Oral Antibiotics as Anti-infectives


Antibiotic

Mechanism of action

Amoxicillin/clavulanate

Binds penicillin-binding proteins, inhibiting final transpeptidation step of peptidoglycan synthesis in bacterial cell walls. Addition of clavulanate inhibits beta-lactamase, which renders antibiotic resistance by destroying the beta-lactam ring common to penicillins and other antibiotics. Bactericidal

Trimethoprim-sulfamethoxazole

Blocks consecutive steps in the synthesis of nucleic acids. Sulfamethoxazole inhibits bacterial synthesis of dihydrofolic acid, while trimethoprim inhibits the formation of tetrahydrofolic acid from dihydrofolic acid. Bacteriostatic

Clindamycin

Suppresses bacterial protein synthesis by binding the 50S ribosomal subunit. Bacteriostatic

Quinolones

Inhibits DNA gyrase, blocking DNA relaxation. Bactericidal

Macrolides

Suppresses bacterial protein synthesis by binding the 50S ribosomal subunit. Bacteriostatic

Doxycycline

Suppresses bacterial protein synthesis by binding the 30S ribosomal subunit. Primarily bacteriostatic




Beta-Lactams


Beta-lactams are one of the more commonly used antibiotics in rhinosinusitis. Amoxicillin with or without clavulanate and less commonly third-generation cephalosporins are often used in CRS. Depending on local resistance patterns that vary from region to region, amoxicillin has fair activity against common sinusitis pathogens such as Streptococcus pneumoniae, Moraxella catarrhalis, and Haemophilus influenzae [51]. Both beta-lactamase and penicillin-binding protein resistance patterns have been documented with amoxicillin, however, and the addition of a beta-lactamase inhibitor like clavulanate improves the coverage against agents such as H. influenzae, M. catarrhalis, and S. aureus [52]. In the case of S. pneumoniae resistance, which is based on penicillin-binding protein changes, resistance can be overcome by higher amoxicillin serum levels. The commonly used adult amoxicillin dosages are usually sufficient [53].

Second- and third-generation cephalosporins have increased activity against H. influenza and gram-negative aerobes. Third-generation cephalosporins generally have very good activity against M. catarrhalis and H. influenzae, with fair activity against S. pneumoniae [51]. No oral cephalosporins are active against Pseudomonas aeruginosa.


Macrolides


Macrolides are frequently prescribed in CRS due to the anti-infective and anti-inflammatory properties. Macrolides used in CRS include azithromycin, clarithromycin, and erythromycin. Their greatest antimicrobial property is against streptococci, staphylococci, and other gram-positive pathogens, but also against atypical microbes such as Mycoplasma pneumoniae. Similarly to beta-lactams, S. pneumoniae resistance is an increasing problem and has reached rates over 20 % in many European countries [54].


Fluoroquinolones


Fluoroquinolones have gained common use in CRS for their broad spectrum of activity, but more importantly for their coverage of P. aeruginosa and other gram-negative bacteria. This group covers many gram-positive agents well, specifically H. influenzae, M. catarrhalis, and S. pneumoniae. The agents in this group used for CRS most commonly are levofloxacin, ciprofloxacin, and moxifloxacin. Ciprofloxacin and levofloxacin generally have the best activity against P. aeruginosa and the least against gram-positives [55]. Therefore, ciprofloxacin and levofloxacin should be thoughtfully used and possibly reserved for P. aeruginosa.


Trimethoprim-Sulfamethoxazole


Used predominantly in acute sinusitis, trimethoprim-sulfamethoxazole has gained use in chronic sinusitis due to its activity against community-acquired methicillin-resistant Staphylococcus aureus. Due to its seldom use in chronic sinusitis, there is often less resistance to trimethoprim-sulfamethoxazole for bacterial organisms associated with chronic sinusitis.


Clindamycin


Clindamycin is known for its activity against anaerobic gram-negative organisms, but it also has fairly good coverage against gram-positive organisms, including S. pneumonia and several staphylococci species. It has also been commonly used to treat MRSA; however resistance rates vary widely in different areas of the country, so local resistance patterns should be considered.


Doxycycline


Doxycycline is an agent whose use can be helpful in CRS because of its activity against methicillin-resistant S. aureus. The effectiveness of this drug against MRSA depends on local resistance rates, but is generally over 80 % [56]. This drug also has good coverage of atypical microbes like Mycoplasma pneumonia.



References



1.

Metson RB, Gliklich RE. Clinical outcomes in patients with chronic sinusitis. Laryngoscope. 2000;110:24–8.PubMedCrossRef


2.

Kaszuba S, Stewart M. Medical management and diagnosis of chronic rhinosinusitis: a survey of treatment patterns by United States otolaryngologists. Am J Rhinol. 2006;20(2):186–90.PubMed


3.

Dubin M, Liu C, Lin S, Senior B. American Rhinologic Society member survey on “maximal medical therapy” for chronic rhinosinusitis. Am J Rhinol. 2007;21(4):483–8.PubMedCrossRef


4.

Soler ZM, Oyer SL, Kern RC, Senior BAM, Kountakis SE, Marple BF, et al. Antimicrobials and chronic rhinosinusitis with or without polyposis in adults: an evidenced-based review with recommendations. Int Forum Allergy Rhinol. 2013;3:31–47.PubMedCrossRef


5.

Van Zele T, Gevaert P, Holtappels G, Beule A, Wormald PJ, Mayr S, et al. Oral steroids and doxycycline: two different approaches to treat nasal polyps. J Allergy Clin Immunol. 2010;125:1069–1076.e4.PubMedCrossRef


6.

Dellamonica P, Choutet P, Lejeune JM, Lucht F, Morgon A, Pessey JJ, et al. Efficacy and tolerance of cefotiam hexetil in the super-infected chronic sinusitis. A randomized, double-blind study in comparison with cefixime. Ann Otolaryngol Chir Cervicofac Bull Soc Otolaryngol Hop Paris. 1994;111:217–22.


7.

Legent F, Bordure P, Beauvillain C, Berche P. A double-blind comparison of ciprofloxacin and amoxycillin/clavulanic acid in the treatment of chronic sinusitis. Chemotherapy. 1994;40:8–15.PubMedCrossRef


8.

Huck W, Reed BD, Nielsen RW, Ferguson RT, Gray DW, Lund GK, et al. Cefaclor vs amoxicillin in the treatment of acute, recurrent, and chronic sinusitis. Arch Fam Med. 1993;2:497–503.PubMedCrossRef


9.

Fokkens W, Lund V, Mullol J. European position paper on rhinosinusitis and nasal polyps. Rhinol Suppl. 2007;2007:1–136.


10.

Schalek P, Petras P, Klement V, Hahn A. Short-term antibiotics treatment in patients with nasal polyps and enterotoxins producing Staphylococcus aureus strains. Eur Arch Otorhinolaryngol. 2009;266:1909–13.PubMedCrossRef


11.

Dubin MG, Kuhn FA, Melroy CT. Radiographic resolution of chronic rhinosinusitis without polyposis after 6 weeks vs 3 weeks of oral antibiotics. Ann Allergy Asthma Immunol. 2007;98:32–5.PubMedCrossRef

Apr 2, 2016 | Posted by in General Surgery | Comments Off on Oral Antibiotics as Anti-infectives

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