LUMIGAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LUMIGAN (LUMIGAN).
Bimatoprost is a prostamide analog that selectively mimics the effects of prostamide F2α, activating prostaglandin F (FP) receptors. It increases aqueous humor outflow through the uveoscleral pathway and may also enhance trabecular outflow, reducing intraocular pressure.
| Metabolism | Extensive metabolism in the eye via hydrolysis and oxidation; no systemic metabolism data available. |
| Excretion | Primarily via renal elimination (approximately 67% of administered dose excreted in urine as metabolites, with less than 1% as unchanged drug). The remainder is excreted in feces (approx. 25%) via biliary elimination. |
| Half-life | Terminal elimination half-life is approximately 78 minutes (range 54-102 minutes) in plasma after ocular administration. This short half-life reflects rapid systemic clearance, but ocular tissue levels persist longer due to local tissue binding. |
| Protein binding | Approximately 85% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is 0.14-0.21 L/kg, indicating distribution mainly into extracellular fluid and limited tissue penetration, consistent with its ocular target. |
| Bioavailability | Systemic bioavailability after topical ocular administration is very low, estimated at <1% of the administered dose due to extensive ocular uptake and local metabolism, with most of the drug remaining in the eye. |
| Onset of Action | Onset of intraocular pressure reduction occurs within 2-4 hours after topical ophthalmic administration; maximal effect is seen at 8-12 hours post-dose. |
| Duration of Action | Duration of intraocular pressure reduction is at least 24 hours, supporting once-daily dosing. Clinical effect persists for up to 24-36 hours after a single dose. |
One drop of 0.01% ophthalmic solution in the affected eye(s) once daily in the evening.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dosage adjustment recommended; use same dosing as adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LUMIGAN (LUMIGAN).
| Breastfeeding | It is not known whether bimatoprost is excreted in human milk after topical ocular administration. In animal studies, bimatoprost was detected in milk of lactating rats after oral administration. Because many drugs are excreted in human milk, caution should be exercised when LUMIGAN is administered to a nursing woman. The milk-to-plasma ratio is not known for humans. |
| Teratogenic Risk | LUMIGAN (bimatoprost ophthalmic solution) is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, bimatoprost administered intravenously during organogenesis resulted in abortion, reduced body weight, and increased pre- and post-implantation losses at doses >0.3 mg/kg/day (approximately 100 times the clinical exposure via ocular route). Systemic exposure from topical ocular use is minimal. Risk cannot be ruled out; use during pregnancy only if potential benefit justifies potential risk to the fetus. |
■ FDA Black Box Warning
None.
| Common Effects | Conjunctival hyperemia Eye itching |
| Serious Effects |
["Hypersensitivity to bimatoprost or any component of the formulation"]
| Precautions | ["Pigmentation changes: may cause increased brown iris pigmentation, eyelid skin darkening, and eyelash changes (length, thickness, color) which may be permanent.","Macular edema: use with caution in aphakic patients, pseudophakic patients with torn posterior lens capsule, or patients with known risk factors for macular edema.","Inflammation: use with caution in patients with active intraocular inflammation (e.g., uveitis) as it may exacerbate inflammation.","Potential for decreased intraocular pressure effect with prolonged use (tachyphylaxis).","Bacterial keratitis: avoid contamination of the dropper tip."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is routinely recommended beyond standard prenatal care. However, because systemic absorption is minimal, ocular side effects (e.g., conjunctival hyperemia, eye irritation) may occur. Monitor for intraocular pressure and eye infection as per standard ophthalmic practice. |
| Fertility Effects | In animal studies, no adverse effects on fertility were observed in male or female rats at oral doses up to 1 mg/kg/day (approximately 100 times the clinical exposure via ocular route). There are no human data on fertility effects from topical bimatoprost. Based on minimal systemic absorption, significant impact on human fertility is unlikely. |