Effect of ketotifen fumarate, olopatadine, and levocabastine on ocular active anaphylaxis in the guinea pig and ocular immediate hypersensitivity in the albino rat.
OBJECTIVE
To study the effects of ketotifen fumarate, olopatadine, and levocabastine on ocular active anaphylaxis in guinea pigs and on ocular immediate hypersensitivity in albino rats.


METHODS
Clinical grading scores and Evans blue dye leakage to eyelids and to eyeballs were assessed in five treatment groups (n = 10): ketotifen fumarate 0.025%, olopatadine 0.1%, levocabastine 0.05%, negative control, and positive control.


RESULTS
At 20 minutes after challenge, edema scores for ketotifen-treated guinea pigs were statistically significantly lower than those for levocabastine or olopatadine. Active treatment significantly reduced vascular leakage in both models. Ketotifen significantly reduced vascular leakage in eyelids compared with the other drugs. In guinea pigs, vascular leakage in eyeballs was significantly reduced with ketotifen fumarate compared with olopatadine and levocabastine.


CONCLUSIONS
In the guinea pig model, ketotifen was more effective than olopatadine and levocabastine at reducing conjunctival edema and vascular permeability in eyelids and eyeballs. In the rat model, ketotifen was more effective at reducing vascular permeability in eyelids than olopatadine and levocabastine.
Schoch
Christian
C
Novartis Pharma AG Basel Switzerland. christian.schoch@pharma.novartis.com
D000707:Anaphylaxis / Q000139:chemically induced / Q000188:drug therapy* / Q000276:immunology; D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects; D003233:Conjunctivitis, Allergic / Q000139:chemically induced / Q000188:drug therapy* / Q000276:immunology; D003990:Dibenzoxepins / Q000627:therapeutic use*; D004195:Disease Models, Animal; D004487:Edema / Q000188:drug therapy; D005143:Eyelids / Q000098:blood supply; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000627:therapeutic use*; D007665:Ketotifen / Q000627:therapeutic use*; D008297:Male; D000069605:Olopatadine Hydrochloride; D009883:Ophthalmic Solutions / Q000627:therapeutic use; D010047:Ovalbumin; D010880:Piperidines / Q000627:therapeutic use*; D051381:Rats
D003990:Dibenzoxepins; D006634:Histamine H1 Antagonists; D009883:Ophthalmic Solutions; D010880:Piperidines; D000069605:Olopatadine Hydrochloride; D010047:Ovalbumin; C047340:levocabastine; D007665:Ketotifen