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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
In pharmacokinetic studies it has been demonstrated that the concentrations of azithromycin measured in tissues are noticeably higher (as much as 50 times) than those measured in plasma, which indicates that the agent strongly binds to tissues. Azithromycin is excreted in bile mainly as unchanged drug. Ten metabolites have also been detected in bile, which are formed through N- and O- demethylation in the liver, hydroxylation of desosamine – and aglycone rings and cleavage of cladinose conjugate. The metabolites of azithromycin are not microbiologically active.
Cethromycin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Cethromycin (formerly ABT-773; Restanza) is a ketolide antibiotic whose development was initiated by Abbott in 1997 but abandoned in 2002. Since 2004 Advanced Life Sciences has promoted the development of cethromycin. The ketolides are structurally derived from erythromycin A and designed to overcome bacterial resistance to macrolides. One of the main features of the ketolide antibiotics is the absence of the neutral sugar L-cladinose at position 3 of the erythonolide ring, which is replaced by a keto group (thus giving rise to the antibiotic class name) (Zhanel et al., 2002). The absence of the L-cladinose moiety also results in better drug absorption and less gastric irritation through improved acid stability.
Clarithromycin laurate salt: physicochemical properties and pharmacokinetics after oral administration in humans
Published in Pharmaceutical Development and Technology, 2019
Bashar A. Alkhalidi, Hatim S. AlKhatib, Mohammad Saleh, Saja Hamed, Yasser Bustanji, Nader Al Bujuq, Naji Najib, Susana Torrado-Susana, Al-Sayed Sallam
CLM has a very bitter taste, is practically insoluble in water, is slightly soluble in methanol and ethanol, and is soluble in acetone (Salem 1996). CLM degrades below pH 3 at 37 °C to 5-O-desosaminyl-6-O-methyl-erythronolide A with the loss of the cladinose sugar (Morimoto et al. 1990; Nakagawa et al. 1992; Ishii et al. 1998; Mordi et al. 2000; Fujiki et al. 2011; Noguchi et al. 2014). However, such instability at low pH doesn’t significantly affect CLM stability in tablet formulation in gastric fluid, which makes it possible to be administered orally without an enteric coating. (Noguchi et al. 2014).