      Document 0178
 DOCN  DRG0178
 UNIQUE IDENTIFIER        DRG-0069
 NAME OF SUBSTANCE        Ibuprofen [USAN 1996]
 REGISTRY NUMBER          15687-27-1
 STANDARD CHEMICAL NAME   Alpha-Methyl-4-(2-methylpropyl)benzeneacetic
                          acid [Merck Index 1989]
 SYNONYMS                 Advil [USAN 1996]
 SYNONYMS                 Haltran [USAN 1996]
 SYNONYMS                 Medipren [USAN 1996]
 SYNONYMS                 Midol 200 [USAN 1996]
 SYNONYMS                 Motrin [USAN 1996]
 SYNONYMS                 Nuprin [USAN 1996]
 SYNONYMS                 Trendar [USAN 1996]
 SYNONYMS                 Cap-Profen [USP DI 1989]
 SYNONYMS                 Ibuprin [USP DI 1995]
 SYNONYMS                 Ifen [USP DI 1989]
 SYNONYMS                 Rufen [USP DI 1995]
 SYNONYMS                 Tab-Profen [USP DI 1989]
 SYNONYMS                 Amersol [USP DI 1989]
 SYNONYMS                 Apo-Ibuprofen [USP DI 1995]
 SYNONYMS                 Novo-Profen [USP DI 1995]
 SYNONYMS                 Apsifen [USP DI 1989]
 SYNONYMS                 Apsifen-F [USP DI 1989]
 SYNONYMS                 Lidifen [USP DI 1989]
 SYNONYMS                 Paxofen [USP DI 1989]
 SYNONYMS                 2-(4-Isobutylphenyl)propionic acid [Merck
                          Index 1989]
 SYNONYMS                 Adran [Merck Index 1989]
 SYNONYMS                 Anflagen [Merck Index 1989]
 SYNONYMS                 Artril 300 [Merck Index 1989]
 SYNONYMS                 Bluton [Merck Index 1989]
 SYNONYMS                 Brufanic [Merck Index 1989]
 SYNONYMS                 Brufen [Merck Index 1989]
 SYNONYMS                 Buburone [Merck Index 1989]
 SYNONYMS                 Butylenin [Merck Index 1989]
 SYNONYMS                 Dolgit [Merck Index 1989]
 SYNONYMS                 Emodin [Merck Index 1989]
 SYNONYMS                 Epobron [Merck Index 1989]
 SYNONYMS                 Ibuprocin [Merck Index 1989]
 SYNONYMS                 Lamidon [Merck Index 1989]
 SYNONYMS                 Liptan [Merck Index 1989]
 SYNONYMS                 Mynosedin [Merck Index 1989]
 SYNONYMS                 Napacetin [Merck Index 1989]
 SYNONYMS                 Nobfelon [Merck Index 1989]
 SYNONYMS                 Nobfen [Merck Index 1989]
 SYNONYMS                 Nobgen [Merck Index 1989]
 SYNONYMS                 Rebugen [Merck Index 1989]
 SYNONYMS                 Roidenin [Merck Index 1989]
 SYNONYMS                 p-Isobutylhydratropic acid [Merck Index 1989]
 SYNONYMS                 Pedia-Profen [USAN 1996]
 SYNONYMS                 Anco [Merck Index 1989]
 SYNONYMS                 Amibufen [Merck Index 1989]
 SYNONYMS                 Brufort [Merck Index 1989]
 SYNONYMS                 Dolgirid [Merck Index 1989]
 SYNONYMS                 Dolocyl [Merck Index 1989]
 SYNONYMS                 Dolo-Dolgit [Merck Index 1989]
 SYNONYMS                 Ebufac [Merck Index 1989]
 SYNONYMS                 Femadon [Merck Index 1989]
 SYNONYMS                 Ibu-Attritin [Merck Index 1989]
 SYNONYMS                 Ibumetin [Merck Index 1989]
 SYNONYMS                 Ibu-slo [Merck Index 1989]
 SYNONYMS                 Ibutid [Merck Index 1989]
 PROTOCOL ID NUMBERS      FDA 044A
 SECONDARY SOURCE ID      U-18,573 [USAN 1996]
 SECONDARY SOURCE ID      RD 13621 [Merck Index 1989]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Nonsteroidal
                          anti-inflammatory analgesics (NSAIAs) such as
                          ibuprofen inhibit the activity of the enzyme
                          cyclo-oxygenase, resulting in decreased
                          formation of precursors of prostaglandins and
                          thromboxanes from arachidonic acid. While the
                          resultant decrease in prostaglandin
                          synthesis/activity in various tissues may
                          cause many of the therapeutic (and adverse)
                          effects of NSAIAs, other actions may also
                          contribute significantly to the therapeutic
                          effects of these medications. These actions
                          include: antirheumatic; analgesic;
                          anti-inflammatory; antipyretic;
                          antidysmenorrheal; and vascular headache
                          prophylaxis. NSAIAs also reversibly inhibit
                          platelet aggregation with possible recovery
                          of platelet function within 1 day after drug
                          discontinuation. Onset of action using
                          ibuprofen for treatment of pain is 0.5 hours,
                          with duration of action being 4-6 hours. The
                          absorption rate of oral ibuprofen is rapid,
                          with 99% bound to protein, and a time to peak
                          plasma concentration of 1.2-2.1 hours; its
                          peak plasma concentration varies with dose
                          level, ranging from 22-27 mcg/ml for 200 mg
                          to 56-66 mcg/ml for 800 mg. Ibuprofen
                          undergoes biotransformation in the liver, is
                          completely eliminated via renal excretion in
                          24 hours (less than 1% remaining as the
                          intact drug), and has an elimination
                          half-life of 1.8-2 hours. [USP DI 1995]
 DISEASES STUDIED/TREATED Inflammation and pain [Int Conf AIDS 1992 Jul
                          19-24;8(3): (abstract no PuB 7304)]
 CLASSIFICATION CODE      Nonsteroidal anti-inflammatory [USP DI 1995]
 OTHER MAJOR USES         Treatment of rheumatoid arthritis;
                          osteoarthritis; mild to moderate pain;
                          dysmenorrhea; nonrheumatic inflammation;
                          acute headache; and reduction of fever [PDR
                          1995]
 SUBSTANCE INTERACTIONS   May interact with acetaminophen,
                          adrenocorticoids, glucocorticoids, alcohol,
                          potassium supplements, chronic therapeutic
                          use of corticotropin, aminoglycosides,
                          digitalis glycosides, and serum digoxin,
                          anticoagulants and thrombolytics, oral
                          antidiabetic agents, insulin,
                          antihypertensives and diuretics (especially
                          triamterene), aspirin, cefamandole,
                          cefoperazone, cefotetan, moxalactam,
                          plicamycin, cohchicine, gold compounds,
                          lithium, methotrexate, nephrotoxic
                          medications, nifedipine, verapamil,
                          photosensitizing medications, other platelet
                          aggregation inhibitors, and probenecid. [USP
                          DI 1995]
 ADVERSE EFFECTS          Gastrointestinal side effects have been
                          reported in 4 to 16% of patients. Nausea,
                          epigastric pain and heartburn occurred in 3
                          to 9% of patients. The incidence of the
                          following adverse effects was greater than 1%
                          but less than 3%: abdominal distress, nausea
                          and vomiting, indigestion, constipation,
                          abdominal cramps or pain, bloating and
                          flatulence have occurred. Hematological,
                          cardiovascular and renal adverse events
                          occurred in less than 1% of patients. [PDR
                          1995]
 CONTRAINDICATIONS        Contraindicated in patients having a history
                          of sensitivity to ibuprofen or other NSAIA's.
                          Risk-benefit should be considered for
                          patients having the following medical
                          problems: anemia, asthma, compromised cardiac
                          function, hypertension, congestive heart
                          failure, diabetes, pre-existing edema,
                          extracellular volume depletion, sepsis,
                          hemophilia or other bleeding problems
                          (coagulation, platelet dysfunction), hepatic
                          dysfunction, peptic ulcer, ulcerative
                          colitis, upper gastrointestinal tract
                          disease, renal impairment, stomatitis,
                          adverse symptoms produced by aspirin or other
                          NSAIAs, or systemic lupus erythematosus. [USP
                          DI 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Arylpropionic acid
                          derivative [USP DI 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C13H18O2 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 206.28 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 75-77 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Practically insoluble in water;
                          very soluble in alcohol and most organic
                          solvents [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White to off-white
                          crystalline powder, having a slight,
                          characteristic odor [AHFS Drug Information
                          1995]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C75.69%, H8.80%,
                          O15.51% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pKa 4.43 [USP DI 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Tablets, 200, 300, 400, 600 and
                          800 mg; pediatric suspension, 100 mg/5ml.
                          [USP DI 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [PDR 1993]
 SUBSTANCE DELIVERY DATA  STORAGE: Store between 15-30 C (59-86 F);
                          store suspension in a well-closed container.
                          [PDR 1995]
 MANUFACTURERS            Whitehall Laboratories
 MANUFACTURERS            Upjohn
 REFERENCES               Lesko SM, Mitchell AA. An assessment of the
                          safety of pediatric ibuprofen. A
                          practitioner-based randomized clinical trial.
                          JAMA. 1995 Mar 22-29;273(12):929-33.
 REFERENCES               Schachtel BP, Cleves GS, Konerman JP, Brown
                          AT, Markham AO. A placebo-controlled model to
                          assay the onset of action of
                          nonprescription-strength analgesic drugs.
                          Clin Pharmacol Ther. 1994 Apr;55(4):464-70.
 REFERENCES               Nephrotoxicity of non-steroidal
                          anti-inflammatory drugs [clinical
                          conference]. Lancet. 1994 Aug
                          20;344(8921):515-8.
 REFERENCES               Chetty KG, Ramirez MM, Mahutte CK.
                          Drug-induced pulmonary edema in a patient
                          infected with human immunodeficiency virus.
                          Chest. 1993 Sep;104(3):967-9.
 REFERENCES               Cooper SA, Quinn PD, MacAfee K, Hersh EV,
                          Sullivan D, Lamp C. Ibuprofen
                          controlled-release formulation. A clinical
                          trial in dental impaction pain. Oral Surg
                          Oral Med Oral Pathol. 1993 Jun;75(6):677-83.
 REFERENCES               Lefkowitz M, Lebovits A, Smith G, Maignan M.
                          The prevalence and management of pain in
                          patients with AIDS: a second look three years
                          later. Int Conf AIDS. 1992 Jul 19-24;8(3):99
                          (abstract no. PuB 7304).
 REFERENCES               Perlman DM. Ibuprofen-induced aseptic
                          meningitis in individuals with HIV. Int Conf
                          AIDS. 1992 Jul 19-24;8(3):119 (abstract no.
                          PuB 7425).
 REFERENCES               Ragni MV, Miller BJ, Whalen R, Ptachcinski R.
                          Bleeding tendency, platelet function, and
                          pharmacokinetics of ibuprofen and zidovudine
                          in HIV(+) hemophilic men. Am J Hematol. 1992
                          Jul;40(3):176-82.
 REFERENCES               Walson PD, Galletta G, Chomilo F, Braden NJ,
                          Sawyer LA, Scheinbaum ML. Comparison of
                          multidose ibuprofen and acetaminophen therapy
                          in febrile children. Am J Dis Child. 1992
                          May;146(5):626-32.
 REFERENCES               Lim L, Fogelman I, Fischl M, Cotton D. The
                          effect of aspirin and other NSAIDS on
                          hematologic toxicity in early ARC individuals
                          treated with zidovudine. Int Conf AIDS. 1991
                          Jun 16-21;7(1):264 (abstract no. M.B.2329).
 ENTRY MONTH              9003
 LAST REVISION DATE       951201
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
