Prednisolone Elfa for v/v.30 mg/ml 1 ml, 3 pcs.

Prednisolone is a synthetic glucocorticoid drug. It has anti-inflammatory, anti-allergic, immunosuppressive, antiexsudative and antipruritic effects. Immunosuppressive effect is associated with inhibition of cytokine release from lymphocytes and macrophages. Other effects are determined by stabilization of cell membranes, decrease of capillaries permeability, improvement of microcirculation.
Prednisolone has a catabolic effect, increases blood glucose levels, causes redistribution of adipose tissue. The drug inhibits synthesis and secretion of ACTH and, secondarily, of corticosteroids by adrenal glands.
When used topically and topically prednisolone therapeutic activity is due to anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect).

Indications

For oral and intravenous administration: Rheumatism; rheumatoid arthritis; dermatomyositis; periarteritis nodosa; scleroderma; Bechterew’s disease; bronchial asthma, asthmatic status; acute and chronic allergic diseases; Addison’s disease, acute adrenal cortex insufficiency, adrenogenital syndrome; Hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulematosis, thrombocytopenic purpura, hemolytic anemia; minor chorea; vesicles, eczema, itching, exfoliative dermatitis, psoriasis, scabies, seborrheic dermatitis, lupus erythroderma, alopecia.

For use in ophthalmology: allergic, chronic and atypical conjunctivitis and blepharitis; corneal inflammation with 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 long-term irritation of the eyeballs.

For intraarticular administration: chronic polyarthritis, posttraumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.

For infiltrative injection into the tissues: epicondylitis, tendovaginitis, bursitis, brachial-oval periarthritis, keloids, sciatica, Dupuytren’s contracture, rheumatic and similar lesions of the joints and various tissues.

Active ingredient

Composition

1 ml of the solution contains:

Active ingredient: prednisolone sodium phosphate (in recalculation on prednisolone) 30 mg;
Excipients: nicotinamide; sodium metabisulfite; disodium edetate; sodium hydroxide; water for injection.

How to take, the dosage

V/v (by trickle, then dropwise) or intramuscularly. The dose of Prednisolone and duration of treatment shall be determined by the physician individually, depending on the indication and severity of the disease.

In acute adrenal insufficiency a single dose of the drug is 100-200 mg and daily 300-400 mg.

In severe allergic reactions, Prednisolone is given in a daily dose of 100-200 mg for 3-16 days.

In bronchial asthma the drug is administered depending on the severity of the disease and the effectiveness of the complex treatment of 75 to 675 mg for a treatment course of 3 to 16 days; in severe cases the dose may be increased to 1400 mg per course of treatment or more with gradual reduction of the dose.

In asthmatic status, Prednisolone is given in a dose of 500-1200 mg per day with subsequent reduction to 300 mg per day and transition to maintenance doses.

In thyrotoxic crisis, 100 mg of the drug is administered in a daily dose of 200-300 mg; if necessary, the daily dose may be increased to 1000 mg. The duration of administration depends on the therapeutic effect, usually up to 6 days.

In case of shock resistant to standard therapy, Prednisolone is usually administered by trickle at the beginning of therapy, after which it is switched to drip administration. If BP does not increase within 10-20 minutes, the drug is repeated by trickle administration. After recovery from shock continue drip administration until BP stabilizes. The single dose is 50-150 mg (in severe cases up to 400 mg). The drug shall be repeatedly administered after 3-4 hours. The daily dose may be 300-1200 mg (with subsequent dose reduction).

In acute hepatic and renal failure (in acute poisoning, in postoperative and postpartum periods), Prednisolone is administered in 25-75 mg per day; if indicated, the daily dose may be increased to 300-1500 mg per day and higher.

In rheumatoid arthritis and systemic lupus erythematosus Prednisolone is administered in addition to systemic administration of the drug in a dose of 75-125 mg daily for not more than 7-10 days.

In acute hepatitis, Prednisolone is administered at 75-100 mg daily for 7-10 days.

In cauterizing fluid poisoning with burns of the digestive tract and upper respiratory tract, Prednisolone is prescribed in a dose of 75-400 mg daily for 3-18 days.

If IV administration is not possible, Prednisolone is administered in m/m in the same doses. After the acute condition is resolved, oral Prednisolone tablets are prescribed, with subsequent gradual reduction of the dose.

In long-term use of the drug, the daily dose should be reduced gradually. Long-term therapy should not be stopped suddenly!

Interaction

Heart glycosides: increased risk of cardiac rhythm disturbances and glycoside toxicity associated with hypokalemia.

Barbiturates, antiepileptic drugs (phenytoin, carbamazepine), rifampicin, glutethimide accelerate the metabolism of GCS (through induction of microsomal enzymes), weaken their effects.

The antihistamines weaken the effects of prednisolone.

Amphotericin B, carbohydrase inhibitors: hypokalemia, left ventricular myocardial hypertrophy, circulatory failure.

Paracetamol: hypernatremia, peripheral edema, increased calcium excretion, risk of hypocalcemia and osteoporosis. Increased risk of hepatotoxicity of paracetamol.

Anabolic steroids, androgens: increased risk of peripheral edema, acne; use with caution, especially in liver and heart disease.

Estrogen-containing oral contraceptives: increase serum glucocorticosteroid-binding globulin concentrations, slow down metabolism, increase T1/2, increase the effect of prednisolone.

Choline-blocking drugs (mainly atropine) – increase in intraocular pressure.

Anticoagulants (coumarin derivatives, indandion, heparin), streptokinase, urokinase:decreased, and in some patients increased effectiveness; dose should be determined based on SP; increased risk of ulceration and bleeding from the GI tract.

Tricyclic antidepressants may exacerbate psychiatric disorders associated with prednisolone administration. They should not be prescribed to treat these disorders.

The oral antidiabetic drugs, insulin: attenuation of hypoglycemic effect, increase in blood glucose concentration. Correction of the dose of antidiabetic drugs is possible.

Antithyroid drugs, thyroid hormones – changes in thyroid function (dose adjustment of these drugs or discontinuation of their use is possible).

Diuretics: weakening of the action of diuretics (potassium-saving), hypokalemia.

Laxatives: weakening of action, hypokalemia.

Ephedrine may accelerate the metabolism of GCS (correction of prednisolone dose is possible).

Immunosuppressive drugs: increased risk of infection, lymphoma and other lymphoproliferative diseases.

Isoniazid: decrease in plasma concentration of isoniazid, mainly in persons with rapid acetylation (possible change in dose).

Mexiletine: acceleration of metabolism of mexiletine and reduction of its concentration in blood serum.

Drugs that block neuromuscular conduction (depolarizing myorelaxants): hypocalcemia associated with the use of prednisolone may increase synaptic blockade, leading to increased duration of neuromuscular blockade.

NSAIDs, acetylsalicylic acid, alcohol: weakening of action, increased risk of peptic ulcer disease and bleeding from the gastrointestinal tract.

Drugs and food containing sodium: peripheral edema, arterial hypertension (it may be necessary to reduce sodium intake with food and medications with high sodium content; sometimes use of GCS requires additional sodium administration).

Vaccines containing live viruses: while using immunosuppressive doses of GCS, viral replication and viral disease may occur; decreased antibody production (concomitant use is not recommended).

Other vaccines: increased risk of neurological complications and decreased antibody production.

Folic acid: increased need for this drug.

Special Instructions

Prednisolone is contraindicated in patients with systemic fungal infections because of the risk of increased infection. The drug may in some cases be used in fungal infections treated with amphotericin B to reduce its side effects, but in these cases it may cause circulatory failure and left ventricular myocardial hypertrophy and severe hypokalemia. Taking the drug with food may reduce gastrointestinal side effects.

The effectiveness of antacid drugs in preventing ulcer formation, bleeding from the digestive tract or intestinal perforation has not been confirmed. With long-term treatment, it may be necessary to limit sodium and increase potassium, and to increase protein in the diet.

If steroid myopathy develops, if therapy with prednisolone cannot be reversed, replacement with another GCS may alleviate the symptoms.

The risk of osteoporosis with prolonged use of GCS may be reduced by taking calcium and vitamin D or by exercise if the patient’s condition allows.

If psychosis or depression occurs, the dose should be reduced if possible, or the drug should be stopped. Phenothiazines or lithium compounds may be used if necessary.

Acetylsalicylic acid or other NSAIDs can be prescribed to alleviate some of the symptoms of GCS withdrawal (without suppressing the hypothalamic-pituitary-adrenal system).

Contraindications

Gastric and duodenal ulcer, osteoporosis, Icenko-Cushing’s syndrome, susceptibility to thromboembolism, renal failure, severe arterial hypertension, systemic mycoses, viral infections, vaccination period, active tuberculosis, glaucoma, productive symptoms in mental disorders. Hypersensitivity to prednisolone.
Infiltration injection into foci of skin and tissue lesions – in chicken pox, specific infections, mycosis, in local reaction to vaccination.

Side effects

In short-term use of prednisolone, like other GCSs, side effects are rare. When using prednisolone for a long time, the following side effects may develop:

Water-electrolyte metabolism disorders: sodium and fluid retention in the body, hypokalemia, hypokalemic alkalosis.

Cardiovascular system disorders: increase in BP, circulatory failure.

Musculoskeletal system disorders: muscle weakness, steroid myopathy, loss of muscle mass, osteoporosis, spinal compression fracture, aseptic necrosis of femoral and humeral heads, pathological fractures of long bones.

Gastrointestinal organs: steroid ulcer with possible perforation and bleeding, pancreatitis, flatulence, ulcerative esophagitis, digestive disorders, nausea, increased appetite.

Skin disorders: atrophic streaks, acne, delayed wound healing, skin thinning, petechiae and bruises, erythema, increased sweating, allergic dermatitis, urticaria, angioedema.

Nervous system and sensory organs: Increased intracranial pressure with optic nipple congestion syndrome (pseudotumor of the brain – more common in children, usually after reducing the dose too quickly, symptoms are headache, worsened visual acuity or double vision); seizures, dizziness, headache, sleep disturbance, posterior subcapsular cataracts, increased intraocular pressure, glaucoma; exophthalmos.

Endocrine status: Secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations such as illness, trauma, surgery); Cushing’s syndrome; growth suppression in children; menstrual disorders; decreased carbohydrate tolerance; manifestation of latent diabetes and increased need for insulin or oral antidiabetic drugs in diabetic patients, hirsutism.

Metabolic side: negative nitrogen balance as a result of protein catabolism, hyperglycemia, glucosuria.

Mental disorders: symptoms mimicking schizophrenia, mania or delirium syndrome (most often appear during the first two weeks of treatment). Women and lupus erythematosus patients are most susceptible to mental disorders.

Others: anaphylactic and hypersensitivity reactions, obliterating endarteritis, weight gain, masking of symptoms of infectious diseases, fainting.

Overdose

The risk of overdose is increased with long-term use of prednisolone, especially in high doses.

Symptoms: increased BP, peripheral edema, increased adverse effects described above.

Treatment: The drug should be temporarily discontinued or the dose should be reduced.

Pregnancy use

The use of GCS by women of childbearing age and pregnant women is acceptable only when its potential benefit to the mother exceeds the potential risk to the fetus. Women of childbearing age should be warned about the potential risk to the fetus.

There are not enough controlled studies in humans. In animal studies, GCS caused an increased incidence of cleft palate, miscarriage, placental insufficiency, and fetal delay. Although teratogenic effects of GCS in humans have not been confirmed, there is evidence indicating an increased risk of placental insufficiency, hypotrophy at birth, and fetal death in women who have taken GCS during pregnancy. They can cause adrenal insufficiency in the fetus and the newborn.

Breastfeeding should be stopped during treatment. Prednisolone is excreted with breast milk and may cause undesirable effects in the baby, such as growth retardation or inhibition of endogenous adrenal hormone production.

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