Brands, Medical Use, Clinical Data
Drug Category
- Anti-Allergic Agents
- Anti-Inflammatory Agents, Non-Steroidal
- Bronchodilator Agents
- Histamine H1 Antagonists
- Lipoxygenase Inhibitors
- Platelet Aggregation Inhibitors
Dosage Forms
- Ophthalmic solution (0.05%)
Brands / Synonyms
Astelin; Astepro; Azelastina [INN-Spanish]; Azelastine; Azelastinum [INN-Latin]; Dymista; Optivar
Indications
For the treatment of itching of the eye associated with allergic conjunctivitis.
Pharmacology
Azelastine is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine. Decreased chemotaxis and activation of eosinophils has also been demonstrated.
Mechanism of Action
Antihistamines such as azelastine appear to compete with histamine for histamine H1- receptor sites on effector cells (mast cells). The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Absorption
Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.
Contraindications
OPTIVAR™ is contraindicated in persons with known or suspected hypersensitivity to any of its
components.
Drug Interactions
No separate information available.
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