Actions and Spectrum: 

• pimecrolimus is a topical immunomodulatory medication that is used for the treatment of atopic dermatitis (eczema). It works by inhibiting the activity of T-lymphocytes, a type of white blood cell that plays a vital role in the immune response. pimecrolimus explicitly inhibits T-lymphocyte activation by blocking the production of cytokine signaling molecules involved in the immune response 
• By inhibiting the activity of T-lymphocytes and the production of cytokines, pimecrolimus can help to reduce inflammation and itching associated with atopic dermatitis. It also helps restore the skin barrier function, which is often compromised in patients with atopic dermatitis 
• pimecrolimus. It has a narrow spectrum of activity and is primarily effective against T-lymphocytes involved in the skin’s immune response. It is effective in the treatment of atopic dermatitis in both adults and children and has been approved by the US FDA for use in patients aged two years and older. 

 

 

 

 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined 

>10% 

Headache (7-25%) 

Nasopharyngitis (8-27%) 

Bronchitis (<11%) 

Burning sensation (2-26%) 

Fever (1-13%) 

Cough (2-16%) 

Upper respiratory tract infection (4-19%) 

<1% 

Malignant melanoma 

Basal cell carcinoma of the skin 

Flushing 

Eczema 

Squamous cell carcinoma 

Septic arthritis 

Ocular irritation 

Skin discoloration 

Malignant lymphoma 

Frequency not defined 

Paraesthesia 

Dryness 

Skin infection 

Desquamation 

Application site pain 

Rash 

 

 

 

 

Black box warning: 

• Rare cancer cases have been documented (although the cause has not been established); uncommon incidences of lymphoma and skin cancer have also been reported. 
• Use short-term and intermittently, using the least amount necessary to treat symptoms; avoid long-term usage, and only apply to areas of atopic dermatitis. 
• Children under two years old are not recommended for usage. 

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: pimecrolimus should not be used in patients with a known hypersensitivity to pimecrolimus or any of the ingredients in the medication 
• Immunocompromised patients: pimecrolimus should not be used in patients with a weakened immune system, as it may increase the risk of infections 
• Malignancy: pimecrolimus should not be used in patients with skin infections, malignancies, or lymphoma 
• Age: pimecrolimus is not indicated for use in children younger than two years of age. 

Caution: 

• pimecrolimus should not be used on skin that is infected or has open wounds, as it can increase the risk of developing a severe infection. 
• It is not recommended for use in individuals under the age of 2 years. 
• The long-term safety of pimecrolimus has not been established, and there have been concerns about an increased risk of skin cancer and lymphoma with its use. However, the risk of these adverse effects is shallow. 
• pimecrolimus can cause skin irritation, burning, and itching at the application site. These side effects are generally mild and disappear within a few days of starting treatment. 
• There is limited information on the use of pimecrolimus during pregnancy or breastfeeding, so it is essential to discuss the risks and benefits of treatment with your healthcare provider if you are pregnant or breastfeeding. 

 

 

Pregnancy consideration: C 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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: 

• pimecrolimus is a topical calcineurin inhibitor used to treat atopic dermatitis, a type of eczema. It works by inhibiting the activity of calcineurin, a protein that plays a vital role in the immune response. pimecrolimus reduces inflammation and itching, common symptoms of atopic dermatitis, by suppressing the immune system in the affected area 
• pimecrolimus is a relatively small molecule that can penetrate the skin and reach the deeper layers where it exerts its effects. After application to the skin, pimecrolimus is absorbed into the bloodstream and metabolized in the liver before being eliminated from the body through the kidneys 
• pimecrolimus has a relatively short half-life of approximately 30 hours, so it is rapidly eliminated from the body. This short half-life, combined with the fact that pimecrolimus is not metabolized by the cytochrome P450 system in the liver, means that there are few drug interactions with other medications. 

Pharmacodynamics: 

pimecrolimus inhibits the activity of calcineurin, a protein that plays a vital role in the activation of T-cells in the immune system. T-cells are involved in the immune response and contribute to inflammation and itching, common symptoms of atopic dermatitis. By suppressing the activity of calcineurin, pimecrolimus reduces the activation of T-cells and therefore reduces inflammation and itching in the affected area  

Pharmacokinetics: 

Absorption 

pimecrolimus is a lipophilic compound well absorbed through the skin. It penetrates the skin and reaches the deeper layers, where it exerts its effects. After topical application, pimecrolimus is absorbed into the systemic circulation, although systemic absorption is minimal.  

Distribution 

pimecrolimus is highly bound to plasma proteins (approximately 99%). The drug is distributed throughout the body and accumulates in the liver but not in the skin.  

Metabolism 

pimecrolimus is extensively metabolized in the liver by the cytochrome P450 enzyme system, primarily by CYP3A4. The metabolites are inactive and are excreted in the urine.  

Elimination and Excretion 

pimecrolimus and its metabolites are excreted primarily in the urine, with a small amount excreted in the feces. The elimination half-life of pimecrolimus is approximately 30 hours, which is relatively short 

 

 

 

 

Administration: 

• Wash and dry your hands before applying the medication 
• Wash the affected skin area with mild soap and water and dry thoroughly 
• Apply a thin layer of pimecrolimus to the affected area of the skin. Rub it in gently and thoroughly 
• Repeat the application twice daily unless otherwise directed by your healthcare provider 
• Avoid contact with the eyes, mouth, and other mucous membranes 
• Do not cover the treated area with airtight dressings or bandages unless instructed by your healthcare provider 
• Wash your hands after applying the medication unless the hands are the area being treated 

 

 

 

Patient information leaflet 

Generic Name: pimecrolimus topical 

Pronounced: [ PIM-e-KROE-li-mus-TOP-ik-al ] 

Why do we use pimecrolimus topical? 

pimecrolimus is used to treat atopic dermatitis, also known as eczema because it is an effective topical immunomodulator that can help reduce inflammation and itching associated with this condition. Atopic dermatitis is a chronic inflammatory skin disorder characterized by itchy, red, and scaly patches on the skin.