Ketotifen 0.05% | Oxymetazoline 1% | Tea Tree Oil 5%

Route: Topical periocular/eyelid margin application. Apply carefully along the eyelid margin and lash bases using a clean applicator (cotton-tipped swab or provided applicator). Keep eyes closed during application. Do not allow to enter the eye. Wash hands before and after. The 1% oxymetazoline concentration is higher than commercially available formulations; apply only the quantity and frequency directed by the prescriber.

Dosing is entirely prescriber-determined:

• Application frequency (typically once to twice daily) and treatment duration are specified by the prescriber.
• Given the higher oxymetazoline concentration (1%), prescribers should specify treatment duration carefully to balance therapeutic benefit against rebound vasodilation risk with extended use.
• Demodex eradication requires a minimum of 6–8 weeks of consistent application.

• Ketotifen 0.05%: Non-competitive H1 receptor antagonist and mast cell stabilizer that inhibits histamine, leukotriene, and PAF-mediated allergic and inflammatory cascades in periocular tissue.
• Oxymetazoline 1%: At this higher concentration, oxymetazoline produces greater fractional occupancy of alpha-1A adrenoceptors (Gq-coupled, activating phospholipase C, increasing intracellular Ca²⁺) and alpha-2B adrenoceptors (Gi-coupled, inhibiting adenylyl cyclase) on periocular vascular smooth muscle, resulting in more potent vasoconstriction and more pronounced reduction in eyelid erythema and conjunctival injection. Greater receptor occupancy also increases the potential for rebound vasodilation upon discontinuation (tachyphylaxis/dependence mechanism).
• Tea Tree Oil 5%: Terpinen-4-ol — the primary bioactive — disrupts Demodex mite cellular membranes, inhibits mite acetylcholinesterase, and reduces pro-inflammatory cytokine production (TNF-α, IL-1β) from human monocytes at the application site.

This higher-oxymetazoline formulation is directed by the prescribing clinician toward patients with more prominent vascular eyelid erythema or conjunctival hyperemia in the context of Demodex blepharitis or allergic periocular disease where the 0.06% formulation provides insufficient vasoconstrictive effect. The prescriber should carefully weigh the indication for the higher concentration.

Monitoring: Eyelid margin erythema and Demodex mite density (epilation and microscopic counting); intraocular pressure (oxymetazoline's mild mydriatic effect may elevate IOP in narrow-angle glaucoma patients); skin tolerance and contact sensitization; rebound erythema upon discontinuation.

Contraindications:

• Known hypersensitivity to any component.
• Narrow-angle glaucoma.
• Concurrent MAOI therapy.

Warnings & Precautions:

• The 1% oxymetazoline concentration exceeds commercially available ophthalmic/dermatologic formulations; systemic absorption risk and rebound vasodilation risk are higher than at 0.06%. Limit application to the prescribed area and duration.
• Tea tree oil: do not allow to enter the eye; risk of contact sensitization with oxidized product.
• Cardiovascular effects: oxymetazoline systemic absorption from periocular application may affect heart rate and blood pressure in patients with cardiovascular disease or those taking antihypertensives.

Drug Interactions:

• MAOIs: contraindicated with oxymetazoline — risk of hypertensive crisis.
• Tricyclic antidepressants and beta-blockers: potential interaction with adrenergic component.

Common Side Effects: Local stinging or burning upon application; eyelid erythema; rebound vasodilation with extended use of oxymetazoline 1%; contact sensitization from tea tree oil.

Store at room temperature (15°C–25°C), protected from light, heat, and air. Keep container tightly closed. Tea tree oil oxidizes on air exposure, increasing sensitization risk. Do not freeze. Use within the beyond-use date specified by Genesis Compounding.

Why is this formula different from the 0.06% oxymetazoline version?

The 1% oxymetazoline concentration produces greater vasoconstriction of periocular vasculature, making it appropriate for patients with more pronounced eyelid or conjunctival erythema. The prescriber selects the concentration based on severity of vascular involvement.

Is the 1% oxymetazoline concentration safe for periocular use?

At prescriber-directed doses applied to the eyelid margin only, systemic absorption is expected to be low. However, the higher concentration carries a greater risk of rebound erythema and requires careful prescriber oversight of treatment duration. Report any changes in blood pressure, heart rate, or vision to your prescriber.

How long do I need to use this?

Treatment duration is prescriber-determined. Demodex eradication requires at least 6–8 weeks. Your prescriber will specify the duration and any maintenance schedule.

Is this FDA-approved?

No. This is a patient-specific, prescriber-directed 503A compounded preparation from Genesis Compounding, not FDA-approved as a compounded drug.

What should I do if the preparation gets into my eyes?

Flush immediately with copious amounts of clean water for at least 15 minutes and contact your prescriber. Tea tree oil is a direct ocular irritant.