Dexamethasone-Vial - instructions for use, dose, side effects, contraindications

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 (TSH) and follicle-stimulating hormone (FSH).

Increases the excitability of the central nervous system (CNS), reduces the number of lymphocytes and eosinophils, increases 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, inhibits the release of arachidonic acid, and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, 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 the synthesis of higher fatty acids and thyroglobulin (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 gastrointestinal tract (GIT); 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 exchange: detains 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.

Anti-inflammatory effect is associated with inhibition of eosinophil release by inflammatory mediators; inducing lipocortin formation and reducing the number of mast cells producing hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes and membranes of organelles (especially lysosomal).

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, decrease in the number of circulating basophils, suppression of lymphoid and connective tissue development, decrease in the number of T and B lymphocytes,reducing the sensitivity of the effector cells to the mediators of allergy, inhibition of antibody production, changes in the immune response.

In chronic obstructive pulmonary disease (COPD), the action is based primarily on the inhibition of inflammation, inhibition of progression or prevention of edema of mucous membranes, inhibition of eosinophil infiltration submucosal bronchial epithelium layer deposition in the bronchial mucosa of circulating immune complexes and braking erozirovaniya and desquamation mucosa . Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus due to oppression or reduction of its production.

Anti-shock and antitoxic action is associated with an increase in blood pressure (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

Immunodepressive effect is caused by 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 intramuscular (IM) injection is absorbed slowly, the maximum content in the plasma - after 7-9 hours. Communication with plasma proteins - 80%. Penetrates through blood-brain and placental barriers. Metabolised in the liver. The half-life is 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;

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

- aboutbrain tissue (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma);

- brohnhialnaya asthma (severe form), asthmatic status;

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

- aboutadrenal insufficiency;

- tiritoksichesky crisis;

- abouthepatitis, hepatic coma;

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

Contraindications:

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

For intraarticular administration: anterior arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intraarticular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (incl.in the history), as well as general infectious disease, expressed near-joint osteoporosis, the absence of signs of inflammation in the joint (the so-called dry joint, for example, with osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), instability of the joint as the outcome of arthritis, aseptic necrosis of the joints forming the epiphyses of bones.

Carefully:

Parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with the patient) - herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles; amoebiasis, strongyloidiasis (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 threat, 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 (including a violation of tolerance to carbohydrates), 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 gravis, acute psychosis, obesity (III-IV st), poliomyelitis (with the exception of the form of bulbar encephalitis), open and closed angle glaucoma.

For intraarticular administration: 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 GCS used).

Pregnancy and lactation:

During pregnancy (especially in the first trimester) the drug can be applied 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.

Dosing and Administration:

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 every 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 the respiratory distress syndrome of the newborn - IV IM 4, 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 mcg / kg (0.83-5 mg / m 2) every 12-24 hours.

Side effects:

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.

From the endocrine system: reduced glucose tolerance, "steroid" diabetes or a manifestation of latent diabetes mellitus, adrenal suppression, Cushing's syndrome (moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae) delayed sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, "steroid" stomach ulcers and 12 duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From 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 sense organs: sudden loss of vision (with parenteral administration in 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 eye, trophic changes of the cornea, exophthalmos.

From the side 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).

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

From the skin and mucous membranes: delayed wound healing, petechiae, ecchymoses, skin thinning, 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 facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

Local for parenteral administration: burning, numbness, pain,paresthesia and infection at the site of administration; 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, seizures.

With intracranial administration: nose bleed.

With intra-articular injection: increased pain in the joint.

Overdose:

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

Treatment: symptomatic, there is no specific antidote.

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 removal of acetylsalicylic acid, reduces the content of its metabolites in the blood (with the abolition of dexamethasone, the concentration of salicylates in the blood increases and the risk of side effects increases).

With simultaneous use with live antiviral vaccines and against other types of immunizations, 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.

Increases the risk of hepatotoxic effects of paracetamol (induction of "liver" enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the content of folic acid.

Hypokalemia caused by SCS can increase the severity and duration of muscle blockade against the background of muscle relaxants.

In high doses reduces the effect of somatropin.

Dexamethasone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.

Weaken the influence of vitamin D on the absorption of calcium ions in the lumen of the intestine. Ergocalciferol and parathyroid hormone interfere with the development of osteopathy caused by SCS.

Reduces the concentration of praziquantel in the blood.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.

Thiazide diuretics, inhibitors of carbonic anhydrase, other glucocorticosteroids and amphotericin B increase the risk of hypokalemia, sodium-containing drugs - edema and increased blood pressure.

Non-steroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of ulceration of the gastrointestinal mucosa and bleeding, in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect.

Indomethacin, displacing dexamethasone from association with albumin, increases the risk of developing its side effects.

Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect of GCS decreases under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of "hepatic" microsomal enzymes (an increase in metabolic rate).

Mitotane and other inhibitors of the function of the adrenal cortex may necessitate an increase in the dose of GCS.

The clearance of GCS rises against the background of thyroid hormones.

Immunosuppressants increase the risk of infection and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of GCS, prolong the half-life and their therapeutic and toxic effects.The emergence of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic, oral contraceptives.

Tricyclic antidepressants can increase the severity of depression caused by SCS (not shown for the therapy of these side effects).

The risk of developing cataracts increases with the use of other SCS, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Simultaneous appointment with m-holinoblokatorami (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.

With simultaneous intertecal application with yofendilate, the risk of developing arachnoiditis increases.

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.

Form release / dosage:

Solution for injection, 4 mg / ml.

Packaging:

1 ml is placed in a vial of dark glass, with a dot to indicate the location of the fracture. Each label is labeled or labeled with a quick-fixing paint.

5 ampoules are placed in a contour mesh packing.

5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

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.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006923/10

Date of registration:21.07.2010

Expiration Date:Unlimited

The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia

Manufacturer: & nbsp

CSPC OUYI PHARMACEUTICAL, Co.Ltd. China

Representation: & nbspVIAL, LLCVIAL, LLC

Information update date: & nbsp21.03.2017

Illustrated instructions

Instructions

Dexamethasone-Vial (DEXAMETHASONE-VIAL)