How Do Topical Androgen Receptor Inhibitors Work?

Reviewed on 6/8/2021

WHAT ARE TOPICAL ANDROGEN RECEPTOR INHIBITORS AND HOW DO THEY WORK?

Topical androgen receptor inhibitors (also called “antiandrogens”) are medications that block the effects of androgens on the body. Androgens are hormones that contribute to growth and reproduction in both men and women. Androgens are usually thought of as male hormones, but the female body also naturally produces a small amount of androgens.

Topical androgen receptor inhibitors are used to treat skin and hair disorders. They when used by women counteract the effect of male sex hormones (testosterone) on the skin; however, they are not suitable for skin problems in men.       

Topical androgen receptor inhibitors work in the following ways:

  • They bind to androgen receptors with high affinity (strength by which two or more molecules interact or bind) and inhibit their action.
  • Androgen receptors act as signaling cascades that promote acne formation which includes sebaceous gland proliferation, excess sebum production leading to plugging, and comedone formation.
  • Androgen receptor inhibitors also inhibit 5-alpha reductase, an enzyme that acts on the skin to increase dihyroxytestosterone (DHT).
  • DHT and testosterone are the major androgens that interact with the androgen receptors on the skin, with DHT being five to 10 times more potent than testosterone to develop skin disorders.

Follow these instructions for proper use:

  • Clean the affected area with water
  • Apply a thin layer of cream on the skin
  • Usually, one to three times daily or as directed by your doctor
  • Rub it gently on the affected site
  • Wash your hands after use
  • Use the medication regularly, preferably at the same times each day to get the most benefit from it

HOW ARE TOPICAL ANDROGEN RECEPTOR INHIBITORS USED?

Topical androgen receptor inhibitors are used in conditions such as:

QUESTION

Testosterone is a chemical found only in men. See Answer

WHAT ARE SIDE EFFECTS OF TOPICAL ANDROGEN RECEPTOR INHIBITORS?

Avoid applying this product to your eyes or inside the mouth. If this occurs, wipe off the medication and rinse thoroughly with water. 

Common side effects include:

  • Drying/flaking of skin
  • Burning and/or stinging at the application site
  • Erythema (a type of skin rash caused by injured or inflamed blood capillaries)
  • Itching
  • Skin irritation
  • Striae (stretch marks)
  • Edema

Other rare side effects include:

  • Skin atrophy (thinning of the skin)
  • Telangiectasia (a condition in which widened venules [tiny blood vessels] cause thread-like red lines or patterns on the skin)
  • Hyperkalemia (high potassium levels in the blood)
  • Allergic reaction
    • Hives
    • Rash
    • Itching/swelling

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.

WHAT ARE DRUG NAMES OF TOPICAL ANDROGEN RECEPTOR INHIBITORS?

Drug names include:                               

References
https://reference.medscape.com/drugs/topical-androgen-receptor-inhibitors

https://dermnetnz.org/topics/anti-androgen-therapy/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2923944/#:~:text=The%20anti%2Dandrogenic%20effects%20are,conversion%20of%20androstenedione%20to%20testosterone%3B

https://www.webmd.com/connect-to-care/hair-loss/what-to-know-about-anti-androgens-for-hair-loss

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