Dexamethasone

Дексаметазон Drug photo

The description is actual on 06.07.2015

  • Latin name: Dexamethasone
  • ATH code: S01BA01
  • Active ingredient: Dexamethasone (Dexamethasone)
  • Producer: RUP of "Belmedpreparata" (Republic of Belarus), JSC Lekhim-Kharkiv, PAO "Farmak", CJSC FF Darnitsa (Ukraine)

Structure

Composition of Dexamethasone in ampoules: Dexamethasone sodium phosphate (4 mg/ml), glycerin, propylene glycol, dinatrium edetat, buffered solution phosphatic (7,5 rn), marked - and propilparagidroksibenzoat, water for and.

Dexamethasone in tablets contains in the structure 0,5 mg of active agent, and also lactose in the form of monohydrate, MKTs, silicon dioxide colloid anhydrous, magnesium stearate, croscarmellose sodium.

Drops for eyes Dexamethasone: Dexamethasone sodium phosphate (1 mg/ml), boric acid, a benzalkoniya chloride (preservative), sodium tetraborate, Trilonum of B, water for and.

Release form

  • Eye drops Dexamethasone of 0,1% (ATX S01BA01 code; bottles of 5 and 10 ml).
  • Tablets 0,5 mg (packaging No. 50).
  • Injection solution of 0,4% (ampoule of 1 and 2 ml).

Pharmacological action

Dexamethasone is a hormonal drug with the antiallergic, antiinflammatory, immunodepressive, desensibilizing, anti-toxic, antishock activity. Raises a susceptibility of β-adrenoceptors to endogenous catecholamines.

Eye drops with dexamethasone have antiallergic, anti-exudative and antiinflammatory effect.

Pharmacodynamics and pharmacokinetics

Dexamethasone represents a synthetic corticosteroid (hormone of cortical substance of adrenal glands). In Wikipedia and the reference book Vidal is specified that substance, entering interaction with cytoplasmatic receptors, forms complexes which get into a cellular kernel and stimulate synthesis m-RNK.

m-RNK in turn induces biosynthesis of proteins (including, regulating the vital processes in cells of enzymes) which oppress A2 phospholipase, release of arachidonic acid, biosynthesis of endoperoxides, LT and PG which are mediators of an allergy, an inflammation, pain, etc.

Brakes activity of proteases, collagenases, hyaluronidases, and also release from eosinophils of mediators of an inflammation, promotes:

  • normalization of function of an intercellular matrix of bone and cartilaginous tissue;
  • to decrease in permeability of capillaries;
  • stabilization of membranes (including lizosomalny) cells;
  • to oppression of release of cytokines from macrophages and lymphocytes (gamma interferon and SILT);
  • involution of an adenoid tissue;
  • to acceleration of a catabolism of proteins;
  • to decrease in utilization of glucose;
  • to strengthening of a gluconeogenesis in a liver;
  • to reduction of absorption and increase of removal of Ca;
  • to delay of Na and water;
  • to delay of secretion of joint stock company

After reception per os substance is almost completely soaked up. Bioavailability of drug in the tableted form — to 80%. Cmax and the maximum effect of use are noted in one-two hours. The effect after reception of a single dose remains within 2,75 days.

Linkng with plasma proteins (mainly with albumine) — about 77%.

Substance zhirorastvorimo therefore it is capable to get both in a cell, and into intracellular space. Action is shown in TsNS (a hypophysis, a hypothalamus) that is caused by ability of dexamethasone to contact receptors of cellular membranes.

In peripheral fabrics communicates and works through cytoplasmatic receptors. Dexamethasone in a cell breaks up (in the place of the action). Metabolization occurs mainly in a liver and — partly — in kidneys and other fabrics. The main way of removal — through kidneys.

Indications to use

For what appoint Dexamethasone in pricks and tablets?

Indications to use of Dexamethasone are the illness GKS which are giving in to system treatment (if necessary drug can be used as addition to the main therapy). Intravenously and intramusculary solution is entered in cases when oral administration or topical treatment is inefficient or it is impossible.

The medicine Dexamethasone (pricks and tablets) is shown at rheumatic and allergic diseases, brain hypostasis, shock of various genesis, separate diseases of kidneys, autoimmune frustration, diseases of a respiratory path, blood diseases, an acute heavy dermatosis, VZK, when carrying out ZGT (for example, at insufficiency of adenohypophysis/glands of adrenal glands).

For what appoint Dexamethasone eye drops?

In ophthalmologic practice use of GKS is reasonable at allergic and not purulent conjunctivitis, an iridocyclitis, an iritis, a keratitis, a keratoconjunctivitis without damage of integrity of an epithelium of a cornea, a blefarokonjyunktivita, a sclerite, a blepharitis, an episcleritis, a sympathetic ophthalmia, and also for stopping of an inflammation after an operative measure or an injury of an eye.

From what the drug instillation in an ear is shown?

To the canal of an external ear drug is dug in at inflammatory and allergic diseases of an ear.

Contraindications

The only contraindication for system use by a short course according to vital indications — hypersensitivity to drug components.

Contraindications to Dexamethasone use (in/in, in oil, per os):

  • infectious and parasitic diseases of the bacterial or virus nature;
  • system mycoses;
  • immunodeficiency;
  • the period before preventive vaccination (especially before and after antiviral inoculations);
  • myasthenia, system osteoporosis;
  • gastrointestinal tract diseases (ulcer, colitis, diverticulitis, recently created intestines anastomosis, etc.);
  • diseases of CCC;
  • diabetes mellitus;
  • psychosis;
  • acute liver/renal failure.

Intra joint introduction is forbidden at:

  • instability of joints;
  • pathological bleeding;
  • to the previous arthroplasty;
  • chressustavny changes;
  • existence of the infected centers of damage of joints, intervertebral spaces,
  • circumarticular soft tissues;
  • the osteoporosis expressed circumarticular.

Contraindications to use of drops for eyes:

  • tubercular, fungal, virus infections of eyes;
  • trachoma;
  • glaucoma;
  • epithelial injury of a cornea.

Instillations in acoustical pass are contraindicated at the broken integrity of a tympanic membrane.

Side effects of Dexamethasone

Frequency of emergence and expressiveness of side effects Dexamethasone depend on a dosage of drug, duration of use of drug, a possibility of use taking into account a circadian rhythm.

System side effects of Dexamethasone:

  • from sense bodys and NANOSECOND — a delirium, euphoria, a depressive/maniacal episode, a disorientation, hallucinations, increase of VChD with a syndrome of a congestive disk (noninflammatory hypostasis) of an optic nerve (benign intracranial hypertensia which development is a consequence of fast decrease in a dosage of drug (more often at children) and is followed by deterioration in sight and headaches), vertigo, sleep disorders, a headache, dizzinesses, sight loss (at administration of solution in the field of nasal sinks, the head, a neck, head skin), a cataract with localization of opacification in back part of a crystalline lens, glaucoma, eye hypertensia with probability of damage of an optic nerve, development of a consecutive virus/fungal infection of an eye, a steroid exophthalmos;
  • from CCC — the arterial hypertension, a myocardial dystrophy characteristic of an ECG change hypopotassemia, hypercoagulation, thrombosis, at predisposition — development of HSN, at parenteral use — rushes of blood to the head;
  • from system of digestion — nausea, a hiccups, vomiting, pancreatitis, erosive cankers of the digestive channel, increase/loss of appetite, an erosive esophagitis;
  • metabolic frustration — peripheral hypostases owing to a delay of water and Na+, nitrogenous deficit, a hypocalcemia, a hypopotassemia, a weight set;
  • endocrine disturbances — a syndrome hyper - or a hypocorticoidism, manifestation of the latent (hidden) diabetes mellitus, steroid diabetes, a growth inhibition at children, disturbance of a regularity of menstrual bleedings, a hirsutism;
  • from locomotory system — joint or muscular pain, a dorsodynia, a steroid myopathy, a rupture of sinews, osteoporosis, muscular weakness, decrease in muscle bulk, at intra joint administration of solution increase of intensity of pain in a joint is possible;
  • from an integument — striya, an ecchymoma and petechias, steroid eels, thinning of skin, sweating strengthening, bad healing of wounds;
  • hypersensitivity reactions — the small tortoiseshell, an enanthesis, the complicated breath, a stridor, puffiness of the person, an acute anaphylaxis.

Are also possible: depression of function of immune system, activation of infectious diseases, withdrawal (general weakness, block, nausea, anorexia, abdominal pain).

Local reactions at administration of solution: numbness, burning, paresthesia, pain, an infection in the place of a prick, formation of hems in an injection site of drug, hypo - or hyperpegmentation. At intramuscular introduction process of an atrophy of hypodermic cellulose and skin can begin.

Reactions to use of eye forms: long (more than 3 weeks in a row) use of drops for eyes can be followed by increase of intraocular pressure, forming of glaucoma with defeat of fibers of an optic nerve, a back subkapsulyarny (cup-shaped) cataract, vision disorders (for example, loss of its fields), thinning / perforation of a cornea, distribution of an infection (bacterial or herpetic).

At hypersensitivity to a benzalkoniya to chloride or dexamethasone the blepharitis and conjunctivitis are possible.

Local reactions are shown by burning and an itch of skin, irritation, dermatitis.

Application instruction of Dexamethasone

Dexamethasone pricks: application instruction

Ways of administration of Dexamethasone: in/in, in oil, locally.

The daily dose is equivalent 1/3-01/2 doses for reception of per os and varies ranging from 0,5 to 24 mg. It is necessary to put it on 2 introductions. Treatment is carried out in minimum effective dose and the shortest course. Drug is cancelled gradually. At prolonged use the highest dose — 0,5 mg/days.

Pricks are appointed at medical emergencies, and also in cases when oral administration is impossible. At medical emergencies introduction of higher doses of drug (4-20 mg) is allowed, and the dose is repeated the required therapeutic effect will not be reached yet. The daily dose in rare instances exceeds 80 mg.

On reaching necessary results treatment continue 2-4 mg in a dose, gradually reducing it to full drug withdrawal.

For maintenance of a long-term effect injections with an interval are shown at 3-4 o'clock. Also administration of Dexamethasone in/in method of long drop infusion is allowed.

After end of an acute phase of an illness of the patient transfer to administration of drug inside.

To the same place it is possible to enter no more than 2 ml of means into a muscle.

The scheme of treatment depends on indications:

  • at shock — 2-6 mg/kg in/in bolyusno; repeated introductions — each 2-6 hours or in the form of long infusion using a dose of 3 mg/kg/days. GKS is appointed as addition to the main antishock therapy. Introduction of the specified doses is admissible only at states which threaten the patient's life, and, as a rule, this period lasts till 72 o'clock.
  • At the brain hypostasis (BH) treatment begin with a dose 10 mg (in/in), then — before stopping of symptomatology (during 12-24 h) — in each 6 h enter 4 mg. In 2-4 days the dose is reduced and within 5-7 days stop administration of Dexamethasone. At oncological diseases the maintenance therapy — 2 mg in/in or in oil 2 or 3 rubles/days can be required.
  • At acute OGM the short-term intensive care is necessary for the patient. A load dose of medicine for the adult — 50 mg, for the child weighing up to 35 kg — 20 mg (it is entered into a vein). After that the dose is gradually reduced at simultaneous increase in intervals between administrations of drug.
  • At an allergy (in particular, at an exacerbation of chronic diseases of the allergic nature and at the acute self-limited reactions) parenteral administration is combined with oral administration of drug. Injections from an allergy are given only in the first days, entering the patient into a vein from 4 to 8 mg of Dexamethasone. For 2-3 days 2 times accept on 1 mg drug inside, for 4-5 days — 2 times on 0,5 mg, for 6-7 days — 0,5 mg (once). For the 8th days estimate efficiency of treatment.

At the asthmatic status demanding immediate in/in introductions of GKS the combination "An Euphyllinum and Dexamethasone" quite often is used: GKS reduces an exit of mediators (heparin, a histamine, serotonin) from a cell, protects fabrics from destructive processes, prevents formation of metabolites of arachidonic acid, and the Euphyllinum reduces resistance of blood vessels, removes a bronchospasm, slows down aggregation of thrombocytes and expands coronary vessels.

The instruction on Dexamethasone in ampoules for topical administration

At topical administration of solution into large joints enter from 2 to 4 mg, into small — from 0,8 to 1 mg. Treatment of infiltrates of soft tissues assumes use of 2-6 mg of drug. In nervous a ganglion it is necessary to enter 1-2 mg of medicine, into joint bags — from 2 to 3 mg, into synovial vaginas — from 0,4 to 1 mg. The dose is entered once. The course lasts from 3-5 to 14-20 days.

To children the drug is administered in minimum effective doses.

Use of Dexamethasone in ampoules for inhalations

Inhalation use of Dexamethasone is shown at acute inflammatory respiratory diseases (for example, at bronchitis or laryngitis, and also at a bronkhoobstruktion).

Inhalation with Dexamethasone for children should do to 3 rubles/days, mixing 0,5 ml of drug from 2-3 ml of physical solution. As a rule, treatment is continued by from 3 to 7 days.

It is possible to dissolve drug in physical solution in a proportion 1:6, and then to apply 3-4 ml of ready solution to inhalations.

Dexamethasone tablets: application instruction

The dose for oral administration is selected individually depending on a type of a disease, activity of its current and character of the response of the patient to the appointed treatment.

The average daily dose makes from 0,75 to 9 mg. At hard proceeding diseases the dose can be increased, at the same time it is divided into several receptions. The highest dose — 15 mg/days.

The optimum dosage to children is selected depending on age, and usually makes from 2,5 to 10 mg/sq.m/days. It is necessary to divide it into 3 or 4 receptions.

Duration of a course is defined by nature of pathological process and reaction of an organism of the patient to treatment. In certain cases reception of Dexamethasone is continued within several months.

Liddl's test

Test with Dexamethasone is carried out in the form of small and big tests.

The small test assumes appointment to the patient on 0,5 mg of Dexamethasone 4 times a day at regular intervals (6 h). Urine for definition of free cortisol should be collected from 8:00 and till 8:00 the second day before purpose of drug and in the same time intervals after reception of a necessary dose.

2 mg of Dexamethasone accepted within a day suppress development of corticosteroids almost at each healthy person. The maintenance of cortisol in 6 h after reception of the last 0,5 mg of drug does not exceed 135-138 nmol/l. Decrease in daily removal of free cortisol is lower the 55th nmol, and 17OKC below an indicator of 3 mg/days allows to exclude hyperfunction of cortical substance of adrenal glands.

At a syndrome of a hypercorticoidism of change of secretion of GKS it is not noted.

Carrying out the big test assumes appointment on 2 mg of 1 times in 6 h during 48 h. Decrease in indicators of free cortisol and 17-OKC on 50 (and more) percent allows to diagnose a hypercorticoidism syndrome.

At patients with AKTG-ektopirovannym a syndrome and tumors of adrenal glands indicators of removal of GKS do not change. In some cases at AKTG-ektopirovannom a syndrome they do not change even at reception of 32 mg of Dexamethasone in days.

Eye drops Dexamethasone: application instruction

Drops for eyes are intended for topical administration. At a strong inflammation in the first days two of treatment in a conjunctival sac dig in 1-2 cap. in each 2 h. Further intervals between instillations extend to 4-6 h.

For prevention of development of an inflammation in the first 24 h after an injury or operation to the patient dig in 4 rubles/days on 1-2 drops, further continue treatment in the same dose, but with smaller frequency rate of uses (usually procedure is repeated by 3 rubles/days). The course lasts 14 days.

As an alternative to drops ointment with Dexamethasone can be used. It is squeezed out a 1-1,5-centimeter strip and put for a lower eyelid. Frequency rate of procedures — 2-3 during the day. It is possible to combine use of ointment and drops (for example, drops in the afternoon, and ointment — before going to bed).

For treatment of otitis the drug is administered in acoustical pass of a sore ear 2-3 rubles/days on 3-4 drops.

Overdose

At overdose of solution and tablets side effects which have dozozavisimy character can amplify. The situation demands a drug dose decline. Therapy: symptomatic.

The bottle dropper has such configuration that accidental exceeding of a dose at an instillation of eyes is considered improbable (there is no information on cases of overdose). When exceeding a dose at topical administration excess of medicine is washed away from an eye warm water.

Interaction

Drug is incompatible with other HP as it can form with them insoluble compounds.

Solution for injections it is possible to mix only with solution of glucose 5% and NaCl solution of 0,9%.

Terms of sale

According to the recipe.

The recipe on Latin (sample):
Rp: Sol. Dexamethasoni phosphatis 0,04
D.t.d. N 25 in amp.
S. 1 ml in oil

Storage conditions

To protect from children. Optimum temperature of storage for drops and solution — to 15 °C (it is forbidden to freeze solutions), for tablets — to 25 °C.

Period of validity

2 years. Drops for eyes are suitable for use within 28 days after opening of a bottle.

Special instructions

Dexamethasone in veterinary science

In veterinary science drug is used as active antishock, antiallergenic and anti-inflammatory drug.

For what appoint to cats and dogs Dexamethasone? Drug is used for treatment of depressed cases, injuries, arthritis, a bursitis, allergic diseases, an edema disease, poisonings, a ketosis and acute mastitis.

Therapeutic dose for dogs and for cats — 0,1-1 ml (depending on the sizes of an animal and indications).

Use in bodybuilding

Reception of Dexamethasone provokes metabolism shift towards anabolism that against use even of an insignificant dose of anabolic steroids can accelerate a gain of muscle bulk and make it more considerable.

Besides, suppressing secretion of catabolic hormones, drug promotes endurance increase, accelerates recovery of the athlete after training, suppresses pain and an inflammation at injury of ligaments and joints.

As GKS belong to group of hormones of a stress, their use in sport is allowed only by short-term courses.

Analogs of Dexamethasone

Coincidence on the ATH code of the 4th level:

Analogs of solution and tablets: Dexasonum, Deksametazon-Vial, Deksamed, Megadeksan, Deksametazon-Ferreyn.

Similar drugs for eye drops: Deksametazon-LENS, Deksapos, Ozurdeks, Maksideks, Deksametazonlong.

Drug Maksidez unlike other analogs has 2 dosage forms: drops and oculentum. Ointment with dexamethasone can be replaced with ointment the Hydrocortisone.

What it is better — Prednisolonum or Dexamethasone?

Prednisolonum is a synthetic analog of a hydrocortisone which is considered standard means with an average duration of action and is most often applied in clinical practice.

In comparison with a hydrocortisone its glucocorticoid activity is 4 times higher, however on mineralokortikoidny activity Prednisolonum concedes to a hydrocortisone.

Dexamethasone is GKS of long action. Unlike analog, drug is fluorinated. Glucocorticoid activity of drug is 7 times higher to what Prednisolonum. At the same time it has no mineralokortikoidny effect.

More than other GKS, oppression gipotalamo - a pituitary and adrenal axis provokes, causes the expressed disturbances of calcic, lipidic and carbohydrate metabolism, has psychogogic effect in this connection it is not recommended for prolonged use.

Zdravzona

  • Dexamethasone 4mgml solution for injections of 1 ml No. 25 ampoule/KRKA/KRKA
  • No. 50 dexamethasone 0,5mg tabletkiakrikhin HFK of joint stock company
  • Oftan-deksametazon 0,1% of a drop eye 5 ml bottle-kapelnitsasanten Oy (Finland)
  • Dexamethasone of 0,1% 10 ml gl.suspenziya
  • Deksametazon-Lens 0,1% of a drop eye 10 ml flakon-kapelnitsalens-Farm Ltd company

Drugstore of IFC

  • Dexamethasone tbl 500 mkg No. 10, Krkasloveniya
  • Dexamethasone solution for in 4mg/ml 1 ml No. 25, Krkasloveniya
  • Oftan Deksametazon of a hl drop. 0.1% of 5 ml, Santenfinlyandiya
  • Dexamethasone kap.gl. 0.1% fl 10 ml, Farmak (Kiev) Ukraine
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Apteka24

  • Deksametazonvarshavsky Federal Law (Poland)
  • Deksametazonoz GNTSLS (Ukraine, Kharkiv)
  • Deksametazonvarshavsky Federal Law (Poland)
  • Deksametazonkrka (Slovenia)
  • Deksametazonkrka (Slovenia)

Paniapteka

  • Dexamethasone of hot-smoked 0.1% 10mldarnitsa
  • Dexamethasone of hot-smoked 0.1% 10mldarnitsa
  • Dexamethasone of hot-smoked 0.1% 10mldarnitsa
  • Dexamethasone of hot-smoked 0.1% 10mldarnitsa
  • Dexamethasone of hot-smoked 0.1% 10mldarnitsa

BIOSPHERE

  • Dexamethasone of 0,1% 10 ml of a drop glazn. Romfarm of the Neuter Company. L. (Romania)
  • Dexamethasone of 0,5 mg No. 10 of table.
  • Oftan-Deksametazon 0,1% 5 ml of a drop glazn.santen (Finland)
  • Dexamethasone of 0,1% 10 ml of a drop glazn. Farmak (Ukraine)
  • Dexamethasone of 0,1% 5 ml susp.glazn. Warsaw pharmaceutical plant of Polf AO (Poland)
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Section: For eyes
PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Dexamethasone surely consult with the attending physician.