benzalkonium
Regulatory sources consulted
Approved indications
- Handwashing to decrease bacteria on the skin.
Clinical warnings
- For external use and hands only. Keep out of reach of children. Avoid contact with the eyes; if contact occurs, rinse thoroughly with water. Stop use if irritation or redness develops and ask a doctor if it persists for more than 72 hours. If swallowed, get medical help or contact a Poison Control Center right away. — DailyMed/openFDA, SPL set ID 0001d1cf-f727-4875-a44f-5a51f7b617a4
Pregnancy and lactation
No specific recommendation is established during pregnancy or breastfeeding.
Recent literature (PubMed)
The aim of this review, is to present an updated revision of topical management of SAC and PAC, based on the available scientific evidence and focused on the impact of ophthalmic solution formulations on eye surface. Physicians treating ocular allergy should be aware of tear film and tear film disruption in SAC and PAC, and how eye drop composition and additives affect the physiology of the allergic eye. Seasonal and perennial allergic conjunctivitis (SAC and PAC) are the most frequent causes of ocular allergy (OA), and both conditions are underdiagnosed and undertreated. SAC and PAC are immunoglobulin E (IgE)-mediated hypersensitivity reactions. The additional tear film disruption caused by the release of inflammatory mediators increases and exacerbates the impact of signs and symptoms and may trigger damage of the ocular surface. Comorbidities are frequent, and dry eye disease in particular must be considered. Clinical guidelines for the management of SAC and PAC recommend topical therapy with antihistamines, mast cells stabilizers or dualaction agents as first-line treatment, but care should be taken, as many medications contain other compounds that may contribute to ocular surface damage.
Preservatives in multidose formulations of topical ophthalmic medications are crucial for maintaining sterility but can be toxic to the ocular surface. Benzalkonium chloride (BAK)-used in approximately 70% of ophthalmic formulations-is well known to cause cytotoxic damage to conjunctival and corneal epithelial cells, resulting in signs and symptoms of ocular surface disease (OSD) including ocular surface staining, increased tear break-up time, and higher OSD symptom scores. These adverse effects are more problematic with chronic exposure, as in lifetime therapy for glaucoma, but can also manifest after exposure as brief as seven days. Multiple strategies are available to minimize or eliminate BAK exposure, among them alternative preservatives, preservative-free formulations including sustained release drug delivery platforms, and non-pharmacological therapies for common eye diseases and conditions. In this paper, we review the cytotoxic and clinical effects of BAK on the ocular surface and discuss existing and emerging options for ocular disease management that can minimize or eliminate BAK exposure. 眼科外用药物多剂量配方中的防腐剂对维持药物无菌至关重要, 但其对眼表有毒性作用。苯扎氯铵 (BAK) 用于约70%的眼科药物中, 众所周知会对结膜和角膜上皮细胞造成细胞毒性损伤, 并引起眼表疾病 (OSD) 相关的症状和体征, 包括眼表染色、泪膜破裂时间延长和OSD症状评分升高等。这些不良反应在长期使用时更加严重, 如青光眼的终生治疗, 但有些患者在使用7天后也会表现出来。有多种策略可用于减少或消除BAK的不良反应, 其中包括更换防腐剂、使用无防腐剂的配方 (包括缓释给药平台) 以及使用常见眼病和眼部症状的非药物疗法等。在这篇文章中, 我们回顾了BAK对眼表的细胞毒性和临床影响, 并讨论了现有的和正在研究的可减少或消除BAK不良反应的眼病治疗方案。
Ocular surface disease (OSD) is a complex condition that can cause a range of symptoms (e.g, dryness, irritation, and pain) and can significantly impact the quality of life of affected individuals. Iatrogenic OSD, a common finding in patients with glaucoma who receive chronic therapy with topical ocular antihypertensive drugs containing preservatives such as benzalkonium chloride (BAK), has been linked to damage to the ocular surface barrier, corneal epithelial cells, nerves, conjunctival goblet cells, and trabecular meshwork. Chronic BAK exposure activates inflammatory pathways and worsens symptoms, compromising the success of subsequent filtration surgery in an exposure-dependent manner. In eyes being treated for glaucoma, symptomatic treatment of OSD may provide some relief, but addressing the root cause of the OSD often necessitates reducing or, ideally, eliminating BAK toxicity. Strategies to decrease BAK exposure in patients with glaucoma encompass the use of preservative-free formulations or drugs with alternative and less toxic preservatives such as SofZia®, Polyquad, potassium sorbate, or Purite®. Though the benefits of these alternative preservatives are largely unproven, they might be considered when financial constraints prevent the use of preservative-free versions. For patients receiving multiple topical preserved drugs, the best practice is to switch to nonpreserved equivalents wherever feasible, regardless of OSD severity. Furthermore, nonpharmacological approaches, including laser or incisional procedures, should be considered. This review explores the effects of BAK on the ocular surface and reviews strategies for minimizing or eliminating BAK exposure in patients with glaucoma in order to significantly improve their quality of life and prevent complications associated with chronic exposure to BAK.
Benzalkonium chloride (BAK) is the most widely used preservative in multidose glaucoma eye drops. Medical management of glaucoma often requires the chronic use of preserved eye drops, resulting in a high incidence of BAK‑associated ocular discomfort, ocular surface disease, accumulation within ocular structures, and inflammatory tissue changes. The use of BAK has also been associated with reduced surgical success in trabeculectomy. Although alternative preservatives exist, they have also been associated with some toxic effects. Switching from BAK‑containing formulations to preservative‑free (PF) formulations results in significantly fewer side effects, improved ocular surface disease, and enhanced patient comfort. However, barriers such as cost and ease of use have impeded the more widespread adoption of PF glaucoma drops.