AzaSite

Dosage Forms And Strengths

2.5 mL of a 1% sterile topical ophthalmic solution.

AzaSite is a sterile aqueous topical ophthalmic formulation of 1% azithromycin.

NDC 31357-040-25: 2.5 mL in 5 mL bottle containing a total of 25 mg of azithromycin in a white, round, low-density polyethylene (LDPE) bottle, with a clear LDPE dropper tip, and a tan colored high density polyethylene (HDPE) eyedropper cap. A white tamper evident over-cap is provided.

NDC 31357-040-03: 2.5 mL in 4 mL bottle containing a total of 25 mg of azithromycin in a white, round, low-density polyethylene (LDPE) bottle, with a clear LDPE dropper tip, and a tan colored high density polyethylene (HDPE) eyedropper cap. A white tamper evident over-cap is provided.

Storage And Handling

Store unopened bottle under refrigeration at 2°C to 8°C (36°F to 46°F). Once the bottle is opened, store at 2°C to 25°C (36°F to 77°F) for up to 14 days. Discard after the 14 days.

Manufactured for: Inspire Pharmaceuticals, Inc., a subsidiary of MERCK & CO., INC., Whitehouse Station, NJ 08889, USA. Manufactured by: Catalent Pharma Solutions, LLC, Woodstock, IL 60098. Revised: Oct 2012

AzaSite® is indicated for the treatment of bacterial conjunctivitis caused by susceptible isolates of the following microorganisms:

CDC coryneform group G*

Haemophilus influenzae
Staphylococcus aureus
Streptococcus mitis group
Streptococcus pneumoniae

*Efficacy for this organism was studied in fewer than 10 infections.

The recommended dosage regimen for the treatment of bacterial conjunctivitis is:

Instill 1 drop in the affected eye(s) twice daily, eight to twelve hours apart for the first two days and then instill 1 drop in the affected eye(s) once daily for the next five days.

Hypersensitivity to any component of this product.

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Topical Ophthalmic Use Only

NOT FOR INJECTION. AzaSite is indicated for topical ophthalmic use only, and should not be administered systemically, injected subconjunctivally, or introduced directly into the anterior chamber of the eye.

Anaphylaxis And Hypersensitivity With Systemic Use Of Azithromycin

In patients receiving systemically administered azithromycin, serious allergic reactions, including angioedema, anaphylaxis, and dermatologic reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported rarely in patients on azithromycin therapy. Although rare, fatalities have been reported. The potential for anaphylaxis or other hypersensitivity reactions should be considered based on known hypersensitivity to azithromycin when administered systemically.

Growth Of Resistant Organisms With Prolonged Use

As with other anti-infectives, prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If super-infection occurs, discontinue use and institute alternative therapy. Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit-lamp biomicroscopy, and where appropriate, fluorescein staining.

Avoidance Of Contact Lenses

Patients should be advised not to wear contact lenses if they have signs or symptoms of bacterial conjunctivitis.

Patient Counseling Information

See FDA-Approved Patient Labeling (PATIENT INFORMATION).

Patients should be advised to avoid contaminating the applicator tip by allowing it to touch the eye, fingers or other credits.

Patients should be directed to discontinue use and contact a physician if any signs of an allergic reaction occur.

Patients should be told that although it is common to feel better early in the course of the therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by AzaSite (azithromycin ophthalmic solution) or other antibacterial drugs in the future.

Patients should be advised not to wear contact lenses if they have signs or symptoms of bacterial conjunctivitis.

Patients should be advised to thoroughly wash hands prior to using AzaSite.

Patients should be advised to invert the closed bottle (upside down) and shake once before each use. Remove cap with bottle still in the inverted position. Tilt head back, and with bottle inverted, gently squeeze bottle to instill one drop into the affected eye(s).

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment Of Fertility

Long-term studies in animals have not been performed to evaluate carcinogenic potential. Azithromycin has shown no mutagenic potential in standard laboratory tests: mouse lymphoma assay, human lymphocyte clastogenic assay, and mouse bone marrow clastogenic assay. No evidence of impaired fertility due to azithromycin was found in mice or rats that received oral doses of up to 200 mg/kg/day.

Use In Specific Populations

Pregnancy

Pregnancy Category B

Reproduction studies have been performed in rats and mice at doses up to 200 mg/kg/day. The highest dose was associated with moderate maternal toxicity. These doses are estimated to be approximately 5,000 times the maximum human ocular daily dose of 2 mg. In the animal studies, no evidence of harm to the fetus due to azithromycin was found. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, azithromycin should be used during pregnancy only if clearly needed.

Nursing Mothers

It is not known whether azithromycin is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when azithromycin is administered to a nursing woman.

Pediatric Use

The safety and effectiveness of AzaSite solution in pediatric patients below 1 year of age have not been established. The efficacy of AzaSite in treating bacterial conjunctivitis in pediatric patients one year or older has been demonstrated in controlled clinical trials.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

SIDE EFFECTS

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in one clinical trial of a drug cannot be directly compared with the rates in the clinical trials of the same or another drug and may not reflect the rates observed in practice.

The data described below reflect exposure to AzaSite in 698 patients. The population was between 1 and 87 years old with clinical signs and symptoms of bacterial conjunctivitis. The most frequently reported ocular adverse reaction reported in patients receiving AzaSite was eye irritation. This reaction occurred in approximately 1-2% of patients. Other adverse reactions associated with the use of AzaSite were reported in less than 1% of patients and included ocular reactions (blurred vision, burning, stinging and irritation upon instillation, contact dermatitis, corneal erosion, dry eye, eye pain, itching, ocular discharge, punctate keratitis, visual acuity reduction) and non-ocular reactions (dysgeusia, facial swelling, hives, nasal congestion, periocular swelling, rash, sinusitis, urticaria).

DRUG INTERACTIONS

No information provided.

Pregnancy Category B

Reproduction studies have been performed in rats and mice at doses up to 200 mg/kg/day. The highest dose was associated with moderate maternal toxicity. These doses are estimated to be approximately 5,000 times the maximum human ocular daily dose of 2 mg. In the animal studies, no evidence of harm to the fetus due to azithromycin was found. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, azithromycin should be used during pregnancy only if clearly needed.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in one clinical trial of a drug cannot be directly compared with the rates in the clinical trials of the same or another drug and may not reflect the rates observed in practice.

The data described below reflect exposure to AzaSite in 698 patients. The population was between 1 and 87 years old with clinical signs and symptoms of bacterial conjunctivitis. The most frequently reported ocular adverse reaction reported in patients receiving AzaSite was eye irritation. This reaction occurred in approximately 1-2% of patients. Other adverse reactions associated with the use of AzaSite were reported in less than 1% of patients and included ocular reactions (blurred vision, burning, stinging and irritation upon instillation, contact dermatitis, corneal erosion, dry eye, eye pain, itching, ocular discharge, punctate keratitis, visual acuity reduction) and non-ocular reactions (dysgeusia, facial swelling, hives, nasal congestion, periocular swelling, rash, sinusitis, urticaria).

No information provided.

The plasma concentration of azithromycin following ocular administration of AzaSite (azithromycin ophthalmic solution) in humans is unknown. Based on the proposed dose of one drop to each eye (total dose of 100 mcL or 1 mg) and exposure information from systemic administration, the systemic concentration of azithromycin following ocular administration is estimated to be below quantifiable limits ( ≤ 10 ng/mL) at steady-state in humans, assuming 100% systemic availability.