tacrolimus (topical)

Contraindicated in:

Hypersensitivity to tacrolimus or any component of the ointment;
Weakened/compromised immune system;
Malignant or pre-malignant skin conditions;
Lactation: Breastfeeding should be avoided;
Pedi: Children <2 yr (safety not established).

Use Cautiously in:

Exposure to sunlight/UV light (may ↑risk of malignant skin changes);
Superficial skin infections;
OB: Hyperkalemia and renal impairment may occur in the newborn; use only if benefit to mother justifies risk to the fetus.

Adv. Reactions/Side Effects ⬆ ⬇

EENT: sinusitis

Neuro: headache

Resp: cough, pharyngitis

Derm: erythema, pruritis, skin infection, acne, folliculitis, rash

Local: burning

MS: back pain, myalgia

Misc: flu-like symptoms, fever, ↑risk of lymphoma/skin cancer

Interactions ⬆ ⬇

Noted primarily for PO and IV use, but should be considered for topical use

Drug-drug:

Risk of nephrotoxicity is ↑ by concurrent use of aminoglycosides, amphotericin B, cisplatin, or cyclosporine (allow 24 hr to pass after stopping cyclosporine before starting tacrolimus).
Concurrent use of potassium-sparing diuretics, ACE inhibitors, or angiotensin II receptor antagonists↑ risk of hyperkalemia.
The following drugs ↑ tacrolimus blood levels: azole antifungals, bromocriptine, calcium channel blockers, chloramphenicol, cimetidine, clarithromycin, cyclosporine, danazol, erythromycin, lansoprazole, magnesium/aluminum hydroxidemethylprednisolone, omeprazole, nefazodone, metoclopramide, protease inhibitors, and voriconazole.
Phenobarbital, phenytoin, caspofungin, sirolimuscarbamazepine, and rifamycins may ↓ tacrolimus blood levels.
Vaccinations may be less effective if given concurrently with tacrolimus (avoid use of live-virus vaccines).

Drug-Natural Products:

Concomitant use with astragalus, echinacea, and melatonin may interfere with immunosuppression.
St. John's wort may ↓ tacrolimus blood levels.

Availability ⬆ ⬇

(Generic available)

Ointment: 0.03%; 0.1%

Route/Dosage ⬆ ⬇

(Adults ): Apply 0.03% or 0.1% ointment twice daily. Discontinue when signs/symptoms of atopic dermatitis resolve.
(Children ≥2–15 yr): Apply 0.03% ointment twice daily. Discontinue when signs/symptoms of atopic dermatitis resolve.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits T-lymphocyte activation.

Therapeutic effects:

Improvement in signs/symptoms of atopic dermatitis.

Classifications ⬆ ⬇

Therapeutic Classification: Immunosuppressant agents

Pharmacokinetics ⬆ ⬇

Absorption: Minimal following topical use.

Distribution: Crosses the placenta and enters breast milk.

Protein Binding: 99%.

Metabolism/Excretion: 99% metabolized by the liver; <1% excreted unchanged in the urine.

Half-Life: Healthy volunteers—21.2 hr.

Time/Action Profile ⬆ ⬇

(immunosuppression)

ROUTE	ONSET	PEAK	DURATION
Topical‡	unknown	1–2 wk	unknown

‡Improvement in atopic dermatitis.

Patient/Family Teaching ⬆ ⬇

Instruct apply ointment as directed. Advise patient to read the Medication Guide prior to starting and with each Rx renewal; new information may be available.
Advise patient not to bathe, shower, or swim right after applying; may wash off ointment. May use moisturizers with ointment. Instruct patient to check with health care professional first about products to use. If moisturizers are used, apply them after application of ointment.
Advise patient to contact health care professional if their symptoms do not improve after 6 wk of treatment, if their symptoms get worse, or they develop a skin infection.
- Instruct patient to use ointment only on areas of skin with atopic dermatitis.
- Advise patient to stop using the ointment when the signs/symptoms of atopic dermatitis (itching, rash, redness) go away.
- Advise patient to limit sun exposure during therapy.
- Advise patient of the risk of using topical tacrolimus during pregnancy.
- Inform patient of the risk of lymphoma or skin cancer with topical tacrolimus therapy.

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Indications ⬇

Contraind./Precautions ⬆ ⬇