Diprospan

General characteristics. Structure:

Active agent: betamethasone Dipropionas (in an equivalent of 5 mg of betamethasone), sodium betamethasone phosphate (in an equivalent of 2 mg of betamethasone).

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

Pharmacological properties:

Pharmacodynamics. Diprospan - glucocorticosteroid (GKS) drug, 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. Sodium betamethasone we will well dissolve phosphate and after intramuscular introduction 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.
Betamatezon well contacts proteins of plasma (62,5%). It is metabolized in a liver with formation of preferential inactive metabolites. It is removed preferential by kidneys.

Indications to use:

Treatment at adulthoods and diseases at which GKS therapy allows to achieve necessary clinical effect (it is necessary to consider that at some diseases of GKS therapy 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 atonic 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 system GKS of therapy (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:

Intramuscular, intra joint, circumarticular, intrabursalny intradermal, interstitial and intra focal injections.
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
NOT TO ENTER INTRAVENOUSLY! NOT TO ENTER SUBCUTANEOUSLY
Strict observance of rules of an asepsis is obligatory at Diprospan's use.
The mode of dosing and way of introduction establish individually, depending on indications, disease severity and reaction of the patient.
At system therapy the initial dose of Diprospan in most cases makes 1-2 ml. Introduction is repeated as required, depending on a condition of the patient.
Intramuscular introduction (in oil) GKS should be carried out deeply in a muscle, choosing at the same time large muscles and avoiding hit in other fabrics (for prevention of an atrophy of fabrics).
The drug is administered by in oil:

- at the serious conditions demanding acceptance of emergency measures; 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 12 ml of suspension. If necessary carry out several repeated injections.
If the satisfactory clinical answer does not come through a certain period, Diprospan it is necessary to cancel and appoint other therapy. At local introduction simultaneous use of mestnoanesteziruyushchy drug is necessary only in rare instances. If it is desirable, then the solutions of Procainum of a hydrochloride or lidocaine which are not containing methylparaben, propylparaben, phenol and other similar substances use 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 Diprospan. Then in the same syringe take away required amount of local anesthetic from an ampoule and stir up during a short span.
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 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 introduction of 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 averages - 0,5-1 ml; in small - 0,25-0,5 ml.
At some dermatological diseases effectively intradermal introduction of 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 - 0,5-1,0 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 betamethasone, time entered through the corresponding intervals. 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.

Features of use:

NOT TO ENTER INTRAVENOUSLY! NOT TO ENTER SUBCUTANEOUSLY!
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 at the patient of anamnestic instructions on allergic reactions to medicines.
Diprospan contains two active agents - betamethasone derivatives, one of which - sodium betamethasone phosphate - quickly gets into a system blood stream. At Diprospan's appointment it is necessary to consider possible systemic action of instant fraction of drug.

Against the background of Diprospan's use disturbances of mentality are possible (especially at patients with emotional instability or tendency to psychoses). At Diprospan's appointment a sick diabetes mellitus correction of hypoglycemic therapy can be required.
The patients receiving GKS. it is not necessary to vaccinate against smallpox. It is not necessary to carry out also other immunization at the patients receiving GKS (especially in high doses), in view of a possibility of development of neurologic complications and a low response immune response (lack of antibody formation). However carrying out immunization is possible when performing replacement therapy (for example, at primary insufficiency of bark of adrenal glands).
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 Diprospan's use it is necessary to consider that GKS can mask symptoms of an infectious disease, and also 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 acceleration of 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 intra joint therapy the patient should avoid overloads of joints.
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 manumissions 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 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 emergence of a stressful situation during this period therapy by 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".

Use in педиатрии.Дети by whom to be carried out therapy by Diprospan (especially long), there have to be under careful medical observation regarding possible lag in growth also development of secondary insufficiency of bark of adrenal glands.

Side effects:

Frequency of development and expressiveness of side effects as at use and other GKS, depend on the size of the used dose and duration of use of drug.
These phenomena are usually reversible and can be eliminated or reduced at a dose decline.
- From water and electrolytic balance: a hypernatremia, increase in release of potassium, increase in removal of calcium, a gipokaliyemichesky alkalosis, a liquid delay in fabrics.
- From cardiovascular system: chronic heart failure (at predisposed patients), increase in arterial pressure.
- 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: digestive tract erosive cankers with possible subsequent perforation and bleeding, pancreatitis, a meteorism, a hiccups.
- From skin and mucous membranes: 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 a 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 insufficient (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 glucose-lowering 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).
- From a metabolism: negative nitric balance (because of a protein catabolism), липоматоз (including mediastinal and epidural липоматоз which can cause neurologic complications), increase in body weight.
- Allergic reactions: anaphylactic reactions, shock, Quincke's disease, lowering of arterial pressure.
- The other reactions connected with parenteral administration of drug: seldom - hyper-or hypopigmentation, a hypodermic and skin atrophy, aseptic abscesses, rush of blood to the person after an injection (or intra joint introduction), a neurogenic arthropathy.

Interaction with other medicines:

- At co-administration of phenobarbital, Rifampinum, Phenytoinum or ephedrine acceleration of metabolism of drug at decrease in its therapeutic activity is possible.
- At simultaneous use of GKS and estrogen dose adjustment of drugs can be required (because of danger of their overdose).
- At combined use of Diprospan and potassium - the removing diuretics raises probability of development of a hypopotassemia.
- Simultaneous use of GKS and cardiac glycosides increases peep of developing of arrhythmia or digitalis intoxication (because of a hypopotassemia)
- Diprospan can strengthen the potassium removal caused by Amphotericinum - Century.
- At combined use of Diprospan and indirect anticoagulants the changes of coagulability of blood demanding dose adjustment are possible.
- At the combined use of GKS with NPVP or with ethanol and 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 introduction of the doses of betamethasone exceeding 0,3-0,45 mg/sq.m of a body surface a day).
- GKS can influence the nitric blue tetrazolevy test for a bacterial infection and cause false and negative result.

Contraindications:

- hypersensitivity to betamethasone or other components of drug, or other GKS,
- system mycoses,
- intravenous or hypodermic administration,
- at intra joint introduction: unstable joint, infectious arthritis,
- introduction to the infected surfaces and to intervertebral space.

With care. A hypothyroidism, cirrhosis, diseases of eyes caused by Herpes simplex (because of risk of perforation of a cornea), nonspecific ulcer colitis, at perforation threat, abscess or other purulent infections, a diverticulitis, a recent intestinal anastomosis, an active or latent peptic ulcer of a stomach and duodenum, a renal failure, arterial hypertension, osteoporosis, a heavy myasthenia, a Werlhof's disease (intramuscular introduction).

Use during pregnancy and a lactation. Due to the lack of controlled researches of safety of use of Diprospan during pregnancy use of drug for pregnant women or for women of childbearing age demands preliminary estimate of estimated advantage and potential risk for mother and a fruit. Newborns whose mothers received therapeutic doses of GKS during pregnancy have to be under medical control (for early detection of adrenal insufficiency)
In need of Diprospan's appointment 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).

Overdose:

Symptoms. The acute overdose of betamethasone does not conduct to life-threatening situations. Introduction within several days of high doses of GKS 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 potassium - the removing diuretics).

Treatment. Careful medical control of a condition of the patient is necessary; 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:

In the unavailable to children and protected from light place, at a temperature not above 25 °C. Not to freeze!

Issue conditions:

According to the recipe

Packaging:

Suspension for injections of 2 mg +5 mg/ml.
On 1 ml in ampoules from glass of a hydrolytic class 1. On 1 or 5 ampoules in a plastic blister strip packaging together with the application instruction in a cardboard pack.