Lotilaner (EENT) (Monograph)

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

Introduction

Lotilaner, a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites, is an anti-parasitic agent.

Uses for Lotilaner (EENT)

Lotilaner has the following uses:

Lotilaner is an ectoparasiticide (anti-parasitic) indicated for the treatment of Demodex blepharitis.

Lotilaner (EENT) Dosage and Administration

General

Lotilaner is available in the following dosage form(s) and strength(s):

Ophthalmic solution containing lotilaner 0.25%.

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Adults

Dosage and Administration

Instill one drop of lotilaner in each eye twice daily (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 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.

Use with Contact Lenses

Contact lenses should be removed prior to instillation of lotilaner and may be reinserted 15 minutes following its administration.

Specific Populations

Pregnancy

There are no available data on lotilaner use in pregnant women to inform any drug associated risk; however, systemic exposure to lotilaner from ocular administration is low. In animal reproduction studies, lotilaner did not produce malformations at clinically relevant doses.

Lactation

There are no data on the presence of lotilaner in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to lotilaner following 6 weeks of topical ocular administration is low and is >99% plasma protein bound; thus it is not known whether measurable levels of lotilaner would be present in maternal milk following topical ocular administration. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for lotilaner and any potential adverse effects on the breast-fed child from lotilaner.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 18 years have not been established.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and other adult patients.

Common Adverse Effects

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

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.

Actions

Mechanism of Action

Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites. Inhibition of these GABA chloride channels causes a paralytic action in the target organism leading to its death. Lotilaner is not an inhibitor of mammalian GABA mediated chloride channels when tested at up to 30 µM (18 µg/mL) in vitro (approximately 1100 times the RHOD).

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 (e.g., 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.
Advise patients that lotilaner contains potassium sorbate, which may discolor soft contact lenses. Contact lenses should be removed prior to instillation of lotilaner and may be reinserted 15 minutes following its administration.
Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes between applications.
Advise patients that if one dose is missed, treatment should continue with the next dose.

Additional Information

AHFSfirstRelease^™. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

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.