Manufacturing Establishments (1)
Bausch & Lomb Incorporated
079587625
Products (1)
Polymyxin B Sulfate and Trimethoprim
24208-315
ANDA064120
ANDA (C73584)
OPHTHALMIC
June 1, 2023
Drug Labeling Information
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
Principal Display Panel
NDC 24208-315-10
Polymyxin B
Sulfate and
Trimethoprim
Ophthalmic
Solution, USP*
(Sterile)
FOR TOPICAL
APPLICATION
IN THE EYE
Rx only
10 mL
BAUSCH + LOMB
9534002
AB31509
DESCRIPTION SECTION
DESCRIPTION
Polymyxin B sulfate and trimethoprim ophthalmic solution, USP is a sterile antimicrobial solution for topical ophthalmic use. It has pH of 4.0 to 5.5 and osmolality of 270 to 310 mOsm/kg.
Chemical Names:
Trimethoprim sulfate, 2,4-diamino-5-(3,4,5-trimethoxybenzyl) pyrimidine
sulfate, is a white, odorless, crystalline powder with a molecular weight of
678.72 and the following structural formula:
C28H38N8O10S Mol. Wt. 678.72
Polymyxin B sulfate is the sulfate salt of polymyxin B1 and B2 which are produced by the growth of Bacillus polymyxa (Prazmowski) Migula (Fam. Bacillaceae). It has a potency of not less than 6,000 polymyxin B units per mg, calculated on an anhydrous basis. The structural formula is:
Each mL contains: Actives: polymyxin B sulfate equal to 10,000 polymyxin B units, trimethoprim sulfate (equivalent to trimethoprim 1 mg); Inactives: purified water, sodium chloride. Sulfuric acid and, if necessary, sodium hydroxide may be added to adjust pH (4.0 – 5.5). Preservative: benzalkonium chloride 0.004%
CLINICAL PHARMACOLOGY SECTION
CLINICAL PHARMACOLOGY
Trimethoprim is a synthetic antibacterial drug active against a wide variety of aerobic gram-positive and gram-negative ophthalmic pathogens. Trimethoprim blocks the production of tetrahydrofolic acid from dihydrofolic acid by binding to and reversibly inhibiting the enzyme dihydrofolate reductase. This binding is stronger for the bacterial enzyme than for the corresponding mammalian enzyme and therefore selectively interferes with bacterial biosynthesis of nucleic acids and proteins.
Polymyxin B, a cyclic lipopeptide antibiotic, is bactericidal for a variety of gram-negative organisms, especially Pseudomonas aeruginosa. It increases the permeability of the bacterial cell membrane by interacting with the phospholipid components of the membrane.
Blood samples were obtained from 11 human volunteers at 20 minutes, 1 hour and 3 hours following instillation in the eye of 2 drops of ophthalmic solution containing 1 mg trimethoprim and 10,000 units polymyxin B per mL. Peak serum concentrations were approximately 0.03 mcg/mL trimethoprim and 1 unit/mL polymyxin B.
Microbiology
In vitrostudies have demonstrated that the anti-infective components of
trimethoprim sulfate and polymyxin B sulfate ophthalmic solution are active
against the following bacterial pathogens that are capable of causing external
infections of the eye:
**Trimethoprim:**Staphylococcus aureus and Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus faecalis, Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus aegyptius, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis (indole-negative), Proteus vulgaris (indole- positive), Enterobacter aerogenes and Serratia marcescens.
**Polymyxin B:**Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes and Haemophilus influenzae.
INDICATIONS & USAGE SECTION
INDICATIONS AND USAGE
Polymyxin B sulfate and trimethoprim ophthalmic solution is indicated in the treatment of surface ocular bacterial infections, including acute bacterial conjunctivitis, and blepharoconjunctivitis, caused by susceptible strains of the following microorganisms: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus viridans, Haemophilus influenzae and Pseudomonas aeruginosa.1
1Efficacy for this organism in this organ system was studied in fewer than 10 infections.
DOSAGE & ADMINISTRATION SECTION
DOSAGE AND ADMINISTRATION
In mild to moderate infections, instill one drop in the affected eye(s) every 3 hours (maximum of 6 doses per day) for a period of 7 to 10 days.
CONTRAINDICATIONS SECTION
CONTRAINDICATIONS
Polymyxin B sulfate and trimethoprim ophthalmic solution is contraindicated in patients with known hypersensitivity to any of its components.
WARNINGS SECTION
WARNINGS
NOT FOR INJECTION INTO THE EYE. If a sensitivity reaction to polymyxin B sulfate and trimethoprim ophthalmic solution occurs, discontinue use. Polymyxin B sulfate and trimethoprim ophthalmic solution is not indicated for the prophylaxis or treatment of ophthalmia neonatorum.
ADVERSE REACTIONS SECTION
ADVERSE REACTIONS
The most frequent adverse reaction to polymyxin B sulfate and trimethoprim ophthalmic solution is local irritation consisting of increased redness, burning, stinging, and/or itching. This may occur on instillation, within 48 hours, or at any time with extended use. There are also multiple reports of hypersensitivity reactions consisting of lid edema, itching, increased redness, tearing, and/or circumocular rash. Photosensitivity has been reported in patients taking oral trimethoprim.
**To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or **www.fda.gov/medwatch.
SPL UNCLASSIFIED SECTION
Rx only
FOR TOPICAL APPLICATION IN THE EYE