Dexamethasone

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

[1], [2], [3], [4]

Indications Dexamethasone

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

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

[5], [6], [7], [8], [9], [10], [11],

Release form

• Dexamethasone is produced as a liquid for injection, which is a clear, slightly yellowish solution. One ampoule with 1 and 2 ml of the drug contains 4 and 8 mg of sodium dexamethasone phosphate, respectively. Ampoules are made of dark glass. Packing is cardboard, with a nested instruction inside.
• Dexamethasone can be produced in the form of white tablets of cylindrical shape, with a metering notch in the center. Tablets have a dosage of 0.5 mg. Packaging contains 5 or 10 cell blisters, 10 tablets each.

[12], [13], [14], [15], [16], [17],

Pharmacodynamics

Synthetic glucocorticosteroid hormone Dexamethasone is a methylated drug of fluoride prednisolone. Its main properties are anti-inflammatory, antiallergic, immunosuppressive, antishock and antitoxic.

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

Dexamethasone has an effect on metabolic processes:

• reduces the percentage of proteins in the plasma, accelerates the production of albumins and protein catabolism in muscle tissues;
• accelerates the production of fatty acids and triglycerides, triggers the redistribution of adipose tissue, increases the content of cholesterol 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 excretion of potassium and calcium from the body.

Dexamethasone inhibits hypophyseal function to a great extent with a slight manifestation of mineralocorticosteroid activity.

[18], [19], [20], [21], [22]

Pharmacokinetics

With internal administration, Dexamethasone is rapidly and fully absorbed in the gastrointestinal tract. The maximum possible amount of the drug in the blood serum is detected after about an hour and a half. In the circulatory system, the active component of the drug comes into contact with a specific protein - transcortin.

Dexamethasone penetrates without difficulty through physiological barriers (placenta, blood-brain barrier).

The metabolism of the drug occurs in the liver with the formation of a number of inactive metabolites.

Excretion of the active component is carried out by the kidneys. The half-life period is on average 4 hours.

[23], [24], [25], [26], [27],

Dosing and administration

Treatment with Dexamethasone is prescribed individually.

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

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

If possible, after 3-4 days of injection, Dexamethasone is switched to the internal reception of the tablet form of the drug.

[32], [33]

Use Dexamethasone during pregnancy

Dexamethasone can be prescribed to pregnant women only in situations where the probable benefit from the drug is significantly higher than the potential risk of violations in the unborn child.

With prolonged treatment with Dexamethasone, various disorders in the development of the fetus can form. If the drug is used during the third trimester of pregnancy, then there is a significant risk that the fetus will develop atrophic changes in the adrenal cortex, which in the future will cause the child to be given hormone replacement therapy.

If Dexamethasone is prescribed to a woman breastfeeding, then for the duration of treatment, breastfeeding is discontinued.

Contraindications

Unambiguous contraindications for the use of dexamethasone are:

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

 Relative contraindications may include:

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

[28], [29], [30]

Side effects Dexamethasone

The probability of side effects is higher the longer the course of treatment and the higher the dosage of Dexamethasone.

In general, the drug is perceived by the body not bad, but in some cases such undesirable symptoms appear:

• steroid form of diabetes mellitus, inhibition of adrenal gland function, Itenko-Cushing syndrome, later sexual development in the child;
• dyspepsia, inflammation of the pancreas, steroid form of peptic ulcer, changes in appetite, increased gas formation;
• disorders of the heart rhythm, changes in the ECG, changes in blood pressure, increasing blood coagulability;
• mood changes, loss of orientation, convulsive syndrome, hallucinations, psychoses, depressive conditions, irritability, headaches;
• increased intraocular pressure, optic nerve damage, corneal dystrophy, cataract;
• hypocalcemia, excessive sweating;
• swelling of the extremities, weight gain;
• osteoporosis, muscle and tendon damage;
• dystrophic skin changes, pigmentation disorders, acne eruptions, increased risk of purulent and fungal skin lesions;
• allergic processes;
• development of the "withdrawal syndrome" of the drug.

[31],

Overdose

Symptoms of an overdose of Dexamethasone are increased side effects.

Treatment of an overdose is always symptomatic, against a background of a decrease in the amount of the drug. Drug withdrawal can not be abruptly canceled, since it is possible to develop a "withdrawal syndrome".

[34], [35], [36], [37]

Interactions with other drugs

Dexamethasone is not prescribed:

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

[38], [39], [40]

Storage conditions

Dexamethasone in ampoules or tablets can be stored at normal room temperature, in places inaccessible to children.

[41], [42], [43], [44]

Shelf life

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

[45], [46]