PROTOPIC 0.1% OINTMENT 60G

Indications

Approved Uses

Second-line treatment of moderate-to-severe atopic dermatitis (eczema) in patients who are not adequately responsive to, or when use of, conventional topical therapies (e.g., topical corticosteroids) is not advisable; Protopic 0.1% is for adults and adolescents ≥16 years.

Dosage & Administration

Dosing by Condition

Atopic dermatitis flare: apply a thin layer twice daily to affected areas until lesions clear. Maintenance (proactive) therapy: after clearance, apply twice weekly (e.g., 2 non-consecutive days) to previously affected areas to reduce flares. Age/strength: 0.1% is for ≥16 years; ages 2-15 years should use 0.03% twice daily.

Initial Dose

Apply a thin layer to the affected skin twice daily (morning and evening).

Maintenance Dose

Apply a thin layer once daily, twice weekly (with 2-3 days between applications) to areas commonly affected by atopic dermatitis.

Maximum Dose

No defined maximum dose; apply a thin layer to affected areas only and avoid continuous long-term use.

Children's Dosage

Children 2-15 years: 0.03% strength only, apply thin layer twice daily to affected areas. Children 16 years and above: 0.1% strength may be used as per adult dosing. Not approved under 2 years of age

Dose Adjustment Notes

No routine dose adjustment is required for renal/hepatic impairment or in the elderly with topical use due to low systemic absorption; avoid use on significant skin barrier defects (e.g., Netherton syndrome) or very large areas where absorption may increase, and use the minimum amount for the shortest duration needed.

How to Take

Apply a thin layer to affected skin twice daily and rub in gently; use on clean, dry skin. Wash hands after application unless treating the hands. Avoid contact with eyes and mucous membranes. Do not use under occlusive dressings/bandages.

Side Effects

Common Side Effects

Application-site burning/stinging, pruritus, erythema; folliculitis/acne; skin infections (e.g., herpes simplex/impetigo) can occur; alcohol-related facial flushing may occur.

Side Effect Frequency

Very common (>10%): application-site burning and pruritus. Common (1-10%): application-site erythema/pain/tingling, folliculitis/acne, herpes simplex/other skin infections, alcohol intolerance (facial flushing).

Safety & Warnings

Contraindications

Contraindication: hypersensitivity to tacrolimus or any component of the formulation.

Warnings & Precautions

Avoid continuous long-term use; limit to affected areas; avoid use on malignant/premalignant lesions; minimize sun/UV exposure (including phototherapy/tanning beds); do not apply to active infections-treat first; avoid occlusion; avoid use in immunocompromised patients; avoid eyes/mucosa and wash hands after application.

Age Restriction

Not approved for children <2 years; Protopic 0.1% is indicated for patients ≥16 years (0.03% is used for ages 2-15).

Driving Warning

Safe

Drug Interactions

Food Interaction

No clinically relevant food interactions (not applicable for topical use).

Alcohol Interaction

Avoid

Special Populations

Pregnancy

Consult Doctor

Breastfeeding

Consult Doctor

Children

Children 2-15 years: 0.03% strength only, apply thin layer twice daily to affected areas. Children 16 years and above: 0.1% strength may be used as per adult dosing. Not approved under 2 years of age

Elderly

Standard adult dosing; no specific dose adjustment required

Kidney Impairment

No dose adjustment needed for topical use.

Storage & Patient Advice

Storage Conditions

Do not store above 25°C; do not freeze; keep the tube tightly closed (in original container).

Stopping the Medicine

Stop when signs/symptoms resolve; no taper is required; for patients with frequent relapses, proactive maintenance (e.g., twice weekly) may be used to reduce flares.

Overdose

Topical overdose is unlikely; if ingested, seek immediate medical attention-systemic tacrolimus toxicity may include tremor, headache, nausea/vomiting; management is supportive.

Patient Counseling

Apply a thin layer to affected areas twice daily (0.1% only for ≥16 years); rub in gently and wash hands after use. Expect transient burning/stinging/itching early in therapy. Avoid eyes/mucosa and do not cover with occlusive dressings. Minimize sun/UV exposure (avoid tanning beds/phototherapy on treated areas) and use sun protection. Alcohol may cause facial flushing. Use the smallest amount for the shortest time needed; seek medical advice for signs of skin infection, swollen lymph nodes, unusual/new skin lesions, or lack of improvement (reassess if not improving within ~2 weeks; reevaluate if not improved by ~6 weeks).

Monitoring Requirements

No routine laboratory monitoring is required. Clinically monitor response and tolerability; reassess if no improvement within ~2 weeks and discontinue/reevaluate if not improved by ~6 weeks. Monitor for signs of skin infection, lymphadenopathy, and new or changing skin lesions with ongoing/intermittent long-term use.

Pharmacology

Mechanism of Action

Topical tacrolimus is a calcineurin inhibitor: it binds FKBP-12, inhibiting calcineurin phosphatase, thereby reducing T-cell activation and downstream pro-inflammatory cytokine transcription (e.g., IL-2) and decreasing cutaneous inflammation and pruritus.

Onset of Action

Some improvement is often seen within about 1 week; more meaningful improvement typically occurs over 1-2 weeks, with continued gains over several weeks.

Duration of Effect

Benefit persists only with continued/proactive use; disease commonly relapses after discontinuation, with flares potentially returning within days to weeks depending on baseline severity.

Bioavailability

Very low systemic bioavailability after topical use (generally <0.5% through intact skin; absorption can increase when applied to inflamed/eroded skin or large body surface areas).

Metabolism

If absorbed systemically, tacrolimus is extensively metabolized primarily by CYP3A4 (and also CYP3A5), mainly in the liver (and intestinal wall).

Protein Binding

>98% protein binding (often cited ~98.8-99%) when systemically present, mainly to albumin and alpha-1-acid glycoprotein.

Product Information

Available Dosage Forms

Ointment

Composition per Dose

Each gram of ointment: 1 mg tacrolimus (as monohydrate) in a white petrolatum-based ointment

OTC Alternatives

No OTC calcineurin inhibitor alternative exists. OTC options for mild disease/supportive care include regular emollients/moisturizers (e.g., petrolatum, ceramide creams) and short courses of low-potency OTC hydrocortisone 0.5-1% for mild flares (if appropriate).

Skin Condition

Eczema

Steroid Potency

N/A - not a corticosteroid

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