What Is Ibuprofen?

Ibuprofen is one of the first options for pain (pain reliever), inflammation or fever.

Widely used, ibuprofen is the all-purpose analgesic par excellence but one that we must take with care.

Ibuprofen thus belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). It is one of the first options when dealing with pain (pain reliever), inflammation or fever.

It is estimated that almost half of the population suffers from headaches. 30 million people suffer from low back pain. At least as many people are affected by pain related to cancer, heart disease and other illnesses.

Ibuprofen will therefore be part of the treatment for the majority of these cases. This gives us an idea of ​​the use of this medicine.

What is ibuprofen used for?

Ibuprofen is a drug that can be found in tablet, powder, or syrup form. In all cases it is an anti-inflammatory, an analgesic and an antipyretic.

The main indications for ibuprofen are as follows:

1. Treatment of situations involving pain or inflammation such as headaches, migraines. It is also taken in case of dysmenorrhea, pharyngitis, ear infections or muscle pain.
2. Symptomatic treatment of fever.
3. In pathologies such as juvenile rheumatoid arthritis and rheumatic processes (osteoarthritis).
4. Treatment of soft tissue injuries such as sprains or strains.

Mechanism of action of ibuprofen

The mechanism of action of ibuprofen is to inhibit the synthesis of prostaglandins.

This inhibition is due to the competitive and reversible union of the enzyme cilco oxygen. This is transformed into arachidonic acid in these so-called prostaglandins.

Structurally, ibuprofen is a derivative of propanoic acid. It is indeed a racemic compound (two compounds which are spectacular images of each other). Its activity is attributed almost entirely to the S isomer.

Pharmacokinetics: What Happens to Ibuprofen in the Body?

Ibuprofen is a drug that is poorly soluble in water. However, it is often used in the form of arginate or lisinate salts to improve its solubility and also its pharmacokinetic profile.

Its most important features are:

• Absorption. The most widely used routes of administration are thus oral and parenteral. Oral administration is good and rapid and its bioavailability is also 80% (it varies depending on the pharmaceutical form). The arginine and lisine salts thus promote the solubility of ibuprofen. It is therefore absorbed more quickly.
• Distribution. Ibuprofen binds efficiently to plasma proteins (90-99%). It is thus able to spread through the tissues, to pass to the synovial fluid but also to cross the placental barrier. On the other hand, its presence has not yet been detected in the milk of nursing women.
• Metabolism. Its metabolization occurs mainly in the liver by hydroxylation and carboxylation, generating various inactive metabolites.
• Excretion. Ibuprofen is mainly excreted in the urine (90%) and in smaller quantities in the stool. Its complete elimination from the body then takes 24 hours.

Dosage

The dosage rules depend on which pharmaceutical form is considered best for each patient. It is therefore recommended to consult the instructions for each drug in a specific way.

However, in general we can say that:

• In adults, oral administration should be between 400 and 600 mg every 6/8 hours. However, do not exceed 2,400 mg per day.
• In children from 3 months to 11 years old, it is recommended to administer 20 to 30 mg / kg / day in 3 or 4 divided doses. However, the safety and efficacy in children under 3 months of age has not yet been evaluated.

The parenteral route is only recommended for adults. Do not exceed 600 mg every 6-8 hours. You will need to switch to oral ibuprofen as soon as possible.

You should also take into account the existence of kidney and liver diseases, which will always require you to use it with caution and in the smallest possible doses.

Ibuprofen contraindications and precautions

It is best to avoid ibuprofen in the following situations:

• Hypersensitivity to ibuprofen. Indeed, cases of hypersensitivity reactions mixed with other NSAIDs have been identified. This is why it should not be used in case of allergy to salicylic acid. These reactions are particularly common in patients with asthma.
• Peptic ulcer, inflammatory bowel disease, or any process that increases the risk of gastrointestinal bleeding. Indeed, because of the inhibition of the synthesis of prostaglandins, ibuprofen could thus increase the risk of digestive hemorrhage and perforation. This is why ibuprofen and any other NSAIDs should therefore be taken with meals to reduce stomach problems. Another option would be to combine it with an anti-ulcer (anti H2 or IBP).
• Coagulation alterations. Ibuprofen exhibits platelet anticoagulant effects and also increases bleeding time.
• Renal failure. The urine eliminates ibuprofen. It could build up in the body in a toxic manner. It could also decrease kidney blood flow.
• Hepatic insufficiency. Along with the previous problem, ibuprofen is metabolized in the liver. In the event of liver failure, it could then accumulate in the body.
• Heart failure and uncontrolled hypertension.
• Pregnancy. The use of ibuprofen is contraindicated during the third trimester of pregnancy. In addition, its use is not recommended for prolonged periods during the first two trimesters.

Interactions

There are many drugs that can alter the behavior of ibuprofen and NSAIDs in the body. This may be a reduction in their effectiveness or an increase in the possibility of suffering from adverse reactions. Among these we find:

• AINEs. Ibuprofen may reduce the platelet anticoagulant function of acetylsalicylic acid when co-administered.
• Alcohol. Its toxicity may be increased. This is because both are metabolized in the liver and we overload it with work.

• Anti-hypertensive drugs. Possible reduction of the antihypertensive effect. When kidney function is compromised, the kidneys can deteriorate more quickly (dehydrated or elderly patients).
• Oral anticoagulants, heparin. Possible increase in the anticoagulant effect with risk of haemorrhage. Periodic consultations are recommended in order to monitor clotting indices.
• Antidiabetics. Possible increase in hypoglycemic effects by reducing renal excretion.
• Paracetamol. The simultaneous and prolonged use of paracetamol and AINE may cause an increased risk of adverse renal effects.

Ibuprofen Adverse Reactions

In the case of doses above 3,200 mg / day, problems and side effects may be noted:

1. Gastrointestinal. Possible onset of dyspepsia, diarrhea, nausea, abdominal pain or gastrointestinal bleeding due to suppression of gastro-protective prostaglandins.
2. Dermatological. Hypersensitivity reactions occur with rashes, hives or erythema. Anaphylactic reactions normally occur in patients who have previously suffered from hypersensitivity to acetyl salicylic acid and other NSAIDs.
3. Central nervous system : asthenia, drowsiness, headache, dizziness.
4. Hematologic. May prolong the bleeding time.
5. Cardiovascular. May develop high blood pressure or heart failure.
6. Renal.