Protopic


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tacrolimus (topical)

(ta-kroe-li-mus) ,

Protopic

(trade name)

Classification

Therapeutic: immunosuppressants
Pregnancy Category: C

Indications

Moderate to severe atopic dermatitis in non-immunocompromised patients who do not respond to or cannot tolerate conventional therapies.

Action

Inhibits T-lymphocyte activation.

Therapeutic effects

Improvement in signs/symptoms of atopic dermatitis.

Pharmacokinetics

Absorption: Minimal following topical use.
Distribution: Crosses the placenta and enters breast milk.
Protein Binding: 99%.
Metabolism and Excretion: 99% metabolized by the liver; <1% excreted unchanged in the urine.
Half-life: Healthy volunteers—21.2 hr.

Time/action profile (immunosuppression)

ROUTEONSETPEAKDURATION
Topical†unknown1–2 wkunknown
†Improvement in atopic dermatitis

Contraindications/Precautions

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; Pediatric: Children <2 yr (safety not established).
Use Cautiously in: Exposure to sunlight/UV light (may ↑risk of malignant skin changes); Superficial skin infections; Obstetric: Hyperkalemia and renal impairment may occur in the newborn; use only if benefit to mother justifies risk to the fetus.

Adverse Reactions/Side Effects

Central nervous system

  • headache

Ear, Eye, Nose, Throat

  • sinusitis

Respiratory

  • cough
  • pharyngitis

Dermatologic

  • erythema (most frequent)
  • pruritis (most frequent)
  • skin infection (most frequent)
  • acne
  • folliculitis
  • rash

Local

  • burning

Musculoskeletal

  • back pain
  • myalgia

Miscellaneous

  • flu-like symptoms (most frequent)
  • fever
  • ↑ risk of lymphoma/skin cancer

Interactions

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

Drug-Drug interaction

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

Route/Dosage

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

Availability

Ointment: 0.03%, 0.1%

Nursing implications

Nursing 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.

Potential Nursing Diagnoses

Risk for infection (Adverse Reactions)

Implementation

  • Do not use continuously for a long time.
  • Topical: Wash their 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 the 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 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.

Evaluation/Desired Outcomes

  • Management of atopic dermatitis.

Protopic

(prō-tŏp′ĭk)
A trademark for the drug tacrolimus.

Protopic

A brand name for TACROLIMUS.
References in periodicals archive ?
The distribution right of Protopic in Japan was transferred to Maruho Co.
Protopic (Atopic Dermatitis) - Forecast and Market Analysis to 2022
But though the protopic cream helped his symptoms, the cycle of itch and scratch remained.
However, two new treatments, an ointment called Protopic and a cream known as Elidel, which ``damp down'' the immune system rather than simply tackling the symptoms, are about to be introduced onto the market and Camp says they could transform the lives of sufferers.
The most recently approved novel topical treatments for atopic dermatitis were topical immunomodulators, Protopic (tacrolimus) and Elidel (pimecrolimus), approved in 2000 and 2001, respectively.
Under the terms of the agreement, the assets and associated responsibilities relating to Astellas global portfolio of dermatology products which include Protopic, treatment for eczema, and other products for the treatment of acne and skin infection will be transferred to LEO Pharma (except for Protopic in Japan1).
Under the terms of the agreement, the assets and associated responsibilities relating to Astellas' global portfolio of dermatology products, which include Protopic, treatment for eczema, and other products for the treatment of acne and skin infection, will be transferred to Leo Pharma (except for Protopic in Japan.
M2 PHARMA-November 26, 2014-Perrigo to market Astellas Protopic Ointment 0.
However, because the effect of extended use of these medications is unknown, the FDA recommends that Elidel and Protopic only be used when a person cannot tolerate other eczema treatments or when all other treatments have failed.
What seems to help the most is Protopic, a prescription ointment for eczema, which we apply once or twice per day.
Two FDA-approved topical medications, Protopic (tacrolimus) and Elidel (pimecrolimus) are available for the treatment of eczema.
Immunosuppressant creams such as Protopic and Elidel are new GP-prescribed treatments that may reduce inflammation in eczema that's unresponsive to steroid cream.