(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 in immunocompetent patients not responsive to conventional therapy or when conventional therapy is not appropriate
Canadian labeling: Additional use (not in U.S. labeling): Maintenance therapy to prevent flares and extend flare-free intervals in patients with moderate-to-severe atopic dermatitis who are responsive to initial therapy and experiencing ≥5 flares per year
Off Label Uses
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 (Canadian labeling; not in US labeling): Apply one application (thin layer of 0.03% or 0.1% ointment) to areas usually affected twice a week, allowing 2 to 3 days between applications (eg, one application on Monday and Thursday). Re-evaluate after 12 months. Safety of maintenance therapy >12 months has not been established.
Note: Patients experiencing flares should resume twice daily treatment.
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 (Canadian labeling; not in US labeling):
Children ≥2 to 15 years: Apply one application (thin layer of 0.03% ointment) to areas usually affected twice a week, allowing 2 to 3 days between applications (eg, one application on Monday and Thursday). Re-evaluate after 12 months. Safety of maintenance therapy >12 months has not been established.
Children >15 years: Refer to adult dosing.
Note: Patients experiencing flares should resume twice daily treatment.
Do not use with occlusive dressings. 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
Antidepressants (Serotonin Reuptake Inhibitor/Antagonist): May decrease the metabolism of Tacrolimus (Topical). Exceptions: TraZODone. 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): Tacrolimus (Topical) may enhance the nephrotoxic effect of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may enhance the nephrotoxic effect of Tacrolimus (Topical). 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
Sirolimus: Tacrolimus (Topical) may enhance the adverse/toxic effect of Sirolimus. Sirolimus may enhance the adverse/toxic effect of Tacrolimus (Topical). 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% (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, arthropathy, basal cell carcinoma, benign neoplasm (breast), blepharitis, bursitis, cataract, chest pain, chills, colitis, conjunctival edema, cutaneous candidiasis, cystitis, dehydration, dermal ulcer, diaphoresis, dry nose, dysgeusia, dyspnea, ecchymoses, edema, epistaxis, furunculosis, gastritis, 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, osteoarthritis, osteomyelitis, otitis externa, pulmonary disease, rectal disease, renal insufficiency, seborrhea, seizure, septicemia, skin discoloration, 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.
Pregnancy Risk Factor
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.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: miscellaneous topical agents
Other brands: Protopic