Universal reference book for medicines
Name of the drug: DEXOPHTHAN

Active substance: dexamethasone

Type: GCS for topical application in ophthalmology

Manufacturer: СЛАВЯНСКАЯ АПТЕКА (Россия)
Description of the active substance:
This information is a reference and it is not enough that the drug was prescribed by a doctor.
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PHARMACHOLOGIC EFFECT
GCS.
Suppresses the function of white blood cells and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. Violates the ability of macrophages to phagocytosis, as well as to the formation of interleukin-1. Promotes the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces the permeability of capillaries due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A 2 , which leads to suppression of the synthesis of prostaglandins and leukotrienes.
Suppresses the release of COX (mainly COX-2), which also contributes to a decrease in 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;
suppresses the formation of antibodies.
Dexamethasone suppresses pituitary release of ACTH and β-lipotropin, but does not reduce the level of circulating α-endorphin.
Oppresses the secretion of TSH and FSH.
With direct application on the vessels has a vasoconstrictor effect.

Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats.
Stimulates gluconeogenesis, promotes the capture 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 protein metabolism products. Increasing the glucose level in the blood activates the release of insulin.
Dexamethasone suppresses the capture of glucose by fat cells, which leads to activation of lipolysis.
However, due to increased secretion of insulin, lipogenesis stimulation occurs, which leads to fat accumulation.
Has catabolic effect in lymphoid and connective tissue, muscles, fatty tissue, skin, bone tissue.
Osteoporosis and Itenko-Cushing's syndrome are the main factors limiting long-term therapy to SCS. As a result of catabolic action, growth can be suppressed in children.
In high doses, dexamethasone can increase the excitability of brain tissue and helps lower the threshold of convulsive readiness.
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 anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

With external and local application, the therapeutic activity of dexamethasone is due to anti-inflammatory, antiallergic and antiexcudative (due to vasoconstrictor effect) action.

For anti-inflammatory activity exceeds hydrocortisone 30 times, does not have mineralocorticoid activity.

PHARMACOKINETICS
Binding to plasma proteins - 60-70%.
It penetrates through the histohematological barriers. In small amounts excreted in breast milk.
Metabolised in the liver.

T 1/2 is 2-3 hours. It is excreted by the kidneys.

When used locally 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 eye tissues or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone is significantly increased.
INDICATIONS
For oral administration: Addison-Birmer disease;
acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis;bronchial asthma; Rheumatoid arthritis in the phase of exacerbation; NNC; connective tissue diseases; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (common), acute eczema (at the beginning of treatment); malignant tumors (as a palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after a previous parenteral application of GCS).
For parenteral administration: shock of different genesis;
cerebral edema (with a brain tumor, craniocerebral trauma, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); asthmatic status; severe allergic reactions (Quincke's edema, bronchospasm, dermatosis, acute anaphylactic reaction to medications, serum transfusion, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute insufficiency of the adrenal cortex; acute croup; diseases of the joints (humeropathy periarthritis, epicondylitis, styloiditis, bursitis, tendovaginitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthrosis).
For use in ophthalmic practice: non-nasal and allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, irit, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia.

DOSING MODE
Individual.
Inside with severe diseases at the beginning of treatment appoint up to 10-15 mg / day, the maintenance dose can be 2-4.5 mg or more per day. The daily dose is divided into 2-3 doses. In small doses take 1 time / day in the morning.
When parenteral administration is administered iv in slowly struyno or drip (in acute and urgent conditions);
in / m; it is also possible periarticular and intraarticular administration. During the day, you can inject 4 to 20 mg of dexamethasone 3-4 times. The duration of parenteral use is usually 3-4 days, then switch to maintenance therapy with an oral form. In an acute period with various diseases and at the beginning of treatment, dexamethasone is used in higher doses. When the effect is achieved, the dose is reduced with an interval of several days until a maintenance dose is reached or until the treatment is terminated.
When used in ophthalmology in acute conditions, they instill in the conjunctival bag 1-2 drops.
every 1-2 hours, then, with decreasing inflammation, every 4-6 hours. Duration of treatment is 1-2 days to several weeks, depending on the clinical course of the disease.
SIDE EFFECT
On the part of the endocrine system: a decrease in glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, oppression of the adrenal gland function, Itzenko-Cushing syndrome (including the lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis , stria), delayed sexual development in children.

On the part of metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, 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, pseudotumor, cerebral palsy, headache, convulsions.

From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest);
development (in predisposed patients) or increased severity of chronic heart failure, changes in ECG, 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; when intracranial introduction - nosebleeds.
On the part of the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccough;
rarely - increased activity of hepatic transaminases and alkaline phosphatase.
From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral eye infections, trophic corneal changes, exophthalmos.

From the musculoskeletal system: slowing growth and ossification processes in children (premature closure of the 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, (atrophy) .

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

Allergic reactions: generalized (including skin rash, skin itching, anaphylactic shock) and with topical application.

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

Local reactions: with parenteral administration - tissue necrosis.

With external application: rarely - itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, striae, sweating.
With prolonged use or application to large areas of the skin, it is possible to develop systemic side effects characteristic of GCS.
CONTRAINDICATIONS
For short-term use according to vital indications - hypersensitivity to dexamethasone.

For intraarticular administration and introduction directly into the lesion: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intraarticular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including in the anamnesis), as well as general infectious disease, expressed near-joint osteoporosis, absence of signs of inflammation in the joint ("dry" joint, for example, with osteoarthritis without synovitis), severe bone destruction
and joint deformity (sharp narrowing of the joint gap, ankylosis), joint instability as the outcome of arthritis, aseptic necrosis of the joints forming the epiphyses of bones.
For external use: bacterial, viral, fungal skin diseases, skin tuberculosis, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), childhood (up to 2 years, with itching in the anus - up to 12 years), rosacea, vulgar acne, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis of the eyes, violation of the integrity of the ocular epithelium, acute form of purulent ocular infection in the absence of specific therapy, corneal diseases, combined with defects of the epithelium, trachoma, glaucoma.

PREGNANCY AND LACTATION
In pregnancy (especially in the first trimester), as well as during lactation, dexamethasone is used taking into account the expected therapeutic effect and the negative effect on the fetus.
With prolonged therapy during pregnancy, the possibility of fetal growth disorders 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.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should be used in severe chronic renal failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should be used in severe chronic liver failure.

APPLICATION FOR CHILDREN
Contraindications for external use: children under 2 years old, with itching in the anus - up to 12 years.

SPECIAL INSTRUCTIONS
Caution should be used for 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, strongyloidiasis (established or suspected), systemic mycosis;
active and latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific therapy.
With caution should be used within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, in immunodeficient conditions (including AIDS or HIV infection).

With caution should be used for gastrointestinal diseases: peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis.

With caution should be used for 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 necrosis focus, slow the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, hypertension, hyperlipidemia), endocrine diseases - diabetes mellitus including violation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, with severe chronic renal and / or hepatic insufficiency, nephrourolythiasis, hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (grade III-IV), poliomyelitis (with the exception of bulbar encephalitis), open and closed angle glaucoma.
If necessary, intraarticular administration with caution should be used in patients with a general severe condition, ineffectiveness (or short-term) of the effect of the previous 2 injections (taking into account the individual properties of the SCS used).

Before and during the treatment of GCS, it is necessary to monitor the overall blood test, the level of glycemia and the content of electrolytes in the plasma.

With intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.

The relative adrenal insufficiency caused by dexamethasone can persist for several months after its withdrawal.
Taking this into account, under stressful situations that arise during this period, hormone therapy is resumed with the simultaneous administration of salts and / or mineralocorticoids.
When using dexamethasone in patients with corneal herpes, one should keep in mind the possibility of perforation.
During treatment, it is necessary to monitor the intraocular pressure and the condition of the cornea.
With the sudden abolition of dexamethasone, especially in the case of previous use in high doses, there is a so-called withdrawal syndrome (not caused by hypocorticism), manifested by anorexia, nausea, inhibition, generalized musculoskeletal pains, general weakness.
After cancellation of dexamethasone for several months, relative insufficiency of the adrenal cortex may persist. If during this period there are stressful situations, prescribe (according to indications) for the time of GCS, if necessary in combination with mineralocorticoids.
During the treatment, control of blood pressure, water-electrolyte balance, picture of peripheral blood and glycemia level, as well as observation of the oculist, are required.

Children during prolonged treatment need careful monitoring of the dynamics of growth and development.
Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.
DRUG INTERACTION
With simultaneous use with antipsychotic drugs, bucarban, azathioprine, there is a risk of developing cataracts;
with drugs that have anticholinergic effects - 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 can occur.

With simultaneous use with diuretics, potassium excretion may be enhanced;
with NSAIDs (including with acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.
When used simultaneously with oral anticoagulants, the anticoagulant effect may be weakened.

With simultaneous use with cardiac glycosides, cardiac glycosides can be impaired because of potassium deficiency.

With simultaneous use with aminoglutethimide, a decrease or depression of dexamethasone effects is possible;
with carbamazepine - a decrease in the effect of dexamethasone; with ephedrine - increasing the excretion of dexamethasone from the body; with imatinib - a decrease in the concentration of imatinib in the blood plasma due to the induction of its metabolism and increased excretion from the body.
With simultaneous application with itraconazole, the effects of dexamethasone are enhanced;
with methotrexate - there may be an increase in hepatotoxicity; with praziquantel - it is possible to reduce the concentration of praziquantel in the blood.
With simultaneous use with rifampicin, phenytoin, barbiturates, it is possible to weaken the effects of dexamethasone due to an increase in its excretion from the body.

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