Dexamethasone tablets 0.5mg, No. 56

• Adrenal insufficiency

• thyroiditis,

• hypothyroidism,

• progressive ophthalmopathy,

• hemoblastosis,

• bronchial asthma,

• allergic diseases,

• rheumatism,

• rheumatoid arthritis,

• systemic connective tissue diseases,

• autoimmune hemolytic anemia,

• aplastic anemia,

• thrombocytopenia,

• agranulocytosis.

Inside, during or after meals (preferably in the early morning hours), the daily dose is 2-3 mg, in severe cases, up to 6 mg. After the onset of the therapeutic effect, the dose is gradually reduced to 0.5Ц1 mg / day.

Pills

1 tab.

dexamethasone 0.0005 g

• Arterial hypertension,

• Itsenko-Cushing's disease,

• psychosis,

• renal failure

• osteoporosis,

• peptic ulcer of the stomach and duodenum,

• bacterial endocarditis,

• syphilis,

• tuberculosis,

• diabetes,

• pregnancy.

pharmachologic effect

GKS. Suppresses the function of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ??inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. Promotes the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ??inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; inhibits the formation of antibodies.

Dexamethasone inhibits the release of ACTH and ?-lipotropin by the pituitary gland, but does not reduce the level of circulating ?-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to the vessels, it has a vasoconstrictor effect.

Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, dexamethasone enhances the storage of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose activates the release of insulin.

Dexamethasone inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to the increase in insulin secretion, lipogenesis is stimulated, which leads to the accumulation of fat.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, it is possible to suppress growth in children.

In high doses, dexamethasone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.

With systemic use, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

Pharmacokinetics

Plasma protein binding - 60-70%. Penetrates through histohematogenous barriers. A small amount is excreted in breast milk.

It is metabolized in the liver.

T1 / 2 is 2-3 hours. It is excreted by the kidneys.

When applied topically in ophthalmology, it is absorbed through the cornea with intact epithelium into the moisture of the anterior chamber of the eye. With inflammation of the tissues of the eye or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone significantly increases.

Side effect

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

From the side of metabolism: increased excretion of calcium ions, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

From the side of the central nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

From the side of 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 down the formation of scar tissue, which can lead to rupture of the heart muscle; with intracranial administration - epistaxis.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcers of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - an increase in the activity of hepatic transaminases and alkaline phosphatase.

From the senses: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

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

Dermatological reactions: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis.

Allergic reactions: generalized (including skin rash, itching of the skin, anaphylactic shock) and when applied topically.

Effects associated with immunosuppressive action: the development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressive drugs and vaccination).

Local reactions: with parenteral administration - tissue necrosis.

Application during pregnancy and lactation

During pregnancy (especially in the first trimester), as well as during lactation, dexamethasone is used taking into account the expected therapeutic effect and negative effect on the fetus. With prolonged therapy during pregnancy, the possibility of fetal growth disorders is not excluded. If used 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.

Application for violations of liver function

It should be used with caution in severe chronic hepatic failure.

Application for impaired renal function

It should be used with caution in severe chronic renal failure.

Application in children

Contraindications for external use: children under 2 years of age, with itching in the anus - up to 12 years.

special instructions

It should be used with caution in parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chickenpox, measles, amebiasis, strongyloidosis (established or suspect), systemic mycosis; active and latent tuberculosis. Application for severe infectious diseases is permissible only against the background of specific therapy.

It should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency conditions (including AIDS or HIV infection).

It should be used with caution in diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

It should be used with caution in diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, it is possible to spread the focus of necrosis, slow down the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases - diabetes mellitus ( including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and / or hepatic failure, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, psychosis, myasthenia gravis , obesity (III-IV degree), with poliomyelitis (except for the form of bulbar encephalitis),open and closed angle glaucoma.

If necessary, intra-articular administration should be used with caution in patients with a general severe condition, ineffectiveness (or short duration) of the action of 2 previous injections (taking into account the individual properties of the GCS used).

Before and during GCS therapy, it is necessary to monitor a complete blood count, blood glucose levels and plasma electrolytes.

With intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously carry out antibiotic therapy.

Dexamethasone-induced relative adrenal insufficiency may persist for several months after its withdrawal. Considering this, in stressful situations that arise during this period, hormonal therapy is resumed with the simultaneous administration of salts and / or mineralocorticoids.

When using dexamethasone in patients with corneal herpes, the possibility of corneal perforation should be borne in mind. During treatment, it is necessary to monitor intraocular pressure and the condition of the cornea.

With the sudden cancellation of dexamethasone, especially in the case of previous use in high doses, the so-called withdrawal syndrome occurs (not due to hypocorticism), manifested by anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness. After discontinuation of dexamethasone, relative adrenal insufficiency may persist for several months. If during this period stressful situations arise, they are prescribed (according to indications) at the time of GCS, if necessary in combination with mineralocorticoids.

During the period of treatment, monitoring of blood pressure, water-electrolyte balance, peripheral blood picture and glycemic level, as well as observation of an ophthalmologist is required.

In children, during long-term treatment, careful monitoring of the dynamics of growth and development is necessary. Children who, during the period of treatment, were in contact with patients with measles or chickenpox, are prophylactically prescribed specific immunoglobulins.

Drug interactions

With simultaneous use with antipsychotics, bukarban, azathioprine, there is a risk of developing cataracts; with drugs that have an anticholinergic effect - the risk of developing glaucoma.

With simultaneous use with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs decreases.

With simultaneous use with hormonal contraceptives, androgens, estrogens, anabolic steroids, hirsutism, acne are possible.

With simultaneous use with diuretics, it is possible to increase the excretion of potassium; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

With simultaneous use with oral anticoagulants, the weakening of the anticoagulant effect is possible.

With simultaneous use with cardiac glycosides, it is possible to impair the tolerance of cardiac glycosides due to potassium deficiency.

With simultaneous use with aminoglutethimide, it is possible to reduce or inhibit the effects of dexamethasone; with carbamazepine - a decrease in the effect of dexamethasone is possible; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - it is possible to reduce the concentration of imatinib in the blood plasma due to the induction of its metabolism and increased excretion from the body.

With simultaneous use with itraconazole, the effects of dexamethasone are enhanced; with methotrexate - an increase in hepatotoxicity is possible; with praziquantel - it is possible to reduce the concentration of praziquantel in the blood.

With simultaneous use with rifampicin, phenytoin, barbiturates, the effects of dexamethasone may be weakened due to an increase in its excretion from the body.