 2007). See manufacturer’s labeling. Other warnings/precautions:

Self-medication (OTC use)

When used for self-medication, notify healthcare provider if condition worsens, or does not improve within 7 days; clears up and occurs again within a few days; or if accompanied by additional symptoms (eg, swelling, rash, headache, nausea, vomiting, or fever). Do not use topical products on open wounds; avoid contact with the eyes. Do not use for a prolonged time and/or on large portions of the body.

Topical application

When topical anesthetics are used prior to cosmetic or medical procedures, the lowest amount of anesthetic necessary for pain relief should be applied. High systemic levels and toxic effects (eg, methemoglobinemia, irregular heartbeats, respiratory depression, seizures, death) have been reported in patients who (without supervision of a trained professional) have applied topical anesthetics in large amounts (or to large areas of the skin), left these products on for prolonged periods of time, or have used wraps/dressings to cover the skin following application.

Pregnancy & Lactation

Pregnancy

Lactation

Probably Compatible Hale L2

Benzocaine should not be applied to the breast or nipple, because the infant may ingest the drug during nursing and it has been associated with severe methemoglobinemia in children under 2 years of age.

Monitoring

Clinical pearlMonitor patients for signs and symptoms of methemoglobinemia such as pallor, fatigue, cyanosis, nausea, muscle weakness, dizziness, confusion, agitation, dyspnea and tachycardia. The classical clinical finding of methemoglobinemia is chocolate brown-colored arterial blood. However, suspected cases should be confirmed by co-oximetry, which yields a direct and accurate measure of methemoglobin levels. Standard pulse oximetry readings or arterial blood gas values are not reliable. Clinically significant methemoglobinemia requires immediate treatment.

Chemistry & Properties

2D structure
FormulaC9H11NO2
Molecular weight165.19 g/mol
IUPAC nameethyl 4-aminobenzoate
CAS94-09-7
PubChem CID2337
InChIKeyBLFLLBZGZJTVJG-UHFFFAOYSA-N
logP1.45 (XLogP 1.9)
Polar surface area52.32 Ų
H-bond acceptors / donors3 / 1
Drug-likeness (QED)0.53
Lipinski violations0
SMILESCCOC(=O)c1ccc(N)cc1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes (logBB 0.27)

Enzyme interactions

EnzymeRoleDetail
CYP1A2Inhibitor
CYP2B6Inhibitor
CYP2C8Inhibitor
CYP3A4Inhibitor

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (4)

BrandForm / strengthPackAgentCitizen (JOD)
Otogesic Ear Drops Eye/Ear Drops 14 mg, 54 mg 15 ml Dar Al Dawa Development and Investment Co Ltd/Jordan 1.250
Otocol ear drops Eye/Ear Drops 50 mg, 50 mg 10 ml Amman Pharmaceutical Indusries 1.430
Benzisol Cream 6.75 g, 0.15 g 150 g tube MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN 3.440
Neosol Aerosol 150gm Cream 1.00 g, 0.090 g 150 g tube MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN 4.410