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Unoprostone

Medically reviewed by Drugs.com. Last updated on Oct 6, 2020.

Pronunciation

(yoo noe PROS tone)

Index Terms

  • Unoprostone Isopropyl

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Ophthalmic, as isopropyl ester:

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

Brand Names: U.S.

  • Rescula [DSC]

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

Open-angle glaucoma or ocular hypertension: 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.

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

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

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>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%, postmarketing, and/or case reports: 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 punctal occlusion to decrease potential exposure to the fetus (Samples, 1988).

Patient Education

What is this drug used for?

• It is used to treat glaucoma.

• It is used to lower high eye pressure.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dry eyes

• Burning

• Stinging

• Eyelash growth

• Flu-like symptoms

• Itching

• Foreign body sensation in eye

• Eye discoloration

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Vision changes

• Eye pain

• Eye discharge

• Sensitivity to light

• Severe eye irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.