Article Date: 2/1/2005

Adopting Steroid Therapy
For many clinicians, loteprednol is the agent of choice for treating inflammatory conditions.

Patients commonly complain of inflammation from a variety of causes, some of which are irritating and others that are potentially damaging. Dry eye is perhaps the most common cause of ocular inflammation, but other maladies include allergy, conjunctivitis and iritis.

Designing Safer Steroids

The safest, most effective ocular medications penetrate quickly, execute the desired effect and break down into inert components. The slower the body metabolizes a drug, the more likely the agent will cause undesirable side effects.

For example, eye doctors know that ketone-based steroids, such as prednisolone (Pred Forte), linger in the anterior compartment of the eye, putting patients at risk of elevated IOP and cataract formation with long-term use.

By replacing a single ketone group with an ester group, Bausch & Lomb designed a steroid that retains the potency of prednisolone but offers an improved safety profile.

Highly lipid-soluble loteprednol etabonate 0.5% (Lotemax) quickly reaches target tissues in the cornea, iris and ciliary body. After exerting its anti-inflammatory effect, naturally occurring esterases in the eye convert this agent to inactive metabolites. One study shows that 1.7% of patients treated with loteprednol for 28 days or more experienced elevated IOP, compared to 6.7% of patients treated with prednisolone for the same length of time.*

"In the past, we were told, 'Save steroids for the big problems,' because we had to worry about preventing elevated IOP," says Jimmy D. Bartlett, O.D., F.A.A.O. "But loteprednol's unique mechanism of action and improved safety profile make it a good treatment option for most inflammatory conditions."

*Bausch & Lomb package insert.

Addressing allergic inflammation

Not too long ago, clinicians considered steroids the class of last resort, but new formulations and improved efficacy have made these agents a viable option for treating the gamut of ocular inflammatory disorders. But the question still remains: When is it appropriate to begin steroid therapy?

"If a patient's eye is very hot, itchy and uncomfortable, and he can't wear his contact lenses, I'll immediately start him on a 2- to 3-week course of loteprednol etabonate 0.5% (Lotemax)," says Walter S. Ramsey, O.D., F.A.A.O.

Paul M. Karpecki, O.D., F.A.A.O., agrees. "Using steroids sooner has had a positive impact on my practice," he says. "If I see a patient with swollen, red eyes, I'm not going to wait for a combination steroid/anti-inflammatory to kick in."

Another panelist who uses steroids as first-line therapy is Ron Melton, O.D., F.A.A.O. "I've been using steroids more and more," he says. "I use loteprednol to reduce inflammation in symptomatic patients and then I revert to monotherapy with artificial tears or azelastine hydrochloride 0.05% (Optivar) to control their symptoms."

Most of the panelists agree they use steroid therapy for patients whose symptoms interfere with their daily activities.

"If a patient's symptoms are merely annoying, I'll usually prescribe the more traditional anti-allergy drugs before moving on to steroids," says Jimmy D. Bartlett, O.D., F.A.A.O.

Effective treatment for GPC

One condition Dr. Bartlett treats immediately with steroids is giant papillary conjunctivitis (GPC). In a phase II study, he and his colleagues administered loteprednol or a placebo to 100 patients with GPC and contact lens intolerance. The patients were not permitted to wear their contact lenses for the duration of the study.

"Loteprednol reduced inflammation and papillae size substantially better than placebo," Dr. Bartlett says. "But we wanted to make sure it was the drug and not abstaining from contact lenses that relieved the patients' inflammation."

In a subsequent 6-week phase III study, Dr. Bartlett and his colleagues applied loteprednol or placebo on top of patients' contact lenses. "Loteprednol relieved the GPC symptoms without affecting corneal integrity or causing an infection," says Dr. Bartlett.

To date, loteprednol is the only steroid that has an FDA indication to work against GPC.

Studies have shown that loteprednol (Lotemax) effectively reduces inflammation associated with GPC (top) and iritis (bottom).  

Start with a bang

Acute inflammatory conditions, such as ocular allergies and GPC, respond to steroid therapy, but does loteprednol have a role in treating potentially recurring conditions like iritis? When polled, the panelists responded with a resounding "yes."

"We need to hit iritis early and hit it big," Dr. Bartlett says. Dr. Melton agrees: "The goal in treating iritis -- even mild to moderate cases -- is to control inflammation with aggressive treatment so it doesn't damage uveal blood vessels. This kind of damage can create a recurrent and inflammatory condition."

The panelists offered several iritis treatment scenarios. "About 70% to 80% of all uveitis patients do very well on loteprednol. Only the most severe cases might require another medication, such as prednis-olone acetate (Pred Forte)," Dr. Bartlett says. "I prescribe loteprednol alone every 1 or 2 hours while awake for the first 24 to 48 hours, rather than starting at q.i.d. After 2 days, I begin to taper."

Dr. Karpecki emphasizes the importance of this hourly dosing. "Many of the patients I see with lingering iritis started using loteprednol or other steroids q.i.d., which wasn't frequent enough to resolve the problem", he says. "I'd rather overtreat and taper than risk having a patient develop long-term problems."

Broad applications

Inflammation plays such a significant role in so many ocular conditions that it only makes sense to treat these conditions with an effective anti-inflammatory agent. The panelists agree its broad labeling and proven clinical efficacy suggest that loteprednol may be what eye doctors are looking for. 


Should Patients Self-treat With Steroids?

Traditionally, clinicians have tried to prevent patients from using topical steroids inappropriately by writing one-time-only prescriptions. Nevertheless, everyone knows that patients tend to keep unfinished prescription drugs for future use.

"Patients know that a medication worked for them once before, so they'll continue to use it whenever they need it," says Paul M. Karpecki, O.D., F.A.A.O. "You'd be amazed how often patients use drops we prescribe, including steroids, on a p.r.n. basis."

What these patients don't realize is that using certain topical steroids without supervision can cause elevated IOP, cataract formation or corneal damage.

But as Ron Melton, O.D., F.A.A.O., points out, the availability of safer topical steroids has changed the way clinicians think about refills.

"At one time, we preached 'Never refill steroids,'" he says. "However, with the inflammatory efficacy and safety of loteprednol, I will allow a refill, or even two on a case-by-case basis. I never did that 5 or 10 years ago." 


Optometric Management, Issue: February 2005