Patanase (olopatadine hydrochloride)

Patanase is an antihistamine with selective H1 -receptor antagonist activity: its principal effects are mediated via inhibition of H1 receptors.

Patanase is specifically indicated for the relief of the symptoms of seasonal allergic rhinitis in patients 12 years of age and older.

Patanase is supplied as a metered-dose manual spray pump designed for intranasal administration. The recommended initial dose of the drug is two sprays per nostril twice daily. Patanase must be primed before initial use and when it has not been used for more than 7 days.

FDA Approval
FDA approval of Patanase was based on the results of three clinical trials. These randomized, double blind, parallel group, multicenter, placebo (vehicle nasal spray)-controlled clinical trials 1,598 subjects, aged 12 years and older, in the United States. The subjects received Patanase Nasal Spray 0.6%, Patanase Nasal Spray 0.4%, or vehicle nasal spray, two sprays per nostril, twice-daily. The duration of the study was two weeks. Efficacy was based on patient recording of 4 individual nasal symptoms (nasal congestion, rhinorrhea, itchy nose, and sneezing) on a 0 to 3 categorical severity scale (0 = absent, 3 = severe) as reflective or instantaneous scores. Reflective scoring recorded symptom severity over the previous 12 hours; instantaneous scoring recorded symptom severity at the time of recording. The primary efficacy endpoint was the difference from placebo in the percent change from baseline in the sum of morning and evening reflective total nasal symptom score (rTNSS) at the end of the treatment period. In all studies Patanase exhibited statistically significantly greater decreases in rTNSS compared to vehicle nasal spray. Study One: In the Patanase 0.6% and 0.4% groups, the change from baseline was -3.63 and -3.38, respectively, compared to -2.67 for the placebo group (p <0.0001 for the high dose group). Study Two: In the Patanase 0.6% and 0.4% groups, the change from baseline was -2.90 and -2.63, respectively, compared to -1.92 in the placebo group (p<0.0001 for the high dose group).

Onset of action was evaluated in three environmental exposure unit studies. In these studies, subjects with seasonal allergic rhinitis were exposed to high levels of pollen in an environmental exposure unit and then treated with either Patanase Nasal Spray or vehicle nasal spray, two sprays in each nostril. Afterwards they self-reported their allergy symptoms hourly as instantaneous scores for the subsequent 12 hours. Patanase 0.6% was found to have an onset of action of 30 minutes after dosing in the environmental exposure unit and a twelve hour duration of effect.

Ongoing Study Commitments

• Alcon has agreed to a deferred pediatric study under PREA for the treatment of allergic rhinitis in pediatric patients ages 2 to 11 years of age.
  Final Report Submission: July 1, 2009
• Alcon has agreed to conduct a one-year, controlled clinical trial in patients with perennial allergic rhinitis to assess the long term safety of povidone-free olopatadine hydrochloride nasal spray with respect to nasal septal perforation. The FDA also requested Alcon assess the long term safety of this product with respect to local nasal adverse effects, including epistaxis and nasal ulceration, as well as systemic effects. Include at least the following three treatment groups: povidone-free olopatadine hydrochloride nasal spray, vehicle placebo with pH matching olopatadine hydrochloride nasal spray, and vehicle placebo with normal pH to evaluate if the low pH of the formulation has an effect on local nasal safety. They were to submit a labeling supplement reflecting the results of the clinical trial.
  Protocol Submission: July 2008
  Trial Start Date: November 2008
  Final Report Submission: November 2012

Adverse reactions associated with the use of Patanase may include, but are not limited to, the following:

• Bitter taste
• Headache
• Epistaxis
• Pharyngolaryngeal Pain
• Post-nasal drip
• Cough
• Urinary tract infection

Patanase is an antihistamine with selective H1 -receptor antagonist activity: its principal effects are mediated via inhibition of H1 receptors. These drugs selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. They act in the bronchi, capillaries, and other smooth muscles. Histamine acts as a pro-inflammatory signal released from mast cells in response to allergic reactions or tissue damage.

Takahashi H, Zhang Y, Morita E Evaluation of the antihistamine effects of olopatadine, cetirizine and fexofenadine during a 24 h period: a double-blind, randomized, crossover, placebo-controlled comparison in skin responses induced by histamine iontophoresis. Archives of Dermatological Research 2008 Feb 28

Fairchild CJ, Meltzer EO, Roland PS, Wells D, Drake M, Wall GM Comprehensive report of the efficacy, safety, quality of life, and work impact of Olopatadine 0.6% and Olopatadine 0.4% treatment in patients with seasonal allergic rhinitis. Allergy and asthma proceedings : the official journal of regional and state allergy societies 2007 Nov-Dec;28(6):716-23

Patel P, Roland PS, Marple BF, Benninger PJ, Margalias H, Brubaker M, Beezley SF, Drake M, Potts SL, Wall GM. An assessment of the onset and duration of action of olopatadine nasal spray. Otolaryngology and head and neck surgery 2007 Dec;137(6):918-24

Hampel FC Jr, Ratner PH, Amar NJ, van Bavel JH, Mohar D, Fairchild CJ, Wall GM, Brubaker MJ, Drake M, Crenshaw KM Improved quality of life among seasonal allergic rhinitis patients treated with olopatadine HCl nasal spray 0.4% and olopatadine HCl nasal spray 0.6% compared with vehicle placebo.Allergy and asthma proceedings : the official journal of regional and state allergy societies. 2006 May-Jun;27(3):202-7

Abelson MB, Gomes PJ, Vogelson CT, Pasquine TA, Gross RD, Turner FD, Wells DT, Bergamini MV, Robertson SM Clinical efficacy of olopatadine hydrochloride ophthalmic solution 0.2% compared with placebo in patients with allergic conjunctivitis or rhinoconjunctivitis: a randomized, double-masked environmental study. Clinical Therapeutics 2004 Aug;26(8):1237-48

Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Japanese Journal of Pharmacology 2002 Apr;88(4):379-97

For additional information regarding Patanase or seasonal allergic rhinitis, please visit the Patanase web page.