Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Uses, Side Effects

Nonsteroidal anti-inflammatory drugs
(usually abbreviated to NSAIDs) are a group of medicines that relieve pain and
fever and reduce inflammation.

There are nearly two dozen different NSAIDs available, but they all work in the same way, and that is by blocking a specific group of enzymes called cyclo-oxygenase enzymes, often abbreviated to COX enzymes. These enzymes are responsible for the production of prostaglandins. Prostaglandins are a group of compounds with hormone-like effects that control many different processes such as inflammation, blood flow, and the formation of blood clots.

What are nonsteroidal anti-inflammatory
agents used for?

NSAIDs are used to treat mild-to-moderate
pain that arises from a wide range of conditions such as headaches,
menstruation, migraines, osteoarthritis or rheumatoid arthritis, sprains and
strains, and toothache.

Aspirin is a NSAID that is used in small
doses to lower the risks of having a heart attack or a stroke caused by a blood
clot. It may also be given as a single dose at the time of a heart attack to
improve outcomes. This is because it irreversibly inhibits the COX-1 enzyme.

What are the differences between
nonsteroidal anti-inflammatory agents?

NSAIDs may be grouped according to their
preference for COX-1 and COX-2 enzymes. Those that favor COX-1 are more likely
to cause gastrointestinal side effects. Those that favor COX-2 have a higher
risk of cardiovascular effects but less gastrointestinal effects. Higher
dosages of NSAIDs tend to result in more COX-2 enzyme inhibition (and more
cardiovascular side effects), even in those NSAIDs traditionally seen as low
risk (such as ibuprofen). NSAIDs with higher activity against COX-2 enzymes
should be used with caution in people with cardiovascular disease or at
increased risk of cardiovascular disease.

Both types of COX enzymes produce
prostaglandins; however, the main function of COX-1 enzymes is to produce
baseline levels of prostaglandins that activate platelets and protect the
lining of the gastrointestinal tract, whereas COX-2 enzymes are responsible for
releasing prostaglandins after infection or injury.

Most NSAIDs inhibit both enzymes to a
certain extent.

Are nonsteroidal anti-inflammatory agents

NSAIDs are one of the most widely
prescribed group of medicines; however, they are associated with some serious
side effects.

NSAIDs can increase your risk of a fatal
heart attack or stroke. The risk increases the higher the dosage and the longer
the length of time you remain on an NSAID for. People with pre-existing heart
disease are more at risk and certain NSAIDs, such as diclofenac and celecoxib,
have been linked to more heart-related side effects than others. NSAIDs should
never be used just before or after heart bypass surgery (coronary artery bypass
graft, or CABG).

Gastrointestinal (GI) side effects are also
common, and usually related to dosage and duration of treatment although some
NSAIDs, such as ketorolac, aspirin and indomethacin, are associated with a
higher risk. Elderly people or those taking other medicines that irritate the stomach
are more likely to experience life-threatening GI side effects, such as stomach
or intestinal bleeding.

Most NSAIDs are not suitable for children
or adolescents under the age of 18 years. Ibuprofen is the only NSAID approved
for children aged three months and older.

Most NSAIDs should not be taken during the
last three months of pregnancy or while breastfeeding except on a doctor’s

Side effects

NSAIDs can potentially cause a range of
side effects, especially when used at higher than recommended dosages for long
periods of time. General side effects include:

Gastrointestinal side effects that may
occur include bloating, diarrhea, constipation, irritation of the lining of the
stomach, nausea or vomiting.

NSAIDs may also affect kidney function and
reduce how quickly blood flows through the kidneys. They may cause retention of
sodium and water which can lead to edema and high potassium levels.
Occasionally, they may cause more serious damage to the kidneys.

Some NSAIDs, particularly diclofenac and
those that are selective for COX-2 enzymes, have a high risk of cardiovascular
thrombotic events such as a heart attack or stroke. Other heart-related side
effects such as high blood pressure, congestive heart failure, and palpitations
have also been reported.

In addition, some people taking NSAIDs have
experienced asthma attacks, bleeding, fatigue, headache, insomnia, low
neutrophil levels, urticaria (hives), vertigo and seizures. Reye’s syndrome, a
life-threatening condition that causes swelling in the liver and brain and is
mostly associated with aspirin use in young children has also been reported.

Keywords: nonsteroidal anti-inflammatory
drugs; NSAIDs.

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