Toxicity and pharmacokinetics of subconjunctival amphotericin B. An experimental study

Cornea. 1991 Sep;10(5):411-7. doi: 10.1097/00003226-199109000-00010.

Abstract

The pharmacokinetics and toxicity of subconjunctival (S/C) amphotericin B (AmB) were evaluated in Dutch-belted rabbits. Following the S/C injection of 1,500 micrograms of AmB, corneal and aqueous levels were determined by bioassay. The highest levels were present in the periphery of debrided corneas at 1 h (90.12 +/- 2.4 micrograms/g). The debrided central cornea contained 30.84 micrograms/g, almost double the amount present in the intact central cornea. These levels were transient; in the central intact cornea only 2.08 micrograms/g could be detected at 2 h. Peak aqueous levels were low (0.95 +/- .24 micrograms/mL in debrided corneas at 1 h). The S/C injection of 1,500 micrograms of AmB in sodium deoxycholate produced a severe inflammatory response in the conjunctiva, episclera, iris, anterior chamber, and superior rectus muscle that persisted 10 days. Injection of sodium deoxycholate alone produced a similar but less severe response.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amphotericin B / pharmacokinetics
  • Amphotericin B / toxicity*
  • Animals
  • Anterior Chamber / metabolism
  • Anterior Chamber / pathology
  • Aqueous Humor / metabolism
  • Conjunctiva
  • Cornea / metabolism
  • Cornea / pathology
  • Deoxycholic Acid / administration & dosage
  • Eye / metabolism*
  • Eye / pathology
  • Oculomotor Muscles / metabolism
  • Oculomotor Muscles / pathology
  • Rabbits
  • Tissue Distribution

Substances

  • Deoxycholic Acid
  • Amphotericin B