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Bimatoprost

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: Latisse, Lumigan

Medically reviewed by Drugs.com. Last updated on June 22, 2020.

Introduction

Ocular hypotensive agent; a synthetic prostaglandin analog.1

Uses for Bimatoprost

Ocular Hypertension and Glaucoma

Bimatoprost 0.01 or 0.03% ophthalmic solution (Lumigan or generic formulations, respectively): Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.1 8

Bimatoprost 0.03% 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

When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost).130 132 With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.130 131

A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.130 131 132 134

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.130 132

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma.130 131 Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal.130 131 132 Adjust target IOP up or down as needed over course of disease.130 131 132

Combination therapy with drugs from different therapeutic classes often required to control IOP.131 133

Hypotrichosis of Eyelashes

Bimatoprost 0.03% ophthalmic solution (Latisse): Used to increase eyelash growth, including lash length, thickness, and darkness, in individuals with hypotrichosis of the eyelashes.9

Effect on lash growth is expected to abate following discontinuance of therapy.9

Bimatoprost Dosage and Administration

Administration

Ophthalmic Administration

For reduction of elevated IOP, apply topically to the affected eye(s).1 8 To increase eyelash growth, apply topically to the skin of the upper eyelash line.9

Remove contact lenses before administering each dose; may reinsert lenses 15 minutes after the dose.1 8 9 (See Use with Contact Lenses under Cautions.)

Ocular Hypertension and Glaucoma

Apply topically to the affected eye(s) as a 0.01 or 0.03% ophthalmic solution (Lumigan or generic formulations, respectively).1 8

Avoid contamination of the solution container.1 (See Bacterial Keratitis under Cautions.)

If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.1 8

Hypotrichosis of Eyelashes

Apply topically to the skin of the upper eyelash line as a 0.03% ophthalmic solution (Latisse).9 Do not apply to the lower lash line.9

Face should be clean and makeup removed prior to application.9

Apply evenly along the skin of the upper lid margin at the base of the lashes using a sterile applicator provided by the manufacturer.9 The upper lid margin in the area of lash growth should feel lightly moist without runoff; blot any excess runoff outside the upper lid margin with a tissue or absorbent cloth.9 (See Hair Growth Outside Treatment Area under Cautions.)

Use a new applicator for each eyelid; discard applicator after one use.9 Do not use other brushes or applicators.9

Avoid contamination of the applicator or solution container.9 (See Bacterial Keratitis under Cautions.)

Dosage

Pediatric Patients

Hypotrichosis of Eyelashes
Ophthalmic

Bimatoprost 0.03% ophthalmic solution (Latisse): One drop applied to the skin of the upper eyelash line of each eye once daily in the evening.9 More frequent dosing will not result in greater increase in lash growth.9 Upon discontinuance of treatment, lash growth is expected to return to pretreatment levels.9

Adults

Ocular Hypertension and Glaucoma
Ophthalmic

Bimatoprost 0.01 or 0.03% ophthalmic solution (Lumigan or generic formulations, respectively): One drop in the affected eye(s) once daily in the evening.1 8 More frequent dosing may paradoxically diminish the IOP-lowering effect of the drug.1

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents.130 131 133 (See Ocular Hypertension and Glaucoma under Uses and also see Concurrent Use of Multiple Prostaglandin Analog Formulations under Cautions.)

Hypotrichosis of Eyelashes
Ophthalmic

Bimatoprost 0.03% ophthalmic solution (Latisse): One drop applied to the skin of the upper eyelash line of each eye once daily in the evening.9 More frequent dosing will not result in greater increase in lash growth.9 Upon discontinuance of treatment, lash growth is expected to return to pretreatment levels.9

Special Populations

No special population dosage recommendations at this time.1 8 9

Cautions for Bimatoprost

Contraindications

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

Warnings/Precautions

Pigmentation

Increased pigmentation of the iris and periorbital tissue (eyelid) reported.1 7 Pigmentation expected to increase as long as bimatoprost is administered.1 Following discontinuance of therapy, pigmentation of the iris is likely to be permanent, while pigmentation of periorbital tissue reportedly is reversible in some patients.1 Long-term effects of increased pigmentation unknown.1

Increased pigmentation of the iris may not be evident until after several months to years of bimatoprost therapy.1 May continue therapy in patients who develop noticeably increased iris pigmentation; however, examine these patients regularly.1

Eyelash Changes

Possible gradual change in eyelashes and vellus hair in the treated eye, including increased length, thickness, pigmentation, and number of eyelashes and/or misdirected growth of eyelashes.1 7 Usually reversible upon discontinuance of therapy.1

Concurrent Use of Multiple Prostaglandin Analog Formulations

Studies in patients with open-angle glaucoma or ocular hypertension indicate that administering bimatoprost or other prostaglandin analogs more than once daily may paradoxically reduce the IOP-lowering effect of the drug.1 9

In studies in patients with eyelash hypotrichosis, bimatoprost reduced IOP, although not to a clinically important extent, in patients with or without elevated IOP.9

In patients receiving prostaglandin analogs, including bimatoprost (e.g., Lumigan 0.01%, generic bimatoprost 0.03%), for reduction of elevated IOP, concomitant use of bimatoprost (Latisse) for treatment of eyelash hypotrichosis may interfere with achieving the desired IOP reduction.9 Patients receiving prostaglandin analogs for IOP reduction should receive bimatoprost (Latisse) for treatment of eyelash hypotrichosis only after consultation with their clinician and with monitoring for changes in IOP.9

Hair Growth Outside Treatment Area

In patients receiving bimatoprost for treatment of eyelash hypotrichosis, hair growth may occur in areas where the drug solution comes in repeated contact with the skin.9 Apply bimatoprost only to the skin of the upper eyelid margin at the base of the lashes; carefully blot any excess solution from the eyelid margin to avoid runoff onto the cheek or other skin areas.9

Intraocular Inflammation

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

Macular Edema

Macular edema, including cystoid macular edema, reported in patients receiving bimatoprost for reduction of elevated IOP.1 9 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 9

Bacterial Keratitis

Bacterial keratitis reported with use of multiple-dose containers of topical ophthalmic preparations.1 Containers were inadvertently contaminated by patients, most of whom had concurrent corneal disease or disruption of the ocular epithelial surface.1

Improper handling of ophthalmic solutions can result in contamination of the solution by common bacteria known to cause ocular infections.1 Reuse of the sterile, disposable, single-use applicators provided with Latisse ophthalmic solution also increases the potential for contamination and infection.9 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions or applicators.1 9 (See Advice to Patients.)

Use with Contact Lenses

Remove contact lenses prior to topical application of each dose to the eyes or eyelid margins, since the preparations contain benzalkonium chloride, which may be absorbed by and cause discoloration of soft contact lenses; may reinsert lenses 15 minutes after the dose.1 8 9

Specific Populations

Pregnancy

In animal studies, abortion, early delivery, reduced fetal body weight, and increased fetal and pup mortality observed at high exposure levels.1 9

No adequate and well-controlled studies in pregnant women.1 9 Postmarketing experience has revealed no increase in risk of major birth defects or spontaneous abortions.1 9 Use only if the potential benefits justify possible risk to the fetus.1 9

Lactation

Distributed into milk in animals following high-dose IV administration; animal data lacking at clinically relevant doses.1 8 Not known whether bimatoprost distributes into human milk after topical application to the eye.1

Consider developmental and health benefits of breast-feeding along with the mother's clinical need for bimatoprost and any potential adverse effects of the drug on the breast-fed infant.1 8 9

Pediatric Use

Not recommended for treatment of open-angle glaucoma or ocular hypertension in pediatric patients <16 years of age because of potential safety concerns related to increased pigmentation following long-term use.1 (See Pigmentation under Cautions.)

In a controlled study in 71 pediatric patients 5–17 years of age, improvement in overall eyelash prominence was observed with bimatoprost 0.03% therapy in 73% of adolescents with hypotrichosis not associated with a contributory medical condition and 85 or 44% of pediatric patients with hypotrichosis associated with chemotherapy or alopecia areata; response rates for vehicle recipients with these respective conditions were 7, 100, and 33%.9 10 No new safety concerns identified.9 10

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.1 9

Common Adverse Effects

Bimatoprost 0.03% for reduction of IOP: Conjunctival hyperemia,2 8 growth of eyelashes,2 8 ocular pruritus,2 8 ocular dryness,2 8 visual disturbance,8 ocular burning,8 foreign body sensation,8 ocular pain,8 pigmentation of the periocular skin,8 blepharitis,8 cataract,1 8 superficial punctate keratitis,8 periorbital erythema,8 ocular irritation,8 eyelash darkening.8 Adverse systemic events include infection (primarily colds and upper respiratory tract infections).8

Bimatoprost 0.01% for reduction of IOP: Conjunctival hyperemia, lid erythema, ocular irritation, eyelash growth, conjunctival hemorrhage, blurred vision.1 12

Bimatoprost 0.03% for eyelash hypotrichosis: Ocular pruritus, conjunctival hyperemia, skin hyperpigmentation.9

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 application of bimatoprost 0.03% ophthalmic solution to the eyes (cornea and/or conjunctival sac) 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 concentrations were achieved during the first week of dosing.1

Onset

Reduction in IOP generally occurs within 4 hours after topical application to the eyes 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 IOP by facilitating outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes.1 6 7

  • Appears to increase eyelash growth by increasing the proportion of hairs in, and the duration of, the anagen (growth) phase.9

Advice to Patients

  • Importance of not exceeding once-daily dosing; more frequent administration may paradoxically decrease IOP-lowering effect of bimatoprost.1

  • Inform patients using prostaglandin analogs (e.g., bimatoprost) to reduce elevated IOP that concomitant use of bimatoprost (Latisse) to increase eyelash growth may interfere with achieving the desired reduction in IOP; advise patients receiving prostaglandin analogs for reduction of elevated IOP that they should initiate such concomitant therapy only after consulting their clinician.9

  • Risk of permanent increase in brown pigmentation of the iris; risk of darkening of the eyelid, which may be reversible after discontinuance of bimatoprost.1 9

  • Risk of changes in eyelashes and vellus hair in the treated eye.1 9 Potential for disparity between the eyes in length, thickness, pigmentation, and number of eyelashes or vellus hairs and/or direction of eyelash growth.1 9 Eyelash changes usually are reversible after discontinuance of bimatoprost.1 9

  • In patients receiving bimatoprost to increase eyelash growth, importance of reading the manufacturer's information for patients and following directions for proper administration.9 Importance of applying bimatoprost only to the skin of the upper eyelid margin at the base of the lashes and not to the lower eyelash line.9 Potential for hair growth to occur outside the target treatment area if the drug solution repeatedly contacts the same skin area.9 Importance of blotting any excess solution outside the upper eyelid margin to avoid runoff.9

  • Advise patients receiving bimatoprost to increase eyelash growth that the onset of effect is gradual and desired results may not be evident for several months.9 Importance of not exceeding once-daily application since more frequent use will not result in greater eyelash growth.9 The effect on lash growth is not permanent and is expected to abate following discontinuance of therapy.9

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the solution or applicator with common bacteria that can cause ocular infections.1 9 Instruct patients that neither applicators nor the tip of the dispensing container should touch the eye or surrounding structures, fingers, or any other surface.1 9 Applicators are for single use only (application of solution to a single eyelid margin) and may become contaminated if reused.9 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions or applicators.1 9

  • Advise patients to immediately contact their clinician for advice regarding continued use of bimatoprost if a new ocular condition (e.g., trauma, infection), ocular reaction (particularly conjunctivitis and eyelid reactions), or sudden decrease in visual acuity occurs or if ocular surgery is planned.1 9

  • If using more than one topical ophthalmic preparation, importance of administering the preparations at least 5 minutes apart.1

  • Advise patients receiving bimatoprost to increase eyelash growth that the drug may lower IOP, although not to a level that will cause clinical harm.9 If the ophthalmic solution inadvertently gets in the eye, harm is not expected; do not rinse the eye.9

  • Importance of removing contact lenses prior to topical application of each bimatoprost dose to the eyes or upper eyelid margins and delaying reinsertion for at least 15 minutes after the dose, since benzalkonium chloride preservative may be absorbed by and cause discoloration of soft lenses.1 8 9

  • 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 plan 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.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Bimatoprost

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.01%

Lumigan

Allergan

0.03%*

Bimatoprost Ophthalmic Solution

Latisse (with sterile disposable applicators)

Allergan

AHFS DI Essentials™. © Copyright 2021, Selected Revisions July 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Allergan, Inc. Lumigan (bimatoprost) ophthalmic solution 0.01% prescribing information. Irvine, CA; 2017 Jul.

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. http://www.ncbi.nlm.nih.gov/pubmed/11281821?dopt=AbstractPlus

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 http://www.kenes.com/glaucoma2001/.

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 http://www.kenes.com/glaucoma2001/.

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.

8. Apotex. Bimatoprost ophthalmic solution 0.03% prescribing information. Weston, FL; 2018 Feb.

9. Allergan. Latisse (bimatoprost) ophthalmic solution 0.03% prescribing information. Irvine, CA; 2017 Jul.

10. Borchert M, Bruce S, Wirta D et al. An evaluation of the safety and efficacy of bimatoprost for eyelash growth in pediatric subjects. Clin Ophthalmol. 2016; 10:419-29. http://www.ncbi.nlm.nih.gov/pubmed/27022239?dopt=AbstractPlus

11. Smith S, Fagien S, Whitcup SM et al. Eyelash growth in subjects treated with bimatoprost: a multicenter, randomized, double-masked, vehicle-controlled, parallel-group study. J Am Acad Dermatol. 2012; 66:801-6. http://www.ncbi.nlm.nih.gov/pubmed/21899919?dopt=AbstractPlus

12. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number: 022184Orig1s000. Medical review(s). From FDA website. Accessed 2019 Nov 14. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022184Orig1s000MedR.pdf

130. Prum BE Jr, Rosenberg LF, Gedde SJ et al. Primary open-angle glaucoma preferred practice pattern guideline [published corrigendum appears in Ophthalmology. 2018; 125: 949]. San Francisco, CA: American Academy of Ophthalmology; 2015. From the American Academy of Ophthalmology website. https://www.aao.org/preferred-practice-pattern/primary-open-angle-glaucoma-ppp-2015

131. Liebmann JM, Lee JK. Current therapeutic options and treatments in development for the management of primary open-angle glaucoma. Am J Manag Care. 2017; 23(15 Suppl):S279-S292. http://www.ncbi.nlm.nih.gov/pubmed/29164845?dopt=AbstractPlus

132. Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma: a review. JAMA. 2014; 311:1901-11. http://www.ncbi.nlm.nih.gov/pubmed/24825645?dopt=AbstractPlus

133. Gupta D, Chen PP. Glaucoma. Am Fam Physician. 2016; 93:668-74. http://www.ncbi.nlm.nih.gov/pubmed/27175839?dopt=AbstractPlus

134. Inoue K. Managing adverse effects of glaucoma medications. Clin Ophthalmol. 2014; 8:903-13. http://www.ncbi.nlm.nih.gov/pubmed/24872675?dopt=AbstractPlus