DURYSTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DURYSTA (DURYSTA).
Prostaglandin analog; selective FP receptor agonist that increases uveoscleral outflow of aqueous humor.
| Metabolism | Hydrolyzed in the cornea by esterases; further metabolism via beta-oxidation and conjugation in the liver; CYP not majorly involved. |
| Excretion | Minimal systemic absorption; no data on specific routes of elimination; expected to be primarily excreted via renal and biliary routes in small amounts. |
| Half-life | Not applicable due to local ocular administration with minimal systemic exposure; bimatoprost systemic half-life is approximately 45 minutes after intravenous administration. |
| Protein binding | Approximately 88% bound to human plasma proteins (primarily albumin) for bimatoprost. |
| Volume of Distribution | 0.7 L/kg for bimatoprost after systemic administration, indicating distribution into total body water; however, DURYSTA is administered locally, so systemic Vd is not clinically relevant. |
| Bioavailability | Systemic bioavailability is negligible after intracameral administration due to low dose and local metabolism. |
| Onset of Action | Reduction in intraocular pressure (IOP) begins within 1-2 hours after intracameral administration, with peak IOP reduction at 12-18 hours. |
| Duration of Action | Sustained IOP reduction for up to 3-4 months following a single intracameral injection; duration may vary by patient and IOP target. |
| Molecular Weight | 415.57 |
One intracameral implant (10 mcg) administered in the study eye by a qualified ophthalmologist. A second administration may be performed if necessary, at least 3 months after the initial implant.
| Dosage form | IMPLANT |
| Renal impairment | No dosage adjustment required based on renal impairment. |
| Liver impairment | No dosage adjustment required based on hepatic impairment. |
| Pediatric use | Safety and efficacy not established in pediatric patients. Use not recommended. |
| Geriatric use | No specific dosage adjustment recommended in elderly patients. Clinical studies included patients aged 65 years and older with no overall differences in safety or efficacy observed. |
| 1st trimester | Use only if potential benefit justifies potential risk to fetus. No adequate and well-controlled studies in pregnant women. In animal studies, bimatoprost administered intravenously during organogenesis caused embryofetal lethality and malformations at doses >125 mcg/kg/day (approximately 600 times the clinical exposure via ocular route). |
| 2nd trimester | Same as T1. Avoid unnecessary exposure; consider alternative treatments if possible. |
| 3rd trimester | Same as T1. Potential risk of preterm labor or uterine contractions due to prostaglandin analog effects, though systemic exposure is minimal with ocular use. |
Clinical note
Comprehensive clinical and safety monograph for DURYSTA (DURYSTA).
| Placental transfer | Bimatoprost is a prostaglandin analog with low molecular weight (415.57 Da). Based on its properties, it is expected to cross the placenta. Animal studies indicate transfer across the placenta following intravenous administration. |
| Breastfeeding |
■ FDA Black Box Warning
None
| Serious Effects |
Active ocular infection (e.g., herpes simplex, bacterial keratitis)Active intraocular inflammation (e.g., uveitis, iritis)Hypersensitivity to bimatoprost or any component of the formulation
| Precautions | Pigmentation of the iris, periorbital tissue, and eyelashes, Eyelash changes (length, thickness, number), Cystoid macular edema in aphakic/pseudophakic patients with torn posterior lens capsule, Bacterial keratitis from contaminated single-dose containers, Concomitant use with other prostaglandin analogs may increase IOP, Use with caution in patients with history of intraocular inflammation (iritis/uveitis) |
| Food/Dietary | No known food interactions. |
Loading safety data…
| Bimatoprost is excreted in breast milk in rats; it is not known whether it is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when DURYSTA is administered to a nursing woman. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for DURYSTA and any potential adverse effects on the breastfed child. |
| Lactation Rating | L3 (Moderately Safe). No human data available; risk cannot be ruled out. |
| Teratogenic Risk | No human data; in animal studies, intravitreal bimatoprim implant (DURYSTA) showed no teratogenicity but did produce embryofetal toxicity at maternally toxic doses. Risk cannot be excluded; use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor intraocular pressure and ocular adverse events. No specific fetal monitoring required unless maternal condition warrants. |
| Fertility Effects | No human data. In animal studies, no effects on fertility were observed. |
| Clinical Pearls |
| DURYSTA (bimatoprost implant) is a sustained-release intracameral implant for reducing intraocular pressure (IOP) in open-angle glaucoma or ocular hypertension. Administer as a single injection per eye; effects last up to 3 months. Monitor for corneal endothelial cell loss with repeated use. Contraindicated in active herpes simplex keratitis. |
| Patient Advice | Do not rub or press on the injected eye for at least 1 week to prevent implant dislocation. · Report sudden vision loss, eye pain, or redness immediately. · Use preservative-free artificial tears if needed; avoid water in the eye for 1 week. · May cause temporary blurred vision after injection; avoid driving until vision clears. · Notify if you have a history of eye infection or inflammation. · Follow up as scheduled for IOP checks and implant evaluation. |