Twice-daily pilocarpine hydrochloride ok to improve near visual acuity in presbyopia: study

United States: Pilocarpine hydrochloride 1.25% given twice daily to people with presbyopia resulted in more significant improvements in near visual acuity at day 14 without compromising distance acuity, showed a phase 3 study.

The safety profile was consistent with once-daily administration of pilocarpine hydrochloride 1.25%, with headache being the most common treatment-related adverse event, and systemic accumulation was minimal, warranting discontinuation. administration twice a day. Pilocarpine is a muscarinic receptor agonist that mimics the actions of the parasympathetic neurotransmitter acetylcholine on smooth muscle to stimulate near vision.

The study, presented in the American Journal of Ophthalmologyled to FDA approval for twice-daily use of pilocarpine hydrochloride eye drops 1.25% for the treatment of presbyopia in March 2023.

Presbyopia is characterized by a gradual decline in near vision that becomes noticeable from the age of 40 and is due to age-related changes in the lens. Surgical and non-surgical methods can correct presbyopia. Non-surgical procedures include bifocal or varifocal glasses, reading glasses, and monovision or multifocal contact lenses. However, these methods can reduce visual acuity at one or more viewing distances (far, intermediate, and near) and are associated with potential risks, complications, and inconveniences.

In the above context, Shane Kannarr, Kannarr Eye Care, Pittsburg, Kansas, USA, and colleagues sought to evaluate the efficacy, safety, and pharmacokinetics of pilocarpine hydrochloride 1.25% (Pilo ) versus vehicle when given bilaterally, twice daily (BID, 6 hour apart) for 14 days in presbyopic patients.

The study included 230 participants between the ages of 40 and 55 with presbyopia impacting daily activities with mesopic, high-contrast, and binocular distance-corrected binocular (CNVA) near visual acuity (CNVA) of 20/40 to 20/100. One hundred and fourteen were randomized to Pilo BID and 116 to vehicle.

Percentage of Participants Gaining ≥ 3 Lines of Mesopic/Photopic, High-Contrast, Binocular DCNVA on Day 14, Hour 9, Without Loss of More Than 5 Letters of Photopic/Mesopic Corrected Distance Visual Acuity with the Same Refractive Correction (Criterion major) . Plasma pilocarpine levels were assessed in approximately 10% of enrolled participants. TEAEs (treatment-related adverse events) and certain ocular measurements were essential safety measures.

The authors reported the following findings:

  • The proportion of participants achieving critical primary and secondary efficacy endpoints was statistically significantly more significant with Pilo BID than vehicle, with treatment differences of 27.3% and 26.4%, respectively .
  • The most common TEAE was headache, reported in 10 (8.8%, Pilo group) and 4 (3.4%, vehicle group) participants.
  • The pilocarpine accumulation index on day 14 was ≤ 1.11 after the second dose.

“Improvements in near vision were statistically greater with Pilo BID than with vehicle, without compromising distance acuity,” the researchers concluded. “The safety profile of Pilo BID was consistent with that of Pilo once daily, and systemic accumulation was minimal, supporting BID administration.”


Kannarr S, El-Harazi SM, Moshirfar M, Lievens C, Kim JL, Peace JH, Safyan E, Liu H, Zheng S, Robinson MR. SAFETY AND EFFECTIVENESS OF TWICE-DAILY PILOCARPINE HCL IN PRESBYOPIA: THE VIRGIN PHASE 3, RANDOMIZED, DOUBLE-MASKED, CONTROLLED STUDY. Am J Ophthalmol. May 4, 2023: S0002-9394(23)00195-2. doi: 10.1016/j.ajo.2023.05.008. Epub ahead of print. PMID: 37149245.

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