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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc. Chapter 85 Bacteriostatic Inhibitors of Protein Synthesis: Tetracyclines, Macrolides, and Others
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.2 Tetracyclines Four members of the tetracycline family available for systemic therapy Tetracycline Demeclocycline Doxycycline Minocycline
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.3 Tetracyclines Tetracyclines Broad-spectrum antibiotics Inhibit protein synthesis Increasing bacterial resistance has emerged Uses Rickettsial disease Chlamydia trachomatis Brucellosis Cholera
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.4 Tetracyclines Uses (cont’d) Mycoplasma pneumoniae Lyme disease Anthrax Helicobacter pylori Acne Peptic ulcer disease Periodontal disease
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.5 Tetracyclines Absorption – chelation Calcium supplements, milk products, iron supplements, magnesium-containing laxatives, and most antacids Adverse effects Gastrointestinal irritation Effect on bone and teeth Superinfection Hepatotoxicity Renal toxicity Photosensitivity and other effects
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.6 Tetracyclines Drug and food interaction Absorption of tetracyclines decreased if given with: Milk products Milk products Calcium supplements Calcium supplements Iron supplements Iron supplements Magnesium-containing laxatives Magnesium-containing laxatives Most antacids Most antacids
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.7 Macrolides (Erythromycin) Broad-spectrum antibiotic MOA – inhibition of protein synthesis Usually bacteriostatic but can be bactericidal Use if allergic to penicillin Active against most gram-positive and some gram-negative bacteria
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.8 Macrolides (Erythromycin) Therapeutic uses Whooping cough, acute diphtheria, Corynebacterium diphtheriae, chlamydial infections, M. pneumoniae, group A Streptococcus pyogenes Drug interactions Adverse effects Gastrointestinal QT prolongation and sudden cardiac death Superinfection
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.9 Other Macrolides Clarithromycin (Biaxin) Azithromycin (Zithromax) Dirithromycin (Dynabac) Troleandomycin (Tao)
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.10 Clindamycin (Cleocin) Inhibits protein synthesis Can induce severe antibiotic-associated pseudomembranous colitis (can be fatal) Active against most anaerobic bacteria (gram-positive and gram-negative) Indicated only for certain anaerobic infections located outside the CNS
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.11 Clindamycin (Cleocin) Adverse effects Antibiotic-associated pseudomembranous colitis Hepatic toxicity Hepatic toxicity Blood dyscrasias Blood dyscrasias Diarrhea Diarrhea Hypersensitivity reactions Hypersensitivity reactions
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.12 Linezolid (Zyvox) First member of a new class of antibiotics – oxazolidinones Use Active against multidrug-resistant gram-positive pathogens (eg,vancomycin-resistant enterococci (VRE), methicillin-resistant Staphylococcus aureus (MRSA) Active against multidrug-resistant gram-positive pathogens (eg, vancomycin-resistant enterococci (VRE), methicillin-resistant Staphylococcus aureus (MRSA)
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.13 Linezolid (Zyvox) Bacteriostatic inhibitor of protein synthesis Cross-resistance with other agents unlikely Active against aerobic and facultative gram- positive bacteria VRE and MRSA
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.14 Linezolid (Zyvox) Most common side effects Diarrhea Nausea and vomiting Headache May also cause myelosuppression Drug interaction with MAOIs
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.15 Telithromycin First representative of ketolides class of antibiotics Use Effective against strains of Streptococcus pneumoniae Adverse effects GI effects Gray syndrome Visual disturbances
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.16 Dalfopristin/Quinupristin First members of streptogramins (new class of antibiotics) Inhibit bacterial protein synthesis Principal indication – VRE Adverse effects Hepatotoxicity Drug interactions CYP3A4
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.17 Chloramphenicol (Chloromycetin) Broad-spectrum antibiotic Inhibits protein synthesis Uses Only for life-threatening infections for which safer drugs are ineffective or contraindicated Adverse effects Reversible bone marrow depression Fatal aplastic anemia Gray syndrome GI effects Peripheral neuropathy
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Elsevier Inc. items and derived items © 2010 by Saunders, an imprint of Elsevier Inc.18 Additional Drugs Spectinomycin (Trobicin) Tigecycline (Tygacil) Retapamulin and mupirocin Topical antibiotics indicated for impetigo Mupirocin – also for MRSA in nostrils
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