Medically reviewed on Nov 15, 2018
(ta KROE li mus)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Protopic: 0.03% (30 g, 60 g, 100 g); 0.1% (30 g, 60 g, 100 g)
Generic: 0.03% (30 g, 60 g, 100 g); 0.1% (30 g, 60 g, 100 g)
Brand Names: U.S.
- Calcineurin Inhibitor
- Immunosuppressant Agent
- Topical Skin Product
Suppresses cellular immunity (inhibits T-lymphocyte activation), by binding to an intracellular protein, FKBP-12 and complexes with calcineurin dependent proteins to inhibit calcineurin phosphatase activity
Minimally absorbed; serum concentrations range from undetectable to 20 ng/mL (~2 ng/mL in majority of adult patients studied)
Use: Labeled Indications
Moderate to severe atopic dermatitis: Treatment of moderate to severe atopic dermatitis in immunocompetent patients not responsive to conventional therapy or when conventional therapy is not appropriate
Off Label Uses
Atopic dermatitis (maintenance therapy)
Guidelines support use of topical calcineurin inhibitors, including tacrolimus, as maintenance to prevent flares and extend flare free intervals in children and adults with moderate to severe atopic dermatitis who responded to initial therapy [Schneider 2012].
Oral lichen planus
Data from controlled trials demonstrate that tacrolimus ointment is effective in improving clinical symptoms of oral lichen planus and may be considered an alternative therapy for patients who do not respond to topical steroids. Additional data may be necessary to further define the role of tacrolimus in this condition.
Guidelines state that topical tacrolimus is a treatment option for intertriginous or facial psoriasis. Initial positive results in controlled and noncontrolled trials suggest that topical tacrolimus may be an effective treatment for psoriasis in areas of thin skin, such as the face, or in the treatment of intertriginous psoriasis.
Results of a published trial and several case reports/case series suggest that topical tacrolimus may be beneficial in the treatment of pyoderma gangrenosum.
Guidelines support use of topical calcineurin inhibitors, including tacrolimus, as first-line therapy for children and adults with vitiligo; use should be limited to the head and neck regions. While the guidelines endorse the use of calcineurin inhibitors, there is poor clinical trial evidence supporting the use of tacrolimus as monotherapy or in combination with narrow-band UVB in the treatment of vitiligo. Long-term safety and efficacy data are unavailable.
Hypersensitivity to tacrolimus or any component of the formulation
Atopic dermatitis (moderate-to-severe): Topical:
Treatment: Apply thin layer of 0.03% or 0.1% ointment to affected area twice daily; rub in gently and completely. Discontinue use when symptoms have cleared. If no improvement within 6 weeks, patients should be re-examined to confirm diagnosis.
Maintenance therapy (off-label use): Apply one application (thin layer of 0.03% or 0.1% ointment) to areas usually affected twice daily twice a week (Schneider 2012).
Oral lichen planus (off-label use): Topical: Apply thin layer of 0.1% ointment to affected area up to 4 times daily; the treatment period in clinical trials ranged from 4 to 6 weeks (Corrocher 2008; Laeijendecker 2006; Radfar 2008).
Psoriasis (off-label use): Topical: Apply thin layer of 0.03% ointment twice daily; the treatment period in clinical trials was 6 weeks (Liao 2007).
Pyoderma gangrenosum (off-label use): Topical: Apply thin layer of 0.1% or 0.3% ointment to affected area once daily (Ghislain 2004; Lyon 2001); the treatment period in one clinical trial (0.3% ointment) was up to 10 weeks (Lyon 2001).
Vitiligo (off-label use): Topical: Apply thin layer of 0.1% ointment to affected area twice daily; may require several months for adequate response; the treatment period in clinical trials ranged from 10 weeks to 18 months (Majid 2010; Radakovic 2009; Taieb 2013).
Refer to adult dosing.
Moderate to severe atopic dermatitis: Topical:
Children ≥2 to 15 years: Apply thin layer of 0.03% ointment to affected area twice daily; rub in gently and completely. Discontinue use when symptoms have cleared. If no improvement within 6 weeks, patients should be re-examined to confirm diagnosis.
Children >15 years: Refer to adult dosing.
Maintenance therapy (off-label use):
Children ≥2 to 15 years: Apply one application (thin layer of 0.03% ointment) to areas usually affected twice daily twice a week (Schneider 2012)
Children >15 years: Refer to adult dosing.
Note: Patients experiencing flares should resume twice daily treatment.
Dosing: Renal Impairment
There are no dosage adjustments provided in the manufacturer's labeling.
Dosing: Hepatic Impairment
There are no dosage adjustments provided in the manufacturer's labeling.
Wash hands before and after application. Use the smallest amount of ointment needed to control the signs and symptoms of atopic dermatitis. Do not use with occlusive dressings. Do not bathe, shower, or swim right after application. Limit sun exposure during the treatment period. Burning at the application site is most common in first few days; improves as atopic dermatitis improves. Limit application to involved areas. Continue as long as signs and symptoms persist; discontinue if resolution occurs; re-evaluate if symptoms persist >6 weeks.
Store at room temperature of 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Alcohol (Ethyl): Tacrolimus (Topical) may enhance the dermatologic adverse effect of Alcohol (Ethyl). Monitor therapy
Antifungal Agents (Azole Derivatives, Systemic): May decrease the metabolism of Tacrolimus (Topical). Applicable Isavuconazonium considerations are addressed in separate monographs. Exceptions: Isavuconazonium Sulfate. Monitor therapy
Calcium Channel Blockers (Nondihydropyridine): May decrease the metabolism of Tacrolimus (Topical). Exceptions: Bepridil. Monitor therapy
CycloSPORINE (Systemic): May enhance the nephrotoxic effect of Tacrolimus (Topical). Tacrolimus (Topical) may enhance the nephrotoxic effect of CycloSPORINE (Systemic). Tacrolimus (Topical) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Tacrolimus (Topical). Avoid combination
Danazol: May increase the serum concentration of Tacrolimus (Topical). Monitor therapy
Grapefruit Juice: May decrease the metabolism of Tacrolimus (Topical). Monitor therapy
Immunosuppressants: Tacrolimus (Topical) may enhance the adverse/toxic effect of Immunosuppressants. Exceptions: Cytarabine (Liposomal). Avoid combination
Macrolide Antibiotics: May increase the serum concentration of Tacrolimus (Topical). Exceptions: Fidaxomicin; Roxithromycin; Spiramycin. Monitor therapy
Ombitasvir, Paritaprevir, and Ritonavir: May increase the serum concentration of Tacrolimus (Topical). Monitor therapy
Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir: May increase the serum concentration of Tacrolimus (Topical). Monitor therapy
Protease Inhibitors: May decrease the metabolism of Tacrolimus (Topical). Monitor therapy
Serotonin Reuptake Inhibitor/Antagonists: May decrease the metabolism of Tacrolimus (Topical). Exceptions: TraZODone. Monitor therapy
Sirolimus: May enhance the adverse/toxic effect of Tacrolimus (Topical). Tacrolimus (Topical) may enhance the adverse/toxic effect of Sirolimus. Avoid combination
Temsirolimus: Tacrolimus (Topical) may enhance the adverse/toxic effect of Temsirolimus. Temsirolimus may enhance the adverse/toxic effect of Tacrolimus (Topical). Avoid combination
As reported in children and adults, unless otherwise noted. Frequency not always defined.
Cardiovascular: Peripheral edema (adults 3% to 4%), hypertension (adults 1%)
Central nervous system: Headache (adults 19% to 20%), tingling of skin (2% to 8%), hyperesthesia (adults 3% to 7%), insomnia (adults 4%), paresthesia (adults 3%), depression (adults 2%), pain (1% to 2%)
Dermatologic: Burning sensation of skin (43% to 58%), pruritus (41% to 46%), erythema (25% to 28%), skin infection (adults 12%), acne vulgaris (adults 4% to 7%), urticaria (adults 3% to 6%), folliculitis (2% to 6%), skin rash (adults 2% to 5%), dermatological disease (children 4%), vesiculobullous dermatitis (children 4%), contact dermatitis (3% to 4%), pustular rash (adults 2% to 4%), contact eczema herpeticum (children 2%), fungal dermatitis (adults 1% to 2%), sunburn (adults 1% to 2%), alopecia (adults 1%), xeroderma (children 1%)
Gastrointestinal: Diarrhea (3% to 5%), dyspepsia (adults 1% to 4%), abdominal pain (children 3%), gastroenteritis (adults 2%), vomiting (adults 1%), nausea (children 1%)
Genitourinary: Dysmenorrhea (adults 4%), urinary tract infection (adults 1%)
Hematologic & oncologic: Lymphadenopathy (children 3%), malignant lymphoma, malignant neoplasm of skin
Hypersensitivity: Hypersensitivity reaction (adults 6% to 12%)
Infection: Herpes zoster (1% to 5%), varicella zoster infection (1% to 5%), infection (adults 1% to 2%)
Neuromuscular & skeletal: Myalgia (adults 2% to 3%), weakness (adults 2% to 3%), arthralgia (adults 1% to 3%), back pain (adults 2%)
Ocular: Conjunctivitis (adults 2%)
Otic: Otitis media (children 12%), otalgia (children 1%)
Respiratory: Flu-like symptoms (23% to 31%), increased cough (children 18%), asthma (adults 6%), rhinitis (children 6%), pharyngitis (adults 4%), sinusitis (adults 2% to 4%), bronchitis (adults 2%), pneumonia (adults 1%)
Miscellaneous: Fever (children 21%), allergic reaction (4% to 12%), alcohol intolerance (adults 3% to 7%), accidental injury (6%), cyst (adults 1% to 3%)
<1%, postmarketing, and/or case reports (Limited to important or life-threatening): Abnormality in thinking, abscess, acne rosacea, acute renal failure, aggravated tooth caries, anaphylactoid reaction, anemia, anorexia, anxiety, application site edema, arthritis, arthropathy, basal cell carcinoma, benign neoplasm (breast), blepharitis, bone disease, bursitis, candidiasis, cataract, chest pain, chills, colitis, conjunctival edema, constipation, cutaneous candidiasis, cystitis, dehydration, dermal ulcer, diaphoresis, dizziness, dry nose, dysgeusia, dyspnea, ear disease, ecchymoses, edema, epistaxis, eye pain, furunculosis, gastritis, gastrointestinal disease, heart valve disease, hernia, hyperbilirubinemia, hypercholesterolemia, hypertonia, hypothyroidism, impetigo (bullous), laryngitis, leukoderma, malaise, malignant lymphoma, malignant melanoma, migraine, muscle cramps, nail disease, neck pain, neoplasm (benign), oral candidiasis, oral mucosa ulcer, osteoarthritis, osteomyelitis, otitis externa, pulmonary disease, rectal disease, renal insufficiency, seborrhea, seizure, septicemia, skin carcinoma, skin discoloration, skin hypertrophy, skin photosensitivity, squamous cell carcinoma, stomatitis, syncope, tachycardia, tendon disease, unintended pregnancy, vaginitis, vasodilatation, vertigo, visual disturbance, vulvovaginal candidiasis, xerophthalmia, xerostomia
Concerns related to adverse events:
• Malignancy: [US Boxed Warning]: Topical calcineurin inhibitors have been associated with rare cases of malignancy (including skin and lymphoma); therefore, it should be limited to short-term and intermittent treatment using the minimum amount necessary for the control of symptoms and only on involved areas. Avoid use on malignant or premalignant skin conditions (eg cutaneous T-cell lymphoma). Limit sun and ultraviolet light exposure; use appropriate sun protection.
• Infection: Do not apply to areas of active bacterial or viral infection; infections at the treatment site should be cleared prior to therapy. Patients with atopic dermatitis are predisposed to skin infections, and tacrolimus therapy has been associated with risk of developing eczema herpeticum, varicella zoster, and herpes simplex.
• Lymphadenopathy: May be associated with development of lymphadenopathy; possible infectious causes should be investigated. Discontinue use in patients with unknown cause of lymphadenopathy or acute infectious mononucleosis.
• Renal failure: Acute renal failure has been observed (rarely) with topical use.
Disease related concerns:
• Immunosuppression: Should not be used in immunocompromised patients. Safety and efficacy have not been evaluated.
• Skin diseases with altered absorption: Not recommended for use in patients with skin disease which may increase systemic absorption (eg, Netherton's syndrome).
• Pediatric: [US Boxed Warning] Use in children <2 years of age is not recommended, only the 0.03% ointment should be used in children ages 2-15.
• Appropriate use: Topical calcineurin agents are considered second-line therapies in the treatment of atopic dermatitis/eczema, and should be limited to use in patients who have failed treatment with other therapies. Safety not established in patients with generalized erythroderma. If atopic dermatitis is not improved in <6 weeks, re-evaluate to confirm diagnosis. Safety of intermittent use for >1 year has not been established, particularly since the effect on immune system development is unknown.
Adverse events were observed in animal reproduction studies. Tacrolimus crosses the human placenta and is measurable in the cord blood, amniotic fluid, and newborn serum following systemic use. Refer to the Tacrolimus (Systemic) monograph for additional information.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience flu-like symptoms, itching, burning, stinging, skin tingling, temperature sensitivity, headache, cough, rhinitis, acne, hair bumps, or nausea. Have patient report immediately to prescriber signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), ear pain, severe skin irritation, signs of skin infection, skin growths, swollen glands, or muscle pain (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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Other brands: Protopic