AzaSite®
azithromycin 1% · ophthalmic solution
Antibiotic
Approved uses
Bacterial conjunctivitis
1 drop in the affected eye(s) BID, 8 to 12 hours apart, x 2 days, then 1 drop QD x 5 days.
OFF-LABELNot in the FDA label for this product
Blepharitis
1 drop BID x 2 days, then 1 drop QD through day 28.
Open-label · n=26 · no control
Multicenter open-label study, 26 subjects with moderate to severe blepharitis treated without warm compresses or lid scrubs: meibomian gland plugging, eyelid margin redness, palpebral conjunctival redness and ocular discharge all fell from baseline at day 29 (P at or below 0.002) and remained improved 4 weeks after stopping (P at or below 0.006). Uncontrolled and unmasked; eyelid margin cultures fell for coagulase-negative staphylococci and Corynebacterium xerosis, while tear cytokine concentrations did not change.
Meibomian gland dysfunction (posterior blepharitis)
1 drop BID x 2 days, then 1 drop QD x 12 days, with warm compresses 5 to 10 minutes BID.
Randomized open-label · n=21
Randomized open-label trial, 21 patients (10 drug plus compresses, 11 compresses alone, 20 completed): greater improvement in meibomian gland plugging, secretion quality and eyelid redness than compresses alone at day 14; small, unmasked, single-site. A 2020 meta-analysis of 18 studies pooling oral and topical azithromycin for MGD (topical arms include both 1% and 1.5% formulations) reported symptom score improvement with SMD 1.54 (95% CI 1.15 to 1.92) and a 25% pooled adverse event rate for topical dosing.
Contraindications
Hypersensitivity to any component of this product.
Available Forms2.5 mL bottle, 1% solution, 25 mg per bottle
Mechanism of ActionMacrolide antibiotic; binds the 50S ribosomal subunit of susceptible organisms and interferes with microbial protein synthesis. Systemic exposure after ocular dosing is estimated to fall below quantifiable limits (10 ng/mL or less) at steady state.
Warnings & Precautions
- Topical ophthalmic use only: Not for injection, subconjunctival administration or introduction into the anterior chamber.
- Systemic azithromycin hypersensitivity: Angioedema, anaphylaxis, Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported rarely in patients taking the drug systemically, with fatalities reported; weigh a known systemic hypersensitivity before ocular use.
- Resistant organism overgrowth: Prolonged use may cause overgrowth of non-susceptible organisms including fungi; discontinue and start alternative therapy if super-infection occurs.
- Contact lens wear: Not appropriate while signs or symptoms of bacterial conjunctivitis are present.
Common Side Effects
- Ocular: Eye irritation 1% to 2%, the most frequent reaction across 698 treated patients.
- Ocular, under 1%: Blurred vision, burning or stinging on instillation, contact dermatitis, corneal erosion, dry eye, eye pain, itching, ocular discharge, punctate keratitis, reduced visual acuity.
- Systemic, under 1%: Dysgeusia, facial swelling, hives, nasal congestion, periocular swelling, rash, sinusitis, urticaria.
Pregnancy & LactationPregnancy: Category B; rat and mouse reproduction studies at up to 200 mg/kg/day, roughly 5,000 times the 2 mg maximum human ocular daily dose, showed no fetal harm, with moderate maternal toxicity at the highest dose; no adequate studies in pregnant women.
Lactation: Excretion in human milk is unknown.
Pediatric UseNot established below 1 year; efficacy demonstrated in controlled trials at 1 year and older.