By reducing the neuronal membrane's permeability to sodium ions, benocaine prevents both the conduction and initiation of neuronal impulses.

• Topical use:

  • Dermal irritation:

    • It is used as ointment 5%, spray 5% and 20%
    • It has been used to treat minor skin irritations, cuts, sunburn, scrapes, small burns, and insect bites temporarily relieve discomfort and itching.
    • Moreover, it is applied to treat minor burns, scrapes, and cuts to avoid infection.

  • Poison ivy/sumac:

    • Spray 5% (Ivy-Rid only):

      • It is used to temporarily relieve the pain and itching brought on by poison oak, sumac, and poison ivy.

• ---

  Topical oral use:

  • Mouth and gum irritation:

    • Ointment 20%:

      • It is used to provide short-term pain relief for cold sores and fever blisters.

    • Gel 10% and 20%, lozenge, spray 5%, liquid 10% and 20%:

      • It is used to treat small oral and gum injuries produced by dentures or orthodontic devices, as well as pain associated with sore gums, a sore throat, toothaches, canker sores, braces, and minor dental treatments.
      • Due to safety concerns over the increased risk of methemoglobinemia in newborns and young children (under the age of two), it is not advised.

• Sore throat/mouth, gag reflex suppression:

  • Spray 20%:
    • It is used topically to parts of the mouth or mucous membranes.
    • It is used to provide momentary relief from slight discomfort and pain associated with sore throats and mouths.
    • Moreover, it is utilised to momentarily reduce the gag reflex.

• ---

  Topical anesthetic:

  • Gel or liquid 20% (Topex only):
    • Prior to local anaesthetic injections, scaling, and prophylaxis, it is used as a topical anaesthetic on the oral mucosa.
    • When taking impressions, it is utilised to ease the discomfort that comes with it.

Benzocaine Dose in Adults

Dosage in the treatment of Dermal irritation:

• Topical (external):

  • Spray 5% and 20%, ointment 5%:
    • When needed, apply to the afflicted area or use 1 spray every 6 hours.
    • Bee stings should be treated without the stinger present first.

Dosage in the treatment of Mouth and gum irritation:

• Topical (oral):

  • Gel 10% or 20%, liquid 10% or 20%, ointment 20%, spray 5%:
    • Use one spray up to four times daily as necessary, or apply a thin layer to the affected region.

Use in the Poison ivy/sumac:

• Topical (external):

  • Spray 5% (Ivy-Rid only):
    • Spray until the afflicted area is moist.

Use in the treatment of Sore throat/mouth, gag reflex suppression:

• Topical (oral):

  • Lozenge:

    • Let one lozenge to dissolve entirely in the mouth.
    • If necessary, it can be repeated every two hours.

  • Spray 20%:

    • Benz-O-Sthetic:
    • Spray it twice to three times, or as needed.
    • Repeat for bigger areas if necessary.

  • Hurricaine:

    • Spray up to four times per day on the neck or afflicted area.

Use in the treatment of Topical anesthetic:

• Topical (oral):

  • Gel or liquid 20% (Topex only):
    • To cause topical anaesthetic, apply a little amount to the mucosa.

Benzocaine Dose in Children

• Due to risk of methemoglobinemia, AAP, FDA, and the American Academy of Pediatric Dentistry does NOT recommend use for teething and mouth pain in infants and children  younger than 2 years

Use in the treatment of Dermal irritation (insect bites, minor cuts, scrapes, minor burns, sunburn):

• Topical:

  • 20% spray, 5% ointment:

    • Children ≥2 years and Adolescents:
      • 3 to 4 times a day, if necessary, it is applied to the affected region.

Use in the treatment of Mouth and gum irritation (including fever blisters and cold sores):

• Topical:

  • Oral 10% or 20% gel/liquid:

    • Children ≥2 years and Adolescents:
      • Up to 4 times a day, as needed, a thin layer is applied to the affected area.

    • Oral 5% spray:

      • Children ≥6 years and Adolescents:
        • Spray the area once, up to four times per day.

Use in the treatment of Sore throat, sore mouth, and gag reflex suppression:

• Oral lozenge:

  • Children ≥5 years and Adolescents:
    • Let one lozenge slowly dissolve in your tongue.
    • If necessary, it can be repeated every two hours.

• Oral spray 5%:

  • Children ≥6 years and Adolescents:
    • Use 1 spray to the throat or afflicted area up to 4 times per day.

• Oral spray 20%:

  • Children ≥2 years and Adolescents:
    • Up to four times each day, spray the throat or the afflicted area.

Benzocaine pregnancy risk category: C

• Benzocaine can only be used for topical purposes. It is not recommended for use during pregnancy, as there is insufficient data.

Use during breastfeeding:

• It can be used while you breastfeed. 

Benzocaine Dose in Renal Disease:

• No dose adjustments have been advised by manufacturer in patient with kidney disease.

Benzocaine Dose in liver Disease:

• No dose adjustments have been advised by manufacturer in patient with liver disease.

Side effects of Benzocaine:

• Central nervous system:

  • Localized burning
  • Stinging sensation

• Dermatologic:

  • Contact dermatitis
  • Localized erythema
  • Localized rash
  • Urticaria

• Hematologic & oncologic:

  • Methemoglobinemia

• Hypersensitivity:

  • Hypersensitivity

• Local:

  • Local pruritus
  • Localized edema
  • Localized tenderness

Contraindication to Benzocaine include:

• Allergy reactions to para-aminobenzoic (PABA) or any other part of the formulation
• Self-medication should be avoided if you are allergic to any local anesthetics such as procaine, benzocaine and butacaine.
• It shouldn't be used on lacerations, puncture wounds or deep wounds.

Warnings and precautions

• Methemoglobinemia:
  • It was reported to be effective when applied topically to the mucous membranes or mouth, in a concentration of 14% to 20%.
  • It is not recommended to spray multiple times or for a longer duration than the indicated time.
  • Be careful in the following situations:
    • Coexisting breathing issues (emphysema and bronchitis in smokers)
    • Mucosa damaged or inflamed
    • Heart disease
    • Children under 6 months old
    • Anomalies in the enzyme or haemoglobin (glucose-6-phosphate dehydrogenase deficiency, hemoglobin-M disease,
    • NADH-methemoglobin reductase deficiency, pyruvate-kinase deficiency).
    • Those who are more vulnerable should think about alternatives to benzocaine sprays, like topical lidocaine.

Benzocaine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

• Examine patients for methemoglobinemia symptoms and signs, such as tachycardia, dyspnea, pallor, weariness, cyanosis, muscle weakness, disorientation, confusion, and agitation.
• The main clinical symptom of methemoglobinemia is the presence of chocolate-brown arterial blood.
• Co-oximetry should be used to confirm suspected instances since it provides a precise and direct measurement of methemoglobin levels.
• Conventional arterial blood gas tests or pulse oximetry readings are frequently unreliable.
• Methemoglobinemia that requires rapid treatment is clinically severe.

How to administer Benzocaine?

• Avoid coming into contact with your eyes and other mucous membranes.
• Do not use some spray products near heat, flame, or fire as they may contain flammable components.
• Avoid coming into contact with clothing or furnishings as some products can stain particular fibres.

Topical, external:

• The ointment should be applied evenly.

Spray:

• It should be shaken well before using.
• Hold the affected area between 6 and 12 inches away.
• Spray onto the palm of your hand before touching your hand to your face to apply to your face.
• Applying it to skin that is damaged, blistered, or abraded is not advised.

Topical, oral: Gel/liquid:

• It should be applied with a cotton applicator or fingertip to the affected area.
• For dental irritation, do not reinsert dentures till irritation or pain is relieved
• rinse mouth well before reinserting.

Lozenge:

• It should be allowed to dissolve slowly in the mouth.

Ointment:

• It should be applied evenly.

Spray:

• Before using, it should be thoroughly mixed. Certain products can be applied more precisely directly using an extension tube.

Mechanism of action of Benzocaine:

• It decreases the permeability of the neuronal membrane to sodium ions, which prevents the conduction and initiation of neuronal impulses.
• Conduction blockage and depolarization inhibition are the results.

Onset:

• Around 15 to 30 seconds, the anaesthetic impact of spray begins.

Absorption:

• Through healthy skin, its absorption is inadequate.
• It penetrates mucosal membranes thoroughly and traumatises skin.

Metabolism:

• It is primarily metabolised via the plasma via hydrolysis and hepatic pathway (to a lesser extent).

Benzocaine international brands:

• Aftertest Topical Pain Relief
• Anacaine
• Anbesol Cold Sore Therapy
• Anbesol JR
• Anbesol Maximum Strength
• Anbesol
• Baby Anbesol
• Benz-O-Sthetic
• Bi-Zets/Benzotroches
• Blistex Medicated
• Cepacol INSTAMAX
• Chiggertox
• Dent-O-Kain/20
• Dentapaine
• Dermoplast
• Foille
• HurriCaine One
• Hurricaine
• HurriPak Starter Kit
• Ivy-Rid
• Kank-A Mouth Pain
• Ora-film
• Pinnacaine Otic
• Sore Throat Relief
• Zilactin Baby
• AAA Spray
• Anaesthesin
• Anesthetite
• Auralyt
• Baby Orajel
• Babydent
• Bumeze
• Claudemor
• Clovaine Gel
• Dentispray
• Dermopur
• Dolodent
• Etylu Aminobenzoesan
• Foille
• Freez-Eze Throat Anesthetic Gel
• Gastobenz
• Gengivarium
• Graneodin-B
• Happy-Dent
• Hurricaine
• Hurricaine Gel
• Hurricane Spray
• Lanacane
• Lodoc
• Mandelay
• Nani Pre Dental
• Neo-angin
• Octicaina
• Oracaine
• Orajel
• Oratics Oral Gel
• Orogel
• Orogel Dental Gel
• Oticaina
• Otisyn
• Solarcaine
• Tonjac Benzogel
• Topex
• Topicaine
• Topispray
• Trimplex

Benzocaine Brands in Pakistan: