The biodisponibility of antiglaucoma drugs, generally delivered in an aqueo
us eye-drop solution depends on their capacity to cross the cornea. The str
ucture of the cornea forms a barrier to strongly lipophilic substances and
the continuous renewal of the lacrimal film creates a major obstacle, preve
nting active substances from penetrating the eye. Active substances must th
us be delivered in highly concentrated solutions. The systemic bioavailabil
ity of antiglaucoma drugs taken orally, for example beta-blockers, is well
known, their behavior after eye-drop administration remains poorly elucidat
ed and highly dependent on individual susceptibility. We reviewed the liter
ature on pilocarpine, beta-blockers, adrenergic drugs (dipivalyl-epinephrin
e, apraclonidine, brimonidine), carbon anhydrase inhibitors (acetazolamide,
dorzolamide).