Products
Isotretinoin is commercially available in capsule and gel form (Roaccutane, generics). It has been approved in many countries since 1983 (United States: 1982, Accutane). This article refers to the capsules. See also under isotretinoin gel.
Structure and properties
Isotretinoin (C20H28O2, Mr = 300.4 g/mol) exists as a yellow to light orange crystalline powder that is practically insoluble in water. The substance is sensitive to air, heat, and light, especially in solution. Isotretinoin is a stereoisomer of tretinoin, the vitamin A acid.
Effects
Isotretinoin (ATC D10BA01) has sebostatic, antiproliferative, proapoptotic, anti-inflammatory, and indirect antibacterial properties. It reduces the activity, differentiation and size of sebaceous glands. Sebum production is greatly reduced. Since sebum is also an important substrate for the growth of , this also reduces bacterial colonization. According to Melnik (2017) and other sources, the effects of isotretinoin are primarily due to the induction of sebocyte apoptosis. Many of the adverse effects can be attributed to apoptosis of other cell types. Accordingly, isotretinoin has similarities to anticancer drugs.
Indication
As a second-line agent for the treatment of severe acne. Isotretinoin is also used for various other skin conditions, but is not approved by the authorities for this purpose (off-label).
Dosage
According to the drug label. The dose is adjusted on an individual basis. The capsules are taken once or twice a day with a meal. The skin is more sensitive to sun and UV radiation during treatment and should be well protected.
Contraindications
Isotretinoin is teratogenic (harmful to the fetus).
- Hypersensitivity
- Pregnancy and lactation
- Women of childbearing age, if all conditions of the pregnancy prevention program are not met. These conditions can be found in the drug information leaflet.
- Hepatic insufficiency
- Hypervitaminosis A
- Severely elevated blood lipid levels
- Combination with tetracyclines
Please refer to the full and comprehensive precautions in the drug label, which are not included in this article.
Interactions
Isotretinoin should not be co-administered with vitamin A, tetracyclines, and skin-irritating acne therapeutics.
Adverse Effects
The most common possible adverse effects include:
- Inflammation of the lips, eczema, dry skin, localized skin sloughing, itching, erythematous rash, skin lesions
- Joint pain, muscle pain, back pain
- Eyelid rim inflammation, conjunctivitis, dry eyes, eye irritation.
- Hypertriglyceridemia, HDL reduction
- Blood count changes such as anemia, thrombocytopenia and thrombocytosis.
In addition, numerous other side effects are possible, including, for example, rarely occurring psychiatric disorders such as depression and anxiety. To prevent the adverse effects, the lips should be maintained with a lip balm, the nose with a nasal ointment, the skin with a body lotion and the eyes with tear substitutes or eye ointments.
