[Densitometric determination of desacetylmetipranolol in blood plasma].
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Biomedical subjects
Publications and source records attributed to V Rejholec.
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The radioreceptor assay (RRA) was used to quantitate plasma triazolam concentrations in eight female volunteers following single 0.5 mg doses of two tablet formulations in a cross-over study. Bioavailability in terms of area under the plasma concentration versus time curve (AUC0 infinity), maximum plasma concentration (Cmax), time to maximum (tmax), and mean residence time (MRT) was not statistically significantly different from one formulation to the other.
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The randomized, double-blind trial was carried out with 50 patients suffering from ankylosing spondylarthritis and belonging all to type B27 in the HLA system. Tolfenamic acid (600 mg daily) was effective as judged by subjective and numerous objective parameters and was preferable to indomethacin (75 mg daily). Indomethacin caused side effects more frequently than tolfenamic acid. In the indomethacin group 16% of the patients interrupted the 6-month trial because of gastrointestinal complications. No discontinuation of treatment owing to adverse effects of tolfenamic acid occurred. Tolfenamic acid offers one new and good alternative for the medical treatment of ankylosing spondylarthritis.
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The protein binding of colchicine and its derivatives demecolcine and desacetylcolchiceine was studied by equilibrium dialysis at 22 degrees C and pH 7.38 in bovine and human serum albumin and human plasma. Colchicine and demecolcine (2 X 10(-4) -5 X 10(-4) mol/l) is not bound to proteins. The binding of desacetylcholchiceine was 60--80% in the range 10(-4)-5 X 10(-4) mol/l. The association constant for a single binding site was 8.03 X 10(3) 1/mol for human serum albumin and 13.20 X 10(3) 1/mol for human plasma. The binding profiles for desacetylcholchiceine were quite similar in human serum albumin (4% conc.) and human plasma (3.8% conc. of albumin fraction). We suggest that desacetylcolchiceine was likely to be bound predominantly to albumin. Salicylic acid in vitro, at clinical concentrations (1.8--14.5 X 10(-4) mol/l), significantly decreases the binding of desacetylcolchiceine to human serum albumin.
Sixty patients with diagnosed rheumatoid arthritis were treated at random with tolfenamic acid, a new nonsteroid anti-inflammatory analgesic, in a daily dose of 600 mg, or with phenylbutazone 300 mg or acetylsalicylic acid 1,500 mg daily. Both the patients and the physician found that tolfenamic acid had a clearly better effect than phenylbutazone or the low-dose acetylsalicylic acid used as a control. Tolfenamic acid and acetylsalicylic acid were well tolerated. Serious side-effects (leukopenia and thrombocytopenia in one case, hematemesis and melena in another) only occurred in those patients who received phenylbutazone.
In an open trial of three months' duration the clinical effect of tolfenamic acid, a new nonsteroid anti-inflammatory analgesic, was found to be good in 85 patients suffering from rheumatoid arthritis. Both subjective and objective parameters clearly improved, and corticoid therapy could be abandoned by 21% of the patients. Tolfenamic acid was for the most part better than or as good as, the previous medication by which the disease had been brought to a stabile state. Side-effects were mild, no severe adverse reactions were observed which could be definitely attributed to tolfenamic acid.