Methods
A multicenter, randomized, double-blind, placebo-controlled study was performed. Patients were recruited from 10 specialized headache centers in Germany.
The study included patients aged 18-55 years with episodic cluster headache. Patients received 100 mg of prednisolone for 5 days, followed by a gradual dose reduction of 20 mg every 3 days. In the control group, patients received placebo for 17 days.
All patients were prescribed oral verapamil as long-term prophylaxis. Dose titration was carried out in parallel with prednisolone therapy.
As a primary endpoint
The average number of headache attacks during the first week of therapy was examined.
Solution for injection Prednisolone (Prednisolon)
Instructions for medical use of the drug
Description of pharmacological action
Synthetic GCS. Has a pronounced anti-inflammatory effect. It is believed that the anti-inflammatory effect of 5 mg of prednisolone is equivalent to the effect of 4 mg of methylprednisolone or triamcinolone, 0.75 mg of dexamethasone, 0.6 mg of betamethasone and 20 mg of hydrocortisone. The mineralocorticoid activity of prednisolone is about 60% of hydrocortisone. The drug inhibits the development of inflammation symptoms. Inhibits the accumulation of macrophages, leukocytes and other cells in the area of inflammation. Inhibits phagocytosis, the release of microsomal enzymes, as well as the synthesis and release of inflammatory mediators. Causes a decrease in capillary permeability and inhibition of leukocyte migration. Enhances the synthesis of lipomodulin, an inhibitor of phospholipase A2, which releases arachidonic acid from phospholipid membranes while simultaneously inhibiting its synthesis.
Indications for use
Endocrinological diseases: - adrenal cortex insufficiency: primary (Addison's disease) and secondary; — adrenogenital syndrome (congenital adrenal hyperplasia); - acute insufficiency of the adrenal cortex; — before surgical interventions and in case of severe illnesses and injuries in patients with adrenal insufficiency; - subacute thyroiditis. Severe allergic diseases resistant to other therapy: - contact dermatitis; - atopic dermatitis; - serum sickness; — hypersensitivity reactions to drugs; - permanent or seasonal allergic rhinitis; - anaphylactic reactions; - angioedema. Rheumatic diseases: - rheumatoid arthritis, juvenile rheumatoid arthritis (in cases resistant to other treatment methods); - psoriatic arthritis; - ankylosing spondylitis; - acute gouty arthritis; - acute rheumatic fever; — myocarditis (including rheumatic); - dermatomyositis; - systemic lupus erythematosus; — granulomatous giant cell mesoarteritis; - systemic scleroderma; - periarteritis nodosa; - relapsing polychondritis; - polymyalgia rheumatica (Horton's disease); - systemic vasculitis. Dermatological diseases: - exfoliative dermatitis; — bullous dermatitis herpetiformis; - severe seborrheic dermatitis; - severe erythema multiforme (Stevens-Johnson syndrome); — mycosis fungoides; - pemphigus; - severe psoriasis; - pemphigoid. Hematological diseases: - acquired autoimmune hemolytic anemia; — congenital aplastic anemia; - idiopathic thrombocytopenic purpura (Werlhof's disease) in adults; - hemolysis. Liver diseases: - alcoholic hepatitis with encephalopathy; - chronic active hepatitis. Hypercalcemia in malignancy or sarcoidosis. Inflammatory diseases of the joints: - acute and subacute bursitis; - epicondylitis; — acute tendovaginitis; - post-traumatic osteoarthritis. Oncological diseases: - acute and chronic leukemia; - lymphoma; - mammary cancer; - prostate cancer; - multiple myeloma. Neurological diseases: - tuberculous meningitis with subarachnoid block; — multiple sclerosis in the acute phase; - myasthenia. Eye diseases (severe acute and chronic allergic and inflammatory processes): - severe sluggish anterior and posterior uveitis; - optic neuritis; - sympathetic ophthalmia. Pericarditis. Respiratory diseases: - bronchial asthma; - berylliosis; - Loeffler's syndrome; - symptomatic sarcoidosis; - fulminant or disseminated pulmonary tuberculosis (in combination with anti-tuberculosis chemotherapy); - chronic pulmonary emphysema (resistant to treatment with aminophylline and beta-agonists). During organ and tissue transplantation to prevent and treat graft rejection (in combination with other immunosuppressive drugs).
Release form
Solution for intravenous and intramuscular administration 30 mg/ml; dark glass ampoule 1 ml contour plastic packaging (pallets) 5 cardboard pack 1; Solution for intravenous and intramuscular administration 30 mg/ml; dark glass ampoule 1 ml contour plastic packaging (pallets) 3 cardboard packs 1; Solution for intravenous and intramuscular administration 30 mg/ml; dark glass ampoule 1 ml cardboard pack 3;
Pharmacodynamics
The mechanism of the immunosuppressive effect of prednisolone is not fully understood. The drug reduces the number of T-lymphocytes, monocytes and acidophilic granulocytes, as well as the binding of immunoglobulins to receptors on the surface of cells, inhibits the synthesis or release of interleukins by reducing the blastogenesis of T-lymphocytes; reduces the early immunological response. It also inhibits the penetration of immunological complexes through membranes and reduces the concentration of complement components and immunoglobulins. Prednisolone acts on the distal part of the renal tubules, increasing the reabsorption of sodium and water, as well as increasing the excretion of potassium and hydrogen ions. Prednisolone inhibits the secretion of ACTH by the pituitary gland, which leads to a decrease in the production of corticosteroids and androgens by the adrenal cortex. After long-term use of the drug in high doses, adrenal function can be restored within a year, and in some cases, persistent suppression of their function develops. Prednisolone enhances protein catabolism and induces enzymes involved in amino acid metabolism. Inhibits the synthesis and enhances the catabolism of proteins in lymphatic, connective, and muscle tissue. With prolonged use, atrophy of these tissues (as well as the skin) may develop. Increases blood glucose concentrations by inducing gluconeogenesis enzymes in the liver, stimulating protein catabolism (which increases the amount of amino acids for gluconeogenesis) and reducing glucose consumption in peripheral tissues. This leads to the accumulation of glycogen in the liver, increasing blood glucose concentrations and increasing insulin resistance. With prolonged use of the drug, redistribution of adipose tissue is possible. Inhibits the formation of bone tissue and enhances its resorption, reducing the concentration of calcium in the blood serum, which leads to secondary hyperfunction of the parathyroid glands and simultaneous stimulation of osteoclasts and inhibition of osteoblasts. These effects, together with a secondary reduction in the amount of protein components as a result of protein catabolism, can lead to suppression of bone growth in children and adolescents and to the development of osteoporosis in children of all ages. Enhances the effect of endo- and exogenous catecholamines.
Use during pregnancy
With extreme caution, especially in the first trimester of pregnancy; When breastfeeding, caution should be exercised if the baby has hyperbilirubinemia.
Contraindications for use
Peptic ulcer of the stomach and duodenum, Cushing's syndrome, osteoporosis, predisposition to thromboembolism, renal failure, severe arterial hypertension, chickenpox, herpes simplex and herpes zoster, vaccination period.
Side effects
With short-term use of prednisolone (as well as other corticosteroids), side effects are rarely observed. When using prednisolone for a long time, the following side effects may develop. From the side of the central nervous system and peripheral nervous system: increased intracranial pressure with optic nerve congestion syndrome (occurs most often in children, after too rapid dose reduction, symptoms - headache, deterioration of visual acuity, double vision); convulsions, dizziness, headache, sleep disturbances. From the endocrine status: secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations: illness, injury, surgery); Cushing's syndrome, growth suppression in children, menstrual irregularities, hyperglycemia, glycosuria, decreased tolerance to carbohydrates, manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus, hirsutism. From the organ of vision: posterior subcapsular cataract, increased intraocular pressure, glaucoma, exophthalmos. From the mental sphere: most often appear during the first 2 weeks of therapy, symptoms can imitate schizophrenia, mania, delirium; Women and patients with systemic lupus erythematosus are most susceptible to developing mental disorders. Metabolism: negative nitrogen balance (as a result of protein catabolism). From laboratory parameters: an increase in the number of leukocytes (20,000/μl), a decrease in the number of lymphocytes and monocytes, an increase or decrease in the number of platelets, an increase in the concentration of calcium in the blood and urine, an increase in the level of total cholesterol, LDL, triglycerides in the blood serum, an increase in the concentration 17-hydroxycorticosteroids and 17-ketosteroids in the urine, decreased uptake of labeled technetium into bone tissue and brain tumor tissue, decreased uptake of labeled iodine into the thyroid gland; weakening of the reaction in skin allergy tests and tuberculin test. Other: anaphylactic reactions, hypersensitivity reactions; obliterating arteritis, weight gain, fainting.
Directions for use and doses
IV (usually first in a stream, then drip), if IV administration is not possible, administer IM in the same doses. For shock, a single dose of 0.05–0.15 g (in severe cases, up to 0.4 g), again after 3–4 hours, a daily dose of 0.3–1.2 g. For acute adrenal insufficiency, a single dose of 0. 1–0.2 g, daily 0.3–0.4 g. For status asthmaticus, administer 0.5–1.2 g/day, followed by a dose reduction to 0.3–0.15–0.1 g/ days For severe allergic reactions, administer at a dose of 0.1–0.2 g/day.
Overdose
The risk of overdose increases with long-term use of prednisolone, especially in high doses. Symptoms: increased blood pressure, peripheral edema; In addition, increased side effects are possible. Treatment: temporarily stop taking the drug or reduce the dose.
Interactions with other drugs
When used together with cardiac glycosides, the risk of developing cardiac arrhythmias and glycoside toxicity associated with hypokalemia increases. Barbiturates, anticonvulsants (phenytoin, carbamazepine), rifampicin, glutethimide accelerate the metabolism of GCS (by inducing microsomal enzymes) and weaken their effect. When used together, histamine H1 receptor blockers weaken the effect of prednisolone. When prednisolone is used together with amphotericin B, carbonic anhydrase inhibitors, hypokalemia, left ventricular myocardial hypertrophy, and circulatory failure may develop. When used together with paracetamol, it is possible to develop hypernatremia, peripheral edema, increase calcium excretion, and increase the risk of hypocalcemia and osteoporosis, as well as hepatotoxic reactions associated with paracetamol. When used together with anabolic steroids and androgens, the risk of developing peripheral edema and acne increases (this combination requires caution, especially in the case of concomitant heart and liver diseases). When used simultaneously with oral contraceptives containing estrogens, it is possible to increase the concentration of steroid-binding globulins in the blood serum, slow down metabolism, increase T1/2 and enhance the effect of prednisolone. When used together with anticholinergics (atropine), intraocular pressure may increase. When used together with anticoagulants (coumarin derivatives, indadione, heparin), streptokinase, urokinase, a decrease (in some patients - an increase) of effectiveness is possible, and the formation of ulcers and bleeding from the gastrointestinal tract is possible; the dose should be determined based on prothrombin time. When used together with tricyclic antidepressants, it is possible to increase mental disorders associated with taking prednisolone (the use of tricyclic antidepressants for the correction of mental disorders while taking corticosteroids is not recommended). When used together with prednisolone, the hypoglycemic effect of insulin and oral hypoglycemic agents may be weakened, and glucose levels may increase (which may require dose adjustment of antidiabetic drugs). When used together with prednisolone, dose adjustment or discontinuation of antithyroid drugs or thyroid hormones may be required, because changes in thyroid function indicators are possible. When used together with prednisolone, the effect of potassium-sparing diuretics and hypokalemia may be weakened. When used together with prednisolone, the effect of laxatives and the development of hypokalemia may be weakened. When used together, ephedrine may accelerate the metabolism of corticosteroids (prednisolone dose adjustment may be required). When prednisolone is used together with other immunosuppressive drugs, the likelihood of developing infections, lymphomas and other lymphoproliferative diseases increases. When used simultaneously with prednisolone, a decrease in the concentration of isoniazid in the blood plasma is possible (mainly in individuals with rapid acetylation); a dose adjustment of prednisolone may be required. When used simultaneously with prednisolone, an accelerated metabolism of mexiletine and a decrease in its concentration in plasma are observed. When used together with depolarizing muscle relaxants, it should be noted that hypocalcemia associated with the use of prednisolone may enhance synaptic blockade, leading to an increase in the duration of neuromuscular blockade. Acetylsalicylic acid and other NSAIDs, ethanol weaken the effect of prednisolone, increase the risk of developing peptic ulcers and bleeding from the gastrointestinal tract. Drugs and foods containing sodium, when used simultaneously with prednisone, increase the likelihood of developing arterial hypertension and peripheral edema. The use of corticosteroids increases the need for folic acid.
Precautions for use
Glucocorticoids should be prescribed in the smallest dosages and for the minimum duration necessary to achieve the desired therapeutic effect. When prescribing, the daily circadian rhythm of endogenous secretion of glucocorticoids should be taken into account: at 6–8 a.m., most (or all) of the dose is prescribed. In the event of stressful situations, patients on corticosteroid therapy are advised to administer parenteral corticosteroids before, during and after the stressful situation. If there is a history of psychosis, high doses are prescribed under the strict supervision of a physician. During treatment, especially with long-term use, the dynamics of growth and development in children should be carefully monitored; observation by an ophthalmologist, monitoring of blood pressure, water and electrolyte balance, blood glucose levels, and regular analyzes of the cellular composition of peripheral blood are necessary. Sudden cessation of treatment may cause the development of acute adrenal insufficiency; with long-term use, the drug should not be suddenly discontinued; the dose should be reduced gradually. With sudden withdrawal after long-term use, withdrawal syndrome may develop, manifested by increased body temperature, myalgia and arthralgia, and malaise. These symptoms can appear even in cases where there is no adrenal insufficiency.
Special instructions for use
Prednisolone is contraindicated in patients with systemic fungal infections due to the risk of worsening the infection. The drug is in some cases used in the treatment of fungal infections with amphotericin B to reduce the side effects of the antifungal drug, but this combination can lead to the development of circulatory failure and left ventricular myocardial hypertrophy, as well as severe hypokalemia. In case of stressful situations, patients receiving Prednisolone are recommended to administer parenteral corticosteroids. Sudden withdrawal of GCS can cause the development of acute adrenal insufficiency, so the dose of Prednisolone should be reduced gradually. Prednisolone can mask the symptoms of infection, reduce the body's resistance to infections, and also reduce the body's ability to localize the infectious process. With the use of the drug, clinical manifestations of latent amoebiasis are possible. In persons arriving from tropical countries or in patients with dysentery of unknown etiology, dysenteric amoebiasis should be excluded before using Prednisolone. Long-term use of Prednisolone increases the risk of developing secondary fungal or viral infections. Long-term use of corticosteroids may lead to the development of cataracts and glaucoma (including damage to the optic nerve). When using Prednisolone in high doses, you should monitor blood pressure (possible development of arterial hypertension), body weight of patients (possible occurrence of peripheral edema). Serum electrolyte concentrations should be monitored periodically. In some cases, you may need to limit your sodium intake and increase your potassium intake. Prednisolone also causes an increase in calcium excretion. Patients receiving GCS should not be vaccinated with live viral vaccines (due to possible viral replication and development of viral diseases), and there may be a decrease in antibody production. Administration of an inactivated viral or bacterial vaccine may not produce the expected increase in antibodies. It is possible to vaccinate patients who receive corticosteroids as replacement therapy, for example, for Addison's disease. In addition, patients taking GCS have an increased risk of developing neurological complications. Prescribing GCS to patients with an active form of tuberculosis is possible only in cases of disseminated or fulminant tuberculosis and only in combination with anti-tuberculosis therapy. Patients with latent tuberculosis or a positive tuberculin test taking Prednisolone should be monitored due to the high risk of activation of the tuberculosis process. With long-term use of GCS, this category of patients should receive chemoprophylaxis. The use of the drug may mask the symptoms of infectious diseases. With sudden withdrawal of Prednisolone (especially after long-term use), withdrawal syndrome may develop (manifested by anorexia, fever, myalgia and arthralgia, general weakness). Symptoms can occur even in cases where there is no adrenal insufficiency. In patients with hypothyroidism or liver cirrhosis, the effect of Prednisolone is enhanced. When using Prednisolone, the development of mental disorders (euphoria, insomnia, sudden mood changes, personality changes, severe depression, symptoms of psychosis) is possible. Pre-existing emotional instability or psychotic tendencies may increase during GCS therapy. When using GCS in patients with hypoprothrombinemia, acetylsalicylic acid should be prescribed with caution. The drug is prescribed with caution for nonspecific ulcerative colitis due to the risk of developing intestinal perforation, abscess or other purulent infections; with intestinal diverticulosis, fresh intestinal anastomoses, erosive and ulcerative lesions of the gastrointestinal tract, with renal failure, arterial hypertension, osteoporosis, myasthenia gravis, diabetes mellitus, liver dysfunction, glaucoma, viral infections, hyperlipidemia, hypoalbuminemia. With the development of gastrointestinal perforation during the use of corticosteroids, the symptoms of peritonitis may be slightly expressed or absent altogether. In some patients, during GCS therapy, the number and motility of sperm changes. Taking the drug with food may reduce the likelihood of developing gastrointestinal side effects. The effectiveness of antacid medications in preventing the formation of ulcers, gastrointestinal bleeding, or intestinal perforation has not been confirmed. With the development of steroid myopathy and the impossibility of discontinuing GCS therapy, replacing prednisolone with another GCS can alleviate the symptoms. The risk of developing osteoporosis associated with long-term use of corticosteroids can be reduced by taking vitamin D and calcium supplements or, if the patient's condition allows, by performing appropriate physical exercise. If psychosis or depression occurs, reduce the dose or stop taking the drug if possible. If necessary, phenothiazine or lithium preparations can be used. The use of tricyclic antidepressants is contraindicated. In order to mitigate some of the symptoms of withdrawal syndrome, it is possible to prescribe acetylsalicylic acid or other NSAIDs. Use in pediatrics When prescribing the drug to children, monitoring of their growth and development is necessary.
Storage conditions
List B.: In a dark place, at a temperature of 15–30 °C.
Best before date
60 months
ATX classification:
H Hormones for systemic use (excluding sex hormones)
H02 Corticosteroids for systemic use
H02A Corticosteroids for systemic use
H02AB Glucocorticoids
H02AB06 Prednisolone
results
- The study included 116 patients, 57 patients were included in the prednisone group and 59 patients were included in the placebo group.
- Patients in the prednisone group had an average of 7.1 headache attacks during the first week, compared with 9.5 attacks in the control group (difference, 2.4 attacks, 95% CI -4.8 to 0.03; p= 0.002).
- During the study period, two serious adverse events occurred in the placebo group, including an inguinal hernia and a significant worsening of cluster headaches.
- During the study period, 270 adverse events were reported: 71% of patients in the prednisone group and 71% of patients in the control group reported adverse events. The most common side effects were nausea, dizziness and headache.
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