Action and Spectrum

Actions and Spectrum 

Action: 

tacrolimus ointment is a medication that belongs to the class of drugs known as calcineurin inhibitors. It is primarily used topically to treat certain skin conditions, such as atopic dermatitis (eczema). The ointment works by modulating the immune response in the skin. 

Spectrum: 

tacrolimus ointment is mainly prescribed for the treatment of atopic dermatitis (eczema) in patients aged 2 years and above. Atopic dermatitis is a persistent inflammatory skin disorder distinguished by redness, itching, and dryness. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

Skin erythema (12-28%) 

Headache (5-20%) 

Pruritus (41-46%) 

Burning sensation (43-58%) 

Flu-like symptoms (23-31%) 

Black Box Warning

Black Box Warning:  

The malignancy case reported (rare) 

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: tacrolimus ointment should not be used in individuals with a known hypersensitivity or allergy to it or any of its components. Allergic reactions may include rash, itching, swelling, or difficulty breathing. 

Pre-existing skin infections: The use of tacrolimus ointment is contraindicated in untreated or uncontrolled skin infections. This is because the medication can suppress the immune system, potentially making the infection worse. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excreted into human milk is known 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

<b>Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

tacrolimus ointment is classified as a calcineurin inhibitor and is prescribed primarily for topical application in the treatment of specific inflammatory skin conditions, notably atopic dermatitis or eczema. 

Pharmacodynamics:  

tacrolimus works by inhibiting the activity of calcineurin, a protein phosphatase that plays a key role in the activation of T-lymphocytes (immune cells). By inhibiting calcineurin, tacrolimus prevents the production and release of inflammatory cytokines from T-cells, thus reducing the immune response and inflammation in the skin.   

Pharmacokinetics: 

Absorption 

 The ointment is applied topically to the skin, where it is absorbed through the epidermis into the systemic circulation. The extent of absorption is generally low, with only a small fraction of the applied dose reaching the bloodstream.  

Distribution 

 tacrolimus is extensively distributed throughout the body. It binds primarily to plasma proteins, such as albumin, and also to lymphocytes. The drug has been found in various tissues, including skin, liver, kidney, and spleen. 

Metabolism 

The drug undergoes extensive metabolism primarily in the liver via the cytochrome P450 (CYP) enzyme system, specifically CYP3A4 and CYP3A5. Metabolism produces several metabolites, with the main metabolite being 31-demethyl tacrolimus.   

Excretion and elimination 

The elimination of tacrolimus and its metabolites primarily occurs through the feces, with a smaller fraction excreted in the urine. The exact proportion of excretion routes needs to be defined. 

Adminstartion

Administration:  

Apply a thin layer: Use a clean fingertip to apply a thin layer of tacrolimus ointment to the affected area. It’s important to apply only a thin layer and avoid excessive application. 

Rub it in gently: Gently rub the ointment into the skin until it is absorbed. Do not wash off the ointment immediately after application.  

Follow the prescribed frequency: Apply tacrolimus ointment as directed by your healthcare provider. Typically, it is applied twice daily, with a gap of at least 12 hours between applications. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tacrolimus ointment 

Why do we use tacrolimus ointment?   

Atopic dermatitis: It is beneficial for cases where other topical treatments have not been effective or are not well-tolerated. It helps reduce inflammation and itching associated with eczema flare-ups. 

Contact dermatitis: The drug can be used to treat contact dermatitis, which is an allergic skin reaction caused by contact with certain substances, such as poison ivy or nickel. It helps relieve itching, redness, and inflammation associated with contact dermatitis. 

Seborrheic dermatitis: Seborrheic dermatitis is a common skin condition characterized by redness, scaling, and flaking of the skin, typically affecting the scalp, face, and other areas with high oil gland activity.