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Unoprostone

Pronunciation

(yoo noe PROS tone)

Index Terms

  • Unoprostone Isopropyl

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as isopropyl ester:

Rescula: 0.15% (5 mL) [contains benzalkonium chloride, edetate disodium, polysorbate 80]

Brand Names: U.S.

  • Rescula

Pharmacologic Category

  • Docosanoid, Synthetic
  • Ophthalmic Agent, Antiglaucoma

Pharmacology

The exact mechanism of action is unknown; however, unoprostone likely decreases IOP by increasing the outflow of aqueous humor. Cardiovascular and pulmonary function were not affected in clinical studies. IOP was decreased by 3-4 mm Hg in patients with a mean baseline IOP of 23 mm Hg. IOP may also be lowered by increased trabecular meshwork outflow via stimulation of calcium-activated BK and CIC-2 type channels (Fung, 2014).

Absorption

Through cornea and conjunctival epithelium (minimal systemic exposure)

Metabolism

Hydrolyzed by esterases unoprostone-free acid

Excretion

Urine (as metabolites)

Half-Life Elimination

14 minutes

Use: Labeled Indications

To lower intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Contraindications

Hypersensitivity to unoprostone or any component of the formulation

Dosing: Adult

Open-angle glaucoma or ocular hypertension: Ophthalmic: Instill 1 drop into affected eye(s) twice daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling.

Administration

May be used with other eye drops to lower intraocular pressure; if using more than one product, wait at least 5 minutes between application of each medication. Remove contact lenses prior to administration and wait 15 minutes before reinserting. Minimize contamination by not touching the eyelids or surrounding areas with the dropper tip; keep bottle tightly closed when not in use.

Storage

Store between 2°C to 25°C (36°F to 77°F).

Drug Interactions

Nonsteroidal Anti-Inflammatory Agents: May diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents may also enhance the therapeutic effects of Prostaglandins (Ophthalmic). Monitor therapy

Adverse Reactions

>10%: Ophthalmic: Burning sensation of eyes (≤25%), stinging of eyes (≤25%), eye pruritus (10% to 25%), eye redness (10% to 25%), xerophthalmia (10% to 25%), increased eyelash length (10% to 14%; ≥1 mm at 12 months)

1% to 10%:

Cardiovascular: Hypertension

Central nervous system: Foreign body sensation of eye (5% to 10%), dizziness, headache, insomnia, pain

Endocrine & metabolic: Diabetes mellitus

Hypersensitivity: Hypersensitivity reaction

Neuromuscular & skeletal: Back pain

Ophthalmic: Abnormal lacrimation (5% to 10%), eyelid disease (5% to 10%), visual disturbance (5% to 10%), decreased eyelash length (7%), blepharitis, cataract, conjunctivitis, corneal lesion, eye discharge, eye irritation, eye pain, hemophthalmos, keratitis, photophobia, vitreous disorder

Respiratory: Flu-like symptoms (6%), bronchitis, cough, pharyngitis, rhinitis, sinusitis

Miscellaneous: Accidental injury

<1% (Limited to important or life-threatening): Blepharoptosis, color blindness, corneal deposits, corneal edema, corneal opacity, diplopia, hyperpigmentation of eyelids, increased growth in number of eyelashes, increased intraocular pressure (acute), iris hyperpigmentation, iritis, optic atrophy, retinal hemorrhage, visual field defect

Warnings/Precautions

Concerns related to adverse effects:

• Ocular pigmentation: May cause permanent change in eye color (increases the amount of brown pigment in the iris, may not be noticeable for months to years); long-term consequences and potential injury to eye are not known. May also cause pigment changes to periorbital tissues and eyelashes during use; reversible upon discontinuation in most patients.

• Infection: Bacterial keratitis, caused by inadvertent contamination of multiple-dose ophthalmic solutions, has been reported. Minimize contamination by not touching the eyelids or surrounding areas with the dropper tip; keep bottle tightly closed when not in use.

Disease-related concerns:

• Ocular disease: Use with caution in patients with intraocular inflammation (eg, uveitis); may exacerbate intraocular inflammatory conditions. May cause macular edema, including cystoid macular edema; use cautiously in aphakic patients, pseudophakic patients with torn posterior lens capsules, or in patients at risk for macular edema.

Special populations:

• Contact lens wearers: Contains benzalkonium chloride which may be adsorbed by contact lenses; remove contacts prior to administration and wait 15 minutes before reinserting.

Dosage form specific issues:

• Contains benzalkonium chloride 0.015% as a preservative.

Pregnancy Risk Factor

C

Pregnancy Considerations

In animal reproduction studies, adverse events were observed when administered subcutaneously at doses greater than the recommended human dose. Following ophthalmic administration, systemic absorption is minimal; systemic absorption would be required in order for unoprostone to cross the placenta and reach the fetus. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctual occlusion to decrease potential exposure to the fetus (Samples, 1988).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dry eyes, burning, stinging, eyelash growth, or eye discoloration. Have patient report immediately to prescriber sudden vision changes, eye pain, or severe eye irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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