[Cefixime, the first oral third-generation cephalosporin]. 1989

G Roche
Pharmuka SF, Paris.

In the early 1980's parenteral third generation cephalosporins changed the hospital use of antibiotics. The MICs of these cephalosporins are several dozen times lower than those of first or second generation cephalosporins for Enterobacteriaceae and they are much more beta-lactamase stable than second generation cephalosporins. After years of research, is has finally been possible to develop orally active compounds possessing the same antibacterial activity as parenteral third generation cephalosporins, either through the use of prodrugs, or by modifying the molecular structure of drugs. Cefixime is an example of the latter. The vinyl group at the 3-position of the cephem nucleus is responsible for the intestinal absorption of the intact molecule, primarily by a carrier-mediated transport mechanism. The aminothiazole ring and the R-oxyimino group on the side-chain at the 7-position are associated with an antibacterial activity similar to that of third generation cephalosporins. Thousands of adults have been treated by cefixime for lower respiratory tract, ear-nose-throat and urinary tract infections, showing that cefixime is a safe and effective antimicrobial agent. The major clinical indications for cefixime in adults are bronchial and pulmonary infections, acute otitis or sinusitis, acute pyelonephritis with no underlying uropathy, and complicated or uncomplicated lower urinary tract infections excluding prostatitis. In all cases, the dosage is 200 mg b.i.d.

UI MeSH Term Description Entries
D011355 Prodrugs A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. Drug Precursor,Drug Precursors,Pro-Drug,Prodrug,Pro-Drugs,Precursor, Drug,Precursors, Drug,Pro Drug,Pro Drugs
D011897 Random Allocation A process involving chance used in therapeutic trials or other research endeavor for allocating experimental subjects, human or animal, between treatment and control groups, or among treatment groups. It may also apply to experiments on inanimate objects. Randomization,Allocation, Random
D002439 Cefotaxime Semisynthetic broad-spectrum cephalosporin. Benaxima,Biosint,Cefotaxim,Cefotaxime Sodium,Cefradil,Cephotaxim,Claforan,Fotexina,HR-756,Kendrick,Klaforan,Primafen,Ru-24756,Taporin,HR 756,HR756,Ru 24756,Ru24756,Sodium, Cefotaxime
D002511 Cephalosporins A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid. Antibiotics, Cephalosporin,Cephalosporanic Acid,Cephalosporin,Cephalosporin Antibiotic,Cephalosporanic Acids,Acid, Cephalosporanic,Acids, Cephalosporanic,Antibiotic, Cephalosporin,Cephalosporin Antibiotics
D002621 Chemistry A basic science concerned with the composition, structure, and properties of matter; and the reactions that occur between substances and the associated energy exchange.
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D004311 Double-Blind Method A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment. Double-Masked Study,Double-Blind Study,Double-Masked Method,Double Blind Method,Double Blind Study,Double Masked Method,Double Masked Study,Double-Blind Methods,Double-Blind Studies,Double-Masked Methods,Double-Masked Studies,Method, Double-Blind,Method, Double-Masked,Methods, Double-Blind,Methods, Double-Masked,Studies, Double-Blind,Studies, Double-Masked,Study, Double-Blind,Study, Double-Masked
D006090 Gram-Negative Bacteria Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method. Gram Negative Bacteria
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations

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