Class: Prostaglandin Analogs
VA Class: OP109
Molecular Formula: C26H40O5
CAS Number: 130209-82-4
Ocular hypotensive agent; a synthetic analog of prostaglandin F2α (PGF2α).1 2 3 32 33
Uses for Latanoprost
Ocular Hypertension and Glaucoma
Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.1 3 10 11 12 13 15 30 31 32 33 48 55 60 One of several first-line agents to reduce elevated IOP.75
Safety and efficacy not established for the treatment of angle-closure, inflammatory, or neovascular glaucoma.1
Appears to be more effective than unoprostone, as effective as travoprost, and slightly less effective than bimatoprost in reducing IOP in patients with open-angle glaucoma or ocular hypertension.76 77 78 79 80 81
May be more effective or at least as effective as twice daily administration of timolol 0.5% in reducing IOP in patients with open-angle glaucoma or ocular hypertension.1 3 10 11 12 30 31 32 33 Appears to be more effective than thrice-daily administration of dorzolamide 2%.86 87
May be used in conjunction with a topical β-adrenergic blocking agent (e.g., betaxolol, carteolol, levobunolol, metipranolol, timolol),3 28 29 32 33 36 topical dipivefrin,33 59 topical epinephrine, an oral carbonic anhydrase inhibitor (e.g., acetazolamide), 33 or a topical carbonic anhydrase inhibitor (e.g., dorzolamide).1 44 56
Tolerance does not occur, and reduction in mean IOP is maintained for up to at least 24 months of therapy after initial stabilization.1 3 10 11 12 15 36 44 48
Latanoprost Dosage and Administration
Apply topically to the affected eye(s).1 10 11 12 32 33 36
Avoid contamination of the solution container.1
If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.1 (See Interactions.)
Ocular Hypertension and Glaucoma
One drop of a 0.005% solution (1.5 mcg) in the affected eye(s) once daily in the evening.1 10 11 12 32 33 36 More frequent dosing may paradoxically diminish the IOP-lowering effect of the drug.1 15 29 39 If a dose is missed, omit the dose and apply the next dose the following evening.15
Cautions for Latanoprost
Known hypersensitivity to latanoprost, benzalkonium chloride, or any ingredient in the formulation.1
Increases in brown pigmentation of the iris and periorbital tissue (eyelid) or increases in length, thickness, and pigmentation of eyelashes or vellus hair in the treated eye reported;1 3 10 11 12 15 31 32 33 36 misdirected growth of eyelashes also may occur.1 Pigmentation is expected to increase throughout the treatment period.1 Increased pigmentation of the iris may be permanent, while pigmentation of the periorbital tissue and eyelash changes reportedly are reversible in some patients.1 Long-term effects (i.e., beyond 5 years) of increased pigmentation are unknown.1
Increased pigmentation of iris develops slowly; may not be evident until after several months to years of latanoprost therapy.1 In clinical studies, noticeable increased pigmentation of the iris generally occurred within the first year of therapy.1 Therapy generally may be continued in the presence of increased iris pigmentation;1 patients should be examined regularly.1 33 36
Macular edema, including cystoid macular edema, reported in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema; use with caution in such patients.1 51 52 53 54 58 61 62 63 64 65
Use with caution in patients with a history of intraocular inflammation (e.g., iritis, uveitis); use generally not recommended in patients with active intraocular inflammation.1
Not known if distributed into milk; use with caution.1
Safety and efficacy not established in pediatric patients.1 15
No substantial differences in safety and efficacy relative to younger adults.1 10 11 12
Common Adverse Effects
Blurred vision, burning and stinging, conjunctival hyperemia, foreign body sensation, pruritus, increased pigmentation of the iris, punctate epithelial keratopathy.1
Interactions for Latanoprost
Ocular Hypotensive Agents
Potential for additive IOP-lowering effects when used concomitantly with another ocular hypotensive agent (e.g., topical β-adrenergic blocking agent, oral or topical carbonic anhydrase inhibitor).1 3 19 28 29 32 33 36 56 59 Additive effect may be used to therapeutic advantage.1 3 19 28 29 32 33 36
Precipitation occurs when ophthalmic solutions containing thimerosal are admixed with latanoprost ophthalmic solution.1 If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.1
Approximately 1% of a topically applied dose penetrates the human eye;15 remaining portion is absorbed into systemic circulation through blood vessels in the conjunctiva and mucous membranes of the nose, pharynx, esophagus, and GI tract.6 15
Prodrug; absorbed through the cornea following ocular instillation and rapidly hydrolyzed to active form (latanoprost acid).1 6 14 15 16 18 Peak plasma concentrations of latanoprost acid occur within 2 hours.1 15
Reduction in IOP generally occurs within 3–4 hours after topical application and peaks within 8–12 hours.
Effects on IOP generally persist for up to 24 hours or longer.1 10 11 12 13 15 17
Following long-term therapy (i.e., 6 months), pharmacologic effects may persist for at least 14 days after the drug is discontinued.15
The volume of distribution of latanoprost acid in humans following ocular or IV administration is 0.36 or 0.16 L/kg, respectively.1 15 Latanoprost acid can be measured in aqueous humor during the first 4 hours, and in plasma only during the first hour after ocular instillation.1
Not known whether the drug or its metabolites distribute into milk in humans.1
Rapidly hydrolyzed by esterases in the cornea and plasma to biologically active form (latanoprost acid).1 15 16 33
Systemically absorbed latanoprost acid is metabolized in the liver.1 15
Metabolites are excreted principally in urine; however, biliary excretion also may occur.1 6 15 Unchanged latanoprost or latanoprost acid generally are not recovered in urine or feces.15 Following topical administration of radiolabeled latanoprost to the eye, 88% of the dose was eliminated in urine.15
The elimination half-life of latanoprost acid from aqueous humor is approximately 3 hours.15
Following topical application to the eye, the plasma elimination half-life of latanoprost acid is approximately 17 minutes.15
Unopened bottles: refrigerate at 2–8°C and protect from light.1 15
Opened bottles: room temperature (not exceeding 25°C) for up to 6 weeks.1
Selective prostanoid agonist.1 2 3 5 6 7 8 9 33 40
Appears to reduce IOP by increasing uveoscleral outflow of aqueous humor.1 2 3 5 6 7 9 31 32 33
Advice to Patients
Risk of changes in eyelashes and permanent darkening of iris, eyelashes, or skin around the eyes associated with therapy.1 Potential for disparity between eyes if only one eye is treated.1 36
Importance of learning and adhering to proper administration techniques to avoid contamination of the solution with common bacteria that can cause ocular infections.1 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions.1
Importance of informing clinicians if intercurrent ocular condition (e.g., trauma, infection) develops or ocular surgery is planned.1 Importance of immediately reporting ocular reactions, particularly conjunctivitis and eyelid reactions.1
Importance of delaying insertion of contact lenses for at least 15 minutes after latanoprost instillation, since benzalkonium chloride preservative may be absorbed by soft lenses.1
Importance of administering different topical ophthalmic preparations at least 5 minutes apart.1
Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
Importance of women informing clinicians if they are or intend to become pregnant or plan to breast-feed.1
Importance of informing patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Xalatan (with benzalkonium chloride)
AHFS DI Essentials. © Copyright 2017, Selected Revisions July 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Pharmacia & Upjohn Inc. Xalatan (latanoprost) sterile ophthalmic solution 0.005% (50 mcg/mL) prescribing information. Kalamazoo, MI; 2003 Sep.
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88. Shin DH, McCracken MS, Bendel RE et al. The additive effect of latanoprost to maximum-tolerated medications with low-dose, high-dose, or no pilocarpine therapy. Ophthalmology. 1999; 106:386-90. [PubMed 9951495]
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