Phenacetin

Phenacetin

Phenacetin is a painkiller and fever reducer that was widely used in the late 19th and early 20th centuries. It was one of the first non-opioid analgesics to be discovered and was a key ingredient in many popular over-the-counter drug formulations. However, due to its association with serious health problems, including cancer and kidney disease, it has been largely phased out and is no longer commercially available in many countries.

History

Phenacetin was first synthesized in 1878 by the German chemist Harmon Northrop Morse. It was initially marketed as a treatment for fever and pain, and was included in a number of popular drug mixtures, including the headache remedy "Bayer's 'Phenacetin-Koffein'". However, by the mid-20th century, evidence began to emerge linking phenacetin to serious health problems, leading to its gradual withdrawal from the market.

Pharmacology

Phenacetin is a prodrug that is metabolized in the body to paracetamol, which is the active compound that exerts the analgesic and antipyretic effects. The metabolism of phenacetin occurs primarily in the liver, involving two main enzymatic pathways: N-deethylation to paracetamol and O-deethylation to phenetidine.

Health effects

Long-term use of phenacetin is associated with serious health problems. It has been linked to methemoglobinemia, a blood disorder that reduces the ability of red blood cells to release oxygen to tissues, and nephropathy, a form of kidney disease. Phenacetin is also a known carcinogen, and its use has been linked to an increased risk of developing bladder cancer and renal pelvis cancer.

Legal status

Due to its health risks, phenacetin has been banned in many countries. In the United States, the Food and Drug Administration (FDA) banned the sale of phenacetin in 1983, citing its carcinogenicity and the risk of kidney damage. In the United Kingdom, the Medicines and Healthcare products Regulatory Agency (MHRA) withdrew phenacetin from the market in 1968.

See also

• Analgesic
• Paracetamol
• Prodrug
• Nephropathy
• Carcinogen