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1.
Antimicrob Agents Chemother ; 34(5): 931-3, 1990 May.
Article in English | MEDLINE | ID: mdl-2360833

ABSTRACT

The effect of sucralfate on the bioavailability of ciprofloxacin was evaluated in eight healthy subjects utilizing a randomized, crossover design. The area under the concentration-time curve from 0 to 12 h was reduced from 8.8 to 1.1 micrograms.h/ml by sucralfate (P less than 0.005). Similarly, the maximum concentration of ciprofloxacin in serum was reduced from 2.0 to 0.2 micrograms/ml (P less than 0.005). We conclude that concurrent ingestion of sucralfate significantly reduces the concentrations in serum produced by a 500-mg dose of ciprofloxacin. On the basis of these findings, ciprofloxacin and sucralfate should not be administered concurrently.


Subject(s)
Ciprofloxacin/blood , Sucralfate/pharmacology , Adult , Biological Availability , Depression, Chemical , Drug Interactions , Female , Humans , Male , Random Allocation
2.
J Med Chem ; 27(5): 654-9, 1984 May.
Article in English | MEDLINE | ID: mdl-6325692

ABSTRACT

A series of phosphorus compounds, designed as analogues of gamma-aminobutyric acid (GABA) in that they possess a P = O moiety separated by three atoms from an amino or acetamido group, was synthesized and tested by using in vitro GABAA and GABAB receptor binding, GABA uptake assays, and was examined for anticonvulsant activity. Weak GABAB receptor affinity was noted for one agent, whereas six compounds displayed moderate to high potencies as inhibitors of electroshock- and pentylenetetrazol-induced seizures. The best anticonvulsant effect was found with the (m-aminophenyl) phosphinic acid compounds, with members of this class selected for further study.


Subject(s)
Anticonvulsants/chemical synthesis , Organophosphorus Compounds/chemical synthesis , gamma-Aminobutyric Acid/analogs & derivatives , Animals , Biological Assay , Brain/metabolism , Indicators and Reagents , Magnetic Resonance Spectroscopy , Mice , Organophosphorus Compounds/pharmacology , Organophosphorus Compounds/therapeutic use , Rats , Receptors, Cell Surface/drug effects , Receptors, Cell Surface/metabolism , Receptors, GABA-A , Seizures/drug therapy , Spectrophotometry, Infrared , Structure-Activity Relationship , Synaptosomes/drug effects , Synaptosomes/metabolism , gamma-Aminobutyric Acid/chemical synthesis , gamma-Aminobutyric Acid/metabolism , gamma-Aminobutyric Acid/pharmacology , gamma-Aminobutyric Acid/therapeutic use
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