bimatoprost (Rx)

>10%

Conjunctival hyperemia (25-45%)

Growth of eyelashes (15-45%)

Ocular pruritus (15-45%)

1-10%

Ocular dryness (3-10%)

Visual disturbance (3-10%)

Ocular burning (3-10%)

Foreign body sensation (3-10%)

Ocular pain (3-10%)

Pigmentation of the periocular skin (3-10%)

Blepharitis (3-10%)

Cataract (3-10%)

Superficial punctate keratitis (3-10%)

Eyelid erythema (3-10%)

Ocular irritation (3-10%)

Eyelash darkening (3-10%)

Ocular discharge (1-3%)

Tearing (1-3%)

Photophobia (1-3%)

Allergic conjunctivitis (1-3%)

Asthenopia (1-3%)

Increases in iris pigmentation (1-3%)

Conjunctival edema (1-3%)

Frequency Not Defined

Periorbital erythema

Eye swelling

Eyelids: burning sensation, edema, irritation, pruritus

Iris hyperpigmentation

Lacrimation increased

Madarosis and trichorrhexis

Periorbital and lid changes associated with a deepening of the eyelid sulcus

Rash (including macular, erythematous, and pruritic limited to the eyelids and periorbital region)

Skin discoloration (periorbital)

Blurred vision

Postmarketing Reports

Effects on intraocular pressure

Iris pigmentation

Lid pigmentation

Hair growth outside treatment area

Intraocular inflammation

Macular edema

Hypersensitivity

Hordeolum

Trichiasis

Asthma-like symptoms

Dizziness

Dyspnea

Eyelid edema

Hypersensitivity reaction including signs and symptoms of eye allergy and allergic dermatitis

Hypertension

Nausea

Contraindications

Hypersensitivity

Cautions

Macular edema, including cystoid macular edema, reported; the 0.01% strength should be used with caution in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema

Contains benzalkonium chloride, which may be absorbed by and cause discoloration of soft contact lenses

Prostaglandin analogs, including bimatoprost, reported to cause intraocular inflammation; because these products may exacerbate inflammation, use caution in patients with active intraocular inflammation

The 0.01% strength contains benzalkonium chloride, which may be absorbed by and cause discoloration of soft contact lenses; contact lenses should be removed prior to instillation and may be reinserted 15 minutes following administration

Bacterial keratitis reported; associated with use of multiple-dose containers of topical ophthalmic products; containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of ocular epithelial surface

May gradually change eyelashes and vellus hair in treated eye; these changes include increased length, thickness, and number of lashes; eyelash changes are usually reversible upon discontinuation of treatment

Not recommended for patients <16 years

Pigmentation

• Pigmentation change is due to increased melanin content in melanocytes rather than to increase in number of melanocytes
• After discontinuation of bimatoprost, pigmentation of iris is likely to be permanent, while pigmentation of periorbital tissue and eyelash changes have been reported to be reversible in some patients
• Patients who receive treatment should be informed of possibility of increased pigmentation
• While treatment with 0.01% can be continued in patients who develop noticeably increased iris pigmentation, these patients should be examined regularly

Pregnancy

There are no adequate and well-controlled studies in pregnant women; there is no increase in risk of major birth defects or miscarriages based on bimatoprost postmarketing experience; administered during pregnancy only if potential benefit justifies potential risk to fetus

Lactation

Not known whether topical ocular treatment with this product could result in sufficient systemic absorption to produce detectable quantities in human milk; the developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Prostaglandin analog; increases outflow of aqueous humor

Pharmacokinetics

Absorption: No significant systemic accumulation

Half Life: 45 min

Peak plasma time: ≤10 min

Onset of action: 4hr (IOP reduction)

Peak effect: 8-12hr

Protein binding: 88%

Vd: 0.67 L/kg

Metabolism: Oxydation; N-deethylation and glucoronidation

Excretion: Urine (67%); feces (25%)