AZELASTINE
BRAND NAME:- AZEP NASAL SPRAY 0.14mg
AZELASTINE is a second generation antihistamine drug .This is newer H1 blocker has good Topical activity; in addition it inhibits histamine realease and inflammatory reaction triggered by LTs and PAF. After intranasal application it has been shown to down regulate intracellular adhesion molecule -1 (ICAM-1) expression on nasal mucosa. Its t½ is 24hr,but action lasts longer due to active metabolite . Its metabolism is inhibited by CYP 3A4 inhibitors. Given by nasal spray for seasonal and perennial allergic rhinitis it provides quick symptomatic relief lasting 12hr.
PHARMACODYNAMIC:-
Azelastine has a triple mode of action:
Anti-histamine effect,Mast-cell stabilizing effect an Anti-inflammatory effect.
PHARMACOKINETICS:-
The systemic bioavailability of azelastine is approximately 40% when administered intranasally.[3] Maximum plasma concentrations (Cmax) are observed within 2–3 hours.[3] The elimination half life, steady-state volume of distribution and plasma clearance are 22 h, 14.5 L/kg and 0.5 L/h/kg respectively (based on intravenous and oral administration data). Approximately 75% of an oral dose is excreted in feces. Pharmacokinetics of orally administered azelastine is not affected by age, gender, or hepatic impairment.
USE:-
Treatment of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis, such as rhinorrhea, sneezing and nasal pruritus in people five years of age and older. In some countries, it is also indicated for the treatment of vasomotor rhinitis in adults and children ≥ 12 years old.[14] Azelastine eye drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.
SIDE EFFECTS:-
Stinging in the nose and altered taste perception are the local side effects. SOME somnolence has been reported on nasal application and a tendency to weight gain noted after oral use.
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