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  • CLASSES

    Ophthalmological Non-steroidal Anti-inflammatories

    DEA CLASS

    Rx

    DESCRIPTION

    Ophthalmic NSAID
    Used for the treatment of pain and inflammation associated with cataract surgery
    May cause increased bleeding of ocular tissues when used in conjunction with ocular surgery

    COMMON BRAND NAMES

    ILEVRO, Nevanac

    HOW SUPPLIED

    ILEVRO/Nevanac Ophthalmic Susp: 0.1%, 0.3%

    DOSAGE & INDICATIONS

    For the treatment of ocular pain and postoperative ocular inflammation following cataract surgery.
    Ophthalmic dosage (0.1% ophthalmic suspension)
    Adults, Adolescents, and Children >= 10 years

    One drop into the affected eye(s) 3 times a day beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period.

    Ophthalmic dosage (0.3% ophthalmic suspension)
    Adults, Adolescents, and Children >= 10 years

    One drop into the affected eye(s) once daily beginning 1 day prior to cataract surgery and continued through the first 2 weeks of the postoperative period. On the day of surgery, 1 drop should be administered as usual with an additional drop administered 30—120 minutes prior to surgery.

    MAXIMUM DOSAGE

    Adults

    3 drops/day 0.1% ophthalmic suspension in each affected eye; 1 drop/day 0.3% ophthalmic suspension in each affected eye.

    Geriatric

    3 drops/day 0.1% ophthalmic suspension in each affected eye; 1 drop/day 0.3% ophthalmic suspension in each affected eye.

    Adolescents

    3 drops/day 0.1% ophthalmic suspension in each affected eye; 1 drop/day 0.3% ophthalmic suspension in each affected eye.

    Children

    >= 10 years: 3 drops/day 0.1% ophthalmic suspension in each affected eye; 1 drop/day 0.3% ophthalmic suspension in each affected eye.
    < 10 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

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Ophthalmic Administration

    For topical application to the eye only.
    If more than one medicine is to be administered in the eye, the medicines should be given 5 minutes apart.
    Instruct patients to remove contact lenses before instillation of the suspension and wait at least 5 minutes before reinsertion.
    Instruct patient on proper instillation of eye suspension (see Patient Information).

    STORAGE

    ILEVRO:
    - Protect from light
    - Store between 36 to 77 degrees F
    Nevanac:
    - Store between 36 to 77 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    NSAID hypersensitivity, salicylate hypersensitivity

    Nepafenac ophthalmic suspension is contraindicated in patients with NSAID hypersensitivity. Use caution when administering nepafenac to patients who have previously exhibited sensitivities to phenylacetic acid derivatives and salicylate hypersensitivity as the potential for cross-sensitivity exists.

    Anticoagulant therapy, coagulopathy, diabetes mellitus, hemophilia, ocular disease, ocular surgery, rheumatoid arthritis

    Nepafenac should be used with caution in patients who are receiving other medications that may prolong bleeding time (e.g., anticoagulant therapy), and in patients with known bleeding tendencies, preexisting coagulopathy, or hemophilia. Like other NSAIDs, nepafenac can prolong bleeding time. There have been reports that ocularly applied NSAIDs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular procedures. Post-marketing experience with ophthalmic NSAIDs suggests that patients with complicated ocular surgery, diabetes mellitus, ocular disease affecting the ocular surface (e.g., xerophthalmia, corneal denervation, or corneal epithelial defects), rheumatoid arthritis, or repeat ocular surgeries within a short period of time may be at increased risk for corneal adverse events that are potentially sight-threatening. Ocular NSAIDs should be used with caution in these patients. Post-marketing experience also suggests that nepafenac use more than 24 hours prior to or use beyond 14 days following ocular surgery may increase risk for the occurrence and severity of corneal adverse events.

    Children, infants, neonates

    The safety and efficacy of nepafenac ophthalmic suspension has not been established for neonates, infants and children < 10 years old.

    Pregnancy

    Nepafenac ophthalmic suspension is classified as an FDA pregnancy risk category C drug. No adequate and well-controlled studies in pregnant women have been performed. The use of nepafenac in pregnant women is only justified if the benefits outweigh the possible risks to the fetus. Because of the possibility of closure of the ductus arteriosus, the use of nepafenac ophthalmic suspension should be avoided in late pregnancy.

    Breast-feeding

    According to the manufacturer, caution should be exercised if nepafenac ophthalmic solution is given to a woman who is breast-feeding. It is not known whether nepafenac is excreted in human milk. Systemic concentrations are low after ophthalmic use ; therefore, breast milk concentrations are likely to be very low, if present at all. Although nepafenac has not been evaluated by the American Academy of Pediatrics (AAP), other NSAIDs such as ibuprofen, indomethacin, and naproxen are considered to be usually compatible with breast-feeding by the AAP. 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 ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    Asthma

    Systemic absorption of ophthalmic NSAIDs through the nasal mucosa has been reported to cause exacerbation of bronchial asthma in at least three patients. Two of the three patients had a previous history of mild to moderate asthma. The third patient experienced acute asthma attacks following each administration of the ophthalmic NSAID. The attacks ceased following discontinuation of the drug and reappeared following re-challenge with the drug. It may be prudent to avoid administration of nepafenac ophthalmic suspension in asthmatic patients until further information is known.

    Contact lenses

    Patients need to remove contact lenses before administering nepafenac ophthalmic suspension (Nevanac). Nepafenac ophthalmic suspension contains the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Also, contact lens removal is needed for drug penetration into the eye. Patients should wait approximately 5 minutes after nepafenac administration before reinserting contact lenses.

    ADVERSE REACTIONS

    Moderate

    hypertension / Early / 1.0-4.0

    Mild

    vomiting / Early / 1.0-4.0
    headache / Early / 1.0-4.0
    sinusitis / Delayed / 1.0-4.0
    nausea / Early / 1.0-4.0

    DRUG INTERACTIONS

    There are no drug interactions associated with Nepafenac products.

    PREGNANCY AND LACTATION

    Pregnancy

    Nepafenac ophthalmic suspension is classified as an FDA pregnancy risk category C drug. No adequate and well-controlled studies in pregnant women have been performed. The use of nepafenac in pregnant women is only justified if the benefits outweigh the possible risks to the fetus. Because of the possibility of closure of the ductus arteriosus, the use of nepafenac ophthalmic suspension should be avoided in late pregnancy.

    According to the manufacturer, caution should be exercised if nepafenac ophthalmic solution is given to a woman who is breast-feeding. It is not known whether nepafenac is excreted in human milk. Systemic concentrations are low after ophthalmic use ; therefore, breast milk concentrations are likely to be very low, if present at all. Although nepafenac has not been evaluated by the American Academy of Pediatrics (AAP), other NSAIDs such as ibuprofen, indomethacin, and naproxen are considered to be usually compatible with breast-feeding by the AAP. 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 ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Mechanism of Action: Following ophthalmic administration, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug (NSAID). The anti-inflammatory and analgesic properties of amfenac are mediated through inhibition of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production. The prostaglandins play a role in the miotic response produced during and after ocular surgery by constricting the iris sphincter independently of cholinergic mechanisms. In the eye, prostaglandins also have been shown to disrupt the blood-aqueous humor barrier, cause vasodilation, increase vascular permeability, promote leukocytosis, and increase intraocular pressure (IOP). The degree of ocular inflammatory response is correlated with prostaglandin-induced increases in ciliary epithelium permeability. With ophthalmic administration, NSAIDs inhibit the synthesis of prostaglandins in the iris, ciliary body, and conjunctiva, and, thus, work to prevent manifestations of ocular inflammation and reduce pain.The pro-drug structure of nepafenac allows for rapid penetration to the cornea and distribution to target sites, while minimizing surface accumulation and reducing ocular surface complications. While not an FDA-approved indication, topical nepafenac appears to inhibit choroidal neovascularization (CNV) and ischemia-induced retinal neovascularization by decreasing production of vascular endothelial growth factor (VEGF).

    PHARMACOKINETICS

    Nepafenac is administered topically to the eye. The clinical significance of the systemic absorption of nepafenac after ophthalmic administration is unknown.

    Other Route(s)

    Ophthalmic Route
    The pro-drug structure allows nepafenac to rapidly penetrate the cornea and reach its target sites, while minimizing surface accumulation and reducing ocular surface complications. Two to three hours after bilateral 0.1% nepafenac ophthalmic administration, given three times daily, low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects. Following ocular administration, the mean steady-state Cmax for nepafenac and for amfenac were 0.310 +/- 0.104 ng/ml and 0.422 +/- 0.121 ng/ml, respectively. The clinical significance of the systemic absorption of nepafenac after ophthalmic administration is unknown.