Dexamethasone, 4 mg/ml 2 ml 10 pcs

Pharmacotherapeutic group: glucocorticosteroid

ATX code: H02AB02

Pharmacological properties

Indications

Adrenal cortical insufficiency replacement therapy (in combination with sodium chloride and/or mineralocorticosteroids): acute adrenal cortical insufficiency (Addison’s disease, bilateral adrenalectomy); relative adrenal cortical insufficiency developing after withdrawal of GCS treatment; primary or secondary adrenal cortical insufficiency.

Symptomatic and pathogenetic therapy of other diseases requiring administration of rapid-acting GCS and when oral administration of the drug is not possible:

– endocrine diseases (congenital hyperplasia of the adrenal cortex, subacute thyroiditis);
– shock (burn, traumatic, surgical, toxic) – when vasoconstrictors, plasma substitute drugs and other symptomatic therapy are ineffective;
– cerebral edema (only after confirming the symptoms of increased intracranial pressure by the results of magnetic resonance imaging or computed tomography), due to a brain tumor in case of craniocerebral injury, neurosurgery, brain hemorrhage, encephalitis, meningitis, radiation injury;
– asthmatic status; Severe bronchospasm (exacerbation of bronchial asthma);
– Severe allergic reactions, anaphylactic shock;
– Rheumatic diseases;
– Systemic connective tissue diseases;
– acute severe dermatoses;
– malignant diseases (palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; In ophthalmological practice (subconjunctival, retrobulbar or parabulbar injection): keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation;
– local application (in the area of pathological formation): keloids, discoidal lupus erythematosus, ring granuloma;
– cauterizing fluid poisoning (reduction of inflammation and prevention of scarring).

Active ingredient

Composition

Active substance:

dexamethasone sodium phosphate (in terms of dexamethasone phosphate) -4.0 mg.

Auxiliary substances: Glycerol (distilled glycerin PK-94) – 22.5 mg, sodium hydrophosphate dodecahydrate (sodium phosphoric acid divalent 12-water) -0.8 mg; diethate dihydrate dinatrate [(salt of diatrium ethylenediamine-N, N, N’, N’ – tetraacetic acid 2-water (trilon B)] – 0.1 mg; water for injection, up to 1 ml.

How to take, the dosage

The dosing regimen is individual and depends on the indication, the patient’s condition and his reaction to therapy. The drug is administered intravenously (IV) slowly by trickle or drip (in acute and emergency conditions); intramuscularly (IV/m); local (into the pathological mass) and subconjunctival, retrobulbar or parabulbar administration is also possible.

In order to prepare the solution for intravenous infusion sodium chloride isotonic solution or 5% dextrose solution should be used.

The drug is administered by IV and IM in a dose of 0.5-24 mg/day in 2 doses (equivalent to 1/3 to 1/2 of the oral dose) in as short a course as possible at the lowest effective dose, treatment should be stopped gradually. If high doses are used over several days, the dose should be reduced gradually over the next few days or longer. Prolonged treatment should be carried out at a dose not exceeding 0.5 mg/day. No more than 2 ml of the solution should be administered intramuscularly at the same site.

In acute conditions, higher doses are used: the initial dose is 4-20 mg, which is repeated until the desired effect is achieved, the total daily dose rarely exceeds 80 mg. After therapeutic effect is achieved, dexamethasone is administered in 2-4 mg doses as needed, followed by gradual withdrawal of the drug. To maintain the long-term effect the drug is administered every 3-4 hours or as a prolonged drip infusion. After acute conditions have resolved, the patient is transferred to oral dexamethasone administration.

In case of shock the drug is administered strictly by IV bolus at a dose of 2-6 mg/kg. If necessary, repeated doses are administered every 2-6 hours or as a prolonged intravenous infusion at a dose of 3 mg/kg/day. Treatment with dexamethasone should be carried out as part of complex therapy of shock. The use of pharmacological doses is acceptable only for life-threatening conditions, and as a rule, this time does not exceed 48 to 72 hours.

In case of cerebral edema, the initial dose of 10 mg is administered by IV, then 4 mg every 6 h until the symptoms subside (usually within 12-24 h). After 2-4 days, the dose is reduced and the drug is gradually discontinued over 5-7 days.

Patients with malignant neoplasms may require maintenance treatment of 2 mg w/in or w/out 2-3 times daily.

In acute cerebral edema short-term intensive therapy is carried out: in adults the loading dose is 50 mg by IV, then on days 1-3 administer 8 mg every 2 hours, on day 4 – 4 mg every 2 hours, on days 5-8 – 4 mg every 4 hours, then the daily dose is reduced by 4 mg/day until its complete withdrawal. In children with body weight over 35 kg a loading dose of 25 mg by IV, then on days 1-3 administer 4 mg every 2 hours, on days 4 – 4 mg every 4 hours, on days 5-8 – 4 mg every 6 hours, then daily dose is reduced by 2 mg/day until complete abolition. In children with body weight less than 35 kg a loading dose is 20 mg intravenously, then on days 1-3 administer 4 mg every 3 hours, on days 4 – 4 mg every 6 hours, on days 5-8 – 2 mg every 6 hours, then the daily dose is reduced by 1 mg/day until complete withdrawal. In acute self-limiting allergic reactions or exacerbations of chronic allergic diseases, parenteral and oral dexamethasone should be combined: day 1 – IV 4-8 mg, day 2-3 – oral 1 mg twice daily, day 4-5 – oral 0.5 mg twice daily, day 6-7 – oral 0.5 mg once daily. On day 8, the effectiveness of therapy is evaluated.

Doses of the drug for children (intravenous): The dose of the drug in substitution therapy (in adrenal insufficiency) is 0.0233 mg/kg body weight or 0.67 mg/m2 body surface area, divided into 3 doses, every 3rd day, or 0.00776-0.01165 mg/kg body weight or 0.233-0.335 mg/m2 body surface area daily. For other indications, the recommended dose is 0.02776 to 0.16665 mg/kg body weight or 0.833 to 5 mg/m2 body surface area every 12 to 24 hours.

Interaction

Dexamethasone is pharmaceutically incompatible with other drugs (drugs) (may form insoluble compounds). It is recommended to administer it separately from other drugs (intravenous bolus, or through another IV, as a second solution). When mixing dexamethasone solution with heparin, a precipitate is formed.

Dexamethasone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of arrhythmias increases).

Accelerates excretion of acetylsalicylic acid, reduces its metabolites in the blood (when dexamethasone is withdrawn, the concentration of salicylates in the blood increases and the risk of side effects increases).

The simultaneous use with live antiviral vaccines and against the background of other types of immunizations increases the risk of virus activation and 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 formation of the toxic metabolite of paracetamol).

Enhances (with prolonged therapy) folic acid.

Hypokalemia caused by dexamethasone may increase the severity and duration of muscle blockade against myorelaxants.

In high doses it reduces the effect of somatropin.

Dexamethasone decreases the effect of hypoglycemic drugs; increases anticoagulant effect of coumarin derivatives.

It reduces the effect of vitamin D on absorption of calcium in the intestinal lumen. Ergocalciferol and parathormone prevent dexamethasone-induced osteopathy.

Decreases the concentration of praziquantel in the blood.

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

Thiazide diuretics, carboanhydrase inhibitors, other GCS and amphotericin B increase the risk of hypokalemia; Na-containing drugs increase the risk of edema and increased BP.

Non-steroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of gastrointestinal mucosal ulceration and bleeding; in combination with NSAIDs for arthritis, the dose of GCS may decrease due to the summation of therapeutic effect.

Indomethacin, by displacing dexamethasone from binding to albumin, increases the risk of its side effects.

Amphotericin B and carboanhydrase inhibitors increase the risk of osteoporosis. The therapeutic effect of dexamethasone is reduced by phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of microsomal liver enzymes (increased metabolic rate). Mitotane and other inhibitors of adrenal cortex function may necessitate increasing the dose of dexamethasone.

The clearance of dexamethasone is increased with the use of thyroid hormone drugs.

Immunosuppressants increase the risk of infections and lymphoma or other lymphoproliferative disorders caused by Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) decrease dexamethasone clearance, prolong the elimination half-life and their therapeutic and toxic effects.

The occurrence of hirsutism and acne is promoted by the simultaneous use of other steroid hormonal drugs – androgens, estrogens, anabolics, oral contraceptives.

Tricyclic antidepressants may increase the severity of depression caused by taking dexamethasone (not indicated for therapy of these side effects).

The risk of cataracts increases with other GCS, antipsychotic drugs (neuroleptics), carbutamide and azathioprine. Concomitant use with m-cholinoblockers (including antihistamines, tricyclic antidepressants), nitrates promotes development of increased intraocular pressure.

Concomitant use with fluoroquinolones increases the risk of tendopathy (mainly Achilles tendonitis) in elderly patients and in patients with tendon disease.

The antimalarials (chloroquine, hydroxychloroquine, mefloquine) in combination with dexamethasone may increase the risk of myopathy, cardiomyopathy.

Angiotensin-converting enzyme inhibitors may alter peripheral blood counts when concomitantly administered with dexamethasone.

Special Instructions

During treatment with dexamethasone (especially long-term), monitoring of ophthalmologist, control of blood pressure and water-electrolyte balance, as well as peripheral blood count and blood glucose levels is necessary.

In order to reduce side effects, the intake of K+ in the body should be increased (diet, potassium preparations). The diet should be rich in proteins, vitamins, with restriction of fat, carbohydrates and table salt.

The action of the drug is increased in patients with cirrhosis. It should be taken into account that dexamethasone clearance is decreased in patients with hypothyroidism and increased in patients with thyrotoxicosis.

The drug may exacerbate 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.

With caution should be used in acute and subacute myocardial infarction, since it is possible to spread the focus of necrosis, delay formation of scar tissue and rupture of the heart muscle.

The patient should be closely monitored for one year after discontinuation of long-term dexamethasone therapy due to possible development of relative adrenal cortical insufficiency in stressful situations.

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

When using dexamethasone, there is a risk of severe anaphylactic reactions and bradycardia.

In therapy with the drug, there is an increased risk of activation of strongyloidiasis.

The dose of dexamethasone should be temporarily increased in case of stressful situations during therapy (surgery, trauma). A temporary increase in the dose of the drug in stressful situations is necessary both before and after the stress.

With dexamethasone treatment it is necessary to use specific antibacterial therapy for therapy of latent tuberculosis, lymphadenitis after BCG vaccination, polio, acute and chronic bacterial, parasitic infections and specific therapy in patients with gastric and intestinal ulcer disease and osteoporosis.

Monitoring of patients with chronic heart failure, uncontrolled arterial hypertension, corneal trauma and ulcers, and glaucoma is required during therapy with the drug.

The course of myasthenia gravis may worsen.

If the drug is suddenly withdrawn, especially if high doses were previously used, acute adrenal insufficiency may develop; “withdrawal” syndrome (not due to adrenal insufficiency): decreased appetite, nausea, vomiting; lethargy, headache, generalized musculo-skeletal pain, asthenia; and exacerbation of the disease for which dexamethasone was prescribed.

In patients with diabetes mellitus, blood glucose concentrations should be monitored and doses of hypoglycemic drugs should be adjusted if necessary.

Dexamethasone may increase susceptibility or mask symptoms of infectious diseases. Chickenpox, measles, and other infections can be more severe and even fatal in non-immunized individuals. Immunosuppression is more common with long-term use, but can also occur with short-term dexamethasone treatment.

The drug may mask symptoms of “peritoneal irritation” in patients with gastric or intestinal wall perforation.

The use of GCS may cause changes in sperm motility and sperm count.

In children who have been in contact with patients with measles or chickenpox during treatment, specific immunoglobulins are given prophylactically. In children during long-term treatment with dexamethasone, the dynamics of growth and development must be closely monitored.

Impact on driving and operating machinery
During treatment, it is not recommended to drive vehicles or engage in potentially dangerous activities requiring rapid psychomotor reactions and increased concentration.

Synopsis

Contraindications

For short-term use for “vital” indications the only contraindication is hypersensitivity to any of the drug components. Breast-feeding period, systemic mycoses.
Simultaneous use of live or weakened vaccines with immunosuppressive doses of Dexamethasone.

Systemic parasitic and infectious diseases of viral, fungal or bacterial nature (current or recent, including recent contact with a patient) – herpes simplex, herpes zoster (viremic phase), chickenpox, measles; amebiasis, strongyloidiasis (established or suspected); active or latent tuberculosis. Use in severe infectious diseases is allowed only against a background of specific antimicrobial therapy.

Vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection).

Gastrointestinal diseases: peptic ulcer, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with risk of perforation or abscess, diverticulitis.

Hepatic insufficiency.

Hypoalbuminemia and conditions predisposing to its occurrence.

Diseases of the cardiovascular system, including recent myocardial infarction, decompensated chronic heart failure, arterial hypertension, hyperlipidemia.

Endocrine diseases – diabetes (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Icenko-Cushing’s disease, and obesity of degree III-IV.

Severe chronic renal failure, nephrourolithiasis.

Systemic osteoporosis, myasthenia gravis, poliomyelitis (except for the form of bulbar encephalitis), epilepsy, “steroid” myopathy.

Acute psychosis, severe affective disorders (including history, especially “steroid” psychosis).

Open- and closed-angle glaucoma, herpes eye (risk of corneal perforation).

Pregnancy.

Elderly patients due to high risk of osteoporosis and arterial hypertension.

In children during growth, dexamethasone should be used only with absolute indications and under the close supervision of the physician.

Side effects

The frequency and severity of side effects depend on the duration of use, the amount of dose used, and the ability to observe the circadian rhythm of administration.

Endocrine system disorders: Decreased glucose tolerance, “steroid” diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Icenko-Cushing’s syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased BP, dysmenorrhea, amenorrhea, myasthenia, “steroid” stretching), delayed sexual development in children.

Disorders of the blood and lymphatic system: moderate leukocytosis, lymphopenia, eosinopenia, polycythemia.

Gastrointestinal disorders: nausea, vomiting, pancreatitis, “steroid” gastric and 12 duodenal ulcer, erosive esophagitis, bleeding and perforation of the stomach or intestine, increased or decreased appetite, flatulence, hiccups, abdominal pain, feeling of discomfort in the stomach area. In rare cases, an increase in the activity of “liver” transaminases and alkaline phosphatase.

Heart and vascular disorders: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or worsening of chronic heart failure; electrocardiogram changes characteristic of hypokalemia; increased BP, hypercoagulation, thrombosis; with intravenous administration: “tides” to the face, vasculitis, increased capillary fragility. In patients with acute and subacute myocardial infarction – spread of the focus of necrosis, delayed formation of scar tissue, which may lead to rupture of the heart muscle.

Mental disorders: nervousness or anxiety, insomnia, emotional lability, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, tendency to suicide.

Nervous system disorders: increased intracranial pressure, dizziness, headache, vertigo, pseudotumor cerebellar, seizures.

VIight organ disorders: sudden loss of vision (with parenteral administration in the head, neck, nasal cavities, scalp, possible deposition of crystals of the drug in the vessels of the eye), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, susceptibility to develop secondary bacterial, fungal or viral eye infections, trophic changes of the cornea, exophthalmos, chemosis, ptosis, mydriasis, corneal perforation, central serous chorioretinopathy.

Metabolic and nutritional disorders: hypercholesterolemia, increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, epidural lipomatosis.

The mineralocorticoid-induced fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

Muscular and connective tissue disorders: growth retardation and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, “steroid” myopathy, decrease of muscle mass (atrophy).

Renal and urinary tract disorders: leukocyturia.

Skin and subcutaneous tissue disorders: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, “steroid” acne, “steroid” stretch marks, tendency to develop pyoderma and candidiasis, rosacea-like perioral dermatitis, suppressed reactions in skin tests, telangiectasia, hypertrichosis.

Immune system disorders: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

Infectious and parasitic diseases: development or exacerbation of infections (the appearance of this side effect is promoted by co-administration of immunosuppressants and vaccination).

General disorders and disorders at the injection site: “withdrawal” syndrome, local in parenteral administration: burning, numbness, pain, paresthesia and infection at the injection site, rarely – necrosis of surrounding tissues, scar formation at the injection site; skin and subcutaneous tissue atrophy when injected in /m (especially dangerous injection in the deltoid muscle).

Overdose

Pregnancy use

Dexamethasone penetrates the placenta and may reach high concentrations in the fetus. During pregnancy (especially in the first trimester) or in women planning pregnancy, administration of Dexamethasone is indicated if the expected therapeutic effect of the drug exceeds the risk of adverse effects on the mother or fetus. GCS should be prescribed in pregnancy only for absolute indications, with prolonged therapy during pregnancy the possibility of fetal growth disturbance cannot be excluded. If used at the end of pregnancy, there is a risk of adrenal atrophy in the fetus, which may require substitution therapy for the newborn.

A small amount of dexamethasone passes into breast milk.

If treatment with the drug is necessary while breastfeeding, breastfeeding should be stopped, as this may cause delayed growth of the baby and decreased secretion of its endogenous corticosteroids.

Similarities