Ibuprofen, along with diclofenac and acetylsalicylic acid, is one of the most commonly used so-called “acidic” analgesics. Thanks to its acidic nature, ibuprofen, unlike substances such as paracetamol or metamizole, is effective not only against pain, but also against inflammation, because these active substances do not penetrate as well into the inflamed and thus acidified tissue.
Effect of ibuprofen
Ibuprofen is used to relieve mild to moderate pain and to stop inflammation – for example, in rheumatic diseases, which are manifested by painful joint inflammation. Ibuprofen also has an antipyretic effect, but is rarely used therapeutically for this purpose. Ibuprofen belongs to the class of non-steroidal anti-inflammatory drugs (NSAIDs), in contrast to cortisone, for example. The active ingredient ibuprofen is also a representative of the non-opioid analgesics, thus belonging to the group of (unlike opioids) non-addictive and widely used cyclooxygenase inhibitors. The effect of ibuprofen is based on the fact that cyclooxygenase is inhibited. This is why the so-called prostaglandins, which promote inflammation, trigger pain and increase fever, are only produced to a reduced extent. Painkillers: which one, when and for what?
Areas of use of ibuprofen
Ibuprofen is commonly used in the following cases:
- Ibuprofen was particularly often used and originally developed for the treatment of rheumatic joint disease. It relieves the inflammation, swelling and pain associated with osteoarthritis, rheumatoid arthritis and gout.
- In lower doses, ibuprofen is also good for headaches and migraines, as well as toothache or period pain.
- Also ibuprofen is used for muscle pain and sports injuries such as strains and torn ligaments, alternatively diclofenac helps here.
- Other areas of application are pain relief in acute otitis media, tonsillitis or sunburn.
Ibuprofen: dosage
Ibuprofen is sold in a wide variety of dosage forms. It is available as a tablet, capsule, suppository, juice, granules or ointment. The drug is commercially available in a variety of dosages, with low dosages available over-the-counter at pharmacies. Ibuprofen in doses above 400 mg require a prescription. The spectrum of ibuprofen’s effect depends on the dose: lower doses between 200 and 800 mg in adults mainly have an analgesic and antipyretic effect. Only at higher doses of up to 2,400 mg daily does the anti-inflammatory effect come into play. The ingested drugs remain in the blood at the same concentration for about two to three hours, after which the effect decreases. For the most part, the breakdown products are excreted by the kidneys, and some are excreted by the liver.
Ibuprofen: side effects
Side effects common with ibuprofen include stomach pain, nausea, and diarrhea. Rarely, dizziness, headache, and reversible loss of visual acuity occur. As with the related cyclooxygenase inhibitors acetylsalicylic acid and diclofenac, frequent use of ibuprofen can cause gastric bleeding and even gastric perforation. This is because the inhibition of cyclooxygenase not only reduces the production of unwanted prostaglandins that promote inflammation. The prostaglandins that normally protect the stomach also drop out, making the stomach very sensitive to the digestive enzymes it contains and to its own gastric acid. Because of this, prolonged ibuprofen therapy should only be used in combination with gastric protection. Medications that reduce the production of stomach acid are recommended for this purpose, for example proton pump inhibitors such as omeprazole or pantoprazole. In addition, it helps to protect the stomach if these medications are not taken fasting.
Ibuprofen: drug interactions
Parallel therapy with steroidal pain relievers such as cortisone is not advised because it would further increase the risk of bleeding. In addition, ibuprofen has an inhibitory effect on the aggregation of platelets, similar to the effect of acetylsalicylic acid. Therefore, there is an increased risk of bleeding. Concomitant use of other anticoagulants such as Marcumar may therefore be of concern. Paradoxically, nevertheless, the effect of other platelet inhibitors such as acetylsalicylic acid is reduced when taken concomitantly due to competition at the same receptor. This can lead to increased thrombi and embolisms.Because of the difficulty in assessing the effect on one’s own blood clotting, it is essential to inform the attending physician about the prior use of pain medication before surgical procedures.
Ibuprofen in pregnancy
Problems with unwanted prolongation of pregnancy in the setting of prostaglandin use have also been reported: Some prostaglandins have a labor-promoting effect. If these are produced in a diminished manner, labor is correspondingly delayed. According to the doctrine, the treatment of rheumatoid arthritis, in a low dosage of up to 600 mg daily, also seems to be safe during pregnancy and breastfeeding. Other physicians see pregnancy as a clear contraindication to therapy with ibuprofen. In each individual case, it is therefore strongly advised to consult again with the attending physician.
Ibuprofen in children
In contrast to the related acetylsalicylic acid, ibuprofen can also be used in children after consultation with a physician. One reason for treatment is in premature infants, for example. To support their still immature hearts, ibuprofen is used to help close the often still persistent ductus arteriosus botalli, a connection between the venous and arterial systems.
Ibuprofen: contraindications
Caution should be exercised in patients with known inflammatory gastrointestinal diseases such as ulcerative colitis or Crohn’s disease, as taking ibuprofen may trigger an acute episode of these diseases. Less frequently, asthmatics suffer from so-called “aspirin asthma“, which can also occur when taking the painkillers ibuprofen and diclofenac. As a result of the reduced production of prostaglandins, the body converts the original substance into leukotrienes. These trigger coughing and constrict the lungs. Patients who have a strained kidney must also be careful when taking ibuprofen and other cyclooxygenase inhibitors, as the kidney vessels also constrict when fewer prostaglandins are produced. This can further reduce an already low kidney function and, in the worst case, lead to the need for dialysis. The use of ibuprofen in the presence of kidney disease must therefore be carefully monitored. Similar considerations apply to liver disease, since part of the drug is metabolized by the liver. Alcohol consumption during treatment is therefore not advisable, as this puts additional strain on the liver. Regular monitoring of kidney and liver values is therefore important when taking ibuprofen over a longer period of time. In the case of concomitant lithium therapy, special care must be taken to monitor the plasma level of this antidepressant, since lithium excretion in the kidney is reduced by ibuprofen intake. The same applies to therapy with the antiepileptic phenytoin, which is metabolized more slowly in the presence of ibuprofen. Sharp pain
