Apsifen - General Information
A nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis.
Pharmacology of Apsifen
Apsifen is a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Apsifen has pharmacologic actions similar to those of other prototypical NSAIAs, that is thought to be associated with the inhibition of prostaglandin synthesis. Apsifen is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and to alleviate moderate pain.
Apsifen for patients
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve pain and inflammation, reduce fever, and treat osteoarthritis, rheumatoid arthritis, and menstrual cramps. Inform your physician if you are pregnant or nursing. Ibuprofen should not be taken during the last three months of pregnancy. Inform your physician if you use alcohol chronically. Ibuprofen should not be taken with aspirin products. This medication should be taken with food, milk or antacids if stomach upset occurs. Ibuprofen may cause dizziness and drowsiness; use caution while driving or operating hazardous machinery. Ibuprofen may cause increased sensitivity to sunlight. Use sunscreens and wear protective clothing until degree of sensitivity is determined. Notify your physician if you develop stomach pain, bloody vomit, bloody or black tarry stools, cloudy urine, trouble breathing, rash or hives.
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).
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.
Additional information about Apsifen
Apsifen Indication: For the treatment of pain (muscular and rheumatic), sprains, strains, backache and neuralgia
Mechanism Of Action: The exact mechanisms of action of Apsifen 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.
Drug Interactions: Acebutolol Risk of inhibition of renal prostaglandins
Atenolol Risk of inhibition of renal prostaglandins
Betaxolol Risk of inhibition of renal prostaglandins
Bevantolol Risk of inhibition of renal prostaglandins
Bisoprolol Risk of inhibition of renal prostaglandins
Carteolol Risk of inhibition of renal prostaglandins
Carvedilol Risk of inhibition of renal prostaglandins
Esmolol Risk of inhibition of renal prostaglandins
Labetalol Risk of inhibition of renal prostaglandins
Nadolol Risk of inhibition of renal prostaglandins
Metoprolol Risk of inhibition of renal prostaglandins
Oxprenolol Risk of inhibition of renal prostaglandins
Penbutolol Risk of inhibition of renal prostaglandins
Pindolol Risk of inhibition of renal prostaglandins
Practolol Risk of inhibition of renal prostaglandins
Propranolol Risk of inhibition of renal prostaglandins
Sotalol Risk of inhibition of renal prostaglandins
Timolol Risk of inhibition of renal prostaglandins
Warfarin The NSAID increases the anticoagulant effect
Acenocoumarol The NSAID increases the anticoagulant effect
Dicumarol The NSAID increases the anticoagulant effect
Anisindione The NSAID increases the anticoagulant effect
Ethacrynic acid The NSAID decreases the diuretic and antihypertensive effect of the loop diuretic
Furosemide The NSAID decreases the diuretic and antihypertensive effect of the loop diuretic
Torasemide The NSAID decreases the diuretic and antihypertensive effect of the loop diuretic
Bumetanide The NSAID decreases the diuretic and antihypertensive effect of the loop diuretic
Aspirin Apsifen reduces ASA cardioprotective effects
Methotrexate The NSAID increases the effect and toxicity of methotrexate
Alendronate Increased risk of gastric toxicity
Cyclosporine Monitor for nephrotoxicity
Lithium The NSAID increases serum levels of lithium
Food Interactions: Avoid alcohol.
Take with food to reduce irritation.
Generic Name: Ibuprofen
Synonyms: P-Isobutylhydratropic Acid; Para-Isobutylhydratropic Acid; Ibuprophen
Drug Category: Analgesics; Cyclooxygenase Inhibitors; Anti-inflammatory Agents; Nonsteroidal Antiinflammatory Agents (NSAIDs)
Drug Type: Small Molecule; Approved
Other Brand Names containing Ibuprofen: 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; Dolgin; Dolgirid; Dolgit; Dolo-Dolgit; Dolocyl; 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; Nobfelon; Nobfen; Nobgen; Novogent N; Novoprofen; Nuprin; Nurofen; Pantrop; Paxofen; Pedia-Profen; Pediaprofen; Pediatric Advil; Profen; Rafen; Rebugen; Roidenin; Rufen; Seclodin; Suspren; Tab-Profen; Tabalon; Trendar; Urem;
Absorption: rapidly absorbed
Toxicity (Overdose): 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)
Protein Binding: 99%
Half Life: 1.8-2.0 hours
Dosage Forms of Apsifen: Tablet Oral
Tablet, chewable Oral
Chemical IUPAC Name: 2-[4-(2-methylpropyl)phenyl]propanoic acid
Chemical Formula: C13H18O2
Ibuprofen on Wikipedia: http://en.wikipedia.org/wiki/Ibuprofen
Organisms Affected: Humans and other mammals