LATISSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LATISSE (LATISSE).
Bimatoprost is a synthetic prostamide analog that selectively mimics the effects of prostamide F2α. It increases the growth of eyelashes by prolonging the anagen (growth) phase and increasing the number of hairs. The exact molecular mechanism is thought to involve binding to prostamide receptors, leading to modulation of intracellular signaling pathways that regulate hair follicle cycling.
| Metabolism | Bimatoprost is primarily metabolized via reduction, hydrolysis, and glucuronidation. No specific CYP450 enzymes have been implicated. The main metabolic pathway involves reduction of the C-13 double bond and oxidation of the C-15 hydroxyl group. |
| Excretion | Primarily renal elimination of metabolites; less than 5% of unchanged bimatoprost is excreted in urine. Fecal excretion accounts for approximately 25% of the dose, predominantly as metabolites. Biliary excretion is minimal. |
| Half-life | The terminal elimination half-life of bimatoprost in plasma is approximately 45 minutes (range 30-60 minutes) after topical ocular application in humans. This short half-life reflects rapid systemic clearance, but the drug's ocular hypotensive effect persists for 24 hours due to tissue binding. |
| Protein binding | Approximately 88% bound to plasma proteins, primarily to albumin. |
| Volume of Distribution | Volume of distribution at steady state (Vss) is approximately 0.7 L/kg, suggesting distribution into total body water and some tissue binding. |
| Bioavailability | Bioavailability after topical ocular administration is approximately 0.03% of the administered dose, due to extensive ocular and systemic metabolism. The drug is not administered systemically; oral bioavailability is not clinically relevant. |
| Onset of Action | Onset of action for eyelash growth occurs within 4-8 weeks of daily topical application to the upper eyelid margin. For intraocular pressure reduction after ophthalmic instillation, onset is within 4 hours. |
| Duration of Action | Duration of action after topical application to the eyelid: effects on eyelash growth persist for several weeks to months after discontinuation, with gradual return to baseline. For intraocular pressure reduction, duration is at least 24 hours after a single dose. |
One drop applied to the upper eyelid margin at the base of the eyelashes once daily using the provided sterile applicators.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required in renal impairment. |
| Liver impairment | No dose adjustment required in hepatic impairment. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific geriatric dose adjustment; use same as adult dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LATISSE (LATISSE).
| Breastfeeding | Excretion in human milk unknown. Single-dose study in rats showed bimatoprost and/or its metabolites were excreted in milk. Due to potential for serious adverse reactions in nursing infants, discontinue nursing or discontinue drug, taking into account importance of drug to mother. M/P ratio not reported. |
| Teratogenic Risk | FDA Pregnancy Category C. No adequate and well-controlled studies in pregnant women. In animal studies, topical ocular administration of bimatoprost to pregnant rabbits and rats caused embryo-fetal toxicity at doses approximately 35-70 times the human exposure. There is a potential for preterm labor and low birth weight if systemically absorbed. Use only if potential benefit justifies risk to fetus. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to bimatoprost or any component of the formulation."]
| Precautions | ["May cause increased brown iris pigmentation, which is likely irreversible.","Potential for darkening of eyelid skin, which may be reversible upon discontinuation.","Possible hair growth outside the treatment area (e.g., on cheek) if solution contacts skin.","May cause eye irritation, redness, or pruritus.","Use with caution in patients with macular edema, ocular inflammation, or intraocular pressure changes.","Safety and efficacy in pediatric patients have not been established."] |
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| Fetal Monitoring | Monitor for increased intraocular pressure if used for glaucoma. For cosmetic use, monitor for local adverse effects (hyperemia, pruritus). No specific fetal monitoring required unless systemic absorption suspected. |
| Fertility Effects | In animal studies, bimatoprost had no effect on male or female fertility at doses up to 0.6 mg/kg/day in rats. No human data on fertility effects. |