tacrolimus (topical)

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

Contraindicated in:

Hypersensitivity to tacrolimus or any component of the ointment;
Weakened/compromised immune system;
Malignant or premalignant skin conditions;
Lactation: Lactation;
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 during pregnancy only if potential maternal benefit justifies potential fetal risk.

Adv. Reactions/Side Effects ⬆ ⬇

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

EENT: pharyngitis, sinusitis

Local: burning

MS: back pain, myalgia

Neuro: headache

Resp: cough

Misc: flu-like symptoms, fever, MALIGNANCY

Interactions ⬆ ⬇

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

Drug-drug:

↑risk of nephrotoxicity with aminoglycosides, amphotericin B, cisplatin, nucleotide reverse transcriptase inhibitors, protease inhibitors, or cyclosporine (allow 24 hr to pass after stopping cyclosporine before starting tacrolimus).
Potassium-sparing diuretics, ACE inhibitors, or angiotensin II receptor antagonists↑ risk of hyperkalemia.
Strong CYP3A4 inhibitors, including chloramphenicol, clarithromycin, cobicistat, itraconazole, ketoconazole, letermovir, nefazodone, posaconazole, protease inhibitors, and voriconazole, may significantly ↑ levels and risk of nephrotoxicity; ↓ tacrolimus dose by ../B/tu0.png when used with voriconazole or posaconazole; closely monitor tacrolimus whole blood trough concentrations
Mild CYP3A4 inhibitorsand moderate CYP3A4 inhibitors, including amiodarone, calcium channel blockers, cimetidine, clotrimazole, danazol, erythromycin, ethinyl estradiol, fluconazole, imatinib, isavuconazonium, lansoprazole, nilotinib, and omeprazole, may ↑ levels and risk of toxicity; closely monitor tacrolimus whole blood trough concentrations and adjust tacrolimus dose if needed.
Magnesium/aluminum hydroxide and metoclopramide may ↑ levels and risk of toxicity; closely monitor tacrolimus whole blood trough concentrations and adjust tacrolimus dose if needed.
Strong CYP3A4 inducers, including carbamazepine, phenobarbital, phenytoin, rifabutin, and rifampin, may ↓ levels; ↑ tacrolimus dose and closely monitor tacrolimus whole blood trough concentrations.
Mild CYP3A4 inducers and moderate CYP3A4 inducers, including methylprednisolone or prednisone, may ↓ levels; closely monitor tacrolimus whole blood trough concentrations and adjust tacrolimus dose if needed.
Vaccinations may be less effective if given concurrently with tacrolimus (avoid use of live-virus vaccines).
May ↑ levels of mycophenolate mofetil or mycophenolic acid.
Caspofungin may ↓ levels; closely monitor tacrolimus whole blood trough concentrations and adjust tacrolimus dose if needed.

Drug-Natural Products:

Concomitant use with astragalus, echinacea, and melatonin may interfere with immunosuppression.
St. John's wort may ↓ levels; ↑ tacrolimus dose and closely monitor tacrolimus whole blood trough concentrations.
Schisandra sphenanthera may significantly ↑ levels; closely monitor tacrolimus whole blood trough concentrations.

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.

Availability ⬆ ⬇

(Generic available)

Ointment: 0.03%; 0.1%

Assessment ⬆ ⬇

Atopic Dermatitis: Assess skin lesions prior to and periodically during therapy.
- Use only for short time, not continuously, and in the minimum dose possible to decrease risk of developing skin cancer.

Implementation ⬆ ⬇

Do not confuse tacrolimus with tamsulosin.
Do not use continuously for a long time.
Topical Wash hands before applying. Apply a thin layer of ointment twice daily to affected skin. Use smallest amount of ointment needed to control the signs and symptoms of eczema. Do not cover treated area with bandages, dressings, or wraps. If not treating areas on hands, wash hands with soap and water after applying to remove any ointment on hands.

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 if they develop a skin infection.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy.
- 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.
- Inform patient of the risk of lymphoma or skin cancer with topical tacrolimus therapy.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇