Pregabalin Eye Drops for Ocular Pain and Glaucoma

Pregabalin is an FDA-approved medication given orally to help treat neuropathic pain associated with diabetes and spinal cord injuries as well as fibromyalgia. However, for patients whose pain is localized to the eye, pregabalin can be reformulated into eye drops to deliver pain relief directly to the eye. In addition to helping manage ocular neuropathic pain, early research suggests that pregabalin might also help treat glaucoma and ocular hypertension. In this blog post, we look at these potential indications and the safety of pregabalin eye drops.

Post-Operative Ocular Pain

Pregabalin’s oral formulation (Lyrica®) is already used off-label by some ophthalmologists to treat eye pain immediately after LASIK surgery.¹ A 2023 systematic review that included six trials found that pregabalin significantly reduced acute eye pain in the first 24 hours after surgery compared with placebo.² Although patients receiving pregabalin reported lower pain scores on day one, there was no apparent benefit for chronic pain or long-term outcomes. However, one of the individual studies showed significantly reduced pain at up to one week after surgery.³ 

For conditions like dry eye disease, where pain may not cause clinical signs and isn’t responding to other therapies, gabapentinoids like gabapentin and pregabalin can be used. In a rat model, continuous pregabalin treatment alleviated ocular pain and hypersensitivity,⁴ suggesting that it may help mitigate the neuropathic symptoms of dry eye disease.

Glaucoma and Ocular Hypertension

Glaucoma is primarily managed by reducing intraocular pressure (IOP), but existing medications often require multiple daily doses and can have side effects like conjunctival hyperemia associated with rho-kinase inhibitors⁵ or permanent iris color changes with prostaglandin analogs like latanoprost.^6,7 Pregabalin has emerged as a candidate for treating glaucoma after genetic studies showed that its binding site was a modulator of IOP.^8,9 By binding this subunit, topical pregabalin lowered IOP, presumably by reducing aqueous production and/or improving outflow. 

Preclinical studies in mice showed that a single drop of 0.6% pregabalin reduced IOP by over 40%.8 A more recent study showed that a single topical application of a pregabalin microemulsion reduced IOP for more than one day in different animal models.¹⁰

Topical Administration 

Although no studies have compared administration routes for pregabalin, a 2021 study showed that topical gabapentin eye drops provided analgesic and anti-inflammatory effects on the ocular surface without causing corneal anesthesia.¹¹ Since gabapentin and pregabalin share similar mechanisms of action,¹² pregabalin drops may provide similar pain relief and may be used in combination with other treatments such as acetaminophen-codeine.¹³ These drops may also help reduce opioid consumption.¹⁴

Why Choose VLS Pharmacy & New Drug Loft?

Because pregabalin is currently only available as an oral medication, it must be reformulated into 0.6% eye drops using specialized equipment in a sterile environment, as mandated by USP for the preparation of all ophthalmic medications. Ophthalmic compounding is a niche area of expertise that our compounding pharmacists at VLS Pharmacy & New Drug Loft specialize in, allowing us to supply prescribers with ophthalmic preparations. 

By working closely with a 503A compounding pharmacy that specializes in ophthalmic compounding, providers can ensure that their pregabalin eye drops are precisely tailored to the specific needs of individual pediatric patients.

 

Please comment below with any thoughts or questions.

Reach out to our team to learn about best practices and to partner with our experts on custom compounded medications for your patients. All medications from VLS Pharmacy and New Drug Loft are prepared in a lab that follows safety and quality standards per our status as a 503A pharmacy.

 

References

1. Paik DW, Lim DH, Chung TY. Effects of taking pregabalin (Lyrica) on the severity of dry eye, corneal sensitivity and pain after laser epithelial keratomileusis surgery. Br J Ophthalmol. 2022;106(4):474-479. doi:10.1136/bjophthalmol-2020-317570
2. Shen X, Chen X, He Y, Xu H, Zhu J. Efficacy and safety of pregabalin in eye pain: A systematic review. Medicine (Baltimore). 2023;102(6):e32875. doi:10.1097/MD.0000000000032875
3. Paik DW, Lim DH, Chung TY. Effects of taking pregabalin (Lyrica) on the severity of dry eye, corneal sensitivity and pain after laser epithelial keratomileusis surgery. Br J Ophthalmol. 2022;106(4):474-479. doi:10.1136/bjophthalmol-2020-317570
4. Tei Y, Mikami Y, Ito M, et al. Pathogenic Mechanism of Dry Eye-Induced Chronic Ocular Pain and a Mechanism-Based Therapeutic Approach. Invest Ophthalmol Vis Sci. 2022;63(1):7. doi:10.1167/iovs.63.1.7
5. Wang J, Wang H, Dang Y. Rho-Kinase Inhibitors as Emerging Targets for Glaucoma Therapy. Ophthalmol Ther. 2023;12(6):2943-2957. doi:10.1007/s40123-023-00820-y
6. Teus MA, Arranz-Márquez E, Lucea-Suescun P. Incidence of iris colour change in latanoprost treated eyes. Br J Ophthalmol. 2002;86(10):1085-1088. doi:10.1136/bjo.86.10.1085
7. TRAVATAN Z [package insert]. Published online 2017. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021994s012lbl.pdf
8. Ibrahim MM, Maria DN, Mishra SR, Guragain D, Wang X, Jablonski MM. Once Daily Pregabalin Eye Drops for Management of Glaucoma. ACS Nano. 2019;13(12):13728-13744. doi:10.1021/acsnano.9b07214
9. Chintalapudi SR, Maria D, Di Wang X, et al. Systems genetics identifies a role for Cacna2d1 regulation in elevated intraocular pressure and glaucoma susceptibility. Nat Commun. 2017;8(1):1755. doi:10.1038/s41467-017-00837-5
10. Maria DN, Ibrahim MM, Kim MJ, et al. Evaluation of Pregabalin bioadhesive multilayered microemulsion IOP-lowering eye drops. J Controlled Release. 2024;373:667-687. doi:10.1016/j.jconrel.2024.07.061
11. Cammalleri M, Amato R, Olivieri M, et al. Effects of Topical Gabapentin on Ocular Pain and Tear Secretion. Front Pharmacol. 2021;12:671238. doi:10.3389/fphar.2021.671238
12. Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P. A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinet. 2010;49(10):661-669. doi:10.2165/11536200-000000000-00000
13. Pakravan M, Roshani M, Yazdani S, Faramazi A, Yaseri M. Pregabalin and gabapentin for post-photorefractive keratectomy pain: a randomized controlled trial. Eur J Ophthalmol. 2012;22 Suppl 7:S106-113. doi:10.5301/ejo.5000143
14. Dauri M, Faria S, Gatti A, Celidonio L, Carpenedo R, Sabato AF. Gabapentin and pregabalin for the acute post-operative pain management. A systematic-narrative review of the recent clinical evidences. Curr Drug Targets. 2009;10(8):716-733. doi:10.2174/138945009788982513

 

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