Active ingredient: Ibuprofen - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Analgesics
• Cyclooxygenase Inhibitors
• Anti-inflammatory Agents
• Nonsteroidal Antiinflammatory Agents (NSAIDs)

Dosage Forms

• Tablet
• Suspension

Brands / Synonyms

Actiprofen; Adran; Advil; Advil Liqui-Gels; Amersol; Amibufen; Anco; Andran; Anflagen; Apo-Ibuprofen; Apsifen; Apsifen-F; Artril 300; Bluton; Brufanic; Brufen; Brufort; Buburone; Butylenin; Cap-Profen; Children's Advil; Children's Elixsure; Children's Ibuprofen; Children's Motrin; Codral; Combunox; Dolgin; Dolgirid; Dolgit; Dolo-Dolgit; Dolocyl; Duexis; Ebufac; Emodin; Epobron; Femadon; Fenbid Spansule; Haltran; Ibu; Ibu-Attritin; Ibu-Slo; Ibu-Tab; Ibu-Tab 200; Ibufen; Ibumetin; Ibuprin; Ibuprocin; Ibuprohm; Ibutid; Ifen; Inabrin; Inoven; Junior Strength Advil; Junior Strength Ibuprofen; Junior Strength Motrin; Lamidon; Lebrufen; Lidifen; Liptan; Medipren; Midol; Midol 200; Motrin; Mynosedin; Napacetin; Neoprofen; Nobfelon; Nobfen; Nobgen; Novogent N; Novoprofen; Nuprin; Nurofen; P-Isobutylhydratropic Acid; Pantrop; Para-Isobutylhydratropic Acid; Paxofen; Pedia-Profen; Pediaprofen; Pediatric Advil; Profen; Rafen; Rebugen; Roidenin; Rufen; Seclodin; Suspren; Tab-Profen; Tabalon; Trendar; Urem ; Vicoprofen

Indications

For the treatment of pain (muscular and rheumatic), sprains, strains, backache and neuralgia

Pharmacology

Ibuprofen is a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Ibuprofen has pharmacologic actions similar to those of other prototypical NSAIAs, that is thought to be associated with the inhibition of prostaglandin synthesis. Ibuprofen is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and to alleviate moderate pain.

Mechanism of Action

The exact mechanisms of action of Ibuprofen is unknown. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis, and results in the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Absorption

rapidly absorbed

Toxicity

Abdominal pain, breathing difficulties, coma, drowsiness, headache, irregular heartbeat, kidney failure, low blood pressure, nausea, ringing in the ears, seizures, sluggishness, vomiting; LD₅₀=1255mg/kg(orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Ibuprofen tablets or ibuprofen children's suspension should not be used in patients who have previously exhibited hypersensitivity to the drug, or in individuals with the syndrome of nasal polyps, angioedema, and bronchospastic reactivity to aspirin or other nonsteroidal anti-inflammatory agents. Anaphylactoid reactions have occurred in such patients.

Drug Interactions

Coumarin-Type Anticoagulants: Several short-term controlled studies failed to wshow that ibuprofen significantly affected prothrombin times or a variety of other clotting factors when administered to individuals on coumarin-type anticoagulants. However, because bleeding has been reported when ibuprofen and other nonsteroidal anti-inflammatory agents have been administered to patients on coumarin-type anticoagulants, the physician should be cautious when administering ibuprofen to patients on anticoagulants.

Aspirin: Animal studies wshow that aspirin given with nonsteroidal anti-inflammatory agents, including ibuprofen, yields a net decrease in anti-inflammatory activity with lowered blood levels of the non-aspirin drug. Single dose bioavailability studies in normal volunteers have failed to wshow an effect of aspirin on ibuprofen blood levels. Correlative clinical studies have not been performed.

Methotrexate: Ibuprofen, as well as other nonsteroidal anti-inflammatory drugs, probably reduces the tubular secretion of methotrexate based on in vitro studies in rabbit kidney slices. This may indicate that ibuprofen could enhance the toxicity of methotrexate. Caution should be used if ibuprofen is administered concomitantly with methotrexate.

H-2 Antagonists: In studies with human volunteers, co-administration of cimetidine or ranitidine with ibuprofen had no substantive effect on ibuprofen serum concentrations.

Furosemide: Clinical studies, as well as random observations, have shown that ibuprofen can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with ibuprofen, the patient should be observed closely for signs of renal failure, as well as to assure diuretic efficacy.

Lithium: Ibuprofen produced an elevation of plasma lithium levels and a reduction in renal lithium clearance in a study of eleven normal volunteers. The mean minimum lithium concentration increased 15% and the renal clearance of lithium was decreased by 19% during this period of concomitant drug administration.

This effect has been attributed to inhibition of renal prostaglandin synthesis by ibuprofen. Thus, when ibuprofen and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity. (Read circulars for lithium preparation before use of such concurrent therapy).