Meningitis: What It Is and How to Avoid It Watch Video

Sulfonamides (Ophthalmic)

This monograph includes information on the following:

1) Sulfacetamide
2) Sulfisoxazole


INN:
Sulfisoxazole— Sulfafurazole

BAN:
Sulfacetamide—Sulphacetamide
Sulfisoxazole—Sulphafurazole

VA CLASSIFICATION
Primary: OP201

Commonly used brand name(s): Ak-Sulf1; Bleph-101; Cetamide1; Gantrisin2; I-Sulfacet1; Isopto-Cetamide1; Ocu-Sul-101; Ocu-Sul-151; Ocu-Sul-301; Ocusulf-101; Ophthacet1; Sodium Sulamyd1; Steri-Units Sulfacetamide1; Sulf-101; Sulfair1; Sulfair 101; Sulfair 151; Sulfair Forte1; Sulfamide1; Sulfex1; Sulten-101.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antibacterial (ophthalmic)—

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

Accepted

Conjunctivitis, bacterial (treatment) or
Ocular infections, other (treatment)—Ophthalmic sulfonamides are indicated in the treatment of conjunctivitis and other superficial ocular infections caused by susceptible organisms.

Trachoma (treatment) or
Chlamydial infections, other (treatment)—Ophthalmic sulfonamides are indicated concurrently with systemic sulfonamides in the treatment of trachoma and other chlamydial infections.

[Blepharitis, bacterial (treatment)]—Ophthalmic sulfonamides are used in the treatment of bacterial blepharitis. {01}

[Blepharoconjunctivitis (treatment)]—Ophthalmic sulfonamides are used in the treatment of blepharoconjunctivitis. {01}

[Keratitis, bacterial (treatment)]—Ophthalmic sulfonamides are used in the treatment of bacterial keratitis. {01}

[Keratoconjunctivitis, bacterial (treatment)]—Ophthalmic sulfonamides are used in the treatment of bacterial keratoconjunctivitis. {01}

Note: Not all species or strains of a particular organism may be susceptible to a specific sulfonamide.



Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    Sulfacetamide sodium: 254.24
    Sulfisoxazole diolamine: 372.44

Mechanism of action/Effect:

Sulfonamides are broad-spectrum, bacteriostatic anti-infectives. They are structural analogs of aminobenzoic acid (PABA) and competitively inhibit a bacterial enzyme, dihydropteroate synthetase, that is responsible for incorporation of PABA into dihydrofolic acid. This blocks the synthesis of dihydrofolic acid and decreases the amount of metabolically active tetrahydrofolic acid, a cofactor for the synthesis of purines, thymidine, and DNA.

Susceptible bacteria are those that must synthesize folic acid. The action of sulfonamides is antagonized by PABA and its derivatives (e.g., procaine and tetracaine) and by the presence of pus or tissue breakdown products, which provide the necessary components for bacterial growth.

Absorption:

Following topical application of sulfacetamide (30% solution) to the eye, small amounts may be absorbed into the cornea.


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to one sulfonamide may be sensitive to other sulfonamides also.

Patients sensitive to furosemide, thiazide diuretics, sulfonylureas, or carbonic anhydrase inhibitors may be sensitive to sulfonamides also.

Pregnancy/Reproduction

Problems in humans have not been documented.

Breast-feeding

Problems in humans have not been documented.

Pediatrics

Appropriate studies on the relationship of age to the effects of sulfonamides have not been performed in the pediatric population.


Geriatrics


Appropriate studies on the relationship of age to the effects of sulfonamides have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

» Silver preparations, such as silver nitrate, mild silver protein    (topical sulfonamides are incompatible with silver salts; concurrent use is not recommended)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problem exists
Sensitivity to sulfonamides


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence more frequent
    
Hypersensitivity (itching, redness, swelling, or other sign of irritation not present before therapy)





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Sulfonamides (Ophthalmic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to sulfonamides, furosemide, thiazide diuretics, sulfonylureas, or carbonic anhydrase inhibitors
Other medications, especially silver preparations, such as silver nitrate or mild silver protein

Proper use of this medication
Proper administration technique for ophthalmic solution and ophthalmic ointment

» Compliance with full course of therapy

» Proper dosing
Missed dose: Applying as soon as possible; not applying if almost time for next dose

» Proper storage

Precautions while using this medication
Blurred vision after application of ophthalmic ointments

Possibility of stinging or burning after application

Checking with physician if no improvement within a few days


Side/adverse effects
Signs of potential side effects, especially hypersensitivity


General Dosing Information
At night the ophthalmic ointment may be used as an adjunct to the ophthalmic solution to provide prolonged contact with the medication.

Although some manufacturers recommend a dose of 2 drops of an ophthalmic solution at appropriate intervals, the conjunctival sac will usually hold only 1 drop.

SULFACETAMIDE


Ophthalmic Dosage Forms

SULFACETAMIDE SODIUM OPHTHALMIC OINTMENT USP

Usual adult and adolescent dose
Ophthalmic antibacterial
Topical, to the conjunctiva, a thin strip (approximately 1.25 to 2.5 cm) of ointment four times a day and at bedtime {07}.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


10% (Rx) [Ak-Sulf{03}] [Bleph-10] [Cetamide{09}] [Ocu-Sul-10] [Sodium Sulamyd] [Sulfair 10][Generic]

Canada—


10% (Rx) [Cetamide] [Sodium Sulamyd{07}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For the eye.
   • Continue medicine for full time of treatment.


SULFACETAMIDE SODIUM OPHTHALMIC SOLUTION USP

Usual adult and adolescent dose
Ophthalmic antibacterial
Topical, to the conjunctiva, 1 drop every one to three hours during the day and less frequently during the night. {03} {07} {08}


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


10% (Rx) [Ak-Sulf{03}] [Bleph-10] [I-Sulfacet] [Ocu-Sul-10{10}] [Ocusulf-10] [Ophthacet] [Sodium Sulamyd] [Sulf-10] [Sulfair] [Sulfair 10] [Sulfamide] [Sulten-10][Generic]


15% (Rx) [Isopto-Cetamide] [I-Sulfacet] [Ocu-Sul-15{10}] [Steri-Units Sulfacetamide] [Sulfair] [Sulfair 15][Generic]


30% (Rx) [I-Sulfacet] [Ocu-Sul-30{10}] [Sodium Sulamyd] [Sulfair] [Sulfair Forte][Generic]

Canada—


10% (Rx) [Ak-Sulf{06}] [Bleph-10] [Isopto-Cetamide] [Sodium Sulamyd{07}] [Sulfex]


30% (Rx) [Sodium Sulamyd{07}]

Packaging and storage:
Store between 8 and 15 °C (46 and 59 °F). {03} Store in a tight, light-resistant container. {08}

Stability:
Sulfonamide solutions become dark brown with time. When this occurs, solutions should be discarded. {03}

Auxiliary labeling:
   • For the eye.
   • Keep in a cool place. {03}
   • Continue medicine for full time of treatment.
   • Discard if dark brown. {03}

Note: Dispense in original unopened container.



SULFISOXAZOLE


Ophthalmic Dosage Forms

Note: The dosing and strengths of the dosage forms available are expressed in terms of sulfisoxazole base.


SULFISOXAZOLE DIOLAMINE OPHTHALMIC OINTMENT USP

Usual adult and adolescent dose
Ophthalmic antibacterial
Topical, to the conjunctiva, a thin strip (approximately 1.25 to 2.5 cm) of ointment one to three times a day and at bedtime. {05}


Usual pediatric dose
See Usual adult and adolescent dose . {05}

Strength(s) usually available
U.S.—


4% (base) (each gram of ophthalmic ointment contains 55.6 mg of sulfisoxazole diolamine, equivalent to approximately 40 mg of sulfisoxazole) (Rx) [Gantrisin{05} (phenylmercuric nitrate 1:50,000)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing. {05}

Auxiliary labeling:
   • For the eye.
   • Continue medicine for full time of treatment.


SULFISOXAZOLE DIOLAMINE OPHTHALMIC SOLUTION USP

Usual adult and adolescent dose
Ophthalmic antibacterial
Topical, to the conjunctiva, 1 drop three or more times a day. {05}


Usual pediatric dose
Ophthalmic antibacterial
Infants up to 2 months of age: Use is not recommended. {05}

Infants and children over 2 months of age: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


4% (base) (each mL of ophthalmic solution contains 55.6 mg of sulfisoxazole diolamine, equivalent to approximately 40 mg of sulfisoxazole) (Rx) [Gantrisin{05} (phenylmercuric nitrate 1:100,000)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container. Protect from freezing. {05}

Auxiliary labeling:
   • For the eye.
   • Continue medicine for full time of treatment.

Note: Dispense in original unopened container.




Revised: 07/01/1993



References
  1. Indications Index review, 1986.
  1. Open.
  1. Sulfacetamide ointment and solution package insert (Ak-Sulf, Akorn—US), PDR Ophthalmology 1993: 204.
  1. Open.
  1. Sulfisoxazole ointment and solution package insert (Gantrisin, Roche—US), PDR Ophthalmology 1993: 311.
  1. Sulfacetamide solution package insert (Ak-Sulf, Akorn—Canada), CPS 1992: 26.
  1. Sulfacetamide ointment and solution package insert (Sodium Sulfamyd, Schering—Canada), CPS 1992: 1057.
  1. Sulfacetamide solution package insert (Isopto Cetamide, Alcon—US), PDR Ophthalmology 1993: 218.
  1. Sulfacetamide ointment package insert (Cetamide, Alcon—US), PDR Ophthalmology 1993: 218.
  1. Sulfacetamide ointment and solution package insert (Ocu-Sul-10, Ocu-Sul-15, and Ocu-Sul-30, Ocumed—US), PDR Ophthalmology 1993: 304.
Hide
(web1)