Betazon ultra
Ukraine
Table of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT BETAZONE ULTRA (BETAZONEULTRA)
Composition:
Active substances: betamethasone, clotrimazole, gentamicin;
1 g of the preparation contains micronized betamethasone dipropionate equivalent to 0.5 mg of betamethasone, 10 mg of clotrimazole, and gentamicin sulfate equivalent to 1 mg of gentamicin;
Excipients: cetyl stearyl alcohol, polyethylene glycol stearate, white soft paraffin, mineral oil, propylene glycol, anhydrous disodium hydrogen phosphate, concentrated phosphoric acid, sodium hydroxide, benzyl alcohol, purified water.
Pharmaceutical form. Topical cream.
Main physicochemical properties: cream ranging from white to almost white, of homogeneous consistency.
Pharmacotherapeutic group. Corticosteroids for dermatological use. Corticosteroids in combination with antibiotics. Betamethasone and antibiotics.
ATC code D07CC01.
Pharmacological properties.
Pharmacodynamics.
The drug combines three actions: the anti-inflammatory effect of betamethasone dipropionate, the antibacterial activity of gentamicin sulfate, and the antifungal activity of clotrimazole.
Betamethasone dipropionate is a potent (class III) corticosteroid with anti-inflammatory, antiallergic, and antipruritic effects.
Gentamicin is an antibiotic from the aminoglycoside group with bactericidal activity. It inhibits protein synthesis in microorganisms sensitive to the antibiotic. Gentamicin is active against many aerobic gram-negative and a few gram-positive bacteria. In vitro, gentamicin at concentrations of 1–8 mcg/mL inhibits most sensitive strains of Escherichia coli, Haemophilus influenzae, Moraxella lacunata, Neisseria, indole-positive and indole-negative strains of Proteus, Pseudomonas (including most strains of Pseudomonas aeruginosa), Staphylococcus aureus, Staphylococcus epidermidis, and Serratia. Different species and strains of the same species may show significant differences in in vitro sensitivity. Moreover, in vitro sensitivity does not always correlate with in vivo sensitivity. Gentamicin is ineffective against most anaerobic bacteria, fungi, and viruses. Gentamicin has minimal efficacy against streptococci.
Resistance to gentamicin may develop in both gram-negative and gram-positive bacteria.
Clotrimazole is a synthetic antifungal agent from the imidazole derivatives group. Its spectrum of activity includes a range of fungi pathogenic for humans and animals. Clotrimazole provides effective action against dermatophytes, yeasts, and molds. In vitro studies have demonstrated clotrimazole's efficacy against Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida (including Candida albicans). Based on current knowledge, the antifungal effect of clotrimazole is due to inhibition of ergosterol synthesis. Ergosterol is a key component of the fungal cell membrane.
Pharmacokinetics.
Studies on penetration or absorption of this medicinal product have not been conducted.
Betamethasone
Under normal conditions, only a portion of topically applied betamethasone is systemically available. The extent of its penetration depends on the site of application, skin condition, pharmaceutical formulation used, patient's age, and method of application.
Gentamicin
Absorption can be considered negligible when gentamicin is applied to intact skin. However, increased transdermal absorption should be considered in cases of keratin layer loss, inflammatory conditions, or when applied under occlusive dressing or over large skin areas.
Clotrimazole
After topical application, systemic absorption is low, with most of the clotrimazole remaining in the stratum corneum. Such concentrations were observed 6 hours after application of 1% radiolabeled clotrimazole to intact skin and to skin with acute inflammation: stratum corneum = 100 mcg/cm³, dermal layer = 0.5–1 mcg/cm³, subcutaneous layer = 0.1 mcg/cm³.
Clinical characteristics.
Indications.
Treatment of dermatoses sensitive to corticosteroids, when there is (or suspected) bacterial and/or fungal infections caused by microorganisms sensitive to the components of the drug.
Contraindications.
The drug is contraindicated in patients with hypersensitivity to the active substances or to any other component of the drug, to other aminoglycoside antibiotics (cross-allergic reactions to gentamicin), or to imidazole derivatives (cross-allergic reactions to clotrimazole). Also contraindicated in cutaneous tuberculosis, cutaneous manifestations of syphilis, skin reactions following vaccination, skin ulcers, acne, widespread plaque psoriasis, viral skin infections (e.g., herpes simplex, herpes zoster), varicose veins, perioral dermatitis, rosacea, chickenpox, and other bacterial and fungal skin infections without appropriate antibacterial and antifungal therapy.
The drug is not indicated for use under occlusive dressings.
The drug should not be applied to mucous membranes, eyes, or the area around the eyes.
Do not use the cream for the treatment of nails or skin infections of the scalp.
Interaction with other medicinal products and other forms of interaction.
When applying the cream to the genital area and the anal opening, the presence of white soft paraffin or mineral oil (excipients in the formulation) may reduce the tensile strength of latex condoms, thereby decreasing their reliability during use.
Topically applied clotrimazole may act as an antagonist to amphotericin and other polyene antibiotics.
Special precautions for use
The cream is particularly suitable for use in the treatment of exudative-stage disorders.
The product is not intended for ophthalmic use.
If skin irritation or hypersensitivity reactions develop during treatment, the product should be discontinued and appropriate therapy initiated.
With topical application, systemic absorption of the active substances may be increased when the product is applied to large skin areas, especially with prolonged use or application to damaged skin. In such cases, adverse effects similar to those observed after systemic administration of the active substances may occur.
When aminoglycoside antibiotics are administered systemically concomitantly, the possibility of cumulative toxicity (ototoxicity/nephrotoxicity) should be considered.
Cross-sensitivity reactions with other aminoglycoside antibiotics should also be taken into account.
Prolonged topical use of antibiotics may occasionally lead to overgrowth of resistant microorganisms. In such cases, as well as in the event of superinfection, treatment with the product should be discontinued and appropriate therapy initiated.
High-potency corticosteroids applied over large skin areas should be used under careful and periodic monitoring, as they may cause suppression of the hypothalamic-pituitary-adrenal (HPA) axis. If HPA axis suppression develops, the drug should be withdrawn, the frequency of application reduced, or the patient switched to a less potent corticosteroid. HPA axis function usually recovers after discontinuation of the drug. In some cases, withdrawal symptoms may develop, requiring the addition of systemic corticosteroid therapy.
Application of the product to open wounds or damaged skin should be avoided.
Continuous treatment for longer than 2–3 weeks is not recommended.
Very potent, potent, and moderately potent corticosteroids should be used with caution when applied to the facial skin or genital areas. In such cases, the treatment course should not exceed 1 week.
Only low-dose corticosteroids should be used in the periorbital area (glaucoma risk).
Corticosteroids may mask symptoms of allergic reactions to one of the components of the product.
Patients should be instructed to use the product only for their own treatment and not to pass it on to others.
Cetyl stearyl alcohol may cause local skin reactions (e.g., contact dermatitis).
Propylene glycol may cause skin irritation.
Use during pregnancy or breastfeeding
Pregnancy
Experimental studies have demonstrated a teratogenic effect of topically applied corticosteroids. There are no data on the use of this product in pregnant women.
Aminoglycosides cross the placental barrier and may harm the fetus when administered to pregnant women. Cases of complete, irreversible, bilateral congenital deafness in children whose mothers received aminoglycosides (including gentamicin) during pregnancy have been reported. Data on the topical use of gentamicin in pregnant women are insufficient. Data on the use of clotrimazole in pregnant women are also insufficient.
Animal studies have not demonstrated any risk of the drug affecting the fetus.
The product should be used only if clearly necessary.
The product should not be used in large doses, over large skin areas, or for prolonged periods.
Breastfeeding
It is unknown whether gentamicin, clotrimazole, and corticosteroids, when applied topically, are excreted in breast milk. However, systemic corticosteroids have been detected in breast milk.
The product should not be applied to the breasts of women who are breastfeeding.
Ability to influence reaction speed when driving or operating machinery
The effect on the ability to drive or operate machinery has not been studied.
Method of Administration and Dosage
The medication should be applied as a thin layer to the entire affected area and adjacent unbroken skin twice daily, in the morning and evening, in adults. The duration of treatment depends on the patient's clinical response as well as clinical and microbiological parameters.
In cases of athlete's foot, a longer treatment course may be required (2–4 weeks).
Children
The use of the medication in children is not recommended due to lack of experience with the drug in this age group.
Overdose
Prolonged or excessive use of topical glucocorticosteroids may lead to suppression of the hypothalamic-pituitary-adrenal system, resulting in secondary adrenal insufficiency and symptoms of hypercorticism, including Cushing's syndrome.
It cannot be excluded that a single overdose of gentamicin may lead to symptoms of overdose.
Excessive and prolonged topical use of gentamicin may result in overgrowth of antibiotic-resistant microorganisms.
Treatment. Appropriate symptomatic therapy should be administered. Symptoms of acute hypercorticism are usually reversible. If necessary, correction of electrolyte imbalance should be performed. In cases of chronic toxic effects, discontinuation of corticosteroids should be gradual.
In case of overgrowth of resistant microorganisms, treatment with the medication should be discontinued and appropriate antifungal or antibacterial therapy should be initiated.
Adverse Reactions
Initial treatment
Skin-related
Rare: skin irritation, burning sensation, pruritus, dry skin, hypersensitivity reactions to one of the components of the medicinal product, and skin discoloration.
With application to large skin areas, under occlusive dressings and/or for prolonged periods, local skin changes may occur. Application to large skin areas may lead to systemic reactions (adrenal suppression, fainting, arterial hypotension, dyspnea, discomfort/pain, malaise).
One should bear in mind the increased risk of secondary infections due to reduced local resistance to infection.
Localized skin changes may occur, for example skin atrophy (particularly on the face), telangiectasia, exudation, blistering, edema, urticaria, maceration, miliaria, pigmentary disturbances (hypopigmentation), hypochromia, striae, focal desquamation, paresthesia, lamellar desquamation, skin induration, skin fissures, sensation of warmth, follicular eruptions, erythema, stretch marks, subcutaneous hemorrhages, purpura, steroid-induced acneiform eruptions, rosacea-like/perioral dermatitis, hypertrichosis, and skin discoloration. It is unknown whether these skin color changes are reversible.
Uncommon: contact sensitization to gentamicin.
In some patients, possible photosensitization has been observed; however, this effect is not reproduced upon repeated application of gentamicin followed by ultraviolet radiation exposure.
Endocrine system: suppression of endogenous corticosteroid synthesis, adrenal hyperactivity with edema.
Metabolism: emergence of latent diabetes mellitus.
Ear, inner ear/kidney-related: with concomitant systemic use of aminoglycoside antibiotics, cumulative ototoxicity/nephrotoxicity may occur when the medicinal product is applied to large skin areas or to damaged skin.
Musculoskeletal system: osteoporosis, growth retardation (in children).
Shelf life. 2 years.
Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.
Packaging. 15 g or 30 g in tubes, in a carton.
Prescription status. Prescription only.
Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".
Manufacturer's address and location of business activity.
Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, building 22.
(all manufacturing stages, quality control, batch release)
Ukraine, 08301, Kyiv region, city of Boryspil, Shevchenka Street, building 100, letter B-II (building 4).
(all manufacturing stages, batch release)