Assay 99% Easing Pain Benzocaine Hydrochloride Benzocaine HCL CAS
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Benzocaine is a 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.
Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA). It can
be prepared from PABA and ethanol 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 88–90 °C, and the boiling point is about 310 °C.
The density of benzocaine is 1.17 g/cm3.
Benzocaine was first synthesized in 1890 by the German chemist
Eduard Ritsert (1859–1946), in the town of Eberbach and introduced
to the market in 1902 under the name "Anästhesin".
Mechanism of action
Pain is caused by the stimulation of free nerve endings. When the
nerve endings are stimulated, sodium enters the neuron, causing
depolarization of the nerve and subsequent initiation of an action
potential. The action potential is propagated down the nerve toward
the central nervous system, which interprets this as pain.
Benzocaine acts to inhibit the voltage-dependent sodium channels
(VDSCs) on the neuron membrane, stopping the propagation of the
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
- Otic Pain (earache)
- Surgical or procedural local anesthesia
- Lozenges (ex. Cepacol, Mycinettes)
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.
Over-application 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. Applying an oral anesthetic and
consuming beverages before going to bed can be particularly
The topical use of higher concentration (14-20%) benzocaine spray
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. This side effect is
most common in children under 2 years of age. As a result, the FDA
has stated that benzocaine products should not be used in children
under 2 years of age, unless directed by and supervised by a
healthcare professional. Symptoms of methemoglobinemia usually
occur 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)
- Other uses
- Jiffy Toothache Drops bottle (7.75% Benzocaine)
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
- 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
Conversely, an erection will also fade faster if stimulus is
Benzocaine mucoadhesive patches have been used in reducing
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 stings. Today's ready made Pudroderm was
once used there as pharmaceutical compound.
Benzocaine is commonly found, particularly in Britain, as an
impurity in street cocaine. Whilst giving a numbing effect similar
to cocaine on users' gums it does not actually produce the effects
of cocaine. Also benzocaine can and has been mistaken for a false
positive for cocaine.
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