Lotilaner is the first FDA-approved ophthalmic antiparasitic indicated for the treatment of Demodex blepharitis in adults. Treatment is for 6 weeks with studies showing significant improvement in mite eradication and erythema cure. There is limited systemic absorption with topical ophthalmic administration and side effects are limited to local reactions.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-Instill topically in the affected eye(s).
-Do not allow the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface to minimize contamination of the solution.
-If more than one topical ophthalmic agent is being used, administer at least 5 minutes apart.
-Remove contact lenses prior to instillation, and wait 15 minutes after dosing before reinserting the lenses.
-If one dose is missed, continue with the next scheduled dose.
The most common adverse reaction to lotilaner ophthalmic solution is ocular irritation, including instillation site stinging and burning, which was reported in 10% of patients. Other ocular adverse events reported in less than 2% of patients included chalazion (meibomian cyst)/hordeolum and punctate keratitis.
Lotinaler ophthalmic solution contains potassium sorbate, which may cause soft contact lens discoloration.
Remove contact lenses prior to instillation of lotilaner ophthalmic solution. They may be reinserted 15 minutes after its administration.
Advise patients to consult with their healthcare provider if they develop any intercurrent ocular conditions (ocular trauma, ocular infection), have ocular surgery, or develop any ocular reactions (conjunctivitis, eyelid reactions).
There are no available data on the use of lotilaner ophthalmic solution during pregnancy to inform on any drug associated risk; however, systemic exposure for ocular administration is low. In animal studies, lotilaner did not produce malformations at clinically relevant doses.
There are no data on the presence of lotilaner ophthalmic solution in human breast milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure after 6 weeks of topical ocular administration is low. Lotilaner is more than 99% plasma protein bound; it is not known whether measurable concentrations of lotilaner would be present in maternal milk after ocular administration. The developmental and health benefits of breast-feeding should be considered along with the clinical need and any potential adverse effects on the breastfed child.
Per the manufacturer, this drug has been shown to be active against most strains of the following microorganisms either in vitro and/or in clinical infections: Demodex brevis, Demodex folliculorum
NOTE: The safety and effectiveness in treating clinical infections due to organisms with in vitro data only have not been established in adequate and well-controlled clinical trials.
For the treatment of Demodex blepharitis:
Ophthalmic dosage:
Adults: Instill 1 drop in each eye twice daily (approximately 12 hours apart) for 6 weeks.
Maximum Dosage Limits:
-Adults
2 drops per eye daily.
-Geriatric
2 drops per eye daily.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Lotilaner products.
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.
Lotilaner is administered topically to the eye. It is more than 99% bound to human plasma proteins. The partitioning of lotilaner to human blood cells is approximately 10% (range, 0% to 20%). The effective half-life in healthy subjects, which is based on the accumulation ratio over the dosing interval of 12 hours, is 264 hours (11 days). Lotilaner is not metabolized by CYP enzymes.
Affected cytochrome P450 isoenzymes and transporters: none
-Route-Specific Pharmacokinetics
Other Route(s)
Ophthalmic Route
Maximum lotilaner concentrations were observed 2 hours after a single ocular administration on day 1 and 1 hour after the last drug administration on day 42. In healthy subjects, the peak concentration (Cmax) and total exposure (AUC0-12) in whole blood increased after 42 days of repeated ocular administration from 0.596 ng/mL to 17.8 ng/mL and from 5.75 hr x ng/mL to 149 h x ng/mL for Cmax and AUC respectively. In patients with Demodex blepharitis who received lotilaner twice daily for 42 days, the mean systemic exposure at the end of treatment was 12 ng/mL (range, 0.4 to 45.1 ng/mL).