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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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Intestinal Gas (Belching, Bloating, Flatulence)
Gas (intestinal gas) means different things to different people. Everyone has gas and eliminates it by belching, burping, or farting (flatulence). Bloating or abdominal distension is a subjective feeling that the stomach is larger or fuller than normal. Belching or burping occurs when gas is expelled from the stomach out through the mouth. Flatulence or farting occurs when intestinal gas is passed from the anus. Causes of belching or burping include drinking too rapidly, anxiety, carbonated drinks, habit, and swallowing air. Learn about causes of intestinal gas, foods that cause gas and bloating, treatments that reduce excessive gas and soothe gas pain, and much more.
Diarrhea is a change is the frequency and looseness of bowel movements. Symptoms associated with diarrhea are cramping, abdominal pain, and the sensation of rectal urgency. Causes of diarrhea include viral, bacterial, or parasite infection, gastroenteritis, food poisoning, and drugs. Absorbents and anti-motility medications are used to treat diarrhea.
Low Back Pain (Lumbar Spine 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.
Acute injuries, medical conditions, and chronic use conditions are causes of knee pain. Symptoms and signs that accompany knee pain include redness, swelling, difficulty walking, and locking of the knee. To diagnose knee pain, a physician will perform a physical exam and also may order X-rays, arthrocentesis, blood tests, or a CT scan or MRI. Treatment of knee pain depends upon the cause of the pain.
Premenstrual Syndrome (PMS)
Premenstrual syndrome (PMS) is a combination of physical and emotional disturbances that occur after a woman ovulates and ends with menstruation. Common PMS symptoms include; depression, irritability, crying, oversensitivity, and mood swings. For some women PMS symptoms can be controlled with natural and home remedies, medications, and lifestyle changes such as exercise, nutrition, and a family and friend support system.
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)
Nausea and Vomiting
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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.
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.
Menstruation (Menstrual Cycle)
Menstruation (menstrual cycle) is also referred to as a "period." When a woman menstruates, the lining of the uterus is shed. This shedding of the uterine linking is the menstrual blood flow. The average menstrual cycle is 28 days. There can be problems with a woman's period, including heavy bleeding, pain, or skipped periods. Causes of these problems may be amenorrhea (lack of a period), menstrual cramps (dysmenorrhea), or abnormal vaginal or uterine bleeding. There are a variety of situations in which a girl or woman should see a doctor about her menstrual cycle.
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.
Shoulder and Neck Pain
Shoulder and neck pain may be caused by bursitis, a pinched nerve, whiplash, tendinitis, a herniated disc, or a rotator cuff injury. Symptoms also include weakness, numbness, coolness, color changes, swelling, and deformity. Treatment at home may incorporate resting, icing, and elevating the injury. A doctor may prescribe pain medications and immobilize the injury.
Neck Pain (Cervical Pain)
Neck pain (cervical pain) may be caused by any number of disorders and diseases. Tenderness is another symptom of neck pain. Though treatment for neck pain really depends upon the cause, treatment typically may involve heat/ice application, traction, physical therapy, cortisone injection, topical anesthetic creams, and muscle relaxants.
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.
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.
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.
Psoriatic arthritis is a disease that causes skin and joint inflammation. Symptoms and signs include painful, stiff, and swollen joints, tendinitis, and organ inflammation. Treatment involves anti-inflammatory medications and exercise.
Menstrual cramps (pain in the belly and pelvic area) are experienced by women as a result of menses. Menstrual cramps are not the same as premenstrual syndrome (PMS). Menstrual cramps are common, and may be accompanied by headache, nausea, vomiting, constipation, or diarrhea. Severity of menstrual cramp pain varies from woman to woman. Treatment includes OTC or prescription pain relief medication.
Nonsteroidal Anti-inflammatory Drugs and Ulcers
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Insomnia is the perception or complaint of inadequate or poor-quality sleep because of difficulty falling asleep; waking up frequently during the night with difficulty returning to sleep; waking up too early in the morning; or unrefreshing sleep. Secondary insomnia is the most common type of insomnia. Treatment for insomnia include lifestyle changes, cognitive behavioral therapy, and medication.
Chronic pain is pain (an unpleasant sense of discomfort) that persists or progresses over a long period of time. In contrast to acute pain that arises suddenly in response to a specific injury and is usually treatable, chronic pain persists over time and is often resistant to medical treatments.
Juvenile Rheumatoid Arthritis (JRA)
Juvenile rheumatoid arthritis (JRA) annually affects one child in every thousand. There are six types of JRA. Treatment of juvenile arthritis depends upon the type the child has and should focus on treating the symptoms that manifest.
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