Skinoren Gel

Skinoren Gel

azelaic acid

Manufacturer:

LEO Pharma

Distributor:

Getz Bros
Full Prescribing Info
Contents
Azelaic acid.
Description
1 g Azelaic acid (Skinoren) gel contains 150 mg (15 %) azelaic acid.
List of excipients: Benzoic acid, Carbomers, Disodium edetate, Lecithin, Polysorbate 80, Propylene glycol, Purified water, Sodium hydroxide, Triglycerides medium chain.
Action
Pharmacotherapeutic group: other anti-acne preparations for topical use. ATC Code: D10AX03.
Pharmacology: Pharmacodynamics: Mechanism of action: The antimicrobial action and a direct influence on follicular hyperkeratosis are assumed to be the basis for the therapeutic efficacy of Azelaic acid (Skinoren) gel in acne.
Clinically, a significant reduction of the colonization density of Propionibacterium acnes and a significant reduction of the fraction of free fatty acids in the skin surface lipids is observed.
In vitro and in vivo, azelaic acid inhibits the proliferation of keratinocytes and normalizes the disturbed terminal epidermal differentiation processes in acne. In the rabbit ear model azelaic acid accelerates the comedolysis of tetradecane-induced comedones.
While the pathophysiology of rosacea is not completely understood, there is increasing consensus that inflammation involving the elevation of several pro-inflammatory effector molecules such as kallikrein-5 and cathelicidin as well as reactive oxygen species (ROS), is a central process of this disease.
Azelaic acid has been demonstrated to modulate the inflammatory response in normal human keratinocytes by: a) activating the peroxisome proliferator-activated receptor γ (PPARγ); b) inhibiting the trans-activation of nuclear factor-kB (NF-kB); c) inhibiting the production of pro-inflammatory cytokines and d) inhibiting the release of ROS from neutrophils, as well as direct scavenging effects on existing ROS.
In addition, azelaic acid has been shown to directly inhibit kallikrein-5 and cathelicidin expression in three models: in vitro (human keratinocytes), in murine skin and in the facial skin of patients with rosacea.
These anti-inflammatory properties of azelaic acid may play a role in the treatment of rosacea.
While the clinical significance of these findings regarding kallikrein-5 and cathelicidin and their impact on the pathophysiology of rosacea has not yet been fully demonstrated in a large clinical study, initial studies in human facial skin appear to confirm the in vitro and murine findings.
Pharmacokinetics: Azelaic acid penetrates into all layers of human skin after topical application of the gel. Penetration is faster into damaged skin than into intact skin. A total of 3.6 % of the dose applied is absorbed percutaneously after a single topical application of 1 g azelaic acid (5 g cream).
Clinical investigations in acne patients indicated similar absorption rates of azelaic acid from Azelaic acid (Skinoren) gel and cream.
A portion of the azelaic acid absorbed through the skin is excreted in unchanged form in the urine. The remaining portion is broken down by β-oxidation into dicarboxylic acids with shorter chain length (C7, C5) which have likewise been found in the urine.
Steady-state plasma levels of azelaic acid in rosacea patients after 8 weeks twice daily treatment with Azelaic acid (Skinoren) gel were within the range also observed in volunteers and acne patients on normal diets. This indicates that the extent of percutaneous absorption of azelaic acid following twice daily application of Azelaic acid (Skinoren) gel does not alter the systemic burden of azelaic acid derived from dietary and endogenous sources in a clinically meaningful way.
Indications/Uses
Treatment of acne vulgaris, papulopustular rosacea.
Dosage/Direction for Use
Method of administration: Cutaneous use.
Dosage regimen: Azelaic acid (Skinoren) gel should be applied to the affected areas of skin twice a day (morning and evening) and rubbed in gently.
Approximately 0.5 g = 2.5 cm (1 inch) of gel is sufficient for the entire facial area.
It is important to continue to use Azelaic acid (Skinoren) gel regularly over the entire period of treatment.
The duration of use of Azelaic acid (Skinoren) gel can vary from patient to patient and also depends on the severity of the skin disorder. In general, a distinct improvement becomes apparent after about 4 weeks. To obtain the best results, Azelaic acid (Skinoren) gel should be used continuously over several months.
In the event of intolerable skin irritation (see Adverse Reactions), the amount of gel per application should be reduced or the frequency of use of Azelaic acid (Skinoren) gel should be reduced to once a day until the irritation ceases. If required, treatment might have to be temporarily interrupted for a few days.
Additional information on special populations: Pediatric Patients: Use in adolescents (12-18 years of age) for the treatment of acne vulgaris. Dose adjustment is not required when Azelaic acid (Skinoren) gel is administered to adolescents aged 12-18 years.
Overdosage
Results from acute toxicity studies do not indicate that any risk of acute intoxication is to be expected following a single dermal application of an overdose (application over a large area under conditions favorable to absorption) or inadvertent oral ingestion.
Contraindications
Hypersensitivity to the active substance or to any of the excipients of the gel.
Special Precautions
For external use only.
Care must be taken when using Azelaic acid (Skinoren) gel to avoid from coming into contact with the eyes, mouth and other mucous membranes, and patients should be instructed accordingly. In the event of accidental contact, the eyes, mouth and/or affected mucous membranes should be washed with large amounts of water. If eye irritation persists, patients should consult a physician. The hands should be washed after each application of the Azelaic acid (Skinoren) gel.
It is advisable to avoid alcoholic cleansers, tinctures and astringents, abrasives and peeling agents when using Azelaic acid (Skinoren) gel for treatment of papulopustular rosacea.
Effects on ability to drive or use machines: Azelaic acid (Skinoren) gel has no influence on the ability to drive and use machines.
Use In Pregnancy & Lactation
Pregnancy: 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.
Lactation: 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 since azelaic acid is not concentrated in milk and systemic uptake of topically applied azelaic acid did not increase endogenous azelaic acid exposure above physiological levels.
However, caution should be exercised when Azelaic acid (Skinoren) gel is administered to a nursing woman.
Adverse Reactions
Summary of the safety profile: Only cutaneous treatment-related adverse events were reported in clinical studies. In the great majority of cases the symptoms were mild or moderate; the frequency of irritative symptoms gradually decreased during the course of therapy.
In clinical studies, most frequently observed side effects included application site pruritus, application site burning, and application site pain.
Tabulated list of adverse reactions: Frequencies of side effects observed in clinical studies and given in the tables as follows are defined according to the MedDRA frequency convention: Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1,000 to <1/100), Rare (≥1/10,000 to <1/1,000), Very rare (<1/10,000), not known (cannot be estimated from the available data).
Acne: See Table 1.

Click on icon to see table/diagram/image

Rosacea: See Table 2.

Click on icon to see table/diagram/image

Description of selected adverse reactions: The following additional adverse reactions have been reported during post-approval use of Azelaic acid (Skinoren) gel (frequency unknown): Hypersensitivity, which may occur with one or more of the following adverse reactions: Angioedema, Eye swelling, Swelling face, Dyspnoea; Skin irritation; Urticaria; Worsening of asthma.
Additional information on special populations: Pediatric patients: Treatment of acne vulgaris in adolescents 12-18 years of age: In 4 clinical phase II and II/III studies involving adolescents 12-17 years of age (120/383; 31%), the overall incidence of adverse events for Azelaic acid (Skinoren) gel was similar for the groups aged 12-17 years (40%), aged ≥18 years (37%) and for the entire patient population (38%). This similarity also applied to the group aged 12-20 years (40%).
Drug Interactions
There have been no interaction studies of Azelaic acid (Skinoren) gel with other drugs.
Caution For Usage
Incompatibilities: None.
Storage
Store at temperatures not exceeding 30°C.
Shelf life: 36 months.
ATC Classification
D10AX03 - azelaic acid ; Belongs to the class of other topical preparations used in the treatment of acne.
Presentation/Packing
Topical gel 150 mg/g (white to yellowish-white opaque gel) x 30 g.
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