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Principles of Sports Medicine & Exercise Science

Anti-Inflammatory Drugs

by Mary Hurd, Lillian Dominguez, Michael A. Buratovich

Category: Drugs

Specialties and related fields: Dermatology, endocrinology, family medicine, internal medicine, ophthalmology, orthopedics, otorhinolaryngology, rheumatology, vascular medicine

KEY TERMS

arthritis: a painful condition that involves inflammation of one or more joints

bursitis: inflammation of the sac of lubricating fluid located between joints

hormone: a substance made by the body that travels through the bloodstream to reach its target organ and have its effect

inflammation: the body’s response to injury that may include redness, pain, swelling, and warmth in the affected area

salicylates: a group of drugs (including aspirin) derived from salicylic acid, used to relieve pain, reduce inflammation, and lower fever

steroids: a class of hormones produced by the adrenal glands; can also be made synthetically

tendinitis: inflammation of a tendon, a tough band of tissue that connects muscle to bone

INDICATIONS

Nonsteroidal anti-inflammatory drugs (NSAIDs), such as aspirin, relieve painful conditions such as arthritis, bursitis, gout, menstrual cramps, tendonitis, sprains, and strains. Additionally, low-dose aspirin is commonly prescribed to reduce the risk of myocardial infarction (heart attack).

The NSAIDs inhibit the enzyme cyclooxygenase, which converts the fatty acid commonly found in cell membranes, arachidonic acid, to prostaglandin H (PGH). PGH is the starting molecule for synthesizing a host of pro-inflammatory molecules called “prostaglandins.” By preventing prostaglandin synthesis, NSAIDs quell inflammation.

Nonsteroidal anti-inflammatory drugs come in two main forms, the salicylates and the classical NSAIDs. Salicylates include aspirin (acetylsalicylate), salsalate, and diflunisal. Some common classical NSAIDs, with their brand names in parentheses, are diclofenac (Voltaren), etodolac (Lodine), flurbiprofen (Ansaid), ibuprofen (Motrin, Advil, Rufen, Nuprin), nabumetone (Relafen), naproxen (Naprosyn or Aleve), meloxicam (Mobic, Vivlodex, Anjesco), and oxaprozin (Daypro). These drugs can come in capsules, caplets, tablets, liquids, and suppositories. While several NSAIDs require a prescription, many are sold over the counter.

Corticosteroids (synthetic glucocorticoids) make up the second group of anti-inflammatory drugs used to alleviate the symptoms associated with asthma, lupus, arthritis, and allergic reactions. Like NSAIDs, corticosteroids are available in various forms, including inhalants, creams, ointments, and oral (systemic) medications. Common corticosteroids are beclomethasone (Beconase, Vancensase, Vanceril), betamethasone (Diprolene, Lotrisone), hydrocortisone, mometasone (Elocon), prednisone (Deltasone, Orasone), and triamcinolone (Azmacort, Nasacort, Kenalog).

Synthetic glucocorticoids come as short-acting, intermediate-acting, or long-acting glucocorticoids. Short-acting glucocorticoids have a duration of action of eight to twelve hours and include cortisone and hydrocortisone. Cortisone comes in tablets that are taken orally. After ingestion, the liver converts cortisone to the active form, hydrocortisone. Consequently, cortisone has no activity if applied topically, but hydrocortisone does. Hydrocortisone or cortisol are also administered orally, intravenously, or injected intramuscularly. Because these drugs act quickly, they are the drugs of choice to treat adrenal insufficiency. Intermediate-acting glucocorticoids have a duration of action of twelve to thirty-six hours. This group includes prednisone, predniso- lone, methylprednisolone, and triamcinolone. Prednisone comes in orally administered formulations, and prednisolone is available in oral, intravenous, and topical formulations. Methylprednisolone comes in oral, intravenous, intramuscular, or intra-articular formulations. Triamcinolone comes ininhaled, oral, topical, intramuscular, and intra-articular formulations. Intermediate-acting glucocorticoids are approximately four to five times more potent compared to short-acting glucocorti- coids. Long-acting glucocorticoids are about twenty- five times more potent than short-acting glucocorti- coids and have a duration of activity of thirty-six to seventy-two hours. Betamethasone and dexameth- asone are two long-acting glucocorticoids given orally, intramuscularly, interarticularly, or intravenously.

Synthetic glucocorticoids help treat various autoimmune and inflammatory conditions, including rheumatoid arthritis, acute multiple sclerosis flares, Crohn disease, ulcerative colitis, idiopathic thrombocytopenic purpura, allergic rhinitis or conjunctivitis, or skin conditions like eczema. They also help treat hypersensitivity states like allergic reactions and prevent graft-versus-host disease in individuals who have received bone marrow transplants.

COMPLICATIONS

Although used across many medical specialties and for many reasons, NSAIDs are not without their dangers. There are two main cyclooxygenase enzymes, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). COX-2 is induced by events that cause inflammation, but COX-1 is a housekeeping enzyme that maintains the help of several tissues, specifically the stomach, kidneys, and blood vessels. COX-1 inhibition in the stomach diminishes the production of the protective mucus coating. Long-term NSAID use increases the risk of peptic ulcers and gastritis. The kidneys can also suffer damage from long-term NSAID use since COX enzymes increase renal blood flow. COX enzymes made by blood vessel cells (endothelial cells) decrease platelet adhesion and keep blood vessels clear.

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Photo via iStock/Shidlovski. [Used under license.]

Common NSAID side effects are mild and can include stomach pains or cramps, nausea, vomiting, indigestion, headache, and dizziness. Despite these relatively mild side effects, individuals currently taking other medications, women who are pregnant or who plan to become pregnant, breastfeeding women, and persons with stomach or intestinal problems, liver disease, heart disease, high blood pressure, bleeding diseases, diabetes, Parkinson’s disease, or epilepsy should consult their physicians before taking NSAIDs. While side effects are rare, some can be life-threatening. Some NSAIDs can increase the risk of strokes and heart attacks. Any feelings of tightness in the chest, irregular heartbeat, swelling, or fainting are reasons to discontinue the use of NSAIDs and consult a physician. It is important to note that children should not be given aspirin if they are recovering from a viral infection. It can lead to Reye’s syndrome—a potentially fatal condition that results in liver and brain swelling.

Corticosteroid therapy produces dramatic, immediate relief from pain, swelling, and inflammation due to arthritis. Small amounts of steroids may be injected directly into the inflamed joint, or they can be taken by mouth. However, the beneficial effects tend to be temporary. Long-term use can lead to cataracts, and increased blood sugar, which can worsen a person’s diabetes, and reduce resistance to infections, gastrointestinal ulcers, and bleeding. The advent of other highly effective alternatives has led to less frequent use of steroids in the setting of arthritis.

Additionally, corticosteroids are a common treatment for persons suffering from more serious asthmatic conditions or when treatment with bronchodilators has not proven effective. Inhaled corticosteroids are not bronchodilators and do not open the airways. Instead, these medications reduce inflammation within the airways and allow the lungs to function properly. They should be used regularly and for the complete course as prescribed to achieve full benefits. Corticosteroids may be sprayed into the nose to relieve stuffy nose, irritation, hay fever, or other allergies. In contrast, oral corticosteroids are used primarily to prevent asthma attacks.

Ophthalmic anti-inflammatory medicines can reduce problems during or following eye surgery by alleviating eye inflammation. These can be obtained only with a doctor’s prescription. Corticosteroids also relieve inflammation of the temporal arteries, the blood vessels that run along the temples. Inflammation here can disrupt the blood supply and result in blindness, partial vision loss, strokes, and even heart attacks.

Individuals who have medical conditions such as allergies, diabetes, pregnancy, osteoporosis, glaucoma, infections, thyroid problems, liver disease, kidney disease, heart disease, or high blood pressure should discuss these conditions with their physician before taking corticosteroids. If corticosteroids are used for a short time, the development of side effects is rare. However, breathing problems or tightness in the chest, pain, rash, swelling, extreme exhaustion, irregular heartbeat, or wounds that do not heal should be reported to a physician. Patients should not stop taking steroids abruptly without consulting a physician, especially if the steroids have been taken for a long time, as the body requires a weaning process to adapt.

PERSPECTIVE AND PROSPECTS

The bark of the willow tree, which contains salicylates, was known in eighteenth-century England to reduce fever and aches. In 1876, the first successful treatment of acute arthritis with sodium salicylate (aspirin) was reported. In the 1970s, pharmacologist John Vane amassed evidence of the effectiveness of NSAIDs.

The earliest demonstration of the importance of corticosteroids as anti-inflammatory agents occurred in the 1940s regarding rheumatoid arthritis. The challenge of corticosteroid therapy lies in achieving the desired results with minimum side effects.

Further Reading

1 

Davis, Jennifer S., et al. “Use of Non-Steroidal Anti- Inflammatory Drugs in US Adults: Changes over Time and by Demographic.” Open Heart, vol. 4, no. 1, 2017, doi:10.1136/openhrt-2016-000550.

2 

Liska, Ken. Drugs and the Human Body, with Implications for Society. 8th ed., Pearson/Prentice Hall, 2009.

3 

Shmerling, Robert H. “Are You Taking Too Much Anti-Inflammatory Medication?” Harvard Health Blog, 23 Mar. 2018, www.health.harvard.edu/blog/are-you- taking-too-much-anti-inflammatory-medication-2018040213540. Accessed 26 May 2022.

4 

Szalay, Jessie. What Is Inflammation? LiveScience, 19 Oct. 2018, www.livescience.com/52344-inflammation.html. Accessed 26 May 2022.

5 

Yaksh, Tony L., et al. “Development of New Analgesics: An Answer to Opioid Epidemic.” Trends in Pharmacological Sciences, vol. 39, no. 12, 2018, pp. 1000-1002, doi:10.1016/j.tips.2018.10.003.

Citation Types

Type
Format
MLA 9th
Hurd, Mary, and Lillian Dominguez, and Michael A. Buratovich. "Anti-Inflammatory Drugs." Principles of Sports Medicine & Exercise Science, edited by Michael A. Buratovich, Salem Press, 2022. Salem Online, online.salempress.com/articleDetails.do?articleName=POSpKin_0125.
APA 7th
Hurd, M., & Dominguez, L., & Buratovich, M. A. (2022). Anti-Inflammatory Drugs. In M. A. Buratovich (Ed.), Principles of Sports Medicine & Exercise Science. Salem Press. online.salempress.com.
CMOS 17th
Hurd, Mary and Dominguez, Lillian and Buratovich, Michael A. "Anti-Inflammatory Drugs." Edited by Michael A. Buratovich. Principles of Sports Medicine & Exercise Science. Hackensack: Salem Press, 2022. Accessed September 16, 2025. online.salempress.com.