Benzocaine (CAS No: 94-09-7)

Buy Benzocaine Powder 99% online.Benzocaine, sold under the brand name Orajel amongst others, is a local anesthetic, belonging to the amino ester drug class, commonly used as a topical painkiller or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is combined with antipyrine to form A/B ear drops. In the US, products containing benzocaine for oral application are contraindicated in children younger than two years old.^[2][3]

It was first synthesised in 1890 in Germany and approved for medical use in 1902.^[4]

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)^[5]
• Otic pain (earache)^[5]
• Surgical or procedural local anesthesia^[6]
• Relief of skin pain caused by sunburn, ingrown toenails, hemorrhoids,^[7]

Examples of combination medications of benzocaine include:

• Antipyrine-benzocaine otic consists of antipyrine and benzocaine, and is used to relieve ear pain and remove earwax.^[8]
• Cepacol consists of menthol and benzocaine, and is used to treat sore throat.^[9]
• A solution of benzocaine and menthol is marketed for the treatment of bee stings, mosquito bites, jellyfish stings, and other insect bites^[10]

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 swimmer’s 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.^[11][12]
• Benzocaine mucoadhesive patches have been used in reducing orthodontic pain.^[13]
• 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^[14] was once used there as pharmaceutical compound.

Benzocaine can come in a variety of preparations including:

Oral preparations:

• Lozenges (ex. Cepacol, Chloraseptic)^[15][16]

Topical preparations:

• Gel (ex. Orajel, Anbesol, Kank-A)^[17][18]

Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA). It can be prepared from PABA and ethanol^[27] by Fischer esterification or via the reduction of ethyl p-nitrobenzoate. Benzocaine is sparingly soluble in water; it is more soluble in dilute acids and very soluble in ethanol, chloroform, and ethyl ether. The melting point of benzocaine is 88–92 °C,^[28] and the boiling point is about 310 °C.^[29] The density of benzocaine is 1.17 g/cm³.

Benzocaine can be prepared by esterification using 4-aminobenzoic acid and ethanol.^[30][31] It can also be prepared by reduction of ethyl 4-nitrobenzoate to the amine.^[32][33] In industrial practice, the reducing agent is usually iron and water in the presence of a little acid.^[34]

Benzocaine was first synthesized in 1890 by the German chemist Eduard Ritsert (1859–1946),^[35] in the town of Eberbach^[36] and introduced to the market in 1902 under the name “Anästhesin”.^[37][38]

Benzocaine is found, particularly in Britain, as an additive in street cocaine and also as a bulking agent in “legal highs”.^[39] Benzocaine gives a numbing effect similar to cocaine and as a bulking and binding agent it can not be detected once mixed. It is the most popular cutting agent worldwide.^[40]

Bath solutions of benzocaine and its derivatives are commonly used to anesthetize amphibians for surgery.^[41][42] Benzocaine-based anesthetics are potent and highly effective for both anesthesia and euthanasia in amphibians.^[43]