13-cis retinoic acid

13-cis Retinoic Acid

13-cis Retinoic Acid, also known as isotretinoin, is a medication primarily used to treat severe acne vulgaris. It is a derivative of vitamin A and belongs to the class of compounds known as retinoids. This article provides an overview of its pharmacology, clinical uses, mechanism of action, and potential side effects.

Pharmacology

13-cis Retinoic Acid is a stereoisomer of all-trans retinoic acid (tretinoin). It is administered orally and is highly effective in reducing the size and activity of the sebaceous glands, thereby decreasing sebum production. This reduction in sebum is crucial in the treatment of acne, as excess sebum can lead to clogged pores and bacterial growth.

The drug is metabolized in the liver and has a half-life of approximately 10-20 hours. It is primarily excreted in the urine and feces.

Clinical Uses

The primary indication for 13-cis Retinoic Acid is the treatment of severe nodular acne that is resistant to other forms of therapy, such as topical treatments and antibiotics. It is also used in some cases of moderate acne that have not responded to other treatments.

In addition to its use in acne, isotretinoin has been investigated for other dermatological conditions, such as rosacea and hidradenitis suppurativa, although these are not standard indications.

Mechanism of Action

13-cis Retinoic Acid works by binding to nuclear receptors in the skin, which modulate gene expression. This action leads to:

• Decreased sebum production by reducing the size and activity of sebaceous glands.
• Inhibition of the growth of Propionibacterium acnes, the bacteria associated with acne.
• Promotion of normal keratinization, reducing the formation of comedones.

Side Effects

The use of 13-cis Retinoic Acid is associated with a range of potential side effects, some of which can be severe. Common side effects include:

• Dry skin and lips (cheilitis)
• Nosebleeds
• Dry eyes and irritation
• Elevated liver enzymes
• Hyperlipidemia

More serious side effects include:

• Teratogenicity: Isotretinoin is highly teratogenic and can cause severe birth defects. It is contraindicated in pregnancy, and women of childbearing potential must use effective contraception during treatment.
• Depression and mood changes: There have been reports of depression, psychosis, and rarely, suicidal ideation associated with isotretinoin use.

Monitoring and Precautions

Patients on isotretinoin require regular monitoring, including:

• Liver function tests
• Lipid profiles
• Pregnancy tests for women of childbearing potential

Also see

• Acne vulgaris
• Retinoid
• Vitamin A
• Tretinoin