Series VI: Medical Sciences – SUPPLEMENT ... - Krongres

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Bulletin of the Transilvania University of Bra�ov • Vol. 2 (51) - 2009 Series 6: Medical Sciences Supplement – Proceeding of The IV th Balkan Congress of History of Medicine THE ASPIRIN – THE FIRST DRUG OBTAINED BY SINTHESYS – FREQUENTLY USED CURRENTLY A. B�LESCU 1 L. NEDELCU 1 Abstract: Hippocrates mentions the use of a bitter powder, obtained from willow bark to ease the pains and the fever. In 1828 the apothecary Henri Leroux and the chemist Raffaele Piria succeed to isolate under the crystalline form the salicin from the willow bark. The saturated water based solution has a pH of 2.4 which gives the acidity and is known as the salicylic acid. The irritant effect of the salicin on the stomach is recorded in 1839. By replacing, in 1897, a hydroxyl group from the salicylic acid with an acetyl group, the negative effects on the stomach are significantly reduced thus the resulting acetyl salicylic acid. The acetyl salicylic acid (Aspirin) is the first drug obtained through synthesis in 1897, but of the inventor there are doubts. Officially, Felix Hoffman is considered the inventor of the aspirin but this right is claimed also by Arthur Eichengrun. Since many years, the aspirin is used as an analgesic, antipyretic or anti-inflammatory, but it was proved to be efficient as antiplatelet effect or in the prevention of the pancreatic cancer, the decrease of the relapse risk of the rectal or colonic cancers, the prevention of some types of cataract and the prevention of severe migraines. It has come into prominence that a reassessment of the current indications and contraindications is needed Key words: Aspirin, history of the discovery, role. Acidum Acetylsalycilicum, the well known aspirin is the first drug obtained by synthesis while being the most used, with the longest lasting commercial success, being considered the most popular drug of the modern era. The oldest written accounts of the curative properties of the willow bark extract are from the Sumerian civilization. The therapeutic properties of the willow have been discovered by chance as many other scientific discoveries. 1 Faculty of Medicine, Transilvania University of Bra�ov. Similar accounts have been found in Egyptian papyruses translated and published in 1875 by Georg Ebers who bought them in 1869 from Edwin Smith, a passionate American historian and archeologist. The papyruses describe a number of other remedies and curative practices used in antiquity: turtle shells, snake skins, milk, myrtle, figs, and dates [2]. Many of these remedies have kept their use even when Egypt was part of empires.
146 Bulletin of the Transilvania University of Bra�ov • Vol. 2 (51) - 2009 • Series VI Hippocrates, the most renown and important Greek medical practitioners, was recommending the willow bark for diminishing the birth pains and the fever. In ancient Rome, Celsius was using the willow leaf extract for treating fever, pains, swallowing and inflammation. Pedanius Dioscorides, a Nero era botanist, writes about the therapeutic potential of the willow in the book: “De Materia Medica”, which was kept in the Arab translation. Claudius Galen has studied in Egypt and after he used to treat the gladiators in Greece, afterwards he uses his medical knowledge at the emperor’s Marcus Aurelius court. He was recommending the willow for moderate pains. A long period of time the medical knowledge as many of the initially used remedies were forgotten or ignored. There have been trialed other remedies and in 1763, in England, the therapeutic properties of the willow have been noticed in the fever decrease by the reverend Edmund Stone. He administered the willow bark extract to 50 feverish persons, observing a decrease of the fever. Later research discovered the active principle from the willow bark, the salicin. The Italians Brugnatelli and Fontana have isolated, in 1826, the impure willow bark extract but have failed to demonstrate the link between this extract and its pharmacologic effects. The salicin was isolated in its pure state, in crystalline form, in 1828 at the University of München by Johann Büchner. In 1829, Henri Leroux improvised a method to extract salicin from the willow bark and obtained 30 grams of salicin from 1.5 kilograms of bark. The obtained salicin has adverse effects (gastric pains and diarrhea) which prevented it to be used with a therapeutic aim. In 1838, Raffaele Piria, Italian chemist, managed to separate salicin and to obtain the salicylic acid. The saturated water solution of salicin has a pH of 2.4 thus a high acidity and is known as salicylic acid. The irritative effect of salicin on the stomach was mentioned in 1839. In 1853, the French chemist born in Alsace Charles Frederic Gerhard managed to synthesize the pure salicylic acid. Felix Hoffman is considered the inventor of the aspirin, replacing a hydroxyl from the salicylic acid with an acetyl chain obtaining acetyl-salicylic acid (1897). By changing the chemical structure the negative effects on the stomach were significantly reduced. Felix Hoffman tested the antalgic and anti-inflammatory effects on his father. The acetyl-salicylic acid is considered the first sensitized drug. Arthur Eichengrün claimed the rights to the aspirin invention because he has overseeing the team work from which Felix Hoffman was part. The Eichengrün version is sustained by Walter Sneader, Professor at Strathclyde University in 1999. However the French consider that Charles Frederic Gerhard is the inventor of the aspirin by isolating the pure state salicylic acid. After the defeat of Germany in 1918, the Allies have confiscated and sold the Bayer facilities and the exclusivity over the Aspirin trade mark. The buyer was the American firm Sterling that makes and sells in the USA and Canada the acetylsalicylic acid under the name generic name of Aspirin. In 1950 the aspirin was included in the Guinness Book of records as the most common analgesic in the world. No other drug was frequently used as the aspirin. The prescriptions for the use of aspirin are well known [6]: • Analgesic – in the treatment of low and moderate pains (muscular, joint, dental and menstrual pains and headaches);
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Series VI: Medical Sciences – SUPPLEMENT ... - Krongres

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