Product Overview
Composition
Active ingredients:
methylprednisolone aceponate 100 mg;
urea 2 g;
Excipients:
liquid paraffin (vaseline oil) - 15 g,
propylene glycol - 5 g,
polysorbate 80 - 1 g,
carbomer interpolymer (type A) - 1 g,
trometamol - 400 mg,
methyl parahydroxybenzoate - 100 mg,
purified water - up to 100 g ...
pharmachologic effect
Comfoderm® M2 is a combined preparation, the action of which is due to its constituent components.
Methylprednisolone aceponate is a non-halogenated synthetic steroid.
When used externally, methylprednisolone aceponate suppresses inflammatory and allergic skin reactions associated with increased proliferation, which leads to a decrease in objective symptoms of inflammation (erythema, edema, oozing) and subjective sensations (itching, irritation, pain, etc.). When methylprednisolone aceponate is used externally at the recommended dose, the systemic effect is minimal in both humans and animals. After repeated application of methylprednisolone aceponate to large surfaces (40-60% of the skin surface), as well as when applied under an occlusive dressing, there are no adrenal dysfunctions: the level of cortisol in plasma and its circadian rhythm remain within normal limits, the concentration of cortisol in daily urine does not decrease. going on.
Methylprednisolone aceponate (especially its main metabolite, 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticoid receptors. The steroid-receptor complex binds to specific regions of the immune response cells' DNA, thus causing a series of biological effects.
In particular, binding of the steroid-receptor complex to DNA cells of the immune response leads to the induction of macrocortin synthesis. Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammatory mediators such as prostaglandins and leukotrienes.
Inhibition of the synthesis of vasodilating prostaglandins by glucocorticosteroids and the potentiation of the vasoconstrictor action of adrenaline lead to a vasoconstrictor effect.
Urea - has keratolytic and moisturizing effects. Urea helps to bind water and thereby soften the stratum corneum. In addition to keratolytic action, urea has proteolytic activity.
Pharmacokinetics
When methylprednisolone is applied topically, aceponate is hydrolyzed in the epidermis and dermis. The main and most active metabolite is 6α-methylprednisolone-17-propionate, which has a significantly higher affinity for glucocorticosteroid receptors in the skin, which indicates the presence of its "bioactivation" in the skin.
The degree of percutaneous absorption depends on the condition of the skin and the method of application (with or without an occlusive dressing).
Percutaneous absorption in patients with atopic dermatitis (neurodermatitis) and psoriasis is no more than 2.5%, which is only slightly higher than that in healthy volunteers (0.5-1.5%).
After entering the systemic circulation, 6α-methylprednisolone-17-propionate is rapidly conjugated to glucuronic acid and thus inactivated.
Metabolites of methylprednisonolone aceponate are eliminated mainly by the kidneys with a half-life of about 16 hours. Methylprednisolone aceponate and its metabolites do not accumulate in the body.
Due to the low absorption of urea when applied topically, the likelihood of its systemic effects is low.
Indications
- atopic dermatitis, neurodermatitis;
- true eczema;
- microbial eczema;
- simple contact dermatitis;
- allergic (contact) dermatitis;
- dyshidrotic eczema.
Contraindications
- Hypersensitivity to drug components;
- tuberculous or syphilitic processes in the area of ​​application of the drug;
- viral diseases (for example, chickenpox, shingles);
- rosacea, perioral dermatitis in the area of ​​application of the drug;
- areas of the skin with manifestations of a reaction to vaccination;
- children under 18 years of age.
Side effects
If the drug is used for more than 4 weeks and / or on an area of ​​10% or more of the body surface, the following reactions may occur: skin atrophy, telangiectasia, striae, acneform skin changes, systemic effects due to the absorption of a corticosteroid.
In rare cases (0.01% -0.1%), folliculitis, hypertrichosis, perioral dermatitis, skin depigmentation, allergic reactions to one of the drug components may occur.
Interaction
borne in mind that the simultaneous use of Comfoderm M2 with other ointments or creams can lead to an increase in the resorption of their constituent drugs.
How to take, course of administration and dosage
The drug is applied 1 time / day with a thin layer on the affected skin. As a rule, the duration of continuous daily treatment with
Comfoderm M2 should not exceed 12 weeks. When treating patients with facial skin lesions, the course of treatment should not exceed 5 days.
Overdose
with excessively long and / or intensive local application of GCS, skin atrophy (thinning of the skin, telangiectasia, striae) may develop.
Treatment:
if signs of skin atrophy appear, the drug must be canceled.
Special instructions
The drug is not intended for use in ophthalmology. Avoid contact with the eyes and mucous membranes.
As with the use of systemic glucocorticoids, with external use of GCS, glaucoma may develop (for example, after use in high doses, due to very long-term use, the use of occlusive dressings or application to the skin around the eyes).
On the skin of the face, more often than on other surfaces of the body, after long-term treatment with GCS for external use, atrophic changes may develop.
Influence on the ability to drive vehicles and control mechanisms
Not identified.
