Celestoderm-V with garamycin cream (1mg+1mg)/1g 30g №1

Product Description Celestoderm-V with Garamycin. Release form Cream. Composition 1 g of cream contains active ingredients: betamethasone 1,000 mg in the form of betamethasone valerate 1,220 mg and gentamicin 1,000 mg (1000 IU) in the form of gentamicin sulfate. excipients: white petrolatum, cetostearyl alcohol, liquid paraffin, macrogol cetostearyl ether, sodium dihydrophosphate dihydrate, chlorocresol, phosphoric acid, phosphoric acid / sodium hydroxide, purified water. DescriptionWhite or almost white homogeneous cream of soft consistency, which does not contain foreign inclusions. Pharmacotherapeutic group Corticosteroids for use in dermatology. Corticosteroids in combination with antibiotics. ATC code D07C С01. Pharmacological properties Pharmacodynamics Betamethasone Betamethasone valerate is a synthetic glucocorticoid for topical use. Betamethasone, a prednisolone derivative, has high glucocorticoid activity and only minimal mineralocorticoid properties. Due to their anti-inflammatory, antipruritic and vasoconstrictive effects, topical glucocorticoids (such as betamethasone valerate) are initially indicated for the treatment of glucocorticoid-responsive dermatoses. For pharmacodynamic comparison of the effectiveness of betamethasone valerate and various known topical fluorinated glucocorticoids, the Mackenzie vasoconstrictor test can be used. In this betamethasone test, valerate showed a blanching level of 360 relative to flucinolone acetonide = 100 (other blanching scores for comparison: hydrocortisone > 1; triamcinolone acetonide: 75). Gentamicin Gentamicin is an aminoglycoside antibiotic. It is a mixture of structurally closed homologously gentamicin Sc Cia and C2. Mechanism of action The mechanism of action of gentamicin is based on disruption of protein biosynthesis through interaction with ribosomal RNA and subsequent incorporation of errors into amino acids during translation. This leads to a bactericidal action. Pharmacokinetic / pharmacodynamic relationships Efficacy mainly depends on the ratio of the maximum concentration achieved at the site of action (Cmax) and the minimum inhibitory concentration of the microorganism. Mechanism of resistance Gentamicin resistance may be due to the following mechanisms: Enzyme inactivation: Enzymatic inactivation of aminoglycoside molecules is the most common resistance mechanism. A role is played by acetyltransferases, phosphotransferases, or nucleotidyltransferases, most of which are encoded by the plasmid. Impaired penetration and active efflux: These resistance mechanisms are mainly related to Pseudomonas aeruginosa. Modification of target structure: modifications within ribosomes are the causes of resistance. They occur either by mutation or by the formation of methyltransferases. Gentamicin, as a rule, has cross-resistance with other aminoglycoside antibiotics. Breakpoints Gentamicin is tested using standard dilution series. The following minimum inhibitory concentrations have been established for susceptible and resistant organisms. EUCAST breakpoints Microorganism Susceptibility Resistance Enterobacteriaceae ≤ 2 mg/l > 4 mg/l Pseudomonas spp. ≤ 4 mg/l > 4 mg/l Acinetobacter spp. ≤ 4 mg/l > 4 mg/l Staphylococcus spp. ≤ 1 mg/l > 1 mg/l Breakpoints, non-species-specific1 * ≤ 2 mg/l1 > 4 mg/l1 1 Breakpoints for intravenous use of gentamicin at a dose of 3-4.5 mg/kg/day. * Based primarily on serum pharmacokinetics. These data are based mainly on the pharmacokinetic levels achieved in the blood serum. However, EUCAST breakpoints are not relevant for topical gentamicin preparations, as local antibiotic concentrations are 250-500 times higher than the breakpoint when using the cream. Since the concentration of the antibiotic is high at the site of application, it is unlikely that resistance will occur with topical application of the cream. In a multicentre in vitro study conducted to determine the resistance of skin microorganisms to gentamicin, all strains of S. aureus and S. pyogenes tested were susceptible starting at concentrations of 128 mg/L. Since concentrations of up to 1000 mg/l are achieved with the cream, no strains of S. aureus and S’, pyogenes with resistance to gentamicin have been found. Как правило, чувствительные виды Аэробные грамположительные микроорганизмы Staphylococcus aureus Staphylococcus saprophyticus Аэробные грамотрицательные микроорганизмы Acinetobacter pittii Citrobacter freundii Enterobacter aerogenes Enterobacter cloacae Escherichia coli# Klebsiella oxytoca Klebsiella pneumoniae Proteus vulgaris Proteus mirabilis Salmonella enterica (сальмонеллезный энтерит) Serratia liquefaciens Serratia marcescens Виды, у которых приобретенная резистентность может быть проблемой во время лечения Аэробные грамположительные микроорганизмы Staphylococcus epidermidis Staphylococcus haemolyticus Staphylococcus hominis Аэробные грамотрицательные микроорганизмы Acinetobacter baumannii Morganella morganii Pseudomonas aeruginosa Виды с естественной резистентностью Аэробные грамположительные микроорганизмы Виды Enterococcus§ Виды Streptococcus§ Аэробные грамотрицательные микроорганизмы Burkholderia cepacia Legionella pneumophila Stenotrophomonas maltophilia Анаэробные микроорга nisms Bacteroides Clostridium difficile spp. Other organisms Chlamydia spp. Chlamydophila spp. Mycoplasma spp. Ureaplasma urealyticum § Proven clinical efficacy in the treatment of endocarditis caused by enterococci and streptococci, in combination with penicillin, if there is no persistent resistance (enterococci). Pharmacokinetics Gentamicin can be used parenterally or topically, but is not suitable for oral administration, since absorption of the drug in the intestine is minimal. Local antibiotics are metabolized after penetration through the skin in the same way as with parenteral administration. Average maximum concentrations of gentamicin 3.5-6.4 mg/l are achieved 30-60 minutes after intramuscular administration of gentamicin at a dose of 1 mg/kg of body weight. The half-life is approximately 2 hours during the first 8-12 hours, after which gentamicin is gradually released from the deep compartments with a half-life of 100-150 hours. Excreted only by the kidneys through glomerular filtration in an unchanged and biologically active form. Based on absorption rates, no systemic effects are expected. After application of gentamicin preparations to intact and undamaged skin, the absorption of the active substance from the cream is approximately 2%. With abundant use for burns, when the stratum corneum is absent or severely damaged, a significantly greater degree of absorption of the drug should be expected, regardless of the water content in the drug or the wound. The pharmacokinetic profile of topical glucocorticoids after penetration through the skin is similar to that of systemic glucocorticoids. Glucocorticoids bind to plasma proteins to varying degrees, are metabolized mainly in the liver and excreted by the kidneys. Systemic absorption of topical glucocorticoids is expected only under unfavorable conditions (long-term treatment, occlusive dressings). Percutaneous absorption of betamethasone valerate from an emulsion (water-oil) was evaluated in healthy men on experimentally damaged skin. After 24 hours, 68.1 ± 6.9% of the 3H-labeled dose of 200 mg was found in the skin. With urine and feces for 72 hours, 7.34 ± 2.74% and 4.80 ± 0.76%, respectively, of the applied dose were excreted. Indications for use Skin diseases that respond to treatment with strong corticosteroids in the presence of bacterial superinfection caused by microorganisms sensitive to gentamicin. Dosage and administration Dosage The cream should be applied 2-3 times a day. With the improvement of the patient’s condition, the frequency of use of the drug can be reduced. How to use The cream should be applied in a thin layer on the affected areas of the skin. The method of application should be adapted to the type of skin and the stage of the disease. The drug is recommended for application, in particular, for oily, weeping, itchy skin, burning sensation and seborrheic skin diseases, in the acute stage of diseases. Duration of use The duration of treatment with the drug should not exceed 7-10 days (7 days in children), since it contains gentamicin. After medical confirmation that the use of a combination agent is not necessary (for example, dermatosis, which requires the use of a potent glucocorticoid, or superinfection caused by microorganisms sensitive to gentamicin), treatment should be continued on the basis of single-component therapy or with a glucocorticoid (possibly of a weaker effect) or with an antibiotic. In mild cases, it is enough to apply the cream once a day. The surface area of the treated skin should not exceed 10% of the body surface. If the drug is used on the face, the treatment should be as short as possible, not more than one week. Features of use in children Once a day, on the smallest possible area and in the shortest course. Not recommended for use in preschool children. In children under 10-15 years of age, strong corticosteroids should not be used unless clearly indicated. Side effectsAdverse reactions with the use of the drug were reported very rarely; these included hypersensitivity, rash, and discoloration of the skin. The following local adverse reactions have been reported with the use of topical corticosteroids, especially with the use of occlusive dressings: burning, itching, irritation, dryness, folliculitis, skin hypopigmentation, steroid acne, acne-like skin rash, dilation of small superficial skin vessels, hypertrichosis, perioral dermatitis, allergic contact dermatitis, skin maceration, skin atrophy, secondary infection, striae and prickly heat, cracking, redness at the application site, telangiectasia. The cream is generally well tolerated. In very rare cases, skin irritation associated with individual hypersensitivity to gentamicin may occur. The composition of the drug includes chlorocresol and cetostearyl alcohol. Chlorocresol may cause allergic reactions. Rarely, hypersensitivity reactions to these substances have been reported. In such cases, drug treatment should be discontinued. Possible manifestation of systemic effects of corticosteroids due to absorption when applied over large areas / prolonged use or under occlusive dressings: reversible suppression of the hypothalamic-pituitary-adrenal axis with manifestations of Cushing’s syndrome (obesity, roundness of the face, hunchback, delayed recovery syndrome, mental symptoms, etc.). hyperglycemia and glucosuria, benign intracranial hypertension, arterial hypertension, edema, hypokalemia, osteoporosis, hyperthyroidism, increased total cholesterol, low-density lipoprotein and triglycerides, peptic ulcer, paresthesia, cataract (subcapsular), unusual hair loss, hypertrichosis, perioral dermatitis and skin discoloration. Local application of gentamicin can lead to disruption of granulation. In addition, after topical application of gentamicin, ototoxic, nephrotoxic and vestibular disorders can be observed, especially with repeated use on large surfaces. Treatment with gentamicin may cause transient irritation (erythema and pruritus). Systemic adverse reactions, such as blurred vision, have also been reported with topical corticosteroids. Children Children may be more susceptible to the action of local glucocorticosteroids, which cause depression of the hypothalamic-pituitary-adrenal system, and to the action of exogenous glucocorticoids than older patients. This is due to the higher absorption of the drug in children due to the greater ratio of surface area to body weight. In children receiving local glucocorticosteroids, depression of the function of the hypothalamic-pituitary-adrenal system, Cushing’s syndrome, linear growth retardation, lag in weight gain, and increased intracranial pressure may be observed. Symptoms of hypothalamic-pituitary-adrenal system depression in children include low plasma cortisol levels and lack of response to ACTH stimulation. An increase in intracranial pressure is manifested by bulging fontanel, headache, bilateral edema of the optic discs. Contraindications The drug is contraindicated in patients with a history of hypersensitivity to betamethasone valerate, gentamicin sulfate, chlorocresol or any other substance that is part of the drug, as well as in patients with hypersensitivity to other glucocorticoids or aminoglycoside antibiotics. The drug should not be used in skin diseases caused initially by bacteria or a virus. The drug is contraindicated in skin tuberculosis and syphilis. Long-term use of the drug, application to large areas of the skin, mucous membranes and / or use under occlusive dressings should be avoided. The drug should not be used in patients with fungal skin diseases. The cream should not be used during pregnancy, since the drug contains betamethasone valerate. The drug should not be used in patients with diseases such as rosacea, perioral dermatitis, atrophic skin diseases and skin reactions to the vaccine. The drug should not be used in the area of the eyes, ear canal or deep wounds, children under the age of one year, while the systemic use of aminoglycosides due to the risk of toxic serum levels, with renal failure. Overdose The drug should be used only in the recommended dose. Symptoms: Excessive or prolonged use of topical glucocorticoids can inhibit the function of the pituitary-adrenal system, leading to secondary adrenal insufficiency and manifestations of excessive use of glucocorticoids, including Cushing’s syndrome. Excessive or prolonged use of topical gentamicin may lead to overgrowth of fungi or non-susceptible bacteria. Treatment: If the patient accidentally ingested the drug, or uses a very large amount of the drug, or for a very long period of time, you should immediately consult a doctor. Acute symptoms of excessive use of corticosteroids are usually reversible. If necessary, carry out a correction of the electrolyte balance. In case of chronic toxic effects, gradual withdrawal of corticosteroids is recommended. In case of excessive growth of resistant microorganisms, it is recommended to stop treatment with the drug and prescribe the necessary therapy. If the patient has forgotten to take the drug, it should be applied immediately after the patient remembers the missed dose and continue to use it as usual. Precautions Systemic absorption of gentamicin when applied topically may be higher if the treatment is carried out on large surfaces of the skin, especially over a long period of time, or if the integrity of the skin is violated. In these cases, the adverse reactions observed with the systemic use of gentamicin can potentially occur. As a result, it is recommended to treat with caution, especially in children. Cross-allergenicity between aminoglycosides has been observed. Cetostearyl alcohol, which is part of the cream, can provoke the development of local skin reactions (for example, contact dermatitis). The drug is intended for use exclusively on the skin. Avoid getting the drug in the eyes. Prolonged use of preparations containing an antibiotic may lead to overgrowth of non-susceptible microorganisms, in particular fungi. Any adverse reaction reported with systemic corticosteroids, including adrenal suppression, may also occur with topical glucocorticoids, especially in infants and children. The cream should not be applied in the area of natural folds. Use with caution on the face. If the drug is to be used to treat psoriasis, the patient should be carefully monitored. It is important to prevent recurrence or the development of local or systemic toxicity due to impaired skin barrier function. The use of the cream can mask the clinical symptoms of diseases, which is typical for all glucocorticoids. With the use of systemic and local corticosteroids (including intranasal, inhalation and intraocular administration), visual disturbances may occur. If symptoms such as blurred vision or other visual disturbances occur, the patient should be evaluated by an ophthalmologist to evaluate possible causes of visual impairment, which may include cataracts, glaucoma, or rare diseases such as central serous chorioretinopathy, which have been reported after corticosteroid use systemic and local action. As with systemic corticosteroids, glaucoma may develop with topical corticosteroids (especially after overuse, when used under occlusive dressings, or after application to the skin around the eyes). Due to the ability of aminoglycosides to cause neuromuscular blockade in the case of systemic action, use with caution in patients with myasthenia gravis, other diseases accompanied by muscle weakness, in Parkinson’s disease, or in conjunction with other drugs that cause neuromuscular blockade. Use during pregnancy or lactation Pregnancy There are not enough data on the use of the drug in pregnant women. Animal studies with active ingredients have shown reproductive toxicity. Gentamicin crosses the placental barrier and reaches fetal tissues and amniotic fluid in measurable concentrations. Animal studies have shown reproductive toxicity. Betamethasone. In animal studies with other members of the glucocorticoid class, typical embryotoxic and teratogenic effects such as palatal malformations, skeletal anomalies, intrauterine growth retardation, and embryonic death have been observed. There is evidence of an increased risk of cleft lip and palate with systemic use of glucocorticoids during the first trimester of pregnancy in humans. Animal studies have shown that the administration of glucocorticoids at subteratogenic doses during pregnancy is associated with an increased risk of intrauterine fetal growth retardation, cardiovascular and/or metabolic disease in adulthood, and persistent changes in glucocorticoid metabolism, neurotransmitters, and behavior. Therefore, the use of Celestoderm-B® cream with Garamycin during pregnancy is contraindicated. If it is necessary to use glucocorticoids during pregnancy, such as hydrocortisone, prednisone or prednisolone should be used, since these substances are metabolized by the 11-beta-HSD enzyme in the placenta to inactive forms, therefore they are safer than most synthetic glucocorticoids. Breast-feeding There are no data on the excretion of betamethasone in breast milk. Other glucocorticoids and gentamicin pass into breast milk. Therefore, the drug can be used during lactation only if the potential benefit outweighs the potential risk. Drugs in this class should not be used in high doses, over large areas, or over a long period of time, and the child should not come into contact with treated skin areas. The ability to influence the reaction rate when driving vehicles or working with other mechanisms The drug does not affect the reaction rate when driving vehicles or working with other mechanisms. Interaction with other medicinal products and other types of interactions Due to the presence of white soft paraffin in the composition of the preparation, when the cream is applied to the genitals or anal area, a decrease in the tensile strength of the latex may be noted and, therefore, there may be a decrease in the safety of using condoms made from latex. Due to potential mutual inactivation, the cream should not be used simultaneously with other topical dermatological agents. Gentamicin is incompatible with amphotericin B, heparin, sulfadiazine and beta-lactam agents (such as cephalosporins), anionic excipients. Light, oxidizing agents and strong alkaline compounds lead to the degradation of glucocorticoids. Storage conditionsKeep out of the reach of children, at a temperature not exceeding 25°C. Shelf life 3 years. Packing 30 g in aluminum tubes. 1 tube in a cardboard box. Conditions of sale By prescription. Buy Celestoderm-V with garamycin cream (1mg + 1mg) / 1g 30g No. 1 Price for Celestoderm-B with garamycin cream (1mg + 1mg) / 1g 30g No. 1 +1mg)/1g 30g №1