Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Ointment, Ophthalmic, as sodium:
Generic: 10% (3.5 g)
Solution, Ophthalmic, as sodium:
Bleph-10: 10% (5 mL)
Generic: 10% (5 mL, 15 mL)
Pharmacology
Mechanism of Action
Interferes with bacterial growth by inhibiting bacterial folic acid synthesis through competitive antagonism of PABA
Pharmacokinetics/Pharmacodynamics
Onset of Action
Improvement of conjunctivitis is usually seen within 3 to 6 days
Use: Labeled Indications
Ocular infections:
Ophthalmic ointment and solution: Treatment of conjunctivitis and other superficial ocular infections due to susceptible microorganisms: Escherichia coli, Staphylococcus aureus, Streptococcus pneumoniae, viridans group streptococci, Haemophilus influenzae, Klebsiella species, and Enterobacter species.
Ophthalmic solution: Treatment of trachoma as an adjunctive to systemic sulfonamide therapy
Limitations of use: Topically applied sulfonamides do not provide adequate coverage against Neisseria species, Serratia marcescens and Pseudomonas aeruginosa. A significant percentage of staphylococcal isolates are also completely resistant to sulfa drugs.
Contraindications
Hypersensitivity to sulfonamides or any component of the formulation.
Documentation of allergenic cross-reactivity for sulfonamides is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Dosage and Administration
Dosing: Adult
Conjunctivitis, other superficial ocular infections: Note: Taper dose by increasing dosage time interval as condition responds; usual duration of treatment: 7 to 10 days:
Ophthalmic ointment: Apply ~1/2-inch ribbon into the conjunctival sac of affected eye(s) every 3 to 4 hours and at bedtime.
Ophthalmic solution: Instill 1 to 2 drops into the conjunctival sac(s) of affected eye(s) every 2 to 3 hours.
Trachoma: Ophthalmic solution: Instill 2 drops into the conjunctival sac(s) of affected eye(s) every 2 hours; must be used in conjunction with systemic therapy.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Conjunctivitis: Infants ≥2 months, Children, and Adolescents: Ophthalmic:
Ointment: Instill 1/2 inch ribbon into the lower conjunctival sac of affected eye(s) every 3 to 4 hours and at bedtime; increase dosing interval as condition responds. Ointment may be used as an adjunct to the solution; usual duration of treatment: 7 to 10 days
Solution: Instill 1 to 2 drops into the lower conjunctival sac of affected eye(s) every 2 to 3 hours initially; increase dosing interval as condition responds; usual duration of treatment: 7 to 10 days
Trachoma: Infants ≥2 months, Children, and Adolescents: Ophthalmic: Solution: Instill 2 drops into the conjunctival sac of affected eye(s) every 2 hours; must be used in conjunction with systemic therapy
Administration
Ophthalmic: For topical ophthalmic use only; not for injection. Avoid contact of tube or bottle tip with skin or eye.
Ointment: May be used as an adjunct to the ophthalmic solution.
Solution: Apply finger pressure to lacrimal sac during and for 1 to 2 minutes after instillation of solution to decrease risk of absorption and systemic effects. For the treatment of trachoma, use must be in conjunction with systemic therapy.
Storage
Solution: Store at 8°C to 25°C (46°F to 77°F); protect from light. Darkened solutions should not be used.
Ointment: Store at 20°C to 25°C (68°F to 77°F).
Drug Interactions
There are no known significant interactions.
Adverse Reactions
Frequency not defined.
Cardiovascular: Edema
Hypersensitivity: Hypersensitivity reaction
Neuromuscular & skeletal: Systemic lupus erythematosus
Ophthalmic: Burning sensation of eyes, conjunctival hyperemia, conjunctivitis, corneal ulcer, eye irritation, stinging of eyes
Warnings/Precautions
Concerns related to adverse effects:
- Blood dyscrasias: Severe reactions (rare fatalities), including agranulocytosis, aplastic anemia, and other blood dyscrasias, have occurred with sulfonamides (regardless of route). Discontinue at the first sign of serious reaction.
- Dermatologic reactions: Severe reactions (rare fatalities), including Stevens-Johnson syndrome and toxic epidermal necrolysis, have occurred with sulfonamides (regardless of route). Discontinue at first sign of rash.
- Hepatic necrosis: Fatalities (rare) associated with fulminant hepatic necrosis have occurred with sulfonamides (regardless of route). Discontinue at first sign of serious reaction.
- Sulfonamide allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling; however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe.
- Superinfection: Prolonged use may lead to overgrowth of nonsusceptible organisms, including fungi. If superinfection is suspected, institute appropriate alternative therapy.
Other warnings/precautions:
- Administration: Do not use concurrently with silver preparations.
- Appropriate use: For topical application to the eye only; not for injection. To avoid contamination, do not touch tip of container to any surface.
- Efficacy: May be inactivated by purulent exudates containing PABA.
Monitoring Parameters
Response to therapy, hypersensitivity reactions
Pregnancy
Pregnancy Considerations
Animal reproduction studies have not been conducted. Use of systemic sulfonamides during pregnancy may cause kernicterus in the newborn.
Patient Education
What is this drug used for?
- It is used to treat eye infections.
Frequently reported side effects of this drug
- Burning
- Stinging
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Severe sulfonamide reaction like rash; red, swollen, blistered, or peeling skin; red or irritated eyes; sores in your mouth, throat, nose, or eyes; fever, chills, or sore throat; cough that is new or worse; loss of strength and energy; any bruising or bleeding; or liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes
- Vision changes
- Eye pain
- Severe eye irritation
- Eye discharge
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
