History of Paracetamol



Introduction
Paracetamol is a medicine commonly used as a mild painkiller. It also reduces body temperatures of individuals with fever. Hence, paracetamol has both analgesic and antipyretic properties.
How paracetamol was discovered
In the 1880s, at the University of Strassburg in the Department of Internal Medicine , Professor Kussmaul requested two assistants to give patients naphthalene for internal worm treatments. They found that naphthalene had little effects on the internal infections. However, one of the patients reported a high reduction in body temperature. This observation prompted them to do a thorough investigation of the patient. The results of their investigation revealed that the patient was given acetanilide but not naphthalene as result of confusion at the pharmacy.

The assistants speedily published the discovery of antipyretic property of acetanilide. After their publication, acetanilide remained in production and use for several years since it was easy to produce. However, its use faced many side effect complaints such as the deactivation of hemoglobin in red blood cell.

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The acetanilide publications news intrigued a chemist at Bayer’s dyeworks to come up with some acetanilide derivatives; N-(4-Methoxyphenyl) ethanamide and N-(4-Ethoxyphenyl) ethanamide (phenacetin). Phenacetin and N-(4-Methoxyphenyl) ethanamide were found to have antipyretic properties. It was discovered that N-(4-Ethoxyphenyl) ethanamide was less toxic as compared to acetanilide. It was preferred and has been in use ever since. However, restrictions were imposed on its use due to the damage it causes to the kidney for its long-term use.

Numerous medicines were produced to improve N-(4-Methoxyphenyl) ethanamide. As early as 1893 Joseph Von Mering synthesized paracetamol. Paracetamol discovered by Mering had both analgesic and antipyretic properties, but it was believed that it could have the same side effects as acetanilide.
In the 1940s, paracetamol was reinvestigated, when it was discovered in the doses of patients who were using phenacetin. In 1953, Sterling Winthrop Company marketed paracetamol and preferred it over aspirin because it could be taken by people with ulcers and children. However, cases of liver damage were reported from its chronic use.

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N.B.: The antipyretic and analgesic properties of phenacetin could be as result of paracetamol. Since the primary metabolic product of phenacetin is paracetamol. Paracetamol readily forms in the gut individuals who take phenacetin.


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