Composition, form of production and packaging
Suspension for injection is transparent, colorless or yellowish, slightly viscous, containing easily suspended particles of white or almost white color, free from foreign impurities; when shaken, a stable suspension of white or yellowish color is formed.
1 ml
betamethasone sodium phosphate 2.63 mg,
which corresponds to the content of betamethasone 2 mg
betamethasone dipropionate 6.43 mg,
which corresponds to the content of betamethasone 5 mg
Auxiliary substances: sodium hydrogen phosphate dihydrate, sodium chloride, disodium edetate, polysorbate 80 (polyoxyethylene sorbitan monooleate), benzyl alcohol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, carmellose sodium, macrogol (polyethylene glycol), hydrochloric acid, water d / u - up to 1 ml.
1 ml - ampoules glass (1) - packings cellular contour plastic (1) - packs cardboard.
1 ml - ampoules glass (5) - packings cellular contour plastic (1) - packs cardboard.
Suspension for injection is transparent, colorless or light yellow, slightly viscous, containing easily suspended particles of white or almost white color, free from foreign impurities; when shaken, a stable suspension of white or yellowish color is formed.
1 ml
betamethasone sodium phosphate 2.63 mg,
which corresponds to the content of betamethasone 2 mg
betamethasone dipropionate 6.43 mg,
which corresponds to the content of betamethasone 5 mg
Auxiliary substances: sodium hydrogen phosphate dihydrate 2.51 mg, sodium chloride 5 mg, disodium edetate 0.1 mg, polysorbate 80 500 Ојg, benzyl alcohol 9 mg, methyl parahydroxybenzoate 1.3 mg, propyl parahydroxybenzoate 200 Ојg, carmellose sodium 5 mg, macrogol 4000 - 20 mg, hydrochloric acid - up to pH 6.7-7.7, water d / u - up to 1 ml.
1 ml - disposable syringes of colorless glass (1) complete with 2 sterile needles - plastic containers (1) - cardboard packs.
2 ml - disposable syringes made of colorless glass (1) complete with 2 sterile needles - plastic containers (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
GCS. Has a high glucocorticoid and minor mineralocorticoid activity. The drug has anti-inflammatory, antiallergic and immunosuppressive effect, and also has a pronounced and diverse effect on various types of metabolism.
PHARMACOKINETICS
Suction and distribution
Betamethasone sodium phosphate is readily soluble and after intravenous administration it is rapidly hydrolyzed and almost immediately absorbed from the injection site, which provides a rapid onset of therapeutic action. Virtually completely eliminated within one day after administration.
Betamethasone dipropionate is slowly absorbed from the depot, metabolized gradually, which causes a prolonged effect of the drug, and is withdrawn for more than 10 days.
The binding of betamatezone to plasma proteins is 62.5%.
Metabolism and excretion
Metabolized in the liver with the formation of mostly inactive metabolites. It is excreted mainly by the kidneys.
INDICATIONS
Treatment of conditions and diseases in which GCS therapy can achieve an adequate clinical effect (it should be borne in mind that in some diseases, GCS therapy is complementary and does not replace standard therapy):
- diseases of the musculoskeletal system and soft tissues, incl. rheumatoid arthritis, osteoarthrosis, bursitis, ankylosing spondylitis, epicondylitis, radiculitis, coccidonia, sciatica, lumbago, torticollis, ganglionic cyst, exostosis, fasciitis, foot diseases;
- allergic diseases, incl. bronchial asthma, hay fever (hay fever), allergic bronchitis, seasonal or all-the-year-round rhinitis, drug allergy, serum sickness, reactions to insect bites;
- dermatological diseases, incl. atopic dermatitis, coin-like eczema, neurodermatitis, contact dermatitis, severe photodermatitis, urticaria, lichen planus, insulinic lipodystrophy, alopecia areata, discoid lupus erythematosus, psoriasis, keloid scars, pemphigus vulgaris, herpetic dermatitis, cystic acne;
- systemic connective tissue diseases, including systemic lupus erythematosus, scleroderma, dermatomyositis, nodular periarteritis;
- hemoblastoses (palliative therapy of leukemia and lymphomas in adults, acute leukemia in children);
- Primary or secondary insufficiency of the adrenal cortex (with simultaneous simultaneous application of mineralocorticoids);
- other diseases and pathological conditions requiring therapy with systemic GCS (adrenogenital syndrome, ulcerative colitis, regional ileitis, malabsorption syndrome, lesions of the eye mucosa when it is necessary to administer the drug into the conjunctival sac, pathological changes in the blood if necessary for the use of GCS, nephritis, nephrotic syndrome).
DOSING MODE
Diprospan В® is used for in / m, intraarticular, periarticular, intra-abdominal, intradermal, interstitial and intramuscular administration.
The insignificant dimensions of the crystals of betamethasone dipropionate allow the use of needles of small diameter (up to 26 calibers) for intradermal administration and introduction directly into the lesion site.
The drug is not intended for intravenous and / or injections.
Injections of Diprospan В® should be carried out with strict adherence to aseptic rules.
The dosage regimen and the mode of administration are set individually, depending on the indications, the severity of the disease and the patient's response.
In systemic use, the initial dose of Diprospan В® is in most cases 1-2 ml. The introduction is repeated as necessary, depending on the patient's condition.
Intramuscular injection
Diprospan В® should be injected deep in the / m, choosing large muscles and avoiding entering other tissues (to prevent tissue atrophy).
In severe conditions requiring urgent therapy, the initial dose is 2 ml.
With various dermatological diseases, as a rule, it is sufficient to administer 1 ml of a suspension of Diprospan.
In diseases of the respiratory system, the onset of action of the drug occurs within a few hours after the IM injection of the suspension. With bronchial asthma, hay fever, allergic bronchitis and allergic rhinitis, a significant improvement is achieved after the introduction of 1-2 ml of Diprospan.
With acute and chronic bursitis, the initial dose for the IM is 1-2 ml of the suspension. If necessary, several repeated injections are carried out.
If a satisfactory clinical response does not occur after a certain period of time, DiprospanВ® should be discontinued and another therapy prescribed.
Local introduction
With local administration, simultaneous application of a local anesthetic is necessary only in rare cases. If required, 1% or 2% solutions of procaine hydrochloride or lidocaine without methyl paraben, propylparaben, phenol and other similar substances are used. In this case, the mixing is carried out in a syringe, first by typing in the syringe from the vial the required dose of suspension of the Diprospan В® preparation. Then the required amount of local anesthetic is taken from the ampoule into the same syringe and shaken for a short time.
In the case of acute bursitis (sub-deltoid, subscapular, elbow and prenadalovenous), the introduction of 1-2 ml of the suspension into the synovial bag alleviates the pain and restores the mobility of the joint for several hours. After relieving the exacerbation of chronic bursitis, smaller doses of the drug are used.
In acute tenosynovitis, tendinitis and peritendinitis, an injection of Diprospan В® improves the patient's condition; when chronic - the injection is repeated depending on the patient's reaction. It is necessary to avoid the introduction of the drug directly into the tendon.
Intra-articular administration of the drug Diprospan В® at a dose of 0.5-2 ml relieves pain, limiting the mobility of joints with rheumatoid arthritis and osteoarthritiswithin 2-4 hours after administration. The duration of the therapeutic effect varies considerably and can be 4 or more weeks.
The recommended dose of the drug when injected into large joints is 1 to 2 ml; in the middle joints - 0.5-1 ml; in small joints - 0.25-0.5 ml.
With some dermatological diseases , intradermal administration of Diprospan В® directly into the lesion is effective, the dose is 0.2 ml / cm 2 . The focus is uniformly corked using a tuberculin syringe and a needle with a diameter of about 0.9 mm. The total amount of the drug administered on all sites should not exceed 1 ml for 1 week. For introduction into the lesion it is recommended to use a tuberculin syringe with a 26 gauge needle.
Recommended single doses of the drug (with the interval between administrations 1 week) for bursitis : with 0.25-0.5 ml of homozygliness (as a rule, 2 injections are effective), with spurs - 0.5 ml, with restriction of mobility of the big toe - 0.5 ml, with synovial cyst - 0.25-0.5 ml, with tenosynovitis - 0.5 ml, with acute gouty arthritis - 0.5-1 ml. For most injections, a tuberculin syringe with a 25 gauge needle is suitable.
After achieving the therapeutic effect, the maintenance dose is selected by gradually reducing the dose of Diprospan В® , which is carried out at intervals. The reduction is continued until the minimum effective dose is reached.
If there is a risk of a stressful situation (not related to the disease), you may need to increase the dose of Diprospan В® .
The cancellation of the drug after prolonged therapy is carried out by a gradual dose reduction.
The patient's condition is monitored for at least a year after the end of long-term therapy or at high doses.
SIDE EFFECT
Metabolism: hypernatremia, increased potassium secretion, increased calcium excretion, hypokalemic alkalosis, fluid retention in tissues, negative nitrogen balance (due to protein catabolism), lipomatosis (including mediastinal and epidural lipomatosis, which can cause neurological complications), weight gain.
From the cardiovascular system: chronic heart failure (in predisposed patients), increased blood pressure.
From the musculoskeletal system: muscle weakness, steroid myopathy, loss of muscle mass, increased myasthenic symptoms in severe pseudo-paralytic myasthenia gravis, osteoporosis, compression fracture of the spine, aseptic necrosis of the head of the femoral or humerus, pathological fractures of the tubular bones, tendon ruptures, joint instability with repeated intraarticular injections).
On the part of the digestive system: erosive and ulcerative lesions of the gastrointestinal tract with possible subsequent perforation and bleeding, pancreatitis, flatulence, hiccough.
Dermatological reactions: disruption of wound healing, atrophy and thinning of the skin, petechiae, ecchymosis, excessive sweating, dermatitis, steroid acne, striae, propensity to develop pyoderma and candidiasis, reduce reaction during skin tests.
From the side of the central nervous system and the peripheral nervous system: convulsions, increased intracranial pressure with edema of the optic disc (more often at the end of therapy) dizziness, headache, euphoria, mood changes, depression (with severe psychotic reactions), personality disorders, increased irritability, insomnia.
On the part of the endocrine system: menstrual disorders, secondary adrenal insufficiency (especially during periods of stress in case of illness, trauma, surgery), Itenko-Cushing syndrome, reduced carbohydrate tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, increased need for insulin or oral hypoglycemic drugs, intrauterine growth, growth retardation and sexual development in children.
From the side of the organ of vision: posterior subcapsular cataract, increased intraocular pressure, glaucoma, exophthalmos; in rare cases - blindness (with the introduction of the drug in the face and head).
Allergic reactions: anaphylactic reactions, shock, angioedema, arterial hypotension.
Local reactions: rarely - hyper- or hypopigmentation, subcutaneous and dermal atrophy, aseptic abscesses.
Other: a rush of blood to the face after injection (or intra-articular injection), neurogenic arthropathy.
The frequency of development and severity of side effects, as in the application of other GCS, depend on the magnitude of the applied dose and the duration of application of the drug. These phenomena are usually reversible and can be eliminated or reduced by lowering the dose.
CONTRAINDICATIONS
- systemic fungal infections;
- iv or s / c introduction;
- for intraarticular administration: unstable joint, infectious arthritis;
- introduction into infected surfaces and into the intervertebral space;
- Children's age to 3 years (the presence of benzyl alcohol);
- hypersensitivity to the components of the drug;
- Hypersensitivity to other GCS.
With caution
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.
Post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection).
Diseases of the gastrointestinal tract: peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis, abscess or other purulent infections.
Diseases of the cardiovascular system, incl. recently suffered 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), decompensated chronic heart failure, hypertension, hyperlipidemia).
Endocrine diseases - diabetes (including a violation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease.
Severe chronic renal and / or hepatic insufficiency, nephrourolythiasis, cirrhosis of the liver.
Thrombocytopenic purpura (IM injection).
Hypoalbuminemia and conditions predisposing to its occurrence.
Systemic osteoporosis, myasthenia gravis, acute psychosis, grade III-IV obesity, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma, eye diseases caused by Herpes simplex (due to the risk of corneal perforation), pregnancy, lactation.
For intraarticular administration: the general severe condition of the patient, ineffectiveness (or short-term) of the effect of the previous 2 injections (taking into account the individual properties of the SCS used).
PREGNANCY AND LACTATION
Due to the lack of controlled studies of the safety of the use of Diprospan В® in pregnancy, when it is necessary to prescribe the drug to pregnant women or women of childbearing age , a preliminary evaluation of the expected benefit of therapy for the mother and potential risk to the fetus is required.
Newborns whose mothers received therapeutic doses of GCS during pregnancy should be under medical supervision (for early detection of signs of adrenal insufficiency).
If you need to prescribe the drug Diprospan В® during lactation, you should decide whether to stop breastfeeding, taking into account the importance of therapy for the mother (due to possible side effects in children).
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in severe chronic renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in severe chronic liver failure, cirrhosis.
APPLICATION FOR CHILDREN
Children who are treated with Diprospan В® (especially long-term) should be carefully monitored for possible growth retardation and secondary adrenocortical insufficiency.
SPECIAL INSTRUCTIONS
The dosage regimen and the mode of administration are set individually, depending on the indications, the severity of the disease and the patient's response.
The drug should be used in the minimum effective dose, the period of application should be as short as possible.
The initial dose is selected until the necessary therapeutic effect is achieved. If after a sufficient period of time the therapeutic effect is not observed, the drug is canceled by gradually reducing the dose of the drug. Diprospan В® and select another appropriate method of treatment.
After achieving the therapeutic effect, the maintenance dose is selected by gradually reducing the dose of betamethasone, which is administered at appropriate intervals. The reduction is continued until the minimum effective dose is reached.
If there is a threat of a stressful situation (not related to the disease), it may be necessary to increase the dose of Diprospan.
Abolition of the drug after prolonged therapy is conducted by gradually reducing the dose.
Monitoring of the patient is performed at least for one year after the end of therapy, or prolonged use at high doses.
The introduction of the drug in soft tissue, intralesional and intra-articular may be expressed at local action at the same time lead to a systemic action.
Given the likelihood of anaphylactoid reactions upon parenteral administration of corticosteroids, should take the necessary precautions before administration of the drug, especially in the presence of indications of a history of allergic reactions to medicines.
diprospan В®It contains two active substances - compound betamethasone, one of which, betamethasone sodium phosphate is rapidly dissolving fraction and therefore penetrates rapidly into the systemic circulation. It should take into account possible systemic effect of the drug.
Against the background of the drug Diprospan В® possible mental disorders, especially in patients with emotional instability or propensity to psychoses.
In appointing Diprospan patients with diabetes mellitus may require adjustment of hypoglycemic therapy.
Patients receiving Diprospan В® at doses that suppress the immune system, it is necessary to warn of the need to avoid contact with sick chicken pox and measles (particularly important when administering the drug to children).
In applying the drug Diprospan В® should be noted that corticosteroids can mask the signs of infection and reduce the resistance to infections.
Appointment Diprospan with active tuberculosis is possible only in cases of fulminant or disseminated tuberculosis in combination with appropriate anti-tuberculosis therapy. In appointing Diprospan patients with latent tuberculosis or a positive reaction to the tuberculin should be considered for preventive therapy. In prophylactic applications, rifampin should take into account the increase in the hepatic clearance of betamethasone (may require dose correction).
When the liquid in the articular cavity should be deleted septic process.
Marked increase in pain, swelling, fever surrounding tissue and further restriction of joint movement testify to infectious arthritis. Upon confirmation of the diagnosis is necessary to appoint antibiotics.
Repeated injections into the joint in osteoarthritis may increase the risk of joint damage. The introduction of corticosteroids in the tendon tissue gradually leads to rupture of the tendon.
After successful treatment of intra-articular injections of drug Diprospan В® patient should avoid overloads joint.
Prolonged use of corticosteroids may cause posterior subcapsular cataracts (especially in children), glaucoma with possible lesion of the optic nerve and can promote the development of secondary ocular infections (fungal or viral).
Periodically carry out an eye examination, especially in patients receiving Diprospan В® for more than 6 months.
With an increase in blood pressure, fluid retention, and sodium chloride in the tissues and increase excretion of potassium (less likely than with other GCS) patients recommended diet with restriction of salt and further kalisodergaszczye prescribed drugs. All corticosteroids increase calcium excretion.
With simultaneous use of cardiac glycosides and diprospana or drugs that affect the electrolyte composition of the plasma requires control of water and electrolyte balance.
Precautions acetylsalicylic acid administered in combination with a preparation Diprospan В® gipoprotrombinemii.
The development of secondary adrenal insufficiency due to too rapid abolition of GCS is possible within a few months after the end of therapy. In the event of a threat or stress within that period therapy with Diprospan В® should be resumed, and simultaneously designate mineralocorticoid preparation (due to possible disturbances secretion mineralocorticoids). Phase-out of corticosteroids reduces the risk of secondary adrenal insufficiency.
Against the background of the use of corticosteroids can change the number and mobility of sperm.
When long-term therapy of corticosteroids useful to consider the possibility of moving from parenteral to oral corticosteroids, taking into account the evaluation of benefit / risk ratio.
Patients receiving corticosteroids should not be vaccinated against smallpox, as well as carry out other immunization, particularly against treatment with high doses of corticosteroids, because of the possibility of neurological complications and low immune response (absence of antibody formation). Immunization possibly during replacement therapy (e.g., primary adrenal insufficiency).
Use in Pediatrics
Children who have conducted drug therapy Diprospan В® (especially long-term) should be under close medical supervision for possible lag in the growth and development of secondary adrenal insufficiency.
OVERDOSE
Symptoms: acute overdose of betamethasone does not lead to life-threatening situation. Administration over several days corticosteroids at high doses does not lead to undesirable consequences, except the use of very high doses or the use for diabetes, glaucoma, exacerbation erosive and ulcerative gastrointestinal lesions or while the use of digitalis preparations, anticoagulants or kaliyvyvodyaschih diuretics.
Treatment: requires careful medical supervision of the patient. It should maintain an optimum fluid intake and to control the content of electrolytes in the plasma and in the urine, particularly the ratio of sodium and potassium ions. If necessary to carry out the appropriate therapy.
DRUG INTERACTION
When concomitant administration of drug Diprospan В® phenobarbital, rifampin, phenytoin or ephedrine may accelerate metabolism betamethasone while reducing its therapeutic activity.
When the joint application Diprospan preparation В® and anticoagulants possible changes in blood clotting, require dosage adjustment.
In a joint application of the drug Diprospan В® and kaliyvyvodyaschih diuretics increases the likelihood of hypokalemia.
Diprospan В® can enhance the excretion of potassium caused by amphotericin B.
With the simultaneous use of corticosteroids and estrogen dose adjustment may require drugs (because of the danger of their overdose).
The simultaneous use of corticosteroids and cardiac glycosides increases the risk of arrhythmia and digitalis intoxication (due hypokalemia).
The combined use of corticosteroids with NSAIDs, with ethanol or ethanol-containing preparations may increase the intensity or frequency of occurrence of erosive-ulcerous lesions of the gastrointestinal tract.
If concomitant use of corticosteroids may reduce the concentration of salicylates in blood plasma.
Simultaneous administration of corticosteroids, and growth hormone may result in slower absorption of the latter (to avoid administration of betamethasone in doses exceeding 0.3-0.45 mg / m 2 body / day surface).
SCS may affect the nitrogen blue tetrazolevy test for bacterial infection and cause a false-negative result.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be kept out of the reach of children, protected from light at a temperature not higher than 25 В° C; Do not freeze. Shelf life - 2 years.
