Lotilaner (EENT) (Monograph)

Brand name: Xdemvy
Drug class: Anti-infectives, Miscellaneous

Medically reviewed by Drugs.com on Feb 10, 2025. Written by ASHP.

Introduction

Anti-parasitic agent; gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites.

Uses for Lotilaner (EENT)

Demodex Blepharitis

Topical treatment of Demodex blepharitis.

The American Academy of Ophthalmology guidelines include lotilaner as a treatment option for Demodex blepharitis; other treatments include other antiparasitic medications (metronidazole, ivermectin), tea tree oil eyelid or shampoo scrubs, hypochlorous acid 0.01% spray, and in-office procedures such as intense pulsed light and microblepharoexfoliation.

Lotilaner (EENT) Dosage and Administration

Administration

Ophthalmic Administration

Administer topically to the eye as a 0.25% ophthalmic solution.

Dosage

Adults

Demodex Blepharitis

Ophthalmic

Instill 1 drop in each eye twice a day (approximately 12 hours apart) for 6 weeks.

Cautions for Lotilaner (EENT)

Contraindications

None.

Warnings/Precautions

Risk of Contamination

Do not allow the tip of the dispensing container to come into contact with eye, surrounding structures, fingers, or any other surface in order to minimize contamination of solution. Serious damage to eye and subsequent loss of vision may result from using contaminated solutions.

Contact Lenses

Remove contact lenses prior to administering lotilaner 0.25% ophthalmic solution; can reinsert 15 minutes after administration.

Specific Populations

Pregnancy

No available data on use of lotilaner 0.25% ophthalmic solution in pregnant women; however, systemic exposure from ocular administration is low.

Lactation

Not known whether lotilaner 0.25% ophthalmic solution is distributed into human milk or if the drug has any effects on the breastfed infant or on milk production; however, systemic absorption is low.

Consider developmental and health benefits of breastfeeding along with mother's clinical need and any potential adverse effects on the breast-fed infant from lotilaner.

Females and Males of Reproductive Potential

No reproductive malformations in animal studies.

Pediatric Use

Not studied in pediatric patients <18 years of age.

Geriatric Use

No overall differences in safety or efficacy observed between geriatric patients and younger adults.

Hepatic Impairment

Not studied in hepatic impairment.

Renal Impairment

Not studied in renal impairment.

Common Adverse Effects

The most common adverse reaction was instillation site stinging and burning (10%).

Drug Interactions

In vitro studies indicate that lotilaner is not metabolized by CYP enzymes nor is a substrate of organic cation transporter (OCT) 1, organic anion transporting polypeptide (OATP) 1B1, OATP1B3, P-glycoprotein, breast cancer resistance protein (BCRP), or bile salt export pump (BSEP).

Lotilaner (EENT) Pharmacokinetics

Absorption

Plasma Concentrations

Maximum systemic exposure after topical ophthalmic administration occurs 2 hours after single administration and by 1 hour after administration on day 42 of treatment.

Distribution

Plasma Protein Binding

High (>99%)

Elimination

Metabolism

Not metabolized by CYP enzymes.

Elimination Route

Nonclinical studies in animals suggest that the drug is excreted in bile as mostly unmetabolized drug.

Half-life

Effective half-life 264 hours when dosed every 12 hours.

Stability

Storage

Ophthalmic

Solution

Store bottle at 15-25°C. After opening bottle, may use up until manufacturer expiration date.

Actions

GABA-gated chloride channel inhibitor that is selective for mites; member of the isoxazoline family of compounds.
Causes paralytic action in target organism, leading to its death.

Advice to Patients

Instruct patients to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to minimize contamination of the solution. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions.
Advise patients that if they develop an intercurrent ocular condition, such as trauma or infection, have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician's advice concerning the continued use of lotilaner 0.25% ophthalmic solution.
Advise patients that lotilaner 0.25% ophthalmic solution contains potassium sorbate, which may discolor soft contact lenses. Contact lenses should be removed prior to administration of lotilaner ophthalmic solution and may be reinserted 15 minutes following administration.
Advise patients that if more than one topical ophthalmic medication is being used, the medications should be administered at least 5 minutes apart.
Advise patients that if one dose is missed, treatment should continue as scheduled and doses should not be doubled.
Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.
Advise patients to inform their clinician if they are or plan to become pregnant or plan to breast-feed.
Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Lotilaner 0.25% ophthalmic solution is obtained through designated specialty pharmacies. Contact the manufacturer at 833-919-4942 or [Web] for specific availability information.