Tacrolimus 0.12% | Ketotifen 0.05% | Zinc Pyrithione 0.2%

Route: Topical application to affected skin (scalp, face, intertriginous areas).

• Apply a thin layer to affected area(s) once or twice daily as directed by the prescriber.
• For scalp use: part hair and apply to affected skin; allow to absorb for at least 15–30 minutes before washing or styling.
• Wash hands before and after application unless hands are the treatment area.
• Avoid eyes, mucous membranes, and open wounds.
• Do not occlude unless specifically directed.
• Protect treated areas from direct UV exposure; use sunscreen or covering.

Applied topically once or twice daily to affected skin as directed by the prescriber. Treatment duration is individualized. For seborrheic dermatitis, intermittent maintenance use after initial clearance is common. The prescribing clinician determines frequency and duration based on disease severity, location, and response.

• Tacrolimus: Inhibits calcineurin by forming a complex with FKBP-12, preventing NFAT dephosphorylation and nuclear translocation → reduced transcription of Th1/Th2 pro-inflammatory cytokines (IL-2, IL-3, IL-4, IL-5, TNF-α, IFN-γ) in activated T lymphocytes and FcεRI-stimulated mast cells. Provides profound topical immunosuppression without the atrophogenic effects of corticosteroids.
• Ketotifen: Competitively and selectively antagonizes H1 histamine receptors in skin, reducing histamine-induced vasodilation, pruritus, and wheal-flare responses; independently inhibits calcium influx into mast cells triggered by IgE-receptor cross-linking, preventing degranulation and release of preformed (histamine, tryptase) and newly synthesized (leukotrienes C4/D4, prostaglandin D2) inflammatory mediators. This dual mechanism provides both acute symptom relief (antihistamine) and disease-modifying activity (mast cell stabilization).
• Zinc Pyrithione: Acts as a lipophilic zinc ionophore; once absorbed into fungal cells, dissociates to release free zinc ions that inhibit mitochondrial electron transport chain complex II, cause mitochondrial membrane potential collapse, disrupt copper/iron homeostasis, and overwhelm fungal antioxidant defenses—leading to Malassezia cell death. Also suppresses lipase gene expression in Malassezia, reducing the production of oleic acid and other irritant free fatty acids that drive barrier disruption and T-cell recruitment in seborrheic dermatitis.

Indication context: This triple combination is prescribed for refractory inflammatory dermatoses with an overlapping seborrheic/fungal component, particularly: moderate-to-severe seborrheic dermatitis (scalp, face, chest), mixed seborrheic-atopic dermatitis, and patients with significant pruritus and Malassezia-associated inflammation who have inadequate response to single-ingredient therapies. The formulation targets all three major pathophysiologic drivers simultaneously: T-cell inflammation (tacrolimus), mast cell/histamine (ketotifen), and Malassezia/sebum (zinc pyrithione).

Monitoring:

• Assess clinical response (erythema, scale, pruritus) at 2–4 weeks.
• Monitor for application site reactions (burning, stinging) from tacrolimus—typically transient.
• Check for signs of secondary skin infection; tacrolimus and ketotifen can mask inflammation from superimposed infection.
• Long-term use: see tacrolimus black box warning guidance; periodic clinical review and documentation of continued indication.

Contraindications:

• Hypersensitivity to tacrolimus, ketotifen, zinc pyrithione, or any excipient.
• Active cutaneous infections at application site; treat before initiating.
• Netherton syndrome or severely impaired skin barrier (risk of increased tacrolimus systemic absorption).
• Not for use in children under 2 years.

Warnings & Precautions:

• FDA Black Box Warning (class—topical calcineurin inhibitors): Avoid continuous long-term use; theoretical risk of lymphoma and skin malignancy; not for use in immunocompromised patients.
• UV exposure: avoid on treated areas; recommend protective clothing or broad-spectrum sunscreen.
• Alcohol: flushing/irritation may occur in tacrolimus-treated areas after alcohol consumption.
• Viral infections (HSV, VZV): monitor for cutaneous viral infections in chronically treated areas.

Drug Interactions:

• Systemic CYP3A4 inhibitors (azole antifungals, macrolide antibiotics) could theoretically increase tacrolimus systemic exposure if skin barrier is impaired; monitor clinically if prescribed concurrently.

Common Side Effects: Burning and stinging at application site (transient, most common); pruritus (initially); skin erythema; folliculitis; alcohol-related flushing in treated areas.

Store at room temperature (15–25°C). Do not freeze. Protect from light and heat. Keep tightly capped. Use within the beyond-use date assigned by Genesis Compounding per USP <795> guidelines. Keep out of reach of children.

Why are three ingredients combined in this preparation?

Seborrheic dermatitis and mixed inflammatory dermatoses involve multiple pathways: T-cell-mediated skin inflammation, mast cell activation and histamine release, and Malassezia yeast overgrowth. Each ingredient in this preparation targets one pathway specifically—tacrolimus for T-cell inflammation, ketotifen for mast cell/histamine activity, and zinc pyrithione for Malassezia. Single-ingredient therapies rarely address all three simultaneously.

Can this be used on the scalp?

Yes. This formulation can be applied to the scalp for seborrheic dermatitis. Part the hair, apply to affected areas, and allow adequate contact time before rinsing or styling. Your prescriber will provide specific application instructions.

Will this cream thin my skin?

Tacrolimus, unlike corticosteroids, does not cause skin atrophy, striae, or telangiectasia, making it well-suited for long-term use in sensitive areas such as the face and scalp.

Is this FDA-approved?

Tacrolimus ointment (Protopic) and ketotifen ophthalmic drops (Zaditor) are FDA-approved in separate formulations. Zinc pyrithione is available in OTC dandruff products. This three-ingredient topical combination is a patient-specific 503A compounded preparation from Genesis Compounding and requires a valid prescriber order.