Unoprostone
Unoprostone Uses, Dosage, Side Effects, Food Interaction and all others data.
Unoprostone isopropyl is a prostaglandin analogue. Ophthalmic Solution 0.15% is a synthetic docosanoid. Unoprostone isopropyl has the chemical name isopropyl (+)-(Z)-7-[(1R,2R,3R,5S)-3,5 dihydroxy-2-(3-oxodecyl)cyclopentyl]-5-heptenoate.The main indication of Unoprostane is treatment of glucoma.
Unoprostone will begin to reduce IOP 30 minutes after ocular instillation.
| Trade Name | Unoprostone |
| Availability | Discontinued |
| Generic | Unoprostone |
| Unoprostone Other Names | Unoprostone |
| Related Drugs | epinephrine ophthalmic, latanoprost ophthalmic, timolol ophthalmic, brimonidine ophthalmic, pilocarpine ophthalmic, Xalatan, Lumigan |
| Type | Ophthalmic |
| Formula | C22H38O5 |
| Weight | Average: 382.541 Monoisotopic: 382.271924324 |
| Protein binding | Intended for local use only, very low systemic absorption. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Unoprostone is a prostaglandin analogue used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are clinically unresponsive to other ocular antihypertensive agents.
For the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are intolerant of other intraocular pressure lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another intraocular pressure lowering medication.
Unoprostone is also used to associated treatment for these conditions: Ocular Hypertension, Open-angle Glaucoma (OAG)
How Unoprostone works
Unoprostone is believed to reduce elevated intraocular pressure (IOP), by increasing the outflow of aqueous humor. The mechanism of action for the IOP-lowering effect of unoprostone is controversial. Early studies showed that unoprostone increases aqueous humor outflow through the uveoscleral pathway similar to the 20-carbon prostaglandin analogs, such as latanoprost.8 More recent evidence, however, shows that it may work, at least in part, through stimulation of Ca2+-activated BK and CIC-2 type channels, leading to increased trabecular meshwork outflow.
Toxicity
LD50 in rats: 1g/Kg (subcutaneous), 93500 µg/Kg (IV).
Unoprostone Disease Interaction
Volume of Distribution
Intended for local use only, very low systemic absorption.
Elimination Route
After application to the eye, unoprostone isopropyl is absorbed through the cornea and conjunctival epithelium where it is hydrolyzed by esterases to unoprostone free acid. mean peak unoprostone free acid plasma concentration was <1.5 ng/mL and dro pped below the lower limit of quantitation (<0.250 ng/mL) 1 hour following instillation, indicating low systemic absorption and rapid plasma excretion.
Half Life
Half-life of Unoprostone is 14 minutes.
Clearance
Intended for local use only, very low systemic absorption.
Elimination Route
Elimination of unoprostone free acid from human plasma is rapid. Plasma levels of unoprostone free acid dropped below the lower limit of quantitation ( < 0.25 ng/mL) 1 hour following ocular instillation. Urinary elimination is the predominant elimination route.
Innovators Monograph
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