Name:
Celestoderm-v with garamycin. Release form Ointment. INN Betamethasone + gentamicin. FTG Glucocorticosteroid + antibiotic aminoglycoside. Composition 1 g of ointment 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 soft paraffin; mineral oil.
Description:
Homogeneous ointment from almost white to light yellow color without 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 C1, C1a 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, the EUCAST breakpoints are not relevant for topical gentamicin preparations, since local antibiotic concentrations are 250-500 times higher than the breakpoints when the ointment is used. 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 ointment. 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 application of the ointment, 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 the 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. The rate of absorption of gentamicin through the skin when applying 0.1% cream topically to intact skin is about 2% of the applied volume. The corresponding figure for 0.1% ointment is approximately 0.5%. On average, when applying gentamicin cream, 6.9 μg per 1 cm2 of the wound surface is absorbed, and approximately 1.5 μg of gentamicin when applied in the form of an ointment. This active substance can reach a concentration of 1 µg/ml in serum, which corresponds to approximately 10% of the level of minimal toxic effect. Serum levels of 3 to 4.3 µg/mL have been achieved following topical application of gentamicin in burn skin lesions. 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. Some topical glucocorticoids and their metabolites are also excreted in the bile. Due to the essential enzymatic mechanism of aminoglycoside resistance, there are numerous cases of incomplete, unilateral and complete parallel resistance between microorganisms and various aminoglycoside antibiotics. Indications for use The drug is indicated for the treatment of skin diseases that require the use of potent glucocorticosteroids, in the presence of superinfection caused by microorganisms sensitive to gentamicin. Dosage and administration Dosage The ointment should be applied 2-3 times a day. In children, the drug is used 1 time per day. With the improvement of the patient’s condition, the frequency of use of the drug can be reduced. How to use The ointment should be applied in a thin layer to the affected areas of the skin. The treated areas should not exceed 10% of the total body surface area. In children, the drug should be used only for a short period of time and on small areas of the skin. Special care should be taken when treating children with drugs containing corticoids, since the absorption of glucocorticoids through the skin of a child is more intense than in adults. Do not use the drug under occlusive dressings due to the possible risk of absorption of betamethasone valerate. The ointment should be applied to dry, flaky and stratum corneum. 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 ointment once a day. 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 Not recommended for use in preschool children. In children younger than 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 use of an occlusive dressing can also enhance the systemic absorption of active substances. 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 Hypersensitivity to the active and auxiliary components of the drug, other glucocorticosteroids and aminoglycosides; viral infections (such as herpes or chickenpox); skin form of tuberculosis and syphilis; skin reactions to vaccines; atrophic skin diseases; rosacea and rosacea-like dermatitis, perioral dermatitis; dermatomycosis; progressive renal failure; simultaneous use of systemic aminoglycoside antibiotics (due to the risk of toxic levels in the blood serum); application in the area of deep wounds, ear canal, eyes, on mucous membranes, under occlusive dressings; pregnancy; children’s age up to 1 year. 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. Since gentamicin is absorbed in minimal amounts, it is likely that there will be no other toxicity associated with overdose. 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 then continue to use it as usual. Precautions: Preparations containing gentamicin should be used with caution for specific therapy. Such drugs should be used only if a rapid response to antiseptic procedures is not achieved, antiseptic therapy is not effective enough, or if an antiseptic is contraindicated. Any adverse reaction reported with systemic corticosteroids, including adrenal suppression, may also occur with topical glucocorticoids, especially in infants and children. 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. Systemic absorption of topical glucocorticoids generally increases with glucocorticoid dose, duration of treatment, and body surface area treated. Therefore, patients receiving large doses of potent glucocorticoids (such as betamethasone valerate) over a large body surface area should be monitored at regular intervals to rule out suppression of the hypothalamic-pituitary-adrenal axis. If suppression is observed, the use of the drug should be discontinued, or it should be used with less frequency or a weaker glucocorticoid should be prescribed. The function of the hypothalamic-pituitary-adrenal system, as a rule, is completely restored after discontinuation of the drug. Very rarely, withdrawal symptoms may occur, requiring additional treatment with a systemic glucocorticoid. Allergies resulting from topical application of preparations containing gentamicin (such as creams/ointments) preclude further use of gentamicin and another aminoglycoside, eg in the form of infusions. Cross-allergenicity between aminoglycosides has been observed. Prolonged use of preparations containing an antibiotic may lead to overgrowth of non-susceptible microorganisms, in particular fungi. In this case, as well as in case of skin irritation, allergic reactions or superinfection, treatment with gentamicin should be discontinued and appropriate treatment instituted. Due to the ability of aminoglycosides to lead to neuromuscular blockade in case of systemic action, caution should be exercised when using the drug in patients with myasthenia gravis, Parkinson’s disease or other conditions accompanied by muscle weakness, as well as in patients who are simultaneously receiving other drugs with a neuroblocking effect. Due to the presence of an excipient in the composition of the preparation, white soft paraffin, when treated with an ointment of the genital organs or the anal area, a decrease in the tensile strength of the latex may be noted and, consequently, there may be a decrease in the safety of using condoms made from latex. The ointment should not be applied to wounds or ulcers on the legs, as well as in the area of u200bu200bnatural folds. Use with caution on the face. If the drug is to be used to treat tssoriasis, 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 an ointment can mask the clinical symptoms of diseases, which is typical for all glucocorticoids. As with systemic corticosteroids, glaucoma may develop with topical corticosteroids (especially after overuse, under occlusive dressings, or after application to the skin around the eyes). 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. 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® ointment 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 forms of interaction Due to the potential for 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 release By prescription. Buy Celestoderm-V with garamycin ointment (1mg + 1mg) / 1g 30g No. 1 Price for Celestoderm-B with garamycin ointment (1mg + 1mg) / 1g 30g No. 1 +1mg)/1g 30g №1
INN | GENTAMYCIN + BETAMETASONE |
---|---|
The code | 135 131 |
Barcode | 4 814 366 000 408 |
Dosage | (1mg+1mg)/1g 30g |
Active substance | Betamethasone, gentamicin |
Manufacturer | Schering-Plough Labo N.V., Belgium |
Importer | IOOO "Interfarmaks", Republic of Belarus, 223028, Minsk region, Minsk district, Zhdanovichsky s / s, ag. Zhdanovichi, st. Zvezdnaya, 19A-5, pom. 5-2; Republican unitary enterprise "Belpharmacy" Minsk, 220005, Republic of Belarus, Minsk, st. V. Khoruzhey, 11; [x] Brest Trade and Production Republican Unitary Enterprise "Pharmacy", 224032, Brest, Ya. Kupala st., 104; [x] Vitebsk Unitary Enterprise "Pharmacy", 210016 Vitebsk, Velikoluksky tract, 63; [x] Gomel Unitary Enterprise "Pharmacy", 246027, Gomel, B. Khmelnitsky str., 75; [x] Grodno Trade and Production Republican Unitary Enterprise "Pharmacia", 230023 Grodno, Ozheshko St., 11; [x] Mogilev Trade and Production Republican Unitary Enterprise "Pharmacy", 212030 Mogilev, Pervomayskaya st., 59; [x] Trade and Production Republican Unitary Enterprise "MINSKAYA PHARMACIA", 220039, Minsk, Chkalova st., 5; [x] Closed Joint Stock Company "BEROLINA", 220114, Minsk, Nezavisimosti Ave., 143/1-3n; [x] Additional Liability Company "Farmin", 220125 Minsk, Nezalezhnosti Avenue, 177, room 62; Private trade unitary enterprise "Improvement", RB, RB, Minsk, Melezha st., 1 office. 1501 |
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