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Non-steroidal anti-inflammatory drugs (NSAIDs) are drugs, which are used to comfort pain and have anti fever effects. This causes the drug to have an anti inflammatory response, which is another, feature which works in favour for the drug.
NSAIDs can be prescribed to a patient in order to relieve pain in arthritis and also reduce stiffness, however it is not a cure. They have several different dosage forms, which can give a patient a variety of taking the drug with the type they feel at most comfortable with. Found in the forms as a; tablet, capsules, liquid suspensions, suppositories or topical cream/gel. However once the drug is taken it is a 'quick worker'. So as soon as you take a dosage it only takes at most several hours to cause a difference to a patient i.e. relieve pain and reduce soreness of bones.
As many drugs do, NSAIDs also have many side effects. Side effects range from; Stomach upsets, heartburn, indigestion, fluid retention and a minute risk in heart disease. So in effect when patients take these drugs depending on our health the benefits have to outweigh the disadvantages created by the side effects. Factors that need to be taken into account about the patient are if they have asthma, high blood pressure and kidney problems.
The theory of the mechanism of action of NSAIDs drugs has been the same in the past twenty-five years (VANE J. R et al BOTTING R. M, 1996). NSAIDs are used to block cyclo-oxgenase enzymes in order to reduce the amount of prostaglandins formed. Prostaglandins are part of the lipid group and have distinct physiological effects on animals. When COX-1 enzymes are activated they produce prostaglandins which then are released by the endothelium causes an blood clotting response, which can be helpful when a person has case of atherosclerosis. However if the mucous membrane layer in the stomach releases these prostaglandins the outcome is an increase in protection for cells from harmful chemicals, working in safety for the body. However the main reason these drugs are taken is to relieve pain.
There are many drugs which are included to be NSAIDs; Aspirin, Ibuprofen and naproxen.
Aspirin is a painkiller, and an antipyretic. Furthermore aspirin has anti platelet stickiness effect, so stopping the formation of blood clots. Therefore reduces risk of atherosclerosis. Aspirin also is used in minor occasions such as for relieving headaches or reducing fevers. This is a common trait in all the types of NSAIDs. The mechanism of aspirin (J. R. Vane et al R. M. Botting, 2003) uses mainly two enzymes, COX-1 and COX-2. As aspirin activity in the body is not specific to a body part so it inhibits these enzymes anywhere aspirin activity is worked in the body. This method of inhibition cannot be reversed. COX- enzymes are responsible for the production of prostaglandins, which help in blood clotting and inflammatory responses. COX-2 made from aspirin releases lipoxins that help limit the inflammatory response in the body. Therefore Aspirin's effect on the prostaglandin is to suppress the production of it, thus as mentioned earlier leads to inactivation of the COX enzymes. Along with prostaglandins, it also suppresses the enzyme called 'Thromboxane'. Thromboxane is an enzyme found in blood platelets, which helps cause blood to clot. This causes another inhibition of platelet aggregation, thereby giving Aspirin its anticoagulant effects.
Aspirin gives three main types of effects in the body; these are Anti-inflammatory response, Antipyretic response and analgesic effects. In anti-inflammatory response given by taking in aspirin means having a response, which inhibits inflammation in the body. This may mean the reduction of histamine released in areas of soreness in the body. Causing a less reddening effect show in the skin. So in the intake of aspirin the drug diminishes COX activity, which means no production of the lipid, which may be used as a substrate to cause a reaction to activate the release of histamine around the body. An antipyretic effect is found to reduce fever. Fever is reduced by lowering the body temperature this change is called an antipyretic effect. Painkillers are also one of the responses given aspirin; this response is called an Analgesic effect.
Cyclo-oxgenase (COX) also known as Prostaglandin H Synthase-1 (Alexey Goltsova, Anton Maryashkinb, Maciej Swatc, Yuri Kosinskyb, d, Ian Humphery-Smithe, Oleg Deminc, d, Igor Goryanina and Galina Lebedevaa, 2009) has two active sites in its structure meaning it is a bifunctional enzyme. The definition of bifunctional enzymes is given as [A]' an enzyme containing two distinct catalytic capacities in the same polypeptide chain'. Enzymes are globular proteins which means they are responsible for the metabolic reactions in living organisms. They are also tertiary structure proteins. Tertiary structure proteins are three-dimensional coil of polypeptides that are more tightly packed together than secondary and primary structure proteins.
I will now talk about the method of Inhibition of cyclo-oxgenase enzymes, which have the main effect an NSAID gives. In NSAIDs there is competitive inhibition; this is when the inhibitor is similar shape to the substrate and binds into the active site of the cyclo-oxgenase enzyme, therefore the enzyme to be halted from doing its job as the substrate cannot bind to the active of the enzyme as the inhibitor found in Aspirin is blocking its path.
Aspirin has many side effects, I will be mentioning about the two main side effects which are Gastric secretion and ischemia.
Gastric Secretion has three stages, Cephalic phase, Gastric phase and the Intestinal phase. In the cephalic phase this is when the thought of food, taste of food in the mouth or smell of food sends nerve impulses to the medulla oblongata in the brain. Nerve impulses are sent back from the medulla to the stomach where the stimulation causes hydrochloric acid and pepsin to be secreted in the stomach. This nerve impulse is sent via the vagus nerve and causes another secretion of gastric in the lower parts of the stomach. Gastrin is then taken through the bloodstream and causes stimulation of more secretion of hydrochloric acid and pepsin the other parts of the stomach. The next stage is the Gastric phase. In this phase food has entered the stomach, causing more nervous stimulations to the brain and thus causing more secretion of hydrochloric acid and pepsin. Finally the last stage of gastric secretion is the intestinal phase. This is when partially digested food that has been pushed to the duodenum (small intestine). Therefore gastric secretion is no longer necessary. So when taking aspirin there is an excess of gastric secretion occurring therefore leading to a higher intensity of acid and gastric acid build up, causing pain and burning sensations around the body.
Ischemia is a restricted flow of blood flow, which may lead to damaged tissues and amputations of certain areas in the body. It occurs due to a series of vaso-constrictions (constriction of the arterioles) and blockage of blood vessels, interrupting blood flow to organs. Ischemia is dangerous as it can lead to heart attacks and even strokes if the blood vessel interrupted is lead to the brain.
Another drug, which can be classified as an NSAID, is Paracetamol. It is used to treat headaches, colds and other sort of body pains. However paracetamol does not have many anti-inflammatory effects therefore it is sometimes not referred to as an NSAID. However it still has Antipyretic and analgesic. Therefore it has two out of the three main benefits an NSAID has. Therefore we can conclude that it has the same mechanism as an NSAID to bring about these benefits.
Ibuprofen or 'Brufen' is another well-known NSAID. Mainly used to ease arthritis pain and reduce fevers like aspirin. However Ibuprofen is a short-term remedy for pain unlike its cousin Aspirin.
Naproxen is a strictly for pain relief in a number of different cases; Arthritis, Kidney stones and Menstrual cramps. It Inhibits both COX-1 and COX-2 enzymes. Another type of cyclo-oxgenase enzyme is COX-2. It is turned on by an inflammatory stimulus and cytokines (VANE J. R et al BOTTING R. M, 1996). Cytokines are proteins released by the nervous and immune systems in the body, they help out with the cell-to-cell communication. COX-2 is responsible for the anti inflammatory effects found in NSAIDs as the inhibition of COX-2 causes it not to be activated by an inflammatory stimulus. Therefore we may say that the inhibition of COX-1 enzyme is found to be responsible for the side effects found in NSAIDs.
The Ideal NSAID drug would have a higher COX-2 inhibition activity than a COX-1 inhibition activity. This ideal drug would give a higher anti-inflammatory response and fewer side effects creating a most effective drug. If a drug had a lower COX-2 inhibition activity and a higher COX-1 inhibition activity therefore the drug would be the least effective as it would give more problems than benefit as it would give the patient taking the drug more effect of side effects than any anti inflammatory effects.
Non-Steroidal Anti-Inflammatory Drugs have many contraindications. Contraindications is guidance on when not to use the drug [B]
'Allergy to aspirin or any NSAID
Aspirin should not be used under the age of 16 years
During breast feeding
On blood thinning agents (anticoagulants)
Suffering from a defect of the blood clotting system (coagulation)
Active peptic ulcer
Care is needed if you have:
If NSAIDs were taken and you have any of the conditions above, this could prove to be dangerous and you will need to contact a doctor as soon as possible.
The main mechanism of NSAIDs and first occurrence, which happens when taking the drugs, is the competitive inhibition of the cyclo-oxgenase enzymes. This in turn causes a stop in the production of prostaglandins. In aspirin this causes an Anti-inflammatory, Antipyretic and analgesic response. However these responses also have many side effects, like gastric secretion or Ischemia, which can lead to either pains caused by excess acidity in the body or atherosclerosis. In other medicines like naproxen, we are able to say that in an optimum NSAID we require a high COX-2 inhibitor activity and a low COX-1 inhibitor activity.