A drug Depo-Medrol- GCS for injection - depot form
Methylprednisolone acetate has the same properties as methylprednisolone, but is less soluble and less actively metabolized, which explains its longer duration of action.
GCS, penetrating through cell membranes, form complexes with specific cytoplasmic receptors. Then these complexes penetrate the cell nucleus, bind to DNA (chromatin) and stimulate the transcription of mRNA and the subsequent synthesis of various proteins (including enzymes), which explains the effect of GCS when used systemically. GCS not only have a significant effect on the inflammatory process and the immune response, but also affect carbohydrate, protein and fat metabolism. They also have effects on the cardiovascular system, skeletal muscles and the central nervous system.
Effect on inflammation and immune response
Most indications for the use of GCS are due to their anti-inflammatory, immunosuppressive and antiallergic properties. Thanks to these properties, the following therapeutic effects are achieved: reducing the number of immunoactive cells in the inflammation site; decreased vasodilation; stabilization of lysosomal membranes; inhibition of phagocytosis; decreased production of prostaglandins and related compounds.
A dose of 4.4 mg methylprednisolone acetate (4 mg methylprednisolone) has the same anti-inflammatory effect as 20 mg hydrocortisone.
Methylprednisolone has only minor mineralocorticoid activity (200 mg methylprednisolone is equivalent to 1 mg deoxycorticosterone).
Effect on carbohydrate and protein metabolism
GCS have a catabolic effect on proteins. The released amino acids are converted into glucose and glycogen during gluconeogenesis in the liver. Glucose uptake in peripheral tissues is reduced, which can lead to hyperglycemia and glycosuria, especially in patients at risk of developing diabetes mellitus.
Effect on fat metabolism
GCS have a lipolytic effect, which primarily manifests itself in the extremities. GCS also enhance lipogenesis, which is most pronounced in the chest, neck and head. All this leads to the redistribution of fat deposits.
The maximum pharmacological activity of GCS does not appear at the peak of plasma concentration, but after it, therefore, their effect is primarily due to the effect on enzyme activity. Pharmacokinetics
Methylprednisolone acetate is hydrolyzed by serum cholinesterases to form an active metabolite. In the human body, methylprednisolone forms a weak, dissociable bond with albumin and transcortin. About 40-90% of methylprednisolone is in a bound state. Due to the intracellular activity of GCS, a pronounced difference is revealed between plasma T1/2 and pharmacological T1/2. Pharmacological activity persists even when the concentration of methylprednisolone in the blood is no longer determined.
The duration of the anti-inflammatory activity of GCS is approximately equal to the duration of suppression of the hypothalamic-pituitary-adrenal (HPA) system.
After intramuscular administration of the drug at a dose of 40 mg/ml, Cmax in the blood serum was achieved on average after 7.3±1 hours (Tmax) and averaged 1.48±0.86 mcg/100 ml (T1/2 = 69.3 hours). After a single intramuscular injection of 40-80 mg of methylprednisolone acetate, the duration of suppression of the HPA system ranged from 4 to 8 days.
After intra-articular injection of 40 mg into each knee joint (total dose = 80 mg), serum Cmax was achieved after 4-8 hours and was approximately 21.5 mcg/100 ml. The entry of methylprednisolone into the systemic circulation from the joint cavity persisted for approximately 7 days, which is confirmed by the duration of suppression of the HPA system and the results of determining the concentrations of methylprednisolone in the serum.
Metabolism of methylprednisolone occurs in the liver, and this process is qualitatively similar to that for cortisol. The main metabolites are 20-β-hydroxymethylprednisolone and 20-β-hydroxy-6-α-methylprednisone. Metabolites are excreted in the urine in the form of glucuronides, sulfates and unconjugated compounds. These conjugation reactions occur primarily in the liver and partly in the kidneys.
Indications for use
Depo-Medrol should be used only as symptomatic treatment, with the exception of some endocrine disorders, for which they are used as replacement therapy.A. IM APPLICATION
Depo-Medrol is not used to treat acute life-threatening conditions. If a rapid hormonal effect of maximum intensity is required, then highly soluble methylprednisolone sodium succinate (SOLU-MEDROL) is prescribed intravenously.
If it is not possible to carry out oral therapy with GCS, then intramuscular use of the drug is indicated for the following diseases:
1. Endocrine diseases: primary and secondary adrenal insufficiency (drugs of choice - hydrocortisone or cortisone; if necessary, in combination with mineralocorticoids, especially in pediatric practice); acute adrenal insufficiency (drugs of choice are hydrocortisone or cortisone; it may be necessary to add mineralocorticoids); congenital adrenal hyperplasia; hypercalcemia due to cancer; subacute thyroiditis.
2. Rheumatic diseases.
As an additional agent for maintenance therapy (non-steroidal anti-inflammatory drugs, kinesiotherapy, physiotherapy, etc.) and for short-term use (to remove the patient from an acute condition or during an exacerbation of the process) for the following diseases: psoriatic arthritis; ankylosing spondylitis.
For the following diseases, the drug should be used in situ whenever possible: post-traumatic osteoarthritis; synovitis in osteoarthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis (in some cases, low-dose maintenance therapy may be required); acute and subacute bursitis; epicondylitis; acute nonspecific tenosynovitis; acute gouty arthritis.
3. Collagenoses. During an exacerbation or in some cases as maintenance therapy for the following diseases: systemic lupus erythematosus; systemic dermatomyositis (polymyositis); acute rheumatic myocarditis.
4. Skin diseases: pemphigus; malignant exudative erythema (Stevens-Johnson syndrome); exfoliative dermatitis; mycosis fungoides; bullous dermatitis herpetiformis (drug of choice is sulfone, systemic use of GCS is adjuvant).
5. Allergic conditions: for the control of the following severe and disabling allergic conditions that cannot be cured by conventional methods: status asthmaticus; contact dermatitis; atopic dermatitis; serum sickness; seasonal or year-round allergic rhinitis; drug allergies; reactions to transfusions and administration of drugs such as urticaria; acute non-infectious laryngeal edema (drug of choice - epinephrine).
6. Ophthalmological diseases. Severe acute and chronic allergic and inflammatory processes with eye damage, such as uveitis and inflammatory eye diseases that do not respond to the use of local corticosteroids.
7. Diseases gastrointestinal tract. To remove a patient from a critical condition with the following diseases: ulcerative colitis (systemic therapy); Crohn's disease (systemic therapy).
8. Respiratory diseases: symptomatic sarcoidosis; berylliosis; focal or disseminated pulmonary tuberculosis (used in combination with appropriate anti-tuberculosis chemotherapy); Loeffler's syndrome, which cannot be treated with other methods; aspiration pneumonitis.
9. Hematological diseases: acquired (autoimmune) hemolytic anemia; secondary thrombocytopenia in adults; erythroblastopenia (thalassemia major); congenital (erythroid) hypoplastic anemia.
10. Oncological diseases. As palliative therapy for the following diseases: leukemia and lymphoma in adults.
11. Edema syndrome. For the induction of diuresis or treatment of proteinuria in nephrotic syndrome, idiopathic type or due to systemic lupus erythematosus.
12. Nervous system: multiple sclerosis in the acute phase.
13. Other indications for use: tuberculous meningitis with subarachnoid block or threatened block, in combination with appropriate anti-tuberculosis chemotherapy; trichinosis with lesions nervous system or myocardium.
B. INTRA-ARTICULAR, PERIARTICULAR, INTRABURSAL APPLICATION AND INTRODUCTION TO SOFT TISSUE.
As an auxiliary therapy for short-term use (to remove the patient from an acute condition or during an exacerbation of the process) for the following diseases: synovitis in osteoarthritis; rheumatoid arthritis; acute and subacute bursitis; acute gouty arthritis; eicondylitis; acute nonspecific tenosynovitis.
B. INTRODUCTION TO THE PATHOLOGICAL FOCUS
Keloid scars and localized foci of inflammation in: lichen planus (Wilson); psoriatic plaques; granuloma annulare; simple chronic lichen (neurodermatitis); discoid lupus erythematosus; diabetic lipodystrophy; alopecia areata.
Also effective for cystic tumors or tendon aponeurosis (tendon sheath cysts).
Mode of application
Methods of using the drug Depo-Medrol:- i/m;
- intra-articular, periarticular, intrabursal or soft tissue injection;
- introduction into the pathological focus.
INTRODUCTION TO THE PATHOLOGICAL SITE TO ACHIEVE A LOCAL EFFECT
Despite the fact that drug treatment Depo-Medrol leads to a decrease in the symptoms of the disease, it does not affect the cause of the inflammatory process, therefore it is necessary to carry out the usual therapy for each specific disease.
Rheumatoid arthritis and osteoarthritis. The dose for intra-articular administration depends on the size of the joint, as well as the severity of the patient’s condition.
For chronic conditions, the number of injections may vary from one to five or more per week, depending on the degree of improvement achieved after the first injection.
Procedure. Before performing an intra-articular injection, it is recommended to evaluate the anatomy of the affected joint. For a full anti-inflammatory effect, it is important that the injection is carried out into the synovial cavity. It is necessary to follow the rules of asepsis and antisepsis in the same way as during lumbar puncture. A sterile 20-24 G needle (attached to a dry syringe) is quickly inserted into the synovial cavity. The method of choice is infiltration anesthesia with procaine. To control the entry of the needle into the joint cavity, a few drops of intra-articular fluid are aspirated. When choosing the injection site, which is individual for each joint, the proximity of the synovial cavity to the surface (as close as possible), as well as the passage of large vessels and nerves (as far as possible), is taken into account. The needle remains in place, the syringe with the aspirated liquid is removed and replaced with another syringe containing required amount drug Depo-Medrol. You should then slowly pull the plunger toward you and aspirate the synovial fluid to ensure that the needle is still in the synovial cavity. After the injection, you should make a few light movements in the joint, which helps mix the suspension with the synovial fluid. The injection site is covered with a small sterile bandage.
The drug can be injected into the knee, ankle, elbow, shoulder, metacarpophalangeal, interphalangeal and hip joints. Sometimes there are difficulties with insertion into the hip joint, since large blood vessels must be avoided. Injections are not made into the following joints: anatomically inaccessible joints, for example, intervertebral joints, including the sacroiliac joint, which lacks a synovial cavity. The failure of therapy is most often the result of an unsuccessful attempt to penetrate the joint cavity. When the drug is introduced into surrounding tissues, the effect is insignificant or absent altogether. If therapy does not produce positive results in cases where entry into the synovial cavity is beyond doubt, as confirmed by aspiration of intra-articular fluid, repeated injections are usually useless.
Local therapy does not affect the process underlying the disease, so complex therapy should be carried out, including basic anti-inflammatory therapy, physiotherapy and orthopedic correction. After intra-articular administration of GCS, care should be taken not to overload joints in which symptomatic improvement has been noted in order to avoid more severe damage to the joint compared to what was before the start of GCS therapy. GCS should not be injected into unstable joints. In some cases, repeated intra-articular injections can lead to joint instability. In some cases, it is recommended to carry out x-ray control to identify damage. If a local anesthetic is used before administering Depo-Medrol, you should carefully read the instructions for use of this anesthetic to ensure all necessary precautions are followed.
Bursitis. After treating the area around the injection site with a suitable antiseptic, local infiltration anesthesia is performed with a 1% procaine solution. A 20-24 G needle is placed on a dry syringe, which is inserted into the joint capsule, and then the liquid is aspirated. The needle is left in place, and the syringe with the aspirated liquid is removed and a syringe containing the required dose of the drug is installed in its place. After the injection, the needle is removed and a bandage is applied.
Tendon sheath cyst, tendonitis, epicondylitis. When treating conditions such as tendinitis or tenosynovitis, care must be taken to ensure that the suspension is injected into the tendon sheath and not into the tendon tissue. The tendon can be easily palpated by running your hand along it. When treating conditions such as epicondylitis, the most painful area should be identified and the suspension should be injected into it using the creeping infiltration method. For tendon sheath cysts, the suspension is injected directly into the cyst. In many cases, it is possible to achieve a significant reduction in the size of the cystic tumor and even its disappearance after a single injection of the drug. Each injection should be done in compliance with the rules of asepsis and antiseptics (treating the skin with a suitable antiseptic).
The dose is selected depending on the nature of the process and is 4-30 mg. In case of relapses or chronic course of the process, repeated injections may be required.
Skin diseases. After treating the skin with a suitable antiseptic, for example, 70% alcohol, 20-60 mg of the suspension is injected into the lesion. For a large affected area, a dose of 20-40 mg is divided into several parts and injected into different areas of the affected surface. When administering the drug, care should be taken to avoid whitening of the skin, which may subsequently lead to peeling. Usually 1-4 injections are performed, the interval between injections depends on the type of pathological process and on the duration of the period of clinical improvement achieved after the first injection.
IM INTRODUCTION TO ACHIEVE A SYSTEMIC EFFECT
The dose of the drug for intramuscular administration depends on the disease being treated. To obtain a long-term effect, calculate the weekly dose by multiplying the daily oral dose by 7, and administer it as one intramuscular injection.
The dose should be selected individually, taking into account the severity of the disease and the patient's response to therapy. In children (including infants), a lower dose is used, which is chosen primarily based on the severity of the disease, rather than using constant regimens calculated on the basis of age or body weight. The course of treatment should be as short as possible. Treatment is carried out under constant medical supervision.
Hormone therapy is an addition to conventional therapy, but does not replace it. The dose of the drug should be reduced gradually, and the drug should also be discontinued gradually if it was administered for longer than several days. The main factors determining the choice of dose are the severity of the disease, prognosis, expected duration of the disease, and the patient's response to therapy. If a period of spontaneous remission occurs in a chronic disease, treatment should be interrupted. For long-term therapy, routine laboratory research, such as a general urine test, determination of blood glucose concentration 2 hours after a meal, determination of blood pressure, body weight, and chest X-ray examination should be performed regularly at certain intervals. In patients with a history of gastric and duodenal ulcers or severe dyspepsia, it is advisable to undergo an X-ray examination of the upper gastrointestinal tract.
For patients with adrenogenital syndrome, it is enough to administer 40 mg intramuscularly once every 2 weeks. For maintenance therapy in patients with rheumatoid arthritis, the drug is administered intramuscularly at a dose of 40-120 mg once a week. The usual dose for systemic GCS therapy in patients with skin diseases, which allows achieving a good clinical effect, is 40-120 mg IM once a week for 1-4 weeks. In acute severe dermatitis caused by the poison contained in ivy, it is possible to eliminate the symptoms within 8-12 hours after a single intramuscular injection of 80-120 mg. For chronic contact dermatitis, repeated injections at intervals of 5-10 days may be effective. For seborrheic dermatitis, to control the condition, it is enough to administer 80 mg once a week.
After intramuscular administration of 80-120 mg to patients with bronchial asthma, symptoms disappear within 6-48 hours, and the effect persists for several days or even 2 weeks. In patients with allergic rhinitis (hay fever), an intramuscular injection of 80-120 mg can also eliminate the symptoms of acute rhinitis within 6 hours, with the effect lasting from several days to 3 weeks.
If the disease for which therapy is aimed also develops symptoms of stress, the dose of the suspension should be increased. To obtain a quick maximum effect, intravenous administration of methylprednisolone sodium succinate, characterized by rapid solubility, is indicated.
Side effects
Listed below side effects typical for all GCS when administered parenterally. Inclusion on this list does not mean that these effects are specific to this drug.FOR INTRAMUSCULAR APPLICATION
Disturbances of water and electrolyte balance: sodium retention, chronic heart failure in patients with a corresponding predisposition, increased blood pressure, fluid retention, hypokalemia, hypokalemic alkalosis.
When using synthetic derivatives such as methylprednisolone acetate, mineralocorticoid effects are less common than when using cortisone or hydrocortisone.
Musculoskeletal: “steroid” myopathy, muscle weakness, osteoporosis, pathological fractures, vertebral compression fractures, aseptic necrosis of the femoral and humeral heads, tendon ruptures, especially the Achilles tendon, decreased muscle mass.
Gastrointestinal/liver: peptic ulcer (possible perforation and bleeding), gastric bleeding, pancreatitis, ulcerative esophagitis, intestinal perforation.
A temporary and moderate increase in the activity of transaminases and alkaline phosphatase in the serum may be observed, but this is not associated with any clinical syndrome and is reversible when the drug is discontinued.
From the skin: deterioration of wound healing, petechiae and ecchymosis, thinning and fragility of the skin.
Metabolic: negative nitrogen balance due to protein catabolism.
Neurological: increased intracranial pressure, pseudotumor cerebri, mental disorders, seizures.
Endocrine: menstrual irregularities, development of Itsenko-Cushing syndrome, suppression of the hypothalamic-pituitary-adrenal system (HPA), decreased glucose tolerance, manifestation of latent diabetes mellitus, increased need for insulin or oral hypoglycemic drugs in patients with diabetes, growth retardation in children.
Ophthalmologic: posterior subcapsular cataract, increased intraocular pressure, exophthalmos.
Immune system: blurred clinical picture of infectious diseases, activation of latent infections, infections caused by opportunistic pathogens, hypersensitivity reactions, including anaphylaxis, possible suppression of reactions during skin tests.
ADDITIONAL REACTIONS ASSOCIATED WITH PARENTERAL GCS THERAPY: cases of blindness associated with local administration of the drug into pathological lesions located in the face and head; anaphylactic or allergic reactions; hyperpigmentation or hypopigmentation; atrophy of the skin and subcutaneous tissue; post-injection exacerbation after injection into synovial fluid; arthropathy according to Charcot type; infection of the injection site due to non-compliance with the rules of asepsis and antisepsis; sterile abscess.
Contraindications
Contraindications to the use of the drug Depo-Medrol are: intrathecal administration; intravenous administration; systemic fungal infections; established hypersensitivity to any component of the drug.With caution: for eye damage caused by a virus herpes simplex; as this may lead to corneal perforation; with ulcerative colitis, if there is a threat of perforation, development of an abscess or other purulent infection, as well as with diverticulitis; in the presence of fresh intestinal anastomoses; with active or latent peptic ulcer; renal failure; diabetes mellitus; arterial hypertension; osteoporosis; myasthenia gravis, when GCS are used as primary or additional therapy; with a history of mental disorders; in children.
Pregnancy
Adequate impact studies Depo-Medrol on reproductive function in humans has not been carried out, therefore, when deciding whether to prescribe GCS to pregnant, nursing mothers, or women who may become pregnant, the potential benefit of using the drug for the mother (future mother) should be weighed against the possible risk to the fetus or child. GCS should be prescribed during pregnancy strictly according to indications.GCS easily penetrate the placenta. Children born to mothers who received fairly high doses of corticosteroids during pregnancy should be closely monitored so that signs of adrenal insufficiency can be identified in a timely manner. The effect of GCS on the course and outcome of labor is unknown. GCS are allocated in breast milk.
Interaction with other drugs
Due to the possibility of pharmaceutical incompatibility, the drug Depo-Medrol should not be diluted or mixed with other solutions.The following examples of drug interactions may have important clinical significance. The combined use of methylprednisolone and cyclosporine causes mutual inhibition of the metabolism of these drugs, so it is likely that side effects symptoms associated with the use of each of these drugs as monotherapy may occur more frequently when used together. Cases of seizures have been reported when these drugs were used together. Microsomal enzyme inducers such as phenobarbital, phenytoin and rifampicin may increase the clearance of methylprednisolone, which may require increasing the drug dose to obtain the desired effect.
Drugs such as oleandomycin and ketoconazole can inhibit the metabolism of GCS, so it is necessary to select the dose of GCS to prevent overdose. Methylprednisolone may increase the clearance of acetylsalicylic acid given in high doses over a long period, which may result in decreased serum salicylate concentrations or increase the risk of salicylate toxicity when methylprednisolone is discontinued. In patients with hypoprothrombinemia, acetylsalicylic acid should be prescribed in combination with GCS with caution. Methylprednisolone has a variety of effects on the action of indirect anticoagulants. Both increased and decreased effects of indirect anticoagulants taken concomitantly with methylprednisolone have been reported. To maintain the required effect of the indirect anticoagulant, constant determination of coagulation parameters (including the international normalized ratio) is necessary.
Overdose
Clinical acute overdose syndrome Depo-Medrol does not exist. Repeated frequent use of the drug (daily or several times a week) over a long period can lead to the development of Cushing's syndrome. You should stop using the drug; but it must be taken into account that its abrupt cancellation can lead to “rebound” adrenal insufficiency. No specific treatment is required.Storage conditions
A drug Depo-Medrol store at a temperature of 15-25°C, out of the reach of children.Release form
Suspension for injection is white.Packaging: 2 ml - bottles (1) - cardboard packs.
Compound
1 ml suspension for injection Depo-Medrol contains: methylprednisolone acetate 40 mg.Excipients: macrogol 3350 29 mg/ml, sodium chloride 8.7 mg/ml, myristyl-γ-picolinium chloride 200 μg/ml, sodium hydroxide (to bring the pH to 3.5-7), hydrochloric acid (to bring the pH to 3.5-7 ), water for up to 1 ml.
1 ml (1 amp.) suspension for injection Depo-Medrol contains: methylprednisolone acetate 40 mg 80 mg.
Excipients: macrogol 3350 29 mg/ml, sodium chloride 8.7 mg/ml, myristyl-γ-picolinium chloride 200 μg/ml, sodium hydroxide (to bring the pH to 3.5-7), hydrochloric acid (to bring the pH to 3.5-7 ), water for up to 1 ml.
Excipients: sodium chloride, macrogol 3350, myristyl-γ-picolinum chloride, sodium hydroxide, hydrochloric acid , water.
Release form
Depo-Medrol is a white suspension.
1 or 2 ml of such a suspension in a bottle; one bottle per package.
pharmachologic effect
Glucocorticoid.
Pharmacodynamics and pharmacokinetics
Slows release interleukin first and second types, gamma interferon from macrophages and lymphocytes. Renders antiallergic, anti-inflammatory, desensitizing, antishock, immunosuppressive And antitoxic action. Slows release adrenocorticotropic hormone And beta-lipotropin , does not lower content beta-endorphin . Suppresses secretion follicle-stimulating hormone And thyroid-stimulating hormone . Increases the excitability of the nervous system and the number of red blood cells, reduces the number of eosinophils and lymphocytes. Interacts with cytoplasmic receptors, penetrates the nucleus, and induces protein synthesis.
After intramuscular administration, maximum serum concentration occurs after 7.5 hours. After intra-articular injection of 40 mg into both knee joints, maximum serum concentrations are achieved within 5-8 hours. The release of the drug into the general bloodstream from the joint continues for a week.
Metabolism occurs in the liver. Excreted in urine as sulfates, glucuronides And unconjugated compounds .
Indications for use
- Adrenal insufficiency, adrenal hyperplasia (congenital), hypercalcemia oncological etiology.
- , pemphigus, exfoliative dermatitis, collagenosis, bullous herpetiformis, severe forms of multiform erythema , severe forms.
- , berylliosis , Loeffler's syndrome , (as part of combination therapy).
- Thrombocytopenic purpura, acute leukemia, hemolytic anemia, erythroblastopenia, hypoplastic anemia, secondary thrombocytopenia.
- Nephrotic syndrome.
- Ulcerative colitis.
- Multiple sclerosis , cerebral edema, tuberculous .
- Organ transplantation.
- Diseases of the musculoskeletal system of various origins.
Contraindications
- Intravenous administration.
- System mycoinfections .
- to the drug.
- For intra-articular injection and injection into the lesion: pathological bleeding, arthroplasty , intra-articular fracture, infectious process in the joint, systemic infectious disease, absence of inflammation in the joint, aseptic necrosis bones.
Side effects
- From the hormonal side: changes in glucose tolerance, Itsenko-Cushing syndrome, adrenal hypofunction , developmental delay in children.
- From the digestive system: vomiting, nausea, bleeding or intestinal perforation, change in appetite.
- From the circulatory system: bradycardia , ECG changes, increased blood pressure, hypercoagulation, .
- From the senses: loss of vision, exophthalmos, posterior subcapsular , increased intraocular pressure, the appearance of secondary eye infections.
- From the nervous system: disorientation, delirium, hallucinations, bipolar disorder, paranoia, , nervousness, headache, , convulsions .
- Metabolism: hypocalcemia , weight gain, increased sweating, hypernatremia
- From the musculoskeletal system: slowing down of growth processes in children, rupture of muscle tendons, atrophy .
- Skin: slow wound healing, ecchymoses, petechiae , change in pigmentation, .
- Allergic reactions: itching, rash,.
- Others: leukocyturia , exacerbation of infections, withdrawal syndrome, burning, pain, scarring, infections at the injection site.
- With intra-articular injection - increased pain in the joint.
Depo-Medrol, instructions for use (Method and dosage)
According to the instructions, Depo-Medrol is administered periarticularly, intraarticularly, into the pathological focus, intrabursally; instillation into the rectum.
Children under 18 years of age: with adrenal insufficiency
- 0.14 mg per kg of weight or 4 mg per square meter body surface per day after 2 days; for other indications - 0.14-0.836 mg per kg of weight or 4.15-25 mg per square meter of body surface after 12-24 hours.
Adults - intramuscularly 40-120 mg per day, duration of treatment - up to a month.
At shocked
And transplant rejection
: 5-20 mg/kg every 0.5-24 hours.
Intra-articular - 6-80 mg: large joints - 41-80 mg, medium - 11-40 mg, small - 6-10 mg.
When administered into the pleural or abdominal cavity - up to 100 mg, when administered epidurally - up to 80 mg, into the area of skin damage - 30-60 mg; with enema – 50-120 mg. Depo-Medrol should be discontinued gradually.
GCS inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
Suppresses the release of ACTH and beta-lipotropin by the pituitary gland, but does not reduce the concentration 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 erythropoietins).
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, Pg, leukotrienes, which contribute to inflammation, allergies, etc.
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 Na+ and water in the body, stimulates the excretion of K+ (MCS activity), reduces the absorption of Ca2+ from the gastrointestinal tract, “washes out” Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys.
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 allergic mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changing the body's immune 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.
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin1, interleukin2; 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.
In COPD, it 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.
5 times more active than hydrocortisone in anti-inflammatory action. After intramuscular administration of 80 mg of the drug, its effect continues for 12 hours, and a suppressive effect on plasma cortisone levels is observed for another 17 days.
Latin name: Depo-Medrol
ATX code: H02ABO4
Active substance: Methylprednisolone
Manufacturer: Pfizer Menufecturing
Belgium, Belgium/USA
Conditions for dispensing from a pharmacy: On prescription
Price: from 70 to 100 rub.
Composition of the drug
“Depo-Medrol” includes the active substance - methylprednisolone acetate, as well as excipients, which include sodium chloride salt, polyethylene glycol, and myristyl-gamma-picolinic acid chloride.
Medicinal properties
Since the active substance of the drug is methylprednisolone, that is, a compound of hormonal nature - a glucocorticosteroid, the main property that Depo-Medrol has is its anti-inflammatory effect. In addition, the drug suppresses immunological and allergic reactions in the patient’s body. This is due to its inhibitory effect on cells that produce pro-inflammatory factors and take part in immunological and allergic reactions.
Once Depo-Medrol is in the blood serum, specific enzymes called cholinesterases hydrolyze methylprednisolone acetate and the active compound is formed. Methylprednisolone binds to proteins: albumin and transcortin. A drug can be active even when it can no longer be detected in the blood. The half-life of the drug (the time during which its concentration is halved) is 69.3 hours.
Depo-Medrol is metabolized intrahepatically. The main metabolite of methylprednisolone is 20-β-hydroxymethylprednisolone and 20-β-hydroxy-6-α-methylprednisone. The latter are excreted in urine in the form of the following substances:
- Glucuronides
- Sulfates
- Unconjugated compounds.
The conjugation reaction with the formation of glucuronides and sulfates occurs not only in the liver, but also in the renal apparatus.
Indications for use
“Depo-Medrol”, like other glucocorticosteroids, is used mainly as medicine symptomatic use (cannot influence the cause of the disease). Sometimes it can be prescribed as a replacement treatment for adrenal hormones that are not produced independently in the patient’s body.
The most common reasons for prescribing methylprednisolone are:
1) Diseases of the endocrine system
- Chronic insufficiency of the adrenal cortex, which normally produces glucocorticosteroids
- Acute adrenal insufficiency
- Subacute thyroiditis
- Congenital anomalies of the adrenal glands
2) Rheumatic pathologies
- Ankylosing spondylitis
- Rheumatoid arthritis
- Systemic lupus erythematosus
- Systemic form of dermatomyositis
- Psoriatic arthritis
3) Skin diseases
- Pemphigus
- Erythema maligna
- Exfoliative dermatitis
4) Allergic pathology
- Bronchial asthma
- Atopic and contact dermatitis
- Allergic rhinitis: year-round or seasonal
- Violent allergic reactions
- Serum sickness
5) Conditions requiring suppression of immune system cells
- Condition after transplantation
- Lymphogranulomatosis
- Leukemoid conditions.
The average price is from 70 to 100 rubles.
Release forms
Depo-Medrol is produced in the form of an injection suspension, which is usually packaged in 1 or 2 ml. One cardboard pack contains 1 bottle. Injection of a drug allows you to quickly achieve a systemic effect from the drug (it affects the entire body at once, and not just locally at the point where it was directly injected).
The drug can also be injected into the joint cavity, into a painful area or soft tissue to achieve a local anti-inflammatory effect. The lack of systemic exposure in such cases avoids serious adverse systemic reactions.
Methods of application
When administering the drug intramuscularly, in order to achieve a systemic effect, the patient may be prescribed various doses. This is usually determined by the severity of the patient’s condition, his weight, as well as the reaction of the individual person’s body to Depo-Medrol. Sometimes the daily dose is multiplied by seven and the weekly dosage is administered once.
The doses that patients usually need are as follows:
- For adrenal insufficiency – 40 mg intramuscularly once every 2 weeks
- For rheumatoid arthritis - intramuscularly 1 time per week at a dose of 40-120 mg
- For skin diseases - intramuscularly once a week for 2-4 weeks at a dose of 40-120 mg
- Skin lesions from poison ivy or hogweed - single dose of 80-120 mg
- For a prolonged attack of bronchial asthma, also called status asthmaticus, administer 80-120 mg once
- Local therapy for the treatment of joints - depending on the size of the joint, intra-articular administration in a dose of 4 to 80 mg is possible
- Local therapy for the treatment of ulcerative colitis is injection of the drug into the rectum 3-7 times a week in doses of 40-120 mg.
Pregnancy and breastfeeding
During pregnancy, as well as during breastfeeding a newborn, it is necessary to use the drug with great caution; it is advisable to completely avoid prescribing such drugs.
The child, along with milk or through the vessels of the child's place, will receive methylprednisolone, which may have consequences for him in the form of suppression of the developing normal immunity, adrenal insufficiency, corticosteroid diabetes, and an imbalance of the ionic composition of the blood. Therefore, if treatment is necessary, you should stop breastfeeding.
Contraindications
“Depo-Medrol” is contraindicated for intravenous use, for administration to patients suffering from fungal tissue infections, for administration to patients known to be hypersensitive to the components of the drug: they can give a violent allergic reaction, intrathecally - into the cerebrospinal fluid directly.
It is also worth showing the lion's share of caution when prescribing the drug to patients with diverticulitis, herpes viral eye damage, purulent infections, ulcerative colitis with deep defects in the intestinal walls, diabetes mellitus, renal failure, myasthenia gravis, hypertension, as well as those who have recently undergone operations with the formation of intestinal anastomoses.
Interactions with other drugs
It is better not to use Depo-Medrol with the following medications:
- Cyclosporine: has a mutual inhibitory effect with methylprednisolone, summing up the side effects from the use of each of them; convulsions have occurred in some patients
- Phenobarbital, rifampicin, phenytoin: are activators of liver enzymes, increase the excretion of methylprednisolone, and therefore may require an increase in its dose for effective treatment
- Ketoconazole, oleandomycin: inhibit the transformation of methylprednisolone in the patient’s body
- Acetylsalicylic acid: when combined with methylprednisolone, it is eliminated faster, and therefore, after discontinuation of Depo-Medrol, its overdose may occur
- Indirect anticoagulants: drugs that interfere with blood clotting processes in combination with methylprednisolone can either weaken or enhance their own effect, and therefore blood counts must be carefully monitored.
Side effects
If Depo-Medrol is used systemically, it is characterized by all the side effects of glucocorticosteroids, which include the following:
- Imbalance of the ionic composition of the blood: hypernatremia, hypokalemia, alkalosis - alkalization of the blood
- Steroid diabetes mellitus
- Heart failure due to fluid retention
- Muscle weakness associated with potassium loss
- Osteoporosis and fractures associated with bone loss of calcium
- The occurrence of ulcerative defects in the stomach
- Petechial hemorrhages
- Upper type obesity: redistribution of adipose tissue to the areas of the face, abdomen, chest and upper limbs.
- Increased susceptibility to infectious diseases
- Cataract
- Adrenal insufficiency
- Discrepancy in the menstrual cycle
- Withdrawal syndrome: if Depo-Medrol is stopped abruptly rather than gradually, the symptoms it is fighting will intensify many times over.
Overdose
There is no acute picture that develops with repeated and constant excess of normal doses of the drug. However, over time, all its characteristic side effects will develop. Then there will be a need to significantly reduce doses or discontinue the medication.
Conditions and shelf life
Depo-Medrol should be stored in a place that is inaccessible to children, at a temperature of 15-25 degrees. Its shelf life is 5 years.
Analogs
There are analogue drugs of Depo-Medrol, listed below:
Pfizer, Italy
Price from 150 to 800
Tablets of 16 mg, 50 in one package. Has anti-inflammatory, immunosuppressive and antiallergic effects
pros
- Taking pills eliminates injection complications
- Easier to control dosages
Minuses
- Price category
- Irritant effect of the tablet on the gastric mucosa during administration.
«
Orion Corporation, Finland
Price from 180 to 350 rub.
Hormonal drug. Release form: lyophilisate used for the preparation of a solution IM and IV 250 mg/ml, 1 in one package.
pros
- Admissibility of intravenous administration
- Speed of effect
Minuses
- Labor intensity of application
- Contraindicated during pregnancy.
«
Pfizer, USA
Price from 450 to 1050
Glucocorticosteroid. It relieves inflammation, reduces sensitization, eliminates allergic reactions, weakens the immune response, regulates metabolism, improves the functioning of the circulatory system, skeletal muscles, brain and spinal cord.
pros
- Quite a large dose in 1 bottle
- High efficiency
Minuses
- Large list of side effects
- Systemic treatment with Solu-Medrol suppresses human immunity.
Depo-Medrol is a drug related to GCS (glucocorticosteroids). Before use, you should consult a specialist.
Depo-Medrol is a drug related to GCS (glucocorticosteroids).
Release form, composition and packaging
Suspension for injection. 1 ml contains 40 mg of active substance, which is methylprednisolone acetate. The drug is in bottles. Each cardboard box contains 1 bottle.
pharmachologic effect
GCS penetrate through the membrane into the cytoplasm and connect with cytoplasmic receptors. They affect the site of inflammation and the immune response, and also have direct influence for the metabolism of proteins, fats and carbohydrates. The drug is metabolized to form an active metabolite.
The drug can affect the central nervous, circulatory systems and skeletal muscles. The effect of the drug can be described as immunosuppressive and antiallergic. It reduces vasodilation, slows down the process of phagocytosis, reduces the number of immunoactive cells in the pathological area, reduces the synthesis of prostaglandins and compounds similar in structure and function.
Due to GCS therapy, fat deposits in the patient's body may be atypically redistributed.
The active component weakly binds to albumin and transcortin. Plasma and pharmacological half-lives vary significantly. The effect of the drug lasts even when it is not possible to fix the active substance in the blood.
After intra-articular injection into the cavity knee joint the maximum concentration in blood plasma can be recorded after approximately 4-8 hours. The drug is also administered intramuscularly.
Metabolism occurs in the liver, and it is similar in its characteristics to the breakdown of cortisol.
Indications for use of Depo-Medrol
Intramuscular administration of the drug is effective in treating the following disorders:
- subacute thyroiditis;
- adrenal insufficiency in acute form;
- hypercalcemia caused by cancer;
- violation of the production of cortisol by the adrenal glands, which is congenital in nature, their primary and secondary insufficiency;
- collagenoses;
- psoriatic arthritis;
- mycosis fungoides;
- pemphigus;
- allergic conditions;
- uveitis and inflammation in the eye that does not respond to the use of topical corticosteroids;
- ulcerative colitis and Crohn's disease;
- sarcoidosis;
- hemolytic anemia;
- leukemia and lymphosis;
- tuberculous meningitis (in combination with anti-tuberculosis treatment);
- multiple sclerosis in exacerbation;
- trichinosis leading to damage to the nervous system or myocardium.
Exposure by intra-articular injection is indicated in the presence of pathologies such as:
- arthritis in the acute stage;
- tenosynovitis;
- acute and subacute course of bursitis.
Injections into the site of pathology are used for plaques associated with psoriasis and granuloma annulare.
Application of Depo-Medrol
The dose for intra-articular administration depends on how intense the joint damage is and the size of the joint. The number of repeated injections after the first administration of the drug can range from 1 to 5, based on how productive the effect is.
If you have a skin disease, after cleansing the skin, you need to inject 20-60 mg of the drug into the site of the inflammatory process. More often than not, 1 to 4 injections are sufficient.
Intramuscular administration should be carried out under constant medical supervision. The dose is selected individually based on what pathology needs to be treated. The dose should be increased or decreased gradually depending on the patient's condition.
For the purpose of maintenance therapy for rheumatoid arthritis, the drug is used once a week in an amount of 40-120 mg. After intramuscular administration of 80-120 mg of the drug to patients with bronchial asthma, its symptoms begin to decrease after 6-48 hours.
Why can't it be administered epidurally?
This can cause bladder or bowel dysfunction, epileptic seizures, and headache.
Side effect
If the medicine is administered intramuscularly, the patient may experience such adverse reactions, such as muscle weakness, decreased muscle volume, fluid retention in the body, increased blood pressure, pancreatitis, intestinal perforation, peptic ulcer, convulsions and nervous disorders, skin fragility, increased intraocular pressure, menstrual irregularities, suppressed reactions to skin tests. The likelihood of developing latent type diabetes also becomes higher.
Parenteral GCS therapy can provoke a sterile abscess, allergic and anaphylactic manifestations, pigmentation pathologies, blindness (if the drug is injected into the head area near the eyes), infection of the injection site (if the rules of asepsis and antisepsis are not followed).
Long-term use of GCS can cause secondary infections, most often caused by fungi and viruses.
Contraindications to the use of Depo-Medrol
It is prohibited to take the medication for medicinal purposes if a person has health problems from the list below:
- systemic fungal infections;
- high sensitivity to one of the components of the drug.
The medicine cannot be administered intravenously or intrathecally (into the spine). The drug is prescribed with caution for diabetes mellitus, osteoporosis, eye damage, mental disorders, inflammatory process of diverticulum and ulcerative colitis, abscess or purulent infection, high blood pressure.
special instructions
If patients are treated with GCS at a dose that does not have an immunosuppressive effect, they can be immunized.
Use during pregnancy and breastfeeding
The effect of GCS on delivery has not been established. There may be a teratogenic effect on the fetus when using the medicine while pregnant. Children, born of women Those who received high doses of corticosteroids during pregnancy should be observed by a specialist. Since the active substance passes into breast milk, natural feeding should be stopped during the period of treatment with the medication.