Betaspan Depot, 7 mg/ml, suspension for injection, 1 ml, 5 pcs.
The dosage regimen and route of administration are determined individually, depending on the indications, severity of the disease and patient response. The dose should be as small as possible and the period of use as short as possible. The initial dose is adjusted until the desired therapeutic effect is achieved. If, after a sufficient period of time, no therapeutic effect is observed, the drug is discontinued by gradually reducing the dose and another appropriate treatment method is selected.
If a stressful situation (not related to the disease) occurs or threatens to occur, it may be necessary to increase the dose of the drug.
Discontinuation of the drug after long-term therapy is carried out by gradually reducing the dose.
The patient's condition is monitored for at least a year after the end of long-term therapy or use in high doses.
Administration of the drug into soft tissues, the lesion and inside the joint can, with a pronounced local effect, simultaneously lead to a systemic effect.
Considering the likelihood of developing anaphylactoid reactions with parenteral administration of GCS, the necessary precautions should be taken before administering the drug, especially if the patient has anamnestic indications of allergic reactions to the drug.
The drug contains two active substances - betamethasone derivatives, one of which - betamethasone sodium phosphate - quickly penetrates the systemic bloodstream. When prescribing, the possible systemic effect of the rapidly soluble fraction of the drug should be taken into account.
While using the drug, mental disorders are possible (especially in patients with emotional instability or a tendency to psychosis).
When using Betaspan® Depot in patients with diabetes mellitus, adjustment of hypoglycemic therapy may be required.
Patients receiving corticosteroids should not be vaccinated against smallpox. Do not carry out other immunizations in patients receiving GCS (especially in high doses), due to the possibility of developing neurological complications and a low immune response (lack of antibody formation). However, immunization is possible during replacement therapy (for example, in case of primary adrenal insufficiency).
Patients receiving Betaspan® Depot in doses that suppress the immune system should be warned about the need to avoid contact with patients with chickenpox and measles (especially important when using the drug in children).
When using the drug, it should be taken into account that GCS can mask the signs of an infectious disease, as well as reduce the body's resistance to infections. Prescribing the drug for active tuberculosis is possible only in cases of fulminant or disseminated tuberculosis in combination with adequate anti-tuberculosis therapy. When prescribing the drug to patients with latent tuberculosis or a positive reaction to tuberculin, the issue of preventive anti-tuberculosis therapy should be considered. When using prophylactic rifampicin, it is necessary to take into account the acceleration of hepatic clearance of betamethasone (dose adjustment may be required).
If there is fluid in the joint cavity, a septic process should be excluded. A noticeable increase in pain, swelling, increased temperature of the surrounding tissues and further limitation of joint mobility indicate infectious arthritis. Once the diagnosis is confirmed, antibacterial therapy must be prescribed.
Repeated injections into a joint for osteoarthritis may increase the risk of joint destruction. The introduction of GCS into the tendon tissue gradually leads to tendon rupture. After successful intra-articular therapy, the patient should avoid overloading the joints.
Long-term use of GCS can lead to posterior subcapsular cataracts (especially in children), glaucoma with possible damage to the optic nerve and contribute to the development of secondary eye infections (fungal or viral). It is necessary to periodically conduct an ophthalmological examination, especially in patients receiving Betaspan® Depot for more than 6 months.
With increased blood pressure, fluid and sodium retention in the body, and increased excretion of potassium from the body, patients are recommended to follow a diet with limited salt and additional use of potassium-containing drugs.
All corticosteroids enhance calcium excretion.
When using Betaspan® Depot simultaneously with cardiac glycosides or drugs that affect the electrolyte composition of plasma, monitoring of the water-electrolyte balance is required.
Use acetylsalicylic acid with caution in combination with Betaspan® Depot for hypoprothrombinemia.
The development of secondary adrenal insufficiency due to too rapid withdrawal of GCS is possible within several months after the end of therapy. If a stressful situation occurs or threatens to occur during this period, therapy with Betaspan® Depot should be resumed and a mineralocorticoid drug should be prescribed at the same time (due to a possible disruption of mineralocorticoid secretion). Gradual withdrawal of GCS can reduce the risk of developing secondary adrenal insufficiency.
With the use of corticosteroids, changes in sperm motility and number are possible.
During long-term therapy with GCS, it is advisable to consider the possibility of switching from parenteral to oral GCS, taking into account the assessment of the benefit/risk ratio.
Application in pediatrics.
Children undergoing drug therapy (especially long-term therapy) should be under close medical supervision for possible growth retardation and the development of secondary adrenal insufficiency.
Impact on the ability to drive vehicles and operate machinery.
During treatment with Betaspan® Depot, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Betaspan depot in Moscow and Moscow Region
Metabolic: hypernatremia, increased potassium excretion, 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), increased body weight. 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 pseudoparalytic myasthenia , osteoporosis, compression fracture of the spine, aseptic necrosis of the head of the femur or humerus, pathological fractures of tubular bones, tendon ruptures, joint instability (with repeated intra-articular injections). From the digestive system: erosive and ulcerative lesions of the gastrointestinal tract with possible subsequent perforation and bleeding, pancreatitis , flatulence, hiccups. Dermatological reactions: impaired wound healing, atrophy and thinning of the skin, petechiae, ecchymosis, increased sweating, dermatitis, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis, decreased response to skin tests. From the nervous system: convulsions, increased intracranial pressure with papilledema (usually after completion of therapy), dizziness, headache, euphoria, mood changes, depression (with severe psychotic reactions), personality disorders, increased irritability, insomnia. From the endocrine system: menstrual irregularities , secondary adrenal insufficiency (especially during periods of stress due to illness, injury, surgery), Itsenko-Cushing syndrome, decreased carbohydrate tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, increased need for insulin or oral hypoglycemic drugs, intrauterine growth disorders, retardation growth and sexual development in children. From the organ of vision: posterior subcapsular cataract, increased intraocular pressure, glaucoma, exophthalmos; in rare cases - blindness (when the drug is administered to the face and head). Allergic reactions: anaphylactic reactions, shock, angioedema, arterial hypotension. Local reactions: rarely - hyper- or hypopigmentation, subcutaneous and skin atrophy, aseptic abscesses. Other: flushing of the face after injection (or intra-articular administration), neurogenic arthropathy. The frequency of development and severity of side effects, as with the use of other corticosteroids, depend on the size of the dose used and the duration of use of the drug. These effects are usually reversible and can be eliminated or reduced by reducing the dose.
Description of the drug BETASPAN DEPO® (BETASPAN DEPO®)
GKS. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects, and also has a pronounced and diverse effect on various types of metabolism.
Suppresses the release of ACTH and beta-lipotropin by the pituitary gland, but does not reduce the level of circulating beta-endorphin. Inhibits the secretion of TSH and FSH.
Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (stimulates the production of erythropoietin).
Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates the synthesis of mRNA; the latter induces the formation of proteins, incl. lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation and allergies.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, T- and B-lymphocytes, mast cells, decreased sensitivity of effector cells to allergy mediators, inhibition of antibody formation, changes in immune body response.
Antishock and antitoxic effects are associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.
In COPD, the action is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1, interleukin-2, interferon gamma) from lymphocytes and macrophages.
Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous corticosteroids. Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Protein metabolism:
- reduces the amount of protein in plasma (due to globulins) with an increase in the albumin/globulin ratio, increases the synthesis of albumins in the liver and kidneys;
- enhances protein catabolism in muscle tissue.
Lipid metabolism:
- increases the synthesis of higher fatty acids and TG, redistributes fat (fat accumulation mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism:
- increases the absorption of carbohydrates from the gastrointestinal tract;
- increases the activity of glucose-6-phosphatase, leading to an increase in the flow of glucose from the liver into the blood;
- increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, leading to the activation of gluconeogenesis.
Water-electrolyte metabolism:
- retains sodium and water in the body, stimulates the excretion of potassium, reduces the absorption of calcium from the gastrointestinal tract, “washes” calcium from the bones, and increases excretion by the kidneys.
Betamethasone sodium phosphate
is an easily soluble compound that is well absorbed after parenteral administration into tissues and provides a rapid effect.
Betamethasone dipropionate
has slower absorption. By combining these salts it is possible to create medicines with both short-term (but fast) and long-term effects. Depending on the method of application (IV, IM, intra-articular, periarticular, IV), a general or local effect is achieved.
Betaspan
Severe neurological impairment, some of which was fatal, has been reported following epidural corticosteroid injection. There have also been reports of spinal cord infarction, paraplegia, quadriplegia, cortical blindness and stroke. These serious neurological disorders were observed regardless of the use of fluoroscopy. Because the safety and effectiveness of epidural administration have not been established, corticosteroids are not recommended for epidural use.
Injections must be administered deeply only into large muscle masses to avoid local tissue atrophy.
When administered into soft tissue at sites of injury and intra-articularly, both local and systemic effects of corticosteroids may occur.
It is necessary to examine the intra-articular fluid to exclude a septic process. Local injections into a previously infected joint should be avoided. A noticeable increase in pain and local swelling, further restriction of joint movement, fever and malaise are signs of septic arthritis. If the diagnosis of sepsis is confirmed, appropriate antimicrobial therapy should be prescribed.
Corticosteroids should not be injected into unstable joints, areas of inflammation, or intervertebral spaces. Repeated injections into joints for osteoarthritis may increase joint destruction. Injecting corticosteroids directly into tendons should be avoided as this may cause delayed tendon rupture.
After intra-articular therapy with betamethasone, the patient should avoid very heavy loads on the joint in which the symptoms were relieved.
Since there have been isolated cases of anaphylactic reactions in patients receiving parenteral therapy with betamethasone, safety precautions should be taken before prescribing the drug, especially in patients with a history of allergies to any drug.
When using corticosteroid therapy for a long time, all potential benefits and risks should be considered before switching from parenteral to oral use.
Changes in the dosage regimen are possible depending on the course of the disease during remission or exacerbation, the patient's response to therapy, negative changes in the patient's emotional and physical state, for example, severe infection, surgery or trauma. After completing a long or intensive course of treatment with glucocorticosteroids, constant monitoring of the patient's condition throughout the year is necessary.
Corticosteroids may exacerbate systemic fungal infections and should therefore not be used in the presence of infections requiring antifungal treatment.
Corticosteroids may mask signs of infections, or new infections may occur while taking corticosteroids. When using corticosteroids, the body's resistance and ability to localize the infection are reduced.
With long-term use, posterior subcapsular cataracts (especially in children), glaucoma with possible damage to the optic nerve, and an increased risk of developing secondary fungal or viral eye infections may occur. An ophthalmological examination should be performed periodically, especially in patients undergoing long-term therapy (more than 6 weeks).
The use of medium and large doses of corticosteroids can cause increased blood pressure, salt and fluid retention, and increased potassium excretion. These effects are less likely when using synthetic derivatives (but not in high doses). However, a low-salt diet and potassium supplements may be necessary. All corticosteroids increase calcium excretion.
Patients should not be vaccinated against varicella while receiving corticosteroids. Patients receiving corticosteroids, especially high doses, should not be vaccinated against other infections due to the risk of developing neurological complications and a decreased immune response. However, immunization is possible in patients receiving corticosteroid replacement therapy, such as Addison's disease.
Patients receiving immunosuppressive doses of corticosteroids should avoid contact with patients with chickenpox and measles. This is especially important for children.
For active tuberculosis, corticosteroid therapy should be limited to cases of fulminant or disseminated tuberculosis, in which a corticosteroid is used only in conjunction with antituberculosis therapy. Patients with latent tuberculosis or those who are reactive to tuberculin and receiving corticosteroids should be under medical supervision, as reactivation of the disease is possible. During long-term corticosteroid therapy, patients should receive chemoprophylaxis. If rifampicin is used as part of chemotherapy, its enhancing effect on the metabolic hepatic clearance of corticosteroids should be taken into account; It may be necessary to adjust the dose of the corticosteroid.
To control the condition during treatment, the lowest dose of corticosteroid should be used; If possible, the dose is reduced gradually.
Due to very rapid withdrawal of the corticosteroid, secondary drug-induced adrenal insufficiency may occur, which can be minimized by gradually reducing the dose of the drug. This relative insufficiency may persist for several months after cessation of therapy, therefore, if the patient experiences a stressful situation during this period, the use of corticosteroids should be resumed. If the patient is already receiving corticosteroids, the dosage may need to be increased. Due to the possible impairment of mineralocorticoid secretion, salt and/or mineralocorticoids should be used concomitantly. Dose reductions must be made under strict medical supervision, and sometimes it is necessary to monitor the patient's condition for a period of up to one year after stopping long-term treatment or using increased doses.
In patients with diabetes, betamethasone can be used only for a short period and only under strict medical supervision, given its glucocorticoid properties (transformation of proteins into glucose).
The effect of the drug is enhanced in persons with hypothyroidism and cirrhosis of the liver.
The drug should be prescribed with caution for ocular herpes zoster due to possible perforation of the cornea.
With corticosteroid therapy, mental disorders may occur (especially in patients with emotional instability or a tendency to psychosis).
The drug should be used with caution in nonspecific ulcerative colitis with the threat of perforation, abscess or other purulent infection, diverticulitis, intestinal anastomosis, gastric and duodenal ulcers, renal failure, arterial hypertension, osteoporosis, myasthenia gravis, glaucoma, acute psychoses, viral and bacterial infections, growth retardation, tuberculosis, Cushing's syndrome, diabetes, heart failure, in case of difficult-to-treat cases of epilepsy, a tendency to thromboembolism or thrombophlebitis, during pregnancy.
Complications of treatment with glucocorticosteroids depend on the dose and duration of treatment, so it is necessary to consider the risk/benefit ratio for each patient.
In some patients, corticosteroids may cause a decrease in sperm count and motility.
Results from one multicenter randomized controlled trial with a different corticosteroid (methylprednisolone hemisuccinate) showed an increase in early mortality (at 2 weeks) and late mortality (at 6 months) in patients with traumatic brain injury who received methylprednisolone compared with placebo. The causes of mortality in the methylprednisolone group have not been established. It should be noted that this study did not include patients who had a direct indication for the use of corticosteroids. High doses of corticosteroids should not be used to treat traumatic brain injury.
The total amount of sodium in 1 ml of solution is 0.06 mmol, that is, the drug is practically free of sodium.
Betaspan depot suspension d/in 7 mg/ml N5 (Farmak)
Severe nervous system complications (including death) have been reported with epidural and intrathecal administration of GCS (with or without fluoroscopic guidance), including spinal cord infarction, paraplegia, quadriplegia, cortical blindness and stroke. Since the safety and effectiveness of epidural corticosteroids have not been established, this route of administration is not indicated for this group of drugs. Recommended routes of administration are listed in the "Method of administration and dosage" section. Intravascular administration of the drug must be avoided. Due to the lack of data regarding the risk of calcification, injection of the drug into the intervertebral space is contraindicated. The dosage regimen and route of administration are determined individually, depending on the indications, severity of the disease and patient response. The dose should be as small as possible and the period of use as short as possible. The initial dose is adjusted until the desired therapeutic effect is achieved. Then gradually reduce the dose of Betaspan® Depot to the minimum effective maintenance dose. If there is no effect from the therapy or if it is used for a long time, the drug is also discontinued, gradually reducing the dose. Gradual withdrawal of GCS can reduce the risk of developing secondary adrenal insufficiency. If a stressful situation (not related to the disease) occurs or threatens to occur, it may be necessary to increase the dose of Betaspan® Depot; the drugs of choice as a supplement should be hydrocortisone and cortisone. The development of secondary adrenal insufficiency due to too rapid withdrawal of GCS is possible within several months after the end of therapy. If a stressful situation occurs or threatens to occur during this period, therapy with Betaspan® Depot should be resumed and a mineralocorticosteroid drug should be prescribed at the same time (due to a possible disturbance in the secretion of mineralocorticosteroids). The patient's condition is monitored for at least one year after the end of long-term therapy or use in high doses. Administration of the drug into soft tissues, into the lesion and intra-articularly can, with a pronounced local effect, simultaneously lead to a systemic effect. Considering the likelihood of developing anaphylactoid reactions with parenteral administration of GCS, the necessary precautions should be taken before administering the drug, especially if the patient has a history of allergic reactions to drugs. The drug Betaspan® Depot contains two active substances - betamethasone derivatives, one of which - betamethasone sodium phosphate - quickly penetrates into the systemic circulation, and therefore its possible systemic effect should be taken into account. When using the drug, mental disorders are possible (especially in patients with emotional lability or a tendency to psychosis). The effect of GCS is enhanced in patients with liver cirrhosis or hypothyroidism. When using Betaspan® Depot in patients with diabetes mellitus, adjustment of hypoglycemic therapy may be required. Patients receiving corticosteroids should not be vaccinated against smallpox. Other immunizations should not be carried out in patients receiving GCS (especially in high doses), due to the possibility of developing neurological complications and a low immune response (lack of antibody formation). Betaspan® Depot should not be used 8 weeks before and 2 weeks after vaccination with killed or inactivated viral and antibacterial vaccines. However, immunization is possible during replacement therapy (for example, with primary adrenal insufficiency). Patients receiving Betaspan® Depot in doses that suppress the immune system should be warned about the need to avoid contact with patients with chickenpox and measles (especially important when using the drug in children). With the use of GCS, it is possible to suppress the reaction during skin tests. When using the drug, it should be taken into account that GCS can mask the signs of an infectious disease, as well as reduce the body's resistance to infections. The immunosuppressive effect of GCS can lead to activation of a latent infection or exacerbation of intercurrent infections, including infections caused by microorganisms: Candida, Mycobacterium, Toxoplasma, Strongyloides, Pneumocystis, Cryptococcus, Nocardia or Ameba. Particular caution should be exercised when using GCS in patients with confirmed or suspected Strongyloides infection. In such patients, GCS-induced immunosuppression can lead to Strongyloides hyperinfection and spread of infection through larval migration, which is often accompanied by severe enterocolitis and Gram-negative septicemia, possibly fatal. Since corticosteroids may aggravate the course of latent amebiasis, all patients with unexplained diarrhea or patients arriving from countries with a tropical climate should be examined to exclude amebiasis before initiating corticosteroid therapy. It is necessary to carefully observe the rules of asepsis and antisepsis when administering the drug. Caution must be exercised when using the drug in patients at high risk of infection (on hemodialysis or with dentures). The use of the drug for active tuberculosis is possible only in cases of fulminant or disseminated tuberculosis in combination with adequate anti-tuberculosis therapy. When using the drug in patients with latent tuberculosis or during the period of tuberculin testing, the dose selection of Betaspan® Depot should be very careful (due to the danger of reactivation of tuberculosis), and with long-term use, anti-tuberculosis chemoprophylaxis is necessary. When using rifampicin prophylactically, acceleration of the hepatic clearance of betamethasone should be taken into account (betamethasone dose adjustment may be required). If there is fluid in the joint cavity, a septic process should be excluded. A noticeable increase in pain, swelling, increased temperature of the surrounding tissues and further limitation of joint mobility indicate septic arthritis. It is necessary to conduct a study of aspirated joint fluid. Once the diagnosis is confirmed, appropriate antibacterial therapy must be prescribed. The use of Betaspan® Depot for septic arthritis is contraindicated. Repeated injections into a joint for osteoarthritis may increase the risk of joint destruction. The introduction of GCS into the tendon tissue gradually leads to tendon rupture. After successful intra-articular therapy, the patient should avoid overloading the joints. Long-term use of corticosteroids can lead to posterior subcapsular cataracts (especially in children), glaucoma with possible damage to the optic nerve, and may contribute to the development of secondary eye infections (fungal or viral). It is necessary to periodically conduct an ophthalmological examination, especially in patients receiving Betaspan® Depot for more than 6 weeks. Particular care must be taken when considering the possibility of systemic use of GCS in patients with active herpetic eye lesions (keratitis caused by the herpes simplex virus). The use of medium and high doses of corticosteroids can lead to increased blood pressure, sodium and fluid retention in the body, and increased excretion of potassium from the body (these phenomena are less likely when taking synthetic corticosteroids, unless they are used in high doses). With long-term use of high doses of Betaspan® Depot, the risk of developing arrhythmia and hypokalemia should consider the need to prescribe potassium-containing drugs and a diet with limited salt. All corticosteroids enhance calcium excretion. When using Betaspan® Depot simultaneously with cardiac glycosides or drugs that affect the electrolyte composition of plasma, monitoring of the water-electrolyte balance is required. Use acetylsalicylic acid with caution in combination with Betaspan® Depot for hypoprothrombinemia. Caution must be exercised when using GCS in elderly patients; in patients with renal or hepatic failure, diverticulitis, active or latent gastric and/or intestinal ulcers or the presence of recently created intestinal anastomoses, osteoporosis, confirmed or suspected parasitic infections (for example, strongyloidiasis). Symptoms of peritoneal irritation or reduction in pain due to perforation of the walls of the stomach or intestines may be minimal or absent in patients receiving GCS. GCS should be used with caution in patients with hypothyroidism or myasthenia gravis. Cases of Kaposi's sarcoma have been reported in patients receiving corticosteroids; discontinuation of this therapy can lead to remission of the disease. With the use of corticosteroids, changes in sperm motility and number are possible. During long-term therapy with GCS, it is advisable to consider the possibility of switching from parenteral to oral use of GCS, taking into account the assessment of the benefit/risk ratio. Use in pediatrics Children undergoing drug therapy (especially long-term) should be under close medical supervision for possible growth retardation and the development of secondary adrenal insufficiency. Use in athletes Patients participating in competitions under the control of the World Anti-Doping Agency (WADA) should familiarize themselves with the WADA rules before starting treatment with the drug, since taking Betaspan® Depot may affect the results of doping control. During treatment with Betaspan® Depot, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.