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Tafluprost: the First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension

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Tafluprost: the First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension See discussions, stats, and author profiles for this publication at: https://www.researchgate.net/publication/232647942 Tafluprost: The First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension Article in Annals of Pharmacotherapy · October 2012 DOI: 10.1345/aph.1R229 · Source: PubMed CITATIONS READS 13 154 2 authors, including: Michael Neville Wingate University School of Pharmacy 11 PUBLICATIONS 87 CITATIONS SEE PROFILE All content following this page was uploaded by Michael Neville on 21 November 2014. The user has requested enhancement of the downloaded file. ARTICLES New Drug Approvals Tafluprost: The First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension Cory Swymer and Michael W Neville afluprost 0.0015% ophthalmic solu- tion (Zioptan) was approved by the T OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical trial data, Food and Drug Administration on Febru- efficacy data, and adverse effect incidence of tafluprost. ary 10, 2012, for the treatment of elevated DATA SOURCES: A literature search was completed using PubMed, Web of intraocular pressure (IOP) in patients with Science, and Google Scholar. Tafluprost was the primary search term. Articles open-angle glaucoma, in addition to ocular published between January 2008 and April 2012 were included in this review. hypertension.1 Although it has been used Additional limits placed on the searches were “human” and “English.” Citations in in other countries since 2008, tafluprost is which tafluprost appeared in the title were 36, 29, and more than 300 in PubMed, Web of Science, and Google Scholar, respectively. the first preservative-free prostaglandin STUDY SELECTION AND DATA EXTRACTION: Three clinical trials were included in analogue commercially available in the this review. One trial enrolled more than 500 subjects in a randomized fashion. US. Another also enrolled more than 500 subjects, although the study design was not randomized. The third trial evaluated the effects of tafluprost on subjects who had Pharmacology recently discontinued use of latanoprost, another prostaglandin that is approved to treat glaucoma and ocular hypertension. The duration of all 3 trials was 12 weeks. Open-angle glaucoma is an ocular dis- DATA SYNTHESIS: Tafluprost 0.0015% is the first topical prostaglandin approved order characterized by changes in the optic by the Food and Drug Administration for treatment of open-angle glaucoma and nerve head that leads to the loss of visual ocular hypertension that does not contain the widely used preservative, field.2 Increased ocular pressure is one of benzalkonium chloride (BAK). Although some controversy surrounds the long- term safety of exposure to BAK, clinical trial data are inconclusive. Tafluprost, like many contributing factors of glaucoma de- other prostaglandin analogues, exerts its effects on prostaglandin F receptors to velopment. Treatment focuses on the use reduce intraocular pressure (IOP). Results from 1 trial demonstrated significant of multiple agents, including α-2-adren- reductions in IOP when monotherapy was switched to tafluprost monotherapy. ergic receptor agonists, β-blockers, car- Reductions in IOP with tafluprost use were compared with those seen with use of bonic anhydrase inhibitors, and prosta- timolol and latanoprost in 2 trials, and noninferiority was observed. Significant reductions in tear osmolarity were noted in subjects who changed from glandin analogues. Varying mechanisms latanoprost, another prostaglandin analogue, to tafluprost therapy. Conjunctival of action offered by these classes lower hyperemia is the most common adverse effect seen in patients receiving drugs IOP and subsequent complications asso- from this class. Many have also reported stinging, ocular pruritus, increased ciated with glaucoma. Prostaglandin darkening or growth of eyelashes, and darkening of eyelids, as well as analogues are a first-line therapy option irreversible brown pigmentation of the iris. in treating elevated intraocular pressure CONCLUSIONS: Clinical trial data suggest that tafluprost is as efficacious as other because of their known efficacy and agents used in the management of ocular hypertension and glaucoma. Its use may be especially advantageous in people with allergies, sensitivities to minimal adverse effects.3 Tafluprost is preservatives, or dry or sensitive eyes. thought to stimulate the selective prosta- KEY WORDS: glaucoma, intraocular pressure, ocular hypertension, preservative- glandin F receptor (FP), which results in free, prostaglandin, tafluprost, Zioptan. increased uveoscleral and trabecular out- Ann Pharmacother 2012;46:1506-10. flow of aqueous humor and subsequent Published Online, 23 Oct 2012, theannals.com, doi: 10.1345/aph.1R229 Author information provided at end of text. 1506 I The Annals of Pharmacotherapy I 2012 November, Volume 46 theannals.com Downloaded from aop.sagepub.com by guest on October 11, 2013 decreased intraocular pressure.4 Although tafluprost offers Pharmacokinetics no significant pharmacologic advantage over its counter- parts within the prostaglandin class, it is the first topical Tafluprost is an ester prodrug that is hydrolyzed into the 4 prostaglandin available in a preservative-free formulation. biologically active metabolite, tafluprost acid, in the eye. Preservatives are contained in most ophthalmic prepara- The acid compound is further metabolized via β-oxidation tions and prolong the shelf life of many by preventing and phase II conjugation. Plasma concentrations of biodegradation and maintaining potency.5 Although several tafluprost acid peak about 10 minutes after instillation of 1 are available, benzalkonium chloride (BAK), which has drop of 0.0015% solution. Plasma tafluprost acid concen- surfactant, bactericidal, and bacteriostatic properties, is the trations are below detectable levels (10 pg/mL) following most commonly used preservative in ophthalmic prepara- topical administration. Pharmacokinetic comparisons4,10-12 tions.6 However, there have been some reports that BAK is between tafluprost and other prostaglandin preparations are associated with potentially harmful effects on the tear film summarized in Table 1. of the eye.7 BAK also appears to increase tear osmolarity.8 Investigators often assess tear film osmolarity as a means Clinical Trials of evaluating eye dryness.5 Normal values typically range from 290 to 300 mOsm/L; as osmolarity rises above this Hommer and colleagues enrolled 544 subjects in an 13 range, the odds of eye irritation increase. As a result, pa- open-label, multicenter, observational study. Subjects had tients report increased discomfort and dry eyes.8 Pellinen a previous diagnosis of ocular hypertension or glaucoma. and colleagues7 determined that higher concentrations of They required add-on therapy, change of medication, or BAK increase the incidence of cytotoxic effects. A positive were naïve to medical treatment. The mean duration of correlation also appears to exist between the amount of glaucoma was 6.5 years (range <1-35) at baseline. Most BAK contained in an ophthalmic preparation and the inci- participants (n = 360, 66.2%) had received monotherapy dence of dry eye and discomfort.9 Tressler and colleagues6 with prostaglandin analogues (n = 124) or β-blockers (n = examined the literature to determine whether BAK is asso- 129) prior to the study, and 25.6% had used a non-fixed or ciated with adverse sequelae when used long term in indi- fixed combination prior to the change of medication. At viduals with glaucoma. They summarized and examined their discretion during the trial, research ophthalmologists published data from in vitro, ex vivo, and in vivo studies changed therapy to or added therapy with tafluprost from 1970 to July 2009. The investigators noted that pre- 0.0015% once daily and monitored the subjects for 12 clinical evidence suggests that exposure to high concentra- weeks. tions of BAK for extended periods increases adverse ef- Data on subjective symptoms, tear-film break-up time fects. However, clinical evidence is more inconclusive; (TBUT), and baseline tear fluid amount in a subgroup of findings are not consistent from study to study. Studies that participants were collected. Satisfaction data were also col- have evaluated the long-term safety of BAK have not lected. IOP measurements were completed prior to treat- demonstrated a clear correlation with BAK concentrations ment and evaluated at 4-6 weeks and at 12 weeks after and ocular surface adverse events. Additionally, the active changing therapy to or adding tafluprost. Five hundred medication may cause ocular surface irritation, confound- forty-four subjects (1088 eyes) were included in the evalu- ing findings. Finally, many people diagnosed with glauco- ation. Diagnoses included open-angle glaucoma (76.6%), ma experience dry eyes and some within this group may ocular hypertension (10.9%), normal tension glaucoma be especially susceptible to ocular surface changes caused (6.2%), pseudo exfoliation glaucoma (3.0%), and other by BAK, the active medication, or the combination. glaucomas (3.3%).13 Table 1. Pharmacokinetics of Commonly Used Prostaglandin Analogues3,10-12 Parameter Bimatoprost Latanoprost Travoprost Tafluprost Maximum concentration Within 10 minutes 2 hours Within 30 minutes Within 10 minutes Distribution Plasma (88% bound) Aqueous humor (first 4 hours); plasma Not reported Not reported (1 hour after local administration) Metabolism N-deethylation and β-oxidation in liver
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