Dexamethasone

The drug Dexamethasone is a typical representative of the hormones of the adrenal cortex, which are successfully used in medicine as strong anti-inflammatory agents. Dexamethasone belongs to the category of corticosteroid drugs for systemic use.

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Indications Dexamethasone

Dexamethasone may be prescribed by a doctor in the following cases:

• in pathologies of the endocrine system, namely: in case of insufficient function of the adrenal cortex, in case of hereditary hyperplasia of the adrenal cortex, in the subacute stage of thyroiditis;
• for various types of shock conditions;
• in cases of cerebral edema caused by tumor processes, traumatic brain injuries, surgery, hemorrhages, inflammatory processes, radiation exposure;
• in case of asthmatic status, bronchospasm;
• in severe allergic processes, anaphylaxis;
• in rheumatological pathologies;
• in autoimmune processes;
• in oncology;
• for blood diseases;
• as part of complex therapy for severe infectious processes;
• for the treatment of eye diseases (keratoconjunctivitis, blepharitis, scleritis, etc.);
• for local use.

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Release form

• Dexamethasone is produced as a liquid for injection, which is a transparent, slightly yellowish solution. One ampoule with 1 and 2 ml of the drug contains 4 and 8 mg of sodium phosphate dexamethasone, respectively. The ampoules are made of dark glass. The packaging is cardboard, with instructions inside.
• Dexamethasone can also be produced in the form of white cylindrical tablets with a dosage notch in the center. The tablets have a dosage of 0.5 mg. The package contains 5 or 10 cell blisters, 10 tablets in each.

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Pharmacodynamics

The synthetic glucocorticosteroid hormone Dexamethasone is a methylated fluoroprednisolone preparation. Its main properties are anti-inflammatory, anti-allergic, immunosuppressive, anti-shock and antitoxic.

Dexamethasone activates the nervous system, reduces the number of lymphocytes and eosinophils, and potentiates the synthesis of erythropoietins.

Dexamethasone affects metabolic processes:

• reduces the percentage of proteins in plasma, accelerates the production of albumins and protein catabolism in muscle tissue;
• accelerates the production of fatty acids and triglycerides, initiates the redistribution of adipose tissue, increases the cholesterol content in the blood;
• improves the absorption of carbohydrates in the digestive system, accelerates the flow of glucose from the liver into the circulatory system, stimulates gluconeogenesis;
• retains sodium and moisture in the body, potentiates the removal of potassium and calcium from the body.

Dexamethasone significantly suppresses pituitary function with little mineralocorticosteroid activity.

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Pharmacokinetics

When taken internally, Dexamethasone is quickly and completely absorbed in the gastrointestinal tract. The maximum possible amount of the drug in the blood serum is detected in about an hour and a half. In the circulatory system, the active component of the drug binds to a specific protein - transcortin.

Dexamethasone easily penetrates physiological barriers (placenta, blood-brain barrier).

The drug is metabolized in the liver, forming a number of inactive metabolites.

The active component is excreted by the kidneys. The half-life is on average 4 hours.

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Dosing and administration

Treatment with Dexamethasone is prescribed individually.

The average daily dose of Dexamethasone for oral administration may be about 9 mg, with a maximum permissible dosage of 15 mg. After achieving the desired effect, the amount of the drug is gradually reduced, switching to a maintenance dosage (from 2 to 4 mg per day).

Injection of 4 to 20 mg of Dexamethasone per day is allowed. The drug can be administered intravenously, intramuscularly or locally (directly into the pathological focus). Physiological solution or 5% glucose solution can be used as a solvent.

If possible, after 3-4 days of Dexamethasone injections, switch to internal administration of the tablet form of the drug.

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Use Dexamethasone during pregnancy

Dexamethasone may be prescribed to pregnant women only in situations where the likely benefit of the drug is significantly higher than the possible risk of problems in the unborn child.

With prolonged treatment with Dexamethasone, various disorders in fetal development may form. If the drug is used during the third trimester of pregnancy, there is a fairly high risk that the fetus will develop atrophic changes in the adrenal cortex, which will subsequently cause hormone replacement therapy for the child born.

If Dexamethasone is prescribed to a woman who is breastfeeding, breastfeeding is stopped for the duration of treatment.

Contraindications

The following are considered clear contraindications to the use of Dexamethasone:

• allergic sensitivity to the ingredients of the drug;
• children under 3 years of age.

Relative contraindications may include:

• viral, fungal and microbial infections, tuberculosis, mycosis;
• the period of 2 months before and 2 weeks after vaccination;
• immunodeficiency states;
• inflammatory and ulcerative diseases of the digestive tract;
• myocardial infarction, cardiac failure in the decompensation stage, hypertension;
• thyroid disease, diabetes;
• insufficient kidney and liver function;
• osteoporosis, poliomyelitis, increased intraocular pressure;
• pregnancy and breastfeeding.

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Side effects Dexamethasone

The longer the course of treatment and the higher the dosage of Dexamethasone, the higher the likelihood of side effects.

In general, the drug is well accepted by the body, but in some cases the following undesirable symptoms appear:

• steroid diabetes mellitus, inhibition of adrenal function, Itsenko-Cushing syndrome, late sexual development in children;
• dyspepsia, inflammation of the pancreas, steroid form of peptic ulcer, change in appetite, increased gas formation;
• heart rhythm disturbances, changes in ECG, changes in blood pressure, increased blood clotting;
• mood changes, disorientation, convulsions, hallucinations, psychosis, depression, irritability, headaches;
• increased intraocular pressure, damage to the optic nerve, corneal dystrophy, cataracts;
• hypocalcemia, excessive sweating;
• swelling of the extremities, weight gain;
• osteoporosis, muscle and tendon damage;
• dystrophic changes in the skin, pigmentation disorders, acne, increased risk of purulent and fungal skin lesions;
• allergic processes;
• development of drug withdrawal syndrome.

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Overdose

Symptoms of Dexamethasone overdose include increased side effects.

Treatment of overdose is always symptomatic, with a reduction in the amount of the drug. It is impossible to abruptly stop taking Dexamethasone, as a “withdrawal syndrome” may develop.

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Interactions with other drugs

Dexamethasone is not prescribed:

• with cardiac glycosides (increases the risk of developing cardiac disorders);
• with a live antiviral vaccine (infection activation is possible);
• with paracetamol (increases toxic effect on the liver);
• with muscle relaxants (the degree of muscle blockade increases);
• with somatotropin (the effectiveness of the latter decreases);
• with antacids (absorption of Dexamethasone is reduced);
• with hypoglycemic drugs (their effect is reduced);
• with cyclosporines and ketoconazole (increases toxic effects);
• with thiazides, carbonic anhydrase inhibitors, other corticosteroids and amphotericin (increases the risk of developing hypokalemia);
• with non-steroidal anti-inflammatory drugs and ethyl alcohol (increases the risk of developing ulcers in the digestive tract);
• with indomethacin (increases the likelihood of developing side effects);
• with carbonic anhydrase inhibitors and amphotericin (increases the risk of osteoporosis);
• with thyroid hormones (increases clearance of corticosteroids);
• with immunosuppressants (the risk of infection and lymphoma development increases);
• with estrogens (decreases clearance of corticosteroids);
• with other steroids (hirsutism and acne may develop);
• with tricyclic antidepressants (the manifestations of depression are aggravated);
• with other glucocorticosteroids, antipsychotic drugs, azathioprine and carbutamide (increases the risk of cataracts);
• with m-anticholinergics (intraocular pressure increases).

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Storage conditions

Dexamethasone in ampoules or tablets can be stored at normal room temperature, out of the reach of children.

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Shelf life

The solution in ampoules is stored for up to 3 years. Dexamethasone tablets are stored for up to 4 years.

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