Azithromycin
Unchecked
Azithromycin
Zithromax, Z-Pak, Zmax
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Summary
Classes
Common uses
Community-acquired pneumonia (atypical coverage)0, Streptococcal pharyngitis (penicillin-allergic)0, Chlamydial urethritis/cervicitis0, MAC prophylaxis in HIV0, COPD exacerbation prevention (selected)0, Pertussis treatment and prophylaxis0
Pharmacy
Starting dose
500 mg PO day 1, then 250 mg PO daily days 2-5 (Z-Pak); 1 g PO single dose for chlamydia; pediatric dosing 10 mg/kg day 1, 5 mg/kg days 2-5
Preparations
250 mg, 500 mg, 600 mg tablets; 100, 200 mg/5 mL suspension; 2 g ER suspension (Zmax); 500 mg IV
US FDA Max
500 mg/d (typical regimen); single 2 g for Zmax; 2 g for select STIs
Pharmacology
Routes
Oral, IV
Onset
Clinical improvement within 24-72 hours
Duration
Tissue half-life supports once-daily and post-treatment effect
Half-life
~68 hours (terminal; reflects deep tissue accumulation, much longer than plasma)[1]
Bioavailability
~37% (oral; food reduces absorption modestly)[1]
Pregnancy
Generally considered safe; commonly used in pregnancy when macrolide indicated.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Azithromycin reversibly binds the 23S rRNA of the bacterial 50S ribosomal subunit, blocking peptide chain translocation and inhibiting protein synthesis; the azalide nitrogen substitution at position 9a of the macrolactone ring extends acid stability and tissue penetration relative to erythromycin.0 Long tissue half-life (uptake into macrophages with delivery to infection sites) supports short courses. QT-interval prolongation is a recognized class effect; FDA 2013 advisory flagged increased cardiovascular death risk in patients with prolonged baseline QT, hypokalemia, or other risk factors[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Zithromax (azithromycin), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/050670s032,050710s045,050784s032lbl.pdf