Benzocaine chemical structure
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Benzocaine

Benzocaine is a local anesthetic commonly used as a topical pain reliever. It is the active ingredient in many over-the-counter analgesic ointments. more...

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Chemical properties

Benzocaine is an ester, a compound made from the organic acid PABA (para-aminobenzoic acid) and ethanol. The process in which this ester is created is known as Fischer esterification.

How it relieves pain

Pain is caused by the stimulation of nerve endings. When the nerve endings are stimulated, sodium enters the nerve ending, which causes an electrical signal to build up in the nerve. Once the electrical signal becomes big enough, it is able to travel to the brain, which then interprets this as pain.

Esters of PABA work as a chemical barrier, stopping the sodium from being able to enter the nerve ending.

Related products

There are various other products that are also made from esters of PABA, many of which have similar anaesthetic properties. Dentists use Procaine (also called Novocaine) to numb teeth and gums.

Benzocaine is also contained in products such as:

  • First aid creams
  • Sore-throat spray
  • Sunburn remedies
  • Condoms (to prevent premature ejaculation)

Other Uses

Benzocaine can also be used as a fish anesthetic. Due to its low solubility in water stock solution can be made with ethanol (95%). 25g of benzocaine per 200ml ethanol will make a solution strong enough to knock saltwater fish out in 2-4 minutes. They will regain equilibrium after 10-15 minutes. Use 5ml stock solution per 1L of saltwater. Some benzocaine will precipitate out of solution when added to the saltwater, so it is recommended to add the volume of stock solution you will be using to a separate container and mix it with some saltwater before adding it to the tank.



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Transdermal Treatment of Pain
From International Journal of Pharmaceutical Compounding, 9/1/05

What types of drugs are found in transdermal preparations?

* Many doctors choose to combine two or more types of medications in the transdermal preparation.

* Adjunct pain relievers: These medications are not anesthetics but reduce pain by blocking transmission of a pain signal to the brain. These include antidepressants such as amitriptyline and many other types of drugs.

* Anesthetics: Anesthetics relieve pain, and when used transdermally can be applied directly to a specific problem area. The most commonly used transdermal pain relievers are benzocaine, lidocaine, and tetracaine.

* Muscle relaxants: A muscle relaxant reduces the contractility of the muscle by blocking the transmission of nerve impulses. Common prescription examples include carisoprodol and cyclobenzaprine.

* Nonsteroidal anti-inflammatory drugs (NSAIDs): While NSAIDs act quickly and can relieve mild pain, their real therapeutic purpose is to minimize inflammation (swelling, redness) in the joints and tissues, which can affect movement in some cases. Examples of common NSAIDs are aspirin and ibuprofen.

Which specific ingredients are used?

Compounding pharmacists have far more options than commercial medicines provide, since commercial medicines are available only in fixed doses and in certain forms. (Many pain medications are available commercially only in oral form.) Transdermal pain formulations can include a number of drugs, including but not limited to those listed here. Some of these can be taken in oral form, but transdermal preparations usually cause fewer, if any, unwanted side effects.

* Amitriptyline

* Cyclobenzaprine

* Dexamethasone

* Gabapentin

* Ketamine

* Ketoprofen

* Lidocaine

* Piroxicam

What conditions are transdermal medications used for?

While there are many specific diagnoses for which transdermal pain medication may be ideal, the following are some of the most common:

* Arthritis

* Localized or acute injury

* Muscle and joint pain

* Nerve pain

Am I a candidate for transdermal pain medication?

Transdermal [trans = through; dermal = the skin] preparations are suitable for most people, and may be particularly useful in those who have an unusually sensitive digestive tract or difficulty swallowing. Transdermal pain medications may not be suitable for broken or raw skin or on very large surface areas. Patients who have allergies or sensitivities to any of the prescription components should not use these medications, and those who are allergic to soy may not be able to use preparations containing certain ingredients such as Pluronic lecithin organogel (PLO). As with any prescription, you should tell your Healthcare provider and pharmacist about all other prescription and overthe-counter medications and supplements you use so that they can screen for possible drug interactions. Talk to your doctor if you are pregnant or nursing a baby. Your pharmacist will advise you about possible side effects.

How are transdermal pain medications usually applied?

Your Healthcare provider will advise you how to apply the medication and for how long. This type of treatment typically is applied in the amount prescribed to the affected area(s) up to three times daily and rubbed in well. Some patients may gradually taper the amount they use as pain lessens. Application of a thin film onto clean, diy skin is generally all that is required to produce the needed effect.

How are transdermal medications dispensed?

Dispensing and packaging vaiy from pharmacy to pharmacy. The medication may come in a tube, a jar, or a syringe. In some cases, a jar with a special adapter is used, and a syringe will be dispensed along with it for easy application. Be sure to ask your pharmacist for a demonstration of how to measure your dose.

Copyright International Journal of Pharmaceutical Compounding Sep/Oct 2005
Provided by ProQuest Information and Learning Company. All rights Reserved

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