Language
Country/Area
No result found
The Amazing History of Drugs: How did 4-aminosalicylic acid go from the laboratory in 1902 to the fight against tuberculosis?
In the history of medicine, there are many drugs that have entered the stage of history due to the efforts of scientists, but the story of 4-aminosalicylic acid (PAS) is particularly special. This drug was first synthesized in 1902, but did not enter clinical use until 1944, specifically to deal with tuberculosis, especially in the face of increasingly serious drug-resistant bacteria. This journey is not only the product of the collision of scientific innovation and human needs, but also a symbol of wisdom and selfless dedication.
4-Aminosalicylic acid is widely believed to prevent bacteria from synthesizing folic acid, thereby inhibiting the further propagation of tuberculosis.
The birth and early application of drugs
The synthesis of 4-aminosalicylic acid began in the early 20th century, when scientists Seidel and Bittner discovered this compound. Swedish chemist Jörgen Lehmann first used salicylic acid as an oral treatment for tuberculosis in 1944 after hearing that tuberculosis bacteria were common. Surprisingly, the patient's condition improved rapidly. This breakthrough discovery caused quite a stir at the time and made the compound a new hope in the treatment of tuberculosis.
Clinical application and efficacy
In the battle against tuberculosis, the introduction of 4-aminosalicylic acid caused the medical community to rethink the direction of anti-tuberculosis therapy. In 1948, the Medical Research Council of the United Kingdom conducted a study that demonstrated that the combined use of PAS and streptomycin was significantly more effective than using it alone. This laid the foundation for subsequent combination treatments for tuberculosis.
“The treatment of tuberculosis is no longer a one-man battle, but a combined attack of multiple drugs.”
Current usage
Although with the development of antibiotics and the advent of many new drugs such as isoniazid and rifampicin, 4-aminosalicylic acid is still used as a second-line drug in many places around the world, specifically used to combat multidrug-resistant tuberculosis. Although its efficacy is not as good as the five current first-line drugs, it still plays an important role in the treatment of drug-resistant tuberculosis. On the U.S. market, 4-aminosalicylic acid is marketed under the brand name "Paser" and is usually sold in the form of delayed-release granules with a daily dose of 150 mg/kg.
Side effects and safety
Patients who use 4-aminosalicylic acid should pay attention to its side effects. Common gastrointestinal discomforts such as nausea, abdominal pain and diarrhea may also lead to hepatitis and allergic reactions. This drug may also cause anemia in some patients, so caution is needed, especially in patients with glucose-6-phosphate dehydrogenase deficiency.
“Although the side effects of 4-aminosalicylic acid are much lower than many other drugs, it still needs to be used under the guidance of a doctor.”
Exploration of drug mechanisms
The mechanism of action of 4-aminosalicylic acid is quite unique. As a prodrug, it enters the folate pathway after being converted in the body, binds to dihydrofolate reductase (DHFR), inhibits its activity, and thus prevents bacterial growth. Studies have shown that the main anti-tuberculosis effect is by interfering with the synthesis of folic acid, and careful study of this process has revealed its potential and challenges in clinical application.
Looking to the future
The history of 4-aminosalicylic acid is not only a history of drug development, but also reflects a society’s persistence in the fight against tuberculosis. It tells us that even today, with the rapid development of science and technology, there are still many old drugs that continue to play a key role in new battles. How to find new treatment options and coping strategies in the ever-evolving microbial world will be an important topic in future medical research.
In the face of tuberculosis, an ancient disease that still threatens mankind, will the story of 4-aminosalicylic acid provide enlightenment for our prevention and treatment?
