Bausch & Lomb LACRISERT (hydroxypropyl cellulose ophthalmic insert) - Manual (Page 3)

STERILE OPTHALMIC INSERT
LACRISERT ®
(hydroxypropyl cellulose
ophthalmic insert)
DESCRIPTION
LACRISERT
® (hydroxypropyl cellulose ophthalmic insert) is a sterile, translucent,
rod-shaped, water soluble, ophthalmic insert made of hydroxypropyl cellulose, for
administration into the inferior cul-de-sac of the eye.
The chemical name for hydroxypropyl cellulose is cellulose, 2-hydroxypropyl ether. It is
an ether of cellulose in which hydroxypropyl groups (-CH
2
CHOHCH
3
) are attached to the
hydroxyls present in the anhydroglucose rings of cellulose by ether linkages. A represen-
tative structure of the monomer is:
The molecular weight is typically 1 × 10 6 .
Hydroxypropyl cellulose is an off-white, odorless, tasteless powder. It is soluble in water
below 38°C, and in many polar organic solvents such as ethanol, propylene glycol,
dioxane, methanol, isopropyl alcohol (95%), dimethyl sulfoxide, and dimethyl formamide.
Each LACRISERT is 5 mg of hydroxypropyl cellulose. LACRISERT contains no
preservatives or other ingredients. It is about 1.27 mm in diameter by about 3.5 mm long.
LACRISERT is supplied in packages of 60 units, together with illustrated instructions
and a special applicator for removing LACRISERT from the unit dose blister and inserting
it into the eye. A spare applicator is included in each package.
CLINICAL PHARMACOLOGY
Pharmacodynamics
LACRISERT acts to stabilize and thicken the precorneal tear film and prolong the tear
film breakup time which is usually accelerated in patients with dry eye states. LACRISERT
also acts to lubricate and protect the eye.
LACRISERT usually reduces the signs and symptoms resulting from moderate to severe
dry eye syndromes, such as conjunctival hyperemia, corneal and conjunctival staining
with rose bengal, exudation, itching, burning, foreign body sensation, smarting, photopho-
bia, dryness and blurred or cloudy vision. Progressive visual deterioration which occurs in
some patients may be retarded, halted, or sometimes reversed.
In a multicenter crossover study the 5 mg LACRISERT administered once a day during
the waking hours was compared to artificial tears used four or more times daily. There was
a prolongation of tear film breakup time and a decrease in foreign body sensation
associated with dry eye syndrome in patients during treatment with inserts as compared
to artificial tears; these findings were statistically significantly different between the
treatment groups. Improvement, as measured by amelioration of symptoms, by slit lamp
examination and by rose bengal staining of the cornea and conjunctiva, was greater in
most patients with moderate to severe symptoms during treatment with LACRISERT.
Patient comfort was usually better with LACRISERT than with artificial tears solution, and
most patients preferred LACRISERT.
In most patients treated with LACRISERT for over one year, improvement was observed
as evidenced by amelioration of symptoms generally associated with keratoconjunctivitis
sicca such as burning, tearing, foreign body sensation, itching, photophobia and blurred
or cloudy vision.
During studies in healthy volunteers, a thickened precorneal tear film was usually
observed through the slit-lamp while LACRISERT was present in the conjunctival sac.
Pharmacokinetics and Metabolism
Hydroxypropyl cellulose is a physiologically inert substance. In a study of rats fed
hydroxypropyl cellulose or unmodified cellulose at levels up to 5% of their diet, it was
found that the two were biologically equivalent in that neither was metabolized.
Studies conducted in rats fed 14 C-labeled hydroxypropyl cellulose demonstrated that
when orally administered, hydroxypropyl cellulose is not absorbed from the gastrointesti-
nal tract and is quantitatively excreted in the feces.
Dissolution studies in rabbits showed that hydroxypropyl cellulose inserts became softer
within 1 hour after they were placed in the conjunctival sac. Most of the inserts dissolved
completely in 14 to 18 hours; with a single exception, all had disappeared by 24 hours
after insertion. Similar dissolution of the inserts was observed during prolonged
administration (up to 54 weeks).
INDICATIONS AND USAGE
LACRISERT is indicated in patients with moderate to severe dry eye syndromes,
including keratoconjunctivitis sicca. LACRISERT is indicated especially in patients who
remain symptomatic after an adequate trial of therapy with artificial tear solutions.
LACRISERT is also indicated for patients with:
Exposure keratitis
Decreased corneal sensitivity
Recurrent corneal erosions
CONTRAINDICATIONS
LACRISERT is contraindicated in patients who are hypersensitive to hydroxypropyl
cellulose.
WARNINGS
Instructions for inserting and removing LACRISERT should be carefully followed.
PRECAUTIONS
General
If improperly placed, LACRISERT may result in corneal abrasion (see DOSAGE AND
ADMINISTRATION). Information for Patients
Patients should be advised to follow the instructions for using LACRISERT which
accompany the package.
Because this product may produce transient blurring of vision, patients should be
instructed to exercise caution when operating hazardous machinery or driving a motor
vehicle.
Drug Interactions
Application of hydroxypropyl cellulose ophthalmic inserts to the eyes of unanesthetized
rabbits immediately prior to or two hours before instilling pilocarpine, proparacaine HCl
(0.5%), or phenylephrine (5%) did not markedly alter the magnitude and/or duration of the
miotic, local corneal anesthetic, or mydriatic activity, respectively, of these agents. Under
various treatment schedules, the anti- inflammatory effect of ocularly instilled dexametha-
sone (0.1%) in unanesthetized rabbits with primary uveitis was not affected by the presence
of hydroxypropyl cellulose inserts.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Feeding of hydroxypropyl cellulose to rats at levels up to 5% of their diet produced no
gross or histopathologic changes or other deleterious effects.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and
younger patients.
ADVERSE REACTIONS
The following adverse reactions have been reported in patients treated with LACRISERT,
but were in most instances mild and transient:
Transient blurring of vision (See PRECAUTIONS)
Ocular discomfort or irritation
Matting or stickiness of eyelashes
Photophobia
Hypersensitivity
Edema of the eyelids
Hyperemia
DOSAGE AND ADMINISTRATION
One LACRISERT ophthalmic insert in each eye once daily is usually sufficient to relieve
the symptoms associated with moderate to severe dry eye syndromes. Individual patients
may require more flexibility in the use of LACRISERT; some patients may require twice daily
use for optimal results.
Clinical experience with LACRISERT indicates that in some patients several weeks may
be required before satisfactory improvement of symptoms is achieved.
LACRISERT is inserted into the inferior cul-de-sac of the eye beneath the base of the
tarsus, not in apposition to the cornea, nor beneath the eyelid at the level of the tarsal plate.
If not properly positioned, it will be expelled into the interpalpebral fissure, and may cause
symptoms of a foreign body. Illustrated instructions are included in each package. While in
the licensed practitioner’s office, the patient should read the instructions, then practice
insertion and removal of LACRISERT until proficiency is achieved.
NOTE: Occasionally LACRISERT is inadvertently expelled from the eye, especially in
patients with shallow conjunctival fornices. The patient should be cautioned against rubbing
the eye(s) containing LACRISERT, especially upon awakening, so as not to dislodge or
expel the insert. If required, another LACRISERT ophthalmic insert may be inserted. If
experience indicates that transient blurred vision develops in an individual patient, the
patient may want to remove LACRISERT a few hours after insertion to avoid this. Another
LACRISERT ophthalmic insert maybe inserted if needed.
If LACRISERT causes worsening of symptoms, the patient should be instructed to inspect
the conjunctival sac to make certain LACRISERT is in the proper location, deep in the
inferior cul-de-sac of the eye beneath the base of the tarsus. If these symptoms persist,
LACRISERT should be removed and the patient should contact the practitioner.
HOW SUPPLIED
LACRISERT, a sterile, translucent, rod-shaped, water-soluble, ophthalmic insert made of
hydroxypropyl cellulose, 5 mg, is supplied as follows:
NDC 25010-805-68 in packages containing 60 unit doses (each wrapped in an aluminum
blister), two reusable applicators, and a plastic storage container to store the applicators
after use.
Storage
Store below 30°C (86°F).
LACRISERT ® (hydroxypropyl cellulose ophthalmic insert)
Distributed by:
Bausch + Lomb, a division of
Valeant Pharmaceuticals North America LLC
Bridgewater, NJ 08807 USA
Manufactured by:
DPT Lakewood, Inc.
Lakewood, NJ 08701 USA
LACRISERT is a registered trademark of Valeant Pharmaceuticals International, Inc.
or its affiliates.
© Valeant Pharmaceuticals International, Inc.
All rights reserved.
9421400
Rev. 08/14