Ibuprofen, the pain "savior", are you really familiar with it?

Author: Jiang Wei Xi'an Medical College

Zhou Yi, Associate Professor, Xi'an Medical College

Reviewer: Xiao Xinli, Associate Professor of Xi'an Jiaotong University

"Headache, back pain, dysmenorrhea, fever..." When it comes to the "savior" of pain and fever, I'm sure many people will think of ibuprofen, this "magic weapon". So, how much do you know about ibuprofen? Today I'm going to give you some popular science!

The past and present of ibuprofen

Ibuprofen is a household name, but do you know its past? It all started with a British chemist named Stuart Adams.

Adams' family was not wealthy. He dropped out of school at the age of 16 and worked as an apprentice in a pharmacy of a little-known drug company called Boz. However, he was very obsessed with drug research and development. With the support of scholarships from Boz and the Royal Pharmaceutical Society of the United Kingdom, Adams eventually obtained a doctorate in pharmacology and returned to work at Boz.

After World War II, aspirin, as a special anti-inflammatory, analgesic and antipyretic drug, achieved great commercial success. However, after taking a large amount of it for the treatment of rheumatoid arthritis, adverse reactions were obvious. There was an urgent need to find a "super aspirin" with strong efficacy and few adverse reactions. In 1953, Adams led his assistants to successfully develop isobutylphenylisopropionic acid after 8 years of hard work. The efficacy was 3 times that of aspirin, and the compound was named ibuprofen. One day in 1961, Adams drank a lot of wine at a dinner party. The next day he had to speak at an important forum, but he had an unbearable headache, so he took 600 mg of ibuprofen, and the pain was relieved immediately, and his mind was unusually clear. Adams also became the first person to test ibuprofen.

In 1962, Boz registered the patent for ibuprofen. In 1969, the UK approved ibuprofen as a prescription drug. In 1983, the UK approved it as an over-the-counter drug. Due to its low price and rapid analgesic effect, it became popular around the world and played a significant role in relieving women's dysmenorrhea, toothache, back pain and joint pain, becoming one of the world's best-selling drugs.

Figure 1 Copyright image, no permission to reprint

How to use ibuprofen

With its good tolerance and definite efficacy, ibuprofen has been developed into a variety of dosage forms, which are mainly divided into three categories: oral dosage forms, suppositories and topical dosage forms. Among them, oral dosage forms mainly include suspensions, granules, capsules, tablets, etc.

For children, ibuprofen suspension or ibuprofen granules are more suitable. First, they are in the form of liquid or easily soluble in liquid, which is easier for children to swallow; second, they contain a smaller dose of ibuprofen, which is convenient for controlling the dosage of the drug; third, the drug tastes sweeter and has the aroma of flavoring, so children are less likely to resist during use, and are willing to take the medicine on time to help relieve discomfort.

For adults, capsules or tablets can be used. Because ibuprofen tablets take effect quickly but last for a short time, they are very effective in reducing fever and can quickly relieve symptoms; while ibuprofen sustained-release capsules or ibuprofen sustained-release tablets are slowly released in the body, taking effect slowly but lasting for a long time. For this reason, they are mainly used to treat persistent pain.

Suppositories are often used to treat fever and pain caused by childhood colds, acute upper respiratory tract infections and other diseases. They are mainly administered rectally. Parents can insert ibuprofen suppositories into the anus of the child, which will be absorbed through the rectal mucosa to exert its efficacy.

Topical ibuprofen includes ointments, creams, gels, etc., which are often used to relieve local pain and joint inflammation. Before use, the affected area should be cleaned, and then according to the size of the painful area, take an appropriate amount of the medicine and gently rub it.

How ibuprofen works

1. Analgesia. When you swallow a pill of ibuprofen, how can it accurately identify pain signals without a "GPS"? In fact, after taking ibuprofen, it will first reach the stomach and remove its outer shell packaging through gastric acid. Secondly, ibuprofen enters the small intestine and is absorbed into the blood. It searches for pain signals one by one with the blood. When it finds the pain signal, ibuprofen will bind to a specific target molecule and call its "large army". Generally, pain is caused by prostaglandins stimulating pain receptors, but ibuprofen does not "fight" it head-on, but finds the "boss" behind the prostaglandins - cyclooxygenase. By inhibiting cyclooxygenase, more prostaglandins are prevented from being synthesized, achieving an analgesic effect. In the next few hours, the remaining ibuprofen is excreted from the body as the body metabolizes.

Figure 2 Copyright image, no permission to reprint

2. Antipyretic. Ibuprofen inhibits cyclooxygenase and reduces the synthesis of prostaglandins, which lowers the set point of the hypothalamic temperature regulation center, causing peripheral vasodilation and increased sweating, thereby helping patients restore normal body temperature.

3. Anti-inflammatory. Ibuprofen can inhibit the occurrence of inflammatory response by reducing the synthesis of prostaglandins, reducing local vascular permeability and leukocyte infiltration.

Precautions for use of ibuprofen

1. Taking ibuprofen when fever occurs in certain diseases may aggravate the condition, so please follow the doctor's advice.

For example, dengue fever can cause high fever, body pain and other symptoms, but dengue fever patients cannot take ibuprofen. The dengue virus can affect the body's blood coagulation function and cause bleeding tendency. Ibuprofen is a non-steroidal anti-inflammatory drug that can affect platelet function and increase bleeding tendency. Therefore, if dengue fever patients use ibuprofen, the risk of bleeding will increase.

2. Ibuprofen should not be used for a long time or in large quantities. It should not be used for analgesia for more than 5 days and for antipyretic for more than 3 days. If symptoms are not relieved, consult a doctor promptly.

3. Do not take other drugs with antipyretic and analgesic functions at the same time. If you take them at the same time, it will be considered as repeated medication and may increase the adverse reactions of the drugs to the gastrointestinal tract.

4. People with allergies, digestive tract diseases, etc. are not suitable for using ibuprofen. Because ibuprofen inhibits the synthesis of prostaglandins, affects the secretion of mucus in the gastric mucosa, and the stomach is easily irritated, resulting in symptoms such as nausea, vomiting, and heartburn, which aggravates the condition of digestive tract diseases.

Figure 3 Copyright image, no permission to reprint

In short, when taking ibuprofen, you must follow the doctor's instructions to ensure the safety of drug use and reduce adverse reactions.