Multiple action agents and the eye: do they really stabilize mast cells?
OBJECTIVE
Multiple action drugs, such as azelastine, epinastine, ketotifen and olopatadine, have recently been suggested to combine antihistaminic effect, mast cell stabilization and anti-inflammatory action. This pharmaceutical class is, therefore, rapidly becoming the first choice for prevention and treatment for allergic conjunctivitis.


RESULTS
Increasing in-vitro studies have been performed to investigate the mast-cell-stabilizing effect of multiple action drugs. Most of the study results agree that these drugs are able to inhibit histamine and several neoformed mediators, including cytokines and arachidonic acid-derived products, from mast cells. However, the mechanisms of action have not yet fully been elucidated. Most of the results from clinical trials as well as the in-vivo experimental studies, including the conjunctival provocation model, support the evidence of a stabilizing effect of these drugs.


CONCLUSIONS
Evidence of a different inhibitory effect of multiple action compounds on the pro-inflammatory mediators released from the mast cells suggests the possibility to target different phases of the allergic reaction, leading to a potential improvement in the management of allergic patients.
Lambiase
Alessandro
A
CIR Laboratory of Ophthalmology, University Campus Bio-Medico, Italy.
Micera
Alessandra
A
Bonini
Stefano
S
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology / Q000627:therapeutic use; D016718:Arachidonic Acid / Q000276:immunology; D003233:Conjunctivitis, Allergic / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology*; D016207:Cytokines / Q000276:immunology; D003984:Dibenzazepines / Q000494:pharmacology / Q000627:therapeutic use; D003990:Dibenzoxepins / Q000494:pharmacology / Q000627:therapeutic use; D006632:Histamine / Q000276:immunology; D006633:Histamine Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology / Q000627:therapeutic use; D007113:Immunity, Innate / Q000187:drug effects; D007665:Ketotifen / Q000494:pharmacology / Q000627:therapeutic use; D008407:Mast Cells / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism / Q000473:pathology; D000069605:Olopatadine Hydrochloride; D010793:Phthalazines / Q000494:pharmacology / Q000627:therapeutic use
D000893:Anti-Inflammatory Agents; D016207:Cytokines; D003984:Dibenzazepines; D003990:Dibenzoxepins; D006633:Histamine Antagonists; D007093:Imidazoles; D010793:Phthalazines; D016718:Arachidonic Acid; D000069605:Olopatadine Hydrochloride; D006632:Histamine; C053090:epinastine; D007665:Ketotifen; C020976:azelastine