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  • 1
    ISSN: 1432-1041
    Keywords: Pivampicillin ; ampicillin ; probenecid ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty male volunteers received oral doses (2100, 1050, and 525 mg) of a pivampicillin-probenecid salt in a 1 to 1 molar ratio (MK-356) at 12 hour intervals. After each dose peak serum concentrations of probenecid were observed 2 hours later than peak concentrations of ampicillin. Following the first dose of MK-356 the apparent elimination rate of ampicillin was dose-dependent and did not follow first order kinetics, as it showed a longer apparent half life after a higher dose. An equal dose of MK-356 administered 12 hours later caused an increase in the peak serum ampicillin level greater than expected from the concentration of ampicillin after the preceding dose. In twelve male volunteers who received at random 525 mg of MK-356 or 350 mg of pivampicillin, each three times daily for 4 days, the areas under the ampicillin concentration curve were the same after the first or last dose of either drug. When 2100 or 1050 mg of MK-356 was taken as an initial dose, 30 to 40 per cent of the ampicillin was recovered from urine in the ensuing 12 hours. The results indicate that when at least 400 mg probenecid was coadministered twice daily with 700 mg pivampicillin (MK-356), the peak serum concentrations of ampicillin were increased and its elimination rate slowed following successive doses.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-0738
    Keywords: Key words Permethrin ; 3-Phenoxybenzyl alcohol ; Skin ; Rabbit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Isolated rabbit ears were single-pass perfused with a protein-free medium. Permethrin (0.05–23.5%, w/w) was applied in four distinct ointments. Permethrin, 3-phenoxybenzyl alcohol, 3-phenoxybenzaldehyde, and 3-phenoxybenzoic acid were analysed by HPLC. Permethrin was not detected in the effluent. The permeation coefficient, calculated from the detection limit was 〈7.3 × 10−12 (cm/sec). The appearance rate of the 3-phenoxybenzyl moieties in the effluent agreed with the absorption of the corresponding impurities in the various ointments. In supernatant of homogenised skin, the hydrolysis rate of permethrin was linear; about 4 pmol/min per cm² at 10 μM substrate concentration. The proportion of 3-phenoxybenzoic acid, a further metabolite of 3-phenoxybenzyl alcohol increased when an oxidizing co-factor system was added. The appearance rate in the effusate of 3-phenoxybenzyl alcohol following the lipophobic ointment was five times faster than from isopropyl myristate. The formation rate of 3-phenoxybenzoic acid followed saturation kinetics. Occupational systemic poisoning by dermal absorption of permethrin seems very unlikely since humans bear more epithelial cell layers than rabbits. These experiments do not contradict, however, possible paraesthesia during systemic poisoning after inhalation or ingestion of the pyrethroid- containing aerosols used in agriculture.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 3 (1971), S. 113-118 
    ISSN: 1432-1041
    Keywords: Enzyme-induction ; man ; phenacetin ; phenazone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After the oral administration to volunteers of phenacetin (15 mg/kg) the highest concentration in blood was reached 2 h later. The decline appeared to follow first order kinetics with an apparent biological half-life (t′/2) of 0.8 h. The highest concentration in blood of the unconjugated metabolite, paracetamol, was twice that of phenacetin. About 70 per cent of a dose of phenacetin was excreted as conjugated paracetamol in the urine, and 70 per cent of this compound was eliminated during the first 12 h period. — After daily administration of 1.4, 2.5 and 3.6 mg/kg of Phenobarbital, each dose sequentially for 1 week, the apparent biological half-life of phenacetin and the elimination rates of its metabolites, unconjugated and conjugated paracetamol, remained unchanged. The elimination rate of phenazone (16 mg/kg) was increased by 40 per cent in the same subjects after treatment with phenobarbital. — The blood concentration of phenacetin varied more than 20 times between individuals, although no individual variation was found for the blood levels of unconjugated paracetamol.
    Type of Medium: Electronic Resource
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