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Percutaneous absorption of chlorquinaldol (Sterosan).

The percutaneous absorption of chlorquinaldol from three different preparations for skin treatment (Sterosan-hydrocortison ointment and cream, Sterosan ointment) was evaluated by measuring the cumulative urinary excretion of chlorquinaldol and was compared to that found after an equivalent oral dose. In the blood the concentrations were below the detection limit of the analytical procedure, i.e., smaller than 0.02 microgram/ml. The study was carried out in 3 healthy volunteers using a four-period change-over design. The topical preparations were applied under occlusive dressings. Following epicutaneous application of the three topicals in quantities containing 30 mg chlorquinaldol each, the mean urinary excretion of the drug amounted to 11.1 +/- 6.6, 19.5 +/- 3.5 and 13.0 +/- 2.5% of the applied dose. When the same dose of chlorquinaldol was administered orally, 67.6 +/- 9.5% of the dose was excreted in the urine. Taking the urinary elimination as the minimal amount of drug absorbed, the extent of percutaneous absorption from the three dermatological preparations varied between 4.2 and 23.5% of the applied dose. There was no difference in the pattern of urinary excretion products among the three topicals and the oral formulation. The bulk of chlorquinaldol (mean 98.0 +/- 0.1%) was excreted as sulfate (mean 1.3 +/- 0.3%) or unchanged drug (mean 0.8 +/- 0.1%).

Administration, Oral↗

Prevention and treatment of atrophic rhinitis in pigs with Getroxel, chlorquinaldol and oxytetracycline.

The sensitivity of ten Bordetella bronchiseptica and ten Pasteurella multocida strains, each isolated from cases of atrophic rhinitis (AR), was examined in tube dilution test. Getroxel, chlorquinaldol and oxytetracycline and the former two ones combined with trimethoprim inhibited the growth of both species in vitro. The minimum inhibitory and the minimum bactericidal concentration was less than 0.5 microgram/ml. When efficacy was tested in SPF in the group fed a combination of Getroxel, chlorquinaldol and oxytetracycline (60 mg, 240 mg and 360 mg/kg of feed, respectively), P. multocida disappeared from the nasal cavity by the end of a 30-day treatment. B. bronchiseptica was reisolated in low numbers from 2 out of 9 piglets. The daily body mass gain was by 7.9% higher and the feed conversion rate was by 19% better than in the control group. After slaughter, only mild signs of AR were seen in 3 out of 9 piglets treated with the above-mentioned drug combination, while in the control group severe lesions were observed in 8 out of 9 pigs. In treated commercial herds P. multocida disappeared from the nasal cavity of the piglets by the end of the treatment (42nd day of life), but the B. bronchiseptica strains could not be completely eliminated. Due to the treatment, mortality between 2 and 6 weeks of age decreased by 0.8-7.6%. Daily body mass gain was, on the average, 16.4% higher, the amount of feed needed for 1 kg body mass gain was by 15.3% lower and the duration of fattening was by 30.8 days shorter than in the control groups.

Animals↗

[In vitro activity of an antiseptic, chlorquinaldol, against Neisseria gonorrhoeae and Chlamydia trachomatis].

The activity of chlorquinaldol, a derivative of hydroxy-8-quinolein used for local antisepsy, was studied against Neisseria gonorrhoeae and Chlamydia trachomatis. The weak solubility of the product and the special growth conditions of the organisms made an adaptation of the AFNOR norm necessary. For 0.1 to 0.2% (W/V) chlorquinaldol concentrations, a reduction of about 10(4) organisms was obtained after 60 minutes for N. gonorrhoeae and C. trachomatis. However, for technical problems, the concentrations tested were 10 to 100 times lower than the doses usually recommended for this antiseptic.

Chlamydia trachomatis↗

[Antibacterial activity of chlorquinaldol esters and 2-styryl-substituted derivatives].

Studied was the bacteriostatic activity of a total of 17 new esters and replaced 2-styryl derivatives of chlorquinaldol. Determined were also the lowest concentrations that suppressed the growth of organisms. Some of the compounds showed higher activity and broader spectrum of antibacterial qualities, mainly against Escherichia coli, Salmonella gallinarum, and Salmonella cholerae suis as compared to the initial therapeutic preparation chlorquinaldol. It was found that the presence of chlorine atoms either in the second or in the second and fourth place in the benzene nucleus of the esters studied, the presence of a NO2-group in the third place of the same nucleus, and the presence of an extranuclear hydroxyacetyl remainder in the ester grouping could lead to a rise of the antibacterial activity. The presence of an F atom in the second and third place of the benzene nucleus of the sterile grouping also raised the activity of these compounds.

Bacteria↗

[Comparative studies on Bi-Nerisona cream (diflucortolone valerinate + chlorquinaldol) and on a combination preparation (betamethasone valerinate + gentamicin + tolnaftate + clioquinol) in a double-blind trial].

Bi-Nerisone cream and a control preparation, also in the form of a cream, have been clinically tested on 343 patients by means of a double blind study. Equilvalent results were obtained without registering any significant statistical differences, a finding, however, proving to be of great importance as Bi-Nerisone only contains two active substances (Diflucortolone valerat + Chlorquinaldol), whereas the control preparation contains a total of four (Betamethasone valerate + Gentamycin + Tolnaftate + Clioquinol).

Betamethasone Valerate↗