Professional Information
Unoprostone (Ophthalmic)
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VA CLASSIFICATION
Primary: OP119
Commonly used brand name(s): Rescula.
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).
Category:
Antiglaucoma agent (ophthalmic) —
antihypertensive, ocular—
Indications
Accepted
Glaucoma, open-angle (treatment) or
Hypertension, ocular (treatment)—Unoprostone is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma who are intolerant of or unresponsive to other agents.{01}
Pharmacology/Pharmacokinetics
Physicochemical characteristics:
Molecular weight—
424.62{01}
pH
5.0–6.5{01}
Mechanism of action/Effect:
Unoprostone decreases elevated intraocular pressure by increasing the outflow of aqueous humor, however the exact mechanism is unknown.{01}
Absorption:
Unoprostone is absorbed via the cornea and conjunctival epithelium. There is little systemic absorption of unoprostone.{01}
Biotransformation:
Unoprostone is hydrolyzed to unoprostone free acid via esterase activity in the cornea and conjunctival epithelium.{01}
Half-life:
Elimination:
14 minutes{01}
Elimination:
Predominately renal{01}
Precautions to Consider
Carcinogenicity
Unoprostone administered to male and female rats in doses of approximately 580 and 240 fold the recommended human dose, respectively, was not found to be carcinogenic over a two-year period.{01}
Mutagenicity
Unoprostone isopropyl and unoprostone free acid were not mutagenic in an Ames assay, nor were they clastogenic in a chromosome aberration assay in Chinese-hamster fibroblasts.{01} Unoprostone isopropyl was not genotoxic in a mouse lymphoma mutation assay or clastogenic in an in vivo chromosomal aberration test in mouse bone marrow.{01}
Pregnancy/Reproduction
Fertility—
Unoprostone did not impair fertility of male or female rats when given in doses up to 10,000 fold the recommended human dose.{01}
Pregnancy—
Adequate and well-controlled studies have not been performed in humans.{01}
Studies in rats showed an increase in miscarriages and a decrease in the live birth index when unoprostone was administered subcutaneously during organogenesis. Increases in miscarriages and resorptions and decrease in the number of live births were noted in rabbits given unoprostone subcutaneously during organogenesis. {01}
FDA Pregnancy Category C{01}
Breast-feeding
It is not known whether unoprostone is distributed into human breast milk. However, intravenous administration of unoprostone to rats has resulted in measurable breast milk concentrations. It is not known whether topical ocular administration will result in distribution into breast milk.{01}
Pediatrics
Appropriate studies on the relationship of age to the effects of unoprostone have not been performed in the pediatric population. Safety and efficacy have not been established.{01}
Geriatrics
Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of unoprostone in the elderly.{01}
Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).
Except under special circumstances, this medication should not be used when the following medical problem exists:
» Hypersensitivity to unoprostone isopropyl or benzalkonium chloride{01}
Risk-benefit should be considered when the following medical problems exist
Intraocular inflammation, active{01} (caution is recommended{01})
Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):
» Pigmentation changes (unoprostone may gradually and permanently affect eye pigmentation, increasing the amount of brown pigment in the iris; the long term consequences of this effect are unknown{01})
Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Those indicating need for medical attention
Incidence less frequent
Cataracts {01}(blurred vision or eye pain)
corneal lesion {01}(eye irritation or redness)
ocular hemorrhage {01}(blood in whites of the eye)
Incidence rare
Acute elevated intraocular pressure {01}(eye pain or blurred vision )
color blindness {01}
corneal deposits {01}(blurred vision)
corneal edema {01}(blurred vision; decreased vision)
optic atrophy {01}(blindness; blurred vision ; decreased vision; eye pain)
retinal hemorrhage {01}(decreased vision or other changes in vision)
{01}
Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
Abnormal vision
{01}
burning or stinging of eyes {01}
diplopia {01}(double vision)
dry eyes {01}
flu-like syndrome {01}(chills ; cough; diarrhea; fever ; general feeling of discomfort or illness; headache; joint pain; loss of appetite; muscle aches and pains; nausea; runny nose; shivering; sore throat; sweating; trouble sleeping; unusual tiredness or weakness; vomiting)
itching of eyes {01}
lacrimation disorder {01}(abnormal tearing of eyes)
{01}
Incidence less frequent or rare
Blepharitis or conjunctivitis {01}( redness, pain, swelling of eye, eyelid, or inner lining of eyelid; burning, dry or itching eyes; discharge; excessive tearing )
{01}
discharge from eye {01}
{01}
eye pain {01}
{01}
keratitis (irritation or inflammation of eye)
{01}
iritis {01}(sensitivity to light; tearing; throbbing pain)
{01}
Those not indicating need for medical attention
Incidence more frequent
Foreign body sensation (feeling of having something in the eye)
increased or decreased length of eyelashes {01}
{01}
Incidence less frequent or rare
Hyperpigmentation of iris or eyelid
{01}
increased number of eyelashes
{01}
photophobia {01}( difficulty seeing at night ; increased sensitivity of eyes to sunlight)
Note: Hyperpigmentation of the iris occurs slowly and may not be noticeable for months to several years.{01} This color change may be permanent.{01}
Overdose
For more information on the management of overdose or unintentional ingestion, contact a poison control center (see Poison Control Center Listing).
Treatment of overdose
There is no specific information regarding overdose with unoprostone. Treatment should be symptomatic and supportive.{01}
Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.
Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Unoprostone (Ophthalmic).
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):
Before using this medication
» Conditions affecting use, especially:
Hypersensitivity to unoprostone isopropyl or benzalkonium chloride{01}
Proper use of this medication
Proper administration technique for ophthalmic solution
Preventing contamination: Not touching applicator tip to any surface; keeping container tightly closed
» Importance of not using more medication than the amount prescribed
» Importance of removing contact lenses prior to administration of medication
Waiting 5 minutes between the use of 2 different ophthalmic preparations{01}
» Proper dosing
Using as soon as possible; not using if almost time for next scheduled dose; not doubling doses
Proper storage
Precautions while using this medication
» Regular visits to physician to check eye pressure during therapy
Checking with physician immediately if having ocular surgery, if trauma to the eye occurs, or an eye infection develops to determine if the present multidose container should continue to be used
» Caution when driving or using machinery because of possible blurred vision
Possible sensitivity of eyes to sunlight or bright light; wearing sunglasses and avoiding exposure to bright light
Side/adverse effects
Signs of potential side effects, especially cataracts, corneal lesion, ocular hemorrhage, acute elevated intraocular pressure, color blindness, corneal deposits, corneal edema, optic atrophy, and retinal hemorrhage
Hyperpigmentation of the iris or eyelid may occur; change in color of iris may not be noticeable for months to several years and may be permanent
General Dosing Information
Because the preservative, benzalkonium chloride, may be absorbed by contact lenses, it is recommended that they be removed prior to administration of unoprostone.{01} The lenses may be reinserted 15 minutes after administration of the medication. {01}
Unoprostone may be used concurrently with other medications instilled in the eye to lower intraocular pressure. However, the medications should be administered at least 5 minutes apart. {01}
Patients should be cautioned that permanent alterations in iris color are possible. These changes may be very gradual and occur over a period of several months to years{01}
Ophthalmic Dosage Forms
UNOPROSTONE ISOPROPYL OPHTHALMIC SOLUTION
Usual Adult Dose
Open-angle glaucoma or
Ocular hypertension
Topical to the conjunctiva, 1 drop in the affected eye(s) two times a day. {01}
Usual Pediatric Dose
Safety and efficacy have not been established. {01}
Usual Geriatric Dose
See Usual adult dose.
Strength(s) usually available
U.S.—
1.5 mg per 1 mL (Rx) [Rescula ( benzalkonium chloride 0.015%) (Edetate disodium ) (mannitol) (polysorbate 80) (sodium hydroxide or hydrochloric acid) (water for injection){01}]
Packaging and storage:
Store between 2 and 25 °C (36 and 77 °F){01}
Auxiliary labeling:
• For the eye.
Developed: 10/10/2000
References
- Product Information: Rescula©, unoprostone. CIBA Vision, Duluth, GA, PI reviewed 09/2000.
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