In a recent high throughput analysis to identify drugs that alter hepatic apolipoprotein A-I (apo A-I) expression, histamine receptor one (H1) antagonists emerged as potential apo A-1 inducing drugs. Thus the present study was undertaken to identify some of the underlying molecular mechanisms of the effect of antihistaminic drugs on apo AI production. Apo A-I levels were measured by enzyme immunoassay and Western blots. Apo A-I mRNA levels were measured by reverse transcription real-time PCR using glyceraldehyde-3-phosphate dehydrogenase (GAPDH) mRNA as the internal control. The effects of histamine and antihistamines on apo A-I gene were determined by transient transfection of plasmids containing the apo A-I gene promoter. Histamine repressed while (H1) receptor antagonist azelastine increased apo A-I protein and mRNA levels within 48 h in a dose-dependent manner. Azelastine and histamine increased and suppressed, respectively, apo A-I gene promoter activity through a peroxisome proliferator activated receptor α response element. Treatment of HepG2 cells with other H1 receptor antagonists including fexofenadine, cetirizine, and diphenhydramine increased apo A-I levels in a dose-dependent manner while treatment with H2 receptor antagonists including cimetidine, famotidine, and ranitidine had no effect. We conclude that H1 receptor signaling is a novel pathway of apo A1 gene expression and therefore could be an important therapeutic target for enhancing de-novo apo A-1 synthesis.

There is considered modern classification of rhinitis and the accents in diagnostic and therapeutic approaches to patients with this disease are indicated, as well as the possibilities of using topical intranasal antihistamines in the treatment of allergic, vasomotor and medicamentous rhinitis.

The objective of the present work was to evaluate the effectiveness of the combination of azelastine hydrochloride and mometasone furoate for the intranasal application to treat the patients presenting with seasonal allergic rhinitis. A total of 60 subjects suffering from seasonal allergic rhinitis were available for the observation. All the patients were allocated to three groups comprised of 20 individuals each. The patients of the first group received the fixed combination of azelastine hydrochloride and mometasone furoate for the intranasal application, those in the second group were given mometasone furoate administered intranasally together with an oral antihistamine preparation of the third generation, and the patients of the third group were treated with intranasal mometasone furoate alone. The effectiveness of the treatment was evaluated on days 7 and 14 after its initiation. It was found that the treatment with the use of the combination of azelastine hydrochloride and mometasone furoate resulted in a more pronounced alleviation of rhinological symptoms and improvement of the quality of life at the early stages of therapy in comparison with mometasone furoate monotherapy. It is concluded that the patients with moderate and severe seasonal allergic rhinitis can be recommended to use the combination of azelastine hydrochloride and mometasone furoate as качестве the initial treatment.