Bimatoprost

Drug overview for BIMATOPROST (bimatoprost):

Generic name: BIMATOPROST (bye-MAT-oh-prost)
Drug class:
Therapeutic class: Dermatological

Bimatoprost, a synthetic prostaglandin analog, is an ocular hypotensive agent.

No enhanced Uses information available for this drug.

DRUG IMAGES

BIMATOPROST 0.03% EYELASH SOLN

The following indications for BIMATOPROST (bimatoprost) have been approved by the FDA:

Indications:
Hypotrichosis of eyelid lashes

Professional Synonyms:
None.

Dosing information for BIMATOPROST
DRUG LABEL	DOSING TYPE	DOSING INSTRUCTIONS
BIMATOPROST 0.03% EYELASH SOLN	Maintenance	Adults apply 1 drop to applicator and apply to upper eyelid, along eyelashes, by topical route once daily at nighttime

Generic dosing information for BIMATOPROST
DRUG LABEL	DOSING TYPE	DOSING INSTRUCTIONS
BIMATOPROST 0.03% EYELASH SOLN	Maintenance	Adults apply 1 drop to applicator and apply to upper eyelid, along eyelashes, by topical route once daily at nighttime

The following drug interaction information is available for BIMATOPROST (bimatoprost):

Contraindicated
Severe
Moderate

There are 0 contraindications.

There are 0 severe interactions.

There are 1 moderate interactions. The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.

Drug Interaction	Drug Names
IOP-Lowering Prostaglandin Analogs/Bimatoprost Topical SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: When used ophthalmically to lower intraocular pressure, prostaglandin analogs may be at the top of the dose-response curve. Use of an additional prostaglandin may result in decreased effectiveness.(1) CLINICAL EFFECTS: Concurrent use of topical bimatoprost may result in decreased effectiveness of ophthalmic prostaglandin analogs and an increase in intraocular pressure.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients using ophthalmic prostaglandin analogs to lower intraocular pressure should be monitored for changes in their intraocular pressure.(1) Use of topical bimatoprost may need to be discontinued in patients who stop responding to their ophthalmic prostaglandin analogue. DISCUSSION: Studies have shown that the ophthalmic administration of bimatoprost twice daily is less effective at lowering intraocular pressure than ophthalmic bimatoprost administered once daily. Concurrent use of topical bimatoprost may decrease the effectiveness of ophthalmic prostaglandin analogs.(1)	BIMATOPROST, DURYSTA, IDOSE TR, IYUZEH, LATANOPROST, LUMIGAN, ROCKLATAN, TAFLUPROST, TIMOLOL-BIMATOPROST, TIMOLOL-BRIMONI-DORZOL-BIMATOP, TIMOLOL-DORZOLAMIDE-BIMATOPRST, TRAVATAN Z, TRAVOPROST, VYZULTA, XALATAN, XELPROS, ZIOPTAN

Drug Interaction

Drug Names

IOP-Lowering Prostaglandin Analogs/Bimatoprost Topical

SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.

MECHANISM OF ACTION: When used ophthalmically to lower intraocular pressure, prostaglandin analogs may be at the top of the dose-response curve. Use of an additional prostaglandin may result in decreased effectiveness.(1)

CLINICAL EFFECTS: Concurrent use of topical bimatoprost may result in decreased effectiveness of ophthalmic prostaglandin analogs and an increase in intraocular pressure.(1)

PREDISPOSING FACTORS: None determined.

PATIENT MANAGEMENT: Patients using ophthalmic prostaglandin analogs to lower intraocular pressure should be monitored for changes in their intraocular pressure.(1) Use of topical bimatoprost may need to be discontinued in patients who stop responding to their ophthalmic prostaglandin analogue.

DISCUSSION: Studies have shown that the ophthalmic administration of bimatoprost twice daily is less effective at lowering intraocular pressure than ophthalmic bimatoprost administered once daily. Concurrent use of topical bimatoprost may decrease the effectiveness of ophthalmic prostaglandin analogs.(1)

BIMATOPROST, DURYSTA, IDOSE TR, IYUZEH, LATANOPROST, LUMIGAN, ROCKLATAN, TAFLUPROST, TIMOLOL-BIMATOPROST, TIMOLOL-BRIMONI-DORZOL-BIMATOP, TIMOLOL-DORZOLAMIDE-BIMATOPRST, TRAVATAN Z, TRAVOPROST, VYZULTA, XALATAN, XELPROS, ZIOPTAN

The following contraindication information is available for BIMATOPROST (bimatoprost):

Overview
Contraindicated
Severe
Moderate

Drug contraindication overview.

Bimatoprost is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.

There are 0 contraindications.

There are 2 severe contraindications. Adequate patient monitoring is recommended for safer drug use.

Severe List
Cystoid macular edema
Macular retinal edema

There are 4 moderate contraindications. Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.

Moderate List
Aphakia
Iritis
Pseudophakia
Uveitis

The following adverse reaction information is available for BIMATOPROST (bimatoprost):

Overview
Severe
Less Severe

Adverse reaction overview.

Conjunctival hyperemia, growth of eyelashes, and ocular pruritus occurred in approximately 15-45% of patients who received bimatoprost 0.03% ophthalmic solution for reduction of IOP in clinical trials. Approximately 3% of patients discontinued therapy because of conjunctival hyperemia.

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, and eyelash darkening have been reported in approximately 3-10% of patients who received bimatoprost 0.03% ophthalmic solution in clinical trials. Adverse ocular effects reported in approximately 1-3% of patients include ocular discharge, tearing, photophobia, allergic conjunctivitis, asthenopia, increases in iris pigmentation, and conjunctival edema.

Adverse systemic events reported in approximately 1-10% of patients include infection (primarily colds and upper respiratory tract infections), headache, abnormal liver function test results, asthenia, and hirsutism. Conjunctival hyperemia was reported in 31% of patients who received bimatoprost 0.01% ophthalmic solution for reduction of IOP in clinical trials.

Approximately 1.6% of patients discontinued therapy because of conjunctival hyperemia. Conjunctival edema, conjunctival hemorrhage, eye irritation, ocular pain, ocular pruritus, eyelid erythema, eyelid pruritus, growth of eyelashes, hypertrichosis, instillation site irritation, punctate keratitis, skin hyperpigmentation, blurred vision, and decreased visual acuity were reported in 1-4% of patients who received bimatoprost 0.01%

ophthalmic solution. The most common adverse reactions reported during clinical trials in patients receiving bimatoprost 0.03% ophthalmic solution applied to the skin of the upper eyelid margins to increase eyelash growth include ocular pruritus, conjunctival hyperemia, and skin hyperpigmentation, each reported in approximately 3-4% of patients. Ocular irritation, dry eye symptoms, periorbital erythema, foreign body sensation, abnormal hair growth, and iris hyperpigmentation also were reported.

There are 17 severe adverse reactions.

More Frequent	Less Frequent
None.	Cataracts Eyelid erythema Infection Ocular pain Punctate keratitis Visual changes

Rare/Very Rare
Abnormal hepatic function tests Allergic conjunctivitis Bacterial keratitis Chemosis Cystoid macular edema General weakness Hypersensitivity drug reaction Hypertension Iris hyperpigmentation Iritis Ocular inflammation

There are 29 less severe adverse reactions.

More Frequent	Less Frequent
Conjunctival hyperemia Dry eye Hirsutism Hyperpigmentation of eyelid Hypertrichosis of eyelid eyelashes Ocular irritation Ocular itching	Blepharitis Blurred vision Foreign body sensation of eye Headache disorder

Rare/Very Rare
Allergic dermatitis Asthenopia Blepharoptosis Deepening of upper eyelid sulcus Dizziness Dry skin Enophthalmos Eye tearing Eyelid edema Hordeolum Hypotrichosis of eyelid lashes Madarosis of eyelid Nausea Ocular discharge Periorbital edema Photophobia Trichiasis Trichorrhexis of eyelashes

The following precautions are available for BIMATOPROST (bimatoprost):

Pediatric
Pregnant
Lactation
Geriatric

Use of bimatoprost for the treatment of open-angle glaucoma or ocular hypertension in pediatric patients younger than 16 years of age is not recommended because of potential safety concerns related to increased pigmentation following long-term use. (See Pigmentation under Cautions: Warnings/Precautions.) In a randomized, double-blind, vehicle-controlled study in 71 pediatric patients 5-17 years of age with hypotrichosis, topical application of bimatoprost 0.03% to the upper eyelid margins once daily for 16 weeks was associated with improvement in overall eyelash prominence, as measured by an increase of at least one grade on the 4-point Global Eyelash Assessment (GEA) scale from baseline to week 16, in 73% of adolescents with hypotrichosis not associated with a contributory medical condition and 85 or 44% of pediatric patients with hypotrichosis caused by chemotherapy or associated with alopecia areata, respectively; response rates for vehicle recipients with these respective conditions were 7, 100, and 33%. No new safety concerns were identified in this study.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

In developmental studies in animals, bimatoprost exposure was compared with the human exposure following once-daily, bilateral, topical administration of bimatoprost 0.3% to the eyes (cornea or conjunctival sac). Abortion or early delivery was observed in mice and rats at exposure levels of at least 33 and 94 times human exposure but not at exposure levels of 2.6

and 47 times human exposure, respectively. Reduced gestation period, reduced fetal body weight, and increased fetal and pup mortality were observed in rats at exposures levels of at least 41 times human exposure. No adverse effects were observed in rat offspring at exposures estimated at 14 times human exposure.

There are no adequate and well-controlled studies using bimatoprost in pregnant women. Postmarketing experience has revealed no increase in the risk of major birth defects or spontaneous abortions. Bimatoprost should be used during pregnancy only if the potential benefits justify the possible risk to the fetus.

It is not known whether bimatoprost is distributed into human milk following topical application to the eye. Bimatoprost is distributed into milk in rats following IV administration at a dose equivalent to 324 times the recommended human ocular dose of bimatoprost 0.03%; animal data are lacking at clinically relevant doses. The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for bimatoprost and any potential adverse effects of the drug on the breast-fed infant.

No overall differences in safety and efficacy have been observed between geriatric patients and younger adults.

Hypotrichosis of eyelid lashes
H02.72	Madarosis of eyelid and periocular area
H02.721	Madarosis of right upper eyelid and periocular area
H02.722	Madarosis of right lower eyelid and periocular area
H02.723	Madarosis of right eye, unspecified eyelid and periocular area
H02.724	Madarosis of left upper eyelid and periocular area
H02.725	Madarosis of left lower eyelid and periocular area
H02.726	Madarosis of left eye, unspecified eyelid and periocular area
H02.729	Madarosis of unspecified eye, unspecified eyelid and periocular area