Ibuprofen (Dosage)

Ibuprofen is a non-steroidal anti-inflammatory drug used as an antipyretic, analgesic and anti-inflammatory, and can be very effective in the treatment of headaches and migraines. Certain variations in genes involved in the metabolism of this drug may condition its efficacy in the treatment of headaches or migraines.

Ibuprofen is a non-steroidal anti-inflammatory drug, also known as an NSAID, used to treat pain, inflammation and fever. It is available as an over-the-counter medication and is also used as an anti-inflammatory medication for the treatment of chronic inflammatory diseases such as rheumatoid arthritis, juvenile idiopathic arthritis and ankylosing spondylitis.

For individuals with severe headaches 400 mg doses are usually much more effective than 200 mg doses.

There are many individuals for whom ibuprofen does not provide relief, and this may or may not be due to the presence of certain genetic variants in ibuprofen metabolization and response genes or to other factors (e.g., severity of migraine or etiology of severe headache).

MECHANISM OF ACTION

The mechanism of action of ibuprofen is based on the inhibition of the enzyme cyclooxygenase (COX).

Cyclooxygenase is an enzyme that plays an important role in the inflammation process. This enzyme is present in two forms: cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). COX-1 helps maintain normal tissue function in the body and is responsible for the production of chemicals that promote inflammation in response to injury. COX-2 is an inducible isoform and is activated in response to inflammatory factors such as trauma, injury and infection. This enzyme is responsible for the production of prostaglandins, which contribute to pain and inflammation.

Ibuprofen blocks COX-2 activity, which reduces the production of prostaglandins and thus reduces pain and inflammation. This makes ibuprofen a very useful drug for the treatment of chronic inflammatory diseases such as arthritis. In addition, ibuprofen can also inhibit COX-1 at high doses, which can have side effects such as stomach ulcers.

CONTRAINDICATIONS AND SIDE EFFECTS

Although ibuprofen is generally considered safe, there are certain contraindications to consider before using it.

The main contraindications of ibuprofen include:

Allergy: Allergy to ibuprofen is considered a contraindication. Symptoms of an allergic reaction to ibuprofen may include rash, hives, rhinitis, sneezing, difficulty breathing, vomiting and diarrhea. If you experience any of these symptoms, you should stop using ibuprofen immediately and seek medical attention.

Stomach ulcers and bleeding: Ibuprofen may increase the risk of stomach ulcers and bleeding. Therefore, the use of ibuprofen is not recommended for people who have ulcers or who are at risk of developing ulcers or stomach bleeding.

Cardiovascular disease: Ibuprofen may increase the risk of cardiovascular disease, such as heart attacks and strokes. Therefore, the use of ibuprofen is not recommended for people who have a history of cardiovascular disease.

Pregnancy: It has been shown that ibuprofen may cause problems in the development of the fetus. Therefore, it is recommended to avoid the use of ibuprofen during pregnancy, especially during the first trimester.

Kidney disease: Ibuprofen may increase the risk of kidney damage in people with kidney disease. Therefore, the use of ibuprofen is not recommended for people with kidney disease.

Liver disease: Ibuprofen may increase the risk of liver damage in people with liver disease. Therefore, the use of ibuprofen is not recommended for people with liver disease.

Ibuprofen may also have other side effects such as peptic ulcer, gastrointestinal perforation and bleeding, nausea, vomiting, diarrhea, flatulence, constipation, dyspepsia, abdominal pain, melena, hematemesis, ulcerative stomatitis, exacerbation of ulcerative colitis and Crohn's disease; fatigue or drowsiness, headache, dizziness; vertigo; skin rash; pain and burning sensation at the injection site (if administered intravenously).

PHARMACOLOGICAL INTERACTIONS

Increased risk of gastrointestinal ulcer and bleeding if ibuprofen is taken together with: other NSAIDs, oral anticoagulants of the dicoumarin type, antiplatelet agents of the acetylsalicylic acid type, oral corticosteroids and SSRI antidepressants.

Ibuprofen reduces the efficacy of: furosemide and thiazide diuretics.

Ibuprofen reduces the hypotensive effect of: ß-blockers, ACE inhibitors, angiotensin II antagonists.

Increases plasma levels of: digoxin, phenytoin and lithium.

Increases toxicity of: methotrexate, hydantoins, sulfonamides and baclofen.

Ibuprofen may potentiate gastrointestinal lesions if taken concomitantly with: salicylates, phenylbutazone, indomethacin and other NSAIDs.

It increases the effect of: oral hypoglycemic agents and insulin.

Ibuprofen causes an additive effect on platelet inhibition with ticlopidine.

It potentiates the bleeding time of anticoagulants.

Increases the risk of nephrotoxicity with: tacrolimus and cyclosporine.

Ibuprofen increases the risk of gastrointestinal bleeding and ulcer with: corticosteroids, bisphosphonates or oxypentifylline, selective cyclooxygenase-2 inhibitors.

May produce risk of hemorrhage if taken with: ginkgo biloba, thrombolytic agents.

Potentiates the nephrotoxic effect of aminoglycosides.

BRAND NAMES

  • Advil®
  • Nurofen®
  • Motrin® Motrin® Motrin® Motrin® Motrin® Motrin® Motrin

Genes analyzed

CYP2C9

Bibliography

Ochoa D, Prieto-Pérez R, Román M, et al.Effect of gender and CYP2C9 and CYP2C8 polymorphisms on the pharmacokinetics of ibuprofen enantiomers. Pharmacogenomics. 2015;16(9):939-48.

Theken KN, Lee CR, Gong L, et al.Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2C9 and Nonsteroidal Anti-Inflammatory Drugs. Clin Pharmacol Ther. 2020 Aug;108(2):191-200.

Zobdeh F, Eremenko II, Akan MA, et al . Pharmacogenetics and Pain Treatment with a Focus on Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Antidepressants: A Systematic Review. Pharmaceutics. 2022 Jun 1;14(6):1190.

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