Ibuprofen. Dosage, Side Effects, Interactions
Ibuprofen is a painkiller (analgesic) from the group of non-steroidal anti-inflammatory drugs (NSAIDs). The active ingredient is used primarily for pain caused by inflammatory processes and for mild to moderate pain such as headaches, toothaches or period pains. Other areas of application are joint pain caused by arthrosis and sports injuries.
Application of Ibuprofen
Ibuprofen belongs to the active substance group of non-steroidal anti-inflammatory drugs/anti-inflammatory drugs (NSAIDs) and is used for the following indications:
- mild to moderate pain
- acute arthritis (including gout attacks )
- chronic arthritis, especially rheumatoid arthritis (chronic polyarthritis)
- Ankylosing spondylitis ( Bechterew’s disease ) and other inflammatory rheumatic diseases of the spine
- Irritation conditions in degenerative joint and spinal diseases ( arthrosis and spondylarthrosis)
- inflammatory soft tissue rheumatic diseases
- painful swelling and inflammation after injury
- Ductus arteriosus Botalli (congenital heart defect)
Ibuprofen is available on the market in the form of tablets, film-coated tablets, soft capsules, suppositories, prolonged-release tablets, syrup, suspensions, effervescent granules, gels and creams.
How Ibuprofen works
Ibuprofen intervenes in the inflammatory process and the perception of pain by inhibiting the cyclooxygenases (COX) COX-1 and COX-2 and thus stopping the formation of prostaglandins. These messenger substances play a key role in the inflammatory process and in the transmission and perception of pain signals. However, prostaglandins also build up the protective gastric mucosa, which is why taking ibuprofen can lead to a reduction in the protective mucus layer inside the stomach. A side effect of COX inhibition is an increased formation of leukotrienes, which can be problematic for asthmatics as they can lead to bronchoconstriction.
In summary, ibuprofen works:
- analgesic (pain reliever)
- anti-inflammatory (anti-inflammatory)
- antipyretic (antipyretic)
- When administered orally, ibuprofen is partially absorbed in the stomach and then completely in the small intestine.
- After hepatic metabolism (hydroxylation, carboxylation), the pharmacologically inactive metabolites are eliminated completely, mainly via the kidneys (90%), but also via the bile.
- The elimination half-life is 1.8 to 3.5 hours in healthy people and those with liver and kidney disease.
- Plasma protein binding is about 99 percent.
- After oral administration of a normal-release dosage form, maximum plasma levels are reached after 1 to 2 hours.
Dosage of Ibuprofen
The recommended dosage of ibuprofen depends on whether patients purchase the drug as self-medication or whether it was prescribed by a doctor.
Within self-medication, the recommended dosages are:
- 5 kg to 6 kg (infants 6 to 8 months): 50 mg ibuprofen every 8 hours
- 7 kg to 9 kg (9 to 12 months): 50 mg ibuprofen every 6 hours
- 10 kg to 15 kg (children: 1 to 3 years): 100 mg ibuprofen every 8 hours
- 16 kg to 20 kg (children: 4 to 6 years): 150 mg ibuprofen every 8 hours
- 20 to 29 kg (children: 6 to 9 years): 200 mg ibuprofen every 8 hours
- 30 to 39 kg (children: 10 to 11 years): 200 mg ibuprofen every 6 hours
- ≥ 40 kg (adolescents 12 years and older and adults): 400 mg ibuprofen every 8 hours
If ibuprofen is prescribed by a doctor, he or she may opt for higher dosages. The recommended dose range for adults and adolescents 15 years and older is between 1200 and 2400 mg ibuprofen per day. The maximum single dose for adults should not exceed 800 mg ibuprofen.
Side effects of Ibuprofen
Adverse drug effects vary with dose and duration of use. Very common side effects (≥1/10) include:
- Gastrointestinal disorders such as heartburn, abdominal pain, nausea, vomiting, flatulence, diarrhea, constipation and minor gastrointestinal blood loss, which in exceptional cases can cause anemia.
Clinical studies indicate that the use of ibuprofen, particularly at high doses (2,400 mg/day), may be associated with a small increased risk of arterial
thrombotic events (e.g. myocardial infarction or stroke ).
Ibuprofen (like other NSAIDs ) should be taken with caution with the following drugs:
- Other NSAIDs including salicylates: Increased risk of gastrointestinal ulcers and bleeding
- Digoxin , phenytoin , lithium : serum levels of these drugs may increase
- Diuretics , ACE inhibitors , beta- blockers and angiotensin II antagonists : Effect of diuretics and antihypertensives can be weakened. Further deterioration in renal function, including possible acute renal failure, may occur in patients with impaired renal function. Such a combination should therefore only be used with caution, especially in elderly patients: Patients must be asked to drink adequate fluids and regular monitoring of their kidney values should be considered
- Potassium-sparing diuretics: hyperkalemia possible
- Glucocorticoids : increased risk of gastrointestinal ulcers or bleeding
- Platelet aggregation inhibitors such as acetylsalicylic acid and selective serotonin reuptake inhibitors ( SSRI ): increased risk of gastrointestinal bleeding
- Low dose acetylsalicylic acid: Effect of low dose acetylsalicylic acid on platelet aggregation may be inhibited. However, due to the limited data, no firm conclusions can be made. A clinically relevant interaction is unlikely with occasional use of ibuprofen
- Methotrexate : increased concentration of methotrexate and increase in its toxic effect
- Ciclosporin : Risk of a kidney-damaging effect by ciclosporin is increased
- Anticoagulants : Effects of anticoagulants such as warfarin can be increased
- Sulfonylureas : Blood glucose monitoring recommended
- Tacrolimus : Risk of nephrotoxicity is increased when both drugs are co-administered
- Zidovudine : evidence of an increased risk of hemarthrosis and hematoma in HIV -positive hemophilia patients taking zidovudine and ibuprofen concomitantly
- Probenecid and sulfinpyrazone : Elimination of ibuprofen may be delayed
Ibuprofen should not be used with:
- a known hypersensitivity to the active substance
- known reactions of bronchospasm, asthma , rhinitis or urticaria after taking acetylsalicylic acid or other non-steroidal anti-inflammatory drugs in the past
- unexplained blood disorders
- Current or history of recurrent peptic ulcer or haemorrhage (at least 2 distinct episodes of proven ulceration or bleeding)
- History of gastrointestinal bleeding or perforation related to previous therapy with non-steroidal anti-inflammatory drugs ( NSAIDs )
- cerebrovascular or other active bleeding
- severe liver or kidney dysfunction
- severe heart failure
- last trimester of pregnancy
Inhibition of prostaglandin synthesis by ibuprofen can adversely affect embryo-foetal development. Epidemiological studies indicate an increased
risk of miscarriage, cardiac malformation and gastroschisis when prostaglandin synthesis inhibitors are used in early pregnancy.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors can cause the following risks:
- cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension)
- Renal dysfunction that may progress to renal failure with oligohydramnios
- possible increase in maternal bleeding time
- Inhibition of uterine contractions, resulting in delayed or prolonged labour
Ibuprofen passes into breast milk, which is why the active ingredient should not be used continuously during breastfeeding.
- In older patients, NSAID therapy is more likely to cause adverse effects, especially gastrointestinal bleeding and perforation, sometimes with a fatal outcome
- Gastrointestinal bleeding, ulceration or perforation, including fatal outcomes, have been reported with all NSAIDs. They occurred with or without prior warning symptoms or a history of serious gastrointestinal events at any time during therapy.
- Appropriate monitoring and counseling of patients with a history of hypertension and/or mild to moderate congestive heart failure is required as fluid retention and edema have been reported in association with NSAID therapy.
- Ibuprofen can temporarily inhibit blood platelet function (platelet aggregation).
- With long-term use, regular monitoring of liver values, kidney function and blood count is required.
- In general, the habitual use of painkillers, especially when several painkillers are combined, can lead to permanent kidney damage with the risk of kidney failure (analgesic nephropathy).
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