Azelaic Acid 15% | Ketotifen 0.05% | Oxymetazoline HCl 0.06%

Applied topically as a thin layer to the affected areas of the face per prescriber instruction:

• Cleanse and dry the face before application.
• Apply a thin, even layer to affected areas (cheeks, nose, chin, forehead) and gently massage in; avoid eye area, eyelids, and mucous membranes.
• Wash hands before and after application.
• Avoid applying to open wounds or irritated skin.
• Patients should be counseled that oxymetazoline may cause transient rebound redness if discontinued abruptly after prolonged use, particularly with higher concentrations.

Dosing frequency is prescriber-determined. General principles:

• Azelaic acid 15% is typically used twice daily (morning and evening) in its FDA-approved commercial form for rosacea (Finacea).
• Oxymetazoline 0.06% (comparable to the FDA-approved Rhofade at 1%) is typically applied once daily for erythema management.
• Ketotifen at 0.05% topically is a compounded strength; the prescriber determines frequency based on individual inflammatory burden.
• Final dosing, frequency, and duration are prescriber-directed; follow-up at 4–8 weeks to assess response and tolerability.

• Azelaic Acid: Reduces reactive oxygen species generated by neutrophils and Demodex folliculorum; inhibits serine protease activity (kallikrein-5) that activates cathelicidins implicated in rosacea pathogenesis; provides antimicrobial activity against commensal bacteria contributing to follicular inflammation; normalizes aberrant keratinocyte differentiation.
• Ketotifen: Stabilizes mast cell membranes, inhibiting degranulation and release of histamine, prostaglandins, and leukotrienes; also competitively antagonizes H1 receptors in skin vasculature, reducing histamine-mediated vasodilation and neurogenic inflammation associated with flushing.
• Oxymetazoline HCl: Acts on alpha-1A and partial alpha-2 adrenergic receptors on cutaneous blood vessels, causing smooth muscle contraction and direct vasoconstriction of superficial dermal vasculature, reducing visible erythema without systemic vasopressor effect at topical doses.

This combination is prescribed for prescriber-directed management of erythematotelangiectatic and papulopustular rosacea, with a multi-mechanism approach targeting the three predominant pathophysiologic contributors: inflammation, vascular reactivity, and mast cell/histamine-mediated flushing. Clinical considerations:

• Azelaic acid 15% has FDA approval for rosacea in its Finacea foam formulation; the compounded 15% gel/cream is a patient-specific alternative.
• Oxymetazoline 1% is FDA-approved (Rhofade) for facial erythema; the 0.06% compounded concentration is a lower-strength prescriber-directed variation.
• Ketotifen topical use is off-label; prescribers should document rationale for inclusion in this formulation.
• Monitor for rebound erythema or tachyphylaxis with prolonged oxymetazoline use; schedule periodic assessments of continued need.
• Azelaic acid may cause transient stinging or burning, particularly on sensitive rosacea-prone skin; counsel patients on expected initiation reactions.
• Reinforce general rosacea trigger management: UV protection, avoidance of heat, spicy food, and alcohol.

Contraindications:

• Hypersensitivity to azelaic acid, ketotifen, oxymetazoline, or any formulation component.
• Concurrent use of monoamine oxidase inhibitors (MAOIs) — oxymetazoline (sympathomimetic) may interact.

Warnings & Precautions:

• Oxymetazoline: avoid contact with eyes; systemic absorption through mucous membranes (nasal or ocular) may cause cardiovascular effects; use with caution in hypertension, angina, or severe cardiovascular disease.
• Azelaic acid: transient stinging, burning, and pruritus are common, especially on sensitized rosacea skin.
• Rebound erythema may occur with abrupt discontinuation of prolonged oxymetazoline therapy; prescriber-directed tapering may be advisable.
• Not for use on eyelids or near the eye.

Drug Interactions:

• Oxymetazoline with MAOIs or tricyclic antidepressants: risk of potentiated sympathomimetic effects.
• Beta-blockers may reduce or blunt vascular response to oxymetazoline.

Common Side Effects: Transient application site burning or stinging (azelaic acid); application site pallor or mild paresthesia (oxymetazoline vasoconstriction); pruritus; erythema if discontinued.

Store at controlled room temperature (15–25°C / 59–77°F). Protect from light and heat. Keep in original container with lid tightly closed. Do not freeze. Keep out of reach of children. Use by the beyond-use date (BUD) per USP <795> standards. Discard if discoloration or phase separation occurs.

Is this preparation FDA-approved?

No. This is a patient-specific, prescriber-directed 503A compounded preparation from Genesis Compounding. While the individual ingredients have FDA-approved commercial counterparts (azelaic acid 15% gel/foam for rosacea; oxymetazoline 1% cream for erythema), this compounded combination at these specific concentrations is not FDA-approved.

Why are all three ingredients needed?

Rosacea involves multiple concurrent pathophysiologic pathways — chronic skin inflammation, cutaneous vascular reactivity, and mast cell/histamine-mediated flushing. Each ingredient addresses a different pathway: azelaic acid targets inflammation and microbial triggers; oxymetazoline directly constricts facial blood vessels; ketotifen stabilizes mast cells and blocks histamine-driven flushing.

What is the oxymetazoline component doing?

Oxymetazoline is an alpha-adrenergic agonist that causes vasoconstriction of the superficial blood vessels in the face, reducing the persistent redness visible in erythematotelangiectatic rosacea. The effect is direct and localized to the application site.

Can I stop using this suddenly?

Gradual tapering rather than abrupt discontinuation may be advisable for the oxymetazoline component, as rebound erythema can occur. Discuss any plan to discontinue with your prescriber.

How long before I see improvement?

Vasoconstriction from oxymetazoline is apparent within 30–60 minutes of application. Anti-inflammatory effects from azelaic acid typically require 4–8 weeks of consistent use. Full composite benefit may take 8–12 weeks; your prescriber will reassess at follow-up visits.