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At least 163 records · Page 9Linked to original sources
PubMed1978

[Determination of azapropazone and 8-hydroxyazapropazone in urine by direct quantitative thin-layer chromatography (author's transl)].

A method for quantitative determination of 5-dimethyl amino-9-methyl-2-propyl-1H-pyrazolo[1,2-a] [1,2,4]benzotriazine-1,3-(2H)-dione (azapropazone) and 8-hydroxyazapropazone in urine has been described. The analysis is performed by quantitatively thin-layer chromatography. The method is selective with a standard deviation of about 5%. After daily oral administration of 3 x 300 mg azapropazone-dihydrate a mean excretion of azapropazone of 62% and a mean excretion of 8-hydroxyazapropazone of 14% was determined.

Apazone↗
PubMed1979

Pharmacokinetics of azapropazone following single oral and intravenous doses.

The pharmacokinetics of azapropazone (Prolixan) was studied in 7 healthy volunters following single oral and i.v. doses of 600 mg. After i.v. injection plasma concentration declined biexponentially with time. The half-life of the beta-phase was 13.6 +/- 2.6 h (mean +/- SD), the apparent volume of distribution 11.9 +/- 3.5 l, and the total clearance 10.1 +/- 2.1 ml . min-1. Following oral administration peak plasma concentrations occurred between 3 and 6 h and declined with a beta-phase half-life of 14.3 +/- 2.8 h. The binding of azapropazone to plasma proteins was high (ranging from 99.52 to 99.67% at a total plasma concentration of 75 micrograms/ml). The bioavailability of azapropazone when administered as capsules was 83 +/- 19%.

Administration, Oral↗
PubMed1984

Distalgesic; safety and efficacy. Efficacy: UK experience.

The UK experience of Distalgesic efficacy is examined, and 18 trials have been reviewed, of which only five were controlled and only three contained a placebo. Three trials are examined in detail and the problems of trial methodology discussed. The assessment of analgesic effect in chronic painful conditions presents considerable problems. Despite the fact that Distalgesic appears to be a useful analgesic in the clinical situation, long-term controlled studies of its effectiveness in chronic pain are still awaited.

Acetaminophen↗
PubMed1984

Comparative effects of some non-steroidal anti-inflammatory drugs on the ultrastructural integrity and prostaglandin levels in the rat gastric mucosa: relationship to drug uptake.

Studies were performed in fasted rats to establish if the propensity of 4 non-steroidal anti-inflammatory (NSAI) drugs to elicit varying degrees of gastric mucosal damage following oral administration is related to their rate of absorption by the mucosal and subsequent inhibitory effects on prostaglandin (PG) production in vivo. Aspirin (200 mg/kg p.o.) and indomethacin (10 mg/kg p.o.) produced ultrastructural signs of damage at 10-60 min to the surface mucous cells, parietal cells and endothelial cells of sub-mucosal capillaries coincident with the relatively rapid absorption of the radiolabelled drugs and reduction in the mucosal content of PGE2 and 6-keto PGF1 alpha determined by gas chromatography/mass spectrometry. Azapropazone (100 mg/kg p.o.) failed to elicit mucosal damage either ultrastructurally or even visually up to 23 h after dosing and did not affect the content of PG's even though the drug was present in the mucosa in sufficient concentration to elicit reduction in prostaglandin synthesis in vitro. Benoxaprofen (110 mg/kg p.o.) reduced the content of PGE2 and somewhat variably, that of 6-keto PGF1 alpha, was more slowly absorbed c.f. aspirin and indomethacin, but failed to elicit appreciable mucosal damage. These results show that while reduction in PG synthesis is a factor in the development of damage by ulcerogenic drugs, it appears that the rate of absorption or other biochemical effects (including e.g. influences on the production of oxyradicals or 5-lipoxygenase products of eicosanoid metabolism) may contribute to the relatively low irritancy of drugs such as azapropazone or benoxaprofen.

Animals↗
PubMed1983

Preliminary studies with azapropazone in gout and hyperuricaemia.

Eight patients with acute gouty arthritis were treated with high dose oral azapropazone 600 mg qds in an open study in order to evaluate its therapeutic potential in acute gout. The drug appeared to be as effective as previous agents used in the management of individual patient's acute gout with resolution of pain in 2-21 days, and it had a potent hypouricaemic and uricosuric effect. The uricosuric effect of azapropazone 300 mg qds and phenylbutazone 100 mg tds was compared in a seven day cross-over study in seven asymptomatic patients with gout and hyperuricaemia. Azapropazone had a more rapid uricosuric effect than phenylbutazone. There was a statistically significant fall in serum uric acid and rise in uric acid clearance 24 hours after starting azapropazone and 72 hours following phenylbutazone.

Adult↗
PubMed1983

The determination of azapropazone and its 6-hydroxy metabolite in plasma and urine by HPLC.

A high-performance liquid chromatography (HPLC) procedure has been developed for the determination of azapropazone and its 6-hydroxy metabolite in plasma and urine. The procedure is simple and rapid since extraction of the drug and its metabolite is not required. Plasma proteins are precipitated with methanol, and the supernate is injected onto a reverse-phase HPLC column. With photometric detection at 254 nm, the procedure can determine as little as 0.4 micrograms/ml azapropazone in plasma or urine and 1.5-3 micrograms/ml of the metabolite in urine, depending upon the level of interference. The procedure has been used successfully in single-dose pharmacokinetic and bioavailability studies of azapropazone dosage forms.

Apazone↗
PubMed1978

Endoscopic evaluation of the effect of azapropazone on the gastric mucosa.

The gastro-intestinal tolerance of azapropazone, a new non-steroidal anti-inflammatory agent, was studied endoscopically in 14 volunteers with no past history of gastro-intestinal disease. This study shows that gastrointestinal tolerance to azapropazone given in a daily dose of 1200 mg for a period of 31 days is good. Istolated erosions with mild hyperemia were found in 2 subjects only. No subjective symptoms were noted during the period of the study.

Apazone↗
PubMed1982

Characterization of an important drug binding area on human serum albumin including the high-affinity binding sites of warfarin and azapropazone.

This paper reports a variety of experimental observations which strongly support the assumption that the warfarin binding site, or site I of human serum albumin, is better described as the warfarin-azapropazone binding area, consisting of the overlapping binding sites for warfarin and azapropazone. In general, drugs interacting with one of the two sites will also displace drugs bound to the other site, although their displacing potencies for both sites may vary considerably. This is most pronounced in the case of glibenclamide, which strongly inhibits the binding of drugs to the azapropazone site with only minor effects on drugs bound to the warfarin site. The lone tryptophan residue of human serum albumin, previously shown to be part of the warfarin binding site, is obviously located in the not-overlapping part of the warfarin site, so that its modification affects only the binding of drugs to the warfarin and not to the azapropazone site of this large binding area. The observation of different but overlapping binding sites might explain the fact that the albumin binding of drugs which seem to be bound to similar sites because of their mutual displacement can be affected differently during several disease states.

Apazone↗
PubMed1982

[Human pharmacokinetics of different i.v. doses of azapropazone (HPLC-determination) (author's transl)].

The pharmacokinetic profile of azapropazone (Prolixan), sodium salt of 5-dimethylamino-9,5-dimethylamine-9-methyl-5-propyl-1H-pyrazolol[1,2-a][1,2,4]benzotriazine-1,3(2H)-dione, was established. Six healthy, adult volunteers received a single dose of either 600 mg or 1200 mg azapropazone as sodium salt intravenously. The drug was selectively separated from its metabolites and other plasmatic compounds and it was quantified by measurement of extinction at 254 nm. The kinetic parameters of azapropazone were independent of the applied dose (600 mg and 1200 mg): Biological half-life (t0.5): 16.8 +/- 2.95 h and 17.2 +/- 3.0 h; Total clearance (Cltot): 10.2 +/- 2.1 ml min-1 (both doses); Central volume of distribution (Vc): 3.7 +/- 0.71 and 3.9 +/- 0.91; Apparent volume of distribution (Vd): 12.5 +/- 2.91 and 14.4 +/- 2.41. Initial serum concentrations were 170 +/- 41.5 micrograms ml-1 and 326.3 +/- 84.5 micrograms ml-1, determined by extrapolation (C0 at time t0). The areas under the plasma concentration curves (AUC0 infinity) were calculated to amount 1052.5 +/- 217.4 micrograms ml-1h-1 and 2078.4 +/- 515.9 micrograms ml-1h-1. Three rate constants associated with the elimination of the drug could be calculated.

Adult↗
PubMedDate not supplied

[Azapropazone versus indomethacin in a double blind test with patients with ankylosing spondylitis].

In a double lind test 60 patients with ankylosing spondylitis received either Azapropazone (30 patients) or Indomethacin (30 patients) during a period of three weeks. In the two well comparable groups the therapeutic effect was equally good. As the results show the Azapropazone group came out a little better concerning the finger-ground distance and the difference in circumference of thorax, and the Azapropazone group was favoured slightly by the general judgement of the patients. However, these differences are not relevant. The influence on the spontaneous pain in the daytime and during the night and the shifting of dorsal and lumbar vertebral column was equally good in both groups. The compatibility was good in 59 out of 60 patients. One patient had to stop the Azapropazone medication because of gastric trouble in the second week of treatment. This result shows that in most patients an adequate medication with Azapropazone or with Indomethacin leads to a distinct reduction of pain and even painlessness already after a 3 weeks' treatment. This is particularly important regarding kinesiatrics. Indomethacin and Phenylbutazone are generally regarded as approved preparations in treatment of ankylosing spondylitis. If Azapropazone which, according to all previous reports has no hematotoxic effect like Phenylbutazone, had the same good effect in a double blind test as Indomethacin, this must be regarded as a very positive result. Concerning the good compatibility of Azapropazone, a change of drug is possible without a reduction of the effect.

Adolescent↗