Cremgen® [Gentamicin, Fluocinonide]

Pharmacological properties

Cremgen is a combined preparation for external use containing corticosteroids fluocinonide and the aminoglycoside antibiotic gentamicin. the effect of the drug is due to the synergistic effects of its components that make up its composition.

Fluocinonide is a synthetic high-performance corticosteroids of the third generation. It has a pronounced and prolonged anti-inflammatory, anti-allergic, decongestant and antipruritic effect. Stabilizes lysosome membranes, inhibits lysosomal phospholipase A₂, which leads to a decrease in the formation of inflammatory mediators of eicosanoids, cytokines (IL-1 and -2, γ-interferon, TNF-α), blocks the cascade of conversion of arachidonic acid to prostaglandins, prevents cell disintegration during the inflammatory process. Stimulation of steroid receptors leads to the formation of a special class of proteins - lipocortins, which have a pronounced decongestant effect.

The second-generation aminoglycoside antibiotic gentamicin has a pronounced bactericidal effect. The mechanism of its antimicrobial activity is the binding of microorganisms to the 30S subunit of the ribosomes, which causes irreversible inhibition of protein synthesis. Gentamicin is fixed on the cytoplasmic membranes of bacteria, violates their permeability, leads to the loss of potassium ions, amino acids, nucleotides by cells. Gentamicin acts bactericidal against Streptococcus spp., Staphylococcus spp. (including MRSA), Pseudomonas spp., Escherichia coli, Proteus spp., Klebsiella spp., Shigella spp., Salmonella spp., Enterobacter spp., Acinetobacter spp. and other bacteria.

Pharmacokinetics The components of the drug, when applied topically, easily penetrate into all layers of the skin, including inflamed, erosive and burned areas, exerting a therapeutic effect. Upon contact with the skin, fluocinonide deesterifies, releasing fluocinolone, which also has a pronounced glucocorticoid effect. Due to the effect of deesterification, fluocinonide, when applied topically, practically does not enter the systemic circulation. The gentamicin molecule is characterized by sharply hydrophilic properties, therefore it does not penetrate biological membranes, such as the skin, intestinal wall, and does not enter the systemic circulation when applied topically.

Indications

Inflammatory and allergic skin diseases, including those complicated by a secondary bacterial infection: eczema of various forms and localization, dermatitis (atopic, contact, allergic, seborrheic, radiation, intertriginous, exfoliative, sun), psoriasis, senile itching, lichen planus, discoid systemic lupus erythematosus, trophic ulcers (except for leg ulcers associated with varicose veins), burns and frostbite of the skin of the first degree, bites of insects and arthropods.

Application

Cremgen is applied a thin layer on the affected skin 2-3 times a day. the duration of the course of treatment is determined by the doctor individually and depends on the nature of the course of the disease.

Children. The drug is prescribed for children over the age of 2 years. The drug should be used with caution, under the supervision of a doctor, only 1 time per day, on a small area of ​​the skin. Do not apply ointment to the skin of the babys face. The use of this drug is possible only if the expected benefit exceeds the potential risk of adverse reactions. In the case of the use of the drug in children, it is necessary to take into account the possibility of signs of depression of the hypothalamic-pituitary-adrenal system, which develop in children more often than in adult patients, which is associated with a greater absorption of the drug in children due to the greater value of the ratio of skin area to body weight . In children receiving corticosteroids for topical administration, inhibition of adrenal function, Itsenko-Cushings syndrome, stunted growth, insufficient weight gain, and increased intracranial pressure were noted. Manifestations of inhibition of the functions of the adrenal cortex: a low level of cortisol in the blood plasma and the lack of reaction to the sample during stimulation of the adrenal glands with the use of ACTH drugs. An increase in intracranial pressure is manifested by protrusion of the fontanel, headache, bilateral edema of the optic disc.

Contraindications

Infectious skin diseases (viral, bacterial, fungal), including skin manifestations of syphilis, tuberculosis of the skin, pyoderma, chicken pox, herpes, actinomycosis, blastomycosis, sporotrichosis; rosacea and acne vulgaris; diaper dermatitis, perioral dermatitis; anogenital itching; neoplasms of the skin, skin tumors; nevus, atheroma, hemangioma, xanthoma; wounds in areas of applications; numerous psoriatic plaques, trophic ulcers of the lower leg associated with varicose veins, ulcerative skin lesions; erosive and ulcerative lesions of the digestive tract, hypersensitivity to active substances or other components of the drug. Cremgen is contraindicated in ophthalmic practice. do not use the drug after preventive vaccinations.

Side effects

On the part of the skin and subcutaneous tissue: burning sensation, irritation, erythema, itching, dry skin, folliculitis, hypertrichosis, striae, acne, perioral dermatitis, allergic contact dermatitis, urticaria, spotted-papular rashes, maceration of the skin at the site of application, integrity skin, hyperkeratosis, furunculosis, fungal infections of the skin. with prolonged use, skin atrophy, local hirsutism, telangiectasia, purpura, pigmentation disorders, hypertrichosis, alopecia, especially in women, may develop secondary infectious skin lesions.

From the digestive tract: when applied to large areas of the skin, especially with prolonged use, gastritis and a steroid ulcer are possible.

From the endocrine system: hyperglycemia. When applied to large areas of the skin, systemic manifestations are possible: adrenal insufficiency, Itsenko-Cushings syndrome, steroid diabetes mellitus.

From the side of the immune system: decreased body resistance. With prolonged use, it is possible: the development of secondary immunodeficiency (exacerbation of chronic infectious diseases, generalization of the infectious process, the development of opportunistic infections), the slowdown of reparative processes, the development of local and generalized manifestations of allergic reactions.

From the cardiovascular system: AH, edema may develop.

special instructions

Treatment must be carried out under the supervision of a physician. it is advisable to use the drug in short courses (no more than 10 days), in small areas of the skin. with prolonged use on large areas of the skin, the incidence of side effects associated with iatrogenic hypercorticism increases: edema, arterial hypertension, hyperglycemia and a decrease in glucose tolerance. Before each repeated application of the preparation, the remnants of the old preparation should be washed off with a warm soapy solution or an antiseptic solution. during treatment it is recommended to wear loose clothing. do not use the drug under an occlusive dressing, as well as with lesions of the mucous membranes of the mouth, nose, eyes. use with caution on parts of the body with thin skin (face, inguinal and axillary areas), since it is possible to increase the degree of absorption and development of local side effects (telangiectasia, perioral dermatitis) even after a short application. do not apply on the skin of the mammary glands. Avoid applying the drug to the eyelids or skin around the eyes of patients with cataracts, angle-closure and open-angle glaucoma due to a possible increase in the severity of the symptoms of the disease. Avoid contact with eyes. if local irritation, fungal skin lesions or the development of hypersensitivity reactions occur during treatment, the drug must be discontinued. in the case of the development of an infection resistant to gentamicin, the appropriate antibacterial or antifungal treatment should be carried out at the place of application of the ointment.

With external use of the drug, it is possible: a decrease in the production of adrenocorticotropic hormone by the pituitary gland due to inhibition of the hypothalamic-pituitary-adrenal system, a decrease in the level of cortisol in the blood, and the development of iatrogenic Itenko-Cushings syndrome, which disappears after drug withdrawal.

If long-term use is necessary, periodic monitoring of the function of the adrenal cortex should be carried out by determining the levels of cortisol in the blood and urine after stimulation of ACTH.

Under special control, the drug should be used in patients with psoriasis, since topical application of GCS to areas affected by psoriasis can lead to the spread of relapse caused by the development of tolerance, the risk of generalized pustular psoriasis and systemic toxicity caused by skin dysfunction.

With caution, the drug should be used in the presence of atrophy of the subcutaneous tissue, especially in elderly patients.

During treatment, vaccination against smallpox is not recommended, as well as other types of immunization.

Gentamicin, which is part of the drug, can cause cross-allergic reactions with other aminoglycoside antibiotics. Systemic absorption of gentamicin with topical application may be higher with treatment on large surfaces of the body, especially with prolonged use or the presence of skin lesions. In such cases, unwanted effects associated with systemic absorption of gentamicin may occur. Appropriate precautions are recommended in such cases, especially in the treatment of infants and children.

Prolonged local use of antibiotics can sometimes lead to the growth of resistant microflora, including fungal. In this case, therapy should be discontinued and appropriate treatment prescribed.

During pregnancy and breastfeeding. the drug is contraindicated during pregnancy. For the period of treatment with the drug, breastfeeding should be canceled.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. The drug does not affect the speed of psychomotor reactions.

Interactions

The drug can enhance the effect of immunosuppressive drugs and suppress the effect of immunostimulating, antihypertensive, diuretic, antiarrhythmic drugs, potassium preparations.

The drug can be used with other antimicrobial agents of local and systemic action. Combined use with systemic corticosteroids increases the effectiveness of the drug, but also increases the likelihood of developing systemic and local side effects.

Combined use with NSAIDs increases the risk of developing systemic and local side effects.

With simultaneous use with diuretics (except potassium-sparing), the likelihood of developing hypokalemia increases.

Insignificant absorption with external use does not lead to interaction with other drugs.

During treatment with the drug, vaccinations against smallpox are not recommended, as well as other types of immunization (especially with prolonged use on large areas of the skin) due to the possible lack of an adequate immunological response in the form of the production of appropriate antibodies.

Overdose

With prolonged or excessive use of local glucocorticosteroids, including fluocinonide, especially in children, the risk of developing systemic effects (secondary adrenal insufficiency and the appearance of symptoms of hypercorticism) is not ruled out. symptoms of hypercorticism are usually reversible. prolonged topical use of gentamicin can lead to the growth of resistant fungal or bacterial microflora. symptomatic treatment. with prolonged use in large areas of the skin, overdose symptoms may develop, which are manifested by an increase in the severity of side effects.

Storage conditions

At a temperature not exceeding 25 ° C.