Increased danger of diclofenac: truth or black PR?

"Magic" pills

There is a group of drugs collectively called non-steroidal anti-inflammatory drugs (NSAIDs), which we all have taken at least once in our lives, and many regularly. These are drugs that have analgesic, anti-inflammatory and/or antipyretic effects. Examples include Aspirin, Nurofen, Nice, Ketanov, Ketoprofen and others. Considering the “magical effects” of their action - relieving inflammation, pain and fever - they are prescribed by almost everyone, everyone, always. Prescribed by traumatologists, rheumatologists, therapists, ENT specialists, dentists. Plus, they can be purchased completely freely at any pharmacy. But, along with the “magical properties”, these drugs have a number of side effects that can be divided into 2 groups: cardio risks and gastro risks. Actually, gastrorisks will be discussed in this article.

How does Ortofen work?

The mechanism of action of all forms of the drug is determined by the non-steroidal anti-inflammatory active component they contain. The injection solution and tablets have a systemic effect, relieve symptoms of fever and acute pain. Diclofenac indiscriminately inhibits the activity of pain and inflammatory prostaglandins, has an antiplatelet property - it increases blood flow. After administration intramuscularly or orally, the medicine is distributed in all fluids and tissues of the body. The liver and kidneys take part in the transformation and filtration of drug metabolites.

Topical preparations: Ortofen ointment and gel have moderate analgesic properties and are used to reduce pain in muscles and joints. Part of the drug is absorbed orally through the skin. With prolonged use, the active substance may accumulate in the blood and affect the tissues of internal organs.

NSAID gastropathy

In the scientific literature, this problem is called “NSAID gastropathy.” The term was first proposed in 1986 to distinguish specific damage to the gastric mucosa that occurs with long-term use of NSAIDs from classic peptic ulcer disease.

The difference between NSAID gastropathy and peptic ulcer disease can also be traced by the affected area. Most often, ulcers can be seen in the stomach, and not in the duodenum. Plus, the changes are more common in older people than in younger people.

Some numbers

Some statistics. In the UK, approximately 24 million NSAIDs are prescribed per year. 70% of people over 70 years of age take NSAIDs once a week, and 34% daily. In the United States, up to 6 billion worth of NSAIDs are sold annually. As a result, the risk of developing gastrointestinal bleeding (GIB) increases 3–5 times, perforation by 6 times, and the risk of death from complications by up to 8 times. Up to 40–50% of all cases of acute gastrointestinal tract infections are associated with NSAIDs.

This problem is also relevant in our country, for example, according to the Scientific Center for Cardiovascular Surgery named after. A.N. Bakulev, out of 240 patients taking aspirin daily, even in small doses, gastroscopy revealed lesions of the stomach and 12 p.c. in 30% (of which ulcers - in 23.6%, erosions - in 76.4%). A similar picture was observed among colleagues from the All-Russian Research Institute of Rheumatology of the Russian Academy of Medical Sciences - in 2126 patients taking NSAIDs without “covering” (protection) of the stomach, erosions and ulcers of the gastroduodenal zone were found in 33.8% of cases. These are very impressive and dramatic numbers of complications from taking NSAIDs, considering the number of people using these drugs in developed countries.

Increased danger of diclofenac: truth or black PR?

The incidence of side effects among patients using the painkiller drug Diclofenac is 50% higher compared to users of other painkillers. This conclusion was reached by a joint group of Danish scientists who conducted a meta-analysis of the side effects of NSAIDs. The result of the study, conducted in Denmark, would not have been in doubt if the work had not been funded by competitors of the drug manufacturer.

Currently, Diclofenac is the most commonly used NSAID. The possibility of its negative side effects on the cardiovascular system has never been specifically studied. However, a number of cohort studies were conducted in Denmark, which formed the basis of this meta-analysis. It was financed by the funds of two pharmaceutical companies - Lundbeck, which specializes in the production of drugs for the treatment of disorders of the central nervous system, and Novo Nordisk. Both firms may have a vested interest in the negative findings of this study.

Although the scientists said funding sources had no influence on the results of the meta-analysis, the findings from the side-effect studies of diclofenac compared with other NSAIDs were so alarming that they suggested a covert order for the result. In particular, scientists say that patients using diclofenac are 50% more likely than patients using other NSAIDs to suffer adverse cardiovascular events. According to the study results, the risk of atrial fibrillation increases by 1.2 times, the risk of ischemic stroke by 1.6 times, the risk of heart failure by 1.7 times, and the risk of myocardial infarction by 1.9 times. Overall mortality from cardiovascular accidents, according to the authors, increases by 1.7 times.

In addition, according to scientists, using diclofenac for a month significantly increases the risk of bleeding in the upper gastrointestinal tract. Compared to the group using other NSAIDs, the risk increases by 2.5 times, and compared to the control group not using drugs - by 4.5 times.

Scientists explain their results by the short half-life of the drugs—1-2 hours after administration. For effective pain relief, the drug is prescribed in a dose significantly higher than the required volume. As the concentration falls, the drug continues to inhibit certain types of enzymes, which contributes to thrombosis, causing pathology of the cardiovascular system.

The result of the meta-analysis was the expected statement that Diclofenac should be excluded from pharmacy sales, and if use is necessary, the patient should be informed about the potential risks. Of course, most often the adverse effects of diclofenac use were noted in patients with high cardiovascular risk, however, according to scientists, the side effect of diclofenac is so strong that it manifests itself within a month after stopping its use, as well as when consuming low doses of the drug. Thus, the study declared the threat of side effects of the drug at any dose, excluding the possibility of a “safe level”.

Such work, by its very existence, will most likely cause a significant drop in sales of diclofenac and, as a result, an increase in the turnover of drugs from competing pharmaceutical manufacturers. There are no indications that the study is biased, but the funding sources suggest deliberate publicity that could deprive diclofenac of its status as the “most commonly used NSAID.”

Pharmedu.ru editors

How it works?

How do these drugs work in our stomachs? Everything is very simple, the negative impact is realized due to the imbalance of defensive and aggressive forces. We have a number of defense mechanisms in our stomach that allow us to withstand the onslaught of aggressors. Among the latest:

• An acid whose pH balance is close to that of battery acid
• Bile and pancreatic juice, which can be thrown into the stomach.
• A number of medications.
• Alcohol and nicotine.
• Irritating food components (spices, spicy foods, etc.)
• Helicobacter pylori infection and so on.

The stomach is protected due to a thick layer of mucus and bicarbonates that neutralize acid, adequate blood supply, and the ability to regenerate very quickly. When we use NSAID drugs, the balance of forces changes towards aggressive mechanisms and damage occurs to the mucous and submucosal layer of the stomach and duodenum.

Diagnostics

To diagnose such changes, gastroscopy is used, which is the “gold standard”. An interesting fact is that about 40% of patients with erosive-ulcerative changes who take these drugs for a long time (more than 6 weeks) do not feel any discomfort or unpleasant, painful sensations. Stomach problems are diagnosed only when visiting other doctors, and not a gastroenterologist. And, conversely, in 40% of patients, despite the complaints they make, nothing is found.

Contraindications and side effects

The drug is not applicable for cases of high sensitivity to salicylates, inflammatory and erosive lesions of the digestive tract mucosa, severe liver and urinary tract diseases. Contraindications also include:

• tendency to internal bleeding, decreased blood clotting;
• Iron-deficiency anemia;
• pregnancy at all stages;
• breastfeeding period.

Ortofen is also prohibited for the treatment of children under 6 years of age. An extensive list of contraindications is explained by high toxicity. Various undesirable reactions are possible against the background of its use:

• loss of appetite, change in taste, pain in the epigastrium, abdominal cavity, exacerbation of gastritis and gastrointestinal pathologies, diarrhea;
• kidney inflammation, impaired diuresis;
• dizziness, asthenic syndrome, insomnia;
• drug hepatosis.

Ortofen should be used with caution in diseases of the heart and blood vessels, bronchial asthma, and diabetes mellitus. Possible signs of a drug overdose: severe headache, vomiting, loss of coordination of movements, deterioration of hearing and vision.

What to do in this case?!

The algorithm of actions for patients who do not have stomach problems and those who have a history of peptic ulcers or erosive changes is different. For the first group, when prescribing non-steroidal anti-inflammatory drugs for more than 5 days, it is mandatory to prescribe drugs from the group of proton pump inhibitors (PPIs). Such as omeprazole, pantoprazole, rabeprazole, etc. (for the entire course of treatment). For the second group, any prescriptions from the NSAID group, regardless of the duration of use, require parallel prescription of proton pump inhibitors. It is also mandatory to take a PPI for patients taking aspirin for a long time.

Myths that we encounter in daily practice

Myth 1. Using NSAID drugs in the form of suppositories is less aggressive for the stomach than taking pills

This is 100% a myth. The pathogenic, destructive effect of the drug is realized through the blood, delivering it through the vessels to the stomach.

Myth 2. Medicines from the group of antacids - Rennie, Maalox, Phosphalugel and H2-blockers (Ranitidine and Famotidine) can be used as “gastroprotectors”

In this case they are not effective.

Myth 3. You can't take proton pump inhibitors regularly

The fact is that if an elderly person has been prescribed an anti-inflammatory drug for life, it is absolutely pointless to prescribe gastroprotection for a month. In such cases, medications should be taken strictly in parallel.

Myth 4. Food products (jelly, etc.) can act as “gastroprotectors”

We will leave this myth as absolutely fantastic without comment.

Application: instructions

Ortofen tablets are taken in one or several doses per day:

• 1 tablet once and up to 3-4 times a day, after eating food or simultaneously with it, the maximum amount of the product is 150 mg;
• in case of severe pain, from the second day of therapy it is recommended to reduce the number of tablets to 2-3 pieces in order to avoid undesirable consequences for the body;
• It is not recommended to take tablets for more than 5 days in a row.

Ortofen injections are indicated intramuscularly. They are administered once, in a dose of no more than 75 mg. active substance. After a single injection, therapy should be continued by taking the drug in tablets.

Gel and ointment are used externally, treating the surface of the skin in the area of ​​damage or inflammation of the joint. The product in an amount of 2–3 g is applied to clean surfaces, rubbing until the medicine is completely absorbed. If necessary, wrap part of the body in warmth. It is recommended to use Ortofen ointment at night or at rest. It is allowed to use up to 8 g of a topical drug per day without health consequences.

Important: when using both systemic and external forms of the medication, you must take into account its total amount when discussing it with your doctor.

When using injections and tablets, you must avoid other NSAIDs and carefully check the dosage of anticoagulants and glucocorticoids, as they increase the toxicity of Ortofen.

How to choose a medicine

In fact, the most important point is which medications we take. In the figure you can see the scale of aggressiveness of various drugs from the NSAID group in relation to the stomach.

The most aggressive drugs are Aspirin, Ketorolac, Piroxicam, Indomethacin. If possible, it is recommended to use selective drugs that have minimal gastrointestinal risks. Their use is always more desirable, these include Celecoxib and Rofecoxib. But despite their relative safety, they should be prescribed strictly according to indications by the attending doctor, do not forget about this.

Summary

So we draw conclusions:

• Before long-term use of NSAIDs, it is mandatory to collect an anamnesis to exclude gastrointestinal pathologies in the past, and, if necessary, perform gastroscopy, diagnosis and treatment of helicobacteriosis.
• When choosing what to treat, if possible, you should choose selective NSAIDs.
• When prescribing non-selective NSAIDs for more than 5 days and in patients with a history of erosive and ulcerative changes, even with selective NSAIDs, it is necessary to take stomach covering drugs (PPIs).
• All patients in the age group over 60 years of age who regularly take aspirin must undergo gastroscopy and, in case of high risks, constantly take drugs from the PPI group.

• Appointment with a gastroenterologist in our clinic
  - 3,900 rubles

Indications for use of Ortofen

The drug is prescribed for moderate to severe pain of various origins, which accompanies injuries, degenerative processes, and inflammatory pathologies. Main area of ​​application: diseases of the joints and muscular system:

• myositis;
• arthritis, arthrosis deformans, spondyloarthrosis;
• tendinitis, sprains and ligament ruptures;
• neuralgic pain;
• rheumatic symptoms;
• lumbago, sciatica, bursitis.

Ortofen helps eliminate pain in intense infectious pathologies, diseases of internal organs and the central nervous system. Including:

• for migraine, tension headache;
• toothache;
• for gynecological pathologies;
• for renal colic;
• for bruises, dislocations.

The antipyretic effect of Ortofen is less pronounced than the analgesic and anti-inflammatory effect, therefore, at high temperatures it is recommended to use other types of NSAIDs.