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COX-2 inhibitors: Uses, common brands, and safety information

Celebrex is a COX-2 inhibitor used to treat pain, inflammation, and fever

If you or a loved one has ever experienced pain from arthritis, you may have heard of a medication called Celebrex (celecoxib). Celebrex is known as a COX-2 inhibitor. Celebrex is an oral prescription drug available in both brand and generic form and approved by the U.S. Food and Drug Administration (FDA). 

This article will discuss uses, common brand names, and safety information regarding COX-2 inhibitors. As Celebrex is the only COX-2 inhibitor on the market, we will use the terms COX-2 inhibitor and Celebrex interchangeably. 

List of COX-2 inhibitors
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Celebrex (celecoxib) Get Celebrex coupons Celebrex details

Other COX-2 inhibitors

Two other COX-2 inhibitors were previously available, but they were both removed from the market and are no longer available. 

  • Bextra (valdecoxib). Made by Pfizer; removed from market in 2005 due to risk of serious cardiovascular events such as heart attack (myocardial infarction) or stroke as well as severe skin reactions.
  • Vioxx (rofecoxib). Made by Merck; removed from market in 2004 due to risk of serious cardiovascular events such as heart attack or stroke.

Another COX-2 inhibitor, Arcoxia (etoricoxib), was developed, but in 2007, the FDA did not approve the drug.

What are COX-2 inhibitors?

Celebrex, the only COX-2 inhibitor, is a nonsteroidal anti-inflammatory drug. Most nonsteroidal anti-inflammatory drugs (NSAIDs) work by inhibiting enzymes called cyclooxygenase-1 (COX-1 enzyme) and cyclooxygenase-2 (COX-2 enzyme)—they are nonselective NSAIDs. Prostaglandins cause pain and inflammation. By inhibiting these enzymes, prostaglandin synthesis is inhibited as well. While most NSAIDs work on COX-1 and COX-2, Celebrex only works on COX-2, so it is known as a selective COX-2 inhibitor. When COX-2 inhibitors (sometimes referred to as “coxibs”) were developed, they were expected to be better tolerated. However, two COX-2 inhibitors, Vioxx and Bextra, were removed from the market in 2004 and 2005 due to an increased risk of serious cardiovascular events. Celebrex is the only remaining COX-2 inhibitor. 

How do COX-2 inhibitors work?

COX-2 inhibitors work by treating pain (analgesic effect), inflammation, and fever. Celebrex works by stopping prostaglandin from being made by inhibiting an enzyme called cyclooxygenase-2 (COX-2). 

What are COX-2 inhibitors used for?

Indications for Celebrex include: 

Who can take COX-2 inhibitors?

Before taking Celebrex, talk to your doctor about all of the medical conditions you have and any medications you take, including prescription drugs, over-the-counter medicines, and vitamins or supplements. Only your doctor can determine if Celebrex is an appropriate treatment for you.

Men

Men can take Celebrex, provided that the medication is needed for one of the approved indications, and the patient does not fall into one of the restricted categories or warnings (see section below). Also, a healthcare provider must determine that it would be safe and effective for the patient based on symptoms, medical conditions, history, and other medications being taken. 

Women (not pregnant or breastfeeding)

Women who are not pregnant or breastfeeding may take Celebrex if the medication is needed for an approved indication and if the patient does not fall into one of the restricted categories or warnings listed below. Also, the healthcare provider will determine if it is safe and effective based on the individual’s symptoms, medical conditions, history, and other drugs being taken. 

Pregnant or breastfeeding women

There are no studies of Celebrex in pregnant women. In animal studies, Celebrex caused harm to the unborn baby. The prescribing information recommends only using Celebrex if the benefits to the mother are greater than potential risks to the unborn baby. 

 

The prescribing information recommends using caution with Celebrex use in breastfeeding women. Consult your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding. 

Children

Celebrex can be used for signs and symptoms of Juvenile rheumatoid arthritis in patients 2 years old and above. The medication’s safety and efficacy have not been studied for longer than 6 months in children. Therefore, it is unknown if there is a risk of long-term cardiovascular toxicity. Children who take Celebrex will be monitored closely by the prescriber. Some children do not metabolize an enzyme called CYP2C9 properly, and they are known as CYP2C9 poor metabolizers. In these patients, Celebrex should not be used. 

Seniors

In clinical trials, there was not a significant difference in efficacy in patients who were ages 65 years and older compared to younger patients. However, there have been more fatal gastrointestinal events and kidney failure in older patients than in younger patients. This applies to COX-2 inhibitors and other NSAIDs (such as ibuprofen, aspirin, diclofenac, meloxicam, indomethacin, and naproxen).  

Are COX-2 inhibitors safe?

Recalls

Restrictions and warnings

Celebrex should not be used (is contraindicated) in people with/who are:

  • Allergic to Celebrex or sulfa drugs (sulfonamides)
  • A history of asthma, hives, or other allergies to aspirin or NSAIDs
  • Having coronary artery bypass graft (CABG) surgery

Celebrex has a boxed warning. This is the strongest warning required by the FDA. The warning states:

  • Celebrex may increase the risk of serious cardiovascular thrombotic events, heart attack, and stroke. These events may be fatal. All NSAID medications have a similar cardiovascular risk. The risk may increase the longer the medication is used. People who have heart disease or risk factors for heart disease may be at higher risk. 
  • Celebrex (and all NSAIDs) may increase the risk of serious gastrointestinal (GI) events, including bleeding, gastrointestinal tract ulcers, and perforation of the stomach or intestines. These events can happen at any time and without warning and can be fatal. Older adults are at higher risk for the incidence of serious GI events. 

Celebrex should also be used with caution in many other situations. These include:

  • Kidney (renal) or liver problems
  • Aspirin triad
  • GI bleed or ulcer history
  • Pregnancy/women trying to conceive/breastfeeding
  • Asthma 
  • Recent heart attack
  • Heart disease or risk of heart disease
  • High blood pressure (hypertension)
  • Congestive heart failure
  • Clotting disorder
  • Fluid retention
  • Older, dehydrated, or debilitated adults 
  • Poor CYP2C9 metabolizers
  • Alcohol or tobacco use
  • Prolonged use 

Are COX-2 inhibitors controlled substances?

No, COX-2 inhibitors are not controlled substances.

Common COX-2 inhibitors side effects

The most common adverse effects of Celebrex include: 

  • Headache
  • GI issues: indigestion, stomach pain, nausea, vomiting, diarrhea, flatulence
  • Upper respiratory infection
  • Rash 
  • Swelling (edema) of the lower legs or hands
  • Dizziness 
  • Abnormal liver or kidney blood tests
  • Sensitivity to light
  • Delayed ovulation
  • Fever, cough, joint pain (in children)

Other side effects and patient information

  • Every time you fill or refill your Celebrex prescription, you will receive a medication guide that outlines side effects, warnings, and other information. Read this guide and consult your healthcare provider if you have any questions. 
  • Celebrex may cause serious cardiovascular effects such as heart attack or stroke, which may be fatal. If you have chest pain, shortness of breath, weakness, slurred speech, get emergency medical attention right away. 
  • Celebrex can cause high blood pressure or worsen preexisting high blood pressure. Ask your doctor about monitoring blood pressure while taking Celebrex. 
  • Celebrex can cause stomach problems, including ulcers and bleeding, which can be fatal. Seek emergency medical help if you have symptoms such as pain, indigestion, dark stools, or bloody vomiting.
  • Celebrex can cause liver problems. If you have symptoms of nausea, tiredness, itching, yellowing of the skin or whites of eyes, abdominal pain, and/or flu-like symptoms, stop taking Celebrex and get medical help right away. 
  • Celebrex is a sulfonamide. Do not take Celebrex if you have a sulfa allergy. It can cause severe skin effects, such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. These conditions can occur without warning and result in hospitalizations and death. If you have a skin rash, itching, blisters, or fever, stop taking Celebrex and get medical help right away. 
  • Long-term use of NSAIDs, including Celebrex, can cause kidney problems. The risk is higher in patients who take diuretics, ACE inhibitors, angiotensin receptor blockers, or in people with kidney or liver problems, heart failure, and older adults. If you have unexplained weight gain or swelling while taking Celebrex, contact your doctor immediately. 
  • Get emergency medical help if you have symptoms of a serious allergic reaction, such as difficulty breathing or swelling of the face or throat. 
  • Tell your doctor if you have a history of asthma or aspirin-sensitive asthma. NSAID use may cause severe bronchospasm, which can be fatal. Do not take Celebrex if you have aspirin sensitivity. If you have asthma and you take Celebrex, get immediate medical help if asthma symptoms worsen.

How much do COX-2 inhibitors cost?

Celebrex is available in generic form, as celecoxib. Most insurance plans and Medicare prescription plans cover celecoxib. Your cost will vary based on your insurance plan, so you can contact your plan for up-to-date coverage information. Or, you can use a free SingleCare card or coupon to save money on your celecoxib prescription and refills. Our members can save up to 80% on medication costs. For example, a typical prescription of celecoxib would be for 30, 200 mg capsules. With a SingleCare card, you can pay as little as $10 at your local pharmacy—or even less with GeniusRx, SingleCare’s home delivery partner.