Universal reference book for medicines
Product name: DEXAMETHASONE-VIAL (DEXAMETHASONE-VIAL)

Active substance: dexamethasone

Type: GCS for injection

Manufacturer: VIAL (Russia) manufactured by CSPC OUYI PHARMACEUTICAL (China) packed OZONE (Russia)
Composition, form of production and packaging
Solution for injection
1 ml

dexamethasone (in the form of sodium phosphate) 4 mg

1 ml - ampoules (10) - packs of cardboard.

1 ml - ampoules (5) - contour plastic packaging (1) - cardboard packs.

1 ml - ampoules (5) - contour plastic packaging (2) - cardboard packs.

1 ml - dark glass ampoules (10) - cardboard boxes.

1 ml - ampoules of dark glass (10) - packs of cardboard.

1 ml - ampoules of dark glass (5) - packs cardboard.

1 ml - dark glass ampoules (5) - plastic contoured packages (1) - cardboard packs.

1 ml - ampoules of dark glass (5) - plastic contoured packages (2) - cardboard packs.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Glucocorticosteroid (GCS) is a methylated derivative of fluoride prednisolone, inhibits the release of interleukin-1, interleukin-2, interferon gamma from lymphocytes and macrophages.
Has anti-inflammatory, antiallergic, desensitizing, anti-shock, antitoxic and immunosuppressive action.
Suppresses pituitary adrenocorticotropic hormone release (ACTH) and beta-lipotropin, but does not reduce the content of circulating beta-endorphin.
Oppressing the secretion of thyroid-stimulating hormone (TTT) and follicle-stimulating hormone (FSH).
Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases the number of erythrocytes (stimulates the production of erythropoietins).

Interacts with specific cytoplasmic receptors and forms a complex that penetrates into the nucleus of the cell and stimulates the synthesis of mRNA;
the latter induces the formation of proteins, incl. lipocortin, mediating cellular effects. Lipocortin depresses phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation processes, allergies.
Protein metabolism: reduces the amount of protein in the plasma (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumins in the liver and kidneys;
enhances protein catabolism in muscle tissue.
Lipid metabolism: increases synthesis of higher fatty acids and thyreoglobulin (TG), redistributes fat (accumulation of fat mainly in the area of ​​the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the digestive tract;
increases the activity of glucose-6-phosphatase, leading to an increase in the intake of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases leading to the activation of gluconeogenesis.
Water-electrolyte metabolism: retards sodium ions and water in the body, stimulates the excretion of potassium ions (mineralocorticosteroid activity), reduces the absorption of calcium ions from the digestive tract, "removes" calcium ions from the bones, increases the excretion of calcium ions by the kidneys.

The anti-inflammatory effect is associated with the inhibition of eosinophil release by inflammatory mediators;
inducing lipocortin formation and reducing the number of mast cells producing hyaluronic acid; and also with a decrease in the permeability of capillaries; stabilization of cell membranes and membranes of organelles (especially lysosomal).
The antiallergic effect develops as a result of suppression of synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, suppression of lymphoid and connective

tissue, reducing the number of T- and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to mediators of allergy, inhibiting antibody formation, changing the immune response of the body.

In chronic obstructive pulmonary diseases (COPD), the action is mainly based on inhibition of inflammatory processes, inhibition of development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the mucosa of the bronchi, and inhibition of erosion and desquamation mucous membrane.
Increases the sensitivity of beta-adrenergic receptors of bronchi of small and medium caliber to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus due to oppression or reduction of its production.
The anti-shock and antitoxic effect is associated with an increase in blood pressure (BP) (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), reducing the permeability of the vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics .

Immunodepressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages.

Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.
It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
The peculiarity of the action is a significant inhibition of the pituitary function and a virtually complete absence of mineralocorticosteroid activity.
Doses of 1-1.5 mg / day inhibit the adrenal cortex; the biological half-life is 32-72 hours (the duration of oppression of the hypothalamic-pituitary-adrenal system).
The strength of the glucocorticosteroid activity of 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone or 17.5 mg of cortisone.

PHARMACOKINETICS

After a / m injection is absorbed slowly, the maximum content in the plasma - after 7-9 hours.

The connection with plasma proteins is 80%.
Penetrates through blood-brain and placental barriers.
Metabolised in the liver.
T 1/2 - 3-5 hours. It is excreted by the kidneys (a small part - with lactating glands).
INDICATIONS

- shock (burn, traumatic, operational, toxic) with ineffectiveness of other therapy;

- Allergic reactions (acute, severe forms), blood transfusion shock, anaphylactic shock, anaphylactoid reactions;

- edema of the brain (including against the background of a brain tumor or associated with surgery, radiation therapy or head trauma);

- bronchial asthma (severe form), asthmatic status;

- systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);

acute adrenal insufficiency;

- thyrotoxic crisis;

acute hepatitis, hepatic coma;

- poisoning with cauterizing fluids (reducing inflammation and preventing cicatricial narrowing).

DOSING MODE

The dosage regimen is individual and depends on the indications, the patient's condition and his reaction to therapy.
The drug is administered intravenously slowly by jet or drip (in acute and urgent conditions); intramuscularly; possibly also local (in pathological education) introduction. To prepare a solution for intravenous (intravenous) drop infusion, an isotonic solution of sodium chloride or a 5% dextrose solution should be used.
Dexamethasone sodium phosphate: intraarticular, in the lesion - 0.2-6 mg, with a repetition of 1 time in 3 days or 3 weeks.

In / m or in / in - 0.5-9 mg / day.

For the treatment of cerebral edema - 10 mg in the first injection, then 4 mg IM once every 6 hours until the symptoms disappear.
The dose can be reduced after 2-4 days with a gradual cancellation in the period of 5-7 days after the removal of cerebral edema. Maintenance dose - 2 mg 3 times / day.
For the treatment of shock, i.v. 20 mg in the first administration, then 3 mg / kg for 24 hours as an IV infusion or intravenously, 2 to 6 mg / kg as a single injection or 40 mg as a single dose an injection administered every 2 to 6 hours;
maybe iv administration of 1 mg / kg once. The shock therapy should be canceled, as soon as the patient's condition stabilizes, the usual duration is not more than 2-3 days.
Allergic diseases - in / m in the first injection of 4-8 mg.
Further treatment is carried out by oral dosage forms.
With nausea and vomiting during chemotherapy - iv 8-20 mg for 5-15 minutes before the chemotherapy session.
Further chemotherapy should be performed using oral dosage forms.
For the treatment of respiratory distress syndrome of newborns - IM / IV 4 injections of 5 mg every 12 hours, then from the seventh day every 24 hours. The maximum daily dose is 80 mg.

For children : for treatment of adrenal insufficiency - in / m at 23 mcg / kg (0.67 mg / m 2 ) every 3 days, or 7.8-12 mcg / kg (0.23-0.34 mg / m 2 / day), or 28- 170 μg / kg (0.83-5 mg / m 2 ) every 12-24 hours.

SIDE EFFECT

The frequency of development and severity of side effects depend on the duration of application, the amount of dose used and the possibility of observing the circadian rhythm of the appointment.

On the part of the endocrine system: a decrease in glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhoea, amenorrhea, myasthenia, striae) , delay in sexual development in children.

On the part of the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccough.
In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.
From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest);
development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.
From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

From the senses: sudden loss of vision (with parenteral administration in the region of the head, neck, nasal concha, scalp may precipitate crystals of the drug in the vessels of the eye), posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial , fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos.

On the part of metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticosteroid activity - fluid retention and sodium ions (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

On the part of the musculoskeletal system: slowing growth and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thighbone), rupture of the tendons of the muscles, steroid myopathy, muscle mass (atrophy).

On the part of the skin and mucous membranes: delayed healing of wounds, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, propensity to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

Other: development or exacerbation of infections (the emergence of this side effect is promoted by jointly used immunosuppressants and vaccination), leukocyturia, the "withdrawal" syndrome.

Local with parenteral administration: burning, numbness, pain, paresthesia and infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site;
atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous is the introduction to the deltoid muscle).
With iv introduction: arrhythmias, "tides" of blood to the face, convulsions.

With intracranial injection , nosebleeds.

When intra-articular introduction - increased pain in the joint.

CONTRAINDICATIONS

- for short-term use according to "vital" indications, the only contraindication is hypersensitivity.

For intraarticular administration: previous arthroplasty, pathological hemorrhage (endogenous or caused by the use of anticoagulants), intraarticular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including in the anamnesis), as well as a common infectious disease, expressed near the articular osteoporosis, absence of signs of inflammation in the joint (so-called "dry" joint, for example, with osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp
narrowing of the joint gap, ankylosis), joint instability as the outcome of arthritis, aseptic necrosis of the joints forming the epiphyses of bones.
Carefully:

- parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles;
amebiasis, strongyloidiasis (established or suspected) systemic mycosis; active and latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific therapy;
- Post-vaccination period (period of 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

- immunodeficiency conditions (including AIDS or HIV infection);

- Diseases of the gastrointestinal tract: peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis;

- diseases of the cardiovascular system, incl.
recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, the spread of the necrosis foci, slowing the formation of scar tissue and, as a result, rupture of the heart muscle), decompensated chronic heart failure, hypertension, hyperlipidemia;
- endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease;

- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV century), poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma.

For intraarticular administration : the general severe condition of the patient, ineffectiveness (or short-term) of the effect of the previous 2 injections (taking into account the individual properties of the SCS used).

PREGNANCY AND LACTATION

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 prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In case of application 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, then breastfeeding should be discontinued.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution in severe chronic renal failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution in severe chronic liver failure.

APPLICATION FOR CHILDREN

Children who, during the treatment with the drug, were in contact with sick measles or chickenpox, prophylactically prescribe specific immunoglobulins. In children in the period of growth, GCS should be used only in absolute indications and under the strictest supervision of the attending physician.

SPECIAL INSTRUCTIONS

Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.
In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.
It should be noted that in patients with hypothyroidism, the clearance of GCS decreases, and in patients with thyrotoxicosis - increases.

OVERDOSE

Symptoms: increased blood pressure, swelling, peptic ulcer, hyperglycemia, impaired consciousness.

Treatment: symptomatic, there is no specific antidote.

DRUG INTERACTION

Dexamethasone is pharmaceutically incompatible with other drugs (may form insoluble compounds).
Dexamethasone increases the toxicity of cardiac glycosides (because of the resulting hypokalemia, the risk of arrhythmias increases). Accelerates the excretion of acetylsalicylic acid, reduces the content of its metabolites in the blood (with the dexamethasone withdrawal, the concentration of salicylates in the blood increases and the risk of side effects increases). When used simultaneously with live antiviral vaccines and against other types of immunization, it increases the risk of virus activation and the development of infections. Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations. It increases the risk of hepatotoxic action of paracetamol (induction "liver" enzymes and education toxic metabolite of paracetamol).
Increases (when long-term therapy) folic acid content.
Hypokalaemia caused by corticosteroids may increase the severity and duration of muscle blockade on the background of muscle relaxants.
In high doses, it reduces the effects of growth hormone.
Dexamethasone reduces the effect of hypoglycemic drugs; It enhances the anticoagulant effect of coumarin derivatives.
Attenuates the effects of vitamin D on the absorption of calcium in the intestinal lumen.
Ergocalciferol and parathyroid hormone hinder the development of osteopathy caused by SCS.
Decreases praziquantel concentration in the blood.
Cyclosporine (inhibits metabolism) and ketoconazole (reduced clearance) increases the toxicity.
Thiazide diuretics, carbonic anhydrase inhibitors, corticosteroids and other amphotericin B increased risk of hypokalemia, sodium-containing drugs - edema and increase blood pressure.
NSAIDs and ethanol increase the risk of gastrointestinal mucosal ulceration and bleeding, in combination with NSAIDs for the treatment of arthritis may decrease the dose of corticosteroids due summation therapeutic effect.
Indomethacin, displacing dexamethasone from its association with albumin, increases the risk of its side effects.
Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect is reduced under the influence of SCS phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers "liver" microsomal enzymes (increased metabolic rate).
Mitotane and other inhibitors of adrenocortical function may necessitate increasing the dose of corticosteroids.
Clearance GCS increased against the background of thyroid hormones.
Immunosuppressants increase the risk of infections and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus.
Estrogens (including estrogen-containing oral contraceptives) reduce clearance SSC, extend half-life and their therapeutic and toxic effects.
The appearance of acne and hirsutism facilitates the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic steroids, oral contraceptives.
Tricyclic antidepressants may increase the severity of depression caused by GCS (not shown for the therapy of side-effects data).
The risk of developing cataracts increases with the use of corticosteroids compared to other antipsychotic drugs (neuroleptics), karbutamida and azathioprine.
Simultaneous administration with m-holinoblokatorami (including antihistamine drugs, tricyclic antidepressants) and nitrate promotes increased intraocular pressure.
At simultaneous application with intertekalnom yofendilatom increased risk of arachnoiditis.
TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

Store in a dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Shelf life - 3 years.

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