Drug

Azelaic acid

definition

Azelaic acid is a chemical substance that belongs to the group of so-called carboxylic acids. Other synonymous terms used to denote azelaic acid are nonadic acid or 1,7-heptadicarboxylic acid. The latter is a detailed description of the chemical composition of azelaic acid.

Azelaic acid salts are called azelates. Azelaic acid is a white, crystalline solid. The chemical substance is mainly used as an active pharmaceutical ingredient in the treatment of acne and rosacea. The drug requires a prescription, so creams and ointments containing azelaic acid are not available over the counter.

Learn more about the clinical pictures: Acne - This works best and rosacea

In the conventional preparation, 20% creams and 15% gels are available. The application is therefore topical. The azelaic acid is made industrially through oxidation castor oil and potassium permanganate. This creates the whitish, solid powder that too Creams and Anoint is processed. However, there is no internal use in the form of tablets or capsules, for example.When applied topically, the active ingredient is hardly absorbed into the blood system through the skin, i.e. it is absorbed, so that there are practically no side effects that would affect the whole body. The Half-life of the drug is approx 12 hours. This is the time after which the concentration of a drug has dropped to half. So it's a fairly long-acting active ingredient.

Indications

There are two main indications for treatment with creams and ointments containing azelaic acid. The first important indication to be mentioned is the mild to moderate severity acne. The second indication for treatment with azelaic acid is Rosacea.
Both diseases are Skin disorderswhich can be quite similar in their appearance. However, the underlying causes are very different.

While acne is a collective name for diseases of the Sebum glands and Hair follicles is, rosacea is a complex skin disease, the cause of which is not yet fully understood.

Involvement of the vessels, the nervous and immune systems and a bacterial component are discussed. Outwardly, the acne is usually impressive Blackheads and Papules such as Pustules of the face and other body regions.
The rosacea, however, manifests itself through Redness of the midface and Growths the nose (bulbous nose), which particularly affects men.

Azelaic acid is only approved for external use in both diseases. In "off-label use" (outside of the approved use), azelaic acid is also used to prevent acne after successful acne treatment. The therapy usually lasts for weeks and months and, provided it does not cause side effects and is well tolerated, can be used for longer.

effect

Azelaic acid has several mechanisms of action that are beneficial in the treatment of rosacea and acne. In its composition it is similar to the fatty acids and helps with that Cornification disorder normalize the skin. This is an important morbid component of acne.
The cornification disorders, too Hyperkeratosis called, arise from an overgrowth of the so-called Keratinocytes, which are skin cells. This growth is inhibited by the azelaic acid.

Hyperkeratosis leads to the development of bothersome Blackheads and clogged pores. The azelaic acid promotes this Peeling off of skin flakes thereby helping to reduce the blackheads and ventilate the pores. Azelaic acid also has an anti-inflammatory effect by reducing the concentration of free fatty acids. This cause Redness of the skin. This mechanism helps, among other things, against the redness of rosacea.

Another very important effect of azelaic acid is a antimicrobial effect. The so-called Propionibacterium acnes is inhibited by azelaic acid. This is significantly involved in the development of acne disease. A very small amount of azelaic acid is absorbed into the body's bloodstream through the skin.
There, the azelaic acid also reduces the number of free fatty acids and thus works anti-inflammatory. However, the effect is very slight, since the azelaic acid actually works purely topically, i.e. at the place of application.

Side effects

As with other drugs, there are side effects with azelaic acid that should be considered. The side effects of therapy with azelaic acid depend on the duration of therapy and the dosage and frequency of use. They are very different between individuals.

In general, however, creams and ointments with azelaic acid are well tolerated, so that side effects usually occur at the beginning of therapy and are only of a temporary nature. The most common are local skin conditions such as reddening of the skin, dry skin and water retention. In addition, there may be slight burning, itching or irritation of the skin on the applied skin.

Mild pain is also possible. Somewhat less often there are nervous discomforts, skin peeling and discoloration of the skin. Azelaic acid interacts with the melanocytes of the skin in a dose-dependent manner, so that the skin becomes slightly lighter with long-term use. Contact dermatitis is a rare side effect of azelaic acid therapy. Contact dermatitis is an allergic reaction of the skin to a certain substance that it comes into contact with.

Read more on this topic at: Contact dermatitis

Other rare side effects are generalized allergic reactions and drug hypersensitivity. These can manifest themselves, for example, in an asthmatic attack. Eczema, ulcers, skin blisters and overheating can rarely occur at the site of application. However, all of these side effects depend on the dosage of azelaic acid and the area of application, as well as the individual who uses the active ingredient. Azelaic acid should not come into contact with mucous membranes or the eyes, as it causes irritation there. In the event of contact, the affected mucous membranes must be rinsed immediately. If irritation persists, a dermatologist should be consulted. Azelaic acid should only be used during pregnancy after consultation with a dermatologist and strict indications. The same goes for breastfeeding. Under no circumstances should the child come into contact with the active substance.

In the event of complaints, the treating dermatologist should be consulted in order to be able to assess whether it is just a slight and temporary intolerance or, for example, a drug allergy.

Azelaic acid in the treatment of acne

Azelaic acid has been used for around 20 years topical acne treatment used. There are no major contraindications to treating acne disease with azelaic acid. For a better understanding of the therapy, it is advisable to know a few facts about the development and symptoms of acne. Acne is a collective term for Disorders of the sebum glands and hair follicles of the skinwhich initially lead to the formation of blackheads, so-called comedones. Later on, other skin symptoms such as papules, pustules, redness and nodules appear. It is the most common skin disease worldwide.

There are a number of different factors that lead to the development of acne. Some of them, such as one genetic predisposition or that Smoke, cannot be influenced by therapy with azelaic acid.
However, other development mechanisms are influenced by the mechanisms of action of azelaic acid, so that the symptoms are alleviated. There are three important ones Main mechanisms of action of azelaic acid, which is in the Pathogenesis (Disease emergence) of acne intervene. The azelaic acid works anti-comedogenic. This means that it reduces the formation of blackheads and also prevents them in the disease-free interval.

This is achieved in that the azelaic acid on the one hand inhibits the activity of the keratinocytes of the skin and on the other hand reduces the number of free fatty acids in the skin. In the case of acne it is Keratinocyte activity increasedso that blackheads form and the skin pores are clogged. The fatty acids are also increased in acne and are an inflammatory stimulus for the skin.

Another important mode of action of azelaic acid is its antimicrobial effect. It has an inhibiting effect on Propionibacterium acnes. This bacterium is significantly involved in the disease, especially in the later stages of acne. The azelaic acid has an inhibitory effect on the bacterium. The anti-inflammatory effect also dampens the activity and irritation of the bacterium on the skin. This fact can be described as para-antibiotic effect because it is directed not only directly against the bacterium, but much more against the inflammability in the context of bacterial infestation. The last important mechanism of action is the anti-inflammatory effect of azelaic acid. This results among other things from the inhibition of free fatty acids and helps to soothe the skin and alleviate the symptoms.

Creams and ointments containing azelaic acid are recommended for use on moderate to severe acne in combination with other active ingredients such as antibiotics, retinoids, and hormonal antiandrogens. However, therapy with azelaic acid alone is not sufficient for moderate to severe acne, as the expected success of the therapy would be too weak. Use can be recommended for mild acne. It should be noted that azelaic acid prevents hyperseborrhea, i.e. the excessive sebum production by the skin in the context of acne, not affected.

Azelaic acid therapy should be carried out for at least 12 weeks. The cream or ointment must be applied 2 times a day. Side effects like local skin reactions in the sense of redness, irritation, itching and the like, are usually only temporary symptoms and subside in most patients within 4 weeks. Very rarely does it happen allergic reactions. There are no contraindications to the use of azelaic acid as it is generally very well tolerated by patients with acne. Only contact with the mucous membranes and the eyes should be avoided, as this can cause irritation.

Dosage form as an ointment

There are several creams and ointments that contain azelaic acid. A common trade name for an azelain-containing ointment is this Skinoren®. There are two compositions that are common and often used in Germany. On the one hand there is a 20% cream and a 15% gel. Both are approved and are for external use in acne or rosacea prescription only. When applying, you should ensure that the affected areas of skin are moistened with the cream or ointment without interruption. The ointment or gel is applied twice a day. The period of application is usually at least 12 weeks. An improvement in the symptoms can be expected after four weeks.

If there is no improvement after four weeks, the attending physician should be consulted. A doctor should also be consulted in the event of allergic reactions. Temporary irritation symptoms (see section side effects) usually disappear on their own after four weeks, when the skin has got used to the application of the cream. Creams, gels and ointments must not come into contact with mucous membranes. It is therefore advisable to wash your hands thoroughly after applying the substances. In the event of contact with the mucous membrane or eyes, rinse immediately with water.

If irritation persists, a doctor must be consulted, especially if there is eye irritation. Before applying the ointments or gels, the affected areas of the skin should be cleaned with a little water or a mild skin cleanser and allowed to dry. After application, the skin must be ventilated, so one should no air or water impermeable covers and bandages invest.