A novel lidocaine hydrochloride ophthalmic gel for topical ocular anesthesia

Abstract

Topical anesthetics play an important role in the practice of ophthalmology, both for procedures in the office and in the operating room. The need for safe, long-acting topical ocular anesthetic agents is ongoing, and has been highlighted by the increase of intravitreal administration of pharmacologic agents. Current practices for ocular anesthesia include subconjunctival injection of 2% aqueous lidocaine, topical 2% lidocaine drops and topical 0.5% tetracaine. Tetracaine is not yet FDA approved, and is associated with corneal epithelial toxicity and delayed epithelial healing after multiple administrations. Lidocaine jelly (2%) preparations have been reported to be beneficial in several systemic procedures, including those of the upper airway, dental, urogenital, and gastrointestinal. It has been theorized, and recent studies support the idea, that gel formulations of lidocaine may enhance anesthetic effect, and therefore be superior to anesthetic solutions for topical cataract surgery. The viscous nature of gel formulations is thought to lengthen contact time, resulting in better anesthesia at lower drug concentrations. Furthermore, several studies suggest that lidocaine is bactericidal and bacteriostatic, and may have a supplementary role in preventing and treating surgical site infections. Akten™, lidocaine 3.5% gel (Akorn, Buffalo Grove, IIlinois) was FDA approved for all ophthalmic procedures in October 2008. This gel is a preservative-free, lidocaine-based anesthetic gel consisting of 35 mg/mL of lidocaine hydrochloride. We describe the properties, including chemical structure, indications, evidence of support, use, adverse effects, and precautions, which we believe enable Akten to provide superior anesthesia, while minimizing side effects.

The Effectiveness of 2% Lidocaine Gel Compared to 0.5% Tetracaine Eye Drop As Topical Anesthetic Agent for Phacoemulsification Surgery

“…Liu et al, mentioned that systemic concentration of lidocaine, following lidocaine gel administration, did not increase significantly following topical administration. This is due to high penetration from the gel preparation into the corneal epithel and its thick preparation creates long duration in the cornea despite of tears ( 10 ).…”

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

“…The thermosensitive ophthalmic gel was developed by Akorn Inc. Pharmaceuticals under the trade name Akten ® received approval from the FDA in 2008 [ 6 , 118 ]. Akten ® is a preservative-free lidocaine (3.5%) ocular anaesthetic indicated for use in ocular procedures with the dose of two drops applied to the ocular surface.…”

“…The appropriate viscosity of this formulation can reduce systemic absorption and thus the possible systemic side effects. Moreover, the viscosity of the formulation was 50% less compared to the gel for non-ophthalmic preparations for ease of administration [ 118 ]. The clinical study of this product was conducted as a multi-center, randomized, controlled, and double-blind study to evaluate the effectiveness and safety of Akten ® in 209 subjects.…”

“…In this group, about 84%, 55%, and 27% of the subjects experienced anesthesia for at least 5 min, more than 10 min, and more than 15 min, respectively. The clinical study concluded that Akten ® is effective and safe to be used as an ocular anesthetic [ 118 , 119 ]. However, it is important to mention that long-term use of ocular anesthetic may cause ulceration and opacification of the corneal owing to delayed wound healing [ 118 , 119 ].…”

Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride

“…It is also used as an antiarrhythmic drug [ 2 ]. It exerts local anesthetic effect by binding with voltage gated Na + channels at axonal membrane and prevents the transport of Na + across the channels, thus inhibiting the postsynaptic neuron from depolarization and stabilizes neuronal membrane [ 3 ]. The most common form of lidocaine administration is through intravenous or hypodermic injection, which causes pain and discomfort [ 4 ].…”