Bimatoprost

Pronunciation

Class: Prostaglandin Analogs
VA Class: OP109
Chemical Name: (Z) - 7 - [(1R,2R,3R,5S) - 3,5,Dihydroxy - 2 - [1E,3S) - 3 - hydroxy - 5 - phenyl - 1 - pentenyl]cyclopentyl] - 5 - N - ethylheptenamide
Molecular Formula: C25H37NO4
Brands: Lumigan

Introduction

Ocular hypotensive agent; a synthetic prostaglandin analog.1

Uses for Bimatoprost

Ocular Hypertension and Glaucoma

Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension who are intolerant of other IOP-lowering drugs or who have not responded adequately (i.e., failed to achieve target IOP as determined after multiple measurements over time) to another IOP-lowering drug.1

Slideshow: Worried About Ebola? You’re More Likely to Get These 10 Serious Infections

Safety and efficacy not established for the treatment of angle-closure, inflammatory, or neovascular glaucoma.1

At least as effective as latanoprost 0.005% in controlling diurnal IOP;2 7 may be more effective than timolol 0.5% in reducing IOP in patients with open-angle glaucoma or ocular hypertension.2 5

Bimatoprost Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the affected eye(s).1

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

Dosage

Adults

Ocular Hypertension and Glaucoma
Ophthalmic

One drop of a 0.03% solution in the affected eye(s) once daily in the evening.1 More frequent dosing may paradoxically diminish the IOP-lowering effect of the drug.1

Cautions for Bimatoprost

Contraindications

  • Known hypersensitivity to bimatoprost or any ingredient in the formulation.1

Warnings/Precautions

Warnings

Ocular Effects

Increases in brown pigmentation of the iris and periorbital tissue (eyelid) or increases in length, thickness, number, and pigmentation of eyelashes reported;7 may be permanent.1

Increased pigmentation of iris develops slowly; may not be evident until after several months to years of bimatoprost therapy.1 Long-term effects of these changes are unknown.1 Patients should be examined regularly; therapy may be discontinued if increased pigmentation persists.1

General Precautions

Ocular Precautions

Macular edema, including cystoid macular edema, reported.1 Use with caution in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema.1

Use with caution in patients with active intraocular inflammation (e.g., uveitis).1

Specific Populations

Pregnancy

Category C.1

Lactation

Distributed into milk in animals.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established in children.1 7

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.1

Common Adverse Effects

Conjunctival hyperemia,1 2 growth of eyelashes,1 2 ocular pruritus,1 2 ocular dryness,1 2 visual disturbance,1 ocular burning,1 foreign body sensation,1 ocular pain,1 pigmentation of the periocular skin,1 blepharitis,1 cataract,1 superficial punctate keratitis,1 eyelid erythema,1 ocular irritation,1 eyelash darkening.1

Adverse systemic events include infection (primarily colds and upper respiratory tract infections).1

Interactions for Bimatoprost

No formal drug interaction studies have been performed.7 The manufacturer states that pharmacokinetic interactions are unlikely.7

Bimatoprost Pharmacokinetics

Absorption

Bioavailability

Following once-daily topical ocular administration for 2 weeks, peak blood concentrations were attained within 10 minutes and were below the lower limit of detection within 1.5 hours.1 Steady-state blood levels were achieved during the first week of dosing.1

Onset

Reduction in IOP generally occurs within 4 hours after topical application and peaks within 8–12 hours.1

Distribution

Extent

Moderately distributed into body tissues with a steady-state volume of distribution of 0.67 L/kg.1 In human blood, bimatoprost resides mainly in the plasma.1

Bimatoprost is distributed into milk in animals; it is not known whether the drug distributes into milk in humans.1

Plasma Protein Binding

88%.1

Elimination

Metabolism

Undergoes oxidation, N-deethylation, and glucuronidation to form various metabolites.1

Elimination Route

Approximately 67% excreted in urine and 25% excreted in feces after IV administration.1

Half-life

45 minutes after IV administration.1

Stability

Storage

Ophthalmic

Solution

15–25°C in the original container.1

Actions

  • Prostamide; a synthetic prostaglandin analog.1 2

  • Mimics the effects of endogenous prostamides and exhibits little or no pharmacologic activity at prostanoid receptors.1 3 4 7

  • Appears to reduce intraocular pressure (IOP) by facilitating outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes.1 6 7

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

  • 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 an 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 bimatoprost 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 as well as any concomitant illnesses.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.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Bimatoprost

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.03%

Lumigan (with benzalkonium chloride)

Allergan

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Latisse 0.03% Solution (ALLERGAN DERMATOLOGICS): 3/$115.99 or 9/$309.97

Lumigan 0.01% Solution (ALLERGAN): 3/$93.99 or 8/$257.96

Lumigan 0.01% Solution (ALLERGAN): 5/$198.00 or 15/$574.00

Lumigan 0.01% Solution (ALLERGAN): 8/$297.00 or 23/$860.99

Lumigan 0.03% Solution (ALLERGAN): 3/$99.99 or 8/$280.98

Lumigan 0.03% Solution (ALLERGAN): 5/$187.99 or 10/$361.98

Lumigan 0.03% Solution (ALLERGAN): 8/$287.98 or 23/$818.99

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Allergan, Inc. Lumigan (bimatoprost) ophthalmic solution 0.03% prescribing information. Irvine, CA; 2001 Mar.

2. Cantor LB. Bimatoprost: a member of a new class of agents, the prostamides, for glaucoma management. Expert Opin Investig Drugs. 2001; 10:721-31. [PubMed 11281821]

3. Woodward DF, Krauss AHP, Burk RM et al. Lumigan (AGN 192024): studies on a pharmacologically novel ocular hypotensive agent. Abstract presented at Third International Glaucoma Symposium. Prague, Czech Republic: 2001 Mar 21-5. From .

4. Krauss AHP, Chen J, Woodward DF. The pharmacology of AGN 192024 (Lumigan), a novel ocular hypotensive agent. Abstract presented at Third International Glaucoma Symposium. Prague, Czech Republic: 2001 Mar 21-5. From .

5. Sherwood M, Brandt J for the Bimatoprost Study Groups 1 and 2. Six-month comparison of bimatoprost once-daily and twice-daily with timolol twice-daily in patients with elevated intraocular pressure. Surv Ophthalmol. 2001; 45(Suppl):S361-8.

6. Brubaker RF, Schoff EO, Nau CB et al. Effects of AGN 192024, a new ocular hypotensive agent, on aqueous dynamics. Am J Opththalmol. 2001; 131:19-24.

7. Allergan, Irvine, CA: Personal communication.

a. Allergan, Inc. Lumigan (bimatoprost) ophthalmic solution 0.03% prescribing information. Irvine, CA; 2002 May.

Hide
(web4)