Tacrolimus-Hyaluronate-Niacin (tacrolimus/hyaluronate sodium/niacinamide)
Macrolide Immunosuppressants - Topical Topical Cream (GRAM)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis.
Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Tacrolimus is commercially available for topical use as a 0.03 or 0.1% ointment. The exact mechanism(s) of action of tacrolimus in the treatment of atopic dermatitis has not been elucidated but appears to involve inhibition of the activation of T cells.
Tacrolimus also has been shown to inhibit release of mediators from skin mast cells and basophils and to downregulate the expression of high-affinity receptors for immunoglobulin E (IgE) on Langerhans cells. Although tacrolimus is not genotoxic and does not interact directly with DNA, the drug may impair local immunosurveillance.
Following single or multiple applications of tacrolimus 0.3% ointment (not commercially available in the US) to atopic dermatitis lesions in adults or children 5-11 years of age, tacrolimus was not appreciably absorbed into systemic circulation (e.g., the apparent systemic bioavailability was less than 0.5%). Use of tacrolimus ointment on the face or neck, large areas of the body (i.e., >50% of the total body surface area), or areas of broken skin theoretically may increase systemic exposure to the drug. The lowest blood tacrolimus concentration at which systemic effects can be observed is as yet unknown.
Tacrolimus does not appear to accumulate systemically following intermittent topical application of the ointment for periods up to 1 year. Following systemic administration, tacrolimus is extensively metabolized in the liver and in the GI tract, principally via oxidation by cytochrome P-450 3A (CYP3A) isoenzymes.
Generic name: tacrolimus/hyaluronate sodium/niacinamide
Drug class: Macrolide Immunosuppressants - Topical
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Tacrolimus-Hyaluronate-Niacin
Indications
No indications are available for this drug.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed to date.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to tacrolimus or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
- Eczema herpeticum
- Graft-versus-host disease
- Herpes simplex infection
- Herpes zoster
- Immunosuppression
- Infectious mononucleosis
- Lamellar ichthyosis
- Netherton's syndrome
- Malignancy
- Malignant lymphoma
- No disease contraindications
Adverse reactions
Adverse effects occurring in 20% or more of patients include burning sensation, pruritus, flu-like symptoms, skin erythema, and headache in adults and burning sensation, pruritus, and flu-like symptoms in pediatric patients. Adverse local effects are most common during the first few days of therapy with tacrolimus ointment and generally improve as the lesions of atopic dermatitis heal. Burning sensation or pruritus usually lasts a median of 15 minutes (range: 2 minutes to 3 hours) or 20 minutes (range: 3 minutes to 10 hours), respectively.
More Frequent
- Flushing
- Skin rash
- Wheezing
Rare or Very Rare
- Malignancy
More Frequent
- Fever
- Flu-like symptoms
- Headache disorder
- Paresthesia
- Pruritus of skin
- Treatment site sequelae
Less Frequent
- Acne vulgaris
- Alcohol intolerance
- Back pain
- Bullous dermatitis
- Dyspepsia
- Dyspnea
- Eye tearing
- Eyelid erythema
- Folliculitis
- Myalgia
- Ocular itching
- Ocular redness
- Sinusitis
Rare or Very Rare
- Localized edema
Precautions
No enhanced messaging available.
Safety and efficacy not established in children younger than 2 years of age. Not recommended for use in children younger than 2 years of age. Not recommended for use in immunocompromised children.
When topical tacrolimus therapy is indicated in immunocompetent children 2-15 years of age, only the 0.03% ointment should be used.
Blood concentrations of tacrolimus in children receiving topical therapy with the drug occasionally have been in the concentration range achieved with systemic therapy. Long-term effects on the developing immune system in infants and children are not known.
Category C.
Tacrolimus is distributed into milk following systemic administration. Not known whether tacrolimus is distributed into milk following topical application to skin. Discontinue nursing or drug, taking into account the importance of the drug to the woman.
No substantial differences in safety relative to younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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