Steroid anti-inflammatory drugs: instructions for the first-generation

The appearance of topical corticosteroids (GCS) in the early 50s of the last century is considered one of the most significant events in dermatology. And today, drugs of this group occupy a leading position among all external dermatological drugs [1]. A wide range of indications, high activity, pleiotropic effects and a convincing evidence base, along with a favorable safety profile, are a solid foundation for the rapid movement towards the heights of popularity of these drugs among doctors and consumers. As a result, first-line physicians need to keep in mind and be able to use knowledge about the drugs of this group in pharmaceutical consulting. Especially considering that some topical drugs containing corticosteroids are available without a prescription. How local glucocorticosteroids work, when they can be recommended, and what to warn clients about is in our new article.

We say pleiotropic, we mean multiple

The mechanism of action of local corticosteroids is based on their ability to interact with corticosteroid-specific receptors, which are located in the epidermis and fibroblasts of human skin. At the same time, they exhibit a complex of different effects, exerting a pleiotropic (multiple - editor's note) effect due to the implementation of a number of mechanisms [2].

Anti-inflammatory effect

Provides the benefits of topical corticosteroids for inflammatory skin lesions.

Mechanisms:

• Inhibition of the release of phospholipase A2, the main enzyme for the formation of inflammatory mediators based on arachidonic acid (prostaglandins and leukotrienes).
• Inhibition of transcription factors that are involved in the activation of proinflammatory genes.
• Inhibition of phagocytosis and stabilization of membranes of phagocytic cells.
• Decreased release of keratinocytes and the pro-inflammatory cytokine interleukin-2 from epidermal principal cells.

Immunosuppressive effect

Provides the anti-inflammatory effect of topical corticosteroids.

Mechanisms:

• Suppression of the production of mediators involved in the inflammatory response (tumor necrosis factor, interleukins and some others).
• Inhibition of leukocyte migration to the site of inflammation.
• Interference with the function of endothelial cells, granulocytes, mast cells and fibroblasts.

Antiproliferative effect aimed at suppressing the excessive proliferation of certain cells.

Provides the effectiveness of topical glucocorticosteroids in conditions accompanied by abnormally high skin proliferation, for example, psoriasis or eczema.

Mechanism:

• Inhibition of DNA synthesis and mitosis.
• Inhibition of fibroblast activity and collagen formation.

Vasoconstrictor effect

Provides high activity of topical corticosteroids for dermatological diseases accompanied by skin redness and swelling.

The mechanism of this effect is still not fully understood. One of its stages is the inhibition of pro-inflammatory mediators that have a vasodilatory effect (histamine, bradykinin, prostaglandin, etc.). Vasoconstrictor activity has become one of the criteria for assessing the power of topical GCS.

Activity of topical corticosteroids

The activity of drugs in this group depends on at least four factors [2, 4].

Release form.

The release form of a local drug is in its own way a “vehicle” that ensures the delivery of active substances deep into the skin. Therefore, the “power” of the topical agent largely depends on its properties.

• Ointments with steroids

  are considered the most effective form of topical corticosteroids. These are water-in-oil emulsions, the high activity of which is due to the ability to form a film on the surface of the skin that is impenetrable to air and moisture and thus provides a “compress effect” - occlusion. As a result, the local concentration and effectiveness of the product increases. But occlusive preparations also have disadvantages: firstly, the skin stops “breathing”, which can contribute to the development of weeping, and secondly, they are inconvenient to apply to the skin of the scalp, chest, etc.

  It is advisable to recommend topical corticosteroids in the form of ointments for the treatment of dry skin diseases.

• Creams

  , unlike ointments, being an “oil in water” emulsion, are not fatty forms. They do not form an occlusive film on the surface of the skin and therefore lack both the disadvantages of ointments and their advantages. GCS creams are less active than steroid ointments.

  Topical corticosteroids in the form of a cream are indicated for acute and subacute inflammation without significant weeping.

• Gels

  - an oil-in-water emulsion with an alcohol base. They liquefy upon contact with skin and have a medium degree of activity.

  It is advisable to recommend gels for the treatment of areas of the body heavily covered with hair.

• Lotions

  , which are aqueous solutions, are considered the least active form of GCS. They evaporate, providing a cooling effect.

  It is advisable to recommend topical GCS in the form of a lotion if it is necessary to treat large areas, as well as areas abundantly supplied with hair follicles.

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The salt to which the steroid is bound.

For example, betamethasone exists as valerate, dipropionate, and benzoate, each of which has different potencies.

Active ingredient concentration

The higher the concentration of the active substance, the higher the activity of the drug.

For example, one of the most powerful topical corticosteroids, clobetasol propionate, in the form of an ointment, is approximately 1000 times “more powerful” than the weakest drug in this group, 1% hydrocortisone.

There are two classifications of topical corticosteroids according to the degree of activity - European, which distinguishes 4 classes, and American, in which drugs are divided into 7 classes of activity. In both the first and second, activity was assessed based on vasoconstrictor tests and according to clinical studies.

European classification of topical glucocorticosteroids [3]

American classification of topical corticosteroids [3]

Indications and contraindications

List of indications

, for which the use of topical steroid drugs (GCS) is advisable, is quite extensive. The most common indications for their use are:

• psoriasis;
• atopic dermatitis;
• eczema;
• seborrheic dermatitis;
• contact dermatitis.

The choice of a specific drug depends, first of all, on the disease and the location of the lesion. Depending on the type of pathology and the area that needs to be treated, the active component, dosage form, and concentration are selected.

For example, high-strength topical corticosteroids are used to treat exacerbations of alopecia areata, resistant atopic dermatitis, hyperkeratotic eczema, lichen planus, severe contact dermatitis and severe hand eczema [5].

Topical corticosteroids of medium strength are used for severe anal inflammation, dry eczema, atopic eczema in children, atopic dermatitis, seborrheic dermatitis and a number of other diseases [5].

Topical corticosteroids classified as “weak” are indicated for diaper dermatitis (severe), as well as eyelid dermatitis and intertrigo (dermatitis in skin folds) [5].

Topical steroids can be prescribed both for exacerbations of dermatological diseases before the onset of a period of remission, and for the treatment of chronic inflammatory process.

Contraindications

for the use of topical corticosteroids are:

• · Acute infectious skin lesions - topical corticosteroids, having immunosuppressive properties, inhibit the healing process [2];
• · Strong and super-strong steroid drugs should not be used on the face, groin and axillary areas. Their use under a bandage is contraindicated to avoid the development of an occlusive effect. As a rule, drugs of these groups are used for a short period [5].

Rebospan / Rebospan

TRADENAME:

Rebospan / Rebospan
INTERNATIONAL NON-PROPENTED NAME:
Betamethasone / Betamethasone

DOSAGE FORM:

suspension for injection
Description:
Slightly viscous liquid containing white particles, free from foreign impurities.

COMPOUND:

1 ml of suspension contains:
Active substances:
betamethasone dipropionate 6.43 mg (equivalent to 5 mg betamethasone), betamethasone sodium phosphate 2.63 mg (equivalent to 2 mg betamethasone).

PHARMACOTHERAPEUTIC GROUP:

Corticosteroids for systemic use.

ATC CODE OF THE DRUG:

H02AB01.

PHARMACOLOGICAL PROPERTIES.

PHARMACODYNAMICS: Rebospan is a synthetic glucocorticosteroid (GCS) drug with high glucocorticoid and low mineralocorticoid activity. The drug has anti-inflammatory, antiallergic and immunosuppressive effects, and also regulates carbohydrate homeostasis and water-electrolyte balance. Betamethasone does not have a clinically significant mineralocorticoid effect. In addition to influencing the inflammatory and immune processes, glucocorticoids also affect the metabolism of carbohydrates, proteins and lipids. In addition, glucocorticoids affect the cardiovascular system, skeletal muscles and the central nervous system. Influence on inflammatory and immune processes. The anti-inflammatory, immunosuppressive and antiallergic properties of glucocorticoids are important when used in therapeutic practice. The main results of these properties are: a decrease in the number of immunoactive cells at the site of the inflammatory process, a decrease in vasodilation, stabilization of lysosomal membranes, suppression of phagocytosis, and a decrease in the production of prostaglandins and related substances. The anti-inflammatory activity of the drug is approximately 25 times higher than that of hydrocortisone and 8-10 times higher than that of prednisolone (in weight ratio). Effect on the metabolism of carbohydrates and proteins. Glucocorticoids stimulate protein catabolism. In the liver, through the process of gluconeogenesis, the released amino acids are converted into glucose and glycogen. Glucose absorption in peripheral tissues is reduced, leading to hyperglycemia and glycosuria, especially in patients predisposed to diabetes. Effect on lipid metabolism. Glucocorticoids have a lipolytic effect. Lipolysis is most pronounced at the level of the extremities. In addition, glucocorticoids affect lipogenesis, which is most pronounced in the torso, neck and head. Together, these effects lead to a redistribution of lipid deposits.

PHARMACOKINETICS:

Betamethasone sodium phosphate and betamethasone dipropionate are absorbed at the injection site, providing a rapid onset of therapeutic action, as well as other local and general pharmacological effects. Betamethasone sodium phosphate quickly dissolves in water and is metabolized in the body to betamethasone (a biologically active glucocorticoid). 2.63 mg of betamethasone sodium phosphate is equivalent to 2 mg of betamethasone. The use of betamethasone dipropionate allows you to achieve a long-lasting effect of the drug. This substance practically does not dissolve, representing a depot, so absorption is slower, and symptom relief lasts longer. Betamethasone is metabolized in the liver. Binding occurs mainly with albumin. In patients with liver disease, the metabolism of betamethasone is longer or slower.

INDICATIONS FOR USE:

Corticosteroid therapy is auxiliary and does not replace conventional treatment. Intramuscular administration: Rebospan is indicated for the treatment of various rheumatological, dermatological, allergic, systemic connective tissue diseases and other diseases that usually respond to treatment with corticosteroids. Intra-articular and periarticular administration, as well as administration directly into soft tissues: as an auxiliary short-term therapy (in acute form or exacerbation of the disease) for osteoarthritis, rheumatoid arthritis. Intradermal administration: for dermatological diseases. Local injection into the tissues of the foot: as an auxiliary short-term therapy (in the acute form or exacerbation of an existing disease) for bursitis against the background of a hard callus, spur, stiffness of the big toe or deformation of the big toe, with a synovial cyst, Morton's metatarsal neuralgia, ten - dosynovitis, periostitis of the cuboid bone. Allergic conditions: bronchial asthma, status asthmaticus, seasonal or perennial allergic rhinitis, severe allergic bronchitis, contact dermatitis, atopic dermatitis, hay fever, angioedema, serum sickness, hypersensitivity reactions to drugs or insect bites. Rheumatic diseases: osteoarthritis, rheumatoid arthritis, bursitis, lumbago, sciatica, coccydynia, acute gouty arthritis, torticollis, ganglion cyst, ankylosing spondylitis, radiculitis, exostosis, fasciitis. Dermatological diseases: atopic dermatitis (coin-shaped eczema), neurodermatitis (limited neurodermatitis), contact dermatitis, severe solar dermatitis, urticaria, hypertrophic lichen planus, lipoid diabetic necrobiosis, alopecia areata, discoid lupus erythematosus, psoriasis, keloid scars, pemphigus vera, herpetiformis dermatitis, cystic acne. Systemic connective tissue diseases: during exacerbation or as maintenance treatment of certain types of disseminated systemic lupus erythematosus, polyarteritis nodosa, systemic sclerosis and dermatomyositis. Oncological diseases: as palliative therapy for leukemia and lymphoma in adults, as well as acute leukemia in children. Other conditions: adrenogenital syndrome, hemorrhagic rectocolitis, Crohn's disease, sprue, pathological changes in the blood that require glucocorticoid therapy, nephritis, nephrotic syndrome. In the presence of primary or secondary adrenal insufficiency, treatment with the drug Rebospan can be carried out, however, if necessary, mineralocorticoids must be used simultaneously.

CONTRAINDICATIONS:

- hypersensitivity to the components of the drug or to other corticosteroids; - systemic mycoses; - with intra-articular injection: unstable joint, infectious arthritis; - intramuscular administration in patients with idiopathic thrombocytopenic purpura.

SIDE EFFECT:

From the cardiovascular system: chronic heart failure (in predisposed patients), increased blood pressure. From the musculoskeletal system: muscle weakness, steroid myopathy, loss of muscle mass. From the digestive system: erosive and ulcerative lesions of the gastrointestinal tract with possible subsequent perforation and bleeding, pancreatitis, flatulence, nausea, vomiting. From the central nervous system: convulsions, increased intracranial pressure with papilledema (usually after completion of therapy), dizziness, headache, euphoria, mood changes, depression (with severe psychotic reactions), increased irritability, insomnia. From the endocrine system: menstrual irregularities, Itsenko-Cushing syndrome, decreased carbohydrate tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, increased need for insulin or oral hypoglycemic drugs. From the skin: impaired wound healing, atrophy and thinning of the skin, petechiae, ecchymosis, increased sweating, dermatitis, rash, urticaria. From the immune system: corticosteroids can help suppress skin tests, mask the symptoms of infection and activate latent infection, as well as reduce resistance to infectious pathogens, in particular mycobacteria (for tuberculosis), Candida albicans and viruses. Allergic reactions: anaphylactic reactions, shock, angioedema, decreased blood pressure.

METHOD OF APPLICATION AND DOSAGE:

Rebospan cannot be administered intravenously or subcutaneously! The ampoule must be shaken before use. THE DOSE IS SELECTED INDIVIDUALLY DEPENDING ON THE PATIENT'S NEEDS, TYPE OF DISEASE, ITS SEVERITY AND REACTION OF THE PATIENT'S BODY. Systemic use For systemic therapy, the initial dose of the drug in most cases is 1-2 ml. The administration is repeated if necessary. The drug is injected deep intramuscularly into the buttock. For serious diseases when urgent treatment is necessary, for example, with systemic lupus erythematosus or status asthmaticus, the initial dose of the drug may be 2 ml. For various dermatological diseases, a good response is usually achieved after intramuscular injection of 1 ml of the drug Rebospan; administration of the drug can be repeated depending on the therapeutic effect. For diseases of the respiratory system, symptom relief is achieved a few hours after an intramuscular injection of the drug Rebospan. For bronchial asthma, hay fever, allergic bronchitis and allergic rhinitis, effective control of symptoms is achieved after administration of 1-2 ml of the drug. In acute or chronic bursitis, effective results are achieved after one intramuscular injection of 1-2 ml of the drug Rebospan. If necessary, you can repeat the administration of the drug. Local application Simultaneous use of a local anesthetic drug is necessary only in isolated cases (the injection is practically painless). If simultaneous administration of an anesthetic drug is desired, then Rebospan can be mixed (in a syringe, not in a vial) with 1% or 2% solution of lidocaine hydrochloride, procaine hydrochloride or similar local anesthetics using paraben-free dosage forms. The use of anesthetics containing methylparaben, propylparaben, phenol and other similar substances is not permitted. First, the required dose of the drug Rebospan should be drawn into a syringe from the bottle; then the required amount of local anesthetic is drawn into the same syringe and shaken for a short period of time. For acute bursitis (subdeltoid, subacromial and prepatellar): injection of 1-2 ml of the drug Rebospan directly into the synovial bursa can relieve pain and completely restore mobility within several hours. For chronic bursitis: if a good effect is obtained after emergency treatment, the dose of the drug can be reduced. For tendinitis, tenosynovitis and peritendinitis: in the acute stage of the disease, one injection of the drug may be enough to improve the patient’s condition; in the chronic stage, repeated administration of the drug may be required, depending on the patient’s condition. For rheumatoid arthritis and osteoarthritis: intra-articular administration of the drug in a dose of 0.5-2 ml, as a rule, reduces pain, tenderness and stiffness of the joints within 2-4 hours after administration. The duration of the therapeutic effect of the drug varies significantly in these two diseases and can be 4 or more weeks. Intra-articular administration of the drug Rebospan is well tolerated both in the joints and periarticular tissues. Recommended doses of the drug: - When administered into large joints (for example, knee, hip): 1-2 ml; — When administered into the middle joints (for example, elbow): 0.5-1 ml; — When administered into small joints (for example, joints of the hand): 0.25-0.5 ml. For skin diseases: for dermatological diseases, administering the drug Rebospan directly to the lesion is effective. The beneficial effect on some lesion sites where the drug is not directly applied may be due to a small systemic effect of the drug. The dose is 0.2 ml/cm2. The drug is administered intradermally (not subcutaneously) using a tuberculin syringe with a 26C needle. The total amount of the drug administered to all affected areas should not exceed 1 ml. For foot diseases sensitive to glucocorticoid therapy: for bursitis against the background of a callus, the use of two consecutive injections of the drug, 0.25 ml each, can be effective. Other conditions, such as hallux rigidus, fifth toe varus, and acute gouty arthritis, may improve very quickly. A tuberculin syringe with a 25C needle 1.9 cm long is suitable for most injections into the foot. Recommended doses (with intervals between administrations of about 1 week) are: For bursitis: - against the background of hard callus 0.25-0.5 ml; - with a spur 0.5 ml; - for stiffness of the big toe 0.5 ml; — for varus deformity of the fifth toe 0.5 ml; For synovial cyst 0.25-0.5 ml; For Morton's metatarsal neuralgia 0.25-0.5 ml; For tenosynovitis 0.5 ml; For periostitis of the cuboid bone 0.5 ml; For acute gouty arthritis 0.5-1 ml.

PRECAUTIONARY MEASURES:

The drug Rebospan cannot be administered intravenously or subcutaneously! Serious neurological reactions (sometimes fatal) have been reported with epidural corticosteroid injections. The safety and effectiveness of epidural corticosteroids have not been established and such use of corticosteroids is prohibited. Administration of the drug must take place under aseptic conditions. Rebospan contains two betamethasone esters, one of which (betamethasone sodium phosphate) is rapidly absorbed at the site of drug administration. Dose reduction should take place under the close supervision of a physician. In addition, it is sometimes necessary to monitor the patient's condition for a period of up to 1 year after the end of long-term treatment or after using high doses of the drug. During long-term therapy with corticosteroids, it is necessary to consider switching from parenteral to oral use of the drug, weighing all the benefits and possible risks. Corticosteroids must be administered deeply intramuscularly to avoid local tissue atrophy. The introduction of corticosteroids into soft tissues or directly into the lesion, as well as intra-articular administration, can have a general and local effect. Excipients

Rebospan contains benzyl alcohol, which can cause toxic and anaphylactoid reactions in newborns and children under 3 years of age. The drug should not be used in premature or full-term newborns. The composition of the drug Rebospan includes methyl parahydroxybenzoate (E218) and propyl parahydroxybenzoate (E216), which can cause allergic reactions (sometimes of a delayed type), and in exceptional cases, difficulty breathing.

INFLUENCE ON THE ABILITY TO DRIVE A VEHICLE AND OPERATE MACHINERY:

Particular caution should be exercised when taking large doses of the drug, which may contribute to the development of central nervous system effects (euphoria, insomnia). Visual impairment is also possible with long-term use of the drug.

USE IN PREGNANCY AND LACTATION:

Due to the lack of studies on the safety of the use of glucocorticoids in pregnant and breastfeeding women, glucocorticosteroids should not be prescribed to women during pregnancy, lactation, or women of childbearing age, unless necessary and only after a careful assessment of the ratio of the expected positive effect and possible risks for the mother , fetus or child. If corticosteroid therapy is indicated in the antenatal period, the expected clinical effect should be compared with possible side effects (in particular growth retardation and increased risk of infection). In some cases, it is necessary to continue corticosteroid therapy during pregnancy or even increase the dose (for example, in the case of corticosteroid replacement therapy). Corticosteroids penetrate well through the placental barrier and into mother's milk. Because corticosteroids cross the placenta, neonates and infants born to mothers treated with corticosteroids during most or part of pregnancy should be monitored particularly closely for the possibility of congenital cataracts, although such cases are very rare. Since Rebospan may cause side effects in breastfed infants, consideration should be given to stopping breastfeeding or the appropriate use of the drug, depending on the importance of this therapy for the mother. Women treated with corticosteroids during pregnancy should be monitored during and after labor and delivery for adrenal insufficiency caused by the stress of labor.

APPLICATION IN PEDIATRICS:

Children undergoing drug therapy (especially long-term therapy) should be under close medical supervision for possible growth retardation and the development of secondary adrenal insufficiency.

Rebospan contains benzyl alcohol, which can cause toxic and anaphylactoid reactions in newborns and children under 3 years of age. The drug should not be used in premature or full-term newborns.

INTERACTIONS WITH OTHER MEDICINES:

Concomitant use with phenobarbital, rifampicin, phenytoin or ephedrine may increase the metabolism of corticosteroids and, as a result, reduce the therapeutic effect. The following treatments are contraindicated in patients receiving corticosteroid therapy: • smallpox vaccination, • other immunization methods (especially in high doses) due to the risk of neurological complications and a weak immune response (insufficient antibody response). However, patients using corticosteroids as replacement therapy may be given immunization (eg, Addison's disease). The condition of patients receiving concomitant treatment with corticosteroids and estrogens should be monitored, as the effects of corticosteroids may be enhanced. Concomitant use of corticosteroids and cardiac glycosides may increase the risk of arrhythmia or digitalis toxicity due to hypokalemia. When used simultaneously with non-steroidal anti-inflammatory drugs or ethanol, the risk of developing gastrointestinal ulcers or exacerbation of an existing ulcer may increase. In patients with diabetes mellitus, in some cases it may be necessary to adapt the dose of oral antidiabetic drugs or insulin, taking into account the hyperglycemic effect of glucocorticosteroids. Rarely, concomitant use of local anesthetics may be necessary. If simultaneous administration of an anesthetic is desired, Rebospan can be mixed (in a syringe, not in a vial) with 1% or 2% solutions of lidocaine or procaine hydrochloride, or other anesthetics that do not contain parabens. The use of anesthetics containing methylparaben, propylparaben, phenol and other similar substances is not permitted.

STORAGE CONDITIONS:

Store in a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children! Do not freeze. Shake before use.

BEST BEFORE DATE:

Shelf life 3 years from the date of production. Do not use after the expiration date.

CONDITIONS FOR DISCHARGE FROM PHARMACIES:

Dispensed by prescription.

*More detailed information is contained in the instructions for use of the drug.

Side effects of topical glucocorticosteroids

This question often worries consumers. So that first-principals can quickly and easily dispel customer doubts, we have created several convincing arguments in the format of dialogues with customers.

• It is better not to use hormones, even externally, as they have many side effects.

  Answer:

  Most drugs in this group are well tolerated. Side effects, as a rule, develop when using high-strength topical corticosteroids when treating large areas over a long period of time [2].

• Hormonal ointments are also absorbed into the blood, so it is better to do without them.

  Answer:

  Modern topical corticosteroids have extremely low absorption and are practically not absorbed into the blood, acting locally at the site of inflammation.

• It is better not to use hormonal ointments to treat children - they can become addictive.

  Answer:

  Topical corticosteroids, which are approved for use in pediatric practice, for example, methylprednisolone aceponate, are practically not absorbed into the blood, acting locally at the site of inflammation. When used, as a rule, the condition is very quickly alleviated and the likelihood of relapse of the disease is reduced. The main thing is to observe the frequency of application and course of treatment.

Returning to the question of side effects of topical corticosteroids, it should be noted that the most common adverse reaction is skin atrophy. It manifests itself in the form of thinning of the skin, shine, telangiectasia, bruising, stretch marks, redness and changes in pigmentation. Hydrocortisone aceponate, fluticasone propionate and methylprednisolone aceponate have the lowest ability to cause skin atrophy. Therefore, they can be used to treat lesions on the face, scrotum, and large areas of the body, including in children [2].

To minimize the likelihood of side effects, topical corticosteroids are recommended to be used in short courses (no more than 3–4 weeks). As the duration of treatment increases, the likelihood of adverse reactions increases.

When using topical glucocorticosteroids in infants, it should be remembered that application of drugs into the folds of the skin and under the diaper may be accompanied by the development of an occlusive effect and a local increase in the concentration of the active component. In this regard, it is not recommended to apply drugs in places where diapers and diapers come into contact with the skin [6].

What should I warn the client about?

When dispensing the drug, it is appropriate to note:

• To reduce the risk of side effects, it is very important to strictly follow the doctor’s recommendations: observing the frequency of use, dosage and course of treatment. It is strictly prohibited to arbitrarily change the duration of treatment and increase the dose.
• Replacing one steroid drug with another without the knowledge of the doctor can lead not only to a decrease in the effectiveness of treatment, but also to the development of side effects of GCS, since only a specialist who takes into account several factors can select them correctly.

How to take Betamethasone

Betamethasone should be taken exactly as prescribed by your doctor.

If you have any doubts about taking the drug, you should consult your doctor or pharmacist before use.

How to use Betamethasone

• Typically, Betamethasone should be used 1-2 times a day. Frequency of use may be reduced as skin condition improves
• Betamethasone is for use on the skin only.
• Do not exceed the prescribed dose of the drug
• Do not use Betamethasone on a large surface of the skin for a long time (every day for weeks or months) - unless, of course, your doctor has prescribed it for you
• Microorganisms can promote the development of infections in warm, moist conditions under dressings and bandages, so the skin should be cleaned before applying a new dressing.
• If you apply the ointment to someone else, wash your hands thoroughly before applying or wear disposable gloves.
• If your skin condition does not improve within 2-4 weeks, contact your doctor

How to use Betamethasone ointment

1. Wash your hands.
2. Apply a thin layer of ointment to the affected areas of the skin and lightly rub it into the skin until completely absorbed. You can dose Betamethasone by applying it to your fingertip. When dosing children, use less ointment, but still use an adult's finger as a dosing unit.

This picture shows the dosage unit - 1 Fingertip Unit (FTU).

FingerTip Unit - the amount of ointment from a tube with a hole diameter of 5 mm, covering the distal phalanx of the index finger of an adult.

1. After applying the ointment, rinse your hands thoroughly, except in cases where the skin of the hands is affected and is the area for applying the ointment.

Dosage for adults

Don't worry if you use a little more or less ointment than you should, it will only be unevenly distributed.

Dosage for children from 1 to 10 years

• Cannot be used by children under 1 year of age
• For children it is especially important not to exceed the prescribed dose
• The course of treatment for children should not exceed 5 days - unless your doctor has prescribed a longer course of treatment

If you have psoriasis

If you have severe psoriatic plaques on your elbows or knees, your doctor may recommend applying ointment under sealed occlusive dressings. However, this is recommended when using the ointment at night to enhance its effect. After a short period of time, you need to return to your normal regimen of taking the ointment.

If you use Betamethasone on the facial skin

You can apply Betamethasone ointment on your face if your doctor has prescribed it for you. It is not recommended to use Betamethasone for more than 5 days, as longer use leads to thinning of the skin. Avoid getting Betamethasone in the eye.

If you use more Betamethasone than recommended

If you have used too much ointment or accidentally swallowed it, contact your doctor or the nearest hospital emergency room immediately.

If you forget to take Betamethasone

If you forget to take the next dose of the drug, take it as soon as you remember. Then continue using as usual.

If you stop taking Betamethasone

If you are using Betamethasone regularly and want to stop taking it, you should talk to your doctor before you stop using this drug as your condition may get worse if you suddenly stop taking the drug.

If you have any additional questions, you should immediately contact your doctor or pharmacist.

Possible side effects

Like other medicines, Betamethasone can cause side effects, although not everyone gets them.

Stop using Betamethasone and tell your doctor immediately if:

• You will find that your skin gets worse, you develop a generalized rash, or your skin swells during treatment. You may be allergic to Betamethasone, have an infection, or need other treatment
• You have psoriasis and there are raised bumps of pus under the skin. This may occur very rarely during or after treatment and is known as pustular psoriasis.

Other side effects

Common ( may affect 1 in 10 )

• burning sensations, pain, irritation or itching at the sites where the ointment is applied.

Very rare (may affect up to 1 in 10,000)

• increased risk of developing infection
• allergic skin reaction where the ointment is applied
• rash, itching, bumpiness, or redness of the skin
• thinning and dryness of the skin, as well as increased susceptibility to damage and wrinkling
• development of stretch marks
• veins beneath the surface of your skin may become more visible
• increase or decrease in hair growth or hair loss and changes in skin color
• weight gain, rounding of the face
• delayed weight gain or slowed growth in children
• thinning, weakening and increased susceptibility to bone fractures
• development of cataracts or glaucoma
• elevated levels of sugar in the blood or urine
• increased blood pressure

Reporting Adverse Events:

If you notice any side effects, tell your doctor, pharmacist or nurse. This includes any side effects not listed in this leaflet. You can also report side effects directly to the Scientific Center for Expertise of Medicines and Medical Technologies. Academician E. Gabrielyan, go to the website www.pharm.am to the section “Report a side effect of a drug” and fill out the form “Card for reporting a side effect of a drug.” Hotline phone: +37410237665; +37498773368. By reporting side effects, you can help provide more information about the safety of this drug.

How to store Betamethasone

• Store out of reach of children, in a dry place, protected from light at a temperature not exceeding 15º C
• Shelf life – 3 years. Shelf life after first opening the tube – 6 months

Do not take Betamethasone after the expiration date indicated on the drug package. When indicating the expiration date, we mean the last day of the specified month.

Medicines should not be disposed of in wastewater or sewer systems. Ask your pharmacist how to dispose of any medicine you no longer need. These measures are aimed at protecting the environment.

Package contents and additional information

What Betamethasone contains

Active substance: betamethasone (in the form of valerate) – 1 mg;

Other components: liquid paraffin, propylparaben (E216), white petrolatum, ethyl alcohol

What Betamethasone looks like and contents of the pack:

Ointment is white to yellowish-white, odorless

Description of packaging

0.1% ointment for external use in an aluminum tube of 15g along with a leaflet in a cardboard pack.

Vacation conditions

Available with prescription

Selected representatives of topical GCS

The list of drugs used in this group is quite large, so we will note the features of only those drugs that have over-the-counter forms.

Hydrocortisone

- a weak synthetic GCS, appropriate for use in acute and subacute skin processes without weeping. To improve penetration, it is recommended to apply with light massaging movements. When positive dynamics appear, the frequency of use is reduced from 1–3 times a day to 2–3 times a week. Approved for use in children over 2 years of age in courses of no longer than 7 days in minimally effective doses [6].

Alclomethasone

- GCS from weak to moderate degree of activity. Absorption through the skin depends on the integrity of the skin and the type of dosage form. In healthy people, 3% alklometasone is absorbed within 8 hours. Can be used on delicate and sensitive areas of the body - face, neck, chest, genital area. Recommended for acute and subacute inflammatory diseases, including those accompanied by weeping. Can be used during pregnancy (under medical supervision), breastfeeding, and in children over 6 months. The maximum duration of treatment in children is 3 weeks.

Betamethasone dipropionate

- strong corticosteroids, when used on the face, the course of treatment should not exceed 5 days to avoid the development of rosacea, perioral dermatitis or acne. Can be used in children from 1 year of age according to strict indications and under medical supervision.

Methylprednisolone aceponate

— GCS of medium strength, can be used in children from 4 months of age in courses of up to 4 weeks. It is available in the form of an emulsion, cream, ointment and fatty ointment, which allows you to select the drug individually, depending on the lesion.

Sources

1. Adaskevich V. P. Local corticosteroids in the treatment of skin diseases // Bulletin of Pharmacy, 2006. No. 3. P. 33.
2. Bardal, Stan K. Applied pharmacology / Elsevier Saunders, 2011.
3. Clinical guidelines “Atopic dermatitis in children.” Union of Pediatricians of Russia. 2021. 60 p.
4. Kondratieva T.S., Ivanova L.A., Zelikson Yu.I. Technology of dosage forms: Textbook in 2 volumes. Volume 1. Medicine. Moscow, 1991. 496 p.
5. Kalyuzhnaya L. D. Should systemic side effects of topical corticosteroids be taken into account? //Ukrainian Journal of Dermatology, Venereology, Cosmetology, 2010. Vol. 1. No. 36. P. 28-31.
6. According to GRLS data as of September 25, 2019.

Betamethasone 0.05% cream for external use, 30g

Registration Certificate Holder

VERTEX (Russia)

Dosage form

Medicine - Betamethasone (Betamethasone-Vertex)

Description

Cream for external use

white or almost white, uniform.

1 g

betamethasone dipropionate 0.643 mg, which corresponds to the content of betamethasone 0.5 mg

Excipients

: white soft paraffin - 150 mg, cetostearyl alcohol - 72 mg, liquid paraffin - 60 mg, macrogol 20 cetostearyl ether - 22.5 mg, sodium dihydrogen phosphate dihydrate - 3.39 mg, methyl parahydroxybenzoate (methylparaben) - 1 mg, propyl parahydroxybenzoate (propylparaben) - 0.5 mg , sodium hydroxide - in the amount necessary to establish the pH, concentrated phosphoric acid - in the amount necessary to establish the pH, purified water - up to 1 g.

15 g - aluminum tubes (1) - cardboard packs. 30 g - aluminum tubes (1) - cardboard packs. 50 g - aluminum tubes (1) - cardboard packs.

Indications

Skin diseases amenable to GCS therapy: atopic dermatitis/neurodermatitis, allergic contact dermatitis, eczema (various forms), contact dermatitis (including occupational) and other non-allergic dermatitis (including sun and radiation dermatitis), reactions to insect bites, psoriasis , bullous dermatoses, discoid lupus erythematosus, lichen planus, exudative erythema multiforme, skin itching of various etiologies, erythroderma.

Contraindications for use

Hypersensitivity, bacterial (skin tuberculosis, skin manifestations of syphilis), fungal, viral (varicella, herpes simplex) skin diseases, skin post-vaccination reactions, open wounds, trophic leg ulcers, rosacea, acne vulgaris, skin cancer, nevus, atheroma, melanoma , hemangioma, xanthoma, sarcoma, children up to 1 year (cream and ointment) and up to 2 years (spray), breastfeeding period.
With caution
Cataracts, diabetes mellitus, glaucoma, tuberculosis (with long-term use or application to large areas of the body), children aged 2 to 12 years (spray).

pharmachologic effect

Betamethasone dipropionate is a synthetic corticosteroid. It has anti-inflammatory, antipruritic, antiallergic, vasoconstrictive, antiexudative and antiproliferative effects. When applied to the surface of the skin, it constricts blood vessels, relieves itching, reduces the release of inflammatory mediators (from eosinophils and mast cells), interleukins 1 and 2, interferon gamma (from lymphocytes and macrophages), inhibits activity and reduces the permeability of the vascular wall. Interacts with specific receptors in the cytoplasm of the cell, stimulates the synthesis of matrix ribonucleic acid, inducing the formation of proteins, including lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, blocks the release of arachidonic acid and the biosynthesis of endoperoxides, prostaglandins, leukoproteins (contributing to the development of inflammation, allergies and other pathological processes).

Dosage regimen

External use. The dosage regimen is individual, depending on the indications, the patient’s age and the clinical situation.

Side effect

For the skin and subcutaneous tissues:

skin itching, burning, irritation, dry skin, folliculitis, hypertrichosis, striae, acne-like rashes (“steroid” acne), hypopigmentation, perioral dermatitis, allergic contact dermatitis, skin maceration, secondary infection, skin atrophy, local hirsutism, telangiectasia, miliaria, purpura.

From the laboratory parameters:

hyperglycemia, glucosuria.
On the part of the organ of vision:
blurred vision.

Other:

reversible inhibition of adrenal cortex function, manifestation of Itsenko-Cushing syndrome.

special instructions

Long-term use of the drug on the skin of the face is not recommended, as the development of rosacea, perioral dermatitis and acne is possible. The course of treatment should not exceed 5 days.

The drug is not intended for use in ophthalmology. Avoid getting the drug into your eyes. If the drug gets on the mucous membranes of the eye, it is possible to develop cataracts, glaucoma, fungal infections of the eye and exacerbation of herpes infection.

With prolonged treatment, when applied to large surfaces of the skin, as well as in the armpits and inguinal folds, when using occlusive dressings, diapers, systemic absorption of GCS is possible.

When used on large surfaces and/or under an occlusive dressing, suppression of the function of the hypothalamic-pituitary-adrenal system and the development of symptoms of hypercortisolism may occur; a decrease in the excretion of growth hormone and an increase in intracranial pressure may be observed.

The spray form is preferable for use in acute forms of dermatosis, including those accompanied by exudation (formation of weeping surfaces).
Use in pediatrics
Use in children aged 1-2 years is possible only under medical supervision. Children are more at risk of suppressing the function of the hypothalamic-pituitary-adrenal system due to the use of corticosteroids for external use than adults, due to their greater ratio of body surface area to body weight and, accordingly, increased absorption of this drug. In children, this is accompanied by low plasma cortisol levels and lack of response to ACTH stimulation. Itsenko-Cushing syndrome may occur, impaired growth and development, slower weight gain, increased intracranial pressure, manifested by protrusion of the fontanelle, headaches, and bilateral papilledema.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated. Contraindicated during pregnancy and lactation (breastfeeding).

Use in children

Restrictions for children - Contraindicated.

The drug is contraindicated for use in children under 1 year (ointment and cream) and under 2 years (spray).
Use caution when using the spray form in children aged 2 to 12 years.