      Document 0090
 DOCN  DRG0090
 UNIQUE IDENTIFIER        DRG-0157
 NAME OF SUBSTANCE        Cefuroxime Axetil [USAN 1996]
 REGISTRY NUMBER          64544-07-6
 STANDARD CHEMICAL NAME   5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxy-
                          lic acid,
                          3-(((aminocarbonyl)oxy)methyl)-7-((2-furanyl(-
                          methoxyimino)  acetyl)-amino)-8-oxo-,
                          1-(acetyloxy)ethyl ester,
                          (6R-(6alpha,7beta(Z)))- [USAN 1996]
 SYNONYMS                 Ceftin [USAN 1996]
 SYNONYMS                 Cefuroxime 1-acetoxyethyl ester [MeSH]
 SYNONYMS                 Axoril [Merck Index 1989]
 SYNONYMS                 Cepazine [Merck Index 1989]
 SYNONYMS                 Ximos [Merck Index 1989]
 SYNONYMS                 Zinnat [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID ACTG 186
 SECONDARY SOURCE ID      CCI 15641 [CHEMLINE]
 SECONDARY SOURCE ID      CCI-15641 [MeSH]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: The bactericidal action of
                          cefuroxime results from inhibition of cell
                          wall synthesis by binding to essential target
                          proteins. Cefuroxime axetil is absorbed from
                          the gastrointestinal tract and hydrolyzed
                          within the intestinal mucosa and blood to
                          release cefuroxime. It is distributed in the
                          extracellular fluid compartment. The axetil
                          moiety is metabolized to acetaldehyde and
                          acetic acid. The drug is excreted unchanged
                          in the urine. It is approximately 50% protein
                          bound: the half-life is 1.2 hours. Absorption
                          is greater when taken after food. The drug
                          has broad spectrum antibacterial activity and
                          is highly stable to bacterial
                          beta-lactamases, especially those found in
                          the Enterobacteriaceae. It is active against
                          gram positive and gram negative cocci, gram
                          negative bacilli, and anaerobes. [PDR 1995]
                          [NIAID ACTG 186]
 DISEASES STUDIED/TREATED Prevention of recurrent HIV-associated
                          sinusitis. [NIAID ACTG 186]
 CLASSIFICATION CODE      Antibiotic [PDR 1995]
 OTHER MAJOR USES         Treatment of pharyngitis and tonsillitis,
                          otitis media, lower respiratory tract
                          infections, urinary tract and gonorrhea
                          infections, and skin infections. [PDR 1995}
 SUBSTANCE INTERACTIONS   Probenecid increases cefuroxime blood levels;
                          drugs lower in gastric acidity may decrease
                          cefuroxime bioavailability. [PDR 1995]
 ADVERSE EFFECTS          Adverse effects include anaphylaxis, nausea,
                          vomiting, diarrhea, loose stools, rash,
                          pruritus, urticaria, headaches, dizziness,
                          vaginitis, transient elevations of
                          transaminases and LDH, eosinophilia, positive
                          Coomb's test, and seizures. [PDR 1995] [NIAID
                          ACTG 186]
 CONTRAINDICATIONS        Contraindicated in patients with known
                          allergy to the cephalosporin group of
                          antibiotics. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Semi-synthetic, broad
                          spectrum cephalosporin antibiotic;
                          acetoxyethylester of cefuroxime; beta lactam
                          class antibiotic [PDR 1995] [NIAID ACTG 186]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C20H22N4O10S [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 510.48 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   STABILITY: Reconstituted oral suspension is
                          stable for 10 days [PDR 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White to cream colored
                          amorphous powder. [AHFS Drug Information
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 125, 250, and 500 mg tablets,
                          oral suspension 125 mg/5 ml. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE INSTRUCTIONS: Store between 15-30 C
                          (59-86 F). Protect from excessive moisture.
                          Store reconstituted suspension between 2-25
                          C. [PDR 1995]
 MANUFACTURERS            Glaxo Wellcome
 REFERENCES               Burack JH, Hahn JA, Saint-Maurice D, Jacobson
                          MA. Microbiology of community-acquired
                          bacterial pneumonia in persons with and at
                          risk for human immunodeficiency virus type 1
                          infection. Implications for rational empiric
                          antibiotic therapy. Arch Intern Med. 1994 Nov
                          28;154(22):2589-96.
 REFERENCES               Goddard JK, Janning SW, Gass JS, Wilson RF.
                          Cefuroxime-induced acute renal failure.
                          Pharmacotherapy; VOL 14, ISS 4, 1994,
                          P488-91.
 REFERENCES               Olmo A, Sabater F, Broto J, Traserra J.
                          [Amoxycillin-clavulanic acid and cefuroxime
                          axetil in the treatment of acute sinusitis. A
                          clinical, radiological and bacteriological
                          evaluation.] Acta Otorrinolaringol Esp 1994
                          Jan-Feb;45(1):25-9.
 REFERENCES               Lopez J, Rosello X, Jane E. Stomatitis
                          aphthous in patients HIV+, treatment. Int
                          Conf AIDS. 1994 Aug 7-12;10(1):183 (abstract
                          no. PBO159)
 REFERENCES               Mevorach D, Lossos IS, Oren R.
                          Cefuroxime-induced fever. Ann Pharmacother;
                          VOL 27, ISS 7-8, 1993, P881-2.
 REFERENCES               Bygdeman SM, Ruden AK, Jonsson A, Lidbrink P,
                          Olofsson MB, Backman M, Gastrin B, Kallings
                          I, Ramberg M, Rylander M, et al. Antibiotic
                          susceptibility, serovars and auxotypes of
                          gonococcal isolates in Stockholm. Relation to
                          geographical origin of the infection. Int J
                          STD AIDS. 1993 Jan-Feb;4(1):33-40.
 REFERENCES               Camacho, AE, Cobo R, Otte J, Spector SL,
                          Lerner CJ, Garrison NA, Miniti A, Mydlow PK,
                          Giguere GC, Collins JJ. Clinical comparison
                          of cefuroxime axetil and
                          amoxicillin/clavulanate in the treatment of
                          patients with acute bacterial maxillary
                          sinusitis. Am J Med. 1992 Sep;93(3): 271-6.
 REFERENCES               Idemyor V, Cherubin CE. Pleurocerebral
                          Nocardia in a patient with human
                          immunodeficiency virus. Ann Pharmacother.
                          1992 Feb;26(2):188-9.
 REFERENCES               Telzak EE, Hii J, Polsky B, Kiehn TE,
                          Armstrong D. Nocardia infection in the
                          acquired immunodeficiency syndrome. Diagn
                          Microbiol Infect Dis. 1989
                          Nov-Dec;12(6):517-9.
 ENTRY MONTH              9212
 LAST REVISION DATE       960614
 

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