Pilocarpine Prodrugs

Pilocarpine is a direct-acting cholinergic agonist that is used to control the elevated IOP associated with glaucoma. Pilocarpine shows a low ocular bioavail-ability (1-3% of instilled dose) due to poor absorption into the cornea coupled with a short duration of action. Because of these drawbacks, pilocarpine is generally instilled 3-4 times per day, which results in undesirable side effects and poor patient compliance. The ocular absorption of pilocarpine is mainly limited by its low lipophilicity (log Papp = -0.15) (Bundgaard et al., 1986b). Thus lipophilic prodrugs have been studied to improve both the ocular absorption and delivery of pilocarpine.

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