clindamycin hydrochloride

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clindamycin hydrochloride-associated colitis

Number of visits:1000 Date:2015/12/15 5:52:17
clindamycin hydrochloride-associated colitis. A prospective study
A prospective study of 200 consecutive patients receiving clindamycin hydrochloride (Cleocin HCl) for various reasons showed a 21% incidence of diarrhea and a 10% incidence of pseudomembranous colitis. The total dosage of clindamycin hydrochloride before the onset of diarrhea and the clinical syndrome associated with the diarrhea were of little help in differentiating those patients with or without pseudomembranous colitis. Pseudomembranous colitis developed most frequently after orally administered clindamycin hydrochloride, but was also seen with clindamycin hydrochloride parenterally administered. Early proctoscopic examination is necessary to diagnose colitis and is the most accurate means of detecting pseudomembranes; rectal biopsy results can confirm the diagnosis and delineate the degree of inflammation present. When the diagnosis is made soon after the onset of diarrhea, and the antibiotic is stopped, the pseudomembranous colitis seems to be self-limiting with no mortality.
Abstract The kinetics and mechanism of degradation of the antibiotic clindamycin hydrochloride were studied in buffered aqueous solution in the pH range 0.4-12. clindamycin hydrochloride showed maximum stability at pH 3-5; however, high temperature studies indicated that not more than 10% degradation will occur in the pH range 1-6.5 after two years at 25. In the pH range 0.4-4 the major degradative pathway was hydrolysis of the thioglycoside linkage to form 1-dethiomethyl-1-hydroxy clindamycin hydrochloride and methyl mercaptan. The major degradative pathway in the pH range 5-10 was scission of the 7-(S)-Cl of clindamycin hydrochloride to form the 7-(R)-OH analog, lincomycin. Evidence was obtained that supports the hypothesis that this conversion to lincomycin proceeds through an oxazolonium intermediate and that the extent of conversion depends on the degree of protonation of the amine function of clindamycin hydrochloride. The activation energy for clindamycin hydrochloride degradation in 0.1 M HCl, where thioglycoside hydrolysis is predominant, is 38.0 卤 1.2 kcal./mole, and the activation energy in 0.2 M citrate buffer adjusted to pH 5, where conversion to lincomycin is predominant
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