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What is benzocaine

  1. What is benzocaine

Benzocaine, sold under the brand name Orajel amongst others, is an ester local anesthetic commonly used as a topical pain reliever or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is also combined with antipyrine to form A/B otic drops to relieve ear pain and remove earwax. In the US, products containing benzocaine for oral application are contraindicated in children younger than two years old.In the European Union, the contraindication applies to children under 12 years of age.It was first synthesised in 1890 in Germany and approved for medical use in 1902.

Benzocaine CAS 94-09-7 raw material, is a white needle-like crystal with a chemical name of ethyl 4-aminobenzoate or ethyl p-aminobenzoate (CAS number: 94-09-7, molecular formula: C9H11NO2, molecular weight: 165), the melting point is 90-92℃, slightly soluble in water, and easily soluble in organic solvents. Such as: ethanol, chloroform, ether, soluble in almond oil, olive oil.

As a water-insoluble local anesthetic, Benzocaine has analgesic and antipruritic effects. It is clinically used for wound anesthesia, ulcer surface anesthesia, mucosal surface anesthesia and hemorrhoid anesthesia. Its pharmacological effect is mainly to block nerve endings to relieve Pain and itching.

The remarkable feature of Benzocaine is that it is easy to combine with the lipid layer on the mucosa or skin surface, and it is not easy to enter the human body to cause toxicity. There are more than 100 kinds of benzocaine preparations abroad, including 27 kinds of tablets, 17 kinds of ointments, 6 kinds of creams, 3 kinds of capsule bases, and other preparations such as suppositories, lotions, Gels, aerosols, etc. are mainly used for oral sterilization, oral ulcers, and sore throat.

Compared with foreign countries, the China use of benzocaine is only used in ointments to relieve itching, and the variety of preparations needs further development. In addition, benzocaine is an important organic synthesis intermediate. Mainly used in the production of medicine, plastics and coatings. Benzocaine has an anesthetic effect. Based on this, it can be used to synthesize Osopram, Osopram, and Neo Osopram. Since then, many excellent para-aminobenzoate local anesthetics have been synthesized. Like procaine and many procaine analogs. This kind of anesthetics has the advantages of good stability, quick onset, long maintenance time and small side effects, so it is widely used.

  • Benzocaine Pharmacological action

The local anesthetic effect of benzocaine is weaker than that of procaine, it cannot be infiltrated, and local absorption is slow and lasting.

It is hydrolyzed to p-aminobenzoic acid. It has no irritation and toxicity when the normal concentration is 2%-10%. The toxicity is only 5% of cocaine or 1Chemicalbook0%. The maximum safe amount for topical use is 5g or 25mL of 20% solution.

 It inhibits the conduction of nerve impulses from sensory nerve endings and makes the sense of taste dull. The structure is similar to procaine, so it absorbs slowly and has a long-lasting anesthetic effect.

  • What Benzocaine CAS 94-09-7 Used for?

Medical uses

Benzocaine is indicated to treat a variety of pain-related conditions. It may be used for:

• Local anesthesia of oral and pharyngeal mucous membranes (sore throat, cold sores, mouth ulcers, toothache, sore gums, denture irritation)

• Otic pain (earache)

• Surgical or procedural local anesthesia

Other uses

Benzocaine is used as a key ingredient in numerous pharmaceuticals:

• Some glycerol-based ear medications for use in removing excess wax as well as relieving ear conditions such as otitis media and swimmers ear.

• Some previous diet products such as Ayds.

• Some condoms designed to prevent premature ejaculation. Benzocaine largely inhibits sensitivity on the penis, and can allow for an erection to be maintained longer (in a continuous act) by delaying ejaculation. Conversely, an erection will also fade faster if stimulus is interrupted.

• Benzocaine mucoadhesive patches have been used in reducing orthodontic pain.

• In Poland it is included, together with menthol and zinc oxide, in the liquid powder (not to be confused with the liquid face powder) used mainly after mosquito bites. Today’s ready made Pudroderm[8] was once used there as pharmaceutical compound.

  • What is the side effects of Benzocaine CAS 94-09-7.

Benzocaine CAS 94-09-7 Side effects

Benzocaine is generally well tolerated and non-toxic when applied topically as recommended

However, there have been reports of serious, life-threatening adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) with over-application of topical products or when applying topical products that contain high concentrations of benzocaine to the skin.

Overapplication of oral anesthetics such as benzocaine can increase the risk of pulmonary aspiration by relaxing the gag-reflex and allowing regurgitated stomach contents or oral secretions to enter the airway.[medical citation needed] Applying an oral anesthetic and consuming beverages before going to bed can be particularly hazardous.

The topical use of higher concentration (10–20%) benzocaine products applied to the mouth or mucous membranes has been found to be a cause of methemoglobinemia, a disorder in which the amount of oxygen carried by the blood is greatly reduced.[16] This side effect is most common in children under two years of age. As a result, the FDA has stated that benzocaine products should not be used in children under two years of age, unless directed by and supervised by a healthcare professional. In European countries, the contraindication applies to children under 12 years of age. Symptoms of methemoglobinemia usually occur within minutes to hours of applying benzocaine, and can occur upon the first-time use or after additional use

Benzocaine may cause allergic reactions. These include:

Contact dermatitis (redness and itchiness)

Anaphylaxis (rare)

Where to buy Benzocaine CAS 94-09-7?

Benzocaine raw material CAS 94-09-7 is the API for the drugs of Benzocaine drugs,Benzocaine raw material CAS 94-09-7 is available online from different China manufacturers. Most users of Benzocaine raw material CAS 94-09-7 buy from different websites, some for retail or wholesale purposes.

Verify the legitimacy of every Benzocaine manufacturer using outlined state laws before purchase.

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  1. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 475. ISBN 9783527607495.
  • AHFS Drug Information 2007. McEvoy GK, ed. Benzocaine. Bethesda, MD: American Society of Health-System Pharmacists; 2007: 2844-5.
  • Sultan Healthcare. Topex metered spray (benzocaine 20%) prescribing information. Englewood, NJ; 2006.
  •  Food and Drug Administration. FDA Public Health Advisory: Life-threatening side effects with use of skin products containing numbing ingredients for cosmetic procedures. 2007 Feb 6, updated 2007 Feb 9. From FDA website
  • Sidhu, S. K.; Shaw, S; Wilkinson, J. D. (1999). “A 10-year retrospective study on benzocaine allergy in the United Kingdom”. American Journal of Contact Dermatitis. 10 (2): 57–61. doi:10.1016/s1046-199x(99)90000-3PMID 10357712
  • Eslamian L, Borzabadi-Farahani A, Edini HZ, Badiee MR, Lynch E, Mortazavi A (2013). “The analgesic effect of benzocaine mucoadhesive patches on orthodontic pain caused by elastomeric separators, a preliminary study”. Acta Odontol Scand. 71 (5): 1168–73. 
  1. Amphibian Anesthesia — Research at Penn State”. PennState Animal Resource Program. State College, U.S.: The Pennsylvania State University. November 8, 2010. Retrieved August 24, 2017.


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