Nonsteroidal anti-inflammatory drugs

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are medications that reduce inflammation (swelling) and pain (analgesic). The term "nonsteroidal" is used to distinguish the drugs from steroids. Unlike NSAIDs, steroidal drugs are synthetic hormones that are used to stop the inflammatory response in the body. NSAIDs are non-narcotic, and therefore, non-addictive.
Most people are familiar with over-the-counter (OTC) NSAIDs, such as ibuprofen (Motrin® or Advil®) or naproxen (Aleve® or Naprosyn®). Most NSAIDs, including ibuprofen, help reduce low-grade (continuous or fluctuating) fevers and prevent blood from clotting in the veins or arteries. NSAIDs are available in the form of pills, oral solutions, injectable solutions, suppositories, and topical creams, gels, and foams.
While acetylsalicylic acid (Aspirin®) is often referred to as an NSAID, it does not truly fall under this category. Although it is also used to relieve inflammation and pain, acetylsalicylic acid is considered a salicylate.
The frequency and severity of side effects vary among NSAIDs. The most common side effects include nausea, vomiting, diarrhea, constipation, decreased appetite, rash, dizziness, headache, and drowsiness.
The U.S. Food and Drug Administration (FDA) requires that all NSAIDs print serious warning labels that highlight the risk of potential heart-related side effects and stomach bleeding. The labels must also state that patients who have recently had heart surgery should not take NSAIDs.

Related Terms

Analgesic, anti-inflammatory, arthritis, COX-1, COX-2, COX enzymes, cyclooxygenase, cyclooxygenase-1, cyclooxygenase-2, diclofenac, duodenal ulcers, etodolac, fever, heart disease, ibuprofen, inflammation, inflammatory response, naproxen, non-allergic drug reaction, non-narcotic, nonsteroidal, OTC drugs, over-the-counter drugs, pain relief, pain reliever, peptic ulcers, prostaglandins, rheumatoid arthritis, stomach ulcers, swelling, ulcers.

function

General: There are two main types of cyclooxygenase enzymes in the blood: cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Both of these enzymes produce prostaglandins, which are substances that cause inflammation. COX-1 enzymes protect the stomach lining from harsh acids and digestive chemicals and help maintain kidney function. The body produces COX-2 enzymes when the joints are injured or inflamed.
Traditional (non-selective) NSAIDs: Traditional NSAIDs (such as ibuprofen and naproxen) block the actions of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. However, since the COX enzymes are needed to protect the stomach and maintain kidney function, traditional NSAIDs may cause indigestion, duodenum or stomach ulcers, or kidney damage.
Non-traditional NSAIDs (selective COX-2 inhibitors): COX-2 inhibitors are only available by prescription. These drugs only target the COX-2 enzyme that stimulates inflammation. Currently, the U.S. Food and Drug Administration has only approved one COX-2 inhibitor called celecoxib (Celebrex®).
Since these medications do not block the actions of the COX-1 enzyme, these medications generally do not cause the kind of stomach upset that is often associated with traditional NSAIDs. COX-2 inhibitors are often prescribed for long-term conditions such as arthritis because they may be safer for the stomach. However, some studies have not shown any difference between the incidence of gastrointestinal side effects from traditional NSAIDs and COX-2 inhibitors. Also, COX-2 inhibitors do not offer the same kind of protection against heart disease as traditional NSAIDs.

uses

NSAIDs are primarily used to reduce inflammation, pain (mild to moderate), and low-grade fever. The anti-inflammatory effects may take anywhere from a few days to three weeks to initiate.
Specific uses include the treatment of headaches, arthritis (including osteoarthritis and rheumatoid arthritis), back pain, sciatica (pain extending from lower back down the leg), pain after surgery, fever, dental pain, kidney stone pain, sports injuries, menstrual cramps, tendonitis (inflamed tendons), and other painful conditions (especially where there is inflammation).
NSAIDs are also added to many cold and allergy drugs to relieve symptoms such as minor aches and pains, headaches, and fevers.

non-allergic drug reactions

Some patients taking nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen (Advil® or Motrin®), may experience non-allergic drug reactions that may cause symptoms similar to drug allergies. Symptoms of non-allergic drug reactions include difficulty breathing, wheezing, cough, tightening in the chest, hives, nasal congestion, watery eyes and, occasionally, facial flushing and swelling. Asthmatics and especially asthmatics who also have nasal polyps, are vulnerable to asthma as a side effect of NSAIDs. However, such reactions to NSAIDs do not involve the immune system, and are therefore not considered allergic reactions. Instead they are considered side effects of the medication.
A non-allergic drug reaction occurs because NSAIDs inhibit the cyclooxygenase-1 (COX-1) enzyme. When COX-1 is inhibited, other enzymes in the body are able to cause severe side effects, such as difficulty breathing and wheezing, in some patients. For instance, one of these enzymes triggers the release of chemicals that cause the airways to swell and increase mucus production, which leads to an asthma attack. Therefore, this reaction is considered an unwanted side effect of the drug, not an allergic reaction.

formulations

Oral:Nonsteroidal anti-inflammatory drugs (NSAIDs) can be taken orally as liquids, tablets, or capsules. Oral NSAIDs are the most widely used form. Examples of over-the-counter traditional NSAIDs that are taken by mouth include ibuprofen (Motrin® or Advil®), aspirin and naproxen (Aleve®). Examples of prescription oral NSAIDs include diclofenac (Cataflam® or Voltaren®-XR), celecoxib (Celebrex®), and etodolac (Lodine®).
Injections: Some NSAIDs like ibuprofen lysine (Neoprofen®) are available as injections. Intravenous NSAIDs are used to treat the pain after surgery, as well as pain caused by kidney stones.
Suppositories: Suppositories are also available. These are typically used for pain after surgery. They may also be used to relieve chronic pain when the patient is unable to take medication by mouth.
Creams, gels, and foams: NSAIDs are also available in creams, gels, and foams, which are applied to the skin to treat conditions such as osteoarthritis. For instance, diclofenac (Solaraze®) is applied to the knee to relieve pain associated with knee osteoarthritis. Topical NSAIDs are considered the least effective form.

side effects

The U.S. Food and Drug Administration (FDA) requires that all nonsteroidal anti-inflammatory drugs (NSAIDs) print serious warning labels that highlight the risk of potential heart-related side effects and stomach bleeding. The labels must also state that patients who have recently had heart surgery should not take NSAIDs.
The frequency and severity of side effects vary NSAIDs. The most common side effects include nausea, vomiting, diarrhea, constipation, decreased appetite, rash, dizziness, headache, and drowsiness. The most serious side effects include kidney failure, liver failure, ulcers, and prolonged bleeding after an injury or surgery. About 15% of patients on long-term NSAID treatment develop ulceration of the stomach and duodenum.
Phenylbutazone (Butazolidine®), a prescription NSAID (not available in the United States), is especially likely to cause serious side effects, including immunosuppression, which makes patients vulnerable to infection and disease.
NSAIDs may also cause fluid retention, which may lead to edema (fluid in the body tissues). Edema often causes swelling in the arms and legs.
Patients who have asthma may develop shortness of breath and are at an increased risk of experiencing a non-allergic drug reaction to NSAIDs.
Patients who are allergic to one type of NSAID are likely to experience a similar reaction to other types of NSAIDs.

precautions

Avoid with a history of peptic ulcers because nonsteroidal anti-inflammatory drugs (NSAIDs) increase the risk of developing duodenal or stomach ulcers.
Avoid with history of kidney or liver damage because NSAIDs may increase the risk of developing kidney or liver failure.
Avoid with indigestion or heartburn because NSAIDs may cause upset stomach or indigestion.
Avoid in patients who consume three or more alcoholic drinks a day because heavy drinkers may have an increased risk of developing liver damage and stomach bleeding from NSAIDs.
Do not take antacids or eat fatty foods with COX-2 inhibitors because they limit the body's ability to absorb the medication.
Do not take traditional NSAIDs (prescription or over-the-counter) with celecoxib (Celebrex®), the only selective COX-2 inhibitor approved by the U.S. Food and Drug Administration (FDA).
Use cautiously with asthma because NSAIDs may cause shortness of breath. Also, asthma patients are at an increased risk of experiencing a non-allergic drug reaction to NSAIDs.
Use cautiously with bleeding disorders because NSAIDs may cause prolonged bleeding after an injury or surgery.
Use cautiously if pregnant or breastfeeding. NSAIDs may damage the heart or blood flow of the fetus or newborn baby if they are taken regularly during the last few months of pregnancy. Some animal studies have shown that if NSAIDs are taken late in pregnancy, they may increase the length of pregnancy, prolong labor, or cause complications during delivery. Pregnant mothers should consult a qualified healthcare provider before taking NSAIDs. Although NSAIDs have not been shown to cause medical problems in breastfeeding babies, diclofenac (Cataflam® Voltaren®-XR), diflunisal (Dolobid®), fenoprofen (Nalfon®), flurbiprofen (Ansaid®), meclofenamate (Meclofenamate sodium®), mefenamic acid (Ponstel®), naproxen (Aleve®), piroxicam (Feldene®), and tolmetin (Tolectin® or Tolectin® DS) can pass into breast milk. Caution is warranted.