[Comparison between local and systemic administration of cyclosporin A on the effective level in conjunctiva, aqueous humor and serum].
Cyclosporine is an important tool for the therapy of immunological diseases of the cornea and conjunctiva, as well as the treatment of patients with high-risk corneal grafts. However, potentially severe systemic side effects are disadvantageous. The purpose of our study was to determine if topical ocular application leads to about the same concentrations in ocular tissues as systemic application. Therefore, the concentration of cyclosporine in conjunctiva, aqueous humor and blood was measured by radioimmunoassay in six patients with systemic administration of cyclosporine and ten patients who received one drop of topical cyclosporine 2% four times prior to cataract surgery. All patients with systemic application showed measurable concentrations of cyclosporine in blood, as did four patients in the group receiving topical cyclosporine. There was no significant difference between both groups concerning cyclosporine concentration in aqueous humor. The level of cyclosporine in the conjunctiva was significantly higher after topical application (P < 0.02). In conclusion, therapy with cyclosporine eye drops results in levels in the conjunctiva and aqueous humor that are comparable to or even higher than those after systemic application if the last application was no more than 18h prior to the measurement. Therefore, topical ocular application of cyclosporine, which reduces or eliminates the drug's systemic side effects, can be used to induce local immunosuppressive activity, particularly in the treatment of superficial immunological diseases and after limbal allograft transplantation.
Pfau
B
B
Universitäts-Augenklinik Heidelberg.
Kruse
F E
FE
Rohrschneider
K
K
Zorn
M
M
Fiehn
W
W
Burk
R O
RO
Völcker
H E
HE
D000284:Administration, Oral; D001082:Aqueous Humor / Q000187:drug effects* / Q000378:metabolism; D001682:Biological Availability; D002387:Cataract Extraction; D003228:Conjunctiva / Q000187:drug effects* / Q000378:metabolism; D016039:Corneal Transplantation; D016572:Cyclosporine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016030:Kidney Transplantation; D009883:Ophthalmic Solutions
D007166:Immunosuppressive Agents; D009883:Ophthalmic Solutions; D016572:Cyclosporine
Vergleich zwischen lokaler und systemischer Applikation von Cyclosporin A auf den Wirkspiegel in Bindehaut, Kammerwasser und Serum.