Betamethasone - instructions for use, dose, side effects, contraindications

Betamethasone is a glucocorticosteroid. 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 A₂, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses release cyclooxygenases (mainly cyclooxygenases-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.

Betamethasone suppresses pituitary release adrenocorticotropic hormone and β-lipotropin, but does not reduce the level of circulating β-endorphin. Oppressing secretion thyrotropic hormone and follicle-stimulating hormone.

With direct application on the vessels has a vasoconstrictor effect.

Betamethasone 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 and increases the activity of gluconeogenesis enzymes. In the liver betamethasone 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.

Betamethasone suppresses the capture of glucose by fat cells, which leads to activation of lipolysis. However, due to an increase in the secretion of insulin, lipogenesis stimulates, which contributes to the accumulation of fat.

It detains sodium ions and water in the body, stimulates the excretion of potassium ions, reduces absorption of calcium from the digestive tract, cleans calcium ions from the bones, increases the excretion of calcium by the kidneys.

Has catabolic effect in lymphoid and connective tissue, muscles, fatty tissue, skin, bone tissue. Osteoporosis and Itenko-Cushing syndrome are the main factors limiting long-term therapy with glucocorticosteroids. As a result of catabolic action, growth can be suppressed in children.

In high doses betamethasone 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 leads to the development of peptic ulcers.

In systemic application, the therapeutic activity of betamethasone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

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

For anti-inflammatory activity hydrocortisone 30 times, does not have mineralocorticoid activity. The presence of fluorine in the molecule enhances the anti-inflammatory activity of betamethasone.

Betamethasone in the form of dipropionate is characterized by a prolonged action.

Pharmacokinetics:

Binding to plasma proteins is about 64%, V_d - 84 liters. Metabolised in the liver. Metabolites are excreted mainly by the kidneys, a small part - with bile.

When absorbed through the skin betamethasone characterized by similar pharmacokinetic properties, both with external and with systemic application. Systemic absorption after external application is 12-14%.

For local and external use with intact skin, absorption may be negligible.The presence of an inflammatory process, as well as the use of an occlusive dressing, can increase the amount of absorption.

Indications:

For oral administration: primary or secondary insufficiency of adrenal function, congenital adrenal hyperplasia, acute (nasal) and subacute thyroiditis, hypercalcemia due to tumor disease, rheumatic diseases, collagen diseases, allergic diseases, symptomatic sarcoidosis, Leffler's syndrome, berylliosis, idiopathic or secondary thrombocytopenia in adults, autoimmune hemolytic anemia, erythroblastopenia (erythrocyte anemia), erythroid hypoplastic anemia, transfusion reactions, palliacy vnaya therapy of leukemia and lymphomas in adults and acute leukemia in children; ulcerative colitis, Bell's paralysis.

For parenteral use: shock (including burn, traumatic, operating, toxic, cardiogenic, blood transfusion, anaphylactic); allergic reactions (acute, severe forms), anaphylactoid reactions; cerebral edema (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma),increased intracranial pressure; bronchial asthma (severe form), asthmatic status; systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis); acute adrenal insufficiency, prevention of insufficiency of the adrenal cortex in patients who received glucocorticosteroids for a long time; thyrotoxic crisis; acute hepatitis, hepatic coma; poisoning with burning liquids; cereals in diphtheria (in combination with appropriate antimicrobial therapy).

For intraarticular administration: Rheumatoid arthritis, osteoarthritis, traumatic arthritis, osteochondritis, acute gouty arthritis. Diseases of soft tissues (including bursitis, fibrositis, tendonitis, tendosinovitis, myositis).

For external use: dermatitis, various types of eczema (including atopic, pediatric, numular), gnawing pruritus of Gaida, simple dermatitis, exfoliative dermatitis, neurodermatitis, sun dermatitis, seborrheic dermatitis, radiation dermatitis, diaper rash, psoriasis (except for extensive plaque psoriasis)cutaneous or anogenital (excluding candidomycosis) itching, discoid lupus erythematosus, as an aid in the complex therapy of generalized erythroderma.

For topical application: diseases of the eye and ear with a pronounced allergic or inflammatory component.

ICD-10

I.A30-A49.A36 Diphtheria

I.B15-B19.B17.1 Acute hepatitis C

I.B15-B19.B16 Acute hepatitis B

III.D55-D59.D59 Acquired hemolytic anemia

III.D60-D64.D60 Acquired pure red cell aplasia (erythroblastopenia)

III.D65-D69.D69.3 Idiopathic thrombocytopenic purpura

III.D80-D89.D86 Sarcoidosis

IV.E00-E07.E06 Thyroiditis

IV.E20-E35.E25 Adrenogenital disorders

IV.E20-E35.E27.1 Primary insufficiency of the adrenal cortex

IV.E20-E35.E27.2 Addison's Crisis

IV.E20-E35.E27.4 Other and unspecified adrenocortical insufficiency

VI.G50-G59.G51.0 Bell's paralysis

VI.G90-G99.G93.2 Benign intracranial hypertension

VI.G90-G99.G93.6 Edema of the brain

VII.H10-H13.H10.1 Acute atopic conjunctivitis

X.J40-J47.J45 Asthma

X.J40-J47.J46 Asthmatic status [status asthmaticus]

X.J60-J70.J63.2 Berylliosis

X.J80-J84.J82 Pulmonary eosinophilia, not elsewhere classified

XI.K50-K52.K51 Ulcerative colitis

XI.K70-K77.K72 Hepatic failure, not elsewhere classified

XII.L20-L30.L20.8 Other atopic dermatitis

XII.L20-L30.L21 Seborrheic dermatitis

XII.L20-L30.L22 Diaper dermatitis

XII.L20-L30.L23 Allergic contact dermatitis

XII.L20-L30.L24 Simple irritant contact dermatitis

XII.L20-L30.L26 Exfoliative dermatitis

XII.L20-L30.L28.0 Simple chronic lichen

XII.L20-L30.L28.1 Scabby nodosum

XII.L20-L30.L29 Itching

XII.L20-L30.L29.3 Anogenital itching, unspecified

XII.L20-L30.L30.0 Coin-like eczema

XII.L20-L30.L30.4 Erythematous intermittence

XII.L40-L45.L40 Psoriasis

XII.L55-L59.L56.2 Photocontact dermatitis [berloque dermatitis]

XII.L55-L59.L58 Radiation dermatitis radiation

XII.L80-L99.L93.0 Discoid lupus erythematosus

XIII.M05-M14.M05 Seropositive rheumatoid arthritis

XIII.M05-M14.M10 Gout

XIII.M15-M19.M15 Polyarthrosis

XIII.M30-M36.M30 Nodular polyarteritis and related conditions

XIII.M30-M36.M32 Systemic lupus erythematosus

XIII.M30-M36.M33 Dermatopolymiositis

XIII.M30-M36.M34 Systemic sclerosis

XIII.M60-M63.M60 Myositis

XIII.M65-M68.M65 Synovitis and tenosynovitis

XIII.M70-M79.M70 Diseases of soft tissues associated with exercise, overload and pressure

XIII.M70-M79.M71 Other bursopathies

XVIII.R50-R69.R57.0 Cardiogenic shock

XVIII.R50-R69.R57.1 Hypovolemic shock

XVIII.R50-R69.R57.8 Other types of shock

XIX.T66-T78.T78.2 Anaphylactic shock, unspecified

XIX.T66-T78.T78.3 Angioedema

XIX.T79.T79.4 Traumatic shock

XIX.T80-T88.T80.6 Other serum reactions

XXI.Z40-Z54.Z51.5 Palliative Care

Contraindications:

For short-term use - Hypersensitivity to betamethasone.

For intraarticular administration and administration directly to the lesion: pre-arthroplasty, abnormal bleeding (endogenous or caused by 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-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 space, ankylosis), unstable joint nost as a result of arthritis, aseptic necrosis of the bones forming the joint epiphysis.

For external use: pink acne, blackheads and ordinary (youthful) acne; primary viral skin infections (including chicken pox).

Carefully:

Use with caution in case of 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), chicken pox, 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.

Use with caution for 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, in immunodeficient conditions (including AIDS or HIV infection).

Be wary of in diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis, with the threat of perforation or abscess, diverticulitis.

With caution apply to diseases of the cardiovascular system, including after a recent myocardial infarction (in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, 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 (including tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, b Izyzenko-Cushing's disease,with severe chronic renal and / or hepatic insufficiency, nephrourolythiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV degree), in poliomyelitis (except for the form of bulbar encephalitis), openly - and zakratougolnoy glaucoma, pregnancy, lactation.

Pregnancy and lactation:

Application in pregnancy is possible in exceptional cases on strict indications.

If it is necessary to use lactation, breastfeeding should be discontinued.

Dosing and Administration:

The dose is set individually.

At intake the daily dose for adults makes 0,25-8 mg, for children - 17-250 mkg / kg. After long-term use, the abolition of betamethasone should be carried out gradually, reducing the dose by 250 micrograms every 2-3 days.

For intravenous administration (struino slowly or drip), a single dose is 4-8 mg, if necessary, an increase of up to 20 mg is possible; the maintenance dose is usually 2-4 mg. A single dose for intramuscular injection is 4-6 mg.

For intraarticular administration and administration directly to the lesion in soft tissue diseases,depending on the size of the joint and the size of the affected area, the single dose is 0.4-6 mg.

Subconjunctivalally single dose - 2 mg.

For external application, apply a thin layer on the affected area of the skin 2-6 times a day before clinical improvement, then apply 1-2 times a day. When using betamethasone in children, as well as in patients with facial lesions, the course of treatment should not exceed 5 days.

Side effects:

From the endocrine system: impaired glucose tolerance, steroid diabetes, or manifestation of latent diabetes mellitus, adrenal suppression, Cushing's syndrome (including moon face, obesity, pituitary type, hirsutism, hypertension, dysmenorrhea, amenorrhea, myasthenia gravis, striae), sexual delay development in children.

From the side of metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, fluid retention and sodium ions (peripheral edema), hypernatremia, hypokalemic syndrome (including hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

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.

From 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. In rare cases, an increase in the activity of hepatic transaminases and alkaline phosphatase.

From the sense organs: sudden loss of vision (with parenteral administration in the head, neck, nasal concha, scalp may precipitate crystals of the drug in the vessels of the eye), posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral infections eye, trophic changes of the cornea, exophthalmos.

From the musculoskeletal system: slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of the tendons of muscles, steroid myopathy, decrease in muscle mass (atrophy); with intra-articular injection - increased pain in the joint.

Dermatological reactions: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, steroid acne, striae, propensity to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

Local reactions: when parenteral introduction - burning, numbness, pain, paresthesia and infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; when intramuscular introduction (especially in the deltoid muscle) - atrophy of the skin and subcutaneous tissue.

Other: development or exacerbation of infections (the appearance of this side effect is promoted by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

With intravenous administration - arrhythmias, "tides" of blood to the face, convulsions.

For external use: rarely - itching, flushing, 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 glucocorticosteroids.

Overdose:

Nausea, vomiting, sleep disorders, euphoria, agitation, depression. With prolonged use in high doses - osteoporosis, fluid retention in the body, increased blood pressure and other signs of hypercorticism, including Itenko-Cushing syndrome, secondary adrenal insufficiency.

Treatment: Against the background of a gradual discontinuation of the drug maintenance of vital functions, correction of electrolyte balance, antacids, phenothiazines, preparations of Li⁺; with the syndrome of Itenko-Cushing - aminoglutethimide.

Interaction:

With simultaneous use with cardiac glycosides, their action is enhanced; with diuretics - the excretion of potassium increases; with hypoglycemic drugs, oral anticoagulants - weakening of their action; with non-steroidal anti-inflammatory drugs - the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

Special instructions:

If necessary, intraarticular administration should be used with caution in patients with a general severe condition, inefficiency (or short-term) of the action of the two previous administrations (taking into account the individual properties of the glucocorticosteroids used).

When ingestion it is necessary to monitor blood glucose level, blood pressure, water-electrolyte balance. In case of irritation or the appearance of symptoms of hypersensitivity to betamethasone treatment should be stopped and appropriate therapy should be carried out.When secondary infection is attached, appropriate antimicrobial agents are treated.

Not indicated for the treatment of hyaline membranes of newborns.

Do not use topically to treat primary skin lesions in fungal (eg, candidiasis, trichophytosis) and bacterial (eg, impetigo) infection, perianal and anogenital itching.

Instructions

Betamethasone (Betamethasonum)