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  • CLASSES

    Ocular Anti-Allergics, Antihistamines
    Topical Nasal Antiallergic Agents

    DEA CLASS

    Rx

    DESCRIPTION

    Ophthamic and nasal antihistamine (H1-blocker) and mast cell stabilizer
    Ophthalmic solution for prevention of ocular pruritus due to allergic conjunctivitis
    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 (0.1% solution)
    Adults

    1 drop in each affected eye(s) twice daily at an interval of 6 to 8 hours.[34128]

    Children and Adolescents 2 years and older

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

    Ophthalmic dosage (0.2% solution and 0.7% solution)
    Adults

    1 drop in each affected eye once a day.

    Children and Adolescents 2 years and older

    1 drop in each affected eye once a day.

    For the management of nasal symptoms of seasonal allergies and seasonal allergic rhinitis (e.g., rhinorrhea, sneezing, and nasal pruritus).
    Nasal dosage (nasal spray solution)
    Adults, Adolescents, and Children 12 years and older

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

    Children 6 to 11 years

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

    Children 2 to 5 years†

    1 spray (665 mcg/spray) in each nostril twice daily has been evaluated in 66 children aged 2 to 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 to 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.
    2 to 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.
    younger than 2 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    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

    To ensure the correct amount of medication is delivered, the unit must be primed before the initial use. 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. 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) have been used even though the bottle is not completely empty. The correct amount of medication cannot be assured after 240 sprays have been used.
    To avoid the spread of infection, do not use the sprayer for more than 1 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

    Safe and effective use of ophthalmic olopatadine and intranasal olopatadine has not been established in neonates, infants, or children younger than 2 years and 6 years, respectively.

    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. Consider stopping treatment if the drug recipient develops nasal ulcerations.

    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

    No adequate and well-controlled studies have been conducted to evaluate the use of olopatadine during human pregnancy; however, published data from postmarketing use of antihistamines with similar mechanisms of action to olopatadine have not identified a drug-associated risk for major birth defects, miscarriages, or adverse maternal or fetal outcomes. In animal studies, a decrease in the number of live fetuses was observed in rabbits and rats at oral olopatadine doses approximately 88- and 100-times the maximum recommended human dose (MRHD) or 1,460- and 110-times the maximum recommended human daily intranasal dose (MRHDID), respectively. Additionally, maternal and fetal toxicities were observed in rats at drug concentrations 1,080- to 14,400-times the maximum recommended human ophthalmic dose (MRHOD) or 110- to 1,100-times the MRHDID. The use of olopatadine in pregnant women is only justified if the benefits outweigh the possible risks to the fetus.

    Breast-feeding

    There are no data on the presence of olopatadine in human milk, the effects on a breastfed infant, or the effects on milk production. Also, it is not known whether intranasal or topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in the human breast milk; however, 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.[34127] [59359]

    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 / 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: (Major) Advise patients to avoid alcohol consumption while taking CNS depressants. Alcohol consumption may result in additive CNS depression.

    PREGNANCY AND LACTATION

    Pregnancy

    No adequate and well-controlled studies have been conducted to evaluate the use of olopatadine during human pregnancy; however, published data from postmarketing use of antihistamines with similar mechanisms of action to olopatadine have not identified a drug-associated risk for major birth defects, miscarriages, or adverse maternal or fetal outcomes. In animal studies, a decrease in the number of live fetuses was observed in rabbits and rats at oral olopatadine doses approximately 88- and 100-times the maximum recommended human dose (MRHD) or 1,460- and 110-times the maximum recommended human daily intranasal dose (MRHDID), respectively. Additionally, maternal and fetal toxicities were observed in rats at drug concentrations 1,080- to 14,400-times the maximum recommended human ophthalmic dose (MRHOD) or 110- to 1,100-times the MRHDID. The use of olopatadine in pregnant women is only justified if the benefits outweigh the possible risks to the fetus.

    There are no data on the presence of olopatadine in human milk, the effects on a breastfed infant, or the effects on milk production. Also, it is not known whether intranasal or topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in the human breast milk; however, 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.[34127] [59359]

    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%.