氯替泼诺混悬滴眼液(Lotemax)中文说明书

Loteprednol Suspension Eye Drops (Lotemax) are sterile, topical anti-inflammatory corticosteroids for ophthalmic use.

Loteprenol Suspension Eye Drops (Lotemax) Indications

Indicated for the treatment of steroid-sensitive inflammatory conditions of the eyelids and bulbar conjunctiva, cornea, and anterior segment of the globe, such as allergic conjunctivitis, rosacea, superficial punctate keratitis, herpetic keratitis, iritis, cyclitis, and selected infectious conjunctivitis when the inherent risks of steroid use are accepted to obtain desirable relief of edema and inflammation.

Loteprednol Suspension Eye Drops (Lotemax) Usage and Dosage

1. Treatment of steroid-sensitive diseases

Instill one to two drops of Loteprednol Suspension Eye Drops into the conjunctival sac of the affected eye four times a day. The dose can be gradually increased to one drop per hour during the first week as needed for treatment.

Care should be taken to avoid premature discontinuation of treatment, and patients should be re-evaluated if their signs and symptoms do not improve after two days.

2. Prevention and treatment of postoperative inflammation

Starting 24 hours after surgery, instill one to two drops of loteprednol suspension eye drops into the conjunctival sac of the operated eye four times a day and continue throughout the first two weeks of the postoperative period.

Loteprednol suspension eye drops are also suitable for the treatment of postoperative inflammation after eye surgery.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Contraindications of Loteprednol Suspension Eye Drops (Lotemax)

Like other ophthalmic corticosteroids, Loteprednol Suspension Eye Drops are contraindicated in most viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), cowpox and varicella, as well as mycobacterial infections of the eye and fungal diseases of the ocular structures.

Loteprednol Suspension Eye Drops are also contraindicated in individuals with known or suspected hypersensitivity to any component of this product or to other corticosteroids.

Precautions for Loteprednol Suspension Eye Drops (Lotemax)

1. Long-term use of corticosteroids may cause glaucoma, accompanied by optic nerve damage, vision and visual field defects, and posterior subcapsular cataract formation. Steroids should be used with caution in the presence of glaucoma.

Chronic use of corticosteroids may suppress the host response, thereby increasing the risk of secondary ocular infection. Perforation has been known to occur with the use of topical steroids in diseases that cause thinning of the cornea or sclera. In acute suppurative eye disease, steroids may mask infection or worsen existing infection.

2. The use of ocular steroids may prolong the course of the disease and may increase the severity of many viral ocular infections (including herpes simplex). Caution is required when using corticosteroid medications in patients with a history of herpes simplex.

3. The use of steroids after cataract surgery may delay healing and increase the incidence of follicle formation.

4. Loteprednol Suspension Eye Drops are for ophthalmic use only. Initial prescriptions and refills for more than 14 days should only be made by doctors after examining the patient with the help of magnifying equipment (such as slit lamp biomicroscopy and fluorescein staining when appropriate).

5. If signs and symptoms do not improve after two days, the patient should be re-evaluated.

6. If loteprednol suspension eye drops are used for 10 days or longer, intraocular pressure should be monitored, although this may be difficult in children and uncooperative patients.

7. Corneal fungal infection is particularly likely to occur simultaneously with long-term topical steroid use. Fungal attack must be considered in any case of persistent corneal ulceration in which steroids have been or are being used. Fungal culture should be performed when appropriate.

8. Patients should not wear soft contact lenses when using loteprednol suspension eye drops.

Loteprednol Suspension Eye Drops (Lotemax) Medication for Special Populations

1. Pregnancy

Teratogenic effects: Loteprednol tobramycin has been shown to be embryotoxic (delayed ossification) and teratogenic (increased incidence of meningocele, left common carotid artery abnormalities, and limb buckling) when administered orally to rabbits during organogenesis at 3 mg/kg/day (35 times the maximum daily clinical dose). This dose did not cause maternal toxicity.

2. Breastfeeding women

It is unknown whether topical ophthalmic administration of corticosteroids results in sufficient systemic absorption to produce detectable amounts in human milk. Systemic steroids are present in human milk and may inhibit growth, interfere with endogenous corticosteroids, or cause other adverse effects. Loteprednol Suspension Eye Drops should be used with caution in nursing mothers.

3. Pediatric use

The safety and effectiveness in pediatric patients have not been established.

Adverse Reactions to Loteprednol Suspension Eye Drops

Reactions associated with ophthalmic steroids include increased intraocular pressure (possibly related to optic nerve damage), visual acuity and visual field defects, posterior subcapsular cataract formation, secondary ocular infections from pathogens including herpes simplex, and globe perforation in the setting of corneal or scleral thinning.

In clinical studies, ocular adverse reactions that occurred in 5%-15% of patients treated with loteprednol tobramycin ophthalmic suspension (0.2%-0.5%) include: abnormal/blurred vision, burning sensation during instillation, bulbar conjunctival edema, discharge, dry eyes, epiphora, foreign body sensation, itching, congestion and photophobia.

Other ocular adverse reactions occurring in less than 5% of patients include conjunctivitis, corneal abnormalities, eyelid erythema, keratoconjunctivitis, ocular irritation/pain/discomfort, papillary protrusions, and uveitis. Some of these events were similar to the underlying eye disease being studied.

The incidence of non-ocular adverse reactions is less than 15%, including headache, rhinitis and pharyngitis.

Clinical Study of Loteprednol Suspension Eye Drops (Lotemax)

1. Postoperative Inflammation

Placebo-controlled clinical studies have proven that Loteprednol Suspension Eye Drops (Lotemax) is effective in treating anterior chamber inflammation (measured by aqueous humor cells and flare).

2. Giant papillary conjunctivitis

Placebo-controlled clinical studies have proven that loteprednol suspension eye drops can effectively reduce the signs and symptoms of giant papillary conjunctivitis after 1 week of treatment and continued treatment for up to 6 weeks.

3. Seasonal allergic conjunctivitis

A placebo-controlled clinical study demonstrated that loteprednol suspension eye drops (Lotemax) can effectively reduce the signs and symptoms of allergic conjunctivitis during peak pollen exposure periods.

Clinical Pharmacology of Loteprednol Suspension Eye Drops (Lotemax)

Corticosteroids suppress the inflammatory response to a variety of triggers and may delay or slow healing. They inhibit inflammation-related edema, fibrin deposition, telangiectasia, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scarring.

There is currently no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to work by inducing a phospholipase A2 inhibitory protein called lipocortin.

It is hypothesized that these proteins control the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Corticosteroids can cause an increase in intraocular pressure (IOP).

Loteprednol suspension eye drops were synthesized by structural modification of prednisolone-related compounds so that they undergo predictable conversion to inactive metabolites. Based on in vivo and in vitro preclinical metabolism studies, loteprednol tobramycin is extensively metabolized to inactive carboxylic acid metabolites.