Dipivefrin: current concepts

Pro-drugs are agents that require biotransformation prior to exhibiting pharmacologic activity. Dipivefrin (dipivalyl epinephrine or DPE) is an epinephrine pro-drug produced by the addition of two pivalic acid groups to the parent compound. This creates a more lipophilic molecule which penetrates the cornea more readily than epinephrine. Enzymes in ocular tissues convert dipivefrin into its active form, epinephrine. In concentrations approximately one-tenth that of epinephrine, topically applied dipivefrin therefore produces: (1) similar intra-ocular concentrations of epinephrine; (2) similar reductions in intra-ocular pressure (IOP); (3) similar degrees of mydriasis; and (4) fewer extraocular and systemic side effects. For reasons that are discussed, dipivefrin should probably not be used in conjunction with anticholinesterases. Dipivefrin offers the same risk of cystoid macular oedema as does epinephrine. Dipivefrin is a safe, effective, and well-tolerated alternative to epinephrine in the treatment of elevated IOP. It is particularly useful for patients who cannot tolerate epinephrine.