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Felbamate (2-phenyl-1,3-propanediol dicarbamate) is a novel agent effective against maximal electroshock, pentylenetetrazol and other chemically induced seizures in mice and rats. Felbamate has been proposed as a novel anticonvulsant for the treatment of generalized tonic-clonic and complex partial seizures. In addition, felbamate has been shown to have(More)
An isocratic liquid-chromatographic method employing one extraction step and a 4.6 mm x 150 mm Spherisorb ODS2, 3 microns high-performance liquid chromatography (HPLC) column using ultraviolet (UV)-absorbance detection at 210 nm has been developed for quantitation of felbamate (FBM) and three felbamate metabolites in 0.100-ml aliquots of human plasma. The(More)
Two major and one minor metabolite of felbamate (FBM) as well as unchanged drug were isolated and identified by electron impact and chemical ionization mass spectrometry from rat and dog urine after dosing with [14C]FBM. The metabolites were 2-(4-hydroxyphenyl)-1,3-propanediol dicarbamate (p-OHF), 2-hydroxy-2-phenyl-1,3-propanediol dicarbamate, and(More)
In a metabolism study, three male and three female pediatric dogs and three male and three female adult beagle dogs received a single oral dose of 60 mg/kg [14C]felbamate. Urine and feces were collected up to 72 hr. Excreta samples were extracted with ethyl acetate and 14C metabolite profiles were generated by HPLC analysis of the extracts. The total 14C(More)
Incubation of [14C]felbamate at 37 degrees C for 60 min with liver microsomes from untreated Sprague-Dawley rats converted 10% of the drug to the p-hydroxy (6%) and 2-hydroxy (4%) metabolites. With microsomes from phenobarbital-pretreated rats, 21% of the drug was metabolized to the p-hydroxy (7.5%) and 2-hydroxy (13.5%) metabolites. With microsomes from(More)
Rats, rabbits, and dogs were given single iv or single and multiple oral doses of felbamate ranging from 1.6-1000 mg/kg. Absorption of oral drug was complete in all species. The mean Cmax increased with dose from 13.9 to 185.9 micrograms/ml in rats, from 19.1 to 161.9 micrograms/ml in rabbits, and from 12.6 to 168.4 micrograms/ml in dogs. The tmax also(More)
The relative bioavailability and pharmacokinetics of felbamate (FBM) after a single oral dose and after 10 once-daily oral doses of 60 mg/kg were investigated in adult and pediatric dogs of both sexes. The pediatric and adult dogs were aged 4-6 weeks and 1-2 years, respectively. Analysis of variance (ANOVA) was performed on the bioavailability parameters(More)
The correlation between the antiasthma activity of azelastine and the concentrations of azelastine and its major metabolite, desmethylazelastine, in the blood and lung were investigated in guinea pigs. Blood and lung tissue samples collected at 15 min after aeroallergen (ovalbumin, 0.5 mg/ml, 30 s, 15 psi) challenge, i.e., 2-1/4 h after oral administration(More)
The stability and biotransformation of D-penicillamine as it relates to assay development is discussed. A review of published literature on assays is presented with respect to blood/plasma levels of D-penicillamine in man and to statistical evaluation of assays. Also, the paper describes gas chromatographic assay for D-penicillamine disulfide and L-cysteine(More)