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Re: dewophile post# 235321

Wednesday, 10/28/2020 4:02:24 PM

Wednesday, October 28, 2020 4:02:24 PM

Post# of 253511
Lotemax is .5% suspension dosed 4X day...Eysuvis is .25% dosed 2X day. Lotemax vs. other steroids....

Impact of the Topical Ophthalmic Corticosteroid Loteprednol Etabonate on Intraocular Pressure

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4846687/

In early pivotal clinical trials of LE ophthalmic suspension for conjunctivitis (allergic, giant papillary), anterior uveitis, and post-operative inflammation, LE had minimal impact on IOP over short-term (<28 days) and long-term (≥28 days) use.

In all studies, LE consistently demonstrated a low propensity to elevate IOP, regardless of formulation, dosage regimen, or treatment duration, including in known steroid responders. The cumulative proportion of patients exhibiting clinically significant IOP increases was 0.8% (14/1725 subjects) in studies evaluating short-term LE treatment and 1.5% (21/1386 subjects) in long-term studies. Furthermore, use of LE was associated with significantly lower rates of IOP elevation ≥10 mm Hg as compared to prednisolone acetate or dexamethasone (when used in combination with tobramycin). The cumulative data to date substantiates a favorable IOP-safety profile for LE with both short-term and long-term use.

Loteprednol etabonate (LE) is unique among corticosteroids in that the drug molecule incorporates a metabolically labile moiety which allows rapid metabolism and degradation following glucocorticoid receptor activation, thereby imparting a lower risk of side effects [21–23]. Unlike other ophthalmic corticosteroids, LE contains a chloromethyl ester instead of a ketone moiety at the carbon 20 (C-20) position of the prednisolone acetate (PA) core structure (Fig. 1). The metabolically labile C-20 ester group undergoes predictable hydrolysis by endogenous esterases into inactive metabolites (Fig. 1). In addition, LE is highly lipophilic and binds the glucocorticoid receptor with 4.3-fold greater affinity than dexamethasone [24]. LE also retains the high potency of prednisolone, with an anti-inflammatory efficacy 20-fold higher than hydrocortisone [22]. These attributes enable LE to penetrate the ocular tissues including the conjunctiva, cornea, and iris-ciliary body, bind to the glucocorticoid receptor, and exert potent anti-inflammatory effects, with minimal propensity for side effects.

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