克拉霉素

Chemical structure: macrolide

Clarithromycin is a semisynthetic macrolide antibiotic that is derived from erythromycin. Clarithromycin may be bacteriostatic or bactericidal depending on the organism and drug concentration . Clarithromycin may be used to attenuate cardiac transplantation rejection via matrix metalloproteinase suppression. Clarithromycin has been used to study inflammatory markers in chronic obstructive pulmonary disease (COPD). It is used to study bacterial protein synthesis and peptide translation.

克拉霉素是一种大环内酯类抗生素，能干扰细菌蛋白质的合成。克拉霉素是红霉素的酸稳定形式，对革兰氏阴性细菌特别有效。它的半衰期很短，但是其代谢产物 14-羟基克拉霉素对某些细菌的活性几乎是克拉霉素的两倍。

Clarithromycin inhibits bacterial protein synthesis by binding to the bacterial 50S ribosomal subunit. Binding inhibits peptidyl transferase activity and interferes with amino acid translocation. Clarithromycin is first metabolized to 14-OH clarithromycin, which is active and works synergistically with its parent compound. Clarithromycin penetrates the bacteria cell wall and reversibly binds to domain V of the 23S ribosomal RNA of the 50S subunit of the bacterial ribosome, blocking translocation of aminoacyl transfer-RNA and polypeptide synthesis. Clarithromycin also inhibits the hepatic microsomal CYP3A4 isoenzyme and P-glycoprotein, an energy-dependent drug efflux pump.

Practically insoluble in water, soluble in acetone and methylene chloride, slightly soluble in methanol.

Keep container tightly closed in a dry and well-ventilated place. Keep in a dry place.