DEKSALIV [Dexamethasone] 0.5 mg Tablets

instructions for the medical use of the medicinal product

DEKSALIV

Tradename: Deksaliv, Дексалив

International non-proprietary name or generic name: Dexamethasone, Дексаметазон

Состав на 1 таблетку:

active substance: dexamethasone 0,5 mg.

excipients: lactose monohydrate, povidone (PVP K30), purified talc, magnesium stearate, tapioca starch, purified water.

Dosage form: tablet, whitish in color, round with a triangle and logo on one side and a line on the other side, with a solid edge.

Pharmacotherapeutic group: Corticosteroids for systemic use, glucocorticoids.

ATX code: H02AB02

Pharmacological properties

Pharmacodynamics

Dexamethasone is a monofluorinated glucocorticoid with pronounced antiallergic, anti-inflammatory and membrane-stabilizing properties and an effect on carbohydrate, protein and fat metabolism.

Dexamethasone has approximately 7.5 times the glucocorticoid effect of prednisolone and is 30 times more effective than hydrocortisone, with no mineralocorticoid effects.

Glucocorticoids such as dexamethasone exert their biological effects by activating the transcription of corticosteroid-responsive genes. Anti-inflammatory, immunosuppressive and antiproliferative effects are due to a decrease in the formation, release and activity of inflammatory mediators, inhibition of specific functions and migration of inflammatory cells. In addition, corticosteroids may prevent sensitized T lymphocytes and macrophages from affecting target cells.

When long-term treatment with corticosteroids is required, the possibility of inducing transient adrenal insufficiency must be considered. Suppression of the hypothalamic-pituitary-adrenal axis also depends on individual factors.

Pharmacokinetics

After oral administration, dexamethasone is quickly and almost completely absorbed from the stomach and small intestine. Its bioavailability is 80–90%. Peak blood levels are reached between 60 and 120 minutes. The binding of dexamethasone to plasma albumin is dose dependent. At very high doses, most of it circulates freely in the blood. With hypoalbuminemia, the proportion of unbound (active) corticoid increases.

The average half-life of dexamethasone (from serum) in adults is 250 minutes (+80 minutes). Due to its long biological half-life of more than 36 hours, daily continuous administration of dexamethasone may lead to accumulation and overdose.

Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. Excreted by the kidneys (a small part by the lactating glands). T1/2 of dexamethasone from plasma - 3-5 hours.

Impaired renal function does not significantly affect the clearance of dexamethasone. However, the half-life is prolonged in severe liver disease.

Indications for use

Neurology

Brain swelling caused by brain tumors, neurosurgery, bacterial meningitis, brain abscess.

Pulmonary and respiratory diseases

Severe acute asthma attack.

Dermatology

Oral initial treatment of extensive, severe, acute skin diseases that respond to glucocorticoids, such as erythroderma, pemphigus vulgaris, acute eczema.

Autoimmune diseases/rheumatology

Oral initial treatment of autoimmune diseases such as systemic lupus erythematosus (especially visceral forms). A severely progressive form of active rheumatoid arthritis, for example, rapidly destructive forms and/or with extra-articular manifestations.

Infectology

Severe infections with toxic conditions (for example, tuberculosis, typhoid fever) only with concomitant anti-infective therapy.

Oncology

Palliative treatment of malignant tumors.

Endocrinology

Congenital adrenogenital syndrome in adulthood.

Contraindications

Hypersensitivity to the active substance or to any of the excipients.

In children during the growth period, glucocorticoids should be used only for absolute indications and under the careful supervision of the attending physician.

Method of administration and dosage

The tablets are taken orally during or after meals with plenty of water.

The dose is set individually depending on the disease, the expected duration of treatment, corticoid tolerance and the body's response.
Adults

The recommended starting dose for adults is 0.5 mg - 9 mg per day. The usual maintenance dose is 0.5 mg - 3 mg per day. The daily dose can be divided into 2-4 doses. The dexamethasone dosage is initially administered until clinical response is achieved, then the dosage is gradually reduced to the lowest level at which the dose remains clinically effective. If treatment with high doses continues for more than a few days, the dose should be reduced over several consecutive days or even over a longer period of time. During long-term oral administration of high doses, it is recommended to take dexamethasone with food and take antacids between meals.

Children

The recommended oral dose for replacement therapy is 0.02 mg/kg body weight or 0.67 mg/m2 body surface, divided into three doses; for other indications the recommended dose is 0.08 mg - 0.3 mg/kg body weight body or 2.5 mg - 10 mg/m2 body surface, divided into three or four doses.

Patients over 65 years of age, patients with kidney and liver diseases

For patients over 65 years of age and patients with kidney and liver diseases, the drug is recommended to be prescribed with extreme caution and subsequent careful medical supervision.

Tablets should not be divided to adjust the dose. If patients require a dose that cannot be provided by one or more 0.5 mg tablets, other suitable forms should be used.

Use during pregnancy and breastfeeding

During pregnancy (especially in the first trimester), the drug can be used only when the expected therapeutic effect exceeds the potential risk to the fetus. With long-term therapy during pregnancy, the possibility of impaired fetal growth cannot be ruled out. If used at the end of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

If it is necessary to carry out treatment with the drug during breastfeeding, breastfeeding should be stopped.

Side effect

The following undesirable effects may occur:

Infections and infestations	Masking of infections, manifestation and exacerbation of viral infections, fungal infections, bacterial, parasitic and opportunistic infections, activation of strongyloidiasis.
Diseases of the blood and lymphatic system	Moderate leukocytosis, lymphocytopenia, eosinopenia, polycythemia.
Immune system disorders	Hypersensitivity reactions (eg, drug rash), severe anaphylactic reactions such as arrhythmias, bronchospasm, hypo- or hypertension, vascular collapse, cardiac arrest, weakened immune system.
Endocrine disorders	Adrenal suppression and induction of Cushing's syndrome (typical symptoms: moon face, central obesity and plethora).
Metabolic and nutritional disorders	Sodium retention with edema, increased potassium excretion (risk of arrhythmias), weight gain, decreased glucose tolerance, diabetes mellitus, hypercholesterolemia and hypertriglyceridemia, increased appetite.
Mental disorders	Depression, irritability, euphoria, increased excitability, psychosis, mania, hallucinations, emotional lability, anxiety, sleep disorders, suicidality.
Nervous system disorders	Pseudotumor cerebri, manifestation of latent epilepsy, increased susceptibility to seizures in manifest epilepsy.
Eye diseases	Cataract, especially with posterior subcapsular opacification, glaucoma, worsening symptoms associated with corneal ulcers, increased incidence of viral, fungal and bacterial ocular inflammation, worsening bacterial corneal inflammation, ptosis, mydriasis, chemosis, iatrogenic scleral perforation, chorioretinopathy, vision, opacities.
Vascular disorders	Hypertension, increased risk of atherosclerosis and thrombosis, vasculitis (as well as withdrawal syndrome after long-term therapy), increased capillary fragility.
Gastrointestinal disorders	Gastrointestinal ulcers, gastrointestinal bleeding, pancreatitis, stomach discomfort, hiccups.
Diseases of the skin and subcutaneous tissue	Red striae, atrophy, telangiectasia, petechiae, ecchymosis, hypertrichosis, steroid acne, rosacea-like (perioral) dermatitis, changes in skin pigmentation.
Diseases of the musculoskeletal system and connective tissue	Myopathy, muscle atrophy and weakness, osteoporosis (depending on the dose, also possible with short-term use), aseptic bone necrosis, tendon lesions, tendinitis, tendon rupture, epidural lipomatosis, growth retardation in children. Note: Reducing the dose too quickly after long-term treatment may cause symptoms such as muscle and joint pain.
Reproductive system and breast diseases	Disturbances in the secretion of sex hormones (as a consequence: irregular menstruation up to amenorrhea, hirsutism, impotence).

If any of the side effects listed in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Special instructions and precautions

Before using the drug, consult your doctor.

During treatment, especially long-term treatment, observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood patterns and blood glucose levels are necessary.

In order to reduce side effects, antacids can be prescribed, and the intake of K+ into the body should be increased (diet, potassium supplements). Food should be rich in proteins, vitamins, and limit the content of fats, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may worsen existing emotional instability or psychotic disorders. If a history of psychosis is indicated, dexamethasone in high doses is prescribed under the strict supervision of a physician.

It should be used with caution in acute and subacute myocardial infarction - the necrosis may spread, the formation of scar tissue may slow down, and the heart muscle may rupture.

In stressful situations during maintenance treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to an increased need for glucocorticosteroids. Patients should be carefully monitored for a year after the end of long-term therapy due to the possible development of relative insufficiency of the adrenal cortex in stressful situations.

With sudden withdrawal, especially in the case of previous use of high doses, the development of withdrawal syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness) is possible, as well as an exacerbation of the disease for which the drug was prescribed.

During treatment with dexamethasone, vaccination should not be performed due to a decrease in its effectiveness (immune response).

When prescribing the drug for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics.

In children during long-term treatment with dexamethasone, careful monitoring of the dynamics of growth and development is necessary. Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

Due to the weak mineralocorticoid effect, the drug is used in combination with mineralocorticoids for replacement therapy for adrenal insufficiency.

In patients with diabetes mellitus, blood glucose levels should be monitored and therapy adjusted if necessary.

X-ray monitoring of the osteoarticular system (images of the spine, hand) is indicated.

In patients with latent infectious diseases of the kidneys and urinary tract, dexamethasone can cause leukocyturia, which may have diagnostic value.

Dexamethasone increases the content of 11- and 17-hydroxyketocorticosteroid metabolites.

Interaction with other medicinal products

Estrogens (eg, oral contraceptives): The half-life of glucocorticoids may be prolonged. Therefore, the effect of corticoids may be enhanced.

Antacids: Concomitant use of aluminum hydroxide or magnesium hydroxide may reduce the absorption of glucocorticoids and reduce the effectiveness of dexamethasone. There should be a 2-hour interval between taking one drug and the other.

Medicines that induce CYP3A4 such as rifampicin, phenytoin, carbamazepine, barbiturates and primidone: the effect of corticoids may be reduced.

Co-treatment with CYP3A inhibitors, including drugs containing cobicistat, is expected to increase the risk of systemic side effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic complications.

Drugs that inhibit CYP3A4 such as ketoconazole and itraconazole: the effect of corticoids may be enhanced.

Ephedrine: The metabolism of glucocorticoids may be accelerated and therefore their effectiveness reduced.

ACE inhibitors: increased risk of changes in blood parameters.

Cardiac glycosides: the effect of glycosides may be enhanced by potassium deficiency.

Saluretics/laxatives: May increase potassium excretion.

Antidiabetic agents: The hypoglycemic effect may be reduced.

Coumarin derivatives: the anticoagulant effect may be reduced or enhanced. If used concomitantly, dose adjustment of the anticoagulant may be required.

Nonsteroidal anti-inflammatory drugs (NSAIDs), salicylates and indomethacin: Increased risk of gastrointestinal ulcers and bleeding.

Non-depolarizing muscle relaxants: the effect of muscle relaxation may last longer.

Atropine, other anticholinergics: with simultaneous use, an additional increase in intraocular pressure is possible.

Praziquantel: Corticosteroids may cause decreased praziquantel blood concentrations.

Chloroquine, hydroxychloroquine, mefloquine: there is an increased risk of developing myopathies, cardiomyopathies.

Somatropin: The effect of somatropin may be reduced with long-term therapy.

Protirelin: When taking protirelin, a decrease in TSH levels may be observed.

Immunosuppressive agents: increased susceptibility to infections and possible exacerbation or manifestation of latent infection.

Cyclosporine: Cyclosporine blood levels increase and there is an increased risk of seizures.

Fluoroquinolones may increase the risk of tendon disorders.

Impact on research methods: skin reactions during allergy tests may be suppressed.

Overdose

Symptoms: the side effects described above may increase.

Treatment: reducing the dose of the drug, symptomatic therapy.

Release form

50 tablets in a bottle along with instructions for use in a box.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30°C.

Keep out of the reach of children!

Shelf life

36 months.

Vacation conditions

By prescription.