How Do Topical Immunosuppressive Agents Work?

Topical immunosuppressive agents are drugs that control or suppress the immune system and are used to treat inflammatory skin diseases.

Topical immunosuppressive agents work on both the immune system (by inhibiting pro-inflammatory cytokines) and the skin cells called “keratinocytes”.

• On the immune system:
  • They bind to a receptor within the cell called FK binding proteins.
  • This results in a drug-protein complex that further inhibits calcineurin (a calcium-dependent phosphatase-transmitting chemical)
  • Inhibition of calcineurin, in turn, reduces the activity of T-lymphocytes in the immune system.
  • T-lymphocytes are responsible for killing infected host cells, activating other immune cells, producing cytokines, and regulating the immune response.
  • As a result, T-cells fail to release cytokines (chemicals that cause inflammation, redness, and itching).
• On the skin cells:
  • They reduce the number of interleukin-8 (IL-8) cytokine receptors on the skin cells, thus reducing inflammation.
  • IL-8 is produced by various tissues and responsible for attracting and activation of neutrophils (white blood cells) at the site of inflammation.

Topical immunosuppressive agents work equally well for both adults and children with more than two-thirds of both groups having an improvement of greater than 50 percent.

Topical immunosuppressive agents should be applied on lesions (a thin layer rubbed in gently) two to three times a day until they subside.

Skin conditions treated with topical immunosuppressive drugs include the following:

• Moderate-to-severe atopic dermatitis in adults and children
  • responding poorly to conventional therapy (oral steroids, antibiotics)
  • suffer from side effects of conventional therapy
• Atopic eczema (an allergic-type condition that causes red, irritated, and itchy skin)
• Psoriasis (a skin disease that causes red, itchy scaly patches, most commonly on the knees, elbows, trunk, and scalp)
• Alopecia areata (a condition that causes hair to fall out in small patches)
• Pemphigus (a rare skin disorder characterized by blistering of your skin and mucous membranes)
• Eosinophilic fasciitis (a syndrome in which tissue under the skin and over the muscle, called fascia, becomes swollen, inflamed. and thick)
• Seborrheic dermatitis (scaly patches, red skin, and stubborn dandruff)
• Genital lichen sclerosus (an uncommon condition that creates patchy, white skin that appears thinner than normal)
• Oral lichen planus (white, lacy patches; red, swollen tissues; or open sores)
• Vitiligo (a disease that causes loss of skin color in patches)
• Discoid lupus erythematosus (a chronic skin condition of sores with inflammation and scarring)

Avoid using in sensitive areas such as eyes and inside mouth/nose, and if you apply the medication in those areas, flush with plenty of water.

Common side effects include:

• Burning/and or stinging
• Dryness
• Pruritis (itchy skin)
• Soreness

Other rare side effects include:

• Headache
• Acne
• Folliculitis (hair bumps)
• Stomach upset
• Flu-like symptoms (fever, chills, runny nose, sore throat, and muscle aches)
• Increased sensitivity of the skin to hot/cold/pain/touch
• Eczema herpeticum (a viral infection characterized by fever and clusters of itchy blisters or punched-out erosions)
• Severe dizziness (feeling faint, weak, or unsteady)
• Trouble breathing
• Serious allergic reaction
  • Rash
  • Hives
  • Itching/swelling of face/tongue/throat

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Drug names include:                               

• Elidel
• Pimecrolimus
• Protopic
• Tacrolimus ointment