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- What are Cox-2 inhibitors?
- For which conditions are Cox-2 inhibitors prescribed?
- Which COX-2 inhibitors are available in the United States?
- What are NSAIDs (nonsteroidal anti-inflammatory drugs)?
- NSAIDs vs. COX-2 inhibitors, which is better?
- What are the side effects of COX-2 inhibitors and/or NSAIDs?
- What drugs interact with COX-2 and/or NSAIDs?
What are Cox-2 inhibitors?
Prostaglandins are made by two different enzymes, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). The prostaglandins made by the two different enzymes have slightly different effects on the body. COX-2 inhibitors are NSAIDs that selectively block the COX-2 enzyme and not the COX-1 enzyme. Blocking this enzyme impedes the production of prostaglandins by the COX-2 which is more often the cause the pain and swelling of inflammation and other painful conditions. Because they selectively block the COX-2 enzyme and not the COX-1 enzyme, these drugs are uniquely different from traditional NSAIDs which usually block both COX-1 and COX-2 enzymes.
For which conditions are Cox-2 inhibitors prescribed?
COX-2 inhibitors are used for treating:
Which COX-2 inhibitors are available in the United States?
What are NSAIDs (nonsteroidal anti-inflammatory drugs)?
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of drugs that reduce inflammation but are different from steroids, another class of drugs that also reduces inflammation. NSAIDs reduce pain, fever, and swelling and are commonly prescribed for inflammation of the joints (arthritis) and other tissues, such as in tendinitis and bursitis. Examples of NSAIDs include:
- indomethacin (Indocin),
- ibuprofen (Advil, Motrin),
- naproxen (Naprosyn),
- piroxicam (Feldene), and
- nabumetone (Relafen).
NSAIDs are used frequently by millions of individuals for treatment of pain, fever and swelling caused by inflammatory conditions as well as for pain alone. NSAIDs work by blocking the production of prostaglandins, chemical messengers that often are responsible for the pain and swelling of inflammatory conditions.
The side effects of NSAIDs are listed below and are compared and contrasted with those of COX-2 inhibitors.
NSAIDs vs. COX-2 inhibitors, which is better?
COX-2 inhibitors impede prostaglandin production. COX-1 is an enzyme which is normally present in a variety of tissues in the body, including sites of inflammation and the stomach. Some of the prostaglandins made by COX-1 protect the inner lining of the stomach. Common NSAIDs such as aspirin block both COX-1 and COX-2 (see below). When the COX-1 enzyme is blocked, inflammation is reduced, but the protection of the lining of the stomach also is lost. This can cause stomach upset as well as ulceration and bleeding from the stomach and even the intestines.
The other cyclooxygenase, COX-2, also produces prostaglandins, but the COX-2 enzyme is located specifically in areas of the body that commonly are involved in inflammation but not in the stomach. When the COX-2 enzyme is blocked, inflammation is reduced; however, since the COX-2 enzyme does not play a role in protecting the stomach or intestine, COX-2 specific NSAIDs do not have the same risk of injuring the stomach or intestines.
Older NSAIDs (for example, aspirin, ibuprofen, naproxen, etc.) all act by blocking the action of both the COX-1 and COX-2 enzymes. COX-2 inhibitors selectively block the COX-2 enzyme and therefore have a lower risk of causing ulcers of the stomach or intestine.
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What are the side effects of COX-2 inhibitors and/or NSAIDs?
Common side effects of COX-2 inhibitors and NSAIDs may include:
- Abdominal pain
- Flatulence (gas)
- Peripheral edema
- Accidental injury
- Upper respiratory tract infection
- Indigestion (dyspepsia)
COX-2 inhibitors may increase the risk of serious, even fatal stomach and intestinal adverse reactions, such as ulcers, bleeding, and perforation of the stomach or intestines but to a lesser extent than other nonselective NSAIDs that block both COX-1 and COX-2. These events can occur at any time during treatment and without warning symptoms.
People allergic to sulfonamides, for example, trimethoprim (Trimpex, Proloprim, Primsol) and sulfamethoxazole (Bactrim), aspirin or other NSAIDs may experience allergic reactions to COX-2 inhibitors and should not take them. Serious allergic reactions have occurred in such patients.
NSAIDs, including COX-2 inhibitors, may increase the risk of heart attacks, stroke, and related conditions. This risk may increase in patients with risk factors for heart disease and related conditions and with longer duration of use; therefore to reduce the risk of heart attacks, stroke, and similar events the lowest effective dose and for the shortest duration of time should be used. NSAIDs should not be used after coronary artery bypass graft (CABG) surgery.
NSAIDs, including COX-2 inhibitors, may cause fluid retention. They should be used cautiously in patients with fluid retention or heart failure.
What drugs interact with COX-2 and/or NSAIDs?
- Combining COX-2 inhibitors with aspirin or other NSAIDs (for example, ibuprofen, naproxen, etc.) may increase the occurrence of stomach and intestinal ulcers. It may be used with low dose aspirin.
- COX-2 inhibitors increase the concentration of lithium (Eskalith, Lithobid) in the blood and may promote lithium toxicity.
- Persons taking the anticoagulant (blood thinner) warfarin (Coumadin, Jantoven) should have their blood tested when initiating or changing COX-2 treatment, particularly in the first few days, for any changes in the effects of the anticoagulant.
- COX-2 inhibitors, like other NSAIDs, may reduce the blood pressure-lowering effects of drugs that are given to reduce blood pressure. This may occur because prostaglandins play a role in the regulation of blood pressure, including ACE inhibitors and angiotensin II antagonists.
- Persons who drink more than three alcoholic beverages per day may be at increased risk of developing stomach ulcers when taking NSAIDs.
COX-2 inhibitors are a class of drugs used for treating the pain and inflammation of conditions such as rheumatoid arthritis and juvenile RA, ankylosing spondylitis, acute pain, and osteoarthritis. Celecoxib (Celebrex) is the only COX-2 inhibitor approved by the FDA for use in the United States.
Common side effects include:
Drug interactions also should be reviewed prior to taking this medication.
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Colon polyps are common growths on the inner lining of the colon. Colon polyps may become cancerous. There are several different types of colon polyps, and the chance of the polyp becoming cancerous depends on the type, size, and histology. Blood in the stool or rectal bleeding are the most common symptoms of colon polyps. Treatment for colon polyps depend on the type, size, and histology.
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Lower Back Pain
There are many causes of back pain. Pain in the low back can relate to the bony lumbar spine, discs between the vertebrae, ligaments around the spine and discs, spinal cord and nerves, muscles of the low back, internal organs of the pelvis and abdomen, and the skin covering the lumbar area.
Nausea and Vomiting
Nausea is an uneasiness of the stomach that often precedes vomiting. Nausea and vomiting are not diseases, but they are symptoms of many conditions. There are numerous cases of nausea and vomiting. Some causes may not require medical treatment, for example, motion sickness, and other causes may require medical treatment by a doctor, for example, heart attack, lung infections, bronchitis, and pneumonia. Some causes of nausea and vomiting may be life-threatening, for example, heart attack, abdominal obstruction, and cancers. Treatment of nausea and vomiting depends upon the cause.
Premenstrual Syndrome (PMS)
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Menstruation (Menstrual Cycle)
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Rheumatoid Arthritis (RA)
Rheumatoid arthritis (RA) is an autoimmune disease that causes chronic inflammation of the joints, the tissue around the joints, as well as other organs in the body. Because it can affect multiple other organs of the body, rheumatoid arthritis is referred to as a systemic illness and is sometimes called rheumatoid disease. The 16 characteristic early RA signs and symptoms include the following. Anemia Both sides of the body affected (symmetric) Depression Fatigue Fever Joint deformity Joint pain Joint redness Joint stiffness Joint swelling Joint tenderness Joint warmth Limping Loss of joint function Loss of joint range of motion Many joints affected (polyarthritis)
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Arthritis (Joint Inflammation)
Arthritis is inflammation of one or more joints. When joints are inflamed they can develop stiffness, warmth, swelling, redness and pain. There are over 100 types of arthritis, including osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, lupus, gout, and pseudogout.
Neck Pain (Cervical Pain)
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Shoulder and Neck Pain
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Ankylosing spondylitis is a type of arthritis that causes chronic inflammation of the spine. The tendency to develop ankylosing spondylitis is genetically inherited. Treatment incorporates medications, physical therapy, and exercise.
Osteoarthritis is a type of arthritis caused by inflammation, breakdown, and eventual loss of cartilage in the joints. Also known as degenerative arthritis, osteoarthritis can be caused by aging, heredity, and injury from trauma or disease.
Sprains and Strains
An injury to a ligament is called a sprain, and an injury to muscle or tendon is called a strain. Sprains and strains may be caused by repetitive movements or a single stressful incident. Symptoms and signs include pain and swelling. Though treatment depends upon the extent and location of the injury, rest, ice, compression, and elevation are key elements of treatment.
Pain management and treatment can be simple or complex, according to its cause. There are two basic types of pain, nociceptive pain and neuropathic pain. Some causes of neuropathic pain include: complex regional pain syndrome, interstitial cystitis, and irritable bowel syndrome. There are a variety of methods to treat chronic pain, which are dependant on the type of pain experienced.
Arthritis, bursitis, IT band syndrome, fracture, and strain are just some of the causes of hip pain. Associated symptoms and signs include swelling, tenderness, difficulty sleeping on the hip, and loss of range of motion of the hip. Treatment depends upon the cause of the hip pain but may include anti-inflammatory medications and icing and resting the hip joint.
Menstrual Cramps and PMS (Premenstrual Syndrome) Treatment
Menstrual cramps and premenstrual syndrome (PMS) symptoms include abdominal cramping, bloating, a feeling of fullness, abdominal pain, mood swings, anxiety and more. Treatment for menstrual cramps and premenstrual syndrome (PMS) symptoms include regular sleep, exercise, smoking cessation, diet changes, and OTC or prescription medication depending on the severity of the condition.
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Nonsteroidal Anti-inflammatory Drugs and Ulcers
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Juvenile Rheumatoid Arthritis (JRA)
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