lotilaner ophthalmic (Rx)

1-10%

Stinging and burning (10%)

Chalazion (<2%)

Hordeolum (<2%)

Punctate keratitis (<2%)

Contraindications

None

Cautions

Remove contact lenses before instillation; may reinsert 15 minutes after administration

In the event of intercurrent ocular condition (eg, trauma or infection), ocular surgery, or ocular reactions, particularly conjunctivitis and eyelid reactions, contact healthcare practitioner for advice concerning continued use

Contaminated solution

• Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions
• To minimize contamination, do not allow tip of dispensing container to contact the eye, surrounding structures, fingers, or any other surface

Pregnancy

There are no available data on use in pregnant females to inform any drug associated risk; however, systemic exposure to lotilaner from ocular administration is low

Animal reproduction studies did not produce malformations at clinically relevant doses

Lactation

There are no data on presence of lotilaner in human milk, effects on breastfed infants, or effects on milk production

Systemic exposure to lotilaner following 6 weeks of topical ocular administration is low, and drug is >99% protein bound in plasma; therefore, it is unknown whether measurable levels would be present in maternal milk following topical ocular administration

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

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 (~1100 times the recommended human ophthalmic dose)

Pharmacokinetics

Systemic exposure was evaluated in patients at the end of 6 weeks of treatment

Absorption

• Peak plasma concentration: 0.596-17.8 ng/mL
• AUC 5.75-149 hr⋅ng/mL
• Mean systemic exposure: 12 ng/mL

Distribution

• Protein bound: >99.9% (in plasma)
• Partitioning to blood cell: ~10%

Metabolism

• Not metabolized by CYP enzymes

Elimination

• Half-life: 264 hr (11 days)

Ophthalmic Administration

For ophthalmic use only

To minimize contamination of solution, do not allow eye drop container tip to contact the eye, surrounding structures, fingers, or any other surface

If >1 topical ophthalmic drug is being used, administer at least 5 minutes apart

Contact lenses: Removed before instilling eye drops; may reinsert 15 minutes after administration

Missed dose: Continue treatment with next scheduled dose

Storage

Store at 15-25ºC (59-77ºF)

After bottle is opened, may be use until expiration date on bottle