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Pain Medications : NSAIDs Last Updated: Jul 1, 2011 - 8:08:19 PM


Ibuprofen
By steve Steele
Jan 15, 2000 - 3:59:16 PM

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Ibuprofen (INN) (from the now-outdated nomenclature iso-butyl-propanoic-phenolic acid) is a non-steroidal anti-inflammatory drug (NSAID) originally marketed as Brufen, and since then under various other trademarks (see availability section), most notably Nurofen, Advil, and Motrin. It is used for relief of symptoms of arthritis, primary dysmenorrhea, fever, and as an analgesic, especially where there is an inflammatory component. Ibuprofen is known to have an antiplatelet effect, though it is relatively mild and short-lived when compared with that of aspirin or other better-known antiplatelet drugs. Ibuprofen also generally acts as a vasodilator, having been shown to dilate coronary arteries and some other blood vessels. Ibuprofen is a core medicine in the World Health Organization's "Essential Drugs List", which is a list of minimum medical needs for a basic health care system.

Mechanism of action

Non-steroidal anti-inflammatory drugs such as ibuprofen work by inhibiting the enzyme cyclooxygenase (COX), which converts arachidonic acid to prostaglandin H2 (PGH2). PGH2, in turn, is converted by other enzymes to several other prostaglandins (which are mediators of pain, inflammation, and fever) and to thromboxane A2 (which stimulates platelet aggregation, leading to the formation of blood clots).

Like aspirin, indomethacin, and most other NSAIDs, ibuprofen is considered a non-selective COX inhibitor—that is, it inhibits two isoforms of cyclooxygenase, COX-1 and COX-2. The analgesic, antipyretic, and anti-inflammatory activity of NSAIDs appears to be achieved mainly through inhibition of COX-2, whereas inhibition of COX-1 would be responsible for unwanted effects on platelet aggregation and the gastrointestinal tract. However, the role of the individual COX isoforms in the analgesic, anti-inflammatory, and gastric damage effects of NSAIDs is uncertain and different compounds cause different degrees of analgesia and gastric damage. In order to achieve the beneficial effects of ibuprofen and other NSAIDS without gastrointestinal ulceration and bleeding, selective COX-2 inhibitors were developed to inhibit the COX-2 isoform without inhibition of COX-1.

Ibuprofen is in a group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). It works by reducing hormones that cause inflammation and pain in the body.

Ibuprofen is used to reduce fever and treat pain or inflammation caused by many conditions such as headache, toothache, back pain, arthritis, menstrual cramps, or minor injury.

Important information about ibuprofen

Ibuprofen can increase your risk of life-threatening heart or circulation problems, including heart attack or stroke. This risk will increase the longer you use ibuprofen. Do not use this medicine just before or after having heart bypass surgery (also called coronary artery bypass graft, or CABG).

Seek emergency medical help if you have symptoms of heart or circulation problems, such as chest pain, weakness, shortness of breath, slurred speech, or problems with vision or balance.

Ibuprofen can also increase your risk of serious effects on the stomach or intestines, including bleeding or perforation (forming of a hole).

Call your doctor at once if you have symptoms of bleeding in your stomach or intestines. This includes black, bloody, or tarry stools, or coughing up blood or vomit that looks like coffee grounds.

Do not take more ibuprofen than is recommended. An overdose can cause damage to your stomach or intestines. Use only the smallest amount of ibuprofen needed to get relief from your pain, swelling, or fever.

Before taking ibuprofen

NSAIDs can increase your risk of life-threatening heart or circulation problems, including heart attack or stroke. This risk will increase the longer you take ibuprofen. Do not use this medicine just before or after having heart bypass surgery (also called coronary artery bypass graft, or CABG).

NSAIDs can also increase your risk of serious effects on the stomach or intestines, including bleeding or perforation (forming of a hole). These conditions can be fatal and gastrointestinal effects can occur without warning at any time while you are taking an NSAID.

Do not use this medication if you are allergic to ibuprofen, aspirin or other NSAIDs.

Ask a doctor or pharmacist if it is safe for you to take this medication if you have:

  • a history of heart attack, stroke, or blood clot;

  • heart disease, congestive heart failure, high blood pressure;

  • a history of stomach ulcers or bleeding;

  • asthma;

  • polyps in your nose;

  • liver or kidney disease;
  • systemic lupus erythematosus (SLE);

  • a bleeding or blood clotting disorder; or

  • if you smoke.

FDA pregnancy category C. It is not known whether ibuprofen is harmful to an unborn baby. However, taking ibuprofen during the last 3 months of pregnancy may result in birth defects. Do not take ibuprofen during pregnancy unless your doctor has told you to. It is not known whether ibuprofen passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medicine to a child without the advice of a doctor.

Ibuprofen side effects

Get emergency medical help if you have any of these signs of an allergic reaction to ibuprofen: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking ibuprofen and seek medical attention or call your doctor at once if you have any of these serious side effects:

  • 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, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);

  • fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;

  • bruising, severe tingling, numbness, pain, muscle weakness; or

  • severe headache, neck stiffness, chills, increased sensitivity to light, and/or seizure (convulsions).

Less serious ibuprofen side effects may include:

  • upset stomach, mild heartburn, diarrhea, constipation;

  • bloating, gas;

  • dizziness, headache, nervousness;

  • skin itching or rash;

  • blurred vision; or

  • ringing in your ears.

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.

What other drugs will affect ibuprofen?

Tell your doctor if you are taking an antidepressant such as citalopram (Celexa), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, Symbyax), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor). Taking any of these drugs with ibuprofen may cause you to bruise or bleed easily.

Before taking ibuprofen, tell your doctor if you are taking any of the following drugs:

  • aspirin or other NSAIDs such as diclofenac (Voltaren), etodolac (Lodine), indomethacin (Indocin), meloxicam (Mobic), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others;

  • an ACE inhibitor such as benazepril (Lotensin), fosinopril (Monopril), enalapril (Vasotec), lisinopril (Prinivil, Zestril), quinapril (Accupril), ramipril (Altace), and others;

  • lithium (Eskalith, Lithobid);

  • diuretics (water pills) such as furosemide (Lasix);

  • methotrexate (Rheumatrex, Trexall);

  • steroids (prednisone and others); or

  • a blood thinner such as warfarin (Coumadin).

This list is not complete and there may be other drugs that can interact with ibuprofen. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

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