Prednisolone-Moxiflo-Nepafenac - Drug Information

Overview

Moxifloxacin is a fluoroquinolone anti-infective agent.

Nepafenac is a prodrug of amfenac, a prototypical nonsteroidal anti-inflammatory agent (NSAIA) that also exhibits analgesic activity.

Prednisolone is a synthetic corticosteroid.

Moxifloxacin is a fluoroquinolone anti-infective agent. Like other commercially available fluoroquinolones, moxifloxacin contains a fluorine at the C-6 position of the quinolone nucleus. Moxifloxacin, like gatifloxacin, contains an 8-methoxy group and has been termed an 8-methoxy fluoroquinolone.

Like other fluoroquinolones, moxifloxacin inhibits DNA synthesis in susceptible organisms via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV).

Moxifloxacin is active in vitro and in vivo in conjunctival infections against some gram-positive bacteria, including Staphylococcus (S. aureus, S. arlettae, S. capitis, S. epidermidis, S. haemolyticus, S. hominis, S. saprophyticus, S. warneri ), Streptococcus (S. mitis, S. parasanguinis, S. pneumoniae, viridans streptococci ), Enterococcus faecalis, Aerococcus viridans, Corynebacterium (C. macginleyi), Micrococcus luteus, and Propionibacterium acnes.

Moxifloxacin also is active in vitro and in vivo in conjunctival infections against some gram-negative bacteria, including Acinetobacter lwoffii, Escherichia coli, Haemophilus influenzae, H. parainfluenzae, and Klebsiella pneumoniae. The drug also is active against Chlamydia trachomatis.

Cross-resistance can occur between moxifloxacin and other fluoroquinolones.

For the topical treatment of conjunctivitis caused by susceptible bacteria, moxifloxacin hydrochloride is commercially available as aqueous ophthalmic solutions containing 5 mg of moxifloxacin per mL. Moxifloxacin 0.5% ophthalmic solution (Moxeza(R)) is isotonic (osmolality of 300-370 mOsm/kg) and has a pH of approximately 7.4. Moxifloxacin 0.5% ophthalmic solution (Vigamox(R)) is isotonic (osmolality of 290 mOsm/kg) and has a pH of approximately 6.8.

Following topical application of moxifloxacin 0.5% ophthalmic solution to the eye, the drug is absorbed systemically and low moxifloxacin concentrations are attained in plasma. In a study in healthy adults using moxifloxacin 0.5% ophthalmic solution (Moxeza(R)), multiple, bilateral, topical ocular doses of the ophthalmic solution were applied twice daily for 4 days and resulted in peak plasma concentrations of moxifloxacin that were approximately 0.02% of those reported with usual dosages of oral moxifloxacin. In a study in healthy adults using moxifloxacin 0.5% ophthalmic solution (Vigamox(R)), bilateral topical doses of the ophthalmic solution were applied 3 times daily for 5 days and resulted in mean steady-state peak plasma concentrations and estimated daily exposure (determined by area under the plasma concentration-time curve (AUC)) 1600 and 1000 times lower, respectively, than values reported with usual dosages of oral moxifloxacin.

The half-life of systemically absorbed moxifloxacin is approximately 13 hours.

Nepafenac is a prodrug of amfenac, a prototypical nonsteroidal anti-inflammatory agent (NSAIA) that also exhibits analgesic activity. Following topical application to the eye, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, which inhibits the synthesis of prostaglandins by inhibiting cyclooxygenase (COX), including both COX-1 and COX-2 isoenzymes. The mechanism(s) of the ocular effects of NSAIAs appears to be associated principally with the inhibition of ocular prostaglandin synthesis.

By reducing ocular production of prostaglandins, NSAIAs can inhibit ocular inflammation and other reactions mediated primarily or secondarily by prostaglandins.

Generic name: prednisolone acetate/moxifloxacin HCl/nepafenac
Drug class: Ophthalmic Antibacterials
Therapeutic class: Ophthalmic Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

No indications are available for this drug.

Dosing

Moxifloxacin is commercially available for topical ophthalmic administration as moxifloxacin hydrochloride; dosage is expressed in terms of moxifloxacin.

The recommended dosage of nepafenac for the treatment of pain and inflammation associated with cataract surgery in adults and children 10 years of age or older is 1 drop of a 0.1% suspension in the affected eye(s) 3 times daily beginning one day prior to cataract surgery and continuing on the day of the surgery and for 2 weeks after surgery.

Potency of some sodium phosphate preparations is expressed in terms of prednisolone phosphate.

For use in the eye, 1 or 2 drops of prednisolone acetate ophthalmic suspension or prednisolone sodium phosphate ophthalmic solution may be instilled into the conjunctival sac every hour during the day and every 2 hours during the night for initial therapy in severe cases. In mild or moderate inflammation or when a favorable response is attained in severe cases, dosage may be reduced to 1 or 2 drops every 3-12 hours.

Alternatively, prednisolone sodium phosphate ophthalmic ointment may be instilled into the conjunctival sac 3 or 4 times daily initially, and once or twice daily thereafter. The ointment also may be used at night in conjunction with daytime use of a suspension or solution to reduce the frequent applications required with the liquid dosage forms.

The lowest effective concentration should be used and, if improvement does not occur within several days, the drug should be discontinued and other therapy begun. The duration of treatment depends on the type and severity of the disease and may range from a few days to several weeks; long-term therapy should be avoided. When the drug is discontinued, dosage should be gradually tapered to avoid exacerbation of the disease.

Drug interactions

No formal drug interaction studies have been performed using moxifloxacin 0.5% ophthalmic solution.

In vitro studies indicate that moxifloxacin does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, C19, 2D6, or 3A4; moxifloxacin is unlikely to alter the pharmacokinetics of drugs metabolized by these CYP isoenzymes.

Contraindications

Moxifloxacin 0.5% ophthalmic solution is contraindicated in patients with known hypersensitivity to moxifloxacin, other quinolones, or any component in the formulation.

Known hypersensitivity to nepafenac or any ingredient in the formulation or to other nonsteroidal anti-inflammatory agents (NSAIAs).

Adverse reactions

Moxifloxacin 0.5% ophthalmic solution (Moxeza(R)): Adverse effects reported in 1-2% of patients include eye irritation, pyrexia, and conjunctivitis.

Moxifloxacin 0.5% ophthalmic solution (Vigamox(R)): Adverse effects reported in approximately 1-6% of patients include conjunctivitis, decreased visual acuity, ocular dryness, keratitis, ocular discomfort/pain/pruritus, ocular hyperemia, subconjunctival hemorrhage, and tearing. Adverse systemic effects reported in approximately 1-4% of patients include fever, increased cough, infection, otitis media, pharyngitis, rash, and rhinitis.

Adverse effects reported in 1% or more of patients receiving nepafenac ophthalmic suspension include capsular opacity, decreased visual acuity, ocular foreign body sensation, increased intraocular pressure, ocular sticky sensation, conjunctival edema, corneal edema, dry eye, lid margin crusting, ocular discomfort, ocular hyperemia, ocular pain, ocular pruritus, photophobia, tearing, vitreous detachment, headache, hypertension, nausea, vomiting, and sinusitis.

Precautions

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ICD codes

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Formulary status

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Prednisolone-Moxiflo-Nepafenac (prednisolone acetate/moxifloxacin HCl/nepafenac)