Ibuprofen (Efficacy)

Ibuprofen may be an effective treatment for some individuals with acute migraines in adults. However, there are many individuals for whom ibuprofen does not provide relief, and this may be due to the presence or not of certain genetic variants in ibuprofen metabolization and response genes or to other factors (such as migraine severity or etiology of severe headaches). These problems seen with ibuprofen in individuals suffering from migraines or very severe headaches are not seen for mild or moderate headaches (since the etiology of the neurological disorder is different). For individuals with severe headaches, doses of 400 mg are often much more effective than 200 mg.

ACTION MECHANISM

Ibuprofen works by inhibiting the synthesis of prostaglandins at the peripheral level (inhibiting the COX-2 or PTGS2 gene).

CONTRAINDICATIONS

- Hypersensitivity to ibuprofen or other NSAIDs

- History of bronchospasm, asthma, rhinitis, angioedema or urticaria associated with the consumption of acetylsalicylic acid or other NSAIDs.

- History of gastrointestinal bleeding or perforation related to previous NSAID treatments, active or recurrent peptic ulcer/gastrointestinal bleeding (2 or more different episodes of proven ulceration or bleeding), or history of peptic ulcer/recurrent bleeding.

- Active inflammatory bowel disease, severe kidney failure; severe liver failure, severe heart failure; bleeding diathesis or other bleeding disorders.

- Third trimester of pregnancy.

- Cerebrovascular hemorrhages or other active hemorrhages, coronary disorders; severe dehydration (caused by vomiting, diarrhea, or insufficient fluid intake).

- If administered intravenously, ibuprofen is contraindicated if there is perioperative pain due to coronary artery bypass graft adjustment surgery.

SIDE EFFECTS

An abuse of ibuprofen can cause the following adverse effects: 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; acne; pain and burning sensation at the injection site (if administered intravenously).

PHARMACOLOGIC INTERACTIONS

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

- Ibuprofen reduces the effectiveness of: furosemide and thiazide diuretics.

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

- Ibuprofen increases plasma levels of: digoxin, phenytoin and lithium.

- Ibuprofen increases the toxicity of: methotrexate, hydantoins, sulfa drugs and baclofen. -Ibuprofen can potentiate gastrointestinal injuries if taken concomitantly with: salicylates, phenylbutazone, indomethacin and other NSAIDs.

- Ibuprofen increases the effect of: oral hypoglycemic agents and insulin.

- Ibuprofen causes an additive effect on platelet inhibition with ticlopidine.

- Ibuprofen power the bleeding time of anticoagulants.

- Ibuprofen increases the risk of nephrotoxicity with: tacrolimus and cyclosporine.

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

- Ibuprofen may cause bleeding risk if taken together with: ginkgo biloba, thrombolytic agents.

- Ibuprofen potentiates the nephrotoxic effect of aminoglycosides.

BRAND NAMES

- Advil® (tablets)

- Advil® Migraine

- Advil® Liqui-Gels®

- Nurofen®

- Motrin® (tablets)

- Motrin® (drops)

- Motrin® Migraine

- Etc.

Genes analyzed

CYP2C8 CYP2C9 PTGS2

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