Zylet loteprednol etabonate and tobramycin 5 mg/mL; 3 mg/mL Suspension/ Drops, 1 bottle
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Aminoglycoside Antibacterial class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Ophthalmic loteprednol products are used to treat different eye conditions: Loteprednol (Inveltys, Lotemax, Lotemax SM) is used to treat swelling and pain after cataract surgery (procedure to treat clouding of the lens in the eye). Loteprednol (Alrex) is used to reduce eye redness, itching, and swelling caused by seasonal allergies. Loteprednol (Lotemax) is used to reduce eye swelling caused by allergies, certain eye infections, ocular rosacea (condition that can cause swelling, redness, and itching of the eye), herpes zoster (shingles; a rash that can occur in people who have had chickenp...
Read the full MedlinePlus article ↗- It's treating both at the same time. Loteprednol etabonate is the steroid that calms the inflammation — the redness, swelling, and irritation in your eye. Tobramycin is the antibio...
- What exactly is this eye drop treating — is it for infection or inflammation?
- The usual schedule is one or two drops in the affected eye every four to six hours. Your doctor might ask you to use them more often — as frequently as every one to two hours — in...
- How often do I put these drops in, and does it matter what time of day?
Patient education
Supplement & herbal interactions
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
-
UNII F5UM2KM3W7
Benzalkonium chloride is a chemical compound that works as a preservative and antimicrobial agent in medications. It prevents bacterial and fungal growth in liquid formulations to keep the product safe during storage and use.
-
UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
-
UNII PDC6A3C0OX
Glycerin is a clear, thick liquid derived from plant oils or fats. It acts as a humectant to retain moisture, a sweetener, and a solvent in medications.
-
UNII FZ989GH94E
Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
-
UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
-
UNII O40UQP6WCF
A strong acid used in small amounts to adjust and maintain the pH balance of a medicine, helping ensure stability and proper dissolution of the active ingredients.
-
UNII Y27PUL9H56
Tyloxapol is a synthetic detergent and surfactant used in medications as a solubilizer and emulsifier. It helps dissolve or blend ingredients that don't naturally mix well, improving how the medicine disperses in liquid formulations.
-
UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
8 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $64.12 | $64.12 / 1 ml |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Loteprednol etabonate and Tobramycin 5 mg/mL; 3 mg/mL 62332-0801-05 | Alembic | 1 bottle | $38.853 | AB | Availability likely | — |
| Loteprednol etabonate and tobramycin 5 mg/mL; 3 mg/mL 82260-0358-05 | Bausch | 1 bottle | $38.853 | AB | Availability likely | — |
| Zylet 5 mg/mL; 3 mg/mLthis 24208-0358-01 | Bausch | 1 bottle | — | AB | FDA listed | — |
| Loteprednol etabonate and Tobramycin 5 mg/mL; 3 mg/mL 46708-0801-05 | Alembic | 1 bottle | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
Where does this data come from?
💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 24208-0358-01 You're viewing this | 1 BOTTLE, DROPPER in 1 CARTON (24208-358-01) / 1 mL in 1 BOTTLE, DROPPER | — | — | 2004-12-14 | Active |
| 24208-0358-05 | 1 BOTTLE, DROPPER in 1 CARTON (24208-358-05) / 5 mL in 1 BOTTLE, DROPPER | $64.39 / mL | $321.96 | 2004-12-14 | Active |
| 24208-0358-10 | 1 BOTTLE, DROPPER in 1 CARTON (24208-358-10) / 10 mL in 1 BOTTLE, DROPPER | $64.51 / mL | $645.12 | 2004-12-14 | Active |
This pack shows little to no recent Medicaid volume — a different pack size carries most fills. See all packs ↓
Pack size FAQ
What quantity is in NDC 24208-0358-01?
What NDC number is used to bill for this package of Zylet loteprednol etabonate and tobramycin 5 mg/mL; 3 mg/mL Suspension/ Drops?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
Why is there no price listed?
Is the NDC printed on the package the same as the 11-digit billing NDC?
What do the three segments of this NDC mean?
Is this package still being marketed?
Does this product come in other package sizes?
Who lists this product with the FDA?
Do I need a prescription for this product?
Where does this data come from?
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE ZYLET ® (loteprednol etabonate and tobramycin ophthalmic suspension), 0.5%/0.3% is a topical anti-infective and corticosteroid combination for steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where superficial bacterial ocular infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and where the inherent risk of steroid use in certain infective conjunctivitides is accepted to obtain a diminution in edema and inflammation.
They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of superficial ocular infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product (tobramycin) is active against the following common bacterial eye pathogens: Staphylococci, including S. aureus and S. epidermidis (coagulase-positive and coagulase-negative), including penicillin-resistant strains.
Streptococci, including some of the Group A-beta-hemolytic species, some nonhemolytic species, and some Streptococcus pneumoniae , Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii , most Proteus vulgaris strains, Haemophilus influenzae , and H. aegyptius, Moraxella lacunata, Acinetobacter calcoaceticus and some Neisseria species. ZYLET is a combination of loteprednol etabonate, a corticosteroid, and tobramycin, an aminoglycoside antibacterial, indicated for steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where superficial bacterial ocular infection or a risk of bacterial ocular infection exists.
( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Apply one or two drops of ZYLET into the conjunctival sac of the affected eye every four to six hours. ( 2.1 )
2.1Recommended Dosing Apply one or two drops of ZYLET into the conjunctival sac of the affected eye every four to six hours. During the initial 24 to 48 hours, the dosing may be increased, to every one to two hours. Frequency should be decreased gradually as warranted by improvement in clinical signs. Care should be taken not to discontinue therapy prematurely.
2.2Prescription Guideline Not more than 20 mL should be prescribed initially and the prescription should not be refilled without further evaluation [see Warnings and Precautions ( 5.3 )].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Ophthalmic suspension containing 5 mg/mL (0.5%) loteprednol etabonate and 3 mg/mL (0.3%) tobramycin. Ophthalmic suspension containing 5 mg/mL (0.5%) loteprednol etabonate and 3 mg/mL (0.3%) tobramycin. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS ZYLET, as with other steroid anti-infective ophthalmic combination drugs, is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures. ( 4.1 )
4.1Nonbacterial Etiology ZYLET, as with other steroid anti-infective ophthalmic combination drugs, is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures.
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Intraocular Pressure (IOP) Increase : Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision. If this product is used for 10 days or longer, IOP should be monitored. ( 5.1 ) • Cataracts : Use of corticosteroids may result in posterior subcapsular cataract formation.
( 5.2 ) • Delayed Healing : The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. The initial prescription and renewal of the medication order should be made by a physician only after examination of the patient with the aid of a magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
( 5.3 ) • Bacterial Infections : Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infection. In acute purulent conditions, steroids may mask infection or enhance existing infection. If signs and symptoms fail to improve after 2 days, the patient should be re-evaluated.
( 5.4 ) • Viral Infections : Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution. Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex). ( 5.5 ) • Fungal Infections : Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application.
Fungus invasion must be considered in any persistent corneal ulceration where a steroid has been used or is in use. ( 5.6 )
5.1Intraocular Pressure (IOP) Increase Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision. Steroids should be used with caution in the presence of glaucoma. If this product is used for 10 days or longer, intraocular pressure should be monitored.
5.2Cataracts Use of corticosteroids may result in posterior subcapsular cataract formation.
5.3Delayed Healing The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. The initial prescription and renewal of the medication order should be made by a physician only after examination of the patient with the aid of magnification such as a slit lamp biomicroscopy and, where appropriate, fluorescein staining.
5.4Bacterial Infections Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infections. In acute purulent conditions of the eye, steroids may mask infection or enhance existing infection. If signs and symptoms fail to improve after 2 days, the patient should be re-evaluated.
5.5Viral Infections Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution. Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex).
5.6Fungal Infections Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application. Fungus invasion must be considered in any persistent corneal ulceration where a steroid has been used or is in use. Fungal cultures should be taken when appropriate.
5.7Aminoglycoside Hypersensitivity Sensitivity to topically applied aminoglycosides may occur in some patients. If hypersensitivity develops with this product, discontinue use and institute appropriate therapy.
5.8Risk of Contamination Do not allow the dropper tip to touch any surface, as this may contaminate the suspension.
5.9 Contact Lens We…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Adverse reactions have occurred with steroid/anti-infective combination drugs which can be attributed to the steroid component, the anti-infective component, or the combination. ZYLET In a 42-day safety study comparing ZYLET to placebo, ocular adverse reactions included injection (approximately 20%) and superficial punctate keratitis (approximately 15%). Increased intraocular pressure was reported in 10% (ZYLET) and 4% (placebo) of subjects.
Nine percent (9%) of ZYLET subjects reported burning and stinging upon instillation. Ocular reactions reported with an incidence less than 4% include vision disorders, discharge, itching, lacrimation disorder, photophobia, corneal deposits, ocular discomfort, eyelid disorder, and other unspecified eye disorders. The incidence of non-ocular reactions reported in approximately 14% of subjects was headache; all other non-ocular reactions had an incidence of less than 5%.
Loteprednol etabonate ophthalmic suspension 0.2% - 0.5% Reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with infrequent optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, delayed wound healing and secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera. In a summation of controlled, randomized studies of individuals treated for 28 days or longer with loteprednol etabonate, the incidence of significant elevation of intraocular pressure (≥10 mm Hg) was 2% (15/901) among patients receiving loteprednol etabonate, 7% (11/164) among patients receiving 1% prednisolone acetate and 0.5% (3/583) among patients receiving placebo.
Tobramycin ophthalmic solution 0.3% The most frequent adverse reactions to topical tobramycin are hypersensitivity and localized ocular toxicity, including lid itching and swelling and conjunctival erythema. These reactions occur in less than 4% of patients. Similar reactions may occur with the topical use of other aminoglycoside antibiotics.
Secondary Infection The development of secondary infection has occurred after use of combinations containing steroids and antimicrobials. Fungal infections of the cornea are particularly prone to develop coincidentally with long-term applications of steroids. The possibility of fungal invasion must be considered in any persistent corneal ulceration where steroid treatment has been used.
Secondary bacterial ocular infection following suppression of host responses also occurs. Most common adverse reactions reported in patients were injection and superficial punctate keratitis, increased intraocular pressure, burning and stinging upon instillation. ( 6 ) 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.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary There are no adequate and well-controlled studies with loteprednol etabonate or tobramycin in pregnant women. Loteprednol etabonate produced teratogenicity at clinically relevant doses in the rabbit and rat when administered orally during pregnancy. Loteprednol etabonate produced malformations when administered orally to pregnant rabbits at doses ≥ 0.54 times the recommended human ophthalmic dose (RHOD) and to pregnant rats at doses ≥ 13 times the RHOD.
In pregnant rats receiving oral doses of loteprednol etabonate during the period equivalent to the last trimester of pregnancy through lactation in humans, survival of offspring was reduced at doses ≥ 1.3 times the RHOD. Maternal toxicity was observed in rats at doses ≥ 135 times the RHOD, and a maternal no observed adverse effect level (NOAEL) was established at 13 times the RHOD. Abortions were observed in pregnant rabbits administered tobramycin via subcutaneous injection at 180 times the RHOD.
Tobramycin did not affect fetal development when administered by subcutaneous injection to pregnant rats at doses 450 times the RHOD. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies.
Data Animal Data Embryofetal studies were conducted in pregnant rabbits administered loteprednol etabonate by oral gavage on gestation days 6 to 18, to target the period of organogenesis. Loteprednol etabonate produced fetal malformations at doses ≥ 0.1 mg/kg/day (0.54 times the recommended human ophthalmic dose (RHOD) based on body surface area, assuming 100% absorption of loteprednol etabonate). Spina bifida (including meningocele) was observed at doses ≥ 0.1 mg/kg/day, and exencephaly and craniofacial malformations were observed at doses ≥ 0.4 mg/kg/day (2.1 times the RHOD).
At 3 mg/kg/day (16 times the RHOD), loteprednol etabonate was associated with increased incidences of abnormal left common carotid artery, limb flexures, umbilical hernia, scoliosis, and delayed ossification. Abortion and embryofetal lethality (resorption) occurred at doses ≥ 6 mg/kg/day (32 times the RHOD). A NOAEL for developmental toxicity was not established in this study.
The NOAEL for maternal toxicity in rabbits was 3 mg/kg/day. Embryofetal studies were conducted in pregnant rats administered loteprednol etabonate by oral gavage on gestation days 6 to 15, to target the period of organogenesis. Loteprednol etabonate produced fetal malformations, including absent innominate artery at doses ≥ 5 mg/kg/day (13 times the RHOD); and cleft palate, agnathia, cardiovascular defects, umbilical hernia, decreased fetal body weight and decreased skeletal ossification at doses ≥ 50 mg/kg/day (135 times the RHOD).
Embryofetal lethality (resorption) was observed at 100 mg/kg/day (270 times the RHOD). The NOAEL for developmental toxicity in rats was 0.5 mg/kg/day (1.3 times the RHOD). Loteprednol etabonate was maternally toxic (reduced body weight gain) at doses of ≥ 50 mg/kg/day.
The NOAEL for maternal toxicity was 5 mg/kg/day. A peri-/postnatal study was conducted in rats administered loteprednol etabonate by oral gavage from gestation day 15 (start of fetal period) to postnatal day 21 (the end of lactation period). At doses ≥ 0.5 mg/kg/day (1.3 times the RHOD), reduced survival was observed in live-born offspring.
Doses ≥ 5 mg/kg/day (13 times the RHOD) caused umbilical hernia/incomplete gastrointestinal tract. Doses ≥ 50 mg/kg/day (135 times the RHOD) produced maternal toxicity (reduced body weight gain, death), decreased number of live-born offspring, decreased birth weight, and delays in postnatal development. A developmental NOAEL was not established in this study.
The NOAEL for maternal toxicity was 5 mg/kg/day. An embryofetal study was conducted in pregnant rabbits…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary There are no adequate and well-controlled studies with loteprednol etabonate or tobramycin in pregnant women. Loteprednol etabonate produced teratogenicity at clinically relevant doses in the rabbit and rat when administered orally during pregnancy. Loteprednol etabonate produced malformations when administered orally to pregnant rabbits at doses ≥ 0.54 times the recommended human ophthalmic dose (RHOD) and to pregnant rats at doses ≥ 13 times the RHOD.
In pregnant rats receiving oral doses of loteprednol etabonate during the period equivalent to the last trimester of pregnancy through lactation in humans, survival of offspring was reduced at doses ≥ 1.3 times the RHOD. Maternal toxicity was observed in rats at doses ≥ 135 times the RHOD, and a maternal no observed adverse effect level (NOAEL) was established at 13 times the RHOD. Abortions were observed in pregnant rabbits administered tobramycin via subcutaneous injection at 180 times the RHOD.
Tobramycin did not affect fetal development when administered by subcutaneous injection to pregnant rats at doses 450 times the RHOD. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies.
Data Animal Data Embryofetal studies were conducted in pregnant rabbits administered loteprednol etabonate by oral gavage on gestation days 6 to 18, to target the period of organogenesis. Loteprednol etabonate produced fetal malformations at doses ≥ 0.1 mg/kg/day (0.54 times the recommended human ophthalmic dose (RHOD) based on body surface area, assuming 100% absorption of loteprednol etabonate). Spina bifida (including meningocele) was observed at doses ≥ 0.1 mg/kg/day, and exencephaly and craniofacial malformations were observed at doses ≥ 0.4 mg/kg/day (2.1 times the RHOD).
At 3 mg/kg/day (16 times the RHOD), loteprednol etabonate was associated with increased incidences of abnormal left common carotid artery, limb flexures, umbilical hernia, scoliosis, and delayed ossification. Abortion and embryofetal lethality (resorption) occurred at doses ≥ 6 mg/kg/day (32 times the RHOD). A NOAEL for developmental toxicity was not established in this study.
The NOAEL for maternal toxicity in rabbits was 3 mg/kg/day. Embryofetal studies were conducted in pregnant rats administered loteprednol etabonate by oral gavage on gestation days 6 to 15, to target the period of organogenesis. Loteprednol etabonate produced fetal malformations, including absent innominate artery at doses ≥ 5 mg/kg/day (13 times the RHOD); and cleft palate, agnathia, cardiovascular defects, umbilical hernia, decreased fetal body weight and decreased skeletal ossification at doses ≥ 50 mg/kg/day (135 times the RHOD).
Embryofetal lethality (resorption) was observed at 100 mg/kg/day (270 times the RHOD). The NOAEL for developmental toxicity in rats was 0.5 mg/kg/day (1.3 times the RHOD). Loteprednol etabonate was maternally toxic (reduced body weight gain) at doses of ≥ 50 mg/kg/day.
The NOAEL for maternal toxicity was 5 mg/kg/day. A peri-/postnatal study was conducted in rats administered loteprednol etabonate by oral gavage from gestation day 15 (start of fetal period) to postnatal day 21 (the end of lactation period). At doses ≥ 0.5 mg/kg/day (1.3 times the RHOD), reduced survival was observed in live-born offspring.
Doses ≥ 5 mg/kg/day (13 times the RHOD) caused umbilical hernia/incomplete gastrointestinal tract. Doses ≥ 50 mg/kg/day (135 times the RHOD) produced maternal toxicity (reduced body weight gain, death), decreased number of live-born offspring, decreased birth weight, and delays in postnatal development. A developmental NOAEL was not established in this study.
The NOAEL for maternal toxicity was 5 mg/kg/day. An embryofetal study was conducted in pregnant rabbits administered 20 or 40 mg/kg/d…
🧒 Pediatric Use ▾
8.4Pediatric Use Two trials were conducted to evaluate the safety and efficacy of ZYLET (loteprednol etabonate and tobramycin ophthalmic suspension) in pediatric subjects age zero to six years; one was in subjects with lid inflammation and the other was in subjects with blepharoconjunctivitis. In the lid inflammation trial, ZYLET with warm compresses did not demonstrate efficacy compared to vehicle with warm compresses. Patients received warm compress lid treatment plus ZYLET or vehicle for 14 days.
The majority of patients in both treatment groups showed reduced lid inflammation. In the blepharoconjunctivitis trial, ZYLET did not demonstrate efficacy compared to vehicle, loteprednol etabonate ophthalmic suspension, or tobramycin ophthalmic solution. There was no difference between treatment groups in mean change from baseline blepharoconjunctivitis score at Day 15.
There were no differences in safety assessments between the treatment groups in either trial.
🧓 Geriatric Use ▾
8.5Geriatric Use No overall differences in safety and effectiveness have been observed between elderly and younger patients.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids.
However, corticosteroids are thought to act by the induction of phospholipase A 2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A 2 .
Corticosteroids are capable of producing a rise in intraocular pressure. Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent.
The anti-infective component in the combination (tobramycin) is included to provide action against susceptible organisms. In vitro studies have demonstrated that tobramycin is active against susceptible strains of the following microorganisms: Staphylococci, including S. aureus and S. epidermidis (coagulase-positive and coagulase-negative), including penicillin-resistant strains. Streptococci, including some of the Group A-beta-hemolytic species, some nonhemolytic species, and some Streptococcus pneumoniae .
Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii, most Proteus vulgaris strains, Haemophilus influenzae and H. aegyptius , Moraxella lacunata , Acinetobacter calcoaceticus and some Neisseria species.
12.3Pharmacokinetics In a controlled clinical study of ocular penetration, the levels of loteprednol etabonate in the aqueous humor were found to be comparable between LOTEMAX ® and ZYLET treatment groups. Results from a bioavailability study in normal volunteers established that plasma levels of loteprednol etabonate and Δ 1 cortienic acid etabonate (PJ 91), its primary, inactive metabolite, were below the limit of quantitation (1 ng/mL) at all sampling times. The results were obtained following the ocular administration of one drop in each eye of 0.5% loteprednol etabonate ophthalmic suspension 8 times daily for 2 days or 4 times daily for 42 days.
This study suggests that limited (<1 ng/mL) systemic absorption occurs with 0.5% loteprednol etabonate.
🧬 Mechanism of Action ▾
12.1Mechanism of Action Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids.
However, corticosteroids are thought to act by the induction of phospholipase A 2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A 2 .
Corticosteroids are capable of producing a rise in intraocular pressure. Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent.
The anti-infective component in the combination (tobramycin) is included to provide action against susceptible organisms. In vitro studies have demonstrated that tobramycin is active against susceptible strains of the following microorganisms: Staphylococci, including S. aureus and S. epidermidis (coagulase-positive and coagulase-negative), including penicillin-resistant strains. Streptococci, including some of the Group A-beta-hemolytic species, some nonhemolytic species, and some Streptococcus pneumoniae .
Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii, most Proteus vulgaris strains, Haemophilus influenzae and H. aegyptius , Moraxella lacunata , Acinetobacter calcoaceticus and some Neisseria species.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING ZYLET (loteprednol etabonate and tobramycin ophthalmic suspension) 0.5%/0.3% is supplied in a white low density polyethylene plastic bottle with a white controlled drop tip and a white polypropylene cap in the following sizes: NDC 24208-358-05 5 mL fill in a 7.5 mL bottle NDC 24208-358-10 10 mL fill in a 10 mL bottle USE ONLY IF IMPRINTED NECKBAND IS INTACT. Storage: Store upright at 15ºC to 25ºC (59ºF to 77ºF). PROTECT FROM FREEZING.
SHAKE VIGOROUSLY BEFORE USING. After opening, ZYLET can be used until the expiration date on the bottle.
📋 Description ▾
11 DESCRIPTION ZYLET (loteprednol etabonate and tobramycin ophthalmic suspension) is a sterile, multiple dose topical anti-inflammatory corticosteroid and anti-infective combination for ophthalmic use. Both loteprednol etabonate and tobramycin are white to off-white powders. The chemical structures of loteprednol etabonate and tobramycin are shown below.
Loteprednol etabonate: Chemical name: chloromethyl 17α-[(ethoxycarbonyl)oxy]-11 β -hydroxy-3-oxoandrosta-1,4-diene-17 β -carboxylate Tobramycin: Chemical name: O-3-Amino-3-deoxy-α-D-glucopyranosyl-(1→4)-O-[2,6-diamino-2,3,6-trideoxy-α-D-ribo-hexopyranosyl-(1→6)]-2-deoxystreptamine Each mL contains : Actives: Loteprednol Etabonate 5 mg (0.5%) and Tobramycin 3 mg (0.3%). Inactives: Edetate Disodium, Glycerin, Povidone, Purified Water, Tyloxapol, and Benzalkonium Chloride 0.01% (preservative). Sulfuric Acid and/or Sodium Hydroxide may be added to adjust the pH to 5.5 to 6.2.
The suspension is essentially isotonic with a tonicity of 260 to 320 mOsm/kg. chemstructure1 image2
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Risk of Contamination This product is sterile when packaged. Advise patients not to allow the dropper tip to touch any surface, as this may contaminate the suspension. Risk of Secondary Infection Advise patients to consult a physician if pain develops, redness, itching or inflammation becomes aggravated.
Contact Lens Wear As with all ophthalmic preparations containing benzalkonium chloride, advise patients not to wear soft contact lenses when using ZYLET. Distributed by: Bausch & Lomb Americas Inc. Bridgewater, NJ 08807 USA Manufactured by: Bausch & Lomb Incorporated Tampa, FL 33637 USA ZYLET and LOTEMAX are trademarks of Bausch & Lomb Incorporated or its affiliates. © 2022 Bausch & Lomb Incorporated or its affiliates 9007709 (FOLDED) 9004409 (FLAT)