Safety and efficacy of olopatadine hydrochloride nasal spray for the treatment of seasonal allergic rhinitis

Abstract

Background: A nasal spray containing the antiallergy agent olopatadine hydrochloride is being developed for the treatment of seasonal allergic rhinitis (SAR).Objective: To evaluate the safety and efficacy of 2 concentrations of olopatadine nasal spray vs placebo in patients with SAR.Methods: This was a multicenter, randomized, double-blind, placebo-controlled study. After a 3-to 21-day placebo run-in, 565 patients aged 12 to 80 years were randomized to receive 0.4% or 0.6% olopatadine or placebo, 2 sprays per nostril twice daily for 2 weeks. Patients evaluated morning and evening reflective and instantaneous nasal symptoms (sneezing, stuffy nose, runny nose, and itchy nose, which compose the total nasal symptom score [TNSS]) and ocular symptoms and completed the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ).Results: Olopatadine spray (0.4% and 0.6%) was significantly superior to placebo for percentage change from baseline in overall reflective (P ϭ .004 and P Ͻ .001, respectively) and instantaneous (P ϭ .02 and P ϭ .003, respectively) TNSSs. Also, 0.6% olopatadine was significantly superior to placebo for reducing the reflective and instantaneous assessments of sneezing, runny and itchy nose, and itchy eyes; the instantaneous assessments of watery eyes; and the overall and all 7 domain scores of the RQLQ (P Ͻ .05). Olopatadine spray exhibited a safety profile comparable with that of placebo.Conclusions: Olopatadine nasal spray (0.4% and 0.6%) provided statistically significant improvements in allergic rhinitis symptoms compared with placebo regarding TNSSs (reflective and instantaneous) and in quality-of-life variables in patients with SAR. Olopatadine nasal spray administered twice daily was safe and well tolerated in adolescents and adults.Ann Allergy Asthma Immunol. 2005;95:600-606.

Allergic Conjunctivitis and the Impact of Allergic Rhinitis

“…Recently, a 16-day, 544-patient study comparing intranasal olopatadine, 0.6%, with intranasal azelastine, 0.1%, found statistically comparable reductions in reflective total P=0.8402 propionate (noninferior) vs fluticasone in rTOSS [54] P=0.003 vs placebo and noninferior vs azelastine in rTNSS [55] Ocular outcomes not reported [55] P<0.05 vs placebo in TNSS [98] Ocular outcomes not reported [98] P≤0.004 vs placebo for olopatadine, 0.6% and 0.4%, in rTNSS [75] P≤0.05 vs placebo for olopatadine, 0.6%, in symptoms of itchy eyes and watery eyes P=NS vs placebo for olopatadine, 0.4%, in symptoms of itchy eyes and watery eyes [75] P<0.001 vs placebo in rTNSS [99] P≤0.009 vs placebo in symptoms of itchy eyes and watery eyes [99] Azelastine Metaanalysis Azelastine was efficacious in the treatment of allergic rhinitis in clinical studies. No specific nasal or ocular symptoms were evaluated in the global analysis of efficacy [100].…”

“…Systemic exposure has been suggested as an explanation for the effects of intranasal antihistamines on ocular allergy symptoms [75]. This is a more plausible mechanism for intranasal antihistamines than for INS, as intranasal antihistamines are associated with greater systemic bioavailability (levocabastine, 60-80%; azelastine, 40%) than the newer INS [76].…”

Seasonal Allergic Rhinitis

“…However, astemizole and terfenadine can cause serious cardiovascular events, including QT prolongation, torsades de pointes, and other cardiac arrhythmias in patients with cardiac disease or Ophthalmic and intranasal preparations of antihistamines such as antazoline (Vasocon-A), levocabastine (Livostin), azelastine (Astelin), and olopatadine (Patanol, Opatanol) are effective in the treatment of ocular and nasal symptoms [37][38][39]. They have a rapid onset of action, but require twicedaily administration [38,39]. These medications not only relieve the itching but also treat the symptoms of allergic rhinoconjunctivitis.…”

Pharmacologic rationale for treating allergic and nonallergic rhinitis

“…The most common side effects at the recommended dose of 2 sprays per nostril twice a day are bitter taste (19.7% vs 0.6% placebo) and sedation (11.5 vs 5.4% placebo). Azelastine [83][84][85] and olopatadine 86 have demonstrated efficacy in seasonal rhinitis, and in recent studies azelastine appears to be slightly superior to cetirizine, 87 desloratadine, 88 and fexofenadine 89 in its ability to reduce total nasal symptoms scores, including nasal congestion. An older study, however, did not find that azelastine was superior to cetirizine in seasonal AR.…”