Ocular Drugs

  1. Sympathomimetics
    Apraclonidine (LOPIDINE)
  2. Indication
    • General
    • Glaucoma. Apraclonidine is used for pre&postlaser prophylaxis of intraocular pressure spikes.

    • Apraclonidine
    • To reduce the penetration of clonidine into the brain, a polar (hydrophilic)
    • analog, apraclonidine, was developed for ophthalmic use. As a single
    • drop, apraclonidine is a very effective ocular hypotensive agent. Maximal
    • pressure reduction in the treated eye was 37% (6.5 mmHg) and lasted up
    • to 12 hours. The dose-response curve for apraclonidine plateaus between
    • 0.25% and 0.5%. Most of the unwanted effects of apraclonidine are local
    • and are related to α1-adrenoceptor stimulation. These include conjunctival
    • blanching, eyelid retraction, and mild mydriasis. Apraclonidine has a very
    • low potential for systemic effects.

    • Brimonidine
    • Approved for use in the United States in 1996, brimonidine is similar to
    • clonidine in its relative α2-adrenoceptor agonism, lipophilicity, and relative
    • lack of α1-adrenoceptor agonism. Brimonidine achieves better penetration
    • of the cornea than apraclonidine, although it has a theoretical potential for
    • greater untoward effects such as sedation and systemic hypotension.
  3. MoA
    • General
    • Decreased production and increased outflow of aqueous humor.
    • α2-adrenoceptor agonists and β-adrenoceptor antagonists reduce aqueous humor flow by reducing aqueous humor production. In contrast to apraclonidine, brimonidine also increases uveoscleral outflow as measured by fluorophotometry.
  4. SEs
    • The most frequent adverse events associated with brimonidine are oral
    • dryness, ocular hyperemia, ocular discomfort, headache, and fatigue.
    • Less frequent effects include corneal staining and photophobia. Rare
    • events included lid crusting, abnormal taste, and depression.
Card Set
Ocular Drugs
Sympathomimetics Alpha-agonists