NSAIDs types, uses, contraindications, and their relation to ulcers

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In a previous article about prostaglandins, we talked about the formation of PGs. Also, we mentioned their effects and functions in details. This article is about diminishing the bad effects of prostaglandins coming from cox 2, the bad guy. Before starting, I highly recommend you to read the post about prostaglandins to fully understand how the NSAIDs work. The abbreviation NSAIDs stands for non steroidal anti-inflammatory drugs.

The body has many immune responses, among which is the inflammation. Basically, it’s the final result of the actions triggered by prostaglandins from cox 2 metabolic pathway. Hence mainly in order to cease the inflammation, the synthesis of cox 2 prostaglandins should be prevented. That is exactly what NSAIDs do to counteract inflammation.

Cox enzymes, cyclooxygenase enzymes, or cyclooxygenases are the enzymes involved in formation of prostaglandins. There are 3 cox enzymes, cox 1, cox 2, and cox 3. Frankly, the two most known are cox 1 and cox 2. Many of the non steroidal anti-inflammatory drugs are non selective and inhibit both cox 1 and cox 2. 

NSAIDs mechanism of action

Both cox 1 and cox 2 are similar in many aspects, except that each of them has its distinct set of actions. Cox 2 is responsible for inflammation and fever. Cox 1 do other functions such as protecting gastric mucosa/stomach lining from the gastric acid naturally produced. In addition, cox 1 has a role in platelets aggregation and sticking together to form clots. Both of the cox enzymes reduce blood flow to the kidneys.

NSAIDs have always been known as the commonly prescribed medications used to bring down the inflammation, fever, and pain. They have great efficacy to reduce the body temperature during fevers.

Taking a non steroidal anti-inflammatory drug with no selectivity to cox enzymes is not always a good choice. But also, it’s not usually a bad choice. It can lead to ulcers in stomach and cause bleeding when excessively used. Simply as the prostaglandins coming from the pathway in which cox 1 is involved, are reduced. PGs coming from cox 1 are very crucial in maintaining the stomach lining. Moreover, they have various beneficial effects.

NSAIDs classification

According to inhibiting both cox enzymes or only cox 2, NSAIDs are classified. Those which non selectively inhibit cox enzymes are called non selective, classic, or traditional NSAIDs. Whereas those which selectively inhibit cox 2 only, are known as selective or newer NSAIDs.

Non selective/classic NSAIDs

Their pharmacological action is done via inhibiting both cox 1 and cox 2. Again, I’m repeating this substantial emphasis and rehearsal for the danger that may occur  Particularly if taken too much and for the long run. Simply because they impair and decrease the formation of mucus layer lining the stomach. Later, the stomach lining will be irritated and this mainly will cause gastric ulcer !

Selective/newer NSAIDs

  • Celecoxib
  • Rofecoxib
  • Etoricoxib
  • Meloxicam

Targeting the cox 2 only is much beneficial and low-risk treatment. Inhibiting cox 2 selectively ensures the bad PGs are greatly decreased. The PGs that are responsible for pain and inflammation.

Natural cox inhibitors

Apart from medications, the newer and the classic NSAIDs, there are also natural inhibitors of cox enzymes. Culinary mushrooms have partial ability in inhibiting cox 1 and cox 2. Flavonoids, or bioflavonoids, which are secondary metabolites found in some plants, can inhibit cox 2. Fish oils are also natural inhibitors of cox enzymes.

NSAIDs classification

The main uses of NSAIDs

  1. Fever/pyrexia
  2. Migraines and headaches
  3. Rheumatoid arthritis
  4. Osteoarthritis
  5. Ankylosing spondylitis
  6. Pain after operations
  7. Reiter’s syndrome
  8. Pains of the menstrual cycle
  9. Inflammations and injuries of tissues
  10. For prevention of clots formation (especially aspirin)

General contraindications of NSAIDs

  • Asthma and urticaria in response to NSAIDs
  • Gastric or duodenal ulcer
  • Active bleeding in the GIT
  • Pregnancy and lactation
  • Rhinitis

Side effects of NSAIDs

  1. Headache and dizziness
  2. Dyspepsia and nausea
  3. Hypertension and dry eyes
  4. Gastrointestinal ulceration or bleeding
  5. Salt and fluid retention
  6. Diarrhea
  7. Elevated level of liver enzymes

Always remember that a medication with all its benefits, may also harm you. Never believe the myth saying that a medication can be 100% safe. NSAIDs like plenty of other medicines, are dispensed with prescriptions. Do not ever hesitate to consult a pharmacist or physician about a medication. Your health is so precious :)