Дипроспан®

General characteristics. Structure:

Active ingredient: 2,63 mg of betamethasone of sodium of phosphate (that corresponds to 2 mg of betamethasone), 6,43 mg of betamethasone of Dipropionas (that corresponds to 5 mg of betamethasone).

Excipients: hydrophosphate sodium a dihydrate, sodium chloride, dinatrium эдетат, polysorbate 80 (polyoxyethylene sorbitanmonooleate), benzyl alcohol, methylparahydroxybenzoate, пропилпарагидроксибензоат, a karmelloza of sodium, a macrogoal (polyethyleneglycol), Acidum hydrochloricum, water for injections.

Pharmacological properties:

Pharmacodynamics. GKS. Has high glucocorticoid and insignificant mineralokortikoidny activity. Drug has an antiinflammatory, antiallergic and immunodepressive effect, and also has the expressed and various effect on different types of a metabolism.

Pharmacokinetics. Absorption and distribution. Sodium betamethasone we will well dissolve phosphate and after introduction in oil quickly is exposed to hydrolysis and practically at once it is absorbed from an injection site that provides quick start of therapeutic action. It is almost completely removed within one day after introduction.

Betamethasone Dipropionas is slowly absorbed from depot, metabolized gradually that causes long effect of drug, and removed during more than 10 days.

Linkng of a betamatezon with proteins of plasma makes 62,5%.

Metabolism and removal. It is metabolized in a liver with formation of generally inactive metabolites. It is removed preferential by kidneys.

Indications to use:

Treatment of states and diseases at which therapy of GKS allows to reach adequate clinical effect (it is necessary to consider that at some diseases therapy of GKS is additional and does not replace standard therapy):

— diseases of a musculoskeletal system and soft tissues, including pseudorheumatism, osteoarthrosis, bursitis, ankylosing spondylarthritis, epicondylitis, radiculitis, coccyalgia, ischialgia, lumbago, wryneck, ganglionic cyst, exostosis, fasciitis, diseases of feet;

— allergic diseases, including bronchial asthma, hay fever (pollinosis), allergic bronchitis, seasonal or year-round rhinitis, medicinal allergy, serum disease, reactions to stings of insects;

— dermatological diseases, including atopic dermatitis, monetovidny eczema, neurodermatitises, contact dermatitis, the expressed photodermatitis, a small tortoiseshell, red flat deprive, an insulin lipodystrophy, a gnezdny alopecia, a diskoidny lupus erythematosus, psoriasis, keloid cicatrixes, an ordinary pemphigus, herpetic dermatitis, cystous eels;

— general diseases of connecting fabric, including a system lupus erythematosus, a scleroderma, a dermatomyositis, a nodular periarteritis;

— hemoblastoses (palliative therapy of a leukosis and lymphoma at adults, an acute leukosis at children);

— primary or secondary insufficiency of bark of adrenal glands (at obligatory simultaneous use of mineralokortikoid);

— other diseases and morbid conditions demanding therapy by system GKS (an adrenogenital syndrome, ulcer colitis, a regional ileitis, a sprue, defeats mucous eyes in need of administration of drug in a conjunctival sac, pathological changes of blood in need of use GKS, nephrite, a nephrotic syndrome).

Route of administration and doses:

Дипроспан® it is applied for in oil, intra joint, circumarticular, intrabursalny, intradermal, interstitial and intra focal introduction.

The insignificant sizes of crystals of betamethasone of Dipropionas allow to apply needles of small diameter (up to the 26th caliber) to intradermal introduction and introduction directly to the defeat center.

Drug is not intended for in/in and п / to introduction.

Injections of the drug Diprospan® should be carried out at strict observance of rules of an asepsis.

The mode of dosing and way of introduction establish individually, depending on indications, disease severity and reaction of the patient.

At system use the initial dose of the drug Diprospan® in most cases makes 1-2 ml. Introduction is repeated as required, depending on a condition of the patient.

Introduction in oil. Дипроспан® it is necessary to enter deeply in oil, choosing at the same time large muscles and avoiding hit in other fabrics (for prevention of an atrophy of fabrics).

At the serious conditions demanding emergency treatment, the initial dose makes 2 ml.

At various dermatological diseases, as a rule, there is enough introduction of 1 ml of suspension of Diprospan.

At diseases of respiratory system the beginning of effect of drug comes within several hours after an injection of suspension in oil. At bronchial asthma, hay fever, an allergic bronchitis and allergic rhinitis significant improvement of a state is reached after introduction of 1-2 ml of Diprospan.

At an acute and chronic bursitis the initial dose for introduction in oil makes 1-2 ml of suspension. If necessary carry out several repeated injections.

If the satisfactory clinical answer does not come through a certain period, Diprospan® should cancel and appoint other therapy.

Local introduction. At local introduction simultaneous use mestnoanesteziruyushchego drug is necessary only in rare instances. If it is required, then the solutions of Procainum of a hydrochloride or lidocaine which are not containing methylparaben, propylparaben, phenol and other similar substances apply 1% or 2%. At the same time mixing is made in the syringe, at first gathering in the syringe from a bottle a required dose of suspension of the drug Diprospan®. Then in the same syringe gain required amount of local anesthetic from an ampoule and stir up within a short period of time.

At an acute bursitis (subdeltoid, infrascapular, elbow and prepatellar) introduction of 1-2 ml of suspension to a synovial bag relieves pain and recovers mobility of a joint within several hours. After stopping of an aggravation at a chronic bursitis apply smaller doses of drug.

At acute tendosinovita, tendinites and peritendinites one injection of the drug Diprospan® improves a condition of the patient; at chronic - the injection is repeated depending on reaction of the patient. It is necessary to avoid administration of drug directly in a sinew.

Intra joint administration of the drug Diprospan® in a dose of 0.5-2 ml kills pain, restriction of mobility of joints at a pseudorheumatism and an osteoarthrosis during 2-4 h after introduction. Duration of therapeutic action considerably varies and can make 4 and more weeks.

The recommended drug doses at introduction to large joints make from 1 to 2 ml; in average joints - 0.5-1 ml; in small joints - 0.25-0.5 ml.

At some dermatological diseases effectively intradermal administration of the drug Diprospan® directly in the defeat center, the dose makes 0.2 ml/cm2. The center is evenly cut away, using the tuberkulinovy syringe and a needle with a diameter about 0.9 mm. Total quantity of the administered drug on all sites should not exceed 1 ml within 1 week. It is recommended to use the tuberkulinovy syringe with a needle of the 26th caliber to introduction to the center of defeat.

The recommended single doses of drug (at an interval between introductions of 1 week) at a bursitis: at callosity of 0.25-0.5 ml (as a rule, 2 injections are effective), at a spur - 0.5 ml, at restriction of mobility of a thumb of foot – 0.5 ml, at a synovial cyst – 0.25-0.5 ml, at a tendosinovita – 0.5 ml, at acute gouty arthritis - 0.5-1 ml. The tuberkulinovy syringe with a needle of the 25th caliber is suitable for the majority of injections.

After achievement of therapeutic effect the maintenance dose is selected by a gradual dose decline of the drug Diprospan® which is carried out bucketed. Decrease is continued before achievement of a minimal effective dose.

At emergence or threat of emergence of the stressful situation (which is not connected with a disease) increase in a dose of the drug Diprospan® can be required.

Drug withdrawal after long therapy is carried out by a gradual dose decline.

Observation of a condition of the patient is carried out, at least, within a year upon termination of long therapy or use in high doses.

Features of use:

Use at pregnancy and feeding by a breast. Due to the lack of controlled researches of safety of use of the drug Diprospan® at pregnancy, in case of need purposes of drug pregnant women or women of childbearing age need preliminary estimate of estimated advantage of therapy for mother and potential risk for a fruit.

Newborns whose mothers received therapeutic doses of GKS at pregnancy have to be under medical control (for early identification of signs of adrenal insufficiency).

In need of purpose of the drug Diprospan® in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination, in view of importance of therapy for mother (because of possible side effects at children).

Use at abnormal liver functions. To apply with care at a heavy chronic liver failure, cirrhosis.

Use at renal failures. To apply with care at a heavy chronic renal failure.

Use for children. Children at whom therapy is carried out by the drug Diprospan® (especially long) have to be under careful medical observation regarding possible lag in growth and development of secondary insufficiency of bark of adrenal glands.

Special instructions. The mode of dosing and a way of introduction establish individually, depending on indications, disease severity and reaction of the patient.

Drug should be used in a minimal effective dose, the period of use has to be as it is possible well.

The initial dose is selected until the necessary therapeutic effect is reached. If after a sufficient period the therapeutic effect is not observed, make drug withdrawal by a gradual dose decline of drug. Дипроспан® also select other corresponding method of treatment.

After achievement of therapeutic effect the maintenance dose is selected by a gradual dose decline of betamethasone which is entered through the corresponding intervals of time. Decrease is continued before achievement of a minimal effective dose.

At emergence or threat of emergence of the stressful situation (which is not connected with a disease) there can be a need for increase in a dose of Diprospan.

Drug withdrawal after long therapy is carried out by a gradual dose decline.

Observation of a condition of the patient is carried out, at least, within a year upon termination of long therapy or use in high doses.

Administration of drug in soft tissues, in the center of defeat and in a joint can lead at the same time at the expressed local action to systemic action.

Considering probability of development of anaphylactoid reactions at parenteral administration of GKS, it is necessary to take necessary precautionary measures before administration of drug, especially in the presence of instructions in the anamnesis on allergic reactions to medicines.

Дипроспан® contains two active agents - compounds of betamethasone, one of which, sodium betamethasone phosphate, is instant fraction, and therefore quickly gets into a system blood stream. It is necessary to consider possible systemic action of drug.

Against the background of use of the drug Diprospan® disturbances of mentality, especially at patients with emotional instability or tendency to psychoses are possible.

At Diprospan's appointment a sick diabetes mellitus correction of hypoglycemic therapy can be required.

The patients receiving Diprospan® in the doses suppressing immunity should be warned about need to avoid contact with patients with chicken pox and measles (it is especially important at purpose of drug to children).

At use of the drug Diprospan® it is necessary to consider that GKS are capable to mask symptoms of an infectious disease, and also to reduce body resistance to infections.

Diprospan's appointment at active tuberculosis is possible only in cases of the fulminant or disseminated tuberculosis in combination with adequate antitubercular therapy. At Diprospan's appointment patients with latent tuberculosis or with positive reaction to tuberculine should resolve an issue of preventive antitubercular therapy. At preventive use of Rifampinum it is necessary to consider increase in hepatic clearance of betamethasone (dose adjustment can be required).

In the presence of liquid in a joint cavity it is necessary to exclude septic process.

Noticeable strengthening of morbidity, puffiness, temperature increase of surrounding fabrics and further restriction of mobility of a joint testify to infectious arthritis. At confirmation of the diagnosis it is necessary to appoint antibacterial therapy.

Repeated injections in a joint at an osteoarthrosis can increase risk of destruction of a joint. Introduction of GKS to sinew tissue gradually leads to a rupture of a sinew.

After successful therapy by intra joint injections of the drug Diprospan® the patient should avoid joint overloads.

Prolonged use of GKS can lead to a back subkapsulyarny cataract (especially at children), glaucoma with possible damage of an optic nerve and can promote development of a consecutive eye infection (fungal or virus).

It is necessary to conduct periodically ophthalmologic examination, especially at the patients receiving Diprospan® more than 6 months.

At increase in the ABP, a delay of liquid and sodium of chloride in fabrics and increase in removal of potassium from an organism (less probable, than at use of other GKS) recommend to patients a diet with restriction of table salt and in addition appoint kaliysoderzhashchy drugs. In total GKS strengthen calcium removal.

At the simultaneous use of Diprospan and cardiac glycosides or drugs influencing electrolytic composition of plasma control of water and electrolytic balance is required.

With care appoint acetylsalicylic acid in a combination with the drug Diprospan® at a prothrombinopenia.

Development of secondary insufficiency of bark of adrenal glands in connection with too bystry cancellation of GKS is possible within several months after the end of therapy. At emergence or threat of a stressful situation during this period therapy by the drug Diprospan® should be resumed and at the same time to appoint mineralokortikoidny drug (because of possible disturbance of secretion of mineralokortikoid). Gradual cancellation of GKS allows to reduce risk of development of secondary adrenal insufficiency.

Against the background of use of GKS change of mobility and number of spermatozoa is possible.

At long therapy of GKS it is reasonable to consider the possibility of transition with parenteral to peroral GKS, taking into account ratio assessment advantage/risk.

The patients receiving GKS should not be vaccinated against smallpox, and also to carry out other immunization, especially against the background of treatment of GKS in high doses, in view of a possibility of development of neurologic complications and a low response immune response (lack of antibody formation). Carrying out immunization is possible when performing replacement therapy (for example, at primary insufficiency of bark of adrenal glands).

Use in pediatrics. Children at whom therapy is carried out by the drug Diprospan® (especially long) have to be under careful medical observation regarding possible lag in growth and development of secondary insufficiency of bark of adrenal glands.

Side effects:

From a metabolism: a hypernatremia, increase in release of potassium, increase in removal of calcium, a gipokaliyemichesky alkalosis, a liquid delay in fabrics, negative nitric balance (because of a protein catabolism), липоматоз (including mediastinal and epidural липоматоз which can cause neurologic complications), increase in body weight.

From cardiovascular system: chronic heart failure (at predisposed patients), increase in the ABP.

From a musculoskeletal system: muscular weakness, a steroid myopathy, loss of muscle bulk, strengthening of myasthenic symptoms at a heavy pseudoparalytic myasthenia, osteoporosis, compression spinal fracture, an aseptic necrosis of a head of a femoral or humeral bone, pathological fractures of tubular bones, ruptures of sinews, instability of joints (at repeated intra joint introductions).

From the alimentary system: GIT erosive cankers with possible subsequent perforation and bleeding, pancreatitis, a meteorism, a hiccups.

Dermatological reactions: disturbance of healing of wounds, an atrophy and thinning of skin, a petechia, ecchymomas, the increased perspiration, dermatitis, steroid eels, striya, tendency to development of a pyoderma and candidiasis, decrease in reaction when carrying out skin tests.

From TsNS and peripheral nervous system: spasms, increase in intracranial pressure with a papilledema (is more often upon termination of therapy) dizziness, a headache, euphoria, changes of mood, a depression (with the expressed psychotic reactions), personal frustration, an acrimony, sleeplessness.

From endocrine system: disturbance of a menstrual cycle, secondary adrenal insufficiency (especially in the period of a stress at a disease, an injury, surgical intervention), an Icenco-Cushing syndrome, decrease in carbohydrate tolerance, a steroid diabetes mellitus or manifestation of a latent diabetes mellitus, increase in need for insulin or peroral hypoglycemic drugs, disturbance of pre-natal development, a growth inhibition and sexual development at children.

From an organ of sight: back subkapsulyarny cataract, increase in intraocular pressure, glaucoma, exophthalmos; in rare instances - a blindness (at administration of drug in a face and the head).

Allergic reactions: anaphylactic reactions, shock, Quincke's disease, arterial hypotension.

Local reactions: seldom - hyper - or hypopigmentation, a hypodermic and skin atrophy, aseptic abscesses.

Others: rush of blood to the person after an injection (or intra joint introduction), a neurogenic arthropathy.

Frequency of development and expressiveness of side effects as at use and other GKS, depend on the size of the applied dose and duration of use of drug. These phenomena are usually reversible and can be eliminated or reduced at a dose decline.

Interaction with other medicines:

At co-administration of the drug Diprospan® with phenobarbital, Rifampinum, Phenytoinum or ephedrine acceleration of metabolism of betamethasone at decrease in its therapeutic activity is possible.

At combined use of the drug Diprospan® and indirect anticoagulants the changes of coagulability of blood demanding dose adjustment are possible.

At combined use of the drug Diprospan® and kaliyvyvodyashchy diuretics the probability of development of a hypopotassemia increases.

Дипроспан® can strengthen the potassium removal caused by Amphotericinum of Century.

At simultaneous use of GKS and estrogen dose adjustment of drugs can be required (because of danger of their overdose).

Simultaneous use of GKS and cardiac glycosides increases risk of developing of arrhythmia or digitalis intoxication (because of a hypopotassemia).

At the combined use of GKS with NPVS, with ethanol or etanolsoderzhashchy drugs increase in frequency of emergence or intensity of erosive cankers of a GIT is possible.

At combined use of GKS can reduce concentration of salicylates in a blood plasma.

Simultaneous introduction of GKS and Somatotropinum can lead to delay of absorption of the last (it is necessary to avoid administration of betamethasone in the doses exceeding 0.3-0.45 mg/sq.m of a surface of bodies/days).

GKS can influence the nitric blue tetrazolevy test for a bacterial infection and cause false-negative result.

Contraindications:

— system mycoses;

— in/in or п / to introduction;

— for intra joint introduction: unstable joint, infectious arthritis;

— introduction to the infected surfaces and to intervertebral space;

— children's age up to 3 years (existence in composition of benzyl alcohol);

— hypersensitivity to drug components;

— hypersensitivity to other GKS.

With care. Parasitic and infectious diseases of the virus, fungal or bacterial nature (now or recently postponed, including recent contact with the patient) - the herpes simplex surrounding herpes (a viremichesky phase), chicken pox, measles; the amebiasis, a strongyloidosis (established or suspected); system mycosis; active and latent tuberculosis. Use at serious infectious diseases is admissible only against the background of specific therapy.

The postvaccinal period (the period lasting 8 weeks to and 2 weeks after vaccination), lymphadenitis after BTsZh inoculation. Immunodeficiency (including AIDS or HIV infection).

Gastrointestinal diseases: a peptic ulcer of a stomach and duodenum, an esophagitis, gastritis, an acute or latent round ulcer, recently created intestines anastomosis, ulcer colitis with threat of perforation or abscessing, a diverticulitis, abscess or other purulent infections.

Diseases of cardiovascular system, including recently postponed myocardial infarction (at patients with an acute and subacute myocardial infarction distribution of the center of a necrosis, delay of formation of cicatricial fabric and thereof a rupture of a cardiac muscle), dekompensirovanny chronic heart failure, arterial hypertension, a lipidemia is possible).

Endocrine diseases - a diabetes mellitus (including disturbance of tolerance to carbohydrates), a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease.

Heavy chronic renal and/or liver failure, нефроуролитиаз, cirrhosis.

Werlhof's disease (introduction in oil).

The hypoalbuminemia and states contributing to its emergence.

System osteoporosis, myasthenia, acute psychosis, obesity of the III-IV degree, poliomyelitis (except for a form of bulbar encephalitis), open and closed-angle glaucoma, diseases of eyes caused by Herpes simplex (because of risk of perforation of a cornea), pregnancy, the lactation period.

For intra joint introduction: the general serious condition of the patient, inefficiency (or short duration) actions of 2 previous introductions (taking into account individual properties of the applied GKS).

Overdose:

Symptoms: the acute overdose of betamethasone does not lead to life-threatening situations. Introduction within several days of GKS in high doses does not lead to undesirable effects, except for cases of use of very high doses or at use at a diabetes mellitus, glaucoma, an aggravation of erosive cankers of a GIT or at simultaneous use of drugs of a digitalis, indirect anticoagulants or kaliyvyvodyashchy diuretics.

Treatment: careful medical control of a condition of the patient is required. It is necessary to support optimum consumption of liquid and to control the content of electrolytes in plasma and in urine, especially a ratio of ions of sodium and potassium. If necessary it is necessary to carry out the corresponding therapy.

Storage conditions:

Drug should be stored in the unavailable to children, protected from light place at a temperature not above 25 °C; not to freeze. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

1 ml - ampoules glass (1) - planimetric strip packagings plastic (1) - packs cardboard.
1 ml - ampoules glass (5) - planimetric strip packagings plastic (1) - packs cardboard.