Document
DailyMed Label: PATANOL
Title
DailyMed Label: PATANOL
Date
2011
Document type
DailyMed Prescription
Name
PATANOL
Generic name
olopatadine hydrochloride
Manufacturer
Physicians Total Care, Inc.
Product information
NDC: 54868-4528
Product information
NDC: 54868-4528
Description
PATANOL® (olopatadine hydrochloride ophthalmic solution) 0.1% is
a sterile ophthalmic solution containing olopatadine, a relatively selective
H 1 -receptor antagonist and inhibitor of histamine release
from the mast cell for topical administration to the eyes. Olopatadine
hydrochloride is a white, crystalline, water-soluble powder with a molecular
weight of 373.88. The chemical structure is presented below:
Chemical
Name: 11-[(Z)-3-(Dimethylamino)propylidene]-6-11-dihydrodibenz[b,e]oxepin-2-acetic
acid hydrochloride.
Each mL of PATANOL contains: Active: 1.11 mg
olopatadine hydrochloride equivalent to 1 mg olopatadine. Preservative: benzalkonium chloride 0.01%. Inactives: dibasic sodium phosphate; sodium chloride;
hydrochloric acid/sodium hydroxide (adjust pH); and purified water. It has a pH
of approximately 7 and an osmolality of approximately 300 mOsm/kg.
imae of chemical structure
Indications
PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is
indicated for the treatment of the signs and symptoms of allergic
conjunctivitis.
Dosage
The recommended dose is one drop in each affected eye two times
per day at an interval of 6 to 8 hours.
Contraindications
PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is
contraindicated in persons with a known hypersensitivity to olopatadine
hydrochloride or any components of PATANOL.
Precautions
Information for Patients To prevent contaminating the dropper tip and solution, care
should be taken not to touch the eyelids or surrounding areas with the dropper
tip of the bottle. Keep bottle tightly closed when not in use.
Patients should be advised not to wear a contact lens if their eye is red.
PATANOL® should not be used to treat contact lens-related irritation. The
preservative in PATANOL, benzalkonium chloride, may be absorbed by soft contact
lenses. Patients who wear soft contact lenses and whose eyes
are not red should be instructed to wait at least ten minutes after
instilling PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% before
they insert their contact lenses.
Carcinogenesis, Mutagenesis, Impairment of
Fertility Olopatadine administered orally was not carcinogenic in mice and
rats in doses up to 500mg/kg/day and 200mg/kg/day, respectively. Based on a 40
µl drop size, these doses were 78,125 and 31,250 times higher than the maximum
recommended ocular human dose (MROHD). No mutagenic potential was observed when
olopatadine was tested in an in vitro bacterial
reverse mutation (Ames) test, an in vitro mammalian
chromosome aberration assay or an in vivo mouse
micronucleus test. Olopatadine administered to male and female rats at oral
doses of 62,500 times MROHD level resulted in a slight decrease in the fertility
index and reduced implantation rate; no effects on reproductive function were
observed at doses of 7,800 times the maximum recommended ocular human use
level.
Pregnancy
Pregnancy Category C. Olopatadine was
found not to be teratogenic in rats and rabbits. However, rats treated at 600
mg/kg/day, or 93,750 times the MROHD and rabbits treated at 400 mg/kg/day, or
62,500 times the MROHD, during organogenesis showed a decrease in live fetuses.
There are, however, no adequate and well-controlled studies in pregnant women.
Because animal studies are not always predictive of human responses, this drug
should be used in pregnant women only if the potential benefit to the mother
justifies the potential risk to the embryo or fetus.
Nursing Mothers Olopatadine has been identified in the milk of nursing rats
following oral administration. It is not known whether topical ocular
administration could result in sufficient systemic absorption to produce
detectable quantities in the human breast milk. Nevertheless, caution should be
exercised when PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is
administered to a nursing mother.
Pediatric Use Safety and effectiveness in pediatric patients below the age of 3
years have not been established.
Geriatric Use No overall differences in safety or effectiveness have been
observed between elderly and younger patients.
Adverse reactions
Headaches have been reported at an incidence of 7%. The following
adverse experiences have been reported in less than 5% of patients: asthenia,
blurred vision, burning or stinging, cold syndrome, dry eye, foreign body
sensation, hyperemia, hypersensitivity, keratitis, lid edema, nausea,
pharyngitis, pruritus, rhinitis, sinusitis, and taste perversion. Some of these
events were similar to the underlying disease being studied.
How supplied
PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is
supplied as follows: 5 mL in plastic DROP-TAINER® dispenser.
5 mL: NDC 54868-4528-0
Storage Store at 39°F-77°F (4°C-25°C).
Rx Only
U.S. Patent Nos. 4,871,865; 4,923,892; 5,116,863; 5,641,805.
© 2000, 2003, 2005 Alcon, Inc.
ALCON LABORATORIES, INC.
Fort Worth, Texas 76134
USA
Printed in USA
Relabeling of "Additional" label by:
Physicians Total Care, Inc. Tulsa, OK 74146
Clinical pharmacology
Olopatadine is an inhibitor of the release of histamine from the
mast cell and a relatively selective histamine H 1 -antagonist that inhibits the in vivo
and in vitro type 1 immediate hypersensitivity
reaction including inhibition of histamine induced effects on human conjunctival
epithelial cells. Olopatadine is devoid of effects on alpha-adrenergic,
dopamine, and muscarinic type 1 and 2 receptors. Following topical ocular
administration in man, olopatadine was shown to have low systemic exposure. Two
studies in normal volunteers (totaling 24 subjects) dosed bilaterally with
olopatadine 0.15% ophthalmic solution once every 12 hours for 2 weeks
demonstrated plasma concentrations to be generally below the quantitation limit
of the assay (<0.5 ng/mL). Samples in which olopatadine was quantifiable were
typically found within 2 hours of dosing and ranged from 0.5 to 1.3 ng/mL. The
half-life in plasma was approximately 3 hours, and elimination was predominantly
through renal excretion. Approximately 60-70% of the dose was recovered in the
urine as parent drug. Two metabolites, the mono-desmethyl and the N-oxide, were
detected at low concentrations in the urine.
Results from an environmental study demonstrated that PATANOL was effective
in the treatment of the signs and symptoms of allergic conjunctivitis when dosed
twice daily for up to 6 weeks. Results from conjunctival antigen challenge
studies demonstrated that PATANOL, when subjects were challenged with antigen
both initially and up to 8 hours after dosing, was significantly more effective
than its vehicle in preventing ocular itching associated with allergic
conjunctivitis.
Package label
PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1%
5 mL
NDC 54868-4528-0
image of package label
1 organization
2 products
Product
OlopatadineOrganization
Physicians Total Care, Inc.