Tuesday, December 12, 2006

History of Paracetamol

Paracetamol is a very widely used as medicine. It is painkiller and reduces the temperature of patients with fever.

These actions are known respectively as analgesic and antipyretic.

In 1893, the white, odorless crystalline compound with a bitter taste that became known as paracetamol was discovered.

This happened at University of Strasburg when Professor Adolf Kussmaul, Department of Internal Medicine , asked two young assistants, Arnold Cahn and Paul Hepp, to treat patients with naphthalene as it had been used elsewhere as an internal antiseptic.

The medicine had little effect on worms, but, paracetamol was found in the urine of patients who had taken phenacetin, who had a great reduction in fever temperature.

In 1887, the Bayer company introduced the 4-ethoxy derivative, phenacetin, as a less toxic analogue of acetanilide.

It was highly successful product and established the Bayer Company as a leading pharmaceutical manufacturer.

Phenacetin was widely used for about 90 years until mounting concerns over carcinogecity and kidney damaging properties.

In 1889 it was demonstrated that paracetamol was a urinary metabolite of acetanilide. These discoveries, however, failed to attract much attention and were largely ignored at the time.

The use of paracetamol was first reported in 1893 by von Mehring who concluded that because of its hematological side effects of methaemoglobinaemia, it could not be recommended despite prompt antipyretic and analgesic actions.

It 1948-1949, Brodie and Axelrod discovered that paracetamol was the main metabolite of both acetanilide and phenacetin, that paracetamol experienced a resurgence of interest. As a derivative of p-aminophenol, paracetamol corresponds to the active principal metabolite phenacetin.

Their investigations showed that both acetanilide and phenacetin were metabolized into paracetamol and to which they owed their antipyretic and analgesic properties.

It was eventually ascertained that phenacetin had its own pharmacological action and was not dependent on paracetamol for its effects.

Because a high proportion of phenacetin is converted into paracetamol in the liver, however, phenacetin required a large dosage to achieve any direct analgesic effect.

In 1950 the first paracetamol product – a combination of paracetamol, aspirin and caffeine – was on the United States market under the name Triagesic.

Due to the report that Triagesic had been stricken with blood diseases, agranulocytoses, a sudden severe drop of white blood cell, it was immediately removed form the market.

Within a few years when became apparent that paracetamol had not connection with blood damage, by 1955 paracetamol was back in the American market.

In 1956, 500 mg tablets of paracetamol went on sale in the United Kingdom and its popularity as an over-the-counter analgesic rapidly increased.

This popularity was partly explained by the fact that paracetamol was proven to be easier on the stomach than some other analgesics.
History of Paracetamol
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