Arthrotec is a combination of diclofenac and misoprostol. Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) similar to ibuprofen, naproxen, and others. Diclofenac, like other NSAIDs work by inhibiting the production of prostaglandins. Prostaglandins are a related family of chemicals that are produced by the cells of the body and have several important functions. They promote inflammation, pain, and fever, support the function of platelets that are necessary for the clotting of blood, and protect the lining of the stomach from the damaging effects of acid.
Prostaglandins are produced by the enzyme cyclooxygenase (Cox). There actually are two Cox enzymes, Cox-1 and Cox-2. Both enzymes produce prostaglandins that promote inflammation, pain, and fever. However, only Cox-1 produces prostaglandins that support platelets and protect the stomach. Diclofenac blocks both Cox enzymes and reduces prostaglandins throughout the body. As a consequence, ongoing inflammation, pain, and fever are reduced. Since prostaglandins that protect the stomach and support platelets and blood clotting also are reduced, NSAIDs can cause ulcers in the stomach and promote bleeding. Misoprostol is a synthetic (man-made) prostaglandin that stimulates secretion of mucus in the gastrointestinal tract. Mucus protects the lining of the stomach from acid. Misoprostol has been shown to reduce the frequency of ulcers of the stomach caused by NSAIDs. Arthrotec was approved by the FDA in December, 1997.
Arthrotec is used for treating signs and symptoms of rheumatoid arthritis or osteoarthritis in patients at risk for developing ulcers from NSAIDs.
Benefits of Arthrotec
How does Arthrotec work? What will it do for me?
Diclofenac sodium - misoprostol is used to treat symptoms of rheumatoid arthritis and osteoarthritis. Diclofenac belongs to the class of medications known as nonsteroidal anti-inflammatories (NSAIDs). It reduces pain and inflammation. Misoprostol helps to protect the stomach from irritation and stomach ulcers that can be caused by diclofenac.
Arthrotec can decrease the uncomfortable symptoms that are associated with both rheumatoid arthritis and osteoarthritis, such as inflammation of the joints, swelling, and pain. Reducing these symptoms can enhance the lifestyles of those living with either medical condition.
FDA Clears Arthrotec For Arthritis Therapy
SKOKIE, IL -- December 29, 1997 -- The United States Food and Drug Administration has granted marketing clearance to Searle’s Arthrotec(R) (diclofenac sodium 50 or 75 mg/misoprostol 200 mcg), the first arthritis therapy that provides both non-steroidal anti-inflammatory drug (NSAID) strength and GI mucosal (stomach lining) protection against ulcers.
Arthrotec, the only product indicated to relieve the signs and symptoms of osteoarthritis and rheumatoid arthritis in patients at high risk for NSAID-induced ulcers and their complications, demonstrated a 65 to 80 percent lower incidence of such ulcers when compared to other commonly used NSAID therapies in worldwide clinical trials.
The dual action of Arthrotec results from its unique formulation, consisting of an enteric-coated core containing diclofenac sodium (50 or 75 mg) surrounded by an outer mantle containing misoprostol (200 mcg). Diclofenac is one of the most widely-used NSAIDs in the world, while misoprostol is the only medication proven to reduce the incidence of NSAID-induced stomach and duodenal (upper small intestine) ulcers and their serious complications.
“For the first time in the U.S., there truly is an arthritis treatment that delivers both NSAID efficacy and improved GI mucosal safety in a single tablet. Physicians continually balance the risks and benefits of NSAID therapy especially for those patients at high risk who could develop a serious GI complication,” said Lee Simon, MD, associate professor of medicine at Harvard Medical School/Beth Israel Deaconess Medical Center and an Arthrotec clinical investigator. “Arthrotec will provide a new level of confidence for physicians who treat this vulnerable patient population.
“At the same time, arthritis sufferers will have a new treatment option available to them to manage their pain while minimising their risk of ulcer complications.”
NSAIDs work by reducing prostaglandins -- naturally-occurring substances that mediate inflammation in the joints. However, prostaglandins also are responsible for protecting the mucosal lining of the stomach and duodenum. Depleted prostaglandin levels in the stomach from chronic NSAID use can lead to a number of potentially serious side effects, including bleeding ulcers and perforating ulcers.
The inclusion of misoprostol in Arthrotec helps to protect the lining of the GI tract by reducing acid production, stimulating secretion of naturally-protective mucus and bicarbonate and promoting adequate blood flow.
Studies suggest nearly 25 percent of arthritis patients who chronically take NSAIDs can develop ulcers or lesions, which lead to approximately 7,600 deaths and 76,000 hospitalisations in the U.S. annually. The NSAID-related mortality rate is higher than deaths due to cervical cancer, melanoma and asthma.
“There are two key reasons why this is an important public health concern. The first is that a significant sub-population of patients are at high risk for ulcers. Moreover, these patients commonly develop NSAID-induced ulcers without symptoms. It's not unusual to be symptom-free one day and the next day wake up requiring immediate medical attention for a bleeding ulcer,” Dr. Simon said.
“Secondly, people don't know how to gauge their personal risk. Once physicians and patients understand how to assess risk profiles, treatment decisions can be tailored to meet the medical needs of the individual.”
Although all NSAID users have a three-fold greater risk of developing serious GI complications over non-NSAID users, there are specific risk factors that increase the likelihood of GI damage even more substantially. One of the biggest risk factors is older age. With increasing age, GI defence mechanisms decrease, causing individuals to be more susceptible to NSAID-induced GI complications such as ulcers.
Other risk factors include: history of gastrointestinal bleeding; history of peptic ulcer disease; longer duration of NSAID therapy; co-therapies including oral corticosteroids, anti-coagulants, or concurrent use of H2 receptor antagonists (acid blockers) and antacids; poor general health including cardiovascular disease; co-morbidities such as alcoholism or smoking; H-pylori positive status.
Level of risk for NSAID-induced GI complications varies from patient to patient. Therefore, experts are developing clinically-based risk calculators to help both healthcare professionals and their patients determine individual risk profiles.
The therapeutic benefits of Arthrotec have been demonstrated in controlled, double-blind international clinical trials involving approximately 2,000 patients. Studies have demonstrated its innovative profile - powerful anti-inflammatory and analgesic properties, and GI mucosal protection -- leading to arthritis relief and significantly fewer GI ulcers, compared to diclofenac,4,5 naproxen or piroxicam alone (naproxen and piroxicam studies in U.S. only).
Arthrotec was well-tolerated by most patients in clinical trials. The most common side effects, which were usually mild and transient, lasting less than one week, include abdominal pain, diarrhea and stomach upset. Because Arthrotec is an NSAID-containing formulation, there remains a risk of ulcers and GI bleeding, though two-to-three times less than with diclofenac and the other studied NSAIDs.
Today, Arthrotec is available in over 40 countries, and now ranks among the best-selling branded NSAIDs in Germany, the United Kingdom, Sweden, the Netherlands and Canada.
Arthrotec Common side effects
The following are side effects known to be common of Arthrotec and they are experienced by users. These are common side effects but if you feel uneasy or they persist do not hesitate to contact your physician.
Increased sensitivity to the sun or ultraviolet light
Constipation or diarrhea
Gas or heartburn
Nausea or vomiting
None of the above listed side effects require immediate medical attention. If you continue to experience these Common side effects for a few days, consult your prescribing physician for more advice. It is very important that you do not try to treat these symptoms on your own. Note: that elderly patients have a higher likelihood of experiencing side effects.
Arthrotec Least Common side effects
The following side effects are rare and should not be taken lightly. If you experience any of these less common side effects from taking Arthrotec consult your healthcare professional immediately. The following are less common side effects associated with Arthrotec:
Black tarry stools
Decrease in the amount of urine passed
Stomach pain or cramps
Blood in urine
Dark yellow or brown urine
Ringing in the ears
Skin rash, redness, blistering, peeling or itching
Swelling of the eyelids, throat, lips or feet
Yellowing of the eyes or skin
Unusual bleeding or bruising, red spots on the skin
It is important that you contact your physician right away if you've experienced any of the Less Common side effects listed above.
CONTRAINDICATIONS AND WARNING
ARTHROTEC® (diclofenac sodium, misoprostol) CONTAINS DICLOFENAC SODIUM AND MISOPROSTOL. ADMINISTRATION OF MISOPROSTOL TO WOMEN WHO ARE PREGNANT CAN CAUSE ABORTION, PREMATURE BIRTH, OR BIRTH DEFECTS. UTERINE RUPTURE HAS BEEN REPORTED WHEN MISOPROSTOL WAS ADMINISTERED IN PREGNANT WOMEN TO INDUCE LABOR BEYOND THE EIGHTH WEEK OF PREGNANCY. ARTHROTEC MUST NOT BE TAKEN BY PREGNANT WOMEN OR THOSE PLANNING TO BECOME PREGNANT.
NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk.
ARTHROTEC (diclofenac sodium, misoprostol) is contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events.
Are there any other precautions or warnings for this medication?
Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health.
If you have swelling of your face or throat or difficulty breathing, stop taking this medication and seek immediate medical attention.
Diclofenac may cause or worsen anemia (loss of red blood cells). People more prone to anemia should get their blood tested regularly and check for signs of anemia (e.g., weakness and tiredness) while taking this medication.
The use of NSAIDs or aspirin has worsened asthma and its symptoms. If you have asthma, be cautious while taking this medication.
Heart attack and stroke
People who take NSAIDs or COX-2 inhibitors have a higher risk of experiencing a heart attack and/or stroke. The risk for these side effects is higher with larger total daily doses and longer treatment periods. If you have a heart condition or high blood pressure or are planning to have open heart (bypass) surgery, you should be closely monitored by your doctor while taking this medication.
Heart failure and fluid retention
People with heart failure, high blood pressure, and fluid retention may experience edema (swelling of the lower legs, ankles, and feet) or shortness of breath while taking NSAIDs or COX-2 inhibitors. If you develop any of these symptoms while taking this medication, contact your doctor immediately.
Long-term use of diclofenac or other NSAIDs can cause kidney damage and thus is not recommended. In general, NSAIDs and COX-2 inhibitors are not recommended for people with severe kidney disease or limited kidney function.
Diclofenac may increase your liver test results and worsen liver disease. If you have liver disease, you should be closely monitored by your doctor while taking this medication. If signs of liver toxicity occur (such as nausea, tiredness, itching, yellowing of the skin or whites of the eyes, stomach pain, or flu-like symptoms), stop taking this medication and contact your doctor.
Medications like this may cause serious skin reactions. Stop taking this medication and contact your doctor right away if you develop a skin rash that is red, blistering, or peeling.
Diclofenac may cause stomach problems such as ulcers or bleeding. Contact your doctor immediately if you experience stomach pain or vomiting blood or notice black, tarry stools. Ulcers and bleeding can happen without warning symptoms and may cause death. The chance of getting an ulcer or bleeding increases in people taking aspirin, corticosteroids, or blood thinners. The risk also increases with taking higher total daily doses, longer treatment periods, smoking, drinking alcohol, older age, and having poor health.
This medication may cause diarrhea, abdominal pain, upset stomach, and/or nausea in some people. In most cases these problems develop during the first few weeks of therapy and stop after about a week with continued treatment. You can minimize possible diarrhea by making sure you take this medication with meals and by avoiding the use of antacids containing magnesium (if needed, use one containing aluminum or calcium instead).
Misoprostol must not be used during pregnancy because it increases your risk of miscarriage, premature birth, or birth defects.
This medication may pass into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Thus, tell your doctor before using arthrotec if you are breast-feeding. It is not known whether using arthrotec during breastfeeding is dangerous.
The safety and effectiveness of this medication have not been established for children.
What other drugs could interact with this medication?
There may be an interaction between diclofenac sodium and any of the following:
ACE inhibitors (e.g., enalapril, ramipril)
acetylsalicylic acid (aspirin) and other salicylate medications
corticosteroids (e.g., prednisone)
diabetic drugs (e.g., insulin, glyburide, metformin)
drugs for high blood pressure (e.g., metoprolol, diltiazem)
thiazide diuretics (e.g., hydrochlorothiazide)
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:
stop taking one of the medications,
change one of the medications to another,
change how you are taking one or both of the medications, or
leave everything as is.
An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, etc. can affect the action of many medications, you should let your prescriber know if you use them.
Arthrotec User Reviews
Here is a collection of user reviews for the medication Arthrotec.
Comment from: 55-64 on Treatment for 1-2 years (Patient), Published: October 10
Allows me to maintain a fairly normal existence while waiting for a knee replacement. Works quickly and effectively
Comment from: firstname.lastname@example.org, 45-54 on Treatment for less than 1 month (Patient), Published: May 03
I have osteoarthritis of both knees. I recently (7 weeks ago) had total knee replacement on my right knee. My left knee was causing me a great deal of pain (I assume compensating for the recovery of the right knee) and was getting to be intolerable. I have only been taking it for a little over a week and the pain is greatly diminished. I have taken may arthritis-type medications, even Vioxx and never had the relief I have from this.
Comment from: Tina, 55-64 on Treatment for 2-5 years (Patient), Published: November 29
All my joints ache. Since I started taking this 3 yrs ago, I have been able to do more and stand the cold months. It takes away 90% of my pain. I can tell a big difference when I forget to take it. Only problem is now is I have a sore stomach from this and other meds I have to take and have been told to come off it. Personally, I'd rather have the sore stomach than the pain I have without it.
Comment from: 55-64 Female on Treatment for less than 1 month (Patient), Published: December 21
This was prescribed for pain relief associated with a partial rotator cuff tear. It was only mildly effective with side effects including stomach pain and anxiety. I had to stop taking it. 600mg of ibuprophen was more effective and carried no side effects.
Comment from: Ju, 65-74 on Treatment for 2-5 years (Patient), Published: December 18
only helped my stiffness 50% no pain only the stiffness
Comment from: Rosie, 55-64 on Treatment for 1-6 months (Patient), Published: January 08
The only medicine that has helped my arthritis. No side effects.
Comment from: 55-64 on Treatment for 5-10 years, Published: January 23
I suffered with arthritis in my legs for quite some time until my doctor suggested I try Arthrotec. I have used it off and on again for the last 5 years. I am satisfied with the results.
Comment from: qhmamma, 55-64 on Treatment for 6 months - 1 year (Patient), Published: April 13
Dr. took me off Naproxen & started me on Arthrotec. Relieves inflamation better, but not as good for pain so I have to take Tylenol. Relieves about 90% of pain & stiffnes, so at least I now get more sleep at night. Have to take Nexium for stomach but this is risk with ALL NSAID's.
Comment from: lvnvtata, 55-64 on Treatment for 2-5 years (Patient)Published: May 22
When all other arthritis meds caused severe gastric symptoms this is the only med that relieved the pain with no upset stomach. When I forget to take it I can really feel the pain. One caveat, my Dr. says it can cause high blood pressure.
Comment from: Kathy, 65-74 on Treatment for 5-10 years (Patient), Published: February 16
Seems to work well. I make sure I take it with food always, feel relief within an hour. I only use it occasionally though, due to the side effects.
Comment from: Arthrotec 50, 55-64 on Treatment for 2-5 years (Patient), Published: January 04
It has been very effective since my doctor also put me on Nexium 40mg. No sore stomach since stating the Nexium.
Comment from: 35-44 on Treatment for less than 1 month (Patient), Published: March 12
i was given this med while undergoing injections for my knee, seems to work well, but does give me a knotted feeling in my stomache for a few hours, but passes. not sure if i will continue after the injections are completed.
Comment from: 65-74 on Treatment for 1-6 months (Patient), Published: June 06
I had stomach cramps for 4-5 hours after each dose (2 daily). At least once weekly I had severe diarrhea. After two months, I changed medications. I do not recommend this because of the side effects.
Comment from: Pam, 55-64 on Treatment for less than 1 month (Patient), Published: December 14
I had shoulder pain and foot pain and it is completely gone.........unbelieveable in 2 days no pain
Comment from: 45-54 on Treatment for 1-6 months (Patient), Published: September 14
This medicine works better for me than Celebrex, which caused severe stomach aches and diarhea. Prior to taking it for knee problems, I was walking with a limp due to inflexibility and pain.