Trade name Optivar
Routes intranasal, ocular
Bioavailability 40% (intranasal)
Half-life 22 hours
A potent, second-generation, selective,histamine-H1-receptor antagonist.
Recommended for the first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis.
Formulated both as a nasal spray (0.1% and 0.15% solutions) and as eye drops (0.05% solution).
Indicated for the local treatment of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis.
Eye drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.
For adults and children ≥ 12 years the recommend dosage is 1 or 2 sprays/nostril twice daily.
Starts working within 15 minutes.
The usual dosage of azelastine eye drops for adults and children is one drop in each eye twice daily.
When administered intranasally systemic bioavailability is approximately 40%.
Maximum plasma concentrations are observed within 2–3 hours after use
Oxidatively metabolized by the cytochrome P450 family into its active metabolite, desmethylazelastine, and two inactive carboxylic acid metabolites.
Approximately 75% of an oral dose is excreted in feces.
Modes of action include: antihistamine effect, mast ell stablization and antiinflammatory effect.
Onset of action; 15 minutes with the nasal spray, and 3 minutes with the eye drops.
Duration of effects lasts for 12 hours.
Clinical studies show nasal spray show that 78% of vasomotor rhinitis patients report some or complete control of post-nasal drip and 90% of patients with seasonal allergic rhinitis reported some or complete control of their sneezing.
Has a more rapid onset of action and is more effective than oral antihistamines in relieving nasal congestion, such as desloratadine or cetirizine in the treatment of allergic rhinitis.
Has shown comparable efficacy to intranasal corticosteroid fluticasone propionate in improving patients’ quality of life and rhinitis symptoms and is superior to intranasal budesonide in improving the symptom of rhinorrhea in patients with perennial allergic rhinitis.
When coadministered with fluticasone additive effects occur.
While it is a weaker anti-inflammatory agent compared to corticosteroids, it has a significantly more rapid onset of action.
Compared to the leukotriene receptor antagonist montelukast in the treatment of perennial allergic rhinitis it has the greater benefit in alleviating the symptoms of rhinorrhea.
Azelastine eye drops are effective at a concentration of 0.05%.
Utilized for the treatment of the symptoms of seasonal allergic conjunctivitis, such as itching, lacrimation and redness.ti
Eye drops start working within 3 minutes, and the effects last least 8–10 hours.
Trade name Astelin
Routes of administration include intranasal, and ocular.
Bioavailability 40% intranasally.
Biological half-life 22 hours.
A potent, second-generation, selective, histamine antagonist used as a first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis.
Azelastine nasal spray is indicated for the local treatment of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis, such as rhinorrhea, sneezing and nasal pruritus in adults and children 5 years of age and older.
Azelastine eyes drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.
Adverse events: Bitter taste, headache, nasal burning and somnolence.
The systemic bioavailability of azelastine is approximately 40% when administered intranasally.
Maximum plasma concentrations are observed within 2–3 hours.
Oxidatively metabolized by the cytochrome P450 family into its active metabolite, desmethylazelastine, and two inactive carboxylic acid metabolites.
Approximately 75% of an oral dose is excreted in feces.
Pharmacokinetics not affected by age, gender or hepatic impairment.
Has a triple mode of action;
Anti-histamine effect,
Mast-cell stabilizing effect
Anti-inflammatory effect.
Available as a generic.