A prostaglandin analogue used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. Tafluprost was approved for use in the U.S. on February 10, 2012. |
Brands | Zioptan
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Categories | Antihypertensive Agents Neuroprotective Agents
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Synonyms | AFP-168 Saflutan
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indication
For the treatment of glaucoma (Open Angle) and intraocular hypertension.
pharmacology
Tafluprost is a novel PGA with high affinity for the fluoroprostaglandin (FP) receptor PGF2α. Tafluprost has an affinity for the FP receptor that is approximately 12 times higher than that of the carboxylic acid of latanoprost, but with almost no potential to bind to other receptors. The active form, tafluprost acid, can be detected in plasma for up to one hour after topical administration, with a peak at 10 minutes.
mechanism of action
Tafluprost is a prostaglandin F2a analogue. Specifically, Tafluprost is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Studies in animals and man suggest that the main mechanism of action is increased uveoscleral outflow.
biotransformation
Rapidly hydrolyzed by corneal esterases to the free acid of tafluprost, which is the active form.