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Active Ingredient: Prednisone

Prednisone is able to help during any severe disease. Its spectrum of action is broad that it covers almost all known diseases of autoimmune, allergic, and tumour origin. It is used all over the world and due to its strong action this medicine has already saved many lives.

Prednisone

Prednisone is a drug from the group of adrenal cortex hormones (glucocorticosteroids). It contains the substance prednisolone.

Prednisolone (lat. Prednisolonum) - a synthetic medium-strength glucocorticoid drug, white crystalline powder, so pl. 240–241 (with decomp.), [Al 5 ° = -f 102 (in dioxane) its acetate melts at 237–239 (with decomp.) And has [a] 25 "= -f-ib (in dioxane).

The synthesis and study of analogs and derivatives of cortisone has led to a number of interesting compounds that have been used in medicine. These include hydrocortisone (I), prednisone (II), prednisone (III) and others.

Pharmachologic Effect

Suppresses the function of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. It contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability due to histamine release. Suppresses the activity of fibroblasts and the formation of collagen.

Inhibits the activity of phospholipase A2, which leads to the suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins. Reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed to the lymphoid tissue; inhibits the formation of antibodies.

Prednisolone inhibits pituitary ACTH and β-lipotropin, but does not reduce the level of circulating β-endorphin. It inhibits the secretion of TSH and FSH. With direct application to the vessels has a vasoconstrictor effect. Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys and increases the activity of gluconeogenesis enzymes. In the liver, prednisone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose activates insulin secretion. Prednisolone inhibits glucose uptake by fat cells, which leads to activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.

It has a catabolic effect in the lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water and electrolyte metabolism: it promotes the excretion of potassium and calcium ions, and the delay in the body of sodium and water ions. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term therapy of SCS. As a result of the catabolic effect, growth can be suppressed in children. In high doses, prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.

With systemic use, the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects. When applied topically and locally, the therapeutic activity of prednisolone is due to the anti-inflammatory, antiallergic and anti-exudative (due to the vasoconstrictor effect) action. Compared with hydrocortisone, anti-inflammatory activity of prednisolone is 4 times more, mineralocorticoid activity is 0.6 times less.

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Pharmacokinetics

When ingestion is well absorbed from the gastrointestinal tract. The maximum plasma concentration is noted after 90 minutes. Metabolized mainly in the liver. T1 / 2 is about 200 minutes. Excreted by the kidneys in unchanged form - 20%. With intravenous administration, the maximum plasma concentration is noted after 30 minutes. In plasma, most (90%) of prednisolone is associated with transcortin (cortisol-binding globulin) and albumin. It is metabolized in the liver, kidneys, small intestine, bronchi. The oxidized forms form complexes with glucuronic and sulfuric acids. T1 / 2 - 2-3 hours. It is excreted by the kidneys - 20% unchanged.

Indications

  • For oral administration:rheumatism; rheumatoid arthritis; dermatomyositis; periarteritis nodosa; scleroderma; ankylosing spondylitis; bronchial asthma, asthmatic status; acute and chronic allergic diseases; Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, systemic lupus erythematosus, erythroderma, alopecia.
  • For intravenous and intramuscular administration:Shock (burn, traumatic, operative, toxic, cardiogenic) with the ineffectiveness of other therapies. Allergic reactions (acute, severe), blood transfusion shock, anaphylactic shock, anaphylactoid reactions. Brain edema (including on the background of a brain tumor or associated with surgery, radiation therapy or head trauma). Bronchial asthma (severe form), asthmatic status. Systemic diseases of the connective tissue (systemic lupus erythematosus, rheumatoid arthritis). Acute adrenal insufficiency. Thyrotoxic crisis. Acute hepatitis, hepatic coma. Poisoning with cauterizing liquids (reducing inflammation and preventing cicatricial contractions).
  • For use in ophthalmology:allergic, chronic and atypical conjunctivitis and blepharitis; corneal inflammation in the intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episclera; sympathetic inflammation of the eyeball; after injuries and operations with prolonged irritation of the eyeballs.
  • For intraarticular injection:chronic polyarthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.
  • For infiltration in the tissues:epicondylitis, tendovaginitis, bursitis, humeroscapular periarthritis, keloids, sciatica, Dupuytren contracture, rheumatic diseases of the joints and various tissues similar to them.

Side Effect

  • From the endocrine system
    Itsenko-Cushing syndrome, weight gain, decrease in growth rate. Hyperglycemia up to the development of steroid diabetes, depletion (up to atrophy) of the function of the adrenal cortex.
  • From the digestive system
    Increased acidity of gastric juice, ulcerogenic effect on the gastrointestinal tract. After the use of the drug in humans, the ability to digest dairy products especially disappears, with the exception of dairy products, which, on the contrary, will help to remove prednisone from the body.
  • Metabolism
    Increased excretion of potassium, sodium retention in the body with the formation of edema, a negative nitrogen balance.
  • Since the cardiovascular system
    Arterial hypertension. In patients receiving prednisone, like other corticosteroids, high doses may develop arterial hypertension. In itself, an increase in blood pressure is not a reason for the abolition of prednisone in the presence of appropriate indications.
  • From the blood coagulation system
    Increased blood clotting.
  • From the musculoskeletal system
    Osteoporosis, aseptic bone necrosis.
  • On the part of the organ of vision
    On the part of the organ of vision
  • From the central nervous system
    Mental disorders.
  • Effects due to immunosuppressive effects
    Decreased resistance to infections, delayed wound healing.
  • For external use
    The appearance of steroid acne, purpura, telangiectasia, as well as burning, itching, irritation, dry skin; with prolonged use and / or when applied to large surfaces of the skin may develop resorptive action. When applied topically: slight burning sensation. After the external use of prednisolone in a person, all side effects of the drug appear as after internal use and for detoxification the same methods are used as after applying prednisolone inside.

Contraindications

Peptic ulcer and duodenal ulcer, osteoporosis, Itsenko – Cushing’s syndrome, propensity for thromboembolism, renal failure, severe arterial hypertension, systemic mycoses, viral infections, parasitic diseases, vaccination period, active tuberculosis, glaucoma, thrombomas, glauma therapy, thrombomash mental illness. Hypersensitivity to prednisone. Infiltration in the lesions of the skin and tissues - with chickenpox, specific infections, mycoses, with a local reaction to vaccination.

In ophthalmology - viral and bacterial diseases of the eye, primary glaucoma, corneal disease with damage to the epithelium.

In dermatology - bacterial, viral, fungal skin lesions, tuberculosis, syphilis, skin tumors.

One of the contraindications to prednisone is arachidonic acid metabolism, which is clinically manifested by an asthmatic triad, possibly developing mucosal edema due to increased vascular permeability due to leukotrienes and is not associated with an IgE-mediated allergic reaction. Often the clinic of metabolic disorders of arachidonic acid is difficult to differentiate from allergic asthma, angioedema. In addition to prednisone, other corticosteroids can be prescribed in such cases.

Pregnancy and Lactation

When pregnancy (especially in the first trimester) is used only for health reasons. If necessary, use during lactation should carefully weigh the expected benefits of treatment for the mother and the risk to the child.

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Special Instructions

During the day, it is recommended to apply, taking into account the circadian rhythm of endogenous GCS secretion in the range from 6 to 8 am. With caution used in patients with an indication of psychosis in history - high doses prescribed under the strict supervision of a physician; non-specific infections subject to simultaneous chemotherapy or antibiotic therapy. In diabetes, use is possible only with absolute indications or to prevent perceived insulin resistance. With latent forms of tuberculosis, prednisone can only be used in combination with anti-tuberculosis drugs.

During treatment (especially long-term), it is necessary to observe an oculist, monitor blood pressure and water-electrolyte balance, as well as a picture of peripheral blood, blood glucose; In order to reduce side effects, you can assign anabolic steroids, antibiotics, as well as increase potassium intake (diet, potassium supplements). It is recommended to clarify the need for the introduction of ACTH after a course of treatment with prednisone (after a skin test).

In Addison's disease, concurrent use with barbiturates should be avoided. After discontinuation of treatment, the onset of withdrawal syndrome, adrenal insufficiency, as well as exacerbation of the disease, for which prednisone was prescribed, may occur. Outwardly should not be used for more than 14 days. In case of use in case of common or pink acne, the exacerbation of the disease is possible.

When used as eye drops, during treatment it is necessary to control the intraocular pressure and the state of the cornea.

In children during the growth period, GCS should be used only if absolutely indicated and under the most careful supervision of the attending physician.

Drug Interactions

  • With the simultaneous use of prednisolone with anticoagulants, it is possible to enhance the anticoagulant action of the latter.
  • When applied simultaneously with salicylates increases the likelihood of bleeding.
  • With simultaneous use with diuretics may aggravate electrolyte disturbances.
  • With simultaneous use with hypoglycemic drugs decreases the rate of decrease in blood glucose levels.
  • With simultaneous use with cardiac glycosides increases the risk of glycosidic intoxication.
  • With simultaneous use of rifampicin, the therapeutic effect of rifampicin may be reduced.
  • With the simultaneous use of antihypertensive drugs may reduce their effectiveness.
  • With the simultaneous use of coumarin derivatives may weaken the anticoagulant effect.
  • With the simultaneous use of rifampicin, phenytoin, barbiturates may weaken the effect of prednisolone.
  • With the simultaneous use of hormonal contraceptives - enhancing the action of prednisone.
  • With simultaneous use of acetylsalicylic acid - a decrease in the content of salicylates in the blood.
  • With the simultaneous use of praziquantel may decrease its concentration in the blood.
  • The emergence of hirsutism and acne contributes to the simultaneous use of other corticosteroids, androgens, estrogens, oral contraceptives and steroid anabolic steroids. The risk of developing cataracts is increased when antipsychotics, carbutamide and azathioprine are used against the background of GCS.
  • The simultaneous appointment with m-holinoblokatorami (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.
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