Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of medications commonly used to relieve pain, reduce inflammation, and lower fever. They work by inhibiting the activity of cyclooxygenase (COX) enzymes, which are responsible for producing prostaglandins. Prostaglandins promote inflammation, pain, and fever, so reducing their production helps alleviate these symptoms.
Pain relievers are medicines that reduce or relieve headaches, sore muscles, arthritis, or other aches and pains. There are many different pain medicines, and each one has advantages and risks. Some types of pain respond better to certain medicines than others. Each person may also have a slightly different response to a pain reliever.
Over-the-counter (OTC) medicines are good for many types of pain. There are two main types of OTC pain medicines: acetaminophen (Tylenol) and nonsteroidal anti-inflammatory drugs (NSAIDs). Aspirin, naproxen (Aleve), and ibuprofen (Advil, Motrin) are examples of OTC NSAIDs.
If OTC medicines don’t relieve your pain, your doctor may prescribe something stronger. Many NSAIDs are also available at higher prescription doses. The most powerful pain relievers are opioids. They are very effective, but they can sometimes have serious side effects. There is also a risk of addiction. Because of the risks, you must use them only under a doctor’s supervision.
There are many things you can do to help ease pain. Pain relievers are just one part of a pain treatment plan.
Nonsteroidal anti-inflammatory drugs — are among the most common pain relief medicines in the world. Every day more than 30 million Americans use them to soothe headaches, sprains, arthritissymptoms, and other daily discomforts, according to the American Gastroenterological Association.
And as if that wasn’t enough, in addition to dulling pain NSAIDs also lower fever and reduce swelling.
How NSAIDs Work:
- COX-1: This enzyme is involved in protecting the stomach lining and regulating blood platelets. Inhibiting COX-1 can lead to gastrointestinal side effects like ulcers and bleeding.
- COX-2: This enzyme is induced during inflammation. Selective COX-2 inhibitors (like Celebrex) target only this enzyme, reducing inflammation with fewer gastrointestinal side effects compared to non-selective NSAIDs.
But how do those little pills do so much? And if they’re so good in some ways, why do they also raise the risk of heart problems in some people?
The answer is complicated. Even researchers don’t fully understand how NSAIDs work.
Nonetheless, with the benefits and risks of NSAIDs in the headlines frequently, WebMD turned to four experts for a rundown of what researchers do know. Our panel consisted of:
- Byron Cryer, MD, a spokesman for the American Gastroenterological Association and an associate professor of medicine at the University of Texas Southwestern Medical Center in Dallas.
- Nieca Goldberg, MD, a spokeswoman for the American Heart Association and chief of Women’s Cardiac Care at Lennox Hill Hospital in New York.
- John Klippel, MD, president and CEO of the Arthritis Foundation in Atlanta.
- Scott Zashin, MD, clinical assistant professor at the University of Texas Southwestern Medical Center in Dallas and author of Arthritis Without Pain.
For What Conditions Are NSAIDs used?
NSAIDs are used primarily to treat inflammation, mild to moderate pain, and fever.
Specific uses include the treatment of:
- headaches,
- arthritis,
- ankylosing spondylitis,
- sports injuries,
- menstrual cramps,
- Pain relief (e.g., headaches, muscle pain, toothaches)
- Reducing inflammation (e.g., in arthritis, tendinitis)
- Lowering fever (antipyretic effect)
- Managing chronic conditions (e.g., osteoarthritis, rheumatoid arthritis)
- Post-surgical pain management
Ketorolac (Toradol) is only used for short-term treatment of moderately severe acute pain that otherwise would be treated with narcotics.
Aspirin (also an NSAID) is used to inhibit the clotting of blood and prevent strokes and heart attacks in individuals at high risk for strokes and heart attacks.
NSAIDs also are included in many cold and allergy preparations.
Celecoxib (Celebrex) is used for treating familial adenomatous polyposis (FAP) to prevent the formation and growth of colon polyps.
Types of NSAIDs:
There are two main categories of NSAIDs:
- Non-selective NSAIDs: These block both COX-1 and COX-2 enzymes.
- Selective COX-2 inhibitors: These mainly block COX-2, reducing inflammation with fewer gastrointestinal side effects.
Detailed Listing of NSAIDs:
1. Non-selective NSAIDs (COX-1 and COX-2 Inhibitors)
- Aspirin (Acetylsalicylic Acid)
- Brand names: Bayer, Bufferin
- Commonly used for pain relief, fever reduction, and heart attack prevention (in low doses).
- Ibuprofen
- Brand names: Advil, Motrin
- Used for pain, inflammation, and fever. Available over-the-counter and in higher prescription doses.
- Naproxen
- Brand names: Aleve, Naprosyn
- Longer-acting NSAID for pain and inflammation, often used for arthritis and menstrual cramps.
- Diclofenac
- Brand names: Voltaren, Cataflam
- Available in oral, topical, and patch forms. Commonly used for arthritis and joint pain.
- Indomethacin
- Brand names: Indocin
- Potent NSAID used for conditions like rheumatoid arthritis, osteoarthritis, and gout.
- Ketoprofen
- Brand names: Orudis, Actron
- Used for pain, swelling, and inflammation. Available over-the-counter and in prescription strength.
- Ketorolac
- Brand names: Toradol
- A powerful NSAID used for short-term management of moderate to severe pain, typically in hospitals.
- Piroxicam
- Brand names: Feldene
- Often used for long-term management of chronic pain, such as in arthritis.
- Sulindac
- Brand names: Clinoril
- Prescribed for long-term treatment of arthritis and gout.
- Meloxicam
- Brand names: Mobic
- A slightly selective COX-2 inhibitor, used for osteoarthritis and rheumatoid arthritis.
- Fenoprofen
- Brand names: Nalfon
- Used to treat pain, inflammation, and arthritis symptoms.
- Flurbiprofen
- Brand names: Ansaid
- Often used for arthritis, and sometimes as a topical eye treatment for inflammation during eye surgery.
- Meclofenamate
- Brand names: Meclomen
- Used for arthritis and dysmenorrhea (menstrual pain).
- Oxaprozin
- Brand names: Daypro
- A long-acting NSAID, used mainly for chronic pain and inflammation in arthritis.
- Tolmetin
- Brand names: Tolectin
- Primarily used for juvenile rheumatoid arthritis, osteoarthritis, and rheumatoid arthritis.
2. Selective COX-2 Inhibitors (Coxibs)
These are designed to reduce inflammation with fewer gastrointestinal side effects by selectively inhibiting the COX-2 enzyme.
- Celecoxib
- Brand names: Celebrex
- Commonly used for arthritis, acute pain, and menstrual pain. It’s a selective COX-2 inhibitor, reducing the risk of stomach issues compared to traditional NSAIDs.
- Rofecoxib (withdrawn from the market)
- Brand names: Vioxx
- Was used for arthritis and pain relief, but withdrawn due to increased cardiovascular risks.
- Valdecoxib (withdrawn from the market)
- Brand names: Bextra
- Similar to Celebrex, but withdrawn due to heart risks and serious skin reactions.
- Etoricoxib (not available in the U.S.)
- Brand names: Arcoxia
- Used in some countries for arthritis and other painful conditions.
- Parecoxib
- Brand names: Dynastat
- Available in an injectable form, used for post-surgical pain.
Are There any Differences Between NSAIDs?
NSAIDs vary in their potency, duration of action, how they are eliminated from the body, how strongly they inhibit COX-1 versus COX-2 and their tendency to cause ulcers and promote bleeding. The more an NSAID blocks COX-1, the greater is its tendency to cause ulcers and promote bleeding. One NSAID, celecoxib (Celebrex), blocks COX-2 but has little effect on COX-1, and is therefore further classified as a selective COX-2 inhibitor. Selective COX-2 inhibitors cause less bleeding and fewer ulcers than other NSAIDs.
Aspirin is a unique NSAID, not only because of its many uses, but because it is the only NSAID that inhibits the clotting of blood for a prolonged period of time (4 to 7 days). This prolonged effect of aspirin makes it an ideal drug for preventing blood clots that cause heart attacks and strokes.
Most NSAIDs inhibit the clotting of blood for only a few hours. Ketorolac (Toradol) is a very potent NSAID and is used for moderately severe acute pain that usually requires narcotics. Ketorolac causes ulcers more frequently than other NSAID. Therefore, it is not used for more than five days. Although NSAIDs have a similar mechanism of action, individuals who do not respond to one NSAID may respond to another.
For more information about NSAIDs, please check following links:
What is Nonsteroidal anti-inflammatory drugs (NSAIDs) and How many NSAIDs Approved in United States?
What Are the Side Effects of NSAIDs ?
Nonsteroidal anti-inflammatory drugs (NSAIDs) are effective for relieving pain, reducing inflammation, and lowering fever, but they can also cause side effects, especially with long-term use or at higher doses. These side effects range from mild to serious, affecting different parts of the body.
Common Side Effects:
These are generally mild and can improve as your body adjusts to the medication:
- Stomach Issues:
- Stomach pain or discomfort
- Nausea and indigestion
- Heartburn
- Diarrhea or constipation
- Headaches and Dizziness:
- Mild headache
- Feeling lightheaded or dizzy
- Fluid Retention:
- Swelling (edema) in the hands, feet, or legs due to fluid retention.
- Increased Blood Pressure:
- NSAIDs can increase blood pressure, which is more common in people with pre-existing hypertension.
- Rash or Skin Irritation:
- Itching or rash can occur in some people, especially with topical NSAID formulations.
Serious Side Effects:
These can be more dangerous, especially when NSAIDs are taken for long periods or in higher doses. People with pre-existing health conditions (heart disease, kidney issues, etc.) are at higher risk.
1. Gastrointestinal (GI) Problems:
NSAIDs block COX-1, which helps protect the stomach lining, so they increase the risk of:
- Stomach ulcers: Open sores in the lining of the stomach or intestines.
- Gastrointestinal bleeding: Symptoms include black, tarry stools, vomiting blood, or severe stomach pain.
- Gastritis: Inflammation of the stomach lining.
2. Cardiovascular Risks:
Long-term use of NSAIDs, especially in high doses, can increase the risk of:
- Heart attack (myocardial infarction)
- Stroke
- Blood clots
- Worsening of heart failure or increased risk of heart-related complications, particularly with selective COX-2 inhibitors like Celebrex.
3. Kidney Damage:
NSAIDs can reduce blood flow to the kidneys, potentially leading to:
- Acute kidney injury or worsening of chronic kidney disease.
- Kidney failure in severe cases, especially in people with pre-existing kidney problems, dehydration, or heart conditions.
- Symptoms may include reduced urine output, swelling, and fatigue.
4. Liver Damage:
While less common, NSAIDs can cause:
- Liver damage or hepatitis (inflammation of the liver), leading to symptoms like yellowing of the skin or eyes (jaundice), fatigue, and dark urine.
- Elevated liver enzymes on blood tests.
5. Allergic Reactions:
Some individuals may experience severe allergic reactions, including:
- Anaphylaxis: A life-threatening reaction with symptoms like difficulty breathing, swelling of the face or throat, and hives.
- Asthma exacerbation: In people with asthma, NSAIDs can sometimes trigger asthma attacks.
- Stevens-Johnson syndrome and toxic epidermal necrolysis: Rare but severe skin reactions that can cause blisters, peeling skin, and flu-like symptoms.
6. Blood Thinning and Bleeding:
NSAIDs, particularly aspirin, can thin the blood and increase the risk of bleeding:
- Bleeding in the stomach, gums, or brain.
- Bruising easily.
Who Is at Higher Risk for NSAID Side Effects:
- Elderly people: More prone to gastrointestinal bleeding and kidney issues.
- Individuals with heart disease, hypertension, or high cholesterol.
- Those with a history of stomach ulcers, kidney disease, or liver disease.
- People taking certain other medications, such as blood thinners (warfarin) or corticosteroids (prednisone), which increase the risk of bleeding.
How to Minimize Side Effects:
- Use the lowest effective dose for the shortest duration possible.
- Take NSAIDs with food to reduce the risk of stomach irritation.
- Avoid alcohol while using NSAIDs, as it increases the risk of stomach bleeding.
- If you’re at high risk for stomach problems, your doctor may prescribe a proton pump inhibitor (PPI) like omeprazole to protect the stomach lining.
- Monitor your kidney function and blood pressure if you’re on long-term NSAID therapy.
What to Do if You Experience Side Effects:
- For mild side effects, like nausea or headache, consult your healthcare provider for guidance.
- If you experience severe symptoms such as chest pain, shortness of breath, severe stomach pain, vomiting blood, or signs of allergic reactions, seek emergency medical attention immediately.
Medical Conditions Treated or Associated with Nonsteroidal anti-inflammatory drugs:
- Ankylosing Spondylitis
- Aseptic Necrosis
- Back Pain
- Bartter Syndrome
- Bursitis
- Chronic Myofascial Pain
- Chronic Pain
- Cluster Headaches
- Costochondritis
- Diffuse Idiopathic Skeletal Hyperostosis
- Dysautonomia
- Eustachian Tube Dysfunction
- Familial Adenomatous Polyposis
- Fever
- Frozen Shoulder
- Gout, Acute
- Headache
- Inflammatory Conditions
- Juvenile Rheumatoid Arthritis
- Migraine
- Muscle Pain
- Neck Pain
- NSAID-Induced Ulcer Prophylaxis
- Osteoarthritis
- Pain
- Pain/Fever
- Patent Ductus Arteriosus
- Period Pain
- Plantar Fasciitis
- Polyarticular Juvenile Idiopathic Arthritis
- Polymyalgia Rheumatica
- Postoperative Pain
- Premenstrual Dysphoric Disorder
- Radiculopathy
- Rheumatoid Arthritis
- Sciatica
- Spondyloarthritis
- Spondylolisthesis
- Temporomandibular Joint Disorder
- Tendonitis
- Toothache
- Transverse Myelitis