Evigrade

Benzocaine

AEMPS

Local anesthetic, aminobenzoic acid ester

ATC code: N01BA05

Brand names: Orajel, Anbesol, Hurricaine

Updated · Methodology

Indications

C

Local anaesthesia for procedures and minor surgery

Adjunct

Benzocaine is a surface anesthetic for the mouth lining. In Spain it is sold over the counter as a spray and a gel, and the AEMPS ficha técnica sets out the use precisely: local relief of dental and oral mucosal pain in adults and children from 6 years, no more than 3 to 4 times a day. Only the surface goes numb, so benzocaine helps before an anesthetic injection, with a denture sore or an aphthous ulcer, while pain from pulpitis or an abscess is merely dulled and its cause stays. While the numbness lasts, eating, drinking and chewing gum are unsafe: biting the tongue or choking comes easily. The ficha also warns about contact dermatitis, taste disturbance and methemoglobinemia in overdose. Benzocaine does not treat the tooth: when pain returns for a third day, a dentist is needed rather than another dose of spray.

C

Sore throat

Adjunct

Benzocaine lozenges – Angileptol, Deratin Complex, Garydol – sit by the till in a Spanish pharmacy, and people reach for them at the first sore throat. The benzocaine in them gives brief numbness of the pharyngeal lining while the lozenge dissolves. That is pain relief, not treatment: viral pharyngitis clears in 5 to 7 days on its own, and no ingredient of the lozenge shortens that. In combinations benzocaine comes with chlorhexidine and enoxolone, and the ficha técnica describes each contribution: antiseptic, anti-inflammatory, anesthetic. The dose must not be exceeded – the ficha states plainly that children, older people and debilitated patients are more sensitive to systemic benzocaine toxicity. If the sore throat lasts beyond three days or fever appears, the situation is reassessed: streptococcus may be behind it, and lozenges do not touch it.

ICD-10: R07.0

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

F

Teething pain in infants

Not recommended

Benzocaine gels were rubbed on babies' gums for decades while teeth were coming through. That practice is unsafe. In 2018 the required over-the-counter oral benzocaine gels to be withdrawn for children under two: the drug has no proven benefit for teething, and methemoglobinemia after it is described in hundreds of cases. The Spanish ficha técnica draws the line its own way: the product is not used under 6 years without medical supervision, because children are more sensitive to systemic benzocaine toxicity. Methemoglobinemia starts quietly – blue lips, shallow breathing, drowsiness, tachycardia – and in an infant it develops within minutes. Teething itself causes neither high fever nor diarrhea, and a chilled teething ring and gum massage are what help. If a pharmacy recommended an anesthetic gel for your child's gums, consider seeking a second opinion from a pediatrician.

ICD-10: K00.7

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

The ethyl ester of 4-aminobenzoic acid. On mucosa benzocaine lowers the permeability of the sensory neuron membrane to sodium ions, depolarization never starts and the nerve impulse does not reach the brain: the area goes numb. The substance barely dissolves in water, so it stays on the surface and is absorbed poorly – hence the fast onset within half a minute and the short duration of 10 to 15 minutes. A systemic fraction still reaches the blood, where part of it turns into aniline derivatives. These oxidize the ferrous iron of hemoglobin to ferric iron, producing methemoglobin, which carries no oxygen. That explains both the age limits and the methemoglobinemia warning in the ficha técnica.

Safety

Contraindications

  • Hypersensitivity to benzocaine
  • Hypersensitivity to other local anesthetics that are para-aminobenzoic acid esters
  • Children under 2 years: risk of methemoglobinemia
  • Children under 6 years without medical supervision

Serious adverse effects

  • Methemoglobinemia, most often with overdose and prolonged use
  • Methemoglobinemia in people with glucose-6-phosphate dehydrogenase deficiency, hemoglobin M disease, methemoglobin reductase deficiency or pyruvate kinase deficiency
  • Anaphylactic reactions
  • Aspiration and tongue biting caused by pharyngeal numbness

Common adverse effects

  • Burning and irritation at the application site
  • Taste disturbance
  • Contact dermatitis

Pregnancy: can you take Benzocaine?

Data on benzocaine in pregnancy are absent or very limited. The ficha técnica advises avoiding the product during pregnancy as a precaution.

Breastfeeding: can you take Benzocaine?

A risk to the infant cannot be excluded and the available evidence is inconclusive. The ficha técnica advises against use while breastfeeding.

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Numbness lasts 10 to 15 minutes. While it lasts, avoid eating and hot drinks: a bitten tongue or a burn goes unnoticed at that moment.

Common myths

Signs of methemoglobinemia: blue lips and nails, breathlessness, headache, dizziness, tachycardia, unusual tiredness. This calls for emergency care, not another dose.

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Frequently asked

What is Benzocaine used for?

Benzocaine is evaluated for the following indications with varying evidence strength: Sore throat (evidence tier C), Local anaesthesia for procedures and minor surgery (evidence tier C), Teething pain in infants (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Benzocaine?

Common side effects of Benzocaine (≥ 1 in 100): Burning and irritation at the application site, Taste disturbance, Contact dermatitis. See the Safety section for uncommon and serious reactions.

Is Benzocaine safe during pregnancy?

Data on benzocaine in pregnancy are absent or very limited. The ficha técnica advises avoiding the product during pregnancy as a precaution.

Is Benzocaine compatible with breastfeeding?

A risk to the infant cannot be excluded and the available evidence is inconclusive. The ficha técnica advises against use while breastfeeding.

Who should not take Benzocaine?

Benzocaine is contraindicated in: Hypersensitivity to benzocaine; Hypersensitivity to other local anesthetics that are para-aminobenzoic acid esters; Children under 2 years: risk of methemoglobinemia; Children under 6 years without medical supervision. Full list in the Safety section.

Official sources

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