Glaucoma benzalkonium chloride Free products

Glaucoma - benzalkonium chloride (BAK)-Free products

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Available Products in the U.S.

• ALPHAGAN® P (brimonidine tartrate) Ophthalmic Solution 0.1% and 0.15%. PURITE® 0.005% (0.05 mg/mL) - similar lowering of IOP to the 0.2% solution.  Reduced incidence of allergic reactions by more than 50%.
  

  Pharmacology:   Brimonidine tartrate ophthalmic solution 0.2% is a relatively selective alpha-2 adrenergic receptor agonist with a peak ocular hypotensive effect occurring at two hours post-dosing.

  Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.

  Dosing: One drop in the affected eye(s), three times daily, approximately 8 hours apart.

• Travatan® Z  (Travoprost 0.004%)- ionic-buffered preservative (sofZia®)
  

  Pharmacology:  Reduction of the IOP starts approximately 2 hours after the first administration with maximum effect reached after 12 hours.

  Travoprost free acid, a prostaglandin analog is a selective FP prostanoid receptor agonist, which is believed to reduce IOP by increasing uveoscleral outflow. The terminal elimination half-life of travoprost free acid was estimated from fourteen subjects and ranged from 17 minutes to 86 minutes with the mean half-life of 45 minutes.

  Dosing: One drop in the affected eye(s) once daily in the evening.

• XELPROS™ (latanoprost ophthalmic emulsion) 0.005%
  

  Pharmacology:  Latanoprost is a prostaglandin F2α analogue that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Reduction of the IOP in man starts about 3-4 hours after administration and maximum effect is reached after 8-12 hours. IOP reduction is present for at least 24 hours. The elimination of the acid of latanoprost from human plasma is rapid (t1/2 =17 min)

  Dosing: One drop in the affected eye(s) once daily in the evening.

 

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Background

 

benzalkonium chloride (BAK)-Free Products

Overview

•  The harmful effects of BAK are time and dose dependent. The risk of harmful effects is much greater in patients using more than one product containing
• These products are not preservative-free.
• XELPROS™ is the first and only BAK-free formulation of latanoprost—delivered with innovative LIPIXELLE™ technology (novel micelle microemulsion formulation).
•  The level of antimicrobial activity of all of the current ophthalmic preservatives is generally inversely proportional to its compatibility with the ocular surface.   Benzalkonium chloride is a highly effective preservative also has the highest ocular toxity.
• Purite oxidizes microbial cellular components, but has no significant effect on human ocular tissues.   SofZia causes oxidative damage and subsequent death in bacteria but have little effect on human cells.  Both are much gentler to the eye (less keratopathy and conjunctival hyperemia)  compared to BAK formulations.
• The BAK-free options have been proven to improve ocular tolerance without a reduction in efficacy.

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