DEXAMETHASONE-VIAL amp 4mg/1ml N25

Nosological classification (ICD-10)

A48.3 Toxic shock syndrome
A49 Bacterial infection of unspecified localization
C71 Malignant neoplasm of the brain
C80 Malignant neoplasm without specification of localization
C82 Follicular [nodular] non-Hodgkin's lymphoma
C83 Diffuse non-Hodgkin's lymphoma
C84 Peripheral and cutaneous T-cell lymphomas
C85 Other and unspecified types of non-Hodgkin's lymphoma
C95 Leukemia of unspecified cell type
C95.0 Acute leukemia of unspecified cell type
C95.9 Leukemia, unspecified
D59 Acquired hemolytic anemia
D69.3 Idiopathic thrombocytopenic purpura
D70 Agranulocytosis
E06.1 Subacute thyroiditis
E27.1 Primary adrenal insufficiency
E27.2 Addison's crisis
E27.4 Other and unspecified adrenal insufficiency
E83.5.0* Hypercalcemia
G00 Bacterial meningitis, not elsewhere classified
G04 Encephalitis, myelitis and encephalomyelitis
G93.6 Cerebral edema
H01.0 Blepharitis
H10.1 Acute atopic conjunctivitis
H10.5 Blepharoconjunctivitis
H15.0 Scleritis
H15.1 Episcleritis
H16.2 Keratoconjunctivitis
H16.8 Other forms of keratitis
H20.9 Iridocyclitis, unspecified
H45.1 Endophthalmitis in diseases classified elsewhere
I61 Intracerebral hemorrhage
J40 Bronchitis, not specified as acute or chronic
J44 Other chronic obstructive pulmonary disease
J45 Asthma
J46 Status asthmaticus
J98.8.0* Bronchospasm
L30.9 Dermatitis, unspecified
L91.0 Keloid scar
L92.0 Granuloma annulare
L93.0 Discoid lupus erythematosus
M35.9 Systemic connective tissue disorders, unspecified
M79.0 Rheumatism, unspecified
Q89.1 Malformations of the adrenal gland
R57.8.0* Burn shock
R57.9 Shock, unspecified
S05.9 Injury to unspecified part of eye and orbit
S06 Intracranial injury
S09 Other and unspecified head injuries
T78.2 Anaphylactic shock, unspecified
T78.4 Allergy, unspecified
T79.4 Traumatic shock
T90.4 Consequences of injury to the eye, periorbital region
Z100* CLASS XXII Surgical practice
Z51.0 Radiotherapy course
Z94.7 Presence of a transplanted cornea

Contraindications

The only absolute contraindication for short-term use of Dexamethasone-Vial for health reasons is individual intolerance to the components of the drug.

Intra-articular injection of the solution is contraindicated in the following conditions:

previous arthroplasty;
pathological bleeding (caused by the use of anticoagulants or endogenous);
intra-articular bone fracture;
infectious diseases, including septic (infectious) inflammatory process in the joint and periarticular infections (including medical history;
severe periarticular osteoporosis;
absence of signs of inflammation in the joint or the so-called “dry joint” (including osteoarthritis without synovitis);
severe bone destruction;
joint deformation, including sharp narrowing of the joint space, ankylosis;
joint instability as a consequence of arthritis;
aseptic necrosis of the epiphyses of the bones that form the joint.

The drug should not be used while breastfeeding.

Dexamethasone-Vial solution in ampoules should be prescribed with caution in the following cases: for infectious and parasitic diseases of viral, bacterial or fungal etiology, including those recently suffered or after recent contact with a patient (herpes simplex, viremic phase of herpes zoster, measles, chicken pox , amebiasis, established or suspected strongyloidiasis, active and latent tuberculosis, systemic mycosis); with lymphadenitis after vaccination with BCG (BCG - bacillus Calmette - Guerin), during the period 8 weeks before and 2 weeks after vaccination; for immunodeficiency conditions, including acquired immunodeficiency syndrome (AIDS) and human immunodeficiency virus (HIV) infections; for gastrointestinal pathologies such as esophagitis, gastric and duodenal ulcers, acute or latent peptic ulcers, gastritis, intestinal anastomosis (created recently), threat of perforation or abscess formation in ulcerative colitis, diverticulitis; for diseases of the cardiovascular system (including arterial hypertension, recent myocardial infarction, decompensated chronic heart failure, hyperlipidemia); for diseases of the endocrine system such as diabetes mellitus (including impaired carbohydrate tolerance), hypothyroidism, thyrotoxicosis, Itsenko-Cushing's disease; with severe chronic liver failure, nephrourolithiasis, severe chronic renal failure, hypoalbuminemia (including conditions predisposing to its occurrence), open- and closed-angle glaucoma, acute psychosis, myasthenia gravis, systemic osteoporosis, stage III–IV obesity, poliomyelitis (not including forms of bulbar encephalitis) and pediatric patients.

When administered intra-articularly, caution is required when administering Dexamethasone-Vial to patients with a general severe condition, as well as if there was ineffectiveness or short-term action of the two previous injections.

During pregnancy, the use of Dexamethasone-Vial is possible only in cases where the expected therapeutic effect for the mother, in the opinion of the doctor, exceeds the potential threat to the fetus.

Directions for use and doses

IV, slow stream or drip (in acute and emergency conditions); i/m; local (into the pathological formation) administration is also possible.

The dosage regimen is individual and depends on the indications, the patient’s condition and his response to therapy.

To prepare a solution for intravenous drip infusion, you should use an isotonic sodium chloride solution or a 5% dextrose solution.

In the acute period for various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. During the day, you can administer from 4 to 20 mg of Dexamethasone 3-4 times.

Doses of the drug for children (i.m.)

When carrying out replacement therapy (for adrenal insufficiency) - 0.0233 mg/kg or 0.67 mg/m2, divided into 3 doses, every 3rd day or 0.00776–0.01165 mg/kg or 0.233–0.335 mg/m2 daily. For other indications, the recommended dose is 0.02776 to 0.16665 mg/kg or 0.833 to 5 mg/m2 every 12 to 24 hours.

When the effect is achieved, the dose is reduced to maintenance or until treatment is stopped. The duration of parenteral use is usually 3-4 days, then switch to maintenance therapy with Dexamethasone tablets.

Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenal insufficiency.

Pharmacological properties

Pharmacodynamics

Dexamethasone-Vial is a corticosteroid for systemic use with anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects. Its active ingredient, dexamethasone, is a synthetic hormone of the adrenal cortex, a methylated derivative of fluoroprednisolone, which inhibits the release of interferon gamma, interleukin-1 and interleukin-2 from lymphocytes and macrophages.

A peculiarity of the action of Dexamethasone-Vial is the significant inhibition of pituitary gland function against the background of the almost complete absence of mineralocorticosteroid activity.

Dexamethasone, without reducing the concentration of circulating beta-endorphin, suppresses the pituitary gland's release of beta-lipotropin and adrenocorticotropic hormone (ACTH), the secretion of follicle-stimulating hormone (FSH) and thyroid-stimulating hormone (TSH). Increases the excitability of the central nervous system (CNS). By stimulating the production of erythropoietins, it helps to increase the number of red blood cells. Reduces the content of lymphocytes and eosinophils.

As a result of the interaction of dexamethasone with specific cytoplasmic receptors, a complex is formed that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid (mRNA), which induces the formation of lipocortin and other proteins that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and the synthesis of endoperoxides, leukotrienes, prostaglandins, which contribute to the processes of allergy and inflammation.

By participating in protein metabolism, the substance helps reduce the amount of protein in plasma and enhance its catabolism in muscle tissue. Increases albumin synthesis in the liver and kidneys.

Dexamethasone affects lipid metabolism, increasing the synthesis of higher fatty acids and thyroglobulin (TG). By redistributing fat, it leads to its preferential accumulation in the face, abdomen, and shoulder girdle, causing the development of hypercholesterolemia.

As a result of the effect of Dexamethasone-Vial on carbohydrate metabolism, the absorption of carbohydrates from the gastrointestinal tract (GIT) increases. The activity of glucose-6-phosphatase increases, which leads to an increase in the flow of glucose into the blood from the liver. As a result of stimulation of phosphoenolpyruvate carboxylase and increased synthesis of aminotransferases, the process of gluconeogenesis is activated.

The effect on water-electrolyte metabolism is manifested by the retention of sodium and water ions in the body. The mineralocorticosteroid activity of dexamethasone stimulates the excretion of potassium ions, reduces the absorption of calcium ions from the gastrointestinal tract, increases their excretion by the kidneys and leaching from the bones.

The anti-inflammatory effect of Dexamethasone-Vial is due to the property of dexamethasone to inhibit the release of inflammatory mediators by eosinophils, induce the formation of lipocortin and reduce the number of mast cells that produce hyaluronic acid. It reduces capillary permeability, stabilizes cell membranes, organelle membranes (including lysosomal ones).

The antiallergic effect is a consequence of changes in the body's immune response as a result of Dexamethasone-Vial suppressing the synthesis and secretion of allergy mediators, delaying the release of histamine and other biologically active substances from sensitized mast cells and basophils. The effect also develops as a result of a decrease in the number of circulating basophils and the sensitivity of effector cells to allergy mediators, inhibition of the development of lymphoid and connective tissue, a decrease in the number of mast cells, T- and B-lymphocytes, and inhibition of antibody formation.

The effect of Dexamethasone-Vial in COPD (chronic obstructive pulmonary disease) is mainly based on the inhibition of processes such as inflammation, erosion and desquamation of the mucous membrane, eosinophilic infiltration of the submucosal layer of the bronchial epithelium. In addition, dexamethasone prevents or inhibits the development of edema of the mucous membranes. Promotes the deposition of circulating immune complexes in the bronchial mucosa, increasing sensitivity to endogenous catecholamines and exogenous sympathomimetics in small and medium bronchial beta-adrenergic receptors, reducing the viscosity of mucus by reducing its production.

The antishock and antitoxic effect is associated with the membrane protective properties of dexamethasone, a decrease in the permeability of the vascular wall, an increase in blood pressure (BP), and activation of liver enzymes that are involved in the metabolism of xeno- and endobiotics.

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

Suppresses the secretion and synthesis of ACTH, secondarily inhibits the synthesis of endogenous GCS. Reducing the rate of connective tissue reactions during the inflammatory process helps reduce the risk of scar tissue formation.

When taking a daily dose of 1–1.5 mg of dexamethasone, suppression of the adrenal cortex occurs. The duration of action on the hypothalamic-pituitary-adrenal system corresponds to the biological half-life of 32 to 72 hours.

The glucocorticosteroid activity of 0.5 mg dexamethasone is equivalent to approximately 3.5 mg prednisolone (or prednisone), 17.5 mg cortisone, or 15 mg hydrocortisone.

Pharmacokinetics

After intramuscular injection, absorption of dexamethasone occurs slowly. Its maximum concentration in plasma is reached after 7–9 hours.

Plasma protein binding at 80%.

Dexamethasone crosses the blood-brain and placental barrier. A small portion is excreted into breast milk.

Metabolism of the drug occurs in the liver. The half-life is 3–5 hours. Excreted through the kidneys.

Drug interactions

cardiac glycosides: the toxicity of cardiac glycosides is likely to increase, the risk of developing arrhythmias increases against the background of resulting hypokalemia;
acetylsalicylic acid: accelerated excretion of acetylsalicylic acid occurs, a decrease in the level of its metabolites in the blood; if dexamethasone is discontinued, the level of salicylates in the blood increases and the risk of adverse reactions increases;
isoniazid, mexiletine: metabolism increases, thereby reducing their plasma level, especially in patients with rapid acetylation processes;
paracetamol: the risk of hepatotoxicity of paracetamol associated with the induction of liver enzymes and the formation of a toxic metabolite of paracetamol increases;
somatropin: high doses of dexamethasone reduce the therapeutic activity of somatropin;
hypoglycemic drugs: their effectiveness decreases;
coumarin derivatives: dexamethasone enhances their anticoagulant effect;
GCS, thiazide diuretics, amphotericin B, carbonic anhydrase inhibitors: these drugs in combination with dexamethasone increase the risk of hypokalemia;
sodium-containing drugs: contribute to increased blood pressure and the occurrence of edema;
cyclosporine, ketoconazole: these drugs increase the toxicity of dexamethasone by inhibiting metabolism and reducing its clearance;
non-steroidal anti-inflammatory drugs (NSAIDs), ethanol: the likelihood of developing ulcerations of the gastrointestinal mucosa and bleeding increases. In the treatment of arthritis, a combination with NSAIDs is possible while reducing the dose of dexamethasone;
indomethacin: the risk of developing side effects of the drug increases when combined with indomethacin, which displaces dexamethasone from its connection with albumin;
amphotericin B, carbonic anhydrase inhibitors: the risk of osteoporosis increases with concomitant therapy with dexamethasone;
barbiturates, ephedrine, phenytoin, theophylline, rifampicin and other inducers of microsomal liver enzymes: the influence of these drugs helps to increase the rate of metabolism of the drug and reduce its therapeutic effect;
inhibitors of adrenal cortex function: taking mitotane and other inhibitors of adrenal cortex function may require increasing the dose of Dexamethasone-Vial;
thyroid hormones: dexamethasone clearance increases during therapy with thyroid hormones;
immunosuppressants: increase the risk of developing infections, lymphoma and other lymphoproliferative disorders caused by the Epstein-Barr virus;
ergocalciferol, parathyroid hormone: prevent the development of osteopathy caused by the drug;
praziquantel: the concentration of praziquantel in the blood decreases;
steroid hormonal drugs (anabolics, androgens, estrogens and oral contraceptives): in combination with dexamethasone, they contribute to the appearance of acne and hirsutism;
tricyclic antidepressants: in combination with them, dexamethasone can increase the severity of depression caused by taking GCS;
other corticosteroids, antipsychotic drugs (neuroleptics), carbutamide, azathioprine: when combined with these drugs, the risk of developing cataracts increases;
estrogens: oral estrogen-containing contraceptives and other estrogens help reduce clearance, lengthen the half-life of the drug, prolong its therapeutic and toxic effects;
muscle relaxants: drug-induced hypokalemia during the use of muscle relaxants may increase the severity and duration of muscle blockade;
m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates: the influence of these drugs contributes to an increase in intraocular pressure;
folic acid: its content increases with long-term therapy;
live antiviral vaccines: the risk of developing infections and viral activation increases with all types of immunization, including live antiviral vaccines;
vitamin D: dexamethasone weakens its effect on the absorption of calcium ions in the intestinal lumen;
Iofendylate: When administered intrathecally in combination with dexamethasone, the likelihood of developing arachnoiditis increases.

Reviews about Dexamethasone-Vial

Reviews of Dexamethasone-Vial are positive. Patients indicate the high efficiency and rapid action of the drug in emergency cases. They describe situations where Dexamethasone-Vial stopped the development of allergic dermatitis and, as a concomitant effect, significantly relieved the pain from heel spurs. The solution is used to relieve swelling from insect bites (wasps, bees), including in veterinary practice. Experts recommend that you always have this injection in your emergency kit, which is indispensable for allergies, croup, meningitis, and shock.

The disadvantages include an extensive list of contraindications and side effects. There are complaints of tachycardia and heartburn.

It is noted that Dexamethasone-Vial ampoules are easy to open, thanks to a special mark at the break site, but their quantity in the package (25 pieces) is too large, since the solution is usually used for a short course.

Side effects

from the endocrine system: decreased glucose tolerance, suppressed adrenal function, manifestation of latent diabetes mellitus or steroid diabetes mellitus, Itsenko-Cushing syndrome (increased blood pressure, pituitary obesity, moon face, hirsutism, amenorrhea, dysmenorrhea, stretch marks, myasthenia gravis), in children – delayed sexual development;
from the digestive system: flatulence, hiccups, nausea, vomiting, decreased or increased appetite, pancreatitis, erosive esophagitis, steroid ulcer of the stomach and duodenum, bleeding and perforation of the gastrointestinal tract; rarely - increased activity of alkaline phosphatase and liver transaminases;
from the cardiovascular system: increased severity or in predisposed patients the development of chronic heart failure, changes in the electrocardiogram (ECG) characteristic of hypokalemia, increased blood pressure, thrombosis, hypercoagulation, bradycardia (up to cardiac arrest), arrhythmias; in acute and subacute myocardial infarction - an increased risk of heart muscle rupture against the backdrop of slower formation of scar tissue and the spread of necrosis;
from the nervous system: insomnia, nervousness (anxiety), dizziness, delirium, headache, disorientation, increased intracranial pressure, hallucinations, euphoria, manic-depressive psychosis, vertigo, depression, paranoia, convulsions, pseudotumor of the cerebellum;
from the sensory organs: increased risk of developing secondary bacterial, fungal or viral eye infections, increased intraocular pressure (including damage to the optic nerve), trophic changes in the cornea, posterior subcapsular cataracts, exophthalmos, with parenteral administration in the head, turbinates, neck and skin head, sudden loss of vision is possible due to the deposition of drug crystals in the vessels of the eye;
on the metabolic side: increased sweating, increased body weight, increased excretion of calcium ions, hypocalcemia, negative nitrogen balance due to increased protein breakdown;
from the musculoskeletal system: steroid myopathy, osteoporosis (including pathological bone fractures), aseptic necrosis of the head of the femur and humerus, rupture of muscle tendons, atrophy (decreased muscle mass); in children – slowdown in growth and ossification processes against the background of premature closure of the epiphyseal growth zones;
on the part of the skin and mucous membranes: steroid acne, slower wound healing, thinning of the skin, ecchymoses, petechiae, hypo- or hyperpigmentation, stretch marks, increased risk of developing candidiasis and pyoderma;
allergic reactions: local allergic reactions, skin rash, itching, anaphylactic shock;
local reactions: with parenteral administration - pain, burning, numbness, paresthesia, infection at the injection site; rarely - necrosis of surrounding tissues, scarring at the injection site; with intramuscular injection - atrophy of the skin and subcutaneous tissue (it is especially dangerous to inject the solution into the deltoid muscle); with intravenous administration – flushing of the face, arrhythmias, convulsions; with intra-articular injection – increased pain in the joint; with intracranial administration - nosebleeds;
other: development or exacerbation of infections (usually due to the simultaneous use of immunosuppressants or vaccination), withdrawal syndrome, leukocyturia; side effects caused by mineralocorticosteroid activity - peripheral edema (fluid and sodium ion retention), hypernatremia, hypokalemic syndrome (hypokalemia, unusual weakness and fatigue, myalgia or muscle spasm, arrhythmia).