- Am I Taking Too Much Ibuprofen?
- Ibuprofen Side Effects
- In Summary
- For the Consumer
- For Healthcare Professionals
- Further information
- More about ibuprofen
- Serious Side Effects Associated with NSAIDs
- How they work
- Risk of heart failure
- Risk of cardiac arrest
Am I Taking Too Much Ibuprofen?
Q1. Are there any side effects associated with taking ibuprofen daily for a long time? I take about 600 mg each day.
Ibuprofen belongs to the class of drugs known as nonsteroidal anti-inflammatory drugs (NSAIDs), which include such other over-the-counter medications as naproxen and aspirin. These drugs are very effective in relieving minor pain associated with musculoskeletal injuries and arthritis, as well as many other causes of pain. There are, however, significant potential side effects associated with both long-term and short-term use.
The most common of these side effects are related to the stomach and bowels. As many as 50 percent of people, in fact, are unable to take these medications because they experience abdominal pain, diarrhea, and upset stomach. Long-term use can also increase your risk of developing an ulcer in either the stomach or the first part of the small bowel (duodenum). In fact, about 15 percent of chronic NSAID users will develop an ulcer. These ulcers may not cause symptoms until they have seriously progressed, and severe bleeding from the bowels may be the first sign of a problem. It has been estimated that in the last year more than 16,000 deaths and 100,000 hospital admissions resulted from ulcer-related bleeding caused by NSAIDs.
Other potential complications can accompany long-term use — for example, kidney damage and liver impairment. People with asthma may also be sensitive to these drugs. In addition, NSAIDs may interact with other medications, including blood thinners.
Ibuprofen and its cousins are valuable drugs, but it’s important to use them with caution. Even though they are available over the counter, significant potential side effects are associated with their use.
If you develop any gastrointestinal symptoms such as the ones I mentioned above, stop taking the ibuprofen and see your doctor. And next time you visit your doctor, be sure to discuss your ibuprofen use with him or her. If you ever see signs of intestinal bleeding (passage of black stools or blood in the stool), seek medical care immediately.
Q2. Indigestion is a daily problem for me. Presently, I am taking Nexium, two Carafate (nightly), antacids when needed, and Zantac when needed. In the long run, am I harming myself by depending on and taking these medications?
— Bobbi, Florida
First things first. With the number of medications you are taking, you should see a gastroenterologist to make sure that your symptoms are not the result of treatable but potentially more serious conditions rather than indigestion caused by peptic ulcer disease. If other causes are ruled out and your doctor tells you that you have non-ulcer dyspepsia (the medical term used for indigestion), then I would try to simplify your regimen, using as few medications as possible. For example, most of the medications you are taking — Nexium, the antacids, and Zantac — have the same effect, that of reducing the acid load present in your stomach, although they work by means of different mechanisms. Carafate coats the stomach and promotes the healing of inflammation caused by acid or bile. Assuming that acid-blocking medicines have improved your symptoms of indigestion, I recommend increasing the dose of Nexium or Zantac to maintain minimal acid secretion, and taking over-the-counter antacids only as needed.
None of these medications have been associated with dependence, but all can cause side effects, so restricting the number of medicines may reduce your risk of side effects. For example, long-term use of Nexium and other proton pump inhibitors may increase the risk of hip, wrist, or spine fractures, or can lead to a vitamin B12 deficiency. Carafate contains aluminum and can cause constipation.
Bottom line: Consider seeing a gastroenterologist to get a solid diagnosis, and then work to minimize your use of medications.
Learn more in the Everyday Health Digestive Health Center.
“But then he delivered the bombshell,” Christine said. “The ibuprofen had caused an inflammation and the subsequent chain of events. I was so shocked. I had never realised ibuprofen could have such scary side effects.”
The mother was kept in over night and had a visit from her children and husband Nigel, which cheered her up. The next day the doctors were happy for her to be discharged.
Christine was prescribed a drug called Omeprazole and iron tablets.
Now, a month later, she feels better. She said: “I have vowed never to take ibuprofen again and will rely on the much safer option of paracetemol. It still frightens me to think that I ended up in hospital after taking what I regarded as a safe medicine. It was truly horrendous.”
NHS advice states you should only take ibuprofen as directed on the label, or as instructed by a health professional.
The risks of internal bleeding can be increased by half due to taking aspirin.
However, stomach bleeds caused by aspirin are considerably less serious than the spontaneous bleeds that can occur in people not taking the drug, a study has revealed.
Taking a daily paracetamol tablet could put you at risk of deadly heart disease and kidney failure, a new study suggests.
Ibuprofen Side Effects
Medically reviewed by Drugs.com. Last updated on Feb 4, 2019.
- Side Effects
Commonly reported side effects of ibuprofen include: hemorrhage, vomiting, anemia, decreased hemoglobin, eosinophilia, and hypertension. Other side effects include: upper gastrointestinal hemorrhage, upper gastrointestinal tract ulcer, dizziness, and dyspepsia. See below for a comprehensive list of adverse effects.
For the Consumer
Applies to ibuprofen: oral capsule liquid filled, oral suspension, oral tablet, oral tablet chewable
Other dosage forms:
- intravenous solution
Oral route (Tablet; Suspension; Capsule, Liquid Filled; Tablet, Chewable)
NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may be increased in patients with cardiovascular disease or risk factors for cardiovascular disease. Ibuprofen is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery. NSAIDs can also cause an increased risk of serious gastrointestinal adverse events especially in the elderly, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal.
Along with its needed effects, ibuprofen may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur while taking ibuprofen:
- Abdominal pain
- acid or sour stomach
- cloudy urine
- decrease in amount of urine
- decrease in urine output or decrease in urine-concentrating ability
- difficulty having a bowel movement (stool)
- excess air or gas in stomach or intestines
- full feeling
- itching skin
- pain or discomfort in chest, upper stomach, or throat
- pale skin
- passing gas
- noisy, rattling breathing
- rash with flat lesions or small raised lesions on the skin
- shortness of breath
- swelling of face, fingers, hands, feet, lower legs, or ankles
- troubled breathing at rest
- troubled breathing with exertion
- unusual bleeding or bruising
- unusual tiredness or weakness
- weight gain
- Abdominal cramps
- stomach soreness or discomfort
- back, leg, or stomach pains
- bleeding gums
- blistering, peeling, loosening of skin
- blood in urine or stools
- bloody, black, or tarry stools
- blurred vision
- burning feeling in chest or stomach
- change in vision
- chest pain
- clay-colored stools
- cough or hoarseness
- dark urine
- decreased urine output
- difficulty breathing
- difficulty swallowing
- dilated neck veins
- dry mouth
- extreme fatigue
- fast, irregular, pounding, or racing heartbeat or pulse
- fever with or without chills
- frequent urination
- general body swelling
- general feeling of tiredness or weakness
- hair loss, thinning of hair
- hives or welts
- impaired vision
- increased blood pressure
- increased volume of pale, dilute urine
- irregular breathing
- joint or muscle pain
- lab results that show problems with liver
- light-colored stools
- loss of appetite
- lower back or side pain
- muscle twitching
- painful or difficult urination
- pains in stomach, side, or abdomen, possibly radiating to the back
- pinpoint red spots on skin
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- red skin lesions, often with a purple center
- red, irritated eyes
- redness of skin
- severe abdominal pain, cramping, burning
- severe and continuing nausea
- sore throat
- sores, ulcers, or white spots in mouth or on lips
- stiff neck or back
- stomach upset
- swollen or painful glands
- tenderness in stomach area
- tightness in chest
- unpleasant breath odor
- upper right abdominal pain
- vomiting of blood
- vomiting of material that looks like coffee grounds
- yellow eyes and skin
Symptoms of overdose
- Bluish lips or skin
- difficulty sleeping
- dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly
- drowsiness to profound coma
- lightheadedness or fainting
- mood or other mental changes
- muscle tremors
- not breathing
- rapid, deep breathing
- slow or irregular heartbeat
- stomach cramps
- sudden fainting
Some side effects of ibuprofen may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
- Continuing ringing or buzzing or other unexplained noise in ears
- hearing loss
- dry eyes
- feeling sad or empty
- lack of appetite
- loss of interest or pleasure
- mental depression
- quick to react or overreact
- rapidly changing moods
- runny nose
- sleepiness or unusual drowsiness
- stuffy nose
- trouble concentrating
- trouble sleeping
- unable to sleep
For Healthcare Professionals
Applies to ibuprofen: compounding powder, intravenous solution, oral capsule, oral suspension, oral tablet, oral tablet chewable
The most frequently reported adverse effects were gastrointestinal (GI) in nature and included nausea, vomiting, flatulence, and diarrhea.
Patent Ductus Arteriosus: The most frequently reported adverse effects were sepsis, anemia, intraventricular bleeding, apnea, GI disorders, impaired renal function, respiratory infection, skin lesions, hypoglycemia, hypocalcemia, and respiratory failure.
Very common (10% or more): Nausea (up to 57%), vomiting (up to 22%), flatulence (up to 16%), diarrhea (up to 10%)
Uncommon (0.1% to 1%): Abdominal distention, dyspepsia, gastritis
Very rare (less than 0.01%): Peptic ulcer, perforation, hematemesis, mouth ulceration, exacerbation of colitis, exacerbation of Crohn’s disease
Frequency not reported: Dry mouth, duodenitis, esophagitis, gastric ulcer, duodenal ulcer, GI bleeding, glossitis, rectal bleeding, stomatitis, eructation, gingival ulcer, pancreatitis
Patent Ductus Arteriosus:
Very common (10% or more): GI disorders non-necrotizing enterocolitis (22%)
Common (1% to 10%): Necrotizing enterocolitis, intestinal perforation
Frequency not reported: Abdominal distension, gastroesophageal reflux, gastritis, ileus, inguinal hernia
Postmarketing reports: GI perforation
Very common (10% or more): Hemorrhage (up to 10%), hypertension (10%), hypotension (10%)
Very rare (less than 0.01%): Cardiac failure
Frequency not reported: Congestive heart failure, tachycardia, arrhythmia, myocardial infarction, palpitations, vasculitis, sinus bradycardia, angina pectoris, thrombotic events
Patent Ductus Arteriosus:
Frequency not reported: Tachycardia, cardiac failure, hypotension
Very common (10% or more): Headache (up to 12%)
Common (1% to 10%): Dizziness, nervousness
Very rare (less than 0.01%): Cerebrovascular accident
Frequency not reported: Syncope, drowsiness, paresthesia, somnolence, tremors, convulsions, coma
Patent Ductus Arteriosus:
Common (1% to 10%): Intraventricular hemorrhage, periventricular hemorrhage
Frequency not reported: Convulsions
Very rare (less than 0.01%): Acute renal failure, renal papillary necrosis, interstitial nephritis, nephrotic syndrome, renal failure, renal insufficiency
Frequency not reported: Cystitis, azotemia, creatinine clearance decreased, glomerulitis, tubular necrosis, nephrotoxicity
Patent Ductus Arteriosus:
Very common (10% or more): Renal events (21%)
Uncommon (0.1% to 1%): Acute renal failure
The incidence of total bleeding events within 30 days of therapy with IV use in preterm infants was 32%. This percentage included grade 1 and 2 intraventricular hemorrhage (15%), grade 3 and 4 intraventricular hemorrhage (15%), and other bleeding (6%).
Very common (10% or more): Anemia (up to 36%), eosinophilia (up to 26%), neutropenia (up to 13%), thrombocythemia (up to 10%)
Common (1% to 10%): Hemoglobin decreased
Very rare (less than 0.01%): Leukopenia, thrombocytopenia, agranulocytosis, hemolytic anemia, aplastic anemia, pancytopenia, hematocrit decreased
Frequency not reported: lymphadenopathy, bleeding episodes
Patent Ductus Arteriosus:
Very common (10% or more): Anemia (32%), total bleeding (32%), intraventricular hemorrhage (29%), Neutropenia, thrombocytopenia
Common (1% to 10%): Rash, maculopapular rash, pruritus
Very rare (less than 0.01%): Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis
Frequency not reported: Ecchymosis, purpura, alopecia, sweating, photosensitivity, angioedema, exfoliative dermatitis, urticaria, vesiculobullous eruptions, Henoch Schonlein vasculitis
Patent Ductus Arteriosus:
Very common (10% or more): Skin lesion/irritation (16%)
Common (1% to 10%): Appetite decreased, fluid retention
Frequency not reported: Appetite changes, hyperglycemia, hypoglycemic reaction, acidosis
Patent Ductus Arteriosus:
Very common (10% or more): Hypoglycemia (12%), hypocalcemia (12%), blood creatinine increased, blood sodium decreased
Common (1% to 10%): Hypernatremia
Frequency not reported: Feeding problems, hyperglycemia
Very common (10% or more): Bacteremia (13%), blood LDH increased (up to 10%)
Common (1% to 10%): Peripheral edema, wound hemorrhage, tinnitus, hearing impairment, edema, fatigue
Very rare (less than 0.01%): Aseptic meningitis, vertigo, exacerbation of infection-related inflammations
Frequency not reported: Fever, infection, sepsis, weight changes, asthenia, malaise, pseudo-tumor, hearing loss, drowsiness
Patent Ductus Arteriosus:
Very common (10% or more): Sepsis (43%)
Common (1% to 10%): Edema, fluid retention
Frequency not reported: Various infections
Very common (10% or more): Bacterial pneumonia (up to 10%)
Common (1% to 10%): Cough
Very rare (less than 0.01%): Asthma, bronchospasm, dyspnea, wheezing
Frequency not reported: Apnea, respiratory depression, pneumonia, rhinitis, epistaxis
Patent Ductus Arteriosus:
Very common (10% or more): Apnea (28%), respiratory infection (19%), respiratory failure (10%), bronchopulmonary dysplasia
Common (1% to 10%): Atelectasis, pulmonary hemorrhage
Uncommon (0.1% to 1%): Hypoxemia
Postmarketing reports: Pulmonary hypertension
Very rare (less than 0.01%): Hepatitis, jaundice
Frequency not reported: Hepatorenal syndrome, liver necrosis, liver failure, abnormal liver function tests
Patent Ductus Arteriosus:
Frequency not reported: Cholestasis, jaundice
Hypersensitivity reactions have been reported and may consist of any of the following: a syndrome of abdominal pain, fever, chills, nausea, vomiting, and anaphylaxis; respiratory tract reactivity comprising bronchospasm, asthma/aggravated asthma, or dyspnea; skin reactions, which rarely included exfoliative and bullous dermatoses, Stevens-Johnson syndrome, toxic epidermal necrolysis, angioedema, pruritus, and urticaria.
Frequency not reported: Anaphylactoid reactions, hypersensitivity reaction
Very rare (less than 0.01%): Visual disturbances
Frequency not reported: Blurred vision, amblyopia, diminished vision, scotomata, changes in color vision, conjunctivitis, dry eyes, diplopia, optic neuritis, cataracts, optic neuritis, toxic optic neuropathy
Frequency not reported: Lupus erythematosus syndrome
Frequency not reported: Anxiety, confusion, depression, dream abnormalities, insomnia, emotional lability, hallucinations
Common (1% to 10%): Urinary retention
Very rare (less than 0.01%): Proteinuria, hematuria
Frequency not reported: Dysuria, oliguria, polyuria, menorrhagia
Patent Ductus Arteriosus:
Very common (10% or more): Oliguria, hematuria
Common (1% to 10%): Urinary tract infection
Frequency not reported: Serum sickness
Common (1% to 10%): Infusion site pain
Postmarketing reports: Transient sensation of burning in mouth/throat
Patent Ductus Arteriosus:
Frequency not reported: Injection site reactions
Frequency not reported: Gynecomastia
Patent Ductus Arteriosus:
Common (1% to 10%): Adrenal insufficiency
1. “Product Information. Motrin (ibuprofen).” Pharmacia and Upjohn, Kalamazoo, MI.
2. Cerner Multum, Inc. “Australian Product Information.” O 0
3. “Product Information. Caldolor (ibuprofen).” Cumberland Pharmaceuticals Inc, Nashville, TN.
4. Cerner Multum, Inc. “UK Summary of Product Characteristics.” O 0
5. “Product Information. NeoProfen (ibuprofen).” Ovation Pharmaceuticals Inc, Deerfield, IL.
6. “Product Information. Ibuprofen (ibuprofen).” Par Pharmaceutical Inc, Spring Valley, NY.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Some side effects may not be reported. You may report them to the FDA.
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Headache. Aching or injured back. Sore muscles or joints after overdoing it on the tennis or basketball court or golf course. Or even a long day in the garden.
These aches and pains are among the reasons that every day, nearly 1 in 5 Americans (17%) turn to a group of over-the-counter and prescription pain relievers collectively known as “NSAIDs” – nonsteroidal anti-inflammatory drugs. The best-known ones are ibuprofen (Advil, Motrin), naproxen (Aleve) and good old aspirin.
They work — and work well — by blocking the production of substances in the body called prostaglandins that trigger pain and inflammation.
Even as misuse and abuse of stronger opioid pain relievers gets all the media attention, there’s long been concern that NSAIDs, too, are overused. And that overuse may be on a much larger scale since it involves tens of millions of Americans who take the medicines regularly for mild pain and muscle soreness, pain that almost always resolves itself in a couple days.
Many older people also take these medicines on a regular basis (often every day) for the joint pain and stiffness associated with osteoarthritis and normal aging. About 1/3 of adults age 65 and older have osteoarthritis.
Serious Side Effects Associated with NSAIDs
The concern on both counts revolves around the quite serious side effects the medicines can cause, and the risks they pose — especially if overused at higher doses for long periods. Two recent reports from Consumer Reports discuss the issue and offer detailed recommendations. One is the cover story in the June 2016 issue of Consumer Reports magazine. The second is an updated report on NSAIDs from Consumer Rehttp://www.consumerreports.org/cro/2013/07/treating-pain-with-nsaid-medications/index.htmports Best Buy Drugs, available online.
“There’s little doubt that NSAIDs are overused for the everyday aches and pains that come with advancing years,” says Marvin M. Lipman, MD, chief medical adviser at Consumer Reports. “Long-term use of any pain killer requires close medical supervision.”
Here’s the most salient advice distilled from both articles, which draw on the latest research:
- All the NSAIDs — there are about 20, with some available only by prescription — can cause serious side effects. These include stomach ulcers, gastrointestinal (GI) bleeding, kidney failure, heart attacks and strokes. Aspirin is the exception. It can cause GI bleeding and stomach ulcers but not heart attacks and strokes. Indeed, at low doses, aspirin can help prevent heart attacks and strokes, which are caused by blood clots that aspirin can counter.
- The risk of GI and stomach ulceration and bleeding is more serious than most people think. An estimated 7,000 to 10,000 Americans die each year from this NSAID risk. That risk increases with age and with length of use. People 75 and over have about a 1% chance of gastrointestinal bleeding if they take an NSAID for over a week or so. (See table below.)
- People of any age who have previously had stomach bleeding or ulcers should consider taking acetaminophen (Tylenol) instead of an NSAID for minor aches and pains.
- If you are taking corticosteroids, or blood thinners — for example, clopidogrel (Plavix) or warfarin (Coumadin) — tell your doctor before taking an NSAID. These medicines also increase the risk of bleeding and thus add to the risk of bleeding you’ll get from an NSAID.
- The bleeding risk is dose and time dependent. That is, taking an NSAID every day at high doses for long periods (more than a few weeks) increases the chances of experiencing a bleeding episode — for people of any age. In contrast, taking NSAIDs every so often (as much as once or twice a week) at low doses does not appear to be associated with any significant stomach or GI bleeding risk. That puts most of us in the clear. But everyone should abide by the general advice to take the lowest dose of an NSAID that brings relief and take it for as short a time as possible.
Bleeding Risk Associated With NSAIDs
|Age||Risk of GI bleeding each year||Risk of dying from GI bleeding each year|
|Risk in any one year is:|
|16-44||1 in 2,100||1 in 12,353|
|45-64||1 in 646||1 in 3,800|
|65-74||1 in 570||1 in 3,353|
|>75||1 in 110||1 in 647|
|Source: Blower A, Brooks A, Fenn G, Hill A, Pearce M, Morant S. Emergency admissions for upper gastrointestinal disease and their relation to NSAID use. Aliment Pharm Ther. 1997(11):283-291.|
Risk of Heart Problems and Stroke
- If you have heart or kidney disease or have high blood pressure, or are considered at risk of having a heart attack or stroke for any reason, talk with your doctor about limiting the use of NSAIDs and taking an alternative medicine instead. All NSAIDs (except aspirin) carry a warning on their labeling that if used in certain ways they have the potential to increase the risk of heart attack and stroke.
- Acetaminophen (Tylenol) is the most commonly used alternative to NSAIDs. It isn’t as effective at relieving some pains — such as muscle and joint pain — as an NSAID, but it doesn’t carry a risk for stomach bleeding or heart attack or stroke.
- The precise dose or length of use at which the heart risks of NSAIDs outweigh the benefits can’t be easily pinned down. The risk differs from person to person. As a rough rule of thumb, though, studies indicate that taking 800mg (4 pills) or more of an NSAID every day for a few weeks or more increases a 55-year old man’s risk of heart attack by 50% to 100%. Since the risk is small to begin with, the increased risk is also small. (By way of illustration, if a risk starts out at 1 in 100 and doubles, it’s 2 in 100, still small but not negligible.)
- Research indicates that all NSAIDs, except naproxen and aspirin, carry about the same heart attack and stroke risk.
- Naproxen may be a better choice for people who have higher risk of heart attacks or strokes, since the available evidence indicates it doesn’t increase the risk of these conditions as much as other NSAIDs.
- NSAIDs can aggravate high blood pressure, which is one way they could raise the risk of heart attack. They also cause fluid retention, which can lead to slight weight gain or swollen legs even in healthy individuals.
- For people who have a “weak heart” (due to congestive heart failure, for example) fluid retention due to NSAIDs could make symptoms worse and increase the risk of hospitalization.
- NSAIDs have been associated with kidney failure, so people with kidney disease due to diabetes or other causes should not take NSAIDs unless your doctor has said it is appropriate for your situation.
- If your doctor prescribes an NSAID, tell him or her about any other medicines or dietary supplements you are taking, including daily aspirin to reduce your risk of heart attack or stroke. NSAIDs can interact with other medicines, including other NSAIDs, such as aspirin, and can increase the risk of having a serious side effect.
Who needs an NSAID?
|May Need an NSAID||
|May Want to Take NSAIDs With Extra Caution||
|May Want to Avoid NSAID||
|Source: Consumer Reports Best Buy Drugs|
Pain Relief: What You Need to Know (Consumer Reports)
Pain Relief with NSAID Medications (Consumer Reports)
Medications such as ibuprofen and aspirin, known as non-steroidal anti-inflammatory drugs or NSAIDs, are widely available over the counter from pharmacies and supermarkets. But health providers have known for some time they can be unsafe for people with chronic health problems such as kidney disease, high blood pressure, or heart failure.
NSAIDs can also have dangerous interactions with other commonly taken medications, notably many types of blood pressure and blood-thinning pills such as warfarin and aspirin.
Two recently published studies have brought back into the spotlight the possible heart-related side effects of NSAIDs. One found an increased risk of heart failure in users of NSAIDs, while another an increased risk of cardiac arrest.
Heart failure is a disease that presents with symptoms such as shortness of breath, fluid retention, leg swelling, and fatigue. This is a result of the heart not being able to pump blood around the body effectively. There are many causes of heart failure, including heart attacks, high blood pressure and excessive alcohol consumption.
A cardiac arrest occurs when the heart stops functioning abruptly and results in complete loss of effective blood flow through the body. The most common cause of a cardiac arrest is a heart attack, where heart muscle is damaged from loss of blood supply due to a blockage in a heart blood vessel. There are many other causes of a cardiac arrest that include structural heart abnormalities and inherited heart diseases of muscle and electrical function.
The recent studies are an important reminder that over-the-counter medicines are not without risk. This class of anti-inflammatory pain killers should no longer be available for sale in grocery stores, but instead restricted to prescription-only or behind-the-counter status in pharmacies.
How they work
Non-steroidal anti-inflammatory drugs are commonly used to relieve pain. They can be either prescribed by a doctor or purchased by the patient over the counter from a supermarket or pharmacy.
NSAIDs are used in a broad range of health conditions associated with pain and inflammation, including types of arthritis, headaches, musculoskeletal injuries, and menstrual cramps. Their easy availability, effectiveness, and presumption of safety contribute to their widespread use.
They work by inhibiting enzymes called cyclooxygenase 1 (COX-1) and 2 (COX-2). These are involved in a number of internal pathways that result in production of hormone-like substances called prostaglandins, which promote inflammation and increase pain perception.
Prostaglandins also protect the stomach lining from acid, by decreasing acid production and increasing mucus secretion and its neutralising properties. So inhibiting prostaglandins also reduces their protective functions. This is why frequent users of anti-inflammatories may suffer from gastric ulcers.
NSAIDs can either inhibit both COX-1 and COX-2 (non selective) or inhibit COX-2 only (selective). Drugs like ibuprofen and aspirin are non-selective and inhibit both the COX enzymes.
COX-1 mediates gastrointestinal, kidney, and clotting function, while COX-2 is induced primarily in states of inflammation and tissue repair. That’s why blocking the COX-2 pathway reduces the effects of inflammation such as fever, swelling, redness and pain.
Importantly, COX-2 inhibition accounts for the anti-inflammatory drug effects of NSAIDs, while COX-1 inhibition can lead to side effects including gastrointestinal ulcers, prolonged bleeding and impaired kidney function. However, it’s not entirely safe for the drugs to inhibit COX-2 only.
Animal studies have shown blocking COX-2 and the subsequent pathway of prostaglandin production may have the unwanted effects of increasing the tendency of blood to clot inside arteries, and a reduced ability of the heart to heal after a heart attack.
In the early 2000s, a number of large studies found a significant association of negative heart events, such as heart attack and stroke, with the use of selective COX-2 inhibitors. This resulted in two of these drugs, Valdecoxib and Rofecoxib or Vioxx, being withdrawn from the market.
In Australia there are only a small number of COX-2 inhibitors available, including Celecoxib and Meloxicam. These are prescription-only medicines and the maximum prescribed dose is at a level at which the heart risks are minimal.
COX-2 inhibitors are used in people who require a non-steroidal anti-inflammatory but have a history of stomach upset or ulcers, or who were thought to be at risk of developing stomach ulcers.
Risk of heart failure
Non-steroidal anti-inflammatory drugs are associated with elevating blood pressure as well as sodium and fluid retention. Both of these effects may unmask previously-undiagnosed heart failure, or worsen the symptoms in people known to already have heart failure.
Research published in the British Medical Journal in September 2016 studied 92,163 people admitted to hospital with heart failure, and found NSAID use in the two weeks prior to admission was associated with a 19% increased risk of hospital admission for heart failure. This was compared with people who had not used NSAIDs prior to admission.
The association of NSAIDs with an exacerbation of heart failure was also seen in many older studies. For example, an Australian study in 2000, suggested almost 20% of all heart failure related admissions to hospital may be attributed to recent NSAID use.
Risk of cardiac arrest
Further heart safety concerns with NSAIDs were raised in a recent study from the University of Copenhagen, published in the European Heart Journal.
Data was collected from nearly 30,000 patients who had suffered cardiac arrest between 2001 and 2010. Of these, around 3,500 were found to have been treated with an NSAID within 30 days of having a cardiac arrest.
Use of any NSAID was associated with a 31% increased risk of cardiac arrest. The commonly used non-selective NSAIDs, diclonenac (Voltaren) and ibuprofen were associated with a 50% and 31% increased risk respectively.
A large proportion of cardiac arrest is a result of clot formation in the arteries of the heart and underlying plaque formation which can rupture. NSAIDs may increase the risk of cardiac arrest by raising blood pressure, forming blood clots and blocking the heart’s own blood vessels.
It is important to emphasize that in people with no known heart disease and who don’t have any heart risk factors, short term use of these anti-inflammatories carries a minimal increase in heart-related risk.
These recent studies should not create community panic about the safety of NSAIDs when used for short periods of time and at low dosage.
But the high burden of heart disease and heart disease risk factors, such as high blood pressure, obesity and diabetes (which are often unrecognized), warrant a personalized approach to NSAIDs, which weighs the benefits and risks of their use.
This was recommended in the Therapeutic Goods Administration review of the heart related effects of NSAIDs in 2014. These anti-inflammatories should be available for purchase through prescription by a medical practitioner or behind the counter at the pharmacy.
Peter Psaltis receives research funding from the National Health and Medical Research Council of Australia, National Heart Foundation of Australia and Abbott Vascular Pty Ltd.
This article was originally published on The Conversation. Read the original article.