LATANOPROSTENE BUNOD
Clinical safety rating: safe
No significant drug interactions Can cause increased pigmentation of the iris and eyelashes.
Latanoprostene bunod is a nitric oxide (NO)-donating prostaglandin F2α analog. It is hydrolyzed by esterases in the eye to latanoprost acid and nitric oxide. Latanoprost acid increases uveoscleral outflow of aqueous humor via FP receptor agonism, while NO enhances trabecular meshwork outflow via soluble guanylate cyclase activation.
| Metabolism | Latanoprostene bunod is rapidly hydrolyzed by esterases in the eye and plasma to its active metabolites, latanoprost acid and nitric oxide. Latanoprost acid is further metabolized via beta-oxidation in the liver. Systemic metabolism is minimal due to low systemic absorption. |
| Excretion | The primary route of elimination is via the kidneys, with approximately 88% of the dose excreted in urine as metabolites; fecal excretion accounts for about 6%, and the remainder is excreted via other routes. Renal excretion of unchanged drug is minimal. |
| Half-life | The terminal elimination half-life of latanoprostene bunod is approximately 17 minutes for the active metabolite (latanoprost acid) after topical ocular administration. This short half-life reflects rapid systemic clearance, consistent with once-daily dosing for intraocular pressure reduction. |
| Protein binding | Latanoprost acid is approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution for latanoprost acid is approximately 0.67 L/kg, indicating distribution into total body water and tissues. |
| Bioavailability | After topical ocular administration, systemic bioavailability is very low due to extensive first-pass metabolism in the eye and systemic circulation; clinically insignificant systemic levels are achieved. |
| Onset of Action | Onset of intraocular pressure reduction occurs within 1–2 hours after topical ocular administration. |
| Duration of Action | The duration of action is at least 24 hours after a single topical ocular dose, allowing for once-daily dosing. Clinical studies show sustained IOP reduction over 24 hours. |
One drop (approximately 1.5 mcg) in the affected eye(s) once daily in the evening.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Not approved for use in pediatric patients. Safety and efficacy not established. |
| Geriatric use | No dosage adjustment necessary; efficacy and safety similar to younger adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions Can cause increased pigmentation of the iris and eyelashes.
| FDA category | Animal |
| Breastfeeding | Unknown if latanoprostene bunod is excreted in human milk. No M/P ratio available. Due to potential for systemic absorption and unknown effects on nursing infant, caution is advised; consider benefit versus risk. |
| Teratogenic Risk | Latanoprostene bunod is not recommended during pregnancy due to the potential for prostaglandin analog effects, including uterine contractions and decreased fetal blood flow. Animal studies have shown embryofetal toxicity at systemic exposures higher than clinical ocular doses. No adequate human data exist. Risk cannot be excluded; avoid use unless clearly needed. |
■ FDA Black Box Warning
None
| Common Effects | ocular hypertension |
| Serious Effects |
["Hypersensitivity to latanoprost, benzalkonium chloride (preservative), or any component of the formulation. Avoid use in patients with a history of bronchial asthma or severe COPD due to potential for bronchospasm (prostaglandin class effect)."]
| Precautions | ["May increase iris pigmentation (irreversible), darkening of eyelid skin, and increased eyelash length/thickness. Use with caution in patients with intraocular inflammation (e.g., iritis/uveitis), macular edema (especially pseudophakic), and in patients with known hypersensitivity to latanoprost or nitrates. Not recommended in patients with active herpes simplex keratitis. Safety in hepatic or renal impairment not established."] |
| Food/Dietary |
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| Fetal Monitoring | Monitor intraocular pressure. No specific fetal monitoring required unless signs of systemic toxicity occur. Advise patients to report uterine cramping or bleeding. |
| Fertility Effects | Based on mechanism, systemic prostaglandin analogs may affect fertility via hormonal disruption or altered uterine/ovarian function. Limited data in humans; animal studies show no effect on fertility at clinically relevant ocular doses. |
| No clinically significant food interactions. Avoid excessive alcohol consumption as it may affect IOP control. |
| Clinical Pearls | Latanoprostene bunod is a nitric oxide-donating prostaglandin F2α analog for reduction of intraocular pressure (IOP) in open-angle glaucoma or ocular hypertension. It is typically dosed one drop in the affected eye(s) once daily in the evening. It may cause gradual change in iris pigmentation (iridial hyperpigmentation), eyelash changes (thickness, length, color), and potential for cystoid macular edema in aphakic or pseudophakic patients with torn posterior lens capsule. Systemic absorption is minimal but may precipitate asthma in susceptible individuals. Use with caution in patients with intraocular inflammation (iritis/uveitis) as it may exacerbate conditions. Contraindicated in patients with known hypersensitivity to any component. |
| Patient Advice | Instill one drop in the affected eye(s) once daily in the evening; do not use more frequently. · Remove contact lenses before instillation; wait at least 15 minutes before reinserting. · Wash hands before use; avoid touching the dropper tip to any surface or the eye. · If using other topical ophthalmic medications, separate administrations by at least 5 minutes. · The medication may cause gradual eye color change (increased brown pigmentation), eyelash changes (longer, thicker, darker), and darkening of eyelid skin; these are usually permanent. · Temporary blurred vision may occur immediately after instillation; do not drive until vision clears. · If you develop a red, painful eye, photosensitivity, or vision changes, contact your ophthalmologist immediately. · Do not share this medication with others. · Store unopened bottles in the refrigerator; once opened, may be stored at room temperature for up to 4 weeks. · Inform all healthcare providers that you are using this medication, especially before surgery due to possible effect on IOP. |