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Bimatoprost (Monograph)

Brand names: Latisse, Lumigan
Drug 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

Medically reviewed by Drugs.com on Jun 21, 2023. Written by ASHP.

Introduction

Ocular hypotensive agent; a synthetic prostaglandin analog.

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.

Bimatoprost 0.03% at least as effective as latanoprost 0.005% in controlling diurnal IOP; may be more effective than timolol 0.5% in reducing IOP in patients with open-angle glaucoma or ocular hypertension.

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). 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.

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.

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

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma. 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. Adjust target IOP up or down as needed over course of disease.

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

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.

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

Bimatoprost Dosage and Administration

Administration

Ophthalmic Administration

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

Remove contact lenses before administering each dose; may reinsert lenses 15 minutes after the dose. (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).

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

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

Hypotrichosis of Eyelashes

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

Face should be clean and makeup removed prior to application.

Apply evenly along the skin of the upper lid margin at the base of the lashes using a sterile applicator provided by the manufacturer. 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. (See Hair Growth Outside Treatment Area under Cautions.)

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

Avoid contamination of the applicator or solution container. (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. More frequent dosing will not result in greater increase in lash growth. Upon discontinuance of treatment, lash growth is expected to return to pretreatment levels.

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. More frequent dosing may paradoxically diminish the IOP-lowering effect of the drug.

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents. (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. More frequent dosing will not result in greater increase in lash growth. Upon discontinuance of treatment, lash growth is expected to return to pretreatment levels.

Special Populations

No special population dosage recommendations at this time.

Cautions for Bimatoprost

Contraindications

Warnings/Precautions

Pigmentation

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

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

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. Usually reversible upon discontinuance of therapy.

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.

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

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. 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.

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. 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.

Intraocular Inflammation

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

Macular Edema

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

Bacterial Keratitis

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

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

Specific Populations

Pregnancy

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

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

Lactation

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

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.

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. (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%. No new safety concerns identified.

Geriatric Use

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

Common Adverse Effects

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

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

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

Drug Interactions

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

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. Steady-state blood concentrations were achieved during the first week of dosing.

Onset

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

Distribution

Extent

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

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

Plasma Protein Binding

88%.

Elimination

Metabolism

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

Elimination Route

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

Half-life

45 minutes after IV administration.

Stability

Storage

Ophthalmic

Solution

15–25°C in the original container.

Actions

Advice to Patients

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 2024, Selected Revisions July 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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