Celecoxib (brand name Celebrex) is a sulfa non-steroidal anti-inflammatory drug used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation, menstrual symptoms. Celebrex (Celecoxib) is also used to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. Celecoxib is a non-steroidal anti-inflammatory drug that is used to treat arthritis, pain, menstrual cramps, and colonic polyps. It works by reducing hormones that cause inflammation and pain. Prostaglandins are chemicals that are important contributors to the inflammation of arthritis that causes pain, fever, swelling and tenderness.
Celecoxib is a highly selective COX-2 inhibitor and primarily inhibits this isoform of cyclooxygenase (and thus causes inhibition of prostaglandin production), whereas nonselective NSAIDs (like asprin, naproxen and ibuprofen) inhibit both COX-1 and COX-2. COX-1, traditionally defined as a constitutively-expressed “housekeeping” enzyme, is the only isoenzyme found in platelets and plays a role in the protection of the gastrointestinal mucosa, renal hemodynamics, and platelet thrombogenesis. COX-2, on the contrary, is extensively expressed in cells involved in inflammation and is upregulated by bacterial lipopolysaccharides, cytokines, growth factors, and tumor promoters. Celecoxib is approximately 10-20 times more selective for COX-2 inhibition over COX-1. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site. In theory, this selectivity allows celecoxib and other COX-2 inhibitors to reduce inflammation (and pain) while minimizing gastrointestinal adverse drug reactions (e.g. stomach ulcers) that are common with non-selective NSAIDs.
Celecoxib inhibits COX-2 without affecting COX-1. COX-1 is involved in synthesis of prostaglandins and thromboxane, but COX-2 is only involved in the synthesis of prostaglandin. Therefore, inhibition of COX-2 inhibits only prostaglandin synthesis without affecting thromboxane (TXA2) and thus offer no cardioprotective effects of non-selective NSAIDs.
In theory the COX-2 selectivity should result in a significantly lower incidence of gastrointestinal ulceration than traditional NSAIDs. The main items of evidence cited to support this theory were the preliminary (6 month) results of the Celecoxib Long-term Arthritis Safety Study (CLASS) as published in 2000, which demonstrated a significant reduction in the combination of symptomatic ulcers plus ulcer complications in those taking celecoxib versus ibuprofen or diclofenac, provided they were not on aspirin (Silverstein et al., 2000). However, this was not significant at 12 months (full study length).
Celecoxib is used to relieve pain, tenderness, swelling and stiffness caused by osteoarthritis (arthritis caused by a breakdown of the lining of the joints), rheumatoid arthritis (arthritis caused by swelling of the lining of the joints), and ankylosing spondylitis (arthritis that mainly affects the spine). Celecoxib is also used to treat painful menstrual periods and pain from other causes. It is also used with surgery and other treatments to reduce the number of polyps (abnormal growths) in the colon (large intestine) and rectum in patients with familial adenomatous polyposis (a condition in which hundreds or thousands of polyps form in the colon and cancer may develop). Celecoxib is in a class of NSAIDs called COX-2 inhibitors. It works by stopping the body's production of a substance that causes pain and inflammation.
This review included five randomized controlled trials with a total of 4465 participants. The evidence reviewed suggests that celecoxib controls the symptoms of rheumatoid arthritis (RA) to a similar degree to that of the active comparators examined (naproxen, diclofenac and ibuprofen). When compared to placebo, the percentage of patients showing improvement by four weeks were 42/82 (51%) in the twice-daily celecoxib 200mg group and 43/82 (52%) in the twice-daily celecoxib 400mg group; these were significantly different from the placebo group in which 25/85 (29%) improved. At six months this study found a reduced rate of upper gastrointestinal complications with celecoxib but there is also evidence to suggest that these benefits may not be evident in the long-term and that celecoxib offers no additional benefit in patients who are also receiving cardio-prophylactic low dose aspirin.
For an individual with RA the potential benefits of celecoxib need to be balanced against the uncertainty that the short-term reduced incidence of upper gastrointestinal complications are maintained in the long-term and its increased cost in comparison to traditional non-steroidal anti-inflammatory drugs.
In clinical studies with OA patients, CELEBREX (Celecoxib) is proven to improve daily physical function, so moving is easier. In fact, CELEBREX improves pain, stiffness, and physical function.
In clinical studies, for patients with RA, CELEBREX demonstrated significant reduction in joint tenderness/pain and joint swelling.
In clinical studies with patients experiencing acute pain, single doses of CELEBREX provided relief within 60 minutes.
CELEBREX doesn't interfere with aspirin. If you're taking low-dose aspirin for your heart and need an NSAID pain reliever, CELEBREX can be used because it doesn't interfere with aspirin's antiplatelet effect. However, taking low-dose aspirin may not reduce the cardiovascular risk associated with NSAID use. With any NSAID, including CELEBREX, patients also taking aspirin are at an increased risk for stomach bleeding and ulcers. CELEBREX (Celecoxib) is not a substitute for aspirin in preventing heart attack or stroke.
Celocoxib may prevent intra-abdominal adhesion formation. Adhesions are a common complication of surgery, especially abdominal surgery, and major cause of bowel obstruction and infertility. Publishing in 2005, researchers in Boston noticed a “dramatic” reduction in post-surgical adhesions in mice taking the drug celecoxib. Multi-institutional trials in adult human patients are planned. The initially suggested course of treatment is a mere 7–10 days following surgery.
Celecoxib may emerge as a potent chemopreventive agent for lung cancer, according to a recent study in Cancer Prevention Research, a journal of the American Association for Cancer Research.
Researchers tested celecoxib, a COX-2 inhibitor, among patients who were former smokers and found a significant benefit in bronchial health as measured by the Ki-67 labeling index, a marker of cellular proliferation or growth, as well as a number of other biomarkers. The findings follow a previous report published in Cancer Prevention Research that showed a similar effect on Ki-67 among former smokers and current smokers.
“Taken together, these findings strongly suggest that celecoxib can be used as a chemopreventive agent in these high-risk groups,” said Jenny Mao, M.D., a professor of medicine at the University of New Mexico and section chief of pulmonary and critical care medicine at the New Mexico VA Health System.
Mao cautioned, however, that both the current study, where she was the lead researcher, and the Feb. 2010 study were phase 2 trials, and that large phase 3 trials are still needed to confirm the findings.
J. Jack Lee, Ph.D., a professor of biostatistics at The University of Texas M. D. Anderson Cancer Center and the statistical editor of Cancer Prevention Research, estimates that there are currently 45 million former smokers and 45 million current smokers in the United States alone.
“The oncology community does not have a good treatment for lung cancer. Unless it is caught in the earliest stages, the five-year survival is only about 15 percent,” said Lee. “The best way is to intercept at the earliest stages and try to reverse the processes that can lead to cancer. These studies suggest celecoxib may be a tool to do that.”
For the current study, Mao and colleagues enrolled 137 patients and randomly assigned them to 400 mg celecoxib twice daily or a placebo. Patients had to be at least 45 years old, and had to have stopped smoking for at least a year.
Researchers conducted bronchoscopies at baseline and six months to measure changes in the Ki-67 labeling index. Treatment with celecoxib reduced this index by 34 percent compared to a 3.8 percent increase with the placebo group. Decreases in this index were also linked with a reduction in lung nodules, a potential precursor to cancer. (Date: June 29, 2011. Source: American Association of Cancer Research)
Celebrex (Celecoxib) is part of a class of nonsteroidal anti-inflammatory drugs ( NSAIDs) called COX-2 inhibitors. It works by blocking a particular enzyme (COX-2) that plays a role in pain and inflammation. Unlike other NSAIDs (such as ibuprofen and naproxen) that target both the COX-1 and the COX-2 enzymes, Celebrex only targets the COX-2 enzyme. The COX-1 enzyme plays an important role in protecting the lining of the stomach.
Celebrex® (celecoxib) is a prescription medication that has been licensed to treat several conditions related to pain and inflammation. These approved uses for Celebrex include:
Acute pain relief, such as for pain following a procedure or straining a muscle.
Treatment of arthritis symptoms, including pain, stiffness, and swelling. Celebrex can be used to treat several different types of arthritis, such as osteoarthritis, rheumatoid arthritis (including juvenile rheumatoid arthritis), and ankylosing spondylitis. The medication is not an arthritis cure, however.
Treatment of painful menstrual periods.
Celebrex was previously approved to decrease the number of colon and rectal polyps in people with familial adenomatous polyposis (FAP), a hereditary condition that can cause hundreds of growths (called polyps) in the colon and rectum. People with FAP usually develop colon cancer and/or rectal cancer by their late 30s. However, Celebrex is no longer approved for this use.
Celebrex is approved for the treatment of juvenile rheumatoid arthritis in children as young as two years old. It is not approved for other uses in children. Talk to your child's healthcare provider about the benefits and risks of using Celebrex in children.
On occasion, your healthcare provider may recommend Celebrex for something other than the conditions listed in this article. This is called an “off-label” use. For example, research scientists are currently exploring the use of Celebrex for the treatment of certain types of cancer, including melanoma and lung cancer.
(WASHINGTON, D.C. -- April 4, 2006) Sustained, high doses of celecoxib reduce the risk of adenomas in patients who have undergone polypectomy, with the greatest benefit seen in patients at highest risk of polyp recurrence, according to results of the Prevention of Sporadic Adenomatous Polyps (PreSAP) trial.
Nadir Arber, MD, principal investigator, PreSAP trial, and head, Gastrointestinal Oncology Unit, Tel Aviv Sourasky Medical Center, Tel Aviv, Israel, noted that there will be over 1 million cases worldwide of colon cancer this year and that as many as half of these patients will die.
“This is inappropriate as up to 90% of cases can be prevented,” he told a press briefing here on April 3rd at the 97th Annual Meeting of the American Association for Cancer Research (AACR).
“Now we have proof of concept that chemoprevention is feasible” in sporadic colon cancer, through use of the cyclo-oxygenase (COX-2) inhibitor celecoxib, Dr. Arber said.
The PreSAP trial enrolled 1,561 patients who had an adenomatous polyp removed within 30 days of enrollment at 107 centers in 32 countries. A total of 933 patients were randomized to 400 mg daily of celecoxib and 628 were randomized to placebo. Patients were stratified according to aspirin use and treatment center.
At year 3, 79.2% of patients had a colonoscopy. Of these patients, 33.6% of those on celecoxib had developed new polyps, compared with 49.3% of those on placebo (P <.0001).
When the researchers looked at high-risk patients -- defined as those with 3 or more adenomas at baseline, those who were 60 years or older and those who with a parent who had colorectal cancer -- they found that 50% of patients on celecoxib and 70% of those on placebo had new adenomas (P =.0002). This translates to a relative risk reduction of 33%, Dr. Arber said.
Cardiovascular events, the main concern of COX-2 inhibitors, developed in 7.5% of patients on celecoxib and in 4.8% of those on placebo (P <.05).
However, Dr. Arber noted that the total number of serious cardiac events was 2.5% in the active arm versus 1.9% in the placebo arm (hazards ratio = 1.3, 95% confidence interval 0.6-2.6).
The trial was sponsored by Pfizer.
Pregnancy: You must not use Celecoxib during pregnancy or if you are trying to become pregnant due to possible harm to the unborn baby and interference with normal labor/delivery.
Breast-feeding: Tell your doctor before using Celecoxib if you are breast-feeding. It is not known whether using Celecoxib during breastfeeding is dangerous. Limited data show celecoxib is excreted into human milk in small amounts. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
This medicine may cause dizziness or sleepiness and so may affect your ability to drive or operate machinery safely. Do not drive or operate machinery until you know how this medicine affects you and you are sure it won't affect your performance.
This medicine may hide a fever, which is a sign of infection. This may make you think mistakenly that an infection is getting better when it isn't, or that an infection is less serious than it is. For this reason you should tell your doctor if you get an infection while you are taking this medicine.
Your doctor will prescribe you the lowest effective dose of this medicine for the shortest possible time necessary to relieve your symptoms. This is to minimise the chances of any side effects, particularly those mentioned below. It is important not to exceed the prescribed dose.
NSAIDs can occasionally cause serious side effects on the gut, such as ulceration, bleeding or perforation of the stomach or intestinal lining. This type of side effect is more likely to occur in elderly people and in people taking high doses of the medicine. The risk can also be increased by taking certain other medicines. It is important that these people, as well as people with a history of disorders affecting the stomach or intestines, are closely monitored by a doctor while taking this medicine. All people taking this medicine should stop treatment and consult their doctor immediately if they experience any sign of bleeding from the stomach or intestine during treatment, for example vomiting blood and/or passing black/tarry/bloodstained stools.
COX-2 inhibitors may carry an increased risk of heart attacks and stroke when compared to placebo (no treatment). If you have risk factors for heart disease or stroke, such as diabetes, high cholesterol or smoking, your doctor will need to assess the overall benefits and risks before deciding if this medicine is suitable for you. In general, if this medicine is suitable, your doctor will prescribe the lowest effective dose for as short a time as possible to control your symptoms, because the risks may increase with higher doses and the longer the medicine is taken. Do not exceed the prescribed dose. Tell your doctor if you experience shortness of breath, chest pains or ankle swelling while taking the medicine. Ask your doctor or pharmacist for further information.
It is recommended that your blood pressure is regularly monitored while you are taking this medicine.
If you have any existing problems with your kidneys, liver or heart function, your kidney function should be regularly monitored while you are taking this medicine.
Some cases of severe liver reactions have been reported in people taking this medicine. Most of these developed within one month of starting treatment. For this reason, while you are taking this medicine you should let your doctor know straight away if you notice any symptoms that could indicate a problem with your liver. These may include yellowing of the skin or whites of the eyes (jaundice), unusually dark urine, nausea and vomiting, loss of appetite or flu-like symptoms.
Very rarely, NSAIDS may cause serious blistering or peeling skin reactions (eg Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis). For this reason, you should stop taking this medicine and consult your doctor if you get a skin rash or sores inside your mouth while taking this medicine. This side effect is very rare, but if it occurs, is most likely to happen in the first month of treatment.
Get emergency medical help if you have any of these signs of an allergic reaction to celecoxib: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using celecoxib and call your doctor at once if you have a serious side effect such as:
chest pain, weakness, shortness of breath, slurred speech, problems with vision or balance;
black, bloody, or tarry stools;
coughing up blood or vomit that looks like coffee grounds;
swelling or rapid weight gain;
urinating less than usual or not at all;
nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
skin rash, bruising, severe tingling, numbness, pain, muscle weakness; or
severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Less serious celecoxib side effects may include:
upset stomach, diarrhea, bloating, gas;
dizziness, nervousness, headache;
runny or stuffy nose, sore throat; or
mild skin rash.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Ask your doctor before using an antidepressant such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, Symbyax), fluvoxamine (Luvox), paroxetine (Paxil), or sertraline (Zoloft). Taking any of these medicines with an NSAID may cause you to bruise or bleed easily.
Tell your doctor about all other medicines you use, especially:
a blood thinner such as warfarin (Coumadin, Jantoven);
a diuretic (water pill) such as furosemide (Lasix);
fluconazole (Diflucan);
lithium (Eskalith, Lithobid);
a heart or blood pressure medication such as candesartan (Atacand), eprosartan (Teveten), irbesartan (Avapro, Avalide), losartan (Cozaar, Hyzaar), valsartan (Diovan), telmisartan (Micardis), or olmesartan (Benicar); or
an ACE inhibitor such as benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril), quinapril (Accupril), ramipril (Altace), and others.
This list is not complete and other drugs may interact with celecoxib. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.
These reviews are from WebMD's homepage:
Condition: Joint Damage causing Pain and Loss of Function - 12/12/2011 9:22:07 PM
Reviewer: ehc0791, 45-54 on Treatment for less than 1 month (Patient)
Comment: I had tennis elbow and tried different kind physical therapies and medicines. This one is the most effective.
Condition: Joint Damage causing Pain and Loss of Function - 11/21/2011 2:05:55 PM
Reviewer: tory1234, 55-64 Male on Treatment for less than 1 month (Patient)
Comment: Did not relieve pain. ... Side effects were horrible: gas, irritable bowel, blood pressure high, moody and irritable. Stopped taking it after 2 2 weeks. Went back to over counter ASID's -...
Condition: Joint Damage causing Pain and Loss of Function - 9/25/2011 1:20:19 PM
Reviewer: msmith, 45-54 Female on Treatment for less than 1 month (Patient)
Comment: Took this medication for shoulder tendonitis. 200mg twice a day for 4-5 days.started experiencing severe leg cramps with bruising. Went to ER for labs and US of legs. All normal labs B/P elavated 148/104 normal B/P 118/66 Also caused fatigue and irritability. ... Effective for pain relief but too many serious side effects.
Condition: Joint Damage causing Pain and Loss of Function - 8/26/2011 12:02:52 AM
Reviewer: Faye, 65-74 Female on Treatment for 5 to less than 10 years (Patient)
Comment: Used to treat chronic pain in both knees. Vioxx worked better but was taken off the market. I have been taking 1 tab daily for over six years and it does help with keeing the inflammation in check.
Condition: Joint Damage causing Pain and Loss of Function - 7/17/2011 4:27:47 PM
Reviewer: 65-74 Female on Treatment for 1 to 6 months (Patient)
Comment: not sure, but do have increased edema over entire body; tiredness and increasing depression.
Condition: Joint Damage causing Pain and Loss of Function - 7/7/2011 11:27:28 AM
Reviewer: bettyannep, 55-64 Female on Treatment for 6 months to less than 1 year (Patient)
Comment: I tried all sorts of medications and nothing worked. It is more expensive than I can afford but it is the only thing that has worked for me so I take it. Improvement in mobility is unbelievable. I was using a power chair or walker. Now I walk unassisted and can even clean my house which I haven't been able to do in three years. Nice not having that expense! Overall I am more than satisfied with effectiveness, not so happy about the costs.
Condition: Joint Damage causing Pain and Loss of Function - 3/9/2011 8:38:56 PM
Reviewer: lpnhipreplacementx2, 45-54 Female on Treatment for 1 to less than 2 years (Patient)
Comment: this is the only NSAID I can take without causing stomach upset. the only bad thing I can say about it is very expensive. When I run out I can really tell the difference in my stiffness/pain d/t hip replacement surgeries, I've had a total of 3 hip surgeries, overall osteoarthritis and fibromyalgia.
Condition: Joint Damage causing Pain and Loss of Function - 10/20/2010 10:48:16 PM
Reviewer: lady, 55-64 Female on Treatment for 1 to 6 months (Patient)
Comment: I had hip pain for 15 years.It got so bad I could hardly walk at all.Since taking Celebrex,I can walk better and do basics of everyday life.I have had 0 side effects.Thank God for the pain relief!!!
Condition: Joint Damage causing Pain and Loss of Function - 9/1/2010 5:28:10 PM
Reviewer: kbear, 45-54 Female on Treatment for 10 years or more (Caregiver)
Comment: I think this product works great! My arthritis pain in my knee was gone in days. I only take this med when needed for 3-4 days. Make sure you take it in the morning with a good full breakfast. I've had no stomach problems taking it in this way.
Condition: Joint Damage causing Pain and Loss of Function - 8/18/2010 7:13:37 PM
Reviewer: Grandma Bean, 55-64 Female on Treatment for 2 to less than 5 years (Patient)
Comment: I suffer from degenerative disc disease as well as arthritis. Celebrex has made it possible to remain active. Should I for what ever reason miss a couple of days I immediately fell the unrelenting pain return.
Condition: Joint Damage causing Pain and Loss of Function - 6/22/2010 1:32:04 PM
Reviewer: mishi girl, Female on Treatment for less than 1 month (Patient)
Comment: I only use this medicine as needed. Recently I took it for only 4 days to treat hand/wrist inflammation. Took 1 200mg a day, and on my fourth day experienced problems with my vision. I could see but my peripherial vision on my left eye was extremely compromised and couldn't see anything but a haze. Plus, I saw a "wiggle" effect on both my eyes. I'm glad it didn't last long; it took over an hour for it to go away. It's an unfortunate side effect, since it works great for pain but the consequence is not one that I want to continue to live with just to get relief.
Condition: Joint Damage causing Pain and Loss of Function - 6/20/2010 6:33:53 PM
Reviewer: czab, 55-64 Female on Treatment for 6 months to less than 1 year (Patient)
Comment: I have been taking this drug for almost a year for lower back pain and left knee pain where it is bone on bone. It helps the knee but does nothing for lower back pain. Asked dr. to switch me to meloxicam 15mg. Ill see if this helps any better.
Condition: Joint Damage causing Pain and Loss of Function - 6/18/2010 3:29:04 PM
Reviewer: apfinch, 25-34 Female on Treatment for less than 1 month (Patient)
Comment: Doctor prescribed it to treat my TMJ Disorder, which was causing intense inflammation to the point of getting a lock-jaw effect. I couldn't eat well or sleep good at night for over 1 1/2 weeks. I took two 200mg pills at night and within in 3 days, the pain was reduced significantly and the TMJ has gone away for the moment. Have stopped using it. Now experiencing carpal tunnel syndrome for over 2 weeks; am contemplating taking Celebrex to overcome inflammation as I've seen that others have said it may help.
Condition: Joint Damage causing Pain and Loss of Function - 5/31/2010 12:29:23 PM
Reviewer: BillS, 75 or over Male on Treatment for 1 to 6 months (Patient)
Comment: ! first used Celebrex some years ago as a remedy for shoulder pain after a fall. It worked beautifully, and It avoided the need for a rotator cuff operation. Then a year or two later I injured the shoulder again and an operation was necessary. Several months ago I injured the other shoulder similarly and also the elbow tendon. I got relief from cortisone shots in both places, but it didn't last long. The orthopedist gave me Rx for Celebrex 200 mg a month ago and the result is amazing- pain gone, and 95% motion restored. Some stomach pain during night at first, but now I'm making sure I take it with a full meal. I also feel tired and drowsy- falling asleep when I don't want to, but not at night when I do want to. Perhaps this will clear up.
Condition: Joint Damage causing Pain and Loss of Function - 5/14/2010 8:41:36 PM
Reviewer: Jimmy J, 55-64 on Treatment for 6 months to less than 1 year (Patient)
Comment: I was prescribed for knee pain following surgery for torn muniscus. Knees are also arthritic. Take probably once a week on average. Pain relief lasts for several days. I have had no side effects. ...