Unoprostone

Chemical formula: C₂₂H₃₈O₅  Molecular mass: 382.541 g/mol  PubChem compound: 5311236

Pharmacodynamic properties

When instilled in the eye, unoprostone is believed to reduce elevated intraocular pressure (IOP), by increasing the outflow of aqueous humor, but the exact mechanism is unknown at this time.

Pharmacokinetic properties

Absorption

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.

A study conducted with 18 healthy volunteers dosed bilaterally with unoprostone isopropyl ophthalmic solution twice daily for 14 days demonstrated little systemic absorption of unoprostone isopropyl. The systemic exposure of its metabolite unoprostone free acid was minimal following the ocular administration. Mean peak unoprostone free acid concentration was less than 1.5 ng/mL. Little or no accumulation of unoprostone free acid was observed.

Elimination

Elimination of unoprostone free acid from human plasma is rapid, with a half-life of 14 minutes. Plasma levels of unoprostone free acid dropped below the lower limit of quantitation (<0.25 ng/mL) 1 hour following ocular instillation. The metabolites are excreted predominately in urine.

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