Chpt 45中 Tetrcyclines and Chloramphenicol.pptVIP

Ⅰ. Tetracyclines 四环素类  A. Mechanism of action Primarily bacteriostatic, inhibiting protein synthesis. bind to the 30S (16S) subunit of microbial ribosomes → block the attachment of charged aminoacyl-tRNA →prevent introduction of new amino acids into the nascent peptide chain. Tetracycline inhibits cell growth by inhibiting translation. It binds to the 16S part of the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. B. Spectrum of activity 1.Tetracyclines are effective against G+and G- bacteria. They are less active against G+ organisms than penicilins and cephalosporins. They are less active against G- organisms than aminoglycosides and chloramphenicol. They have the favorable effects on Rickettsiae立克次体, Mycoplasma支原体, Chlamydiae衣原体 and Spirochete. They are effective against some protozoa, eg, amebas. C. Clinical uses 1. The second choice drugs for treatment: infectious diseases by G+and G- bacteria. 2. First choice for treatment: The infection of Rickettsiae , Mycoplasma , Chlamydiae and Brucella 布鲁氏菌. D. Untoward effects Gastrointestinal reactions: stomach upset, diarrhea, nausea, or vomiting. Superinfection : staphylococcal enterocolitis , interstitial candidiasis念珠菌病, pseudomembranous colitis. The effects on the bone and teeth of children : Yellow - brown discoloration of their teeth, depression of bone growth. Serious hepatic damage. Phototoxicity: drug intermediates accumulate in skin, exposed to UV →toxic compounds→accelerated sunburning . Nephrotoxicity: oliguria . Pseudotumor cerebri (Intracranial Hypertension) : Headache is the most common presenting complaint. Dizziness, nausea, and vomiting may also be encountered, but typically there are no alterations of consciousness or higher cognitive function. E. Resistance (1) decreased intracell