Chapter 198 Macrolides Scott P. Shaw, DVM, DACVECC KEY POINTS • Macrolides are concentrated in macrophages, resulting in high drug levels at the site of infection. • Macrolides exhibit high levels of efficacy against gram-positive organisms and moderate efficacy against anaerobic organisms. INTRODUCTION Macrolides represent a large group of similar compounds that are all products of Streptomyces spp. Biochemically they are characterized by a macrocyclic lactone ring attached to one or more sugar moieties. Macrolides with the greatest clinical efficacy generally are derived from erythromycin. It should be noted that azithromycin is not technically a macrolide, but rather an azalide. It generally is grouped with the macrolides because it shares most of their properties. MECHANISM OF ACTION All macrolides work by reversibly binding the 50s ribosome. This results in suppression of ribonucleic acid–dependent protein synthesis. Macrolides are bacteriostatic at clinical concentrations. They are particularly effective against gram-positive organisms and Mycoplasma spp. In addition, they have fair efficacy against anaerobic organisms. Many macrolides are actively concentrated in macrophages. This can result in very high drug concentrations at the site of infection.1 PHARMACOLOGY In general, macrolides are characterized by low serum concentrations and large volumes of distribution. They are concentrated in tissues including the lung, heart, and macrophages. Newer macrolides such as azithromycin have high oral bioavailability (40% to 60%) and long half-lives. The main route of excretion is through bile and the intestinal tract.2 Only gold members can continue reading. Log In or Register to continue Share this:Click to share on Twitter (Opens in new window)Click to share on Facebook (Opens in new window) Related Related posts: Deteriorating Mental Status Hyperthermia and Fever Ventilator-Associated Lung Injury Allergic Airway Disease in Dogs and Cats and Feline Bronchopulmonary Disease Stay updated, free articles. Join our Telegram channel Join Tags: Small Animal Critical Care Medicine Sep 10, 2016 | Posted by admin in SMALL ANIMAL | Comments Off on Macrolides Full access? Get Clinical Tree
Chapter 198 Macrolides Scott P. Shaw, DVM, DACVECC KEY POINTS • Macrolides are concentrated in macrophages, resulting in high drug levels at the site of infection. • Macrolides exhibit high levels of efficacy against gram-positive organisms and moderate efficacy against anaerobic organisms. INTRODUCTION Macrolides represent a large group of similar compounds that are all products of Streptomyces spp. Biochemically they are characterized by a macrocyclic lactone ring attached to one or more sugar moieties. Macrolides with the greatest clinical efficacy generally are derived from erythromycin. It should be noted that azithromycin is not technically a macrolide, but rather an azalide. It generally is grouped with the macrolides because it shares most of their properties. MECHANISM OF ACTION All macrolides work by reversibly binding the 50s ribosome. This results in suppression of ribonucleic acid–dependent protein synthesis. Macrolides are bacteriostatic at clinical concentrations. They are particularly effective against gram-positive organisms and Mycoplasma spp. In addition, they have fair efficacy against anaerobic organisms. Many macrolides are actively concentrated in macrophages. This can result in very high drug concentrations at the site of infection.1 PHARMACOLOGY In general, macrolides are characterized by low serum concentrations and large volumes of distribution. They are concentrated in tissues including the lung, heart, and macrophages. Newer macrolides such as azithromycin have high oral bioavailability (40% to 60%) and long half-lives. The main route of excretion is through bile and the intestinal tract.2 Only gold members can continue reading. Log In or Register to continue Share this:Click to share on Twitter (Opens in new window)Click to share on Facebook (Opens in new window) Related Related posts: Deteriorating Mental Status Hyperthermia and Fever Ventilator-Associated Lung Injury Allergic Airway Disease in Dogs and Cats and Feline Bronchopulmonary Disease Stay updated, free articles. Join our Telegram channel Join
