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The Pharmacy Newsletter, Cocaine and Local Anesthesia, Really?

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William Garst HSThe use of chewing coca leaves (Erythroxylon coca) dates back centuries for the indigenous peoples of South America, particularly the Peruvians and Incas. When the Spanish explored the region in the 1500s they were initially skeptical of the properties of the plant, but soon learned of its mental as well as its physical properties. The indigenous people told the explorers that chewing the leaf gave them strength, energy, and that it had local numbing properties. Ultimately, the Spanish were convinced of the properties of the plant and began to exploit it for export to Europe.

It was not until 1855 that the German chemist Frederich Gaedcke isolated the crude alkaloid and he named it erythroxyline. Subsequently, in 1860 Albert Niemann published a much-improved purification process and called his substance cocaine because he isolated the chemical from the coca leaves.

The first recorded use of cocaine as a local anesthetic was in 1884, when Karl Koller, an associate of Sigmund Freud, experimented with a cocaine solution as an ophthalmic anesthetic. He instilled the solution into his own eyes, then pricked his eyes with needles and experienced no pain. Apparently, it was a relatively common practice for scientists to experiment on themselves in the early years of medical research.  It was not long after this that cocaine was used as a respiratory anesthetic and in nerve blocks. In 1898 Heinrich Quincke, a German physician used cocaine for spinal anesthesia.

The popularization of cocaine quickly caught on as it was incorporated into medicine for its energy stimulant properties. In Europe cocaine was mixed with wine as a medicinal beverage and in the United States, Atlanta pharmacist John Pemberton included cocaine in his 1886 recipe for Coca-Cola, but the cocaine was removed from the formula in 1906 because of the restrictions imposed by the Pure Food and Drug Act of 1906.

During this time, it was quickly recognized that cocaine had strong addictive qualities, and we are still experiencing the toll that cocaine addiction presents on our society. However, there is a medical product still in use in the United States that contains cocaine: a 4 percent topical solution of cocaine used in nasal surgeries for its anesthetic and vasoconstrictive properties. It deadens the pain and lessens the bleeding, a good combination in these types of surgeries.

The search for other local anesthetics having fewer addictive qualities led to the discovery of popular drugs like procaine (Novocain), lidocaine, tetracaine, bupivacaine, and benzocaine. These local anesthetics have a variety of uses, all of which involve the relieving of pain. They are used frequently for dental and eye procedures, nerve blocks, post-operative spinal anesthesia, dermatological procedures, and even included in patches for the topical relief of pain.

Additionally, there are natural products other than cocaine used for their local anesthetic properties: menthol, obtained from peppermint, and eugenol, obtained from cloves, nutmeg, cinnamon, and basil. Clove oil is a popular over-the-counter topical treatment for toothaches.

The drug category we know as local anesthetics can be traced back to the discovery of cocaine from the coca leaves. The history of cocaine is long and relevant today and filled with many interesting stories and characters. I once asked an Emergency Department physician what one drug would they want if stranded on a deserted island and the quick answer was “lidocaine” or some local anesthetic for the relief of pain, so it seems we all can be thankful for the development of this class of drugs.

Stay informed and stay healthy.

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William Garst is a consultant pharmacist who resides in Alachua, Florida. He received his B.S. in Pharmacy from Auburn University in 1975. He earned a master’s degree in Public Health in 1988 from the University of South Florida, and a Master’s in Pharmacy from UF in 2001. In 2007 he received his Doctor of Pharmacy from the University of Colorado. Dr. Garst is a member of many national, state, and local professional associations. He serves on the Alachua County Health Care Advisory Board and stays active as a relief pharmacist. In 2016 he retired from the VA.  Dr. Garst enjoys golf, reading (especially history), and family. He writes a blog called The Pharmacy Newsletter (https://thepharmacynewsletter.com/). William Garst can be contacted at communitypharmacynewsletter@gmail.com.

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Email editor@

alachuatoday.com

William Garst HSThe use of chewing coca leaves (Erythroxylon coca) dates back centuries for the indigenous peoples of South America, particularly the Peruvians and Incas. When the Spanish explored the region in the 1500s they were initially skeptical of the properties of the plant, but soon learned of its mental as well as its physical properties. The indigenous people told the explorers that chewing the leaf gave them strength, energy, and that it had local numbing properties. Ultimately, the Spanish were convinced of the properties of the plant and began to exploit it for export to Europe.

It was not until 1855 that the German chemist Frederich Gaedcke isolated the crude alkaloid and he named it erythroxyline. Subsequently, in 1860 Albert Niemann published a much-improved purification process and called his substance cocaine because he isolated the chemical from the coca leaves.

The first recorded use of cocaine as a local anesthetic was in 1884, when Karl Koller, an associate of Sigmund Freud, experimented with a cocaine solution as an ophthalmic anesthetic. He instilled the solution into his own eyes, then pricked his eyes with needles and experienced no pain. Apparently, it was a relatively common practice for scientists to experiment on themselves in the early years of medical research.  It was not long after this that cocaine was used as a respiratory anesthetic and in nerve blocks. In 1898 Heinrich Quincke, a German physician used cocaine for spinal anesthesia.

The popularization of cocaine quickly caught on as it was incorporated into medicine for its energy stimulant properties. In Europe cocaine was mixed with wine as a medicinal beverage and in the United States, Atlanta pharmacist John Pemberton included cocaine in his 1886 recipe for Coca-Cola, but the cocaine was removed from the formula in 1906 because of the restrictions imposed by the Pure Food and Drug Act of 1906.

During this time, it was quickly recognized that cocaine had strong addictive qualities, and we are still experiencing the toll that cocaine addiction presents on our society. However, there is a medical product still in use in the United States that contains cocaine: a 4 percent topical solution of cocaine used in nasal surgeries for its anesthetic and vasoconstrictive properties. It deadens the pain and lessens the bleeding, a good combination in these types of surgeries.

The search for other local anesthetics having fewer addictive qualities led to the discovery of popular drugs like procaine (Novocain), lidocaine, tetracaine, bupivacaine, and benzocaine. These local anesthetics have a variety of uses, all of which involve the relieving of pain. They are used frequently for dental and eye procedures, nerve blocks, post-operative spinal anesthesia, dermatological procedures, and even included in patches for the topical relief of pain.

Additionally, there are natural products other than cocaine used for their local anesthetic properties: menthol, obtained from peppermint, and eugenol, obtained from cloves, nutmeg, cinnamon, and basil. Clove oil is a popular over-the-counter topical treatment for toothaches.

The drug category we know as local anesthetics can be traced back to the discovery of cocaine from the coca leaves. The history of cocaine is long and relevant today and filled with many interesting stories and characters. I once asked an Emergency Department physician what one drug would they want if stranded on a deserted island and the quick answer was “lidocaine” or some local anesthetic for the relief of pain, so it seems we all can be thankful for the development of this class of drugs.

Stay informed and stay healthy.

*    *     *

William Garst is a consultant pharmacist who resides in Alachua, Florida. He received his B.S. in Pharmacy from Auburn University in 1975. He earned a master’s degree in Public Health in 1988 from the University of South Florida, and a Master’s in Pharmacy from UF in 2001. In 2007 he received his Doctor of Pharmacy from the University of Colorado. Dr. Garst is a member of many national, state, and local professional associations. He serves on the Alachua County Health Care Advisory Board and stays active as a relief pharmacist. In 2016 he retired from the VA.  Dr. Garst enjoys golf, reading (especially history), and family. He writes a blog called The Pharmacy Newsletter (https://thepharmacynewsletter.com/). William Garst can be contacted at This email address is being protected from spambots. You need JavaScript enabled to view it..

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alachuatoday.com