Pharmacological action Depo-Medrol Injection:
Depo-Medrol GCS, inhibits the release of interleykina1, interleykina2, interferon gamma from lymphocytes and macrophages. Anti-inflammatory, antiallergic, desensitizing, antishock, anti-toxic and immunosuppressive effects. Inhibits the release of pituitary ACTH and beta-lipotropin but not reduces 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 – 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, including lipokortina, mediating cellular effects. Lipokortina inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperekisey, Pg, leukotrienes that contribute to inflammation, allergies and other protein metabolism: it reduces the amount of protein in the plasma (due to globulin) with an increase in the coefficient of albumin / globulin, albumin synthesis increases in liver and kidney, strengthens the protein catabolism in muscle tissue. Lipid metabolism: increased synthesis of fatty acids and triglycerides, redistributes fat (fat accumulation predominantly 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 of glucose from the liver into the blood, increases the activity and synthesis фосфоэнолпируваткарбоксилазы aminotransferases, resulting in the activation of gluconeogenesis. Water and electrolyte metabolism: Na + and delays the water in the body, stimulates the excretion of K + (ISS activity), reduces the absorption of Ca2 + from the gastrointestinal tract, “washes” Ca2 + from the bones, increases the excretion of Ca2 + by the kidneys. Anti-inflammatory effect associated with inhibition of eosinophil release of inflammatory mediators, inducing the formation lipokortina and reduce the number of mast cells that produce hyaluronic acid, with a decrease in the permeability of capillaries, stabilizing cell membranes and membrane organelles (especially lysosomal). Antiallergic effect is caused by suppression of synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances that reduce the number of circulating basophils, suppressing the development of lymphoid and connective tissue, reducing the number of T-and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to the mediators of allergy, inhibition of antibody production, changes in immune response. Antishock and anti-toxic effect associated with elevated blood pressure (by increasing the concentration of circulating catecholamines and restore sensitivity to adrenergic receptors, and vasoconstriction), decrease the permeability of the vascular wall, oxidant properties, activation of liver enzymes involved in the metabolism of endo-and xenobiotics. Immunosuppressive effect is due to inhibition of cytokine release (interleykina1, interleykina2, interferon gamma) from lymphocytes and macrophages. Inhibits the synthesis and secretion of ACTH and again – the synthesis of endogenous corticosteroids. Inhibits connective tissue reaction in the inflammatory process and reduces scarring. In COPD is mainly based on inhibition of inflammatory processes, inhibition or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosa of bronchial epithelium, deposition in the bronchial mucosa of circulating immune complexes, as well as braking erozirovaniya and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic bronchial small-and medium-sized to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus through oppression or reduce its production. 5 times more active on anti-inflammatory effects of hydrocortisone. After i / m administration of 80 mg of the drug its effect lasts for 12 hours, and the suppressive effect on plasma cortisol levels is observed even for 17 days.
Uses Depo-Medrol Injection:
Shock (Burn, Trauma, surgery, toxic, cardiogenic) the ineffectiveness of other treatment. Allergic reactions (acute, severe), blood transfusion shock, anaphylactic shock, anaphylactoid reactions. Cerebral edema (also against the background of a brain tumor or associated with surgery, radiation therapy, or head trauma). Asthma (severe), status asthmaticus. Systemic connective tissue disorders (SLE, rheumatoid arthritis). Acute adrenal insufficiency. Thyrotoxic crisis. Acute hepatitis, hepatic coma. Poisoning by cauterizing liquids (decrease inflammation and prevent scarring of the restrictions).
Contraindications Depo-Medrol Injection:
For short-term use of “real life” testimony only contraindication is hypersensitivity. For intraarticular administration: prior arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in joints and periarticular infections (including history), as well as general infectious disease, marked periarticular osteoporosis, no evidence of inflammation in the joints (so-called “dry” joint, such as osteoarthritis, without synovitis), marked bone destruction and deformation of the joint (marked joint space narrowing, ankylosis), instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint. C carefully. Parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with a patient) – Herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles, amoebiasis, strongyloidiasis (or suspected); system mycosis, active and latent tuberculosis. Application for serious infectious diseases is permissible only against specific therapy. Post-vaccination period (the period of duration of 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency (including AIDS or HIV infection). Gastrointestinal diseases – stomach ulcer and 12 duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis of the intestine, ulcerative colitis, with the threat of perforation or abscess formation, diverticulitis. Diseases of the cardiovascular system, including recent myocardial infarction (in patients with acute and subacute myocardial necrosis may spread the fire, slowing the formation of scar tissue and because of that – break the heart muscle), decompensated heart failure, hypertension, hyperlipidemia). Endocrine disease – diabetes mellitus (including breach of tolerance to carbohydrates), hyperthyroidism, hypothyroidism, Cushing’s disease. Severe chronic renal and / or liver failure, nefrourolitiaz. Hypoalbuminemia and conditions that predispose to its occurrence. Systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV cent.), Polio (with the exception of bulbar form of encephalitis), and Open-closure glaucoma, pregnancy, lactation. For intra-articular administration: the general plight of the patient, failure (or brevity) of the 2 previous injections (with the individual properties used SCS).
Side effects Depo-Medrol Injection:
The frequency and severity of side effects depend on the duration of application, size of the dosage used and adhering to the circadian rhythm of destination. With the endocrine system: impaired glucose tolerance, “steroid” diabetes or a manifestation of latent diabetes mellitus, adrenal suppression, Cushing’s syndrome (moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, male, striae) , delayed sexual development in children. Part of the digestive system: nausea, vomiting, pancreatitis, “steroid” stomach ulcers and 12 duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases – increased activity of “liver” enzymes and alkaline phosphatase. From the CCC: arrhythmia, bradycardia (up to heart failure), development (in predisposed patients) or increased severity of heart failure, ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute and subacute myocardial infarction – the spread of foci of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle. Nervous system disorders: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness, or restlessness, insomnia, dizziness, vertigo, pseudotumor cerebellum, headache, convulsions. From the senses: a sudden loss of vision (for parenteral administration in the head, neck, nasal cavities, the scalp may be the deposition of crystals of drug in the vessels of the eye), posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, the propensity to develop secondary bacterial , fungal or viral eye infections, corneal trophic changes, exophthalmos. From a metabolism: increased excretion of Ca2 +, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating. The resulting ISS-activity – fluid retention and Na + (peripheral edema), hypernatremia, gipokaliemichesky syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness, and fatigue). With the musculoskeletal system: slowing growth and ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rare – pathological fractures, aseptic necrosis of head of humerus and femur), muscle tendon rupture, “steroid” myopathy, reduced muscle mass (atrophy). For the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, skin thinning, hyper-or hypopigmentation, steroid acne, striae, susceptibility to the development of pyoderma and candidiasis. Allergic Reactions: generalized (skin rash, itching, and anaphylactic shock), local allergic reaction. Other: the development or exacerbation of infection (appearance of this side effect contribute jointly used immunosuppressive drugs and vaccinations), Pyuria, the syndrome of “cancellation”. Local for parenteral administration: burning, numbness, pain, paresthesia at the injection site, infection at the injection site, rarely – necrosis of surrounding tissue, scarring at the injection site, atrophy of skin and subcutaneous tissue in V / m, the introduction (especially the danger of introducing into the deltoid muscle .) With a / in the introduction: arrhythmia, “tides” of blood to the face, and convulsions. When intracranial introduction – nosebleeds. With intraarticular injection – increased pain in the joint.
Dosage and administration Depo-Medrol Injection:
V / m / in. Children: When adrenal insufficiency – 0.14 mg / kg or 4 mg / sqm per day in two days or 0.039-0.0585 mg / kg / day every day, according to other indications – 0.139-0.835 mg / kg or 4.16-25 mg / m every 12-24 hours for adults – 4-60 mg / day, a suspension (depot form) – 40-120 mg for 1-4 weeks. B / B in shock (anaphylactic, burn, cardiogenic, traumatic) and reaction of graft rejection: adults and children – 4-20 mg / kg dose can be increased to 30 mg / kg in a short period. When i / v infusion of high-dose infusion duration should be at least 10 minutes. The intervals between injections – from 30 minutes to 24 hours ‘pulse therapy’ in patients with autoimmune rheumatic diseases: the drug is diluted in 100-250 ml 0.9% NaCl or 5% dextrose and administered over 35-45 minutes every day – on 15-20 mg / kg / day or 1 g / sq.m. Course – 3 days. For relief of nausea and vomiting caused by cytotoxic drugs intake: 250 mg 20 minutes before and 250 mg at 6 h after administration of cytotoxic drugs, the children – not less than 25 mg / day. If needed – again every 6 h in the same dose. A suspension of the depot: / m – 40-120 mg for 1-4 weeks, intra – 4-80 mg depending on the severity of inflammation and joint: large joints (knee, ankle, shoulder) – 40-80 mg, mean ( elbow, wrist) – 10-40 mg, the small (metacarpal and metatarsal) – 4-10 mg, when administered in the bursa and tendon sheath – 4-60 mg, in the abdominal and chest cavity – up to 100 mg, epidural – 80 mg, when administered directly into the area of skin lesions – 20-60 mg, with retention enema for ulcerative colitis – 40-120 mg 3-7 times weekly by mixing with 100 ml 0.9% solution of NaCl (to enhance absorption in the sigmoid and descending colon) . In the event of spontaneous remission therapy is stopped. After taking several days to produce gradually lifting.
Cautions Depo-Medrol Injection:
At the time of treatment can not be vaccinated because of possible reduction in the immune response. With active tuberculosis can be used only in conjunction with appropriate antituberculous therapy. Ineffective in septic shock (possibly increasing mortality). During pregnancy or when the alleged pregnancy must be treated only by strict indications. Available clinical experience with SCS in the first trimester of pregnancy indicates that there is no risk to the fetus. During the injection of the newborn and especially premature baby should be used as a solvent, distilled water. Due to the weak effect of methylprednisolone ISS can not be used for replacement therapy in Addison’s disease. Extreme caution should be the introduction of corticosteroids in patients with severe hypertension and heart failure (requires monitoring of ECG and blood pressure). In patients with diabetes should monitor blood glucose and adjust therapy. Shows the X-ray monitoring system kostnosustavnoy (images spine, wrist). Pyuria can cause that may have diagnostic value for detection of latent leukocyturia for kidney and urinary tract. Increases the concentration of metabolites of 11 – and 17-oksiketokortikosteroidov. In rare cases – increased activity of “liver” enzymes and alkaline phosphatase. With stress during treatment with corticosteroids showed an increase in dose. Perhaps the development of the syndrome of “lifting” (usually for non-compliance chronopharmacology, as well as the original latent adrenal insufficiency). I / O to the introduction should not be deep. Depo-form does not introduce non-recommended methods (including I / O). The children in the period of growth GCS should be used only if absolutely indicated and under particularly close observation doctor.
Interaction Depo-Medrol Injection:
Methylprednisolone Pharmaceutical incompatible with other drugs (can form insoluble compounds). Methylprednisolone increases the toxicity of cardiac glycosides (due to an increased risk of hypokalemia arrhythmias). Accelerating the elimination of ASA reduces its concentration in the blood (with the abolition of methylprednisolone concentration of salicylates in the blood increases, and increases the risk of side effects). While the use of live vaccines and the background of other types of immunization increases the risk of activation of viruses and infections. Increases the metabolism of isoniazid, meksiletina (especially in “fast acetylators”), which leads to a decrease in their plasma concentrations. Increases the risk of hepatotoxic reactions of paracetamol (induction of “liver” enzymes and formation of toxic metabolite of paracetamol). Increases (with prolonged therapy) the concentration of folic acid. Hypokalemia caused by corticosteroids, may increase the severity and duration of muscle blockade against muscle relaxants. In high doses, reduces the effect of growth hormone. Antacids reduce the absorption of corticosteroids. Methylprednisolone reduces the effect of hypoglycemic drugs, strengthens the anticoagulant effect of coumarin derivatives. Weakens the influence of vitamin D on the absorption of Ca2 + in the lumen of the intestine. Ergocalciferol and parathyroid hormone inhibit the development of osteopathy caused by SCS. Reduces the concentration of praziquantel in blood. Cyclosporine (inhibits metabolism) and ketoconazole (reduced clearance) increased the toxicity. Thiazide diuretics, carbonic anhydrase inhibitors, corticosteroids, etc., and amphotericin B increase the risk of hypokalemia, Na +-containing drugs – swelling and increase blood pressure. NSAIDs and ethanol increases the risk of ulceration of the mucous membrane and gastrointestinal bleeding, in combination with NSAIDs to treat arthritis may reduce the dose of GCS due to summation of the therapeutic effect. Indomethacin, methylprednisolone, displacing from its association with albumin, increases the risk of its side effects. Amphotericin B and carbonic anhydrase inhibitors increase risk of osteoporosis. The therapeutic effect of corticosteroids reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of “liver” of microsomal enzymes (increased metabolic rate). Mitotane and other inhibitors of adrenocortical function may necessitate increasing the dose of GCS. Clearance of GCS increased against the background of thyroid hormones. Immunodepresanty increase the risk of infection and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus. Estrogens (including oral contraceptives, estrogen) reduce the clearance of corticosteroids, extend T1 / 2 and their therapeutic and toxic effects. The appearance of hirsutism and acne promotes the simultaneous use of other steroid hormone drugs – androgens, estrogens, anabolic steroids, oral contraceptives. Tricyclic antidepressants may increase the severity of depression caused by GCS (not shown for the treatment of these side effects.) Risk of cataracts increases with the use of the background of other corticosteroids, antipsychotic drugs (neuroleptics), karbutamida and azathioprine. Simultaneous with the appointment of Mr. holinoblokatorami (including antihistamine drugs, tricyclic antidepressants), nitrate promotes increased intraocular pressure.
