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  • CLASSES

    Ocular Anti-Allergics, Antihistamines
    Topical Nasal Antiallergic Agents

    DEA CLASS

    Rx

    DESCRIPTION

    Antihistamine and mast cell stabilizer; marketed as ophthalmic solution for prevention of ocular pruritus due to allergic conjunctivitis and as nasal spray for seasonal allergic rhinitis.

    COMMON BRAND NAMES

    Pataday, Patanase, Patanol, Pazeo

    HOW SUPPLIED

    Olopatadine Hydrochloride/Pataday/Pazeo Ophthalmic Drops: 0.2%, 0.7%
    Olopatadine Hydrochloride/Patanase Nasal Spray Met: 1actuation, 665mcg
    Olopatadine Hydrochloride/Patanol Ophthalmic Sol: 0.1%

    DOSAGE & INDICATIONS

    For the treatment of the signs and symptoms of allergic conjunctivitis, including ocular pruritus.
    Ophthalmic dosage (Patanol 0.1%)
    Adults, Adolescents, and Children 3 years and older

    1 drop in each affected eye twice daily at an interval of 6 to 8 hours.

    Ophthalmic dosage (Pataday 0.2% and Pazeo 0.7%)
    Adults, Adolescents, and Children 2 years and older

    1 drop in each affected eye once a day.

    For the treatment of symptoms associated with seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus.
    Intranasal dosage
    Adults, Geriatric, Adolescents, and Children >= 12 years

    2 sprays (665 mcg/spray) in each nostril twice daily.

    Children 6—11 years

    1 spray (665 mcg/spray) in each nostril twice daily.

    Children 2—5 years†

    1 spray (665 mcg/spray) in each nostril twice daily has been evaluated in 66 children aged 2—5 years for safety; however, efficacy has not been established in this population.

    MAXIMUM DOSAGE

    Adults

    2 drops/day 0.1% ophthalmic solution in each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye; 4 nasal sprays/day in each nostril.

    Geriatric

    2 drops/day 0.1% ophthalmic solution in each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye; 4 nasal sprays/day in each nostril.

    Adolescents

    2 drops/day 0.1% ophthalmic solution each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye; 4 nasal sprays/day in each nostril.

    Children

    >= 12 years: 2 drops/day 0.1% ophthalmic solution each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye; 4 nasal sprays/day in each nostril.
    6—11 years: 2 drops/day 0.1% ophthalmic solution each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye; 2 nasal sprays/day in each nostril.
    3—5 years: 2 drops/day 0.1% ophthalmic solution in each affected eye; 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye. Safety and efficacy have not been established for the nasal spray; however, 2 nasal sprays/day in each nostril has been studied.
    2 years: 1 drop/day 0.2% or 0.7% ophthalmic solution in each affected eye. Safety and efficacy have not been established for the nasal spray; however, 2 nasal sprays/day in each nostril has been studied.
    < 2 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    No dosage adjustments are needed.

    Renal Impairment

    No dosage adjustments are needed.

    ADMINISTRATION

    Inhalation Administration
    Intranasal Inhalation Administration

    Before initial use, the unit must be primed. Pointed away from the body, pump the activator 5 times or until a fine mist appears. If the unit has not been used for 7 days, re-prime by pumping twice or until a fine mist appears.
    Instruct the patient on the proper use of olopatadine nasal spray (see Patient Information). Avoid spraying in the eyes.
    After administration, wipe the tip of the spray bottle with a clean tissue. Replace the cap.
    Discard after 240 sprays (enough for 30 days at the recommended dosage).
    To avoid the spread of infection, do not use the sprayer for more than one person.

    Ophthalmic Administration

    For topical application to the eye only.
    Take care to avoid contamination. Wash hands before and after use. Do not touch the tip of the dropper to the eye, fingertips, or other surface. Do not share ophthalmic drops between patients.
    Remove contact lenses before instilling drops. Instruct patients to wait at least ten minutes before reinserting contact lenses.
    For products supplied in an oval DROP-TAINER dispensers (Pataday and Pazeo):
    Remove cap. Hold bottle upside down between thumb and index finger.
    Tilt the head back slightly and pull the lower eyelid down with the index finger of the opposite hand to create a pocket between the eye and the lower eyelid. 
    With the bottle positioned above the eye, gently squeeze the side of the bottle to dispense 1 drop.
    Keep head tilted backwards and close eyes for 2 to 3 minutes while gently pressing index finger on the inside corner of the eye.
    For products supplied in a round DROP-TAINER dispensers (Patanol):.
    Remove cap. Hold bottle upside down between thumb and middle finger.
    Tilt the head back slightly and pull the lower eyelid down with the index finger of the opposite hand to create a pocket between the eye and the lower eyelid.
    With the bottle positioned above the eye, place the index finger on the bottom of the bottle and push to dispense 1 drop.
    Keep head tilted backwards and close eyes for 2 to 3 minutes while gently pressing index finger on the inside corner of the eye.

    STORAGE

    Pataday:
    - Store between 36 to 77 degrees F
    Patanase:
    - Discard 30 days after first use
    - Store between 39 to 77 degrees F
    Patanol:
    - Store between 39 to 77 degrees F
    Pazeo:
    - Store between 36 to 77 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    Contact lenses

    Olopatadine ophthalmic solution is formulated with the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Users of soft contact lenses should not administer olopatadine while wearing the lenses. Contact lenses may be inserted 10 minutes after instilling the drug. Do not use olopatadine to treat contact lens related ocular irritation. Avoid spraying olopatadine nasal spray in the eyes.

    Geriatric

    No overall differences in safety or effectiveness have been observed between the geriatric patients and younger patients receiving olopatadine ophthalmic solution (Patanol, Pataday) or olopatadine nasal spray; however, clinical studies have not included sufficient numbers of patients > 65 years of age to determine whether they respond differently than younger patients.

    Driving or operating machinery

    Somnolence has been reported in patients using olopatadine nasal spray. Caution should be used when driving or operating machinery or participating in any activities requiring mental alertness.

    Children, infants, neonates

    The safe and effective use of ophthalmic olopatadine and intranasal olopatadine has not been established in neonates, infants, or children below the age of 3 years and 6 years, respectively. Safety has been evaluated in children 2—5 years of age; however, efficacy has not been established in this population.

    Nasal septal perforation, nasal trauma

    Patients using olopatadine nasal spray have reported epistaxis, nasal ulceration, and nasal perforation. Examine nasal mucosa prior to initiating and periodically during olopatadine nasal spray therapy to ensure patients are free of pre-existing or drug-induced nasal trauma or nasal septal perforation. Use of povidone-free olopatadine nasal spray formulations (i.e., Patanase) may reduce the incidence of nasal septum perforation (see Adverse Reactions).

    Depression

    Depression and worsening of depression have been reported among patients using olopatadine nasal spray and nasal spray vehicle in a 12-month safety trial. Of an undisclosed number of studied patients 9 using olopatadine nasal spray reported depression symptoms; 3 patients were hospitalized. Five patients using the nasal spray vehicle reported the same, and none were hospitalized. Two of the 3 hospitalized olopatadine-using patients had a pre-existing history of depression. The likelihood of a drug-event relationship has not been released. Screen and monitor patients accordingly.

    Pregnancy

    Olopatadine is classified as FDA pregnancy risk category C. No adequate and well-controlled studies in pregnant women have been performed. The use of olopatadine in pregnant women is only justified if the benefits outweigh the possible risks to the fetus.

    Breast-feeding

    According to the manufacturer, caution is needed if olopatadine is administered to a breast-feeding woman. Olopatadine has been identified in the milk of nursing rats after oral dosing. Olopatadine via intranasal and ophthalmic administration typically results in low systemic concentrations; therefore, it is unlikely that nursing infants would be exposed to clinically significant amounts via breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Severe

    keratitis / Delayed / 0-5.0
    nasal septum perforation / Delayed / Incidence not known

    Moderate

    hyperemia / Delayed / 0-5.0
    conjunctivitis / Delayed / 0-5.0
    blurred vision / Early / 0-5.0
    wheezing / Rapid / 3.0-3.0
    depression / Delayed / 2.0-2.0

    Mild

    epistaxis / Delayed / 3.2-25.0
    dysgeusia / Early / 0-12.8
    pharyngitis / Delayed / 10.0-10.0
    diarrhea / Early / 0-9.1
    headache / Early / 4.4-7.0
    asthenia / Delayed / 0-5.0
    ocular pruritus / Rapid / 0-5.0
    ocular irritation / Rapid / 0-5.0
    xerophthalmia / Early / 0-5.0
    blepharedema / Early / 0-5.0
    foreign body sensation / Rapid / 0-5.0
    cough / Delayed / 1.4-5.0
    sinusitis / Delayed / 0-5.0
    rhinitis / Early / 0-5.0
    influenza / Delayed / 0.9-5.0
    nausea / Early / 0-5.0
    back pain / Delayed / 0-5.0
    rhinorrhea / Early / 4.5-4.5
    rash (unspecified) / Early / 1.3-1.3
    fever / Early / 1.3-1.3
    infection / Delayed / 1.2-1.2
    fatigue / Early / 0.9-0.9
    drowsiness / Early / 0.9-0.9
    xerostomia / Early / 0.9-0.9
    throat irritation / Early / 0.9-0.9
    anosmia / Delayed / Incidence not known

    DRUG INTERACTIONS

    Ethanol: (Moderate) Caution should be used when olopatadine nasal spray is used in combination with CNS depressants like ethanol. Patients should be advised to limit ethanol ingestion while taking olopatadine nasal spray; increased drowsiness may occur.

    PREGNANCY AND LACTATION

    Pregnancy

    Olopatadine is classified as FDA pregnancy risk category C. No adequate and well-controlled studies in pregnant women have been performed. The use of olopatadine in pregnant women is only justified if the benefits outweigh the possible risks to the fetus.

    According to the manufacturer, caution is needed if olopatadine is administered to a breast-feeding woman. Olopatadine has been identified in the milk of nursing rats after oral dosing. Olopatadine via intranasal and ophthalmic administration typically results in low systemic concentrations; therefore, it is unlikely that nursing infants would be exposed to clinically significant amounts via breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Mechanism of Action: Olopatadine exhibits two distinct mechanisms of action. It inhibits histamine release from mast cells and is a relatively selective antagonist of H1-receptors. As a result, olopatadine prevents type 1 immediate hypersensitivity reactions. Topical ocular administration relieves the ocular pruritus associated with allergic conjunctivitis. Intranasal administration relieves symptoms associated with seasonal allergic rhinitis. Olopatadine does not act upon alpha-adrenergic, dopaminergic, type 1 or type 2 muscarinic, or serotonergic receptors.

    PHARMACOKINETICS

    Olopatadine is administered topically to the eye or intranasally. Olopatadine exhibits moderate protein binding (approximately 55% in human serum) and is mainly bound to serum albumin. Olopatadine is not extensively metabolized. After oral administration, at least 6 minor metabolites are present in human plasma. Excretion is primarily renal with approximately 60—70% of a dose recovered in the urine. Of the recovered drug-related material within the first 24 hours, approximately 86% is unchanged olopatadine. The plasma elimination half-life of olopatadine is 8—12 hours. Olopatadine exhibits linear pharmacokinetics over a large dose range.

    Topical Route

    Following topical ocular administration, plasma concentrations of olopatadine were in the range of 0.5—1.3 ng/ml within 2 hours of dosing and were undetectable after 2 weeks of dosing in normal volunteers.

    Other Route(s)

    Intranasal Route
    After twice daily intranasal administration to adults, peak plasma concentrations (Cmax) were reached within 30—60 minutes. The mean steady-state Cmax was 16 +/- 8.99 ng/ml. The average absolute bioavailability of intranasal olopatadine is 57%.