1. Name Of The Medicinal Product
Lotemax 0.5% Eye Drops, Suspension
2. Qualitative And Quantitative Composition
The suspension contains 0.5%w/v loteprednol etabonate (5 mg/ml).
Each drop contains 0.19 mg loteprednol etabonate.
Excipient: Benzalkonium Chloride (0.01%)
For a full list of excipients, see section 6.1.
3. Pharmaceutical Form
Eye-drops, suspension
Milky-white
4. Clinical Particulars
4.1 Therapeutic Indications
Treatment of post-operative inflammation following ocular surgery.
4.2 Posology And Method Of Administration
Adults and elderly
One to two drops four times daily beginning 24 hours after surgery and continuing throughout the post-operative period.
The duration of treatment should not exceed 2 weeks.
Children and adolescents
Lotemax should not be used in the paediatric age group until further data become available.
Shake the bottle vigorously before using the eye drops.
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. The bottle should be closed immediately after use.
4.3 Contraindications
Lotemax is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures; untreated purulent acute infections which, similar to other infectious diseases, can be masked and worsened by corticoids, 'red eye' with unknown diagnosis and infection caused by amoeba.
It is also contraindicated in hypersensitivity to the active substance, to any of the excipients, and to other corticosteroids.
4.4 Special Warnings And Precautions For Use
Prolonged use of corticosteroids may result in ocular hypertension or 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 presence of glaucoma.
Prolonged use of corticosteroids may suppress the host response and may increase the possibility of secondary ocular infections. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. In acute purulent conditions of the eye, steroids may mask infection or enhance existing infection. The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation.
Long term treating with corticosteroids can cause fungal disease. Fungal disease should be considered in the differential diagnosis when a corneal ulcer persists.
Lotemax contains benzalkonium chloride which may cause eye irritation.
In general patients should not wear contact lenses after cataract surgery, unless contact lens wearing is medically indicated.
Contact with soft contact lenses should be avoided. Patients should be advised to remove contact lenses prior to application and wait at least 15 minutes before reinsertion. Known to discolour soft contact lenses.
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.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Since loteprednol etabonate is not detected in plasma following the topical administration of Lotemax, it is not expected to affect the pharmacokinetics of systemically administered medicinal products. However, the low potential of ocular loteprednol etabonate eye drops to increase the intraocular pressure may be adversely affected by systemically administered medicinal products with anticholinergic activity. In patients receiving concomitant ocular hypotensive therapy, the addition of loteprednol etabonate may increase intraocular pressure and decrease the apparent ocular hypotensive effect of these medicinal products.
Concurrent administration of cycloplegics may increase the risk of raised intraocular pressure.
4.6 Pregnancy And Lactation
Pregnancy
For Lotemax no clinical data on exposed pregnancies are available. Studies in animals have shown reproductive toxicity (see section 5.3). The potential risk for humans is unknown and Lotemax should not be used in pregnancy unless clearly necessary.
Lactation
It is not known whether loteprednol etabonate is excreted in human milk. Excretion of loteprednol etabonate in breast milk has not been investigated in animal studies. Therefore, the use of loteprednol etabonate is contraindicated in lactating women.
4.7 Effects On Ability To Drive And Use Machines
No studies on the effects on the ability to drive and use machines have been performed.
If there are any transient effects on vision, the patient should be advised to wait until these subside before driving or operating machinery.
4.8 Undesirable Effects
Reactions associated with ophthalmic steroids include elevated intraocular pressure in steroid responsive patients, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.
Ocular adverse reactions occurring in patients treated with loteprednol etabonate ophthalmic suspension in clinical studies included the following:
All undesirable effects have been classified as follows very common (>1/10), common (>1/100, <1/10), uncommon (>1/1000, <1/100), rare (>1/10,000, <1/1000), or very rare (<1/10,000).
Eye Disorders
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In a summation of controlled, randomised studies of individuals treated for 28 days or longer with loteprednol etabonate, the incidence of significant elevation of intraocular pressure (
4.9 Overdose
No case of overdose has been reported. Acute overdosage is unlikely to occur via the ophthalmic route.
5. Pharmacological Properties
Pharmacotherapeutic group: Corticosteroid
ATC code: S01BA14
5.1 Pharmacodynamic Properties
Corticosteroids suppress the inflammatory response to inciting agents of mechanical, chemical or immunological nature. No generally accepted explanation of this steroid property has been advanced. Loteprednol etabonate is a new class of corticosteroid with potent antiinflammatory activity designed to be active at the site of action. Its antiinflammatory activity is similar to the most powerful steroid used in ophthalmology but with less intraocular pressure. Animal studies have shown that loteprednol etabonate has a binding affinity to steroid receptors that is 4.3 times greater than dexamethasone. This new class of steroids consists of bioactive molecules whose in-vivo transformation to non-toxic substances can be predicted from their chemistry and knowledge of enzymatic pathways in the body. Cortienic acid is an inactive metabolite of hydrocortisone and analogs of cortienic acid are also devoid of corticosteroid activity. Loteprednol etabonate is an ester derivative of one of these analogs, cortienic acid etabonate.
Placebo controlled studies demonstrated that Lotemax is significantly more effective than placebo for the treatment of external ocular inflammation.
Corticosteroids are capable of producing a rise in intraocular pressure in susceptible individuals. In a small study, Lotemax demonstrated a significantly longer time to produce a rise in pressure than did prednisolone acetate. The overall incidence of patients who had an intraocular pressure elevation of
5.2 Pharmacokinetic Properties
Results from oral and ocular administration of Lotemax in normal volunteers have shown that there are low or undetectable concentrations of either unchanged material or the metabolite. Results from a bioavailability study established that plasma concentrations of loteprednol etabonate following ocular administration of one drop in each eye of Lotemax eight times daily for 2 days or four times daily for 42 days were below the limit of quantitation (1 ng/mL) and detection (500 pg/mL) at all sampling times. In the same study, plasma cortisol concentrations were measured and no evidence of adrenal cortex suppression was observed. All cortisol measurements were within normal range. This study suggests that limited, if any, systemic absorption occurs with Lotemax.
5.3 Preclinical Safety Data
Preclinical data reveal no special hazard for humans based on conventional studies of repeated dose toxicity and genotoxicity.
Embryotoxicity and teratogenic effects were observed in reproductive toxicity studies in rabbits (delayed ossification, increased incidence of meningocele, abnormal left carotid artery and limb flexures) at oral doses 35 times the maximum daily clinical dose and in rats (decreased foetal body weight and skeletal ossification, absent innominate artery, cleft palate and umbilical hernia) at oral doses greater than 60 times the maximum daily clinical dose.
Mild ocular irritation was noted with both the acute and multidose rabbit ocular studies.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Disodium Edetate
Glycerol
Povidone
Purified Water
Tyloxapol
Hydrochloric Acid (pH adjuster)
Sodium Hydroxide (pH adjuster)
Benzalkonium Chloride
6.2 Incompatibilities
In the absence of incompatibility studies, this medicinal product should not be mixed with other medicinal products.
6.3 Shelf Life
2 years (unopened).
Discard any unused contents 28 days after first opening the bottle.
6.4 Special Precautions For Storage
Do not store above 25°C. Do not freeze.
6.5 Nature And Contents Of Container
Lotemax is available in the following packaging configurations:
2.5 mL and 5 mL supplied in a white low density polyethylene bottle (7.5 mL) with a white control drop tip and a pink polypropylene cap.
10 mL supplied in a white low density polyethylene bottle (10 mL) with a white control drop tip and a pink polypropylene cap.
6.6 Special Precautions For Disposal And Other Handling
Store the container in an upright position.
7. Marketing Authorisation Holder
Bausch & Lomb GmbH
Brunsbütteler Damm 165-173
13581 Berlin, Germany
8. Marketing Authorisation Number(S)
PL 17947/0001
9. Date Of First Authorisation/Renewal Of The Authorisation
31/03/2008
10. Date Of Revision Of The Text
31/03/2008
11. Legal Category
POM
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