Azelaic Acid

Registered South African indications:

• Acne vulgaris
• Rosacea (gel)

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Contact with eyes, mouth and mucous membranes
• Asthma 

Forms avail. in SA and covered in this monograph: cre, gel

Acne vulgaris - mild to moderate

• Topical (cre, gel): Apply small quantity to the affected area(s), 12hrly; Max: 10g/24hrs (cre)

Papulopustular rosacea - mild to moderate

• Topical (gel): Apply small quantity to the affected area(s), 12hrly

1g is equivalent to 4cm cream or 5cm gel

See additional prescribing points

Not established for use in children below 12 years

Pregnancy

• Caution
• There are no adequate and well-controlled studies of topically administered azelaic acid in pregnant women
• Animal studies do indicate the potential for effects with respect to pregnancy, embryo-fetal development, parturition or postnatal development. However, the dose levels without observed adverse effects in animals ranged across studies from 3-32 times the maximum recommended human dose based on body surface area
• Caution should be exercised when prescribing azelaic acid to pregnant women

Breastfeeding

• Caution
• It is not known if azelaic acid is secreted into human milk in vivo. However an in vitro equilibrium dialysis experiment demonstrated that passage of drug into maternal milk may occur. But the distribution of azelaic acid into maternal milk is not expected to cause a significant change from baseline azelaic acid levels in the milk.
• Azelaic acid is not concentrated in milk and less than 4% of topically applied azelaic acid is systemically absorbed, not increasing endogenous azelaic acid exposure above physiological levels. However, caution should be exercised when azelaic acid is administered to a breastfeeding woman
• Infants must not come into contact with treated skin/breast

Renal Impairment

• Caution; no dose adjustment recommended 

Hepatic Impairment

• Caution; no dose adjustment recommended 

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warnings

Respiratory Disorders

• Worsening of asthma
• Dyspnoea

Skin and Subcutaneous Tissue Disorders

• Seborrhoea
• Acne
• Skin depigmentation
• Cheilitis
• Urticaria rash
• Application site reactions
• Contact dermatitis 
• Swelling face
• Skin irritation

Immune, Blood and Lymphatic System Disorders

• Drug hypersensitivity
• Angioedema
• Hypersensitivity

Sensory Disorders

• Eye swelling

• Alcoholic cleansers
• Tinctures and astringents
• Abrasives
• Peeling agents

None routine

Administration directions

• Prior to application, the skin must be thoroughly cleansed with clear water or, if necessary, with a mild cleansing agent
• As a guide, a daily dose of 2g (1g per application) will be sufficient for the treatment of the entire facial area 
• If other areas of acne, in addition to the face, require treatment, for example the chest and back, a daily dose of 10g of cream should not be exceeded
• Sensitive skin: Apply cream/gel only once daily; for 1 week THEN continue with two applications, dly. If marked irritative reactions persist, the frequency of use should be reduced to one application per day until the symptoms of irritation regress, or the treatment should be interrupted temporarily

Azelaic acid exerts an antibacterial effect on Propionibacterium acnes and causes a significant reduction of the colonisation density of Propionibacterium acnes. A significant reduction of the fraction of free fatty acids in the skin surface lipids also occurs. The antimicrobial property of azelaic acid and a direct influence on follicular hyperkeratosis.

Gel (per g) 0.15g

• Skinoren (Bayer) originator

Cream (per g) 0.2g

• Skinoren (Bayer) originator