Tacrolimus ointment

PROTOPIC

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Pronunciation: ta-KROE-li-mus (proe-TOP-ik)

Tacrolimus ointment ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Tacrolimus ointment ballicule

What it isTopical calcineurin inhibitor that suppresses T-cell inflammation; moderate to severe atopic dermatitis.

Why this oneMore potent than pimecrolimus, it is the stronger steroid-sparing choice for face, eyelids, and folds.

What limits itBurning often ends the trial; avoid active infection and excessive UV exposure, and discuss the boxed malignancy warning.

Tacrolimus ointment molecular structure (skeletal formula) — Molecular structure: Tacrolimus ointment

Classes and tags

Clinical profile

Therapeutic safety burden4 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityApplication-site burning and itching. Boxed: long-term safety is not established and rare skin cancer and lymphoma have been reported (causality not established), so avoid continuous long-term use and treat only affected skin; not under age 2.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Long-term safety of topical calcineurin inhibitors not established; rare cases of malignancy (skin, lymphoma) reported. Avoid continuous long-term use; limit application to areas of involvement. Not indicated for children under 2 years; only 0.03% is indicated for children 2-15 years.

FDA dosing	Population	Start	Target	Max
Moderate to severe atopic dermatitis (second-line, short-term/intermittent)	Adults (0.03% or 0.1%)	Apply thin layer BID	Thin layer BID to affected skin	Apply BID
Moderate to severe atopic dermatitis (second-line, short-term/intermittent)	Children 2-15 y (0.03% only)	Apply thin layer BID	Thin layer BID to affected skin	Apply BID

Renal No adjustment needed (dose adjustment not expected to be needed)

Hepatic No adjustment needed (dose adjustment not expected to be needed)

Continuous long-term use should be avoided; limit to areas of atopic dermatitis involvement

Instructions

Apply a thin layer to affected skin twice daily; rub in gently and completely
Stop use when signs and symptoms resolve; re-examine if no improvement within 6 weeks
Do not use with occlusive dressings
Minimize/avoid natural or artificial sunlight
Avoid eyes and mouth; wash hands after application (if not treating hands)
Not for immunocompromised patients; avoid on pre-malignant/malignant skin

Available strengths

ointment 0.03, 0.1 %
cap 0.5, 1, 5 mg
ER cap 0.5, 1, 5 mg
ER tab 0.75, 1, 4 mg
susp 0.2, 1 mg/packet
inj 5 mg/mL

Cautions

Local skin burning, stinging, pruritus
Bacterial and viral skin infections (resolve before treatment; risk of varicella zoster, herpes simplex, eczema herpeticum)
Lymphadenopathy — investigate etiology
Sun exposure — minimize/avoid
Not studied in immunocompromised patients or generalized erythroderma
Rare post-marketing acute renal failure; caution in patients predisposed to renal impairment

Adverse reactions

Skin burning
Pruritus
Flu-like symptoms
Skin erythema
Headache
Skin infection

Pregnancy Pregnancy Category C — use only if potential benefit justifies potential risk to the fetus

Lactation Tacrolimus excreted in human milk; decide whether to discontinue nursing or drug

Cost

Tacrolimus ointment (PROTOPIC)

Strength		#/mo	generic $/unit	CostPlus
0.03 %	ointment	per unit		not offered
0.1 %	ointment	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Tacrolimus ointment is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Other forms: Tacrolimus (PROGRAF)

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Self-check

How does topical tacrolimus potency compare with pimecrolimus?
More potent.
What local adverse effect often ends a topical tacrolimus trial?
Burning.