Prednisolon Nycomed (Tablets, Solution) Instructions for Use

ATC Code

H02AB06 (Prednisolone)

Active Substance

Prednisolone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Corticosteroids for oral administration

Pharmacotherapeutic Group

Glucocorticosteroid

Pharmacological Action

Glucocorticosteroid. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Impairs the ability of macrophages to phagocytose and to form interleukin-1. Promotes stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability caused by the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A₂, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also contributes to the reduction of prostaglandin production.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses antibody formation.

Prednisolone suppresses the release of ACTH and β-lipotropin by the pituitary gland but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it 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, Prednisolone enhances glycogen storage by stimulating the activity of glycogen synthase and the synthesis of glucose from protein metabolism products. The increase in blood glucose levels stimulates insulin secretion.

Prednisolone suppresses glucose uptake by fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which promotes fat accumulation.

Has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, and bone tissue. To a lesser extent than hydrocortisone, it affects water-electrolyte metabolism: promotes the excretion of potassium and calcium ions, and the retention of sodium ions and water in the body. Osteoporosis and Cushing’s syndrome are the main factors limiting long-term glucocorticosteroid therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, Prednisolone can increase the excitability of brain tissue and contribute to a lowering of the seizure threshold. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, leading to the development of peptic ulcer.

When used systemically, the therapeutic activity of prednisolone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

Compared to hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, and its mineralocorticoid activity is 0.6 times less.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. C_max in plasma is noted after 90 minutes. In plasma, most of the prednisolone is bound to transcortin (cortisol-binding globulin). Metabolized mainly in the liver.

T_1/2 is about 200 minutes. Excreted by the kidneys unchanged – 20%.

Indications

For oral and parenteral administration: rheumatism; rheumatoid arthritis, dermatomyositis, polyarteritis nodosa, scleroderma, ankylosing spondylitis, bronchial asthma, status asthmaticus, acute and chronic allergic diseases, anaphylactic shock, Addison’s disease, acute adrenocortical insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia; Sydenham’s chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, prurigo, seborrheic dermatitis, systemic lupus erythematosus, erythroderma, alopecia.

For intra-articular administration: chronic polyarthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.

For infiltrative administration into tissues: epicondylitis, tenosynovitis, bursitis, scapulohumeral periarthritis, keloids, sciatica, Dupuytren’s contracture, rheumatic and similar lesions of joints and various tissues.

ICD codes

Dosage Regimen

Tablets, Solution

When taken orally for replacement therapy in adults, the initial dose is 20-30 mg/day, the maintenance dose is 5-10 mg/day. If necessary, the initial dose can be 15-100 mg/day, the maintenance dose – 5-15 mg/day. The daily dose should be reduced gradually. For children, the initial dose is 1-2 mg/kg/day in 4-6 doses, the maintenance dose is 300-600 mcg/kg/day.

For intramuscular or intravenous administration, the dose, frequency and duration of use are determined individually.

For intra-articular administration into large joints, a dose of 25-50 mg is used, for medium-sized joints – 10-25 mg, for small joints – 5-10 mg. For infiltrative administration into tissues, depending on the severity of the disease and the size of the affected area, doses from 5 to 50 mg are used.

Adverse Reactions

From the endocrine system menstrual cycle disorders, suppression of adrenal function, Cushing’s syndrome, suppression of the pituitary-adrenal system function, decreased carbohydrate tolerance, steroid diabetes or manifestation of latent diabetes mellitus, growth retardation in children, delayed sexual development in children.

From the digestive system nausea, vomiting, steroid ulcer of the stomach and duodenum, pancreatitis, esophagitis, gastrointestinal bleeding and perforation, increased or decreased appetite, flatulence, hiccups. In rare cases – increased activity of liver transaminases and alkaline phosphatase.

From metabolism negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.

From the cardiovascular system potassium loss, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (development or worsening of symptoms), ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute myocardial infarction – spread of the necrosis focus, slowing of scar tissue formation, which can lead to rupture of the heart muscle.

From the musculoskeletal system slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological fractures, aseptic necrosis of the humeral and femoral head), muscle tendon rupture, muscle weakness, steroid myopathy, decrease in muscle mass (atrophy).

From the nervous system headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, convulsive seizures.

From the organ of vision posterior subcapsular cataract, increased intraocular pressure (with possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, tendency to develop secondary infections (bacterial, fungal, viral).

From the skin and subcutaneous tissue petechiae, ecchymoses, thinning and fragility of the skin, hyper- or hypopigmentation, acne, striae, tendency to develop pyoderma and candidiasis.

Reactions due to immunosuppressive action slowing of regeneration processes, reduced resistance to infections.

With parenteral administration in isolated cases anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of the skin and subcutaneous tissue, exacerbation after intrasynovial use, Charcot-like arthropathy, sterile abscesses, when injected into lesions on the head – blindness.

Contraindications

For short-term use for vital indications – hypersensitivity to prednisolone.

For intra-articular administration and administration directly into the lesion previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including in the anamnesis), as well as general infectious disease, pronounced periarticular osteoporosis, absence of signs of inflammation in the joint (“dry” joint, for example in osteoarthritis without synovitis), pronounced bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as a result of arthritis, aseptic necrosis of the bone epiphyses forming the joint.

Use in Pregnancy and Lactation

During pregnancy (especially in the first trimester), it is used only for vital indications. If it is necessary to use during lactation, the expected benefit of treatment for the mother and the risk for the child should be carefully weighed.

Use in Hepatic Impairment

Use with caution in severe chronic liver failure.

Use in Renal Impairment

Use with caution in severe chronic renal failure.

Pediatric Use

In children during the growth period, glucocorticosteroids should be used only for absolute indications and under the careful supervision of a physician.

Contraindication for external use: children’s age (under 2 years, for anal itching – under 12 years).

Geriatric Use

Use with caution in elderly patients to avoid the risk of exacerbation of chronic diseases.

Special Precautions

Use with caution in parasitic and infectious diseases of viral, fungal, or bacterial nature (current or recently experienced, including recent contact with a patient) – herpes simplex, herpes zoster (viremic phase), varicella, measles, amebiasis, strongyloidiasis (established or suspected), systemic mycosis; active and latent tuberculosis. Use in severe infectious diseases is permissible only against the background of specific therapy.

Use with caution within 8 weeks before and 2 weeks after vaccination, in lymphadenitis after BCG vaccination, in immunodeficiency states (including AIDS or HIV infection).

Use with caution in gastrointestinal diseases: gastric and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with threat of perforation or abscess formation, diverticulitis.

Use with caution in diseases of the cardiovascular system, including after recent myocardial infarction (in patients with acute and subacute myocardial infarction, spread of the necrosis focus, slowing of scar tissue formation and, as a result, rupture of the heart muscle are possible), in decompensated chronic heart failure, arterial hypertension, hyperlipidemia), in endocrine diseases – diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Cushing’s disease, in severe chronic renal and/or hepatic insufficiency, nephrourolithiasis, in hypoalbuminemia and conditions predisposing to its occurrence, in systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (grades III-IV), poliomyelitis (except for the form of bulbar encephalitis), open-angle and angle-closure glaucoma.

When intra-articular administration is necessary, use with caution in patients with a generally severe condition, in case of ineffectiveness (or short duration) of the action of 2 previous administrations (taking into account the individual properties of the glucocorticoids used).

During treatment (especially long-term), observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood picture, blood glucose is necessary; to reduce side effects, anabolic steroids, antibiotics can be prescribed, and potassium intake can be increased (diet, potassium supplements). It is recommended to clarify the need for ACTH administration after a course of prednisolone treatment (after a skin test!).

In Addison’s disease, simultaneous use with barbiturates should be avoided.

After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as exacerbation of the disease for which Prednisolone was prescribed may occur.

In intercurrent infections, septic conditions, and tuberculosis, simultaneous antibiotic therapy is necessary.

In children during the growth period, glucocorticoids should be used only for absolute indications and under the careful supervision of a physician.

Drug Interactions

When used concomitantly with salicylates, the likelihood of bleeding may increase.

When used concomitantly with diuretics, electrolyte metabolism disorders may worsen.

When used concomitantly with hypoglycemic drugs, the rate of decrease in blood glucose levels is reduced.

When used concomitantly with cardiac glycosides, the risk of glycoside intoxication increases.

When used concomitantly with rifampicin, the therapeutic effect of rifampicin may be weakened.

When used concomitantly with antihypertensive agents, their effectiveness may be reduced.

When used concomitantly with coumarin derivatives, the anticoagulant effect may be weakened.

When used concomitantly with rifampicin, phenytoin, barbiturates, the action of prednisolone may be weakened.

When used concomitantly with hormonal contraceptives – the action of prednisolone is enhanced.

When used concomitantly with acetylsalicylic acid, the content of salicylates in the blood may decrease.

When used concomitantly with praziquantel, its concentration in the blood may decrease.

The appearance of hirsutism and acne is facilitated by the simultaneous use of other glucocorticoids, androgens, estrogens, oral contraceptives, and steroid anabolic agents. The risk of cataract development increases when antipsychotic agents, carbutamide, and azathioprine are used against the background of glucocorticoids.

Concomitant administration with m-cholinoblockers (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.