Lotezar Eye Drops

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Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position Ketone group is absent. It is highly lipid soluble which enhances its penetration into cells. Loteprednol etabonate is synthesirized through structural modifications of prednisolone related compounds so that is will undergo a predictable transformation to an inactive metabolite. Based upon in vivo and in vitro preclinical metabolism studies, Loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites. Results from a bioavailability study in normal volunteers esstablished that plasma levels of Loteprednol etabonate and 1 cortienic acid Etabonate (PJ 91), its primary, inactive metabolite, were below the limit of quantitation (1 ng/rnI) at all sampling times. The results were obtained following the ocular administration of one drop in each eye of 0.5% Loteprednol etabonate 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 Loteprednol etabonate. 

INDICATIONS AND USAGE:

Loteprednol etabonate is indicated for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctive, Cornea and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitis, when the inherent hazard of steroid use is accepted to obtain an advisable diminution in edema and inflammation. Loteprednol etabonate is less effective than prednisolone acetate 1% in two 28 day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with Loteprednol etabonate experienced resolution of anterior chamber cells, compared to 87% of patients treated with prednisolone acetate 1%. The incidence of patients with clinically significant increases in 10P (' 10 mmHg) was 1% with Loteprednol etabonate and 6% with prednisolone acetate 1%. Loteprednol etabonate should not be used in patients who require a more potent corticosteroid for this indication, Loteprednol, Loteprednol etabonate is also indicated for the treatment of post operative inflammation following ocular surgery. 

CONTRAINDICATIONS:

Loteprednol etabonate as with other ophthalimic corticosteroids, is contraindicated is 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. Loteprednol etabonate is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

WARNINGS:

  Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision, and in posterior subcapsular cataract formation. Steroids should be used with caution in the presnce of glaucoma. Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infections. In those diseases causing thinning of the cornea or Sclera, perfoations have been known of occur with the use of topical steroids. In acute purulent conditions of the eye, steroids may mask infection or engance existing infection. Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infection of the eye (including herpes simplex). Employment of a codicosteroid medicatin in the treatment of patients with a history of herpes simplex requires great caution. The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. 

PRECAUTIONS:

General: for ophthalmic use only. The initial prescription and renewal of the medication order beyond 14 days should be made by a physician only after examination of the patient with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining. If signs and symptoms fail to improve after two days, the patient should be re-evaluated. If this product is used for 10 days or longer, intraocular pressure should be monitored even though it may be difficult in children and uncooperative patients. Fungal infections of the cornea are particularly prone to develop coincidentally with long term local steroid application. Fungus invasion must be considered any persistent corneal ulceration where a steroid has been used or is in use. Fungal cultures should be taken when appropriate. 

Information for Patients:

This product is sterile when packaged. Patients should be advised not to allow the dropper tip to touch any surface, as this may contaminate the suspension. If pain develops, redness, itching or inflamation becomes aggravated, the patient should be advised to consult a physician. As with all ophthalmic preparations containing benzalkonium chloride, patients should be advisedd not to wear soft contact lenses when using Loteprednol etabonate.

Pregnancy: Teratogenic effects:

Pregnancy Category C. Loteprednol etabonate has been shown to be embryotoxic (delayed ossification) and teratogenifc (increased incidence of meningocele, abnormal left common carotid artery, and limb flexures) when administered orally to rabbits during organogenesis at a dose of 3mg/kg/day (35 times the maximum daily clinical dose), a dose which caused no maternal toxicity. The no observed effect level (NOEL) for these effects was 0.5 mg/kg/day (6 times the maximum daily clinical dose). Oral treatment of rats during organogenesis resulted in teratogenicity (absent innominate artery at' 5mg/kg/day doses, and cleft palate and umbilical hernia at 50mg/kg/day) and ernbryotoxicity (increased post implantation losses at 100 mg/kg/day and decreased fetal body weight and skeletal ossification with 50 mg/kg/day). Treatment of rats with 0.5 mg/kg/day (6 times the maximum clinical dose) during organogenesis did not result in any reproductive toxicity.Loteprednol etabonate was maternally toxic (significanity reduced body weight gain during treatment) when administered to pregnant rats during organogenesis at doses of 5mg/kg/day. 

 ADVERSE REACTIONS:

Reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posteror subcapsular cataract formation, secondary ocular infection from pathogens includhing herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera. Ocular adverse reaction occuring in 5-15% of patients [rated with Loterprednol etabonate ophthalmic suspension (0.2% - 0.5%) in clinical included abnormafivision/ blurring, burning on installiation, chemosis, discharge, dry eyes, epiphora, foreigh body sensation, Itching, injection and photophobia. Other ocular adverse reactions occuring in less than 5% of patients include conjunctivites, corneal abnormalities, eyelid erythema, keratoconjunctivitis, ocularirritation/pain/discomfort, papillae, and uneitis. Some of these events were similar to the underifying ocular disease being studied. Non ocular adverse reaction occurred in less than 15% of patients. These include headache, rhinities and pharyngitis. In a summation of controllled, randomized studies of individuals treated for 28 days or longer with Loteprednol etabonate, the incidence of significant elevation of intraocular pressure )' 10 mmHg) 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 palcebo. 

DOSAGE AND ADMINISTRATION:

Shake well before use Steroid Responsive Disease Treatment: Apply one to two drops of LOTEZAR into the conjunctival sac of the affected eye(s) four times daily. During the initial treatment within the first week, the dosing may be increased, up to 1 drop every hour, if necessary. Care should be taken not to discontinue therapy prematurely. If signs and symptoms fail to improve after two days, the patient should be re evaluated. Post Operative Inflammation: Apply one to two drops of LOTEZAR into the conjunctival sac of the operated eye(s) four times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the post operative period. HOW SUPPLIED: LOTEZAR is available as a sterile suspension in 5 mL plastic dropper bottle Storage: Sotre in a cool & dark place. KEEP OUT OF REACH OF CHILDREN. 

A product of : 1 rizer IRIZER Laboratories India (P) Ltd. 478/22, A-Block Indira Nagar, Lucknow-226016