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The benzylpenicillin ester-HI is 50% hydrolyzed within 23 min. in 0.9% NaCl solution at pH 7.3 and 37° to penicillin and diethylaminoethanol.The HI salt is sparingly soluble and the HCl salt is very soluble in aqueous solutionBoth salts are slowly absorbed and partly hydrolyzed in the gastrointestinal tract.The HI salt is less toxic than the HCl salt when administered orally, subcutaneously, or intramuscularly.Intravenous administration can, according to the dose, cause either a transient drop in arterial blood pressure or complete circulatory failure due to cardiac arrest.

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

A Note on the Stability of the Trifluoromethyl Group of Bendroflumethiazide in Rats

3区 · 医学

Article

作者: Hasselmann, G ; Roholt, K

AbstractThe effect of bendroflumethiazide on the teeth of rats on a carious diet was examined and compared to that of sodium fluoride to determine whether release of fluoride takes place from the trifluoromethyl group of the substance. No detectable fluoride was released.

2002-08-01·British Journal of Dermatology1区 · 医学

Randomized comparison of the type 4 phosphodiesterase inhibitor cipamfylline cream, cream vehicle and hydrocortisone 17-butyrate cream for the treatment of atopic dermatitis

1区 · 医学

Article

作者: E.J.M. Van Leent ; J. Traulsen ; C.E.M. Griffiths ; M. Gilbert

BACKGROUNDTherapeutic options to treat atopic dermatitis are limited. Leukocytes from atopic patients have an abnormally high activity of cyclic adenosine monophosphate (AMP)-phosphodiesterase (PDE), which can be normalized in vitro by PDE inhibitors. Cipamfylline is a new potent and selective inhibitor of PDE-4.OBJECTIVESTo compare the efficacy and safety of up to 14 days' topical treatment with cipamfylline (0.15%) cream with vehicle and with hydrocortisone 17-butyrate (0.1%) cream.PATIENTS AND METHODSInternational, multicentre, prospective, randomized double-blind, left-right studies of cipamfylline vs. vehicle and cipamfylline vs. hydrocortisone 17-butyrate in adult patients with stable symmetrical atopic dermatitis on the arms.RESULTSBoth cipamfylline and hydrocortisone 17-butyrate reduced the Total Severity Score significantly (P < 0.001). The reduction with cipamfylline was significantly greater than that with vehicle (difference vehicle-cipamfylline 1.67 95% confidence interval (CI) 1.06, 2.28; P < 0.001) and was significantly less than with hydrocortisone 17-butyrate (difference hydrocortisone-cipamfylline -2.10 95% CI -2.93, -1.27; P < 0.001). Investigator and patient assessments of the overall treatment response showed a similar picture.CONCLUSIONSCipamfylline cream is significantly more effective than vehicle, but significantly less effective than hydrocortisone 17-butyrate cream in the treatment of atopic dermatitis.

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