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NSAIDs Presentation
  
 

The most common NSAIDs

Acetylsalycilic acid
Aspirin
Ketoprofen
Orudis
Diflunisal
Dolobid
Piroxicam
Feldene
Diclofenac
Etodolac
Lodine
Rizatriptan
Meloxican

Non-steroidal anti-inflammatory drugs or NSAIDs are a vast group of medications, which are widely used and highly praised nowadays for their triple action: analgesic, antipyretic and anti-inflammatory. In other words, NSAIDs help to relieve pain, lower high body temperature or fever and reduce inflammation. Better than opioids because of no narcotic effect and dependence risk, NSAIDs became the most widely prescribed pain-killers of the 20th century.

 

The official history of non-steroidal anti-inflammatory drugs started in 1899, when Bayer registered Aspirin as a trademark. Since then Aspirin had been considered to be one of the real “wonder drugs” in the history of pharmaceutics. Aspirin was the first representative of a NSAIDs family, which now contains dozens of medications, including Celebrex, the most up-to-date NSAID, characterized with high selectivity in affecting body chemistry.

 

The timeline of non-steroidal anti-inflammatory drugs

Around 1500 BC

Egyptians learned to use dried myrtle leaves to relieve back pain. At that time they did not know that myrtle contained salicylic acid, which would be transformed into aspirin in future.

Around 200 BC

Doctors of Ancient Greece prescribed willow bark to relieve pain and fever, still not knowing that willow also contained salicylic acid.

Year 1763

Edward Stone, an English clergyman, reported to the Royal Society of London of his successful use of willow bark to reduce fever in his patients.

Year 1828

Salicin was isolated from the willow bark for the first time in history.

Year 1853

Charles Frederic Gerhardt first synthesized acetylsalicylic acid, which later became world known as aspirin. However, he failed to understand its importance to humanity.

Year 1897

The first pure samples of acetylsalicylic acid were synthesized at the Bayer laboratory. 

Year 1899

Bayer registered Aspirin trademark and started selling the first NSAID. Still, scientists did not know how exactly aspirin worked.

Year 1971

British scientist, John Vane, explained that aspirin worked by inhibiting prostaglandins.

Year 1982

John Vane received Nobel Prize for his research.

Year 1998

Scientists discovered COX-2 enzyme, and suggested COX-2 selective inhibitors as the newest class of NSAIDs.

Year 1999-2000

Vioxx, Bextra and Celebrex were approved as new COX-2 selective NSAIDs with low risks of gastrointestinal side effects.

Year 2004

Vioxx and Bextra were removed from the market because of negative influence on the cardiovascular system.

Year 2008

Of all COX-2 NSAIDs, only Celebrex is still on the market. Older NSAIDs are among the most widely prescribed pain medications in the world.

 

Non-steroidal anti-inflammatory drugs in use

NSAIDs are commonly used today to treat many conditions associated with pain and inflammation. Due to their anti-inflammatory action and ability to reduce joint swelling, NSAIDs are widely prescribed for rheumatoid arthritis and osteoarthritis treatment. NSAIDs are also used to treat gout attacks, bursitis, tendonitis; they are also used to relieve menstrual cramps and renal colics. Headache and migraines are also among the diseases, treated with NSAIDs.

Thanks to the blood thinning action of some NSAIDs (e.g. aspirin), these medications can be prescribed to prevent arteries thrombosis. Aspirin is known as a cardio-protective medication.

Due to ability to lower high body temperature, NSAIDs are often included into complex medications to treat colds and flu.

NSAIDs Mode of Action

The exact mode of action of NSAIDs remained a secret for scientists until 1970th. Now it is known that non-steroidal anti-inflammatory drugs work by inhibiting or suppressing the production of prostaglandins in the human organism.

Prostaglandins are special chemicals, which promote pain, inflammation, and fever in humans. These chemicals are produced by enzyme cyclooxygenase (COX enzyme). NSAIDs suppress the activity of COX enzymes and thus reduce the amount of prostaglandins produced by body cells. As the result, the reduction of pain and inflammation is achieved.

However there are two types of COX enzymes: COX-1 and COX-2. COX-1 enzymes are characterized with one specific feature – these chemicals are responsible for the formation of protective lining in the human stomach, which protects it from the negative influence of digestive acids. That is why all traditional NSAIDs not only reduce pain and inflammation, but also negatively influence digestive tract, reducing its protective layer, which often results in stomach bleeding and ulcers. COX-2 inhibitors, such as Celebrex, Vioxx and Bextra were called to eliminate this adverse reaction, because they were designed to inhibit only COX-2 enzymes without affecting COX-1 chemicals.

In fact, the goal was achieved - new selective NSAIDs demonstrated the reduction of risks to develop gastrointestinal problems. However, a new problem arose – when used for a long period   of time (which is necessary in the treatment of such disorders as arthritis), selective COX-2 NSAIDs caused serious heart problems, which led to deaths of patients. As the result, Vioxx and Bextra were removed from the market, since the risks of their use exceeded the benefits provided by those medications. Celebrex, another COX-2 inhibitor, still remains available on the market by prescription.

In spite of the many disputable issues entailed by the introduction of COX-2 inhibitors, non-steroidal anti-inflammatory drugs as a class remain among the most popular medications around the word. Traditional NSAIDs are still the first-line option to relieve pain, reduce inflammation and fever, associated with many common disorders.

 
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